Basic and Clinical Pharmacology and ToxicologyThis is an RSS file. You can use it to subscribe to this data in your favourite RSS reader, such as GoogleReader, or to display this data on your own website or blog. Subscribe to this data using MyMedWorm.Subscribe to this data using GoogleReader.Subscribe to this data using Bloglines.Subscribe to this data using MyYahoo.

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285 records returned

Chitosan Oligosaccharides Inhibit the Expression of Interleukin-6 in Lipopolysaccharide-induced Human Umbilical Vein Endothelial Cells Through p38 and ERK1/2 Protein KinasesEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
In conclusion, our results suggest that COS inhibit LPS-induced up-regulation of IL-6 in HUVECs, and this can be regulated by at least two parallel signalling pathways: one via p38 MAPK pathway independent of NF-[kappa]B activation and one via ERK1/2 pathway dependent on NF-[kappa]B activation. (Source: Basic and Clinical Pharmacology and Toxicology)
Source: Basic and Clinical Pharmacology and Toxicology - November 17, 2009 Category: Drugs & Pharmacology Authors: Hong-Tao Liu, Wen-Ming Li, Xiu-Ying Li, Qing-Song Xu, Qi-Shun Liu, Xue-Fang Bai, Chao Yu, Yu-Guang Du Source Type: journals

Dynamic Epigenetic Changes Involved in Testicular Toxicity Induced by Di-2-(Ethylhexyl) Phthalate in MiceEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract: The aim of this study was to analyse epigenetic (specifically, DNA methylation) change in testes induced by maternal exposure to di-2-(ethylhexyl) phthalate (DEHP) in mice. Testicular dysgenesis syndrome was induced in foetuses by maternal exposure to DEHP. High-performance liquid chromatography was performed to analyse DNA methylation status, and expression levels of the DNA methyltransferases were examined by quantitative real-time polymerase chain reaction and western blotting. DEHP significantly had more than 10% relative increase in the global DNA methylation and also increased DNA methyltransferases' expres...
Source: Basic and Clinical Pharmacology and Toxicology - November 11, 2009 Category: Drugs & Pharmacology Authors: Shengde Wu, Jing Zhu, Yasha Li, Tao Lin, Liqiang Gan, Xingang Yuan, Jing Xiong, Xing Liu, Mingdeng Xu, Dan Zhao, Chao Ma, Xuliang Li, Guanghui Wei Source Type: journals

Effects of Selective Serotonin Reuptake Inhibitors on Timolol Metabolism in Human Liver Microsomes and Cryo-Preserved HepatocytesEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
In conclusion, compounds known to be potent CYP2D6 inhibitors inhibited timolol metabolism in in vitro experiments. The present results strongly suggest that fluoxetine and paroxetine may significantly affect the metabolism of timolol also in vivo and may thus potentiate the adverse cardiovascular effects of topically administered timolol. (Source: Basic and Clinical Pharmacology and Toxicology)
Source: Basic and Clinical Pharmacology and Toxicology - November 11, 2009 Category: Drugs & Pharmacology Authors: Marjo Volotinen, Timo Korjamo, Ari Tolonen, Miia Turpeinen, Olavi Pelkonen, Jukka Hakkola, Jukka Mäenpää Source Type: journals

Physiologically Based Modelling and Prediction of Drug InteractionsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
This article reviews briefly past developments in the area of physiologically based pharmacokinetic (PBPK) modelling of interactions. It also demonstrates a systems biology approach to the question, and the capabilities of new software tools to facilitate that development. Individual Systems Biology Markup Language models of metabolic pathways can now be automatically merged and coupled to a template PBPK pharmacokinetic model, using for example the GNU MCSim software. The global model generated is very efficient and able to simulate the interactions between a theoretically unlimited number of substances. Development time ...
Source: Basic and Clinical Pharmacology and Toxicology - November 11, 2009 Category: Drugs & Pharmacology Authors: Frédéric Y. Bois Source Type: journals

Impact of Concentrative Nucleoside Transporter 1 Gene Polymorphism on Oral Bioavailability of Mizoribine in Stable Kidney Transplant RecipientsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract: Mizoribine, an immunosuppressive anti-metabolite, is largely excreted into urine in its unchanged form, and its pharmacokinetics has been considered to be dependent on the glomerular filtration rate. However, the pharmacokinetic disposition of mizoribine has not been fully clarified. The aim of this study was to evaluate the pharmacokinetic disposition of mizoribine based on polymorphism of concentrative nucleoside transporter (CNT) 1 gene in kidney transplant recipients. Thirty-four Japanese stable recipients receiving an immunosuppressive regimen containing mizoribine for more than four months after transplanta...
Source: Basic and Clinical Pharmacology and Toxicology - November 11, 2009 Category: Drugs & Pharmacology Authors: Takafumi Naito, Shunsuke Tokashiki, Yasuaki Mino, Atsushi Otsuka, Seiichiro Ozono, Yoshiyuki Kagawa, Junichi Kawakami Source Type: journals

Cardioprotective Effect of SMND-309, A Novel Derivate of Salvianolic Acid B on Acute Myocardial Infarction in RatsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract: (2E)-2-{6-[(E)-2-carboxylvinyl]-2,3-dihydroxyphenyl}-3-(3,4-dihydroxyphenyl) propenoic acid, a novel compound designated SMND-309, is a new derivate of salvianolic acid B. The present study was designed to investigate the cardioprotective potential of SMND-309 and to elucidate the possible mechanisms on the basis of biochemical, histopathological and immunohistochemical studies in a rat model of acute myocardial infarction induced by permanent ligation of the left coronary artery. The results showed that treatment with SMND-309 via tail vein at doses of 10 and 20 mg/kg significantly prevented the elevation in ST ...
Source: Basic and Clinical Pharmacology and Toxicology - November 11, 2009 Category: Drugs & Pharmacology Authors: Jianxiong Yang, Guanbo Zhang, Jingwei Tian, Chunmei Li, Wanglin Jiang, Yanli Xing, Haibo Zhu, Jian Hou, Hong Xu, Juan Wu Source Type: journals

Induced DNA Damage by Dental Resin Monomers in Somatic CellsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract: The present in vivo study investigated the genotoxicity of four dental resin monomers: triethyleneglycoldimethacrylate (TEGDMA), hydroxyethylmethacrylate (HEMA), urethanedimethacrylate (UDMA) and bisphenol A-glycidylmethacrylate (BisGMA). The Somatic Mutation and Recombination Test (SMART) in Drosophila melanogaster was applied to analyse their genotoxicity expressed as homologous mitotic recombination, point and chromosomal mutation. SMART detects the loss of heterozygosity of marker genes expressed phenotypically on the fly's wings. This fruit fly has an extensive genetic homology to mammalians, which makes it ...
Source: Basic and Clinical Pharmacology and Toxicology - November 11, 2009 Category: Drugs & Pharmacology Authors: Guilherme Anziliero Arossi, Mauricio Lehmann, Rafael Rodrigues Dihl, Maria Luiza Reguly, Heloisa Helena Rodrigues de Andrade Source Type: journals

l-Carnitine Attenuates Cardiac Remodelling rather than Vascular Remodelling in Deoxycorticosterone Acetate-Salt Hypertensive RatsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
This study has determined whether oral administration of l-carnitine prevents remodelling and the development of impaired cardiovascular function in deoxycorticosterone acetate (DOCA)-salt hypertensive rats (n = 6[ndash]12; #p < 0.05 versus DOCA-salt). Uninephrectomized rats administered DOCA (25 mg every 4th day s.c.) and 1% NaCl in drinking water for 28 days developed cardiovascular remodelling shown as systolic hypertension, left ventricular hypertrophy, increased thoracic aortic and left ventricular wall thickness, increased left ventricular inflammatory cell infiltration together with increased interstitial collagen a...
Source: Basic and Clinical Pharmacology and Toxicology - November 11, 2009 Category: Drugs & Pharmacology Authors: Daniel O'Brien, Prasad Chunduri, Abishek Iyer, Lindsay Brown Source Type: journals

Different Effects of Scopolamine and Inhibition of Prolyl Oligopeptidase on Mnemonic and Motility Functions of Young and 8- to 9-Month-Old Rats in the Radial-Arm MazeEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract: Prolyl oligopeptidase (POP) has been connected to memory and mood through regulation of the brain levels of its biologically active peptide substrates and phosphatidylinositol system. This is the first study in a radial-arm maze of the effects of a single dose of a novel potent prolyl oligopeptidase inhibitor, KYP-2047 (5 mg/kg, dissolved in 5% Tween 80), on memory and learning of scopolamine-treated (0.4 mg/kg, dissolved in saline) rats. Habituated (days 1 and 2) and trained (days 3[ndash]11) young (3 months) and old (8[ndash]9 months) male Wistar rats were given (i) saline + Tween, (ii) saline + KYP-2047, (iii)...
Source: Basic and Clinical Pharmacology and Toxicology - November 11, 2009 Category: Drugs & Pharmacology Authors: Iida Peltonen, Aaro J. Jalkanen, Veijo Sinervä, Katja A. Puttonen, Pekka T. Männistö Source Type: journals

Variability and Impact on Design of Bioequivalence StudiesEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract: In 2008, the European Agency for the Evaluation of Medicinal Products released a draft guidance on the investigation of bioequivalence for immediate release dosage forms with systemic action to replace the former guidance of a decade ago. Revisions of the regulatory guidance are based upon many questions over the past years and sometimes continuing scientific discussions on the use of the most suitable statistical analysis methods and study designs, particularly for drugs and drug products with high within-subject variability. Although high within-subject variability is usually associated with a coefficient of va...
Source: Basic and Clinical Pharmacology and Toxicology - November 11, 2009 Category: Drugs & Pharmacology Authors: Achiel Van Peer Source Type: journals

Cardiac and Haemodynamic Effects of Tacrolimus in the Halothane-Anaesthetized DogEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract: Tacrolimus (FK506) is a potent immunosuppressant widely used for the treatment of patients with solid organ transplantation and autoimmune diseases. The present study investigated the cardiac, haemodynamic and electrophysiological effects of tacrolimus. Tacrolimus in doses of 0.01 and 0.1 mg/kg was infused over 10 min. with a pause of 20 min. in halothane-anaesthetized dogs under monitoring of plasma drug concentrations (n = 5). Sub-therapeutic dose of 0.01 mg/kg hardly affected any of the cardiovascular variables except that it slightly delayed the repolarization. The clinically relevant dose of 0.1 mg/kg had ne...
Source: Basic and Clinical Pharmacology and Toxicology - November 11, 2009 Category: Drugs & Pharmacology Authors: Hiroaki Kise, Yuji Nakamura, Minako Hoshiai, Hisashi Sugiyama, Kanji Sugita, Atsushi Sugiyama Source Type: journals

Drug Dispensing Errors in a Ward Stock SystemEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract: The aim of this study was to determine the frequency of drug dispensing errors in a traditional ward stock system operated by nurses and to investigate the effect of potential contributing factors. This was a descriptive study conducted in a teaching hospital from January 2005 to June 2007. In five wards, samples of dispensed solid drugs were collected prospectively and compared with the prescriptions. Data were evaluated using multivariable logistic regression. Overall, 2173 samples were collected, 95.5% of which were correctly dispensed (95% CI 94.5[ndash]96.2). In total, 124 errors in 6715 opportunities for er...
Source: Basic and Clinical Pharmacology and Toxicology - November 11, 2009 Category: Drugs & Pharmacology Authors: Stig Ejdrup Andersen Source Type: journals

Tanshinone II A Induces Apoptosis and S Phase Cell Cycle Arrest in Activated Rat Hepatic Stellate CellsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract: Tanshinone IIA, a major component extracted from the traditional herbal medicine, Salvia miltiorrhiza Bunge, improves blood circulation and treats chronic hepatitis and hepatic fibrosis. Activation of hepatic stellate cells (HSCs) is the predominant event in liver fibrosis. The therapeutic goal in liver fibrosis is the reversal of fibrosis and selective clearance of activated HSCs. We used rat HSCs transformed by Simian virus 40 (t-HSC/Cl-6) to overcome the limitations inherent in studying subcultures of HSCs. Treatment of t-HSC/Cl-6 cells with tanshinone IIA inhibited cell viability in a dose- and time-dependent...
Source: Basic and Clinical Pharmacology and Toxicology - November 9, 2009 Category: Drugs & Pharmacology Authors: Xian-Hua Che, Eun-Jeon Park, Yu-Zhe Zhao, Woong-Hyun Kim, Dong Hwan Sohn Source Type: journals

Vanishing Bile Duct Syndrome Associated with Azithromycin in a 62-Year-Old ManEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
We present a case of a 62-year-old male patient who developed vanishing bile duct syndrome a month after Stevens-Johnson syndrome. These adverse drug reactions were associated with the use of azithromycin (500 mg daily for 3 days). The patient was initially treated for Stevens-Johnson syndrome with steroids, antihistamines and proton pump inhibitors and fully recovered. However, a month after the beginning of Stevens-Johnson syndrome, he developed vanishing bile duct syndrome and was treated with steroids, ursodeoxycholic acid, antihistamines and tacrolimus. Unfortunately, the treatment was unsuccessful and he was listed f...
Source: Basic and Clinical Pharmacology and Toxicology - November 9, 2009 Category: Drugs & Pharmacology Authors: Juricic Danica, Hrstic Irena, Radic Davor, Skegro Mate, Coric Marijana, Vucelic Boris, Francetic Igor Source Type: journals

Cardiovascular Effects of Azelnidipine in Comparison with Those of Amlodipine Assessed in the Halothane-Anaesthetized DogEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract: Azelnidipine is a new dihydropyridine Ca2+ channel blocker with long plasma half-life. To understand the in vivo cardiovascular profile of azelnidipine, it was assessed in the halothane-anaesthetized, closed-chest canine model and compared with the effect of amlodipine. We administered azelnidipine in doses of 10, 20 and 70 [mu]g/kg, i.v. or amlodipine in doses of 30, 70 and 200 [mu]g/kg, i.v. cumulatively to the animals. The hypotensive effects of azelnidipine and amlodipine were slow in onset and long-lasted, while their extents of dose-related hypotensive effects were similar. Azelnidipine hardly affected the ...
Source: Basic and Clinical Pharmacology and Toxicology - November 9, 2009 Category: Drugs & Pharmacology Authors: Tomomichi Ishizaka, Akira Takahara, Hiroshi Iwasaki, Yoshitaka Mitsumori, Hiroaki Kise, Yuji Nakamura, Atsushi Sugiyama Source Type: journals

Nano Titanium Dioxide Particles Promote Allergic Sensitization and Lung Inflammation in MiceEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract: The purpose of this study was to investigate whether photocatalytic TiO2 nanoparticles have adjuvant effect, when administered in combination with ovalbumin (OVA) in mice. Mice were immunized via intraperitoneal injections of OVA, OVA + TiO2 or OVA + Al(OH)3 and challenged with aerosols of OVA. At the end of the study, serum was analysed for content of OVA-specific IgE, IgG1 and IgG2a antibodies, and the bronchoalveolar lavage fluid (BALF) was analysed for content of inflammatory cells and levels of interleukin (IL)-4, IL-5, IL-10 and interferon-[gamma]. The TiO2 particles promoted a Th2 dominant immune response ...
Source: Basic and Clinical Pharmacology and Toxicology - October 29, 2009 Category: Drugs & Pharmacology Authors: Søren T. Larsen, Martin Roursgaard, Keld A. Jensen, Gunnar D. Nielsen Source Type: journals

Effects of Insulin-Like Growth Factor-1 on Rotenone-Induced Apoptosis in Human Lymphocyte CellsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract: Human peripheral blood lymphocytes have been useful as a putative model of oxidative stress-induced apoptosis for Parkinson's disease. The present work shows that rotenone, a mitochondrial complex I inhibitor, induced time- and concentration-dependent apoptosis in lymphocytes which was mediated by anion superoxide radicals (O2[bull][minus])/hydrogen peroxide, depolarization of mitochondria, caspase-3 activation, concomitantly with the nuclear translocation of transcription factors such as NF-[kappa]B, p53, c-Jun and nuclei fragmentation. Since insulin-like growth factor-1 (IGF-1) interferes with a cell's apoptoti...
Source: Basic and Clinical Pharmacology and Toxicology - October 28, 2009 Category: Drugs & Pharmacology Authors: Isabel Cristina Avila-Gomez, Carlos Velez-Pardo, Marlene Jimenez-Del-Rio Source Type: journals

Design, Synthesis and Pharmacological Characterization of Endomorphin Analogues with Non-Cyclic Amino Acid Residues in Position 2Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract: A series of endomorphin-1 (EM-1) and endomorphin-2 (EM-2) analogues, containing non-cyclic amino acids (Ala, d-Ala, [beta]-Ala, NMeAla, d-NMeAla or Sar) instead of Pro in position 2 was synthesized, where NMeAla = N-methylalanine and Sar = N-methylglycine, sarcosine. The opioid activity profiles of these peptides were determined in [mu] and [delta] opioid receptor (MOR and DOR)-representative binding assays and bioassays in vitro, as well as in the mouse hot-plate test in vivo. Finally, the degradation rates of all analogues in the presence of either rat brain homogenate or selected proteolytic enzymes were deter...
Source: Basic and Clinical Pharmacology and Toxicology - October 28, 2009 Category: Drugs & Pharmacology Authors: Renata Perlikowska, Jakub Fichna, Anna Wyrębska, Jeroen Poels, Jozef Vanden Broeck, Geza Toth, Martin Storr, Jean-Claude do Rego, Anna Janecka Source Type: journals

Apoptin Enhances Radiation-Induced Cell Death in Poorly Responding Head and Neck Squamous Cell Carcinoma CellsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
We examined whether chicken anaemia virus-derived apoptin protein would have a beneficial effect on irradiation of radiosensitive SCC61 and radioresistant SQD9 human head and neck squamous carcinoma cell lines. In both cell lines, concurrent exposure to irradiation and apoptin resulted in analysed mitochondrial cytochrome c release and in cleavage of caspase-3, whereas irradiation alone of SQD9 cells under identical conditions did not. Moreover, in comparison with the irradiation, only the synchronized treatment of apoptin and irradiation resulted in increased cell death in especially the radioresistant SQD9 cells, as meas...
Source: Basic and Clinical Pharmacology and Toxicology - October 28, 2009 Category: Drugs & Pharmacology Authors: Remilio A. L. Schoop, Elizabeth M. E. Verdegaal, Robert J. Baatenburg de Jong, Mathieu H. M. Noteborn Source Type: journals

Sub-Chronic Exposure to Methylmercury at Low Levels Decreases Butyrylcholinesterase Activity in RatsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
In conclusion, long-term exposure to low doses of MeHg decreases plasmatic BuChE activity. Moreover, the decrease in the enzyme is strongly correlated with the oxidative stress promoted by the metal exposure. This preliminary finding highlights a possible mechanism for MeHg to reduce BuChE activity in plasma. Additionally, this enzyme could be an auxiliary biomarker on the evaluation of MeHg exposure. (Source: Basic and Clinical Pharmacology and Toxicology)
Source: Basic and Clinical Pharmacology and Toxicology - October 27, 2009 Category: Drugs & Pharmacology Authors: Juliana Valentini, Juliana Vicentini, Denise Grotto, Raquel Tonello, Solange C. Garcia, Fernando Barbosa Jr Source Type: journals

Melatonin and Vitamin C Attenuates Alcohol-Induced Oxidative Stress in AortaEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract: Epidemiological studies have shown that low to moderate doses of alcohol consumption are beneficial to cardiac health. However, chronic high doses of alcohol ingestion cause cardiovascular complications. The aim of this study was to investigate both the effects of melatonin and vitamin C and expression of endothelial nitric oxide synthase in aorta of chronic alcoholic rats. Twenty-four adult male Wistar rats weighing 200[ndash]250 g were used in the study. Rats were divided into four equal groups. Group I (control): rats were not fed on alcohol; Group II: rats were fed on alcohol; Group III: rats were fed on alco...
Source: Basic and Clinical Pharmacology and Toxicology - October 14, 2009 Category: Drugs & Pharmacology Authors: Mehmet Fatih Sönmez, Figen Narin, Esra Balcioğlu Source Type: journals

The Effect of Tetramethylpyrazine on Hydrogen Peroxide-Induced Oxidative Damage in Human Umbilical Vein Endothelial CellsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract: Tetramethylpyrazine has been widely used in traditional Chinese medicine to treat cardiovascular diseases such as atherosclerosis and hypertension. The underlying mechanism of cardioprotective effects, however, remains to be elucidated. Here, using human umbilical vein endothelial cells (HUVECs), we have assessed the protective effect of tetramethylpyrazine on H2O2-induced oxidative damage. After pre-incubation with tetramethylpyrazine (50, 100 and 150 [mu]g/ml) for 24 hr., viability loss in H2O2-induced HUVECs (76.5% of the control level, p < 0.05, at 400 [mu]M of H2O2 for 12 hr.) was restored in a concentration...
Source: Basic and Clinical Pharmacology and Toxicology - October 12, 2009 Category: Drugs & Pharmacology Authors: Wen-Ming Li, Hong-Tao Liu, Xiu-Ying Li, Jian-Yong Wu, Gang Xu, Yong-Zhen Teng, Song-Tao Ding, Chao Yu Source Type: journals

Betulin Elicits Anti-Cancer Effects in Tumour Primary Cultures and Cell Lines In VitroEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
In this study, we demonstrated a remarkable anti-proliferative effect of betulin in all tested tumour cell cultures. Neuroblastoma (SK-N-AS) and colon carcinoma (HT-29) were the most sensitive to the anti-proliferative effect of betulin. Furthermore, betulin altered tumour cells morphology, decreased their motility and induced apoptotic cell death. These findings demonstrate the anti-cancer potential of betulin and suggest that they may be applied as an adjunctive measure in cancer treatment. (Source: Basic and Clinical Pharmacology and Toxicology)
Source: Basic and Clinical Pharmacology and Toxicology - October 11, 2009 Category: Drugs & Pharmacology Authors: Wojciech Rzeski, Andrzej Stepulak, Marek Szymański, Małgorzata Juszczak, Aneta Grabarska, Marco Sifringer, Józef Kaczor, Martyna Kandefer-Szerszeń Source Type: journals

Comparative Effects of Pesticides on In Vivo Dopamine Release in Freely Moving RatsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract: The effects of different types of pesticides on the in vivo striatal dopamine release were investigated by using in vivo brain microdialysis technique. MPTP, paraquat, maneb, dicofol, DDT, lindane and flutriafol (1 mM) were administered directly into the striatum, and levels of dopamine and its metabolites dihydroxyphenylacetic acid (DOPAC) and homovallinic acid (HVA) were measured using HPLC-EC. Intrastriatal administration of pesticides induced the following maximal effects on the dopamine levels: maneb 791 ± 87%, dicofol 101 ± 1%, DDT 779 ± 32%, paraquat 956 ± 80%, lindane 281 ± 28% and flutriafol 218 ± ...
Source: Basic and Clinical Pharmacology and Toxicology - October 11, 2009 Category: Drugs & Pharmacology Authors: Lilian R. F. Faro, Miguel Alfonso, Rosa Cervantes, Rafael Durán Source Type: journals

Effect of Uric Acid on Gentamicin-Induced Nephrotoxicity in Rats – Role of Matrix Metalloproteinases 2 and 9Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract: In this work, we aimed to study the effect of uric acid on gentamicin-induced nephrotoxicity. Male Sprague-Dawley rats were assigned to one of six groups (six rats each) which received intraperitoneal injections for 9 days: (S) saline; (UA) Uric acid alone; (G) Gentamicin alone; (G + UA) Gentamicin + uric acid; (G rec) Gentamicin recovery and (G + UA rec) Gentamicin + uric acid recovery. In (G rec) and (G + UA rec), rats recovered for 7 days after the last injection. Urine and blood samples were taken on day 0 and at the end of every stage. Kidneys were harvested for histological scoring, determination of renal m...
Source: Basic and Clinical Pharmacology and Toxicology - October 11, 2009 Category: Drugs & Pharmacology Authors: Freddy Romero, Mariela Pérez, Maribel Chávez, Gustavo Parra, Paula Durante Source Type: journals

Oestradiol Protects Against the Harmful Effects of Fluoride More by Increasing Thiol Group Levels than Scavenging Hydroxyl RadicalsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract: The aim of the study was to investigate the role of oestrogens in free radical detoxication upon exposure to fluoride. Interactions between xenobiotics and oestrogens need to be investigated, especially as many chemicals interact with the oestrogen receptor. It is still unknown whether free radical-generating xenobiotics can influence the antioxidative ability of oestradiol (E2). In an in vitro examination of human placental mitochondria, thiobarbituric active reagent species (TBARS), hydroxyl radical ([bull]OH) generation and protein thiol ([ndash]SH) groups were detected. 17[beta]-E2 was examined in physiologic...
Source: Basic and Clinical Pharmacology and Toxicology - October 1, 2009 Category: Drugs & Pharmacology Authors: Anna Dlugosz, Anna Roszkowska, Mariusz Zimmer Source Type: journals

Antioxidant Activity of Limonene on Normal Murine Lymphocytes: Relation to H2O2 Modulation and Cell ProliferationEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract: Limonene is a monoterpene present in citrus fruit and is used as flavouring agents of foods. It was shown that monoterpenes possess antioxidant activity. Previously, it was demonstrated that limonene exerts anti-proliferative action on a lymphoma cell line without modifying normal lymphocyte viability. H2O2 has a modulator role in cell proliferation. In the present study, the effect of limonene on normal lymphocytes proliferation and its relation with H2O2 level modulation was analysed, evaluating its effect on the activity of cell antioxidant enzymes, such as catalase, peroxidase and superoxide dismutase. Limone...
Source: Basic and Clinical Pharmacology and Toxicology - September 30, 2009 Category: Drugs & Pharmacology Authors: Davicino Roberto, Patricia Micucci, Turner Sebastian, Ferraro Graciela, Claudia Anesini Source Type: journals

The Effects of Peroral Glycerol on Plasma Osmolarity in Diabetic Patients and Healthy IndividualsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
In conclusion, peroral glycerol had similar effects on blood glucose, MAP and pOSM in the diabetic patients and healthy individuals. Specific precautions should not be implemented when treating diabetic patients with a single dose up to 1.7 g/kg body weight. A peak increase of 8% in the pOSM within 1 hr can be expected from this dose. (Source: Basic and Clinical Pharmacology and Toxicology)
Source: Basic and Clinical Pharmacology and Toxicology - September 30, 2009 Category: Drugs & Pharmacology Authors: Dorte Nellemann Thornit, Birgit Sander, Morten la Cour, Henrik Lund-Andersen Source Type: journals

Rossicaside B Protects against Carbon Tetrachloride-induced Hepatotoxicity in MiceEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract: The protective effect of rossicaside B, the major phenylpropanoid glycoside from Boschniakia rossica, on CCl4-induced hepatotoxicity and the mechanisms underlying its protective effect were investigated. The mice were administered orally with rossicaside B (100 or 200 mg/kg of body weight) 48, 24 and 1 hr before CCl4 (0.5 ml/kg of body weight) administration. The CCl4 challenge caused a marked increase in the levels of serum aspartate aminotransferase, alanine aminotransferase and of tumour necrosis factor-[alpha], and propagated lipid peroxidation with a concomitant reduction in reduced glutathione (GSH) and ant...
Source: Basic and Clinical Pharmacology and Toxicology - September 29, 2009 Category: Drugs & Pharmacology Authors: Jishu Quan, Long Piao, Xia Wang, Tian Li, Xuezhe Yin Source Type: journals

Biological Evaluation of 2-(4-Amino-Phenyl)-3-(3,5-Dihydroxylphenyl) Propenoic AcidEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract: 2-(4-Aminophenyl)-3-(3,5-dihydroxylphenyl) propenoic acid (CSN-07001) is a new compound based on the combination of resveratrol and propenoic acid derivatives. In vitro cyclooxygenase (COX)/5-lipoxygenase (5-LOX) inhibition assays showed that the test compound exhibited a dual inhibitory activity against the COX (COX-1 IC50 = 2.20 [mu]M, COX-2 IC50 = 1.76 [mu]M) and 5-LOX (IC50 = 0.28 [mu]M) enzymes. Further, the enhanced COX-1/COX-2/5-LOX expression in lipopolysaccaride-induced lung inflammation in mice was also suppressed by CSN-07001 in a concentration-dependent manner. In vivo studies showed that CSN-07001 ex...
Source: Basic and Clinical Pharmacology and Toxicology - September 8, 2009 Category: Drugs & Pharmacology Authors: Guang-Lin Xu, Fei Liu, Yue Zhao, Gui-Zhen Ao, Liang Xi, Min Ju, Ting Xue Source Type: journals

Nitrite-Induced Methemoglobinaemia Affects Blood Ionized and Total Magnesium Level by Hydrolysis of Plasma Adenosine Triphosphate in RatEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
In conclusion, NaNO2-induced methemoglobinaemia is a cause of hydrolysis of plasma ATP which is responsible for the increase of blood iMg2+ and plasma tMg2+ in rats. (Source: Basic and Clinical Pharmacology and Toxicology)
Source: Basic and Clinical Pharmacology and Toxicology - August 10, 2009 Category: Drugs & Pharmacology Authors: Md. Mizanur Rahman, Shang-Jin Kim, Gi-Beum Kim, Chul-Un Hong, Young-Up Lee, Sung-Zoo Kim, Jin-Sung Kim, Hyung-Sub Kang Source Type: journals

Roles of Different CYP Enzymes in the Formation of Specific Fluvastatin Metabolites by Human Liver MicrosomesEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract: Fluvastatin has been considered to be metabolised to 5-hydroxy fluvastatin (M-2), 6-hydroxy fluvastatin (M-3) and N-desisopropyl fluvastatin (M-5) in human liver microsomes by primarily CYP2C9. To elucidate the contribution of different CYP enzymes on fluvastatin metabolism, we examined the effect of CYP inhibitors and CYP2C-specific monoclonal antibodies on the formation of fluvastatin metabolites in human liver microsomes. Human liver microsomes were incubated with fluvastatin with or without pre-treatment with CYP inhibitors or monoclonal antibodies. Selective inhibitors of CYP2C9 (sulfaphenazole), CYP3A (keto...
Source: Basic and Clinical Pharmacology and Toxicology - August 6, 2009 Category: Drugs & Pharmacology Authors: Takaki Toda, Erik Eliasson, Birgitta Ask, Nobuo Inotsume, Anders Rane Source Type: journals

Different Effects on Dopamine Release in Nucleus Accumbens in Mice by the Morphine Metabolites Morphine-6-Glucuronide and Morphine-3-GlucuronideEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
(Source: Basic and Clinical Pharmacology and Toxicology)
Source: Basic and Clinical Pharmacology and Toxicology - August 5, 2009 Category: Drugs & Pharmacology Authors: Vigdis Vindenes, Bjørg Sjøgren Pettersen, Andre Gottås, Nina Lieng Christiansen, Fernando Boix, Jørg Mørland Source Type: journals

The Consideration of Synthetic Short Interfering RNA for Therapeutic UseEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract: Small RNA molecules can act as regulators of post-transcriptional gene silencing and can target any given protein via the RNA interference pathway. This leads to the high expectation of small interference RNA (siRNA) as a therapeutic platform. Many companies and organisations are active in this development, which consequently forces siRNA's pharmacokinetic studies because pharmacokinetics plays an important role in elucidating the pharmacodynamic and toxicological mechanism of test articles. In particular, pharmacokinetics is mandatory in investigational new drug application in many countries. Some pre-clinical a...
Source: Basic and Clinical Pharmacology and Toxicology - August 5, 2009 Category: Drugs & Pharmacology Authors: Jun Li, Zicai Liang Source Type: journals

Clinical Pathology Alterations in Pregnant and Non-Pregnant Rats following Scorpion EnvenomationEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
This study was performed to evaluate conventional haematological and serum chemical measurements as potential indices of scorpion envenomation. Adult, cycling nulliparous and near-term primiparous, white Wistar rats received a single subcutaneous injection of crude venom (600 µg/kg) from the Buthidae scorpion (Buthus occitanus tunetanus). All envenomed rats were observed for external signs and symptoms of toxicity until necropsy, which entailed terminal blood collection at either 0.5, 1, 2, or 4 hr after venom administration (n = 6 per reproductive state per time-point) for evaluation of selected clinical chemistry and ha...
Source: Basic and Clinical Pharmacology and Toxicology - August 4, 2009 Category: Drugs & Pharmacology Authors: Hmed Ben Nasr, Brad Bolon, Serria Turky Hammami, Zouhier Sahnoun, Kamel Jamoussi, Amina Lahyani, Khaled Mounir Zeghal Source Type: journals

The Effect of Scheduling and Withdrawal of Carisoprodol on Prevalence of Intoxications with the DrugEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
This study showed that the rescheduling and withdrawal of carisoprodol from the Norwegian market had a positive effect on the prevalence of carisoprodol in impaired driving, deaths and contacts regarding intoxications. This, together with previous publications, indicates that the population reflected in our data uses regularly prescribed carisoprodol and, to a lesser degree, drug from an illegal street market. (Source: Basic and Clinical Pharmacology and Toxicology)
Source: Basic and Clinical Pharmacology and Toxicology - August 4, 2009 Category: Drugs & Pharmacology Authors: Gudrun Høiseth, Ritva Karinen, Hanne Kristin Sørlid, Jørgen G. Bramness Source Type: journals

Irinotecan Side Effects Relieved by the Use of HI-6 Oxime: In Vivo Experimental ApproachEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract: Some compounds, although not primarily designed as supportive drugs in chemotherapy, are promising candidates for clinical use. The ability of HI-6 oxime to relieve the side effects of irinotecan was recently determined in vitro. In this animal study, we investigated the efficacy of HI-6 in vivo, when given as a pre-treatment and concomitantly with irinotecan. We evaluated the cholinesterase (ChE)/acetylcholinesterase (AChE) activity, the levels of oxidative stress markers, DNA damage and the radical scavenging capacity of HI-6. Both HI-6 and irinotecan inhibited ChE/AChE activity but showed different levels of C...
Source: Basic and Clinical Pharmacology and Toxicology - August 4, 2009 Category: Drugs & Pharmacology Authors: Ana Lucić Vrdoljak, Suzana Berend, Davor Želježić, Jasenka Piljac-Žegarac, Stjepko Ple[scaron]tina, Kamil Kuča, Božica Radić, Marin Mladinić, Nevenka Kopjar Source Type: journals

Effects of Long-Term Mildronate Treatment on Cardiac and Liver Functions in RatsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract: Mildronate is a cardioprotective drug that improves cardiac function during ischaemia and functions by lowering l-carnitine concentration in body tissues and modulating myocardial energy metabolism. The aim of the present study was to characterise cardiovascular function and liver condition after long-term mildronate treatment in rats. In addition, changes in the plasma lipid profile, along with changes in the concentration of mildronate, l-carnitine and [gamma]-butyrobetaine were monitored in the rat tissues. Wistar rats were perorally treated daily with a mildronate dose of either 100, 200 or 400 mg/kg for 4, 8...
Source: Basic and Clinical Pharmacology and Toxicology - August 4, 2009 Category: Drugs & Pharmacology Authors: Edgars Liepinsh, Janis Kuka, Baiba Svalbe, Reinis Vilskersts, Elina Skapare, Helena Cirule, Osvalds Pugovics, Ivars Kalvinsh, Maija Dambrova Source Type: journals

Anti-CD20 Antibody Rituximab in the Treatment of Rheumatoid ArthritisEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract: Rheumatoid arthritis (RA) is a chronic, autoimmune reaction-driven systemic inflammatory disease that affects joints and several other organs. Although anti-TNF therapy and combination therapy with traditional anti-rheumatic drugs have improved the treatment of RA, still quite a significant proportion of patients do not reach adequate anti-rheumatic response. The understanding of the pathogenesis of RA has developed markedly during the last two decades, and this has brought up new targets for anti-rheumatic therapy. B cells have been found to have a pivotal role in the development of arthritis both in experimenta...
Source: Basic and Clinical Pharmacology and Toxicology - July 21, 2009 Category: Drugs & Pharmacology Authors: Riku Korhