MedWorm.com provides a medical RSS filtering service. Over 6000 RSS medical sources are combined and output via different filters. This feed contains the latest items from the 'Chemical and Pharmaceutical Bulletin' source. Wed, 08 Feb 2012 14:04:04 +0100 http://www.medworm.com/index.php?rid=5663343&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22293474%26dopt%3DAbstract Authors: Gouda H, Kobayashi Y, Yamada T, Ideguchi T, Sugawara A, Hirose T, Omura S, Sunazuka T, Hirono S Abstract The three-dimensional (3D) structure of bottromycin A(2), a natural anti-methicillin-resistant Staphylococcus aureus (MRSA) and anti-vancomycin-resistant Enterococci (VRE) agent consisting of seven amino acids, has been investigated through NMR spectroscopy. On the basis of 57 experimental constraints, a total of 34 converged structures were obtained. The average pairwise atomic root mean square difference is 0.74±0.59 Å for all heavy atoms. The resulting structure indicates an interesting feature in that the three C-terminal residues of bottromycin A(2) fold back on the 12-membered cyclic skeleton made by the four N-terminal residues. Thus, MePro(2) and Thia-β-Ala-O... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5663343 Mon, 06 Feb 2012 14:06:02 +0100 5663343 http://www.medworm.com/index.php?rid=5663342&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22293475%26dopt%3DAbstract Authors: Tavakoli N, Varshosaz J, Dorkoosh F, Motaghi S, Tamaddon L Abstract Acyclovir (ACV), a model drug for this study, is one of the most effective drugs against viruses of the herpes group. Absorption of orally administered ACV is variable and incomplete, with a bioavailability of ca. 15-30%. The drug is absorbed in the duodenum after oral administration and hence, preparation of a floating drug delivery system (FDDS) for ACV may increase oral absorption of the drug. ACV matrix tablets (200 mg) containing an effervescent base (sodium bicarbonate and citric acid) and a binary combination of hydroxypropyl methylcellulose (HPMC) K4M with carbopol or sodium carboxymethyl cellulose (Na CMC) or polyvinylpyrrolidone (PVP) and/or sodium alginate were prepared by the direct compressi... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5663342 Mon, 06 Feb 2012 14:06:02 +0100 5663342 http://www.medworm.com/index.php?rid=5663341&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22293476%26dopt%3DAbstract This study characterized the acaricidal activity of constituents of patchouli oil extracted from (Pogostemon cablin (Blanco) BENTH) against the house dust mite, Dermatophagoides farinae. A new compound, 2-(1,3-dihydroxy-but-2-enylidene)-6-methyl-3-oxo-heptanoic acid (DHEMH), was isolated from patchouli oil and characterized by (1)H-NMR, (13)C-NMR, LC-MS and elemental analysis (EA). This active component was identified as the hydrolysate of pogostone. Fifteen other constituents found in patchouli oil were also identified by GC-MS, including patchouli alcohol and pogostone. LD(50) studies carried out over 24 h using contact toxicity tests identified DHEMH as the most toxic compound to D. farinae (2.04 μg/cm(2)), followed by patchouli oil (6.11 μg/cm(2)), benzyl benzoate (BP) (9.31 ... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5663341 Mon, 06 Feb 2012 14:06:02 +0100 5663341 http://www.medworm.com/index.php?rid=5663340&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22293477%26dopt%3DAbstract In this study, we have constructed a prediction scheme with target-specific scores for estimating ligand-binding affinities to human estrogen receptor α (ERα), considering the major conformational change between agonist- and antagonist-bound forms and the change in protonation states of histidine at the ligand-binding site. The generated scheme calibrated with fewer training compounds (23 for the agonist-bound form, 17 for the antagonist-bound form) demonstrated good predictive power (a predictive r(2) of 0.83 for 154 validation compounds); this was also true for compounds with frameworks that were quite different from those of the training compounds. Our prediction scheme will be useful in drug development targeting ERα and in primary screening of endocrine disruptors, and provides a s... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5663340 Mon, 06 Feb 2012 14:06:02 +0100 5663340 http://www.medworm.com/index.php?rid=5663339&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22293478%26dopt%3DAbstract Authors: Luo J, Li Y, Wang JS, Lu J, Wang XB, Luo JG, Kong LY Abstract A series of novel and structurally related C-15-acyl 16-norphragmalin-type limonoids, chuktabrins C-J (1-8) and chuktabularins U-X (9-12), were isolated from the stem bark of Chukrasia tabularis var. velutina. Their structures were established on the basis of detailed spectroscopic analysis, and the absolute configuration of compound 1 was determined by a single-crystal X-ray study using a mirror CuKα radiation. Compounds 7 and 8 were unprecedent C-15-acyl 16-norphragmalins with ketonic alkyl appendage at C-15, and compounds 4 and 8 were first examples of limonoid with a characteristic carbonate moiety esterified at OH-9/OH-8 or OH-1/OH-8 respectively. A biosynthetic pathway of these limonoids was reasonably pr... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5663339 Mon, 06 Feb 2012 14:06:02 +0100 5663339 http://www.medworm.com/index.php?rid=5663338&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22293479%26dopt%3DAbstract Authors: Warashina T, Umehara K, Miyase T Abstract A MeOH extract from the roots of Taraxacum platycarpum has shown significant effects on the proliferation of normal human skin fibroblasts. Chemical analysis of the extract resulted in the isolation of 26 compounds, including eight new triterpenes, one new sesquiterpene glycoside, and seventeen known compounds. The structure of each new compound was established using NMR spectroscopy. Some triterpenes had a significant effect on the proliferation of normal human skin fibroblasts. PMID: 22293479 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5663338 Mon, 06 Feb 2012 14:06:02 +0100 5663338 http://www.medworm.com/index.php?rid=5663335&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22293480%26dopt%3DAbstract Authors: He F, Nugroho AE, Wong CP, Hirasawa Y, Shirota O, Morita H, Aisa HA Abstract Eight new guaipyridine sesquiterpene alkaloids, rupestines F-M (1-8) were isolated from the leaves of Artemisia rupestris and their structures were elucidated on the basis of 2D-NMR data. The absolute configurations of 1-8 have been assigned by comparison of their experimental and calculated circular dichroism (CD) spectra. PMID: 22293480 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5663335 Mon, 06 Feb 2012 14:06:02 +0100 5663335 http://www.medworm.com/index.php?rid=5663333&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22293481%26dopt%3DAbstract Authors: Deguchi J, Hirahara T, Hirasawa Y, Ekasari W, Widyawaruyanti A, Shirota O, Shiro M, Morita H Abstract Four new alkaloids, cassiarins G, H, J, and K (1-4) which showed moderate antiplasmodial activity against Plasmodium falciparum 3D7, were isolated from the leaves of Cassia siamea (Leguminosae) and the structures of 1-4 were elucidated by 1D- and 2D-NMR analysis and X-ray crystallographic analysis. PMID: 22293481 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5663333 Mon, 06 Feb 2012 14:06:02 +0100 5663333 http://www.medworm.com/index.php?rid=5663332&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22293482%26dopt%3DAbstract Authors: Watanuki S, Matsuura K, Tomura Y, Okada M, Okazaki T, Ohta M, Tsukamoto S Abstract We synthesized and evaluated the inhibitory activity of a series of 2-(1-alkylpiperidin-4-yl)-N-[(1R)-1-(4-fluorophenyl)-2-methylpropyl]acetamide derivatives against T-type Ca(2+) channels. Structure-activity relationship studies revealed that the position of the amide structure was important for the potent inhibitory activity toward T-type Ca(2+) channels. In addition, the introduction of an appropriate substituent on the pendant benzene ring played a crucial role for the selectivity towards T-type Ca(2+) channels over L-type Ca(2+) channels and the potent bradycardic activity of these derivatives. Oral administration of N-[(1R)-1-(4-fluorophenyl)-2-methylpropyl]-2-(1-{2-[2-(2-methoxyethoxy... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5663332 Mon, 06 Feb 2012 14:06:02 +0100 5663332 http://www.medworm.com/index.php?rid=5663331&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22293483%26dopt%3DAbstract Authors: Kim J, Kino T, Kato H, Yamamoto F, Sano K, Mukai T, Maeda M Abstract As a part of our efforts to develop potential imaging agents for ascorbate bioactivity, 5-O-(4-[(125)I]iodobenzyl)-L-ascorbic acid ([(125)I]1) was prepared through a two-step sequence which involved radioiodo-destannylation of a protected tributylstannyl precursor 6, followed by hydrolysis in acidic methanol of the protecting groups in 61% overall radiochemical yield, with a radiochemical purity of over 98% and a specific activity of more than 15.4 GBq/μmol. Tissue distribution of [(125)I]1 in tumor-bearing mice showed signs of distribution profiles similar to the reported results for 6-deoxy-6-[(18)F]fluoro-L-ascorbic (6-(18)FAsA) acid and 6-deoxy-6-[(131)I]iodo-L-ascorbic acid (6-(131)IAsA) but with ... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5663331 Mon, 06 Feb 2012 14:06:02 +0100 5663331 http://www.medworm.com/index.php?rid=5663330&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22293484%26dopt%3DAbstract Authors: Wang ZW, Wang JS, Luo J, Wei DD, Kong LY Abstract A novel naphthalene glucoside, rheumone A (1), with an unprecedented skeleton containing a seven-membered lactone, and two new compounds, 1-O-phloroglucinyl-2-O-galloyl-6-O-cinnamoyl-β-D-glucoside (2) and chrysophanol 1-O-β-D-(6'-O-malonyl)glucoside (3), together with three known compounds (4-6) were isolated from the roots of Rheum palmatum. Their structures were elucidated mainly by spectroscopic analysis. These compounds were evaluated in vitro for their cytotoxicities towards human hepatocellular cancer cell lines Bel-7402 and Bel-7402/5Fu, and human gastric carcinoma cell line BGC-823. None of them showed cytotoxicity with IC(50) far beyond 50 μM. PMID: 22293484 [PubMed - in process] (Source: Chemical and Phar... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5663330 Mon, 06 Feb 2012 14:06:02 +0100 5663330 http://www.medworm.com/index.php?rid=5663329&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22293485%26dopt%3DAbstract Authors: Kiem PV, Anh Hle T, Nhiem NX, Minh CV, Thuy NT, Yen PH, Hang DT, Tai BH, Mathema VB, Koh YS, Kim YH Abstract The rhizomes of Hedychium coronarium have been used for the treatment of inflammation, skin diseases, headache, and sharp pain due to rheumatism in traditional medicine. From this plant, two new labdanes, 15-methoxylabda-8(17),11E,13-trien-16,15-olide (1) and 16-methoxylabda-8(17),11E,13-trien-15,16-olide (3), named hedycoronens A and B, as well as four known, labda-8(17),11,13-trien-16,15-olide (2), 16-hydroxylabda-8(17),11,13-trien-15,16-olide (4), coronarin A (5), and corronarin E (6) were isolated. Their chemical structures were elucidated by mass, 1D- and 2D-nuclear magnetic resonance (NMR) spectroscopy. They were evaluated for inhibitory effects on the lipopol... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5663329 Mon, 06 Feb 2012 14:06:02 +0100 5663329 http://www.medworm.com/index.php?rid=5663328&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22293486%26dopt%3DAbstract Authors: Aoki S, Honda Y, Kikuchi T, Miura T, Sugawara R, Yaoita Y, Kikuchi M, Machida K Abstract Six new secoiridoid constituents, named isoligustrosidic acid (1), 6'-O-trans-cinnamoyl 8-epikingisidic acid (2), 6'-O-cis-cinnamoyl 8-epikingisidic acid (3), oleopolynuzhenide A (4), nuzhenals A (5) and B (6) were isolated from the dried fruits of Ligustrum lucidum AIT. Their structures were established on the basis of spectral and chemical data. PMID: 22293486 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5663328 Mon, 06 Feb 2012 14:06:02 +0100 5663328 http://www.medworm.com/index.php?rid=5663327&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22293487%26dopt%3DAbstract In this study, a new aporphine alkaloid named annonamine (1) was isolated from the leaves of A. muricata L. together with four known benzylisoquinoline alkaloids (2-5). The structures of the isolated compounds were elucidated by the spectroscopic method. PMID: 22293487 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5663327 Mon, 06 Feb 2012 14:06:02 +0100 5663327 http://www.medworm.com/index.php?rid=5663326&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22293488%26dopt%3DAbstract Authors: Suzuki T, Uchino T, Miyazaki Y, Kagawa Y Abstract Characterization and release profiles of commercial dexamethasone dipropionate (DDP) from an innovator and 2 generic ointments (Methaderm (IM), Promethasone (GP), and Mainvate (GM)) and their admixtures with heparinoid ointment (Hirudoid Soft) were investigated. The admixtures were prepared using 2 mixing methods (slab or rotation/revolution mixer). Microscopic and FT-Raman spectrometric analyses revealed that the ointments, except for IM, contained DDP crystals. A silicone membrane was used for the evaluation of the DDP permeation. The permeated DDP amounts from GP and GM were lower than that from IM, indicating that DDP solubility in the ointment vehicle affected the release of DDP from the ointment. No significant differ... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5663326 Mon, 06 Feb 2012 14:06:02 +0100 5663326 http://www.medworm.com/index.php?rid=5663325&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22293489%26dopt%3DAbstract Authors: Ochiai K, Kojima A, Kohno Y Abstract An improved method for 4,4-dimethylpyrazolone synthesis with t-butylcarbazate was described. The applicability of this method to dihydropyridazinone formation was demonstrated. This method is useful for suppressing the side reaction caused by the high nucleophilicity of hydrazine. PMID: 22293489 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5663325 Mon, 06 Feb 2012 14:06:02 +0100 5663325 http://www.medworm.com/index.php?rid=5663324&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22293490%26dopt%3DAbstract Authors: Zhang P, Yang Y, Zheng X, Huang W, Ma Z, Shen Z Abstract An improved chemical reaction protocol with short time and easy work-up was described here for 2-phenylbenzofuran derivatives. The final purified products, 2-phenylbenzofuran derivatives 5a-g and the intermediate diols 4a-g, were evaluated for their estrogen receptor (ER) binding affinity and selective activity in vitro. Among these fourteen tested compounds, 4g and 5g showed higher binding affinity on ER subtypes, ERα and ERβ. Compound 4g exhibited preferable ERα binding, while 5g was more estrogen selective for ERβ. The molecular docking was also performed to explore the detailed interactive interface between ER and the compounds. PMID: 22293490 [PubMed - in process] (Source: Chemical and Pharmaceutical Bul... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5663324 Mon, 06 Feb 2012 14:06:02 +0100 5663324 http://www.medworm.com/index.php?rid=5663323&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22293491%26dopt%3DAbstract Authors: Yokosuka A, Suzuki T, Mimaki Y Abstract Four new cholestane glycosides (1-4) were isolated from the leaves of Cordyline terminalis (Agavaceae). The structures of the new compounds were determined on the basis of spectroscopic analysis and a few chemical transformations followed by chromatographic and spectroscopic analyses. PMID: 22293491 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5663323 Mon, 06 Feb 2012 14:06:02 +0100 5663323 http://www.medworm.com/index.php?rid=5663321&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22293492%26dopt%3DAbstract Authors: Lan YH, Peng YT, Thang TD, Hwang TL, Dai DN, Leu YL, Lai WC, Wu YC Abstract Further investigation of the methanolic extract of Fissistigma latifolium resulted in two new compounds whose structures were assigned as 2,5,6,7-tetramethoxyflavan (1) and 2'-hydroxy-4',5',6'-trimethoxybenzil (2). These two compounds were determined on the basis of chemical and spectroscopic evidences. Compound 2 is the first report of benzil from Fissistigma species. 2,5,6,7-Tetramethoxyflavan (1) showed a potent inhibitory effect on superoxide anion production in formyl-L-methionyl-L-leucyl-L-phenylalanine (fMLP)/cytochalasin B (CB)-activated human neutrophils. PMID: 22293492 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5663321 Mon, 06 Feb 2012 14:06:02 +0100 5663321 http://www.medworm.com/index.php?rid=5580166&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22223369%26dopt%3DAbstract Authors: Hamada Y Abstract 2,6-Dimethyl-9-Aryl-9-phosphabicyclo[3.3.1]nonanes (9-PBN and 9-NapBN) and the chiral diaminophosphine oxides (DIAPHOXs) derived from aspartic acid have been introduced as useful ligands and preligands, respectively, for transition metal-catalyzed asymmetric synthesis. anti-Selective asymmetric hydrogenation 
of α-amino-β-ketoesters using Ru-, Rh-, Ir-, and Ni-catalysts through dynamic kinetic resolution have been developed for the first time, producing efficiently important anti β-hydroxy-α-amino acids. The total synthesis of several biologically active natural products was achieved by use of the transition metal-catalyzed reaction using DIAPHOX, anti-selective asymmetric hydrogenation, and reactions developed by us. Synthesis of 
tangutorine, an... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5580166 Fri, 13 Jan 2012 03:30:03 +0100 5580166 http://www.medworm.com/index.php?rid=5580165&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22223370%26dopt%3DAbstract Authors: Okado R, Nowaki A, Matsuo J, Ishibashi H Abstract A catalytic amount of tin(IV) chloride catalyzed formal [4+2] cycloaddition reaction of di-tert-butyl 2-ethoxycyclobutane-1,1-carboxylate with ketones or aldehydes to give diethyl 6-ethoxydihydro-2H-pyran-3,3(4H)-dicarboxylates, whereas two equivalents of trimethylsilyl triflate promoted tandem [4+2] cycloaddition and lactonization to afford 3-oxo-2,6-dioxabicyclo[2.2.2]octane-4-carboxylate esters. PMID: 22223370 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5580165 Fri, 13 Jan 2012 03:30:03 +0100 5580165 http://www.medworm.com/index.php?rid=5580164&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22223371%26dopt%3DAbstract Authors: Qu J, Gong T, Ma B, Zhang L, Kano Y, Yuan D Abstract The purpose of the study is to compare alkaloid profile of Uncaria rhynchophylla hooks and leaves. Ten oxindole alkaloids and four glycosidic indole alkaloids were identified using HPLC-diode array detection (DAD) or LC-atmospheric pressure chemical ionization (APCI)-MS method, and a HPLC-UV method for simultaneous quantification of major alkaloids was validated. The hooks are characterized by high levels of four oxindole alkaloids rhynchophylline (R), isorhynchophylline (IR), corynoxeine (C) and isocorynoxeine (IC), while the leaves contained high level of two glycosidic indole alkaloids vincoside lactam (VL) and strictosidine (S). The presented methods have proven its usefulness in chemical characterization of U. rhync... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5580164 Fri, 13 Jan 2012 03:30:03 +0100 5580164 http://www.medworm.com/index.php?rid=5580163&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22223372%26dopt%3DAbstract Authors: Takeshita K, Kinoshita S, Okazaki S Abstract To develop an estimation method of gadolinium magnetic resonance imaging (MRI) contrast agents, the effect of concentration of Gd compounds on the ESR spectrum of nitroxyl radical was examined. A solution of either 4-oxo-2,2,6,6-tetramethylpiperidine-N-oxyl (TEMPONE) or 4-hydroxy-2,2,6,6-tetramethylpiperidine-N-oxyl (TEMPOL) was mixed with a solution of Gd compound and the ESR spectrum was recorded. Increased concentration of gadolinium-diethylenetriamine pentaacetic acid chelate (Gd-DTPA), an MRI contrast agent, increased the peak-to-peak line widths of ESR spectra of the nitroxyl radicals, in accordance with a decrease of their signal heights. A linear relationship was observed between concentration of Gd-DTPA and line width o... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5580163 Fri, 13 Jan 2012 03:30:03 +0100 5580163 http://www.medworm.com/index.php?rid=5580162&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22223373%26dopt%3DAbstract Authors: Waki T, Nakanishi I, Matsumoto K, Kitajima J, Chikuma T, Kobayashi S Abstract The antioxidant activities of flavonoids and their glycosides were measured with the 2,2-diphenyl-1-picrylhydrazyl radical (DPPH radical, DPPH(·)) scavenging method. The results show that free hydroxyl flavonoids are not necessarily more active than O-glycoside. Quercetin and kaempferol showed higher activity than apigenin. The C- and O-glycosides of flavonoids generally showed higher radical scavenging activity than aglycones; however, kaempferol C3-O-glycoside (astragalin) showed higher activity than kaempferol. In the radical scavenging activity of flavonoids, it was expected that OH substitutions at C3 and C5 and catechol substitution at C2 of B ring and intramolecular hydrogen bonding betwe... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5580162 Fri, 13 Jan 2012 03:30:03 +0100 5580162 http://www.medworm.com/index.php?rid=5580161&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22223374%26dopt%3DAbstract Authors: Suzuki T, Araki T, Kitaoka H, Terada K Abstract Sitafloxacin (STFX) hydrate is a non-stoichiometric hydrate. The hydration state of STFX hydrate varies non-stoichiometrically depending on the relative humidity and temperature, though X-ray powder diffraction (XRPD) of STFX hydrate was not affected by storing at low and high relative humidities. The detailed properties of crystalline water of STFX hydrate were estimated in terms of hygroscopicity, thermal analysis combined with X-ray powder diffractometry, crystallography and density functional theory (DFT) calculation. STFX hydrate changed the water contents continuously and reversibly from an equivalent amount of dihydrate through that of sesquihydrate depending on the relative humidity at 25°C. Thermal analysis and X-ra... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5580161 Fri, 13 Jan 2012 03:30:03 +0100 5580161 http://www.medworm.com/index.php?rid=5580160&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22223375%26dopt%3DAbstract Authors: Naito T, Takashina Y, Yagi T, Kawakami J Abstract A few complicated and time-consuming methods are available for the determination of residual fentanyl in Durotep(®) MT transdermal patches, however, their application to clinical settings is limited. The aim of this study was to develop a simple and rapid HPLC-UV method using an ultrafine particle octadecylsilane (ODS) for the determination of residual fentanyl in applied Durotep(®) MT transdermal matrix patches. Patch extraction involved sonicating a shredded Durotep(®) MT patch in acetonitrile for 15 min. Fentanyl separation was completed within 2 min using a 2.3-μm particle ODS column (50×4.6 mm i.d.) at a flow rate of 1.5 mL/min. No peaks interfering with fentanyl (1.27 min) and papaverine (0.89 min) as... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5580160 Fri, 13 Jan 2012 03:30:03 +0100 5580160 http://www.medworm.com/index.php?rid=5580159&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22223376%26dopt%3DAbstract Authors: Chaipech S, Morikawa T, Ninomiya K, Yoshikawa M, Pongpiriyadacha Y, Hayakawa T, Muraoka O Abstract Two new phenolic glycosides, kaempferiaosides A and B were isolated from the rhizomes of Kaempferia parviflora (Zingiberaceae) together with 24 known compounds. Their structures including absolute stereochemistry were elucidated on the basis of chemical and spectroscopic evidence. Among the isolates, 5,3'-dihydroxy-3,7,4'-trimethoxyflavone showed higher activity than silybin, a commercial hepatoprotective agent. PMID: 22223376 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5580159 Fri, 13 Jan 2012 03:30:03 +0100 5580159 http://www.medworm.com/index.php?rid=5580158&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22223377%26dopt%3DAbstract Authors: Mohebbi S, Falcón-Pérez JM, González E, Millet O, Mato JM, Kobarfard F Abstract A series of 2-substituted-4,6-diaminipyrimidine derivatives were synthesized and evaluated for their dihydrofolate reductase (DHFR) inhibitory activity. Saturation transfer difference (STD) (1)H-NMR experiments were used to probe the binding characteristics of the compounds with human DHFR enzyme. The most potent molecules, 12 and 15, in enzyme assay study showed the best results in STD experiments indicating their intimate interaction with the receptor. The docking studies were followed to explain the structural basis for the observed interaction between the ligands and DHFR. All the compounds were also assayed in vitro for their growth inhibitory activity on MCF-7, HepG2, SKHep1, and Hela ... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5580158 Fri, 13 Jan 2012 03:30:03 +0100 5580158 http://www.medworm.com/index.php?rid=5580157&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22223378%26dopt%3DAbstract Authors: Kimura H, Mori D, Harada N, Ono M, Ohmomo Y, Kajimoto T, Kawashima H, Saji H Abstract (99m)Tc-tricarbonyl [(99m)Tc(CO)(3)] complexes have been conventionally synthesized by heating [(99m)Tc(CO)(3)(H(2)O)(3)](+) and a tridentate chelating ligand under atmospheric pressure; however, this method is poor in terms of chemical yield and reproducibility. Moreover, since the half-life of (99m)Tc is very short (6 h), the development of facile and rapid methods of synthesizing (99m)Tc-labeled compounds, which could be used as radioactive tracers for single photon emission computed tomography (SPECT), is required. Thus, we initiated a study on the application of a microwave reaction to the synthesis of (99m)Tc(CO)(3)-2-picolylamine monoacetic acid (PAMA) [(99m)Tc(CO)(3)-PAMA] compl... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5580157 Fri, 13 Jan 2012 03:30:03 +0100 5580157 http://www.medworm.com/index.php?rid=5580156&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22223379%26dopt%3DAbstract Authors: Onuki Y, Ikegami-Kawai M, Ishitsuka K, Hayashi Y, Takayama K Abstract The precipitation of phenytoin sodium injection provoked by mixing with infusion fluids renders its use in clinical practice difficult, as rapid intravenous (i.v.) push and i.v. infusion are supposed to be avoided. As some of its aspects remain unclear, this study tried to elucidate this precipitation mechanism. In particular, this study focused on the significant precipitation induced by glucose infusion fluid. The precipitation provoked by 5% glucose infusion fluid was obviously different from the precipitation that accompanied simple pH reduction, in terms of the growth mode and morphology of crystals. In addition, the effect of glucose was partially unrelated to pH reduction. NMR measurements includi... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5580156 Fri, 13 Jan 2012 03:30:03 +0100 5580156 http://www.medworm.com/index.php?rid=5580155&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22223380%26dopt%3DAbstract Authors: Nomura S, Arimitsu K, Yamaguchi S, Kosuga Y, Kakimoto Y, Komai T, Hasegawa K, Nakanishi A, Miyoshi T, Iwasaki H, Ozeki M, Kawasaki I, Kurume A, Ohta S, Yamashita M Abstract (±)-8-Deisopropyladunctin B, the deisopropyl form of adunctin B, which was isolated from the leaves of Piper aduncum (Piperaceae) collected in Papua New Guinea, was synthesized in 0.77% overall yield in 17 steps from 5,7-dimethoxycoumarin-3-carboxylate. The key step was our original stereoconvergent skeleton transformation from 1,2,2a,8b-tetrahydro-3H-benzo[b]cyclobuta[d]pyran-3-one to 1,2,4a,9b-tetrahydrodibenzofuran-4-ol with dimethylsulfoxonium methylide. PMID: 22223380 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5580155 Fri, 13 Jan 2012 03:30:03 +0100 5580155 http://www.medworm.com/index.php?rid=5580154&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22223381%26dopt%3DAbstract Authors: Kunda UM, Balam SK, Nemallapudi BR, Chereddy SS, Nayak SK, Cirandur SR Abstract A green and efficient preparation method for the amino bisphosphonates is accomplished by simple mixing and stirring of diethylphosphite, triethylorthoformate and various amines in the presence of amberlyst-15 as catalyst at room temperature under solvent free conditions. The title compounds are characterized by IR, (1)H-, (13)C-, (31)P-NMR and mass spectra, also studied their antimicrobial and antioxidant activity. PMID: 22223381 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5580154 Fri, 13 Jan 2012 03:30:03 +0100 5580154 http://www.medworm.com/index.php?rid=5580153&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22223382%26dopt%3DAbstract Authors: Ragab FA, Eid NM, Hassan GS, Nissan YM Abstract New series of furosalicylic acids 3a-c, furosalicylanilides 6a-n, furobenzoxazines 8a-f, 1-benzofuran-3-arylprop-2-en-1-ones 12a,b, 6-(aryl-3-oxoprop-1-enyl)-4H-chromen-4-ones 16a-c and 6-[6-aryl-2-thioxo-2,5-dihydropyrimidin-4-yl]-4H-chromen-4-ones 17a-c were synthesized. Anti-inflammatory activity evaluation was performed using carrageenan-induced paw edema model in rats and prostaglandin E(2) (PGE(2)) synthesis inhibition activity. Some of the tested compounds revealed comparable activity with less ulcerogenic effect than Diclofenac at a dose 100 mg/kg. All the synthesized compounds were docked on the active site of cyclooxygenase-2 (COX-2) enzyme and most of them showed good interactions with the amino acids of the acti... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5580153 Fri, 13 Jan 2012 03:30:03 +0100 5580153 http://www.medworm.com/index.php?rid=5580152&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22223383%26dopt%3DAbstract Authors: Murata T, Miyase T, Yoshizaki F Abstract An extract of Keiskea japonica MIQ. showed an inhibitory effect on hyaluronidase activity. From the extract, four new phenylpropanoids, two new maltol glycosides, two new monoterpene glycosides, and two new phenolic compounds were isolated together with 19 known compounds. Among these constituents, two phenylpropanoids and a flavone glucuronide were revealed as hyaluronidase inhibitors. PMID: 22223383 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5580152 Fri, 13 Jan 2012 03:30:03 +0100 5580152 http://www.medworm.com/index.php?rid=5580151&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22223384%26dopt%3DAbstract Authors: Yahagi T, Daikonya A, Kitanaka S Abstract Obesity is a serious health problem worldwide. We investigated the anti-obesity effect of the flower of Albizia julibrissin DURAZZ. (Leguminosae). A 90% EtOH extract of the flower inhibited adipogenesis in 3T3-L1 preadipocytes, as well as the activity of glycerol-3-phosphate dehydrogenase (GPDH) activity. New flavonol acylglycosides (1-4) and eighteen known compounds (5-22) were isolated by bioassay-directed fractionation. These new glycosides were elucidated to be 3″-(E)-p-coumaroylquercitrin (1), 3″-(E)-feruloylquercitrin (2), 3″-(E)-cinnamoylquercitrin (3), and 2″-(E)-cinnamoylquercitrin (4) on the basis of spectroscopic and chemical analysis. These compounds inhibited adipogenesis in 3T3-L1 preadipocytes. In particular,... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5580151 Fri, 13 Jan 2012 03:30:03 +0100 5580151 http://www.medworm.com/index.php?rid=5580150&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22223385%26dopt%3DAbstract We describe the total synthesis and structural determination of (+)-akaterpin (1), an inhibitor of phosphatidylinositol-specific phospholipase C (PI-PLC). The key features of the synthetic strategy include the resolution of β,γ-unsaturated ketone (±)-2a with chiral sulfoximine 6. The absolute stereochemistry was determined by comparison of the specific optical rotation data of (+)-1 and (-)-1 with that of natural akaterpin. PMID: 22223385 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5580150 Fri, 13 Jan 2012 03:30:03 +0100 5580150 http://www.medworm.com/index.php?rid=5580149&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22223386%26dopt%3DAbstract Cardioactive C(19)-Diterpenoid Alkaloids from the Lateral Roots of Aconitum carmichaeli "Fu Zi". Chem Pharm Bull (Tokyo). 2012;60(1):144-9 Authors: Liu XX, Jian XX, Cai XF, Chao RB, Chen QH, Chen DL, Wang XL, Wang FP Abstract Bioassay-guided fractionation of an n-BuOH extract of the lateral roots of Aconitum carmichaeli. led to the isolation of 5 cardioactive C(19)-diterpenoid alkaloids: N-deethylaconine (1), beiwutinine (2), hypaconine (3), mesaconine (4), and 15α-hydroxyneoline (5). N-Deethylaconine and beiwutinine are new aconitine-type C(19)-diterpenoid alkaloids. Hypaconine was isolated from this species for the first time. Among them, mesaconine, hypaconine, and beiwutinine showed the strongest cardiac actions on the isolated perfused bullfrog heart. Furthermore, mes... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5580149 Fri, 13 Jan 2012 03:30:03 +0100 5580149 http://www.medworm.com/index.php?rid=5580148&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22223387%26dopt%3DAbstract Authors: Nakata N, Tokudome A, Yanai H, Nohara T Abstract A spirosolane derivative possessing a hydroxyl group at C-23, esculeogenin A, a sapogenol of tomato saponin, was found to be easily converted into the corresponding pregnane derivative by refluxing with aqueous pyridine. Therefore, introduction of a hydroxyl group into the C-23 of diosgenin (as representative of spirostane derivatives) and solasodine (as representative of spirosolane derivatives) was attempted by the reaction of NaNO(2)-BF(3) · Et(2)O. In diosgenin, the objective compound was obtained by the reaction in AcOH. However, in solasodine, we obtained a 23-nitroso derivative by the reaction in AcOH and 23,24-bisnorcholanic acid 22-16 lactone, or vespertilin, in AcOH and CHCl(3). PMID: 22223387 [PubMed - in... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5580148 Fri, 13 Jan 2012 03:30:03 +0100 5580148 http://www.medworm.com/index.php?rid=5580147&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22223388%26dopt%3DAbstract Authors: Janar J, Nugroho AE, Wong CP, Hirasawa Y, Kaneda T, Shirota O, Morita H Abstract Six new diterpenoids, sabiperones A-F (1-6) have been isolated from the aerial part of Juniperus sabina. Their structures were elucidated by spectroscopic methods including 2D NMR techniques. Sabiperone F showed moderate cell growth inhibitory activities against five human cancer cell lines. PMID: 22223388 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5580147 Fri, 13 Jan 2012 03:30:03 +0100 5580147 http://www.medworm.com/index.php?rid=5580146&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22223389%26dopt%3DAbstract Authors: Chen YH, Hwang TL, Su YD, Chang YC, Chen YH, Hong PH, Hu LC, Yen WH, Hsu HY, Huang SJ, Kuo YH, Sung PJ Abstract Two new 6-hydroxyeunicellin diterpenoids, cladieunicellin G (1) and 6-epi-cladieunicellin F (2), were isolated from an Indonesian octocoral Cladiella sp. The structures of eunicellins 1 and 2 were established by spectroscopic methods and 2 was found to be an epimer of the known eunicellin cladieunicellin F (3). Eunicellin 2 displayed inhibitory effects on the generation of superoxide anion and the release of elastase by human neutrophils. PMID: 22223389 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5580146 Fri, 13 Jan 2012 03:30:03 +0100 5580146 http://www.medworm.com/index.php?rid=5580145&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22223390%26dopt%3DAbstract Authors: Okada T, Hiromura M, Otsuka M, Enomoto S, Miyachi H Abstract Adipocyte fatty acid binding protein (A-FABP; FABP4), which is predominantly expressed in macrophages and adipose tissue, regulates fatty acid storage and lipolysis, and is also an important mediator of inflammation. Here, we report a synthesis of (14)C-labeled 2-[2'-(5-ethyl-3,4-diphenyl-1H-pyrazol-1-yl)biphenyl-3-yloxy]acetic acid (BMS309403), a potent and selective small-molecular FABP4 inhibitor, as a chemical tool for investigating the roles of FABP4 in inflammatory and metabolic disorders. The structure-activity relationship of several BMS derivatives for inhibition of FABP4 is also reported. PMID: 22223390 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5580145 Fri, 13 Jan 2012 03:30:03 +0100 5580145 http://www.medworm.com/index.php?rid=5478855&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22130363%26dopt%3DAbstract Authors: Mizukami S Abstract Molecular imaging technologies, which enable the visualization of the behaviors or functions of biomolecules in living systems, have received considerable attention from life scientists. Novel imaging technologies that overcome the limitations of current imaging techniques are desired. In this review, two independent technologies that were recently developed by the authors are described. The first technology is for smart (19)F magnetic resonance imaging (MRI) probes that were developed for in vivo applications. These probes were developed by exploiting paramagnetic relaxation enhancement in order to detect hydrolase activity. With respect to cellular applications, gene expression in cells was visualized using one of the (19)F MRI probes. It was confirme... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5478855 Wed, 07 Dec 2011 18:48:02 +0100 5478855 http://www.medworm.com/index.php?rid=5478854&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22130364%26dopt%3DAbstract Authors: Maeda H, Kusuhara T, Tsuhako M, Nakayama H Abstract The phosphorylation of 5'-deoxy-5-fluorouridine (doxifluridine, 5'-DFUR) has been achieved using inorganic cyclo-triphosphate (P(3m), Na(3)P(3)O(9)) and monoimido-cyclo-triphosphate (MCTP, Na(3)P(3)O(8)NH) in aqueous solution. In the reaction of 5'-DFUR with P(3m), 2'-monophospho-5'-DFUR and 3'-monophospho-5'-DFUR were synthesized with a total yield of more than 95%. In the reaction of 5'-DFUR with MCTP, 2'-diphosphoramidophosphono-5'-DFUR and 3'-diphosphoramidophosphono-5'-DFUR were synthesized with a total yield of more than 40%. The phosphorylated products with P(3m) and MCTP were stable in neutral and alkaline solutions. PMID: 22130364 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5478854 Wed, 07 Dec 2011 18:48:02 +0100 5478854 http://www.medworm.com/index.php?rid=5478853&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22130365%26dopt%3DAbstract In this study, we focus on troglitazone which is composed of diastereomers, RR/SS and RS/SR, as model compound, because each diastereomer has the same molecular weight and similar chemical structure. Troglitazone is isolated into each diastereomer, and both amorphous prepared from RR/SS and RS/SR showed similar T(g) (around 60°C). The surface relaxation of each amorphous troglitazone prepared from two diastereomers, RR/SS and RS/SR, was determined to compare surface molecular mobility, using inverse gas chromatography under dry conditions. As a result, amorphous prepared from RS/SR, showed the shorter surface relaxation time at 40°C (temperature below T(g)), which means it has higher molecular mobility than that from RR/SS at the surface although both have the same molecular weight and s... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5478853 Wed, 07 Dec 2011 18:48:02 +0100 5478853 http://www.medworm.com/index.php?rid=5478852&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22130366%26dopt%3DAbstract Authors: Nishimura Y, Okamoto Y, Ikunaka M, Ohyama Y Abstract A mixture of alkyl 1,4-dihydro-2-methylthio-4,4,6-trisubstituted pyrimidine-5-carboxylate 1 and its tautomeric isomer, alkyl 1,6-dihydro-2-methylthio-4,6,6-trisubstituted pyrimidine-5-carboxylate 2 is synthesized by the Atwal-Biginelli cyclocondensation reaction of S-methylisothiourea hemisulfate salt 3 with 2-(gem-disubstituted)methylene-3-oxoesters 4 that can be accessed by the Lehnert procedure for the Knoevenagel-type condensation. The structures of the tautomeric products of the Atwal-Biginelli cyclocondensation reaction, 1 and 2, which are inseparable from each other, are determined unambiguously by (1)H-NMR spectroscopy at various temperatures and nuclear Overhauser enhancement spectroscopy (NOESY) experiment. Bec... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5478852 Wed, 07 Dec 2011 18:48:02 +0100 5478852 http://www.medworm.com/index.php?rid=5478851&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22130367%26dopt%3DAbstract Authors: Yokosuka A, Matsuo Y, Jitsuno M, Adachi K, Mimaki Y Abstract Two new lignan glycosides, named larrealignans A (1) and B (2), and a known lignan (3) were isolated from the aerial parts of Larrea tridentata (Zygophyllaceae). The structures of 1 and 2 were determined on the basis of spectroscopic analysis and the results of hydrolytic cleavage. The isolated compounds (1-3) and aglycones (1a, 2a) of 1 and 2 were evaluated for their cytotoxic activities against HL-60 human leukemia cells. PMID: 22130367 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5478851 Wed, 07 Dec 2011 18:48:02 +0100 5478851 http://www.medworm.com/index.php?rid=5478850&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22130368%26dopt%3DAbstract Authors: Ricci J, Kim M, Chung WY, Park KK, Jung M Abstract Novel artemisinin-glycolipid hybrids were directly synthesized from 12β (C-C)-type deoxoartemisinin and glycolipid and exhibited exceptional in vitro anticancer activity, particularly against the oral carcinoma cancer cell lines, respectively. The artemisinin-glycolipid hybrids, with effective concentrations under 20 µM, demonstrated better anticancer activity than either artemisinin or glycolipid alone and showed five times more anti-oral cancer activity than either cisplatin or paclitaxel. PMID: 22130368 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5478850 Wed, 07 Dec 2011 18:48:02 +0100 5478850 http://www.medworm.com/index.php?rid=5478849&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22130369%26dopt%3DAbstract In this study, we investigated its effect on breast cancer cell proliferation and its potential mechanism of action in vitro. Treatment of cells with fangchinoline significantly inhibited MDA-MB-231 cell proliferation in a concentration- and time-dependent manner. To define the mechanism underlying the antiproliferative effects of fangchinoline, we studied its effects on critical molecular events known to regulate the apoptotic machinery. Specifically, we addressed the potential of fangchinoline to induce apoptosis of breast cancer cells. Fangchinoline induced internucleosomal DNA fragmentation, chromatin condensation, activation of caspases-3, -8, and -9, and cleavage of poly(ADP ribose) polymerase, as well as enhanced mitochondrial cytochrome c release. Furthermore, fangchinoline increas... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5478849 Wed, 07 Dec 2011 18:48:02 +0100 5478849 http://www.medworm.com/index.php?rid=5478848&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22130370%26dopt%3DAbstract Authors: Tamaki M, Takanashi K, Harada T, Fujinuma K, Shindo M, Kimura M, Uchida Y Abstract To find candidates with high antimicrobial and low hemolytic activities, many gramicidin S (GS) analogs of various ring sizes have been designed and synthesized. However, syntheses of antimicrobially active analogues of GS having a disordered symmetry structure from C(2) have almost never been reported, because the stable, amphiphilic β-sheet structure of GS with C(2) symmetry is considered essential for its strong antibacterial activity. In the present studies, novel thirteen cycloundecapeptides 1-13 related to GS were synthesized and examined. Among them, cyclo(-Va1(1)-Orn(2)-Leu(3)-D-Phe(4)-X(5)-Pro(6)-Val(7)-Orn(8)-Leu(9)-D-Phe(10)-Pro(11)-) (X=Lys (10), Orn (11), Arg (12) and Lys(Lys) ... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5478848 Wed, 07 Dec 2011 18:48:02 +0100 5478848 http://www.medworm.com/index.php?rid=5478847&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22130371%26dopt%3DAbstract Authors: Mahrouse MA, Elkady EF Abstract A binary mixture of ciprofloxacin hydrochloride (CIP) and metronidazole (MET) was determined by five simple and accurate methods, without prior separation. In the first method, CIP was determined by second derivative spectrophotometric method ((2)D) by measuring the amplitude at 282 nm (zero ordinate value of MET). On the other hand, the determination of MET was based on isosbestic point technique, where the total content of the mixture was determined at 294.5 nm (isosbestic point), then the content of MET could be calculated by subtraction. The second method was first derivative ratio spectrophotometric method ((1)DD) where the total amplitude at 261 and 285 nm and the amplitude at 295.5 nm were selected to simultaneously determine CIP and ... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5478847 Wed, 07 Dec 2011 18:48:02 +0100 5478847 http://www.medworm.com/index.php?rid=5478846&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22130372%26dopt%3DAbstract Authors: Kambe T, Maruyama T, Naganawa A, Asada M, Seki A, Maruyama T, Nakai H, Toda M Abstract For the purpose of discovering an orally available EP4 subtype-selective agonist, a series of 8-aza prostaglandin E(1) (PGE(1)) analogs were synthesized and evaluated for their affinity for PGE(2) receptor subtypes. Additionally, the structure-activity relationships of these compounds were studied. Among the tested compounds, the 8-aza PGE(1) analog 6 and 8-aza-5-thiaPGE(1) analog 12 had highly potent EP4 receptor affinity, good functional activity, and excellent subtype-selectivity. Furthermore, these analogs demonstrated good stability in human liver microsomes. As a result, we concluded that these two series of 8-aza PGE(1) analogs could be promising chemical leads for an orally avail... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5478846 Wed, 07 Dec 2011 18:48:02 +0100 5478846 http://www.medworm.com/index.php?rid=5478845&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22130373%26dopt%3DAbstract Authors: Padmaja A, Muralikrishna A, Rajasekhar C, Padmavathi V Abstract A new class of pyrrolyl/pyrazolyl arylaminosulfonylmethyl 1,3,4-oxadiazoles, 1,3,4-thiadiazoles, and 1,2,4-triazoles were prepared and tested for antimicrobial activity. Amongst the tested compounds, 5c displayed high antimicrobial activity. PMID: 22130373 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5478845 Wed, 07 Dec 2011 18:48:02 +0100 5478845 http://www.medworm.com/index.php?rid=5478844&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22130374%26dopt%3DAbstract Authors: Nakamura H, Sugino Y, Iwasaki T, Watano S Abstract A novel single punch tablet machine was developed for a tiny amount of powder sample. This tablet machine mainly consists of upper and lower punches, single die, and conical powder feeder equipped with micro-vibrators. By using the powder feeder, mass of discharged powder can be maintained constant even if a tiny amount of powder having poor flowability is used. Motions of both upper and lower punches can be set arbitrarily. Thus, this machine enables us to prepare tablets with a tiny amount of powder sample under the same compression mechanism as conventional rotary tablet machines. Performance of the developed tablet machine was evaluated in a continuous direct tableting using a model powder with poor flowability. Thirty... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5478844 Wed, 07 Dec 2011 18:48:02 +0100 5478844 http://www.medworm.com/index.php?rid=5478843&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22130375%26dopt%3DAbstract Authors: Kambe T, Maruyama T, Nakano M, Yamaura Y, Shono T, Seki A, Sakata K, Maruyama T, Nakai H, Toda M Abstract Analogs 8-aza-16-aryl prostaglandin E(1) (PGE(1)) and 8-aza-5-thia-16-arylPGE(1) were synthesized and evaluated with respect to their subtype receptor affinity and EP4 agonist activity for the purposes of identifying subtype-selective EP4 agonists that demonstrate oral efficacy. Using an inhibition assay of lipopolysaccharide (LPS)-induced tumor necrosis factor (TNF)-α production in rats, representative compounds were evaluated for their pharmacokinetic profiles and in vivo efficacy. Structure-activity relationships (SARs) were characterized and presented. Of the compounds tested, several demonstrated better oral exposure and/or in vivo efficacy compared with the prev... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5478843 Wed, 07 Dec 2011 18:48:02 +0100 5478843 http://www.medworm.com/index.php?rid=5478842&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22130376%26dopt%3DAbstract Authors: Furukawa M, Suzuki H, Makino M, Ogawa S, Iida T, Fujimoto Y Abstract Two flavanones, 5,2',6'-trihydroxy-7,8-dimethoxyflavanone (1), 5,2',6'-trihydroxy-6,7,8-trimethoxyflavanone (2) and their 2'-O-β-D-glucosides (3, 4), and a neoclerodane-type diterpene, 15-demethoxyscupolin I (5), together with twenty-eight known compounds were isolated from the extracts of Lagochilus leiacanthus. The structures of the new compounds were determined by spectroscopic means. The two new flavanones and some known flavonoids showed the inhibitory activity on the release of β-hexosaminidase from RBL-2H3 cells. PMID: 22130376 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5478842 Wed, 07 Dec 2011 18:48:02 +0100 5478842 http://www.medworm.com/index.php?rid=5478841&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22130377%26dopt%3DAbstract Authors: Ge HL, Zhang DW, Li L, Xie D, Zou JH, Si YK, Dai J Abstract Two new terpenoids, (+)-(3S,6S,7R,8S)-periconone A (1) and (-)-(1R,4R,6S,7S)-2-caren-4,8-olide (2), have been isolated from an endophytic fungus Periconia sp., which was collected from the plant Annona muricata. Their structures were elucidated on the basis of extensive spectroscopic analyses. In the in vitro assays, the two compounds showed low cytotoxic activities against six human tumor cell lines (HCT-8, Bel-7402, BGC-823, A549, A2780 and MCF-7) with IC(50)>10(-5) M. PMID: 22130377 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5478841 Wed, 07 Dec 2011 18:48:02 +0100 5478841 http://www.medworm.com/index.php?rid=5478840&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22130378%26dopt%3DAbstract Authors: Kogure N, Katsuta N, Kitajima M, Takayama H Abstract Two new alkaloids (1, 2) were isolated from the whole plants of Crinum asiaticum var. sinicum together with seven known alkaloids. The structures of the new alkaloids were elucidated by spectroscopic analyses and chemical conversions from known alkaloids. New alkaloid 1 was isolated for the first time as a natural product, although it has been prepared as a synthetic product. PMID: 22130378 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5478840 Wed, 07 Dec 2011 18:48:02 +0100 5478840 http://www.medworm.com/index.php?rid=5478839&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22130379%26dopt%3DAbstract Authors: Reddy MV, Chen SS, Lin ML, Chan HH, Kuo PC, Wu TS Abstract The chalcone basic skeleton is a unique template which is associated with widespread biological activities. In the present study, a series of novel bichalcones linked with a 1,4-dimethylenepiperazine moiety was prepared through Mannich reaction and Clasien-Schmidt condensation. The synthetic analogs 2-16 were subjected into the cytotoxicity examinations using a panel of 25 human tumor cell lines. Among the tested compounds, 3 and 4 which possessed the 3-pyridyl and phenyl groups as the substructure, respectively, displayed significant cytotoxicity against all the tumor cell lines. The results suggested that these bichalcones were potential to be the anticancer lead drugs. PMID: 22130379 [PubMed - in process] (S... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5478839 Wed, 07 Dec 2011 18:48:02 +0100 5478839 http://www.medworm.com/index.php?rid=5478838&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22130380%26dopt%3DAbstract We report the development of a NF-κB inhibiting Cu(2+) complex with improved cell-penetrating activity arising from the coupling of a Tat peptide to HPH-Pep-Cu(2+). PMID: 22130380 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5478838 Wed, 07 Dec 2011 18:48:02 +0100 5478838 http://www.medworm.com/index.php?rid=5478837&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22130381%26dopt%3DAbstract Authors: Matsumoto T, Hosoya T, Tomoda H, Shiro M, Shigemori H Abstract Two new antimicrobial chlorinated cyclopentenones, palmaenones A (1) and B (2) were isolated from the culture broth of discomycete Lachnum palmae (NBRC-106495), and the structures of 1 and 2 were elucidated by spectroscopic data and the stereochemistry of 1 was directly determined by a single-crystal X-ray diffraction analysis. Palmaenones A (1) and B (2) are cyclopentenones containing three chlorines. Compound 1 exhibited potent antimicrobial activity against Micrococcus luteus, Mycobacterium smegmatis, Escherichia coli, Xanthomonas campestris, and Mucor racemosus, while the activities of compound 2 were weaker than 1. PMID: 22130381 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5478837 Wed, 07 Dec 2011 18:48:02 +0100 5478837 http://www.medworm.com/index.php?rid=5478836&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22130382%26dopt%3DAbstract Authors: Hu Z, Zhan R, Du X, Su J, Li XN, Yang JH, Zhang HB, Li Y, Sun HD, Li GP, Pu JX Abstract Five new ent-kaurane diterpenoids, isodonhenrins A-E (1-5), together with thirteen known ones were isolated from the aerial parts of Isodon henryi. Their structures were identified by means of extensive spectroscopic analysis, and the absolute configurations of 1 were determined by single-crystal X-ray diffraction. Most of the diterpenoids were evaluated for their cytotoxicity against HL-60, SMMC-7721, A-549, MCF-7, and SW480 cell lines. Compound 17 showed significant inhibitory effects on five cell lines, and compounds 6, 9, 10, 11, 12 and 16 exhibited selective activity. PMID: 22130382 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5478836 Wed, 07 Dec 2011 18:48:02 +0100 5478836 http://www.medworm.com/index.php?rid=5478835&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22130383%26dopt%3DAbstract This article is the first report on phytochemical study of S. yunnanensis. PMID: 22130383 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5478835 Wed, 07 Dec 2011 18:48:02 +0100 5478835 http://www.medworm.com/index.php?rid=5478834&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22130384%26dopt%3DAbstract Authors: Hayashi M, Sasano Y, Nagasawa S, Shibuya M, Iwabuchi Y Abstract A highly active organocatalyst for alcohol oxidation has been developed. 9-Azanoradamantane N-oxyl (Nor-AZADO 4), constituting an unhindered, stable nitroxyl radical, exhibits superior catalytic activity to 2,2,6,6-tetramethylpiperidine-1-oxyl (TEMPO) and AZADOs in the oxidation of alcohols to their corresponding carbonyl compounds. PMID: 22130384 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5478834 Wed, 07 Dec 2011 18:48:02 +0100 5478834 http://www.medworm.com/index.php?rid=5383276&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22041065%26dopt%3DAbstract Authors: Tu F, Dai Y, Yao Z, Wang X, Yao X, Qin L Abstract Five new flavonol glycosides (1, 3, 5-7) were isolated from the aerial parts of Epimedium pubescens MAXIM., along with two known compounds, sagittasine C (2) and 4',5-dihydroxyl-8-(3,3-dimethylallyl)-flavonol 3-O-[β-D-xylopyranosyl(1→3)-4-O-acetyl-α-L-rhamnopyranoside]-7-O-β-D-glucopyranoside (4). The structures were elucidated on the basis of their 1D-, 2D-NMR, MS, UV and IR spectra data. PMID: 22041065 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5383276 Tue, 08 Nov 2011 05:50:03 +0100 5383276 http://www.medworm.com/index.php?rid=5383275&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22041066%26dopt%3DAbstract Authors: Zhao Y, Yu Z, Fan R, Gao X, Yu M, Li H, Wei H, Bi K Abstract A high-performance liquid chromatographic-mass spectrometric method was developed for the simultaneous determination of 10 flavonoids in Viscum coloratum obtained from different host species and different sources. Viscum coloratum was extracted with 50% methanol. The extracts were separated on a C(18) column with a gradient of 0.1% (v/v) formic acid and methanol. The flavonoids in the extracts were detected by negative electrospray ionization mass spectrometry in selective ion monitoring mode. The calibration curves showed good linearity (r>0.998) within the test ranges (homoeriodictyol: 0.149-8.940 µg/ml, homoeriodictyol-7-O-β-D-glycoside: 0.230-13.80 µg/ml, homoeriodictyol-7-O-β-D-apiose (1→2)-β-D-gly... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5383275 Tue, 08 Nov 2011 05:50:03 +0100 5383275 http://www.medworm.com/index.php?rid=5383274&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22041067%26dopt%3DAbstract Authors: Nakahara Y, Okawa M, Kinjo J, Nohara T Abstract To facilitate effective resource utilization, we have investigated triterpene saponins such as saikosaponin from the aerial parts of Bupleurum (B.) falcatum L., which are commonly discarded. Seven oleanene saponins were isolated from this plant; they were classified as the 13,28-epoxy type, 12-ene type, 9(11),12-diene type, and 28-acid type on the basis of their structural characteristics. For comparison, we also examined the oleanene saponins of the seeds of B. falcatum and the aerial parts of B. rotundifolium L. to obtain seven saponins and one sapogenol from the former and thirteen oleanene saponins from the latter. Several compounds obtained from them were investigated for their hepatoprotective activity and hepatotoxicit... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5383274 Tue, 08 Nov 2011 05:50:03 +0100 5383274 http://www.medworm.com/index.php?rid=5383273&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22041068%26dopt%3DAbstract Authors: El-Aasr M, Fujiwara Y, Takeya M, Ono M, Nakano D, Okawa M, Kinjo J, Ikeda T, Miyashita H, Yoshimitsu H, Nohara T Abstract Garlicnin A (1), a new stable, sulfur-containing compound isolated from a fraction of the acetone extracts of Allium sativum L. garlic bulbs, showed the potential to suppress tumor cell proliferation by inhibiting the polarization of M2 alternatively activated macrophages, and its structure was characterized as 3,4-dimethyl-5-(4,5-dithia-1E,7-octadiene)-tetrahydrothiophene-2-sulfoxide-S-oxide, on the basis of the results of spectroscopic analysis results. PMID: 22041068 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5383273 Tue, 08 Nov 2011 05:50:03 +0100 5383273 http://www.medworm.com/index.php?rid=5383272&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22041069%26dopt%3DAbstract Authors: Yang GY, Wang RR, Mu HX, Li YK, Xiao WL, Yang LM, Pu JX, Zheng YT, Sun HD Abstract Four new neolignans, marphenols G-J (1-4), together with two known ones, were isolated from the leaves and stems of Schisandra wilsoniana. The structures of 1-4 were elucidated by spectroscopic methods, including extensive 1D- and 2D-NMR techniques. New compounds 1-4 were tested for their anti-human immunodeficiency virus (HIV)-1 activities and they showed weak bioactivities. PMID: 22041069 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5383272 Tue, 08 Nov 2011 05:50:03 +0100 5383272 http://www.medworm.com/index.php?rid=5383271&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22041070%26dopt%3DAbstract Authors: Ono M, Toyohisa D, Morishita T, Horita H, Yasuda S, Nishida Y, Tanaka T, Okawa M, Kinjo J, Yoshimitsu H, Nohara T Abstract Three new norlanostane-type triterpene glycosides, scillanostasides A, B, and C, and two new lanostane-type triterpene glycosides, scillanostasides D and E, were isolated from the bulbs of Scilla scilloides DRUCE (Liliaceae) along with one known norlanostane-type triterpene heptaglycoside, scillascilloside G-1. Their chemical structures were determined on the basis of spectroscopic data as well as chemical evidence. PMID: 22041070 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5383271 Tue, 08 Nov 2011 05:50:03 +0100 5383271 http://www.medworm.com/index.php?rid=5383270&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22041071%26dopt%3DAbstract In this report, we report on the synthesis of some new photocleavable 8-QS derivatives, in which halogen atoms or a nitro group was introduced at the 7-position, in an attempt to improve photoreactive properties and to produce a red-shift in the irradiation wavelength. The introduction of bromine and iodine resulted in an acceleration in the photoreaction by about 1.5 times, possibly due to a heavy atom effect. It was also found that 7-nitro-8-QS absorbs at >360 nm, and, as a result, the S-O bond of this compound can be cleaved by photoirradiation with a fluorescent lamp in aqueous solution and on silicon surface. PMID: 22041071 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5383270 Tue, 08 Nov 2011 05:50:03 +0100 5383270 http://www.medworm.com/index.php?rid=5383269&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22041072%26dopt%3DAbstract Authors: Bahashwan SA, Al-Omar MA, Ezzeldin E, Abdalla MM, Fayed AA, Amr AG Abstract In continuation of our previous work, a novel series of steroid derivatives were synthesized and their androgen receptor (AR) antagonist activities and in vivo antiandrogenic properties were evaluated. Twenty-one heterocyclic derivatives containing a cyanopyrane ring fused to a steroidal moiety were conveniently synthesized and screened for their antagonistic, antiandrogen and prostate anticancer activities comparable to that of bicalutamide as the reference control. Some of the compounds exhibited better antagonistic, antiandrogen and prostate anticancer activities than the reference controls. Initially the acute toxicity of the compounds was assayed via the determination of their LD(50). Syntheti... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5383269 Tue, 08 Nov 2011 05:50:03 +0100 5383269 http://www.medworm.com/index.php?rid=5383268&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22041073%26dopt%3DAbstract Authors: Ogino M, Nakada Y, Negoro N, Itokawa S, Nishimura S, Sanada T, Satomi T, Kita S, Kubo K, Marui S Abstract As a part of our research for novel potent and orally available acyl-CoA: cholesterol acyltransferase (ACAT) inhibitors that can be used as anti-atherosclerotic agents, we recently reported the discovery of the (4-phenylcoumarine)acetanilide derivative 1. However, compound 1 showed adrenal toxicity in animal models. In order to search for safer ACAT inhibitors that do not have adrenal toxicity, we examined the inhibitory activity of ACAT in human macrophage and adrenal cells. The introduction of a carboxylic acid moiety on the pendant phenyl ring and the adjustment of the lipophilicity led to the discovery of (2E)-3-[7-chloro-3-[2-[[4-fluoro-2-(trifluoromethyl)phenyl]a... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5383268 Tue, 08 Nov 2011 05:50:03 +0100 5383268 http://www.medworm.com/index.php?rid=5383267&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22041074%26dopt%3DAbstract Authors: Watanuki S, Matsuura K, Tomura Y, Okada M, Okazaki T, Ohta M, Tsukamoto S Abstract We synthesized and evaluated inhibitory activity against T-type Ca(2+) channels for a series of 1-alkyl-N-[(1R)-1-(4-fluorophenyl)-2-methylpropyl]piperidine-4-carboxamide derivatives. Structure-activity relationship studies have revealed that the isopropyl substituent at the benzylic position plays an important role in exerting potent inhibitory activity, and the absolute configuration of the benzylic position was found to be opposite that of mibefradil, which was first launched as a new class of T-type Ca(2+) channel blocker. Oral administration of N-[(1R)-1-(4-fluorophenyl)-2-methylpropyl]-1-[2-(3-methoxyphenyl)ethyl]piperidine-4-carboxamide (17f) lowered blood pressure in spontaneously hy... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5383267 Tue, 08 Nov 2011 05:50:03 +0100 5383267 http://www.medworm.com/index.php?rid=5383266&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22041075%26dopt%3DAbstract In this study, we hypothesized that a liposomal formulation of HDACI might efficiently deliver HDACI into tumors. To incorporate HDACI efficiently into the liposomal membrane, we synthesized six HDACI-lipid conjugates, in which polyethylene glycol(2000) (PEG(2000))-lipid or cholesterol (Chol) was linked with a potent hydroxamic acid, HDACI, SAHA or K-182, by cleavable linkers, such as ester, carbamide and disulfide bonds. Liposomal HDACI-lipid conjugates were prepared with distearoylphosphatidylcholine (DSPC) and HDACI-Chol conjugate or with DSPC, Chol and HDACI-PEG-lipid conjugates, and their cytotoxicities were evaluated for human cervix tumor HeLa and mouse colon tumor Colon 26 cells. Among the liposomes, liposomal oleyl-PEG(2000)-SAHA conjugated with SAHA and oleyl-PEG(2000) via a carb... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5383266 Tue, 08 Nov 2011 05:50:03 +0100 5383266 http://www.medworm.com/index.php?rid=5383265&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22041076%26dopt%3DAbstract Authors: Wu LZ, Wu HF, Xu XD, Yang JS Abstract Two new flavone C-glycosides, trollisin A (1) and trollisin B (2), along with seven known flavonoids, isoswertisin (3), isoswertiajaponin (4), orientin (5), 2″-O-β-L-galactopyranosylvitexin (6), 2″-O-β-L-galactopyranosylorientin (7), neodiosmin (8) and acacetin-7-O-neohesperidoside (9) were isolated from the flowers of Trollius ledebourii REICHB. The structures of the new compounds were elucidated based on spectral analysis, including MS, 1D- and 2D-NMR experimentation. PMID: 22041076 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5383265 Tue, 08 Nov 2011 05:50:03 +0100 5383265 http://www.medworm.com/index.php?rid=5383264&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22041077%26dopt%3DAbstract Authors: Sasaki T, Li W, Morimura H, Li S, Li Q, Asada Y, Koike K Abstract The MeOH extract from the whole plants of Sambucus adnata has shown significant protein-tyrosine phosphatase 1B (PTP1B) inhibitory activity. Chemical study on the extract resulted in the isolation of thirteen compounds, including a novel triterpene (1). The structure of 1 was determined to be 1α,3β-dihydroxy-urs-12-en-11-one-3-yl palmitate on the basis of extensive spectroscopic analyses. Among the isolated compounds, ursolic acid, oleanolic acid and (±)-boehmenan showed the most potent PTP1B inhibitory activity in vitro with the IC(50) values of 4.1, 14.4 and 43.5 µm, respectively. The kinetic analysis indicated that (±)-boehmenan inhibits PTP1B activity in a competitive manner. PMID: 22041077 [Pub... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5383264 Tue, 08 Nov 2011 05:50:03 +0100 5383264 http://www.medworm.com/index.php?rid=5383263&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22041078%26dopt%3DAbstract In this study, we investigated the surface properties of raw wheat bran (R-WB) and wheat bran treated with Pectinase PL (P-WB) to evaluating its efficacy for removal of cadmium from waste water. The concentration of cadmium ions adsorbed by them was evaluated. The concentration of carboxyl groups of R-WB (3.56 mmol/g) was greater than that of P-WB (2.11 mmol/g), which indicated that the pectin of R-WB was broken down, resulting in a decrease in the concentration of carboxyl groups due to the enzyme treatment. From the scanning electron microscope (SEM) images of P-WB, the pores were newly generated with enzyme treatment. The concentration of cadmium ions adsorbed onto R-WB was greater than that of cadmium ions adsorbed onto P-WB. These results show that the adsorption mechanism of cadmium ... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5383263 Tue, 08 Nov 2011 05:50:03 +0100 5383263 http://www.medworm.com/index.php?rid=5383262&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22041079%26dopt%3DAbstract Authors: Ohno M, Ono M, Nohara T Abstract A new solanocapsine-type tomato glycoside, a novel and interesting natural steroidal glycoside, was isolated from a mini tomato, Solanum lycopersicum L. The chemical structure of the new minor glycoside, esculeoside B-5 (3), was determined to be (5S,22R,23S,24R,25S)-22,26-epimino-16β,23-epoxy-3β,23,24-trihydroxycholestane 3-O-β-lycotetraoside. PMID: 22041079 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5383262 Tue, 08 Nov 2011 05:50:03 +0100 5383262 http://www.medworm.com/index.php?rid=5383261&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22041080%26dopt%3DAbstract Authors: Manabe H, Takemoto A, Maehara H, Ohno M, Murakami Y, Itoh S, Nohara T Abstract In the conventional method of mixer blending extraction, the yields of the tomato-saponin, esculeoside A, in the mini and middy tomatoes were found to be 0.043% and 0.046%, respectively. In order to improve the yields, we attempted a more efficient extraction using shock waves. The yields of esculeoside A were 0.0987% in air after 1 shock, 0.0792% in air after two shots, 0.0648% in half water after 1 or 2 shocks, and 0.0599% in water after 1 or 2 shocks. The yields obtained by the proposed method were approximately twice those of the conventional mixer blending method; therefore, this method is regarded to be very efficient. Moreover, two spirosolane glycosides, tomatine and lycoperoside A, were... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5383261 Tue, 08 Nov 2011 05:50:03 +0100 5383261 http://www.medworm.com/index.php?rid=5383260&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22041081%26dopt%3DAbstract Authors: Iwata N, Kitanaka S Abstract Two new cannabinoid-like chromane and chromene derivatives named anthopogocyclolic acid (1) and anthopogochromenic acid (2) and five related compounds (3-7) which are known as synthetic analogues of cannabinoids: cannabichromene (CBC) type, cannabicyclol (CBL) type, and cannabicitran (CBT) type, have been isolated together with geranyl orsellinic acid (8) from the Chinese medicinal plant Rhododendron anthopogonoides. Their structures were elucidated based on spectroscopic and chemical evidence. The absolute configuration of the asymmetric carbons at C-2 of 1-7 was determined to be S from their circular dichroism (CD) spectra. Compounds 2, 4 and 6 inhibited compound 48/80-induced histamine release from rat peritoneal mast cells. PMID: 220410... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5383260 Tue, 08 Nov 2011 05:50:03 +0100 5383260 http://www.medworm.com/index.php?rid=5383259&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22041082%26dopt%3DAbstract Authors: Alam MS, Liu L, Lee DU Abstract A series of 5-phenyl-4,5-dihydro-1,3,4-thiadiazoles were synthesized and their cytotoxicity was examined against four human cancer cell lines, e.g. lung cancer (A549), ovarian cancer (SK-OV-3), skin cancer (SK-MEL-2), and colon cancer (HCT15). The title compounds were synthesized by condensation of thiosemicarbazide with substituted benzaldehydes, followed by cyclization with acetic anhydrides in good yields. Most of the compounds exhibited significant suppressive activity against the growth of all of the cancer cell lines. The 4-hydroxy analogue of 5-phenyl-4,5-dihydro-1,3,4-thiadiazole (2h) was most active in the inhibition of growth of the SK-MEL-2 cell line, with an IC(50) value of 4.27 µg/ml; followed by compound 2a (IC(50) 5.16 µg/ml... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5383259 Tue, 08 Nov 2011 05:50:03 +0100 5383259 http://www.medworm.com/index.php?rid=5383258&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22041083%26dopt%3DAbstract Authors: Tung NH, Quang TH, Ngan NT, Minh CV, Anh BK, Long PQ, Cuong NM, Kim YH Abstract Ten oleanane-type saponins (1-10), including three new compounds, namely bifinosides A-C (1-3), were isolated from the roots of Panax bipinnatifidus SEEM. Their structures were elucidated on the basis of chemical and spectroscopic methods. PMID: 22041083 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5383258 Tue, 08 Nov 2011 05:50:03 +0100 5383258 http://www.medworm.com/index.php?rid=5383257&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22041084%26dopt%3DAbstract Authors: Hu QF, Mu HX, Huang HT, Lv HY, Li SL, Tu PF, Li GP Abstract Two new secolignans and one new neolignan, named feddeiphenols A-C (1-3), together with eight known compounds (4-11), were isolated from the leaves and stems of Daphne feddei. Their structures were established on the base of spectroscopic methods, mainly extensive NMR, UV spectroscopy, and MS spectrometry. Compounds 1-11 were tested for their anti-human immunodeficiency virus (HIV)-1 activity and cytotoxicity. The results revealed that compounds 1, 2, 3, 7, and 9 showed therapeutic index (TI) values above 30, respectively, and the other compounds also showed weak anti-HIV-1 activity. Compound 1 showed modest cytotoxic activity. The other compounds also showed weak cytotoxic activity. PMID: 22041084 [PubMed - i... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5383257 Tue, 08 Nov 2011 05:50:03 +0100 5383257 http://www.medworm.com/index.php?rid=5383256&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22041085%26dopt%3DAbstract Authors: Kim KH, Ha SK, Choi SU, Kim SY, Lee KR Abstract Two new lignans, termed pharsyringaresinol (1) and pharbilignoside (2), a new phenylethanoid glycoside, termed pharbiniloside (3), and 22 known compounds, were isolated from the ethanol extract of the seeds of Pharbitis nil. The structures of the new compounds (1-3) were determined on the basis of spectroscopic analyses, including 2D-NMR and circular dichroism (CD) spectroscopy studies. Among the isolates, compounds 2, 11, 12, and 24 exhibited significant cytotoxicity against human tumor cell lines (A549, SK-OV-3, SK-MEL-2, and HCT-15) with IC(50) values ranging from 8.07 to 28.30 µM. In addition, compounds 11, 12 and 24 potently inhibited nitric oxide (NO) production in lipopolysaccharide (LPS)-activated BV-2 cells, a micro... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5383256 Tue, 08 Nov 2011 05:50:03 +0100 5383256 http://www.medworm.com/index.php?rid=5383255&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D22041086%26dopt%3DAbstract Authors: Yang Z, Yang Y, Yang X, Zhang Y, Zhao L, Xu L, Ding Z Abstract Three new sesquiterpenes were isolated from the fermentation broth of Streptomyces sp. and their structures were determined as caryolane-1,7α-diol (1), 1,6,11-eudesmanetriol; (1α,6β)-form (2), 11-eudesmene-1,6-diol; (1α,6β)-form (3), together with nine known compounds as caryolane-1,9α-diol (4), 2-methyl-5-nonanol (5), soyasaponin I (6), cyclo (Ala-Leu) (7), homononatinic acid (8), β-sitosteryl glucoside-3'-O-heptadecoicate (9), 2'-deoxythymidine (10), 2'-deoxyuridine (11), trehalose (12). The structures were elucidated by spectral analysis. PMID: 22041086 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5383255 Tue, 08 Nov 2011 05:50:03 +0100 5383255 http://www.medworm.com/index.php?rid=5284076&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21963628%26dopt%3DAbstract Authors: Hosseiny Davarani SS, Kalate Bojdi M, Mehdinia A Abstract Electrochemical oxidation of hydroquinone (1a) and 2,3-dimethylhydroquinone (1b) have been studied in the presence of 2-aminophenol (3a) and 2-amino-4-chlorophenol (3b), as nucleophiles in phosphate buffer solution (pH 7.2) using cyclic voltammetry and controlled potential coulometry. We proposed different mechanisms for the electrode process. The products were derived with good yield and purity using controlled-potential electrochemical oxidation of 1a, b in the presence of 3a and 3b at the graphite electrode in an undivided cell. PMID: 21963628 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5284076 Wed, 05 Oct 2011 12:10:02 +0100 5284076 http://www.medworm.com/index.php?rid=5284075&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21963629%26dopt%3DAbstract In this study, in order to address the problems with manufacturing orally rapidly disintegrating tablets (ODT) containing functional (taste masking or controlled release) coated particles, such as the low compactability of coated particles and the rupture of coated membrane during compression, a novel ODT containing taste-masked coated particles (TMP) in the center of the tablets were prepared using one-step dry-coated tablets (OSDrC) technology. As a reference, physical-mixture tablets (PM) were prepared by a conventional tableting method, and the properties of the tablets and the effect of compression on the characteristics of TMP were evaluated. OSDrC was found to have higher tensile strength and far lower friability than PM, but the oral disintegration time of OSDrC is slightly longer ... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5284075 Wed, 05 Oct 2011 12:10:02 +0100 5284075 http://www.medworm.com/index.php?rid=5284074&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21963630%26dopt%3DAbstract Authors: Fukuda M, Goto A Abstract A novel floating sustained release tablet having a cavity in the center was developed by utilizing the physicochemical properties of L-menthol and the penetration of molten hydrophobic polymer into tablets. A dry-coated tablet containing famotidine as a model drug in outer layer was prepared with a L-menthol core by direct compression. The tablet was placed in an oven at 80°C to remove the L-menthol core from tablet. The resulting tablet was then immersed in the molten hydrophobic polymers at 90°C. The buoyancy and drug release properties of tablets were investigated using United States Pharmacopeia (USP) 32 Apparatus 2 (paddle 100 rpm) and 900 ml of 0.01 N HCl. The L-menthol core in tablets disappeared completely through pathways in the outer l... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5284074 Wed, 05 Oct 2011 12:10:02 +0100 5284074 http://www.medworm.com/index.php?rid=5284073&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21963631%26dopt%3DAbstract In this study, a novel selenophene-based compound, 1,4-diselenophene-1,4-diketone (DSeD), has been synthesized by Double Friedel-Crafts reaction and identified as a potent antiproliferative agent against a panel of six human caner cell lines. Despite this potency, DSeD was relatively nontoxic toward human normal cells, HS68 fibroblasts and HK-2 kidney cells. These results suggest that DSeD possesses great selectivity between cancer and normal cells. Induction of apoptosis in human melanoma A375 cells by DSeD was evidenced by accumulation of sub-G1 cell population, DNA fragmentation and nuclear condensation. Activation of caspase-9 and depletion of mitochondrial membrane potential indicated the initiation of the mitochondria-mediated apoptosis pathway. Pretreatment of cells with general cas... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5284073 Wed, 05 Oct 2011 12:10:02 +0100 5284073 http://www.medworm.com/index.php?rid=5284072&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21963632%26dopt%3DAbstract In conclusion, 14c is a promising candidate for an efficacious and safe anti-diabetic drug with triple actions as a PPARα/γ dual agonist with PTP-1B inhibitory activity. PMID: 21963632 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5284072 Wed, 05 Oct 2011 12:10:02 +0100 5284072 http://www.medworm.com/index.php?rid=5284071&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21963633%26dopt%3DAbstract Authors: Nishida M, Yoshimitsu H Abstract Three new 15-hydroxy-trinor type (1-3), a new tetranor type (4), and two new 3,15,23,24-tetrahydroxy-16-oxo type cycloartane glycosides (5, 6) were isolated from the rhizome of Cimicifuga heracleifolia KOMAROV. Their structures were determined by the use of the 2D-NMR techniques and chemical evidence. PMID: 21963633 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5284071 Wed, 05 Oct 2011 12:10:02 +0100 5284071 http://www.medworm.com/index.php?rid=5284070&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21963634%26dopt%3DAbstract Authors: Chen XQ, Li Y, Li KZ, Peng LY, He J, Wang K, Pan ZH, Cheng X, Li MM, Zhao QS, Xu G Abstract Four new acylphloroglucinols with an unusual 6/6/5 spirocyclic skeleton, hyperbeanols A-D (1-4), were isolated from the methanol extract of Hypericum beanii along with 16 known compounds. Their structures were established on the basis of spectroscopic and X-ray diffraction analysis. Hyperbeanols A-C were three stereoisomers different only at the relative configuration of C-4 and C-13, which were distinguished by the nuclear Overhauser effect spectroscopy (NOESY) spectroscopic data in combination with the single X-ray analysis of hyperbeanol A (1). The cytotoxic activity of hyperbeanols A-D against the cancer cell lines SK-BR-3, HL-60, SMMC-7721, PANC-1, MCF-7, and K562 was also eval... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5284070 Wed, 05 Oct 2011 12:10:02 +0100 5284070 http://www.medworm.com/index.php?rid=5284069&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21963635%26dopt%3DAbstract In this study, 19 kinds of single amino substitutions were introduced at position 2 of this 9-mer WT1 peptide. We performed molecular dynamics simulation on the complex of each of WT1 epitope peptides and HLA-β2 micro globulin (β2m) molecule, and subsequently estimated the binding affinity using molecular mechanics/generalized-Born surface area method combined with normal mode analysis. Our computation indicated that the peptide containing M2Y or M2W mutation showed high binding affinity to the HLA-β2m molecule as well as the natural peptide. We have also examined the role of the residue at position 2 in peptide binding to HLA-β2m. The calculation showed that van der Waals interaction between the side chain of the residue at position 2 and hydrophobic residues inside B-pocket of HLA ar... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5284069 Wed, 05 Oct 2011 12:10:02 +0100 5284069 http://www.medworm.com/index.php?rid=5284068&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21963636%26dopt%3DAbstract In conclusion, the present in vivo and in silico studies suggest that the instilled drugs initially reached the posterior vitreous body by diffusion through the sclera and then later by corneal penetration and systemic circulation. PMID: 21963636 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5284068 Wed, 05 Oct 2011 12:10:02 +0100 5284068 http://www.medworm.com/index.php?rid=5284067&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21963637%26dopt%3DAbstract Authors: Ogino M, Fukui S, Nakada Y, Tokunoh R, Itokawa S, Kakoi Y, Nishimura S, Sanada T, Fuse H, Kubo K, Wada T, Marui S Abstract Acyl-CoA: cholesterol acyltransferase (ACAT) is an intracellular enzyme that catalyzes cholesterol esterification. ACAT inhibitors are expected to be potent therapeutic agents for the treatment of atherosclerosis. A series of potent ACAT inhibitors based on an (4-phenylcoumarin)acetanilide scaffold was identified. Evaluation of the structure-activity relationships of a substituent on this scaffold, with an emphasis on improving the pharmacokinetic profile led to the discovery of 2-[7-chloro-4-(3-chlorophenyl)-6-methyl-2-oxo-2H-chromen-3-yl]-N-[4-chloro-2-(trifluoromethyl)phenyl]acetamide (23), which exhibited potent ACAT inhibitory activity (IC(50)=12 ... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5284067 Wed, 05 Oct 2011 12:10:02 +0100 5284067 http://www.medworm.com/index.php?rid=5284066&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21963638%26dopt%3DAbstract Authors: Matsunami K, Otsuka H, Takeda Y Abstract Chemical investigation of the 1-BuOH soluble fraction of the dried fruits of Myrsine seguinii (Myrsinaceae) led to the isolation of five new glycosides, named myrseguinosides A-E (1-5), together with eight known compounds (6-13). The absolute structures of the new glycosides were elucidated by spectroscopic and chemical analyses to be a monoterpene glucoside (1), two flavonol glycosides (2, 3), and two oleanane-type triterpene saponins (4, 5). Myrseguinosides B (2), D (4), and E (5) exhibited 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical-scavenging activity and growth inhibitory activity toward human cancer cells, respectively. PMID: 21963638 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5284066 Wed, 05 Oct 2011 12:10:02 +0100 5284066 http://www.medworm.com/index.php?rid=5284065&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21963639%26dopt%3DAbstract Authors: Kim SY, Kashiwada Y, Kawazoe K, Murakami K, Sun HD, Li SL, Takaishi Y Abstract Four new lindenane sesquiterpenoid dimers, spicachlorantins G-J (1-4), were isolated from the roots of Chloranthus spicatus together with seven known compounds, including chloramultilide A, shizukaol B, shizukaol D, shizukaol F, shizukaol P, chlorahololide D, and cycloshizukaol A. The planar structures of the new compounds were established by 1D-, 2D-NMR, and MS analyses. The absolute configurations of these compounds were determined by analyzing rotating Overhauser enhancement and exchange spectroscopy (ROESY) and circular dichroism (CD) spectra. PMID: 21963639 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5284065 Wed, 05 Oct 2011 12:10:02 +0100 5284065 http://www.medworm.com/index.php?rid=5284064&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21963640%26dopt%3DAbstract Authors: Thanigaimalai P, Lee KC, Sharma VK, Sharma N, Roh E, Kim Y, Jung SH Abstract Based on the hits, 3,4-dihydroquinazoline-2-thione (1) and benzimidazole-2-thione (2), a series of indole-2-thione (3) and indole-2-thiol inhibitors (4) of melanogenesis were designed, synthesized and evaluated in melanoma B16 cells under the stimulant of α-melanocyte stimulating hormone (α-MSH). The indole-2-thione compounds (3a-g) exhibited an effective inhibitory activity on melanin synthesis. The Structure-Activity Relationship (SAR) studies of 2 have revealed that in potent inhibitor 3a (>100% inhibition at 30 µM, IC(50)=1.40 µM) the role of nitrogen (3-N) at 3-position is insignificance. In addition, the hydrophobic substituents of 3 were better than the hydrophilic one. However, conv... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5284064 Wed, 05 Oct 2011 12:10:02 +0100 5284064 http://www.medworm.com/index.php?rid=5284063&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21963641%26dopt%3DAbstract Authors: Yamashita M, Ueda K, Sakaguchi K, Tokuda H, Iida A Abstract In this paper, a concise one-pot method for the construction of benzo[f]indole-4,9-dione motifs is described. These transformations proceed via a sequential palladium- and copper-catalyzed coupling reaction of 1,4-naphthoquinones with terminal acetylenes, followed by a copper-catalyzed intramolecular cyclization reaction of the resulting coupling product. PMID: 21963641 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5284063 Wed, 05 Oct 2011 12:10:02 +0100 5284063 http://www.medworm.com/index.php?rid=5284062&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21963642%26dopt%3DAbstract Authors: Ayyad SE, Al-Footy KO, Alarif WM, Sobahi TR, Bassaif SA, Makki MS, Asiri AM, Al Halawani AY, Badria AF, Badria FA Abstract The petroleum ether extract of the red alga Laurencia obtusa afforded three new C(15) acetogenins (cyclic ether enyne): (12Z)-cis-maneonene-D (1), (12E)-cis-maneonene-E (2), and (12Z)-trans-maneonene-C (3), along with one known cis-maneonene-A (4). Blood neutrophils were prepared, cultured, and incubated for 24, 48, and 72 h in medium with and without isolated compounds. Blood neutrophils were prepared, cultured, and incubated for 24, 48 and 72 h in medium with and without the isolated compounds. Both morphology and DNA fragmentation methods assessed the percentage of neutrophils apoptosis in each culture. In the present study, several observations hav... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5284062 Wed, 05 Oct 2011 12:10:02 +0100 5284062 http://www.medworm.com/index.php?rid=5284061&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21963643%26dopt%3DAbstract Authors: Inoue Y, Hasegawa N, Tozuka Y, Yonemochi E, Oguchi T, Higashi K, Moribe K, Yamamoto K Abstract Changes in molecular states of p-dimethylaminobenzonitrile (DMABN) coground with β-cyclodextrin (β-CD) were examined using solid-state fluorescence measurements. Formation of a DMABN/β-CD inclusion complex by coprecipitation was confirmed by powder X-ray diffraction measurement. The powder X-ray diffraction pattern of the ground mixture was a halo pattern and differed from the pattern of the mixture prepared by coprecipitation. Solid-state fluorescence measurements revealed emission by DMABN crystals in a twisted intermolecular charge-transfer state at 473 nm. DMABN in the DMABN/β-CD coprecipitate had a fluorescence emission peak at 393 nm due to its planar structure. In cont... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5284061 Wed, 05 Oct 2011 12:10:02 +0100 5284061 http://www.medworm.com/index.php?rid=5284060&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21963644%26dopt%3DAbstract Authors: Kurimoto S, Kashiwada Y, Morris-Natschke SL, Lee KH, Takaishi Y Abstract Three new steroids dyscusins A-C (1-3), including a stigmastane-type sterol and two pregnanes, together with two known steroids were isolated from the leaves of Dysoxylum cumingianum (Meliaceae). Their structures were elucidated on the basis of extensive spectroscopic analyses. In a cytotoxicity assay, compound 1 showed ten-fold enhanced cytotoxicity against multi-drug resistant cancer cells (KB-C2) in the presence of 2.5 µM colchicine as compared with the absence of colchicine. This notable finding indicated that 1 possessed a multi-drug resistant reversal effect. PMID: 21963644 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5284060 Wed, 05 Oct 2011 12:10:02 +0100 5284060 http://www.medworm.com/index.php?rid=5284059&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21963645%26dopt%3DAbstract Authors: Nishiyama K, Yamada A, Takeuchi T, Arata Y, Kasai K, Oshitari T, Natsugari H, Takahashi H Abstract Useful segments (1, 2) for chemical probes embedded in a Galβ1→4Fuc unit were designed and prepared for characterizing sugar-binding proteins in Caenorhabditis elegans. Segment 1 with an amino group terminus was used as a recognition unit in affinity chromatography. It was revealed that some proteins (annexins and galectins) in C. elegans have an affinity for Galβ1→4Fuc. PMID: 21963645 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5284059 Wed, 05 Oct 2011 12:10:02 +0100 5284059 http://www.medworm.com/index.php?rid=5284058&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21963646%26dopt%3DAbstract Authors: Trianto A, Hermawan I, de Voogd NJ, Tanaka J Abstract Chemical investigations on a sponge Haliclona sp. found a meroditerpene 1 having a new carbon skeleton. By analyzing spectroscopic data, the structure was elucidated to comprise a substituted hydroquinone, a tetrahydrooxepine, and a cyclohexene, and these components were united with C1 and C2 units. Compound 1 showed moderate cytotoxicity against NBT-T2 cells with IC(50) 4.8 µg/ml and also antioxidant activity against 1,1-diphenyl-2-picrylhydrazyl (DPPH) with IC(50) 3.2 µg/ml. PMID: 21963646 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5284058 Wed, 05 Oct 2011 12:10:02 +0100 5284058 http://www.medworm.com/index.php?rid=5284057&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21963647%26dopt%3DAbstract Authors: Demizu Y, Wakana D, Kamakura H, Kurihara M, Okuda H, Goda Y Abstract We isolated a new illegal sildenafil analogue named mutaprodenafil from a dietary supplement for erectile dysfunction (ED) and proposed that it is an aildenafil derivative containing an imidazole moiety. We subsequently synthesized mutaprodenafil from a thioaildenafil and authenticated its structure. PMID: 21963647 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5284057 Wed, 05 Oct 2011 12:10:02 +0100 5284057 http://www.medworm.com/index.php?rid=5195541&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21881248%26dopt%3DAbstract Authors: Yejella RP, Atla SR Abstract Chalcone derivatives (3a-m) were prepared by condensing 4-aminoacetophenone with various substituted aromatic and hetero aromatic aldehydes according to Claisen-Schmidt condensation. These chalcones, on reaction with guanidine hydrochloride under basic alcoholic conditions gave 2,4,6-trisubstituted pyrimidines (5a-m) in quantitative yields. All the newly synthesized pyrimidines were characterized by means of IR, (1)H- and (13)C-NMR, Electron Ionization (EI)-mass and elemental analyses and screened for anti-inflammatory and analgesic activities by in vivo. 2-Amino-4-(4-aminophenyl)-6-(2,4-dichlorophenyl)pyrimidine (5b) and 2-amino-4-(4-aminophenyl)-6-(3-bromophenyl) pyrimidine (5d) were found to be the most potent anti-inflammatory and analgesic... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5195541 Tue, 06 Sep 2011 01:28:03 +0100 5195541 http://www.medworm.com/index.php?rid=5195540&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21881249%26dopt%3DAbstract Authors: Ku WS, Cho HJ, Yoon IS, Kim JH, Cha BJ, Kim JS, Kim KM, Kang SK, Chung SJ, Shim CK, Kim DD Abstract A rapid and sensitive analytical method for udenafil in rat plasma was developed and validated using liquid chromatography-tandem mass spectrometry (LC-MS/MS). This chromatographic procedure was then applied to the in vivo pharmacokinetic studies in rats for determining the advantages of intranasal administration of the drug over oral administration. Using liquid-liquid extraction (LLE), udenafil and the internal standard (IS) sildenafil were extracted with dichloromethane from 100 μl of plasma samples. Chromatographic separation was performed using Pursuit XRS C(18) column (50 mm×2.1 mm, i.d., 3 μm, Varian Inc., CA, U.S.A.) with an isocratic mobile phase consisting of ac... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5195540 Tue, 06 Sep 2011 01:28:03 +0100 5195540 http://www.medworm.com/index.php?rid=5195539&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21881250%26dopt%3DAbstract Authors: de Regil-Hernández R, Martínez-Lagos F, Rodríguez-Bayón A, Sinisterra JV Abstract Different green synthesis of alkyl esters of acyclovir (acyclovir prodrugs) is described. Hexanoic, decanoic, dodecanoic and tetradecanoic acyclovir esters were synthesized reacting acyclovir and the respective acid anhydride in dimethyl sulfoxide (DMSO), in solvents from renewable sources and without solvent (T=30°C). Yields in prodrugs after 10 min of reaction were >95% using DMSO as solvent. The purification methodology was very simple, shorter and greener than previously described. The biosolvent, N,N-dimethylamide of decanoic acid, let us to obtain >95% yield at 24 h. This oily biosolvent is not dermotoxic and the reaction crude can directly be used in topic formulations. Synt... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5195539 Tue, 06 Sep 2011 01:28:03 +0100 5195539 http://www.medworm.com/index.php?rid=5195538&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21881251%26dopt%3DAbstract Authors: Liang W, Gong H, Yin D, Lu S, Fu Q Abstract In order to enhance the gene delivery efficiency and decrease cytotoxicity of polyplexes, copolymers consisting of branched polyethyleneimine (PEI) 25 kDa grafted with Pluronic (F127, F68, P105) were successfully synthesized using a simple two-step procedure. The copolymers were tested for cytotoxicity and DNA condensation and complexation properties. Their polyplexes with plasmid DNA were characterized in terms of DNA size and surface charge and transfection efficiency. The complex sizes were below 300 nm, which implicated their potential for intracellular delivery. The Pluronic-g-PEI exhibited better condensation and complexation properties than PEI 25 kDa. The cytotoxicity of PEI was strongly reduced after copolymerization. Th... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5195538 Tue, 06 Sep 2011 01:28:03 +0100 5195538 http://www.medworm.com/index.php?rid=5195537&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21881252%26dopt%3DAbstract Authors: Yang LB, Li L, Huang SX, Pu JX, Zhao Y, Ma YB, Chen JJ, Leng CH, Tao ZM, Sun HD Abstract Four new diterpenoides, isolophanthins A-D (1-4) together with seven known abietane diterpenoides (5-11), have been isolated from Isodon lophanthoides var. gerardianus. The new diterpenoides were elucidated by spectroscopic analysis. Some of them showed significant activities against HBsAg and HBeAg of hepatitis B virus in Hep G 2.2.15 cells, as well as the human tumor cell lines, HL-60, A-549, MOLT-4, and BEL-7402. PMID: 21881252 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5195537 Tue, 06 Sep 2011 01:28:03 +0100 5195537 http://www.medworm.com/index.php?rid=5195536&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21881253%26dopt%3DAbstract In this study, we investigated the effects of glycyrrhiza on the activity of sennoside A metabolism in intestinal bacteria using mouse feces. A high-performance liquid chromatography (HPLC) method for the determination of sennoside A in incubation mixture of DKT with mouse feces was established. The retention time of sennoside A was 9.26±0.02 min with a TSKgel ODS-80TsQA column by linear gradient elution using a mobile phase containing aqueous phosphoric acid and acetonitrile and detection at 265 nm. We found that the activity of sennoside A metabolism in intestinal bacteria was significantly accelerated when glycyrrhiza, liquiritin or liquiritin apioside coexisted with sennoside A, whereas that of glycyrrhizin was not altered. This method is applicable for determination of the activity o... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5195536 Tue, 06 Sep 2011 01:28:03 +0100 5195536 http://www.medworm.com/index.php?rid=5195535&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21881254%26dopt%3DAbstract In conclusion, the impact of log P and pK(a) on hERG inhibition was clarified relatively and quantitatively. The quantitative risk assessment established based on both parameters, was considered to be a practical and useful tool in avoiding hERG inhibition and in the rational drug design for drug discovery, especially in lead optimization. Moreover, we also carried out a trend analysis using a different derivative and demonstrated that both parameters were equally significant for hERG inhibition. PMID: 21881254 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5195535 Tue, 06 Sep 2011 01:28:03 +0100 5195535 http://www.medworm.com/index.php?rid=5195534&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21881255%26dopt%3DAbstract Authors: Hafner A, Dürrigl M, Pepić I, Filipović-Grčić J Abstract The aim of this study was to establish a freeze-drying process for melatonin-loaded lecithin/chitosan nanoparticles (NPs) to preserve their chemical and physical stability for a longer time period that what is possible in an aqueous suspension. Glucose and trehalose were investigated as potential excipients during freeze-drying of NP suspensions. Lecithin/chitosan NPs were characterised by mean diameter and zeta potential, ranging between 117.4 and 328.5 nm and 6.7 and 30.2 mV, respectively, depending on the lecithin type and chitosan content in the preparation. Melatonin loadings were up to 7.1%. For all lecithin/chitosan NPs, no notable differences in the mean particle size, size distribution, zeta potential o... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5195534 Tue, 06 Sep 2011 01:28:03 +0100 5195534 http://www.medworm.com/index.php?rid=5195533&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21881256%26dopt%3DAbstract Authors: Abou-Seri SM, Farag NA, Hassan GS Abstract Several hybrid molecules of diphenylamine-2,4'-dicarboxamide with various azolidinones and related heterocyclic rings have been synthesized and explored as epidermal growth factor receptor (EGFR) kinase inhibitors. Most of them displayed promising in vitro tyrosine kinase inhibition as well as potent cellular antiproliferative activity in the EGFR over-expressing breast cancer cell line (MCF-7). Compounds 12b and 13b that exhibited the highest inhibition in the kinase assay (89, 81% inhibition at 10 μM, respectively), showed potent antiproliferative effect against MCF-7 tumor cell line (IC(50) 1.04, 0.91 μM respectively). Molecular docking studies revealed that these compounds can bind to ATP binding site of the EGFR kinase doma... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5195533 Tue, 06 Sep 2011 01:28:03 +0100 5195533 http://www.medworm.com/index.php?rid=5195532&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21881257%26dopt%3DAbstract Authors: Ohta K, Koketsu E, Nagase Y, Takahashi N, Watanabe H, Yoshimatsu M Abstract Direct scandium- and lanthanum-catalyzed etherifications of propargyl alcohols 1 and 6 in MeNO(2)-H(2)O provided propargyl ethers 3, 4 and 7 in high yields. In addition, reactions of 1 and 6 with thiols exclusively yielded the corresponding propargyl sulfides. PMID: 21881257 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5195532 Tue, 06 Sep 2011 01:28:03 +0100 5195532 http://www.medworm.com/index.php?rid=5195531&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21881258%26dopt%3DAbstract Authors: Nakano T, Sugimoto S, Matsunami K, Otsuka H Abstract From aerial parts of Dianthus japonicus, six new and seven known oleanane-type triterpene saponins were isolated. The structures of the new saponins, named dianthosaponins A-F, were elucidated by means of high resolution mass spectrometry, and extensive inspection of one- and two-dimensional NMR spectroscopic data. A new C-glycosyl flavone, a glycosidic derivative of anthranilic acid amide and a maltol glucoside were also isolated. PMID: 21881258 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5195531 Tue, 06 Sep 2011 01:28:03 +0100 5195531 http://www.medworm.com/index.php?rid=5195530&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21881259%26dopt%3DAbstract Authors: Adibi H, Rashidi A, Khodaei MM, Alizadeh A, Majnooni MB, Pakravan N, Abiri R, Nematollahi D Abstract In this research, synthesis, antimicrobial and antioxidant activities of a series of catecholthioethers having benzoxazole and tetrazole moieties are described. Antimicrobial activity was evaluated by minimum inhibitory concentration (MIC) assay. The synthesized compounds were tested in vitro against three Gram-positive bacteria including Staphylococcus aureus (clinical isolated), Staphylococcus aureus ATCC 25922, Enterococcus faecium (clinical isolated), and two Gram-negative bacteria including Klebsiella pneumoniae (clinical isolated) and Pseudomonas aeruginosa 27853 and the yeast Candida albicans in comparison with control drugs. Microbiological results indicated that th... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5195530 Tue, 06 Sep 2011 01:28:03 +0100 5195530 http://www.medworm.com/index.php?rid=5195529&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21881260%26dopt%3DAbstract Authors: Subudhi BB, Sahoo SP Abstract A new series of novel (2S)-2-({2-[1,4-dihydro-3,5-bis(methoxycarbonyl)-2,6-dimethyl-4-(2-nitrophenyl)pyridin-1-yl]-2-oxoethyl}amino)-3-(4-hydroxyphenyl) propanoic acid (3a) and its analogues 3b-j has been synthesized. These compounds were evaluated for their in vitro antioxidant activity, anti-inflammatory activity and antiulcer activity. Compounds 3b and f exhibited significant antioxidant action comparable with that of standard. Efficacy against inflammation and ulceration was also found to be significant. The chemical structures of these compounds were confirmed on the basis of spectral data. PMID: 21881260 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5195529 Tue, 06 Sep 2011 01:28:03 +0100 5195529 http://www.medworm.com/index.php?rid=5195528&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21881261%26dopt%3DAbstract Authors: Isaka M, Palasarn S, Prathumpai W, Laksanacharoen P Abstract Two new pimarane-type diterpenes, eutypellones A (1) and B (2), were isolated from the endophytic fungus Eutypella sp. BCC 13199. Cytotoxic activities of the pimaranes 1-5, isolated from this fungus, were evaluated. PMID: 21881261 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5195528 Tue, 06 Sep 2011 01:28:03 +0100 5195528 http://www.medworm.com/index.php?rid=5195527&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21881262%26dopt%3DAbstract Authors: Sahakitpichan P, Disadee W, Ruchirawat S, Kanchanapoom T Abstract A new 3-hydroxydihydrobenzofuran glucoside, gnaphaliol 9-O-β-D-glucopyranoside (2), was isolated from the aerial parts of Gnaphalium polycaulon together with 1-{(2R(*),3S(*))-3-(β-D-glucopyranosyloxy)-2,3-dihydro-2-[1-(hydroxyl methyl)vinyl]-1-benzofuran-5-yl}-ethanone or gnaphaliol 3-O-β-D-glucopyranoside (1), (Z)-3-hexenyl O-β-D-glucopyranoside (3) and adenosine (4). The absolute configurations at C-2 and C-3 positions of compound 1 were determined to be 2R and 3R. The structures of these compounds were elucidated on the basis of their physical and spectroscopic data. PMID: 21881262 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5195527 Tue, 06 Sep 2011 01:28:03 +0100 5195527 http://www.medworm.com/index.php?rid=5195526&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21881263%26dopt%3DAbstract Authors: Takigawa A, Setoguchi H, Okawa M, Kinjo J, Miyashita H, Yokomizo K, Yoshimitsu H, Nohara T, Ono M Abstract Alkaline hydrolysis of the crude resin glycoside fraction of the leaves, stems, and roots of Calystegia soldanella ROEM. et SCHULT. (Convolvulaceae) gave four new glycosidic acids, named calysolic acids A, B, C, and D, along with one known glycosidic acid, soldanellic acid B, and three organic acids, 2S-methylbutyric, tiglic, and 2S,3S-nilic acids. The structures of the new glycosidic acids were characterized on the basis of spectroscopic data and chemical evidence. PMID: 21881263 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5195526 Tue, 06 Sep 2011 01:28:03 +0100 5195526 http://www.medworm.com/index.php?rid=5195525&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21881264%26dopt%3DAbstract Authors: Van HT, Khadka DB, Le TN, Yang SH, Cho WJ Abstract Cycloaddition reaction between toluamides and benzonitriles was applied to prepare the 3-arylisoquinolines, and their chemical transformation to the dienes 4 was performed. The ring-closing metathesis (RCM) reaction afforded the desired heterocyclic compounds, benzo[3,4]azepino[1,2-b]isoquinolinones 5 in good yield. PMID: 21881264 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5195525 Tue, 06 Sep 2011 01:28:03 +0100 5195525 http://www.medworm.com/index.php?rid=5195524&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21881265%26dopt%3DAbstract Authors: Yang G, Sandjo L, Yun K, Leutou AS, Kim GD, Choi HD, Kang JS, Hong J, Son BW Abstract Flavusides A (1) and B (2), two new antibacterial cerebroside derivatives, and the previously described phomaligol A (3), kojic acid (4), methyl kojic acid (5), and dimethyl kojic acid (6) have been isolated from the extract of a marine isolate of the fungus Aspergillus flavus. The structure and absolute stereochemistry of two cerebrosides were assigned on the basis of NMR and Tandem FAB-MS/MS experiments. Compounds 1, 2, and 3 exhibited a mild antibacterial activity against Staphylococcus aureus, methicillin-resistant S. aureus, and multidrug-resistant S. aureus. The minimum inhibitory concentration (MIC) values for each strain are as follows: compounds 1 and 2 showed 15.6 μg/ml for S. ... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5195524 Tue, 06 Sep 2011 01:28:03 +0100 5195524 http://www.medworm.com/index.php?rid=5195523&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21881266%26dopt%3DAbstract Authors: Bokesch HR, Gardella RS, Rabe DC, Bottaro DP, Linehan WM, McMahon JB, McKee TC Abstract A new trimethoxycinnamoyl-2-pyrrolinone alkaloid, langkamide (1), along with the known compounds piplartine (2) and 3,4,5-trimethoxycinnamic acid (3) were isolated from the roots and stems of the shrub Piper sarmentosum ROXB. The structures were established by spectroscopic analyses and comparison of their spectral data with values reported in the literature. The compounds were tested for their ability to modulate hypoxia inducible factor-2 (HIF-2) transcription activity and all three showed HIF-2 inhibitory activity with EC(50) values of 14.0, 4.8, and 60.6 μM, respectively, for compounds 1, 2, and 3. PMID: 21881266 [PubMed - in process] (Source: Chemical and Pharmaceutical Bullet... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5195523 Tue, 06 Sep 2011 01:28:03 +0100 5195523 http://www.medworm.com/index.php?rid=5195522&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21881267%26dopt%3DAbstract Authors: Fu SB, Yang JS, Cui JL, Feng X, Sun DA Abstract Endophytic fungi were used not only for their producing bioactive products but also for their ability to transform natural compounds. An endophytic fungus, isolated from medicinal plant Huperzia serrata, was identified as Umbelopsis isabellina based on the internal transcribed spacer of ribosomal DNA (rDNA-ITS) region. It was used to transform ursolic acid (1), a pentacyclic triterpene. Incubation of ursolic acid with U. isabellina afforded three products, 3β-hydroxy-urs-11-en-28,13-lactone (2), 3β,7β-dihydroxy-urs-11-en-28,13-lactone (3), 1β,3β-dihydroxy-urs-11-en-28,13-lactone (4). Although product 2 was a known compound, it was first obtained by microbial transformation. Products 3 and 4 were new compounds. The struct... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5195522 Tue, 06 Sep 2011 01:28:03 +0100 5195522 http://www.medworm.com/index.php?rid=5195521&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21881268%26dopt%3DAbstract Authors: Shii T, Miyamoto M, Matsuo Y, Tanaka T, Kouno I Abstract Chromatographic separation of black tea polyphenols is too difficult to supply sufficient quantities of pure compounds for biological experiments. Thus, facile methods to prepare black tea constituents were desired. Treatment of epigallocatechin gallate with copper(II) chloride efficiently afforded an unstable quinone dimer, dehydrotheasinensin A, and subsequent treatment with ascorbic acid stereoselectively yielded theasinensin A. The latter is a dimer with an R-biphenyl bond, one of the major polyphenols found in black tea. The method is simpler and more effective than enzymatic preparation. PMID: 21881268 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5195521 Tue, 06 Sep 2011 01:28:03 +0100 5195521 http://www.medworm.com/index.php?rid=5195520&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21881269%26dopt%3DAbstract Authors: Song YX, Cheng B, Zhu X, Qiao LT, Wang JJ, Gu YC, Li MF, Liu L, Lin YC Abstract Nine new derivatives (6-14) of the eremophilane sesquiterpene 07H239-A (5) were designed and semisynthesized with two types of R-groups by amidation. Most of them were active against five human tumor cell lines, and compounds 6-10 were more potent than the natural product 5. In particular, compounds 6 and 9 exhibited the strongest cytotoxic activity against MDA-MB-435 with IC(50) values of 0.91 and 0.96 μM, respectively. Preliminary structure-activity relationships (SARs) analysis indicated that the 14-carboxyl in 5 was an ideal target for chemical modification, and the side chain of 5 might play a necessary role in facilitating their cytotoxic potencies. PMID: 21881269 [PubMed - in proces... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5195520 Tue, 06 Sep 2011 01:28:03 +0100 5195520 http://www.medworm.com/index.php?rid=5195519&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21881270%26dopt%3DAbstract We describe here a Tf(2)NH-catalyzed formal (3+3) cycloaddition of silyl enol ethers with acrylates as a new domino reaction. In the domino sequence, the catalyst activates Michael addition, deprotonation of the resulting silyloxonium cation and intramolecular Claisen condensation. It was found that reaction modes significantly depend on the reaction temperature. We also examined the mechanistic detail of the reaction by (1)H-NMR experiment. PMID: 21881270 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5195519 Tue, 06 Sep 2011 01:28:03 +0100 5195519 http://www.medworm.com/index.php?rid=5195518&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21881271%26dopt%3DAbstract Authors: Li F, He YM, Awale S, Kadota S, Tezuka Y Abstract Two new phenylallylflavanones, (2R,3R)-6-[1-(4'-hydroxy-3'-methoxyphenyl)prop-2-en-1-yl]pinobanksin (1) and (2R,3R)-6-[1-(4'-hydroxy-3'-methoxyphenyl)prop-2-en-1-yl]pinobanksin 3-acetate (2) were isolated from a methanolic extract of Mexican propolis. Their structures were elucidated with spectroscopic analysis. Both compounds (1, 2) exhibited preferential cytotoxic activity against PANC-1 human pancreatic cancer cells in a nutrient-deprived medium with the concentration at which 50% cells died preferentially in NDM (PC(50)) values of 17.9 μM and 9.1 μM, respectively. PMID: 21881271 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5195518 Tue, 06 Sep 2011 01:28:03 +0100 5195518 http://www.medworm.com/index.php?rid=5195517&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21881272%26dopt%3DAbstract Authors: Numao N, Fukazawa Y, Tanaka K Abstract Mulliken's electronegativity (M) scale was found as a parameterization to predict (elucidate) a virtually specific interaction between Poliovirus proteinase 2A and mitogen-activated protein (MAP) kinase p38α, as well as that between the 2A and apoptotic protein activating factor 1c (Apaf 1c) (or prion) with intermolecular frequency symmetry (IFS) rule. Also, Lacey's hydropathical (H) scale and Garel's (G) one could be found in the specific relationship between the 2A and the extracellular signal-regulated kinase 2 (ERK2) [or fibroblast growth factor receptor 3 (FGFR3)], and that between the 2A and the c-Jun N-terminal kinase 2 (JNK2) [or forkhead box P2-1 (FOXP2-1)], respectively. Based on these, both the same physicochemical scale a... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5195517 Tue, 06 Sep 2011 01:28:03 +0100 5195517 http://www.medworm.com/index.php?rid=5195516&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21881273%26dopt%3DAbstract Authors: Kondo S, Yamamoto K, Sawama Y, Sasai Y, Yamauchi Y, Kuzuya M Abstract We fabricated novel pH-sensitive polymeric micelles consisting of amphiphilic block copolymer containing pyridyl groups as side chains in the hydrophobic block. The number average particle diameter of the polymeric micelles at pH 7 was approximately 200 nm. A decrease in pH resulted in deformation of the polymeric micelles over a very narrow pH range (between pH 5.7 and 5.6). Interestingly, micellization and demicellization occurred reversibly in this narrow pH range. Polymeric micelles incorporating 5-fluorouracil (5FU) were also prepared. Decreasing the pH of this polymeric micelle solution from 7 to 5.5 resulted in the rapid release of 5FU at pH 5.6; the drug was completely released within 30 min. The... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5195516 Tue, 06 Sep 2011 01:28:03 +0100 5195516 http://www.medworm.com/index.php?rid=5195515&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21881274%26dopt%3DAbstract Authors: Uchiyama N, Kikura-Hanajiri R, Goda Y Abstract A new cannabimimetic phenylacetylindole (cannabipiperidiethanone, 1) has been found as an adulterant in a herbal product which contains two other known synthetic cannabinoids, JWH-122 and JWH-081, and which is distributed illegally in Japan. The identification was based on analyses using GC-MS, LC-MS, high-resolution MS and NMR. Accurate mass spectrum measurement showed the protonated molecular ion peak of 1 at m/z 377.2233 [M+H](+) and the molecular formula of 1 was C(24)H(29)N(2)O(2). Both mass and NMR spectrometric data revealed that 1 was 2-(2-methoxyphenyl)-1-{1-[(1-methylpiperidin-2-yl)methyl]-1H-indol-3-yl}ethanone. Compound 1 has a mixed structure of known cannabimimetic compounds: JWH-250 and AM-2233. Namely, the moie... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5195515 Tue, 06 Sep 2011 01:28:03 +0100 5195515 http://www.medworm.com/index.php?rid=5195514&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21881275%26dopt%3DAbstract Authors: Ueda M, Sugita S, Aoi N, Sato A, Ikeda Y, Ito Y, Miyoshi T, Naito T, Miyata O Abstract The synthetic utility of N-alkoxyimidoyl halides is demonstrated using the palladium-catalyzed cross-coupling reaction. The Sonogashira and Suzuki-Miyaura coupling reactions of N-alkoxyimidoyl bromides produced versatile ketoxime ethers in good to excellent yields. A one-pot reaction of the imidoyl bromides with arylboronic acid and allylmagnesium bromide to produce N-arylamines via Suzuki-Miyaura coupling followed by domino reaction involving sequential addition-eliminative rearrangement-addition reactions was developed. PMID: 21881275 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5195514 Tue, 06 Sep 2011 01:28:03 +0100 5195514 http://www.medworm.com/index.php?rid=5111236&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21804233%26dopt%3DAbstract Authors: Mahendran S, Badami S, Ravi S, Thippeswamy BS, Veerapur VP Antioxidant and related properties of the plant Embelia ribes and embelin are well known. In the present study embelin was condensed with various aromatic substituted primary amines to yield ten new and one reported derivatives along with monomethyl embelin. All these compounds along with embelin were evaluated for in vitro antioxidant activity using 2,2'-azino-bis(3-ethylbenzo-thiazoline-6-sulfonic acid) diammonium salt (ABTS) and 2,2'-diphenyl-1-picryl hydrazyl (DPPH) methods. Two para-substituted embelin derivatives showed potent antioxidant activity. These compounds along with embelin were studied for analgesic and anti-inflammatory activities at 10 and 20 mg/kg doses by standard methods. Potent analgesic activity ... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5111236 Wed, 10 Aug 2011 20:30:06 +0100 5111236 http://www.medworm.com/index.php?rid=5111235&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21804234%26dopt%3DAbstract Authors: Sheshala R, Khan N, Darwis Y The aims of the present research were to mask the intensely bitter taste of sumatriptan succinate and to formulate orally disintegrating tablets (ODTs) of the taste masked drug. Taste masking was performed by coating sumatriptan succinate with Eudragit EPO using spray drying technique. The resultant microspheres were evaluated for thermal analysis, yield, particle size, entrapment efficiency and in vitro taste masking. The tablets were formulated by mixing the taste masked microspheres with different types and concentrations of superdisintegrants and compressed using direct compression method followed by sublimation technique. The prepared tablets were evaluated for weight variation, thickness, hardness, friability, drug content, water content, in ... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5111235 Wed, 10 Aug 2011 20:30:06 +0100 5111235 http://www.medworm.com/index.php?rid=5111234&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21804235%26dopt%3DAbstract In conclusion, optimization of the aerosolization properties of inhalation dry powders could be achieved by appropriately selecting the composition of the particles. PMID: 21804235 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5111234 Wed, 10 Aug 2011 20:30:06 +0100 5111234 http://www.medworm.com/index.php?rid=5111233&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21804236%26dopt%3DAbstract Authors: Yamamoto Y, Toyohara J, Ishiwata K, Sano K, Yamamoto F, Mukai T, Maeda M There is great potential in the use of positron emission tomography (PET) and suitable radiotracers for the study of cyclooxygenase type 2 (COX-2) enzyme in living subjects. In the present study, we prepared and evaluated five (11)C-labeled ester and amide analogs derived from indomethacin as potential PET imaging agents for the in vivo visualization of the brain COX-2 enzyme. Five (11)C-labeled COX-2 inhibitors, with different lipophilicities and moderate COX-2 inhibitory activity, were prepared by treatment of the corresponding O-desmethyl precursors with [(11)C]methyl triflate and purified by HPLC (radiochemical yields of 55-71%, radiochemical purity of >93%, and the specific activities of 22-331 GB... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5111233 Wed, 10 Aug 2011 20:30:06 +0100 5111233 http://www.medworm.com/index.php?rid=5111232&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21804237%26dopt%3DAbstract Authors: Itoh A, Saitoh T, Tani K, Uchigaki M, Sugimoto Y, Yamada J, Nakajima H, Ohshiro H, Sun S, Tanahashi T From the embryos of the seeds of Nelumbo nucifera, three bisbenzylisoquinoline alkaloids, nelumboferine and nelumborines A and B, were isolated along with four known compounds, neferine, liensinine, isoliensinine and anisic acid. The structures of the new alkaloids were determined mainly by spectroscopic methods. PMID: 21804237 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5111232 Wed, 10 Aug 2011 20:30:06 +0100 5111232 http://www.medworm.com/index.php?rid=5111231&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21804238%26dopt%3DAbstract Authors: Baloglu E, Ay Senyıgıt Z, Karavana SY, Vetter A, Metın DY, Hilmioglu Polat S, Guneri T, Bernkop-Schnurch A The main objective of this work was to develop antifungal matrix tablet for vaginal applications using mucoadhesive thiolated polymer. Econazole nitrate (EN) and miconazole nitrate (MN) were used as antifungal drugs to prepare the vaginal tablet formulations. Thiolated poly(acrylic acid)-cysteine (PAA-Cys) conjugate was synthesized by the covalent attachment of L-cysteine to PAA with the formation of amide bonds between the primary amino group of L-cysteine and the carboxylic acid group of the polymer. Vaginal mucoadhesive matrix tablets were prepared by direct compression technique. The investigation focused on the influence of modified polymer on water uptake behavio... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5111231 Wed, 10 Aug 2011 20:30:06 +0100 5111231 http://www.medworm.com/index.php?rid=5111230&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21804239%26dopt%3DAbstract This study investigated the effects of binder type and binder content in orally disintegrating tablets, and provided evidence that the binder exerts a strong influence on tablet properties, and is therefore an important component of orally disintegrating tablets. PMID: 21804239 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5111230 Wed, 10 Aug 2011 20:30:06 +0100 5111230 http://www.medworm.com/index.php?rid=5111229&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21804240%26dopt%3DAbstract In this study, the metal-binding ability of 21 synthetic peptides representing regions of human PrP(C) was investigated by column switch high-performance liquid chromatography (CS-HPLC). The CS-HPLC system is composed of a metal chelate affinity column and an octadecylsilica (ODS) reversed-phase column that together enable the identification of metal-binding regardless of conformational conversion. Synthetic peptides were designed with respect to the position of H residues as well as the secondary structure of human PrP (hPrP). The ability of the octapeptide (PHGGGWGQ)-repeating region (OP-repeat) to bind metals was analyzed by CS-HPLC and supported by CD analysis, and indicated that CS-HPLC is a reliable and useful method for measuring peptide metal-binding. Peptides from the middle regio... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5111229 Wed, 10 Aug 2011 20:30:06 +0100 5111229 http://www.medworm.com/index.php?rid=5111228&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21804241%26dopt%3DAbstract In conclusion, Zn(asp)(2) complex is newly proposed as a potent anti-diabetic and anti-metabolic syndrome agent. PMID: 21804241 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5111228 Wed, 10 Aug 2011 20:30:06 +0100 5111228 http://www.medworm.com/index.php?rid=5111227&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21804242%26dopt%3DAbstract Authors: Gregan F, Gregan J, Skorsepa M Two homologous series of racemic diastereomeric cis- and trans-(2-dimethylaminomethylcycloheptyl)-2-alkoxyphenylcarbamates with alkyl chain lengths ranging from C(1) to C(8) were synthesized by stereoselective reactions. The chemical structures of these compounds were confirmed by (1)H-NMR, (13)C-NMR and IR spectroscopy and their physico-chemical properties were characterized. The two new series of diastereomeric compounds were tested for their local anesthetic activity and parabolic relationship between the local anesthetic activity and lipophilicity was found for both cis- and trans-series. Interestingly, cis-stereoisomers exhibited higher local anesthetic activity. PMID: 21804242 [PubMed - in process] (Source: Chemical and Pharmaceutical B... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5111227 Wed, 10 Aug 2011 20:30:06 +0100 5111227 http://www.medworm.com/index.php?rid=5111226&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21804243%26dopt%3DAbstract Authors: Xie L, Zhai X, Ren L, Meng H, Liu C, Zhu W, Zhao Y In an attempt to develop potent and selective anti-tumor agents, two novel series of artemisinin-chalcone hybrids were designed, synthesized and screened for their antitumor activities against HT-29, A549, MDA-MB-231, HeLa and H460 cell lines in vitro. Nearly all of the tested compounds showed significantly increased anti-tumor activity compared with the corresponding dihydroartemisinin (DHA). Most of the title compounds displayed good selectivity toward HT-29 and HeLa cell lines with IC(50) values ranging from 0.09 to 0.85 µM. Among them, the most promising compound 9c (IC(50) range of 0.09-0.93 µM) was 10.5- to 70-times more active than DHA (IC(50) range of 5.6-15.6 µM) respectively. PMID: 21804243 [PubMed - in proces... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5111226 Wed, 10 Aug 2011 20:30:06 +0100 5111226 http://www.medworm.com/index.php?rid=5111225&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21804244%26dopt%3DAbstract Authors: Horiuchi T, Takeda Y, Haginoya N, Miyazaki M, Nagata M, Kitagawa M, Akahane K, Uoto K The design, synthesis, and evaluation of novel thieno[2,3-d]pyrimidin-4-yl hydrazone analogues as cyclin-dependent kinase 4 (CDK4) inhibitors are described. In continuing our program aim to search for potent CDK4 inhibitors, the introduction of a thiazole group at the hydrazone part has led to marked enhancement of chemical stability. Furthermore, by focusing on the optimization at the C-4' position of the thiazole ring and the C-6 position of the thieno[2,3-d]pyrimidine moiety, compound 35 has been identified with efficacy in a xenograft model of HCT116 cells. In this paper, the potency, selectivity profile, and structure-activity relationships of our synthetic compounds are discussed. P... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5111225 Wed, 10 Aug 2011 20:30:06 +0100 5111225 http://www.medworm.com/index.php?rid=5111224&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21804245%26dopt%3DAbstract Authors: Liu HB, Zhang CR, Dong SH, Dong L, Wu Y, Yue JM Three limonoids (1-3), and two triterpenes (4) and (5), along with twelve known compounds, were isolated from the seeds of Melia azedarach. Their structures were established on the basis of extensive spectroscopic analysis. Compound 3 showed moderate antimicrobial activity. PMID: 21804245 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin) Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5111224 Wed, 10 Aug 2011 20:30:06 +0100 5111224 http://www.medworm.com/index.php?rid=5111223&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21804246%26dopt%3DAbstract Authors: Tsutsumi H, Kinoshita Y, Sato T, Ishizu T Crystals of the complexes of (+)-catechin (CA) of non-galloylated catechin and (-)-catechin-3-O-gallate (Cg) of galloylated catechin with caffeine were prepared, and their stereochemical structures and intermolecular interactions were determined by X-ray crystallographic analysis. CA formed a 1 : 1 complex with caffeine by intermolecular hydrogen bonds, whereas Cg formed a 1 : 2 complex with caffeine, which was formed by face-to-face and offset π-π interactions and intermolecular hydrogen bonds. A solution of two kinds of non-galloylated catechin, CA and (-)-epicatechin (EC), and caffeine (molar ratio 1 : 1 : 2) in water afforded a 1 : 1 : 2 complex, the crystal structure of which had two layers, one layer in which CA and caffeine fo... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5111223 Wed, 10 Aug 2011 20:30:06 +0100 5111223 http://www.medworm.com/index.php?rid=5111222&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21804247%26dopt%3DAbstract Authors: Yang Y, Feng Z, Jiang J, Yang Y, Pan X, Zhang P A series of novel 1,3,4-thiadiazine derivatives were synthesized via chemical optimization on phthiobuzone. Their anti-herpes simplex virus (HSV) activities in vitro were also tested. Several compounds exhibited more highly potent anti-HSV activity and much higher selectivity index (SI) values than those of phthiobuzone. The most potent anti-HSV compound was 4f, which showed marked inhibition against HSV-1 (IC(50)=77.04 µg/ml) and HSV-2 (IC(50)=30.00 µg/ml). Meanwhile it had low cytotoxicity (CC(50)=1000.00 µg/ml), resulting in high (SI(HSV-1)=12.98, SI(HSV-2)=33.33, respectively). Furthermore, a computational study for prediction of absorption, distribution, metabolism, excretion (ADME) properties of compound 4f was performed... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5111222 Wed, 10 Aug 2011 20:30:06 +0100 5111222 http://www.medworm.com/index.php?rid=5111221&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21804248%26dopt%3DAbstract Authors: Nakamura S, Zhang Y, Matsuda H, Ninomiya K, Muraoka O, Yoshikawa M The methanolic extract from the leaves of Salacia chinensis collected in Thailand was found to show a protective effect on D-galactosamine-induced cytotoxicity in primary cultured mouse hepatocytes. From the methanolic extract, eight new glycosides, named foliachinenosides E, F, G, H, and I, and foliasalaciosides J, K and L, were isolated together with 26 known constituents. The structures of new glycosides were determined on the basis of physicochemical and chemical evidence. In addition, the hepatoprotective effects of the isolated compounds on D-galactosamine-induced cytotoxicity were examined. Among them, lignans, eleutheroside E(2) and 7R,8S-dihydrodehydrodiconiferyl alcohol 4-O-β-D-glucopyranoside, were ... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5111221 Wed, 10 Aug 2011 20:30:06 +0100 5111221 http://www.medworm.com/index.php?rid=5111211&cid=s_37782_13_f&fid=37782&url=http%3A%2F%2Fwww.ncbi.nlm.nih.gov%2Fentrez%2Fquery.fcgi%3Ftmpl%3DNoSidebarfile%26db%3DPubMed%26cmd%3DRetrieve%26list_uids%3D21804249%26dopt%3DAbstract Authors: Watanuki S, Matsuura K, Tomura Y, Okada M, Okazaki T, Ohta M, Tsukamoto S A series of 1-isopropyl-1,2,3,4-tetrahydroisoquinoline derivatives were synthesized and their bradycardic activities were evaluated in isolated guinea pig right atria. Structure-activity relationship studies revealed that the introduction of an appropriate substituent and its position on the 1,2,3,4-tetrahydroisoquinoline ring are essential for potent in vitro activity. Furthermore, the tether between the piperidyl moiety and the terminal aromatic ring is important for potent antihypertensive activity. Oral administration of 6-fluoro-1-isopropyl-2-{[1-(2-phenylethyl)piperidin-4-yl]carbonyl}-1,2,3,4-tetrahydroisoquinoline (3b) to spontaneously hypertensive rats (SHR) elicited antihypertensive effects with... Chemical and Pharmaceutical Bulletin journals http://www.medworm.com/rss/comments.php?id=5111211 Wed, 10 Aug 2011 20:30:06 +0100 5111211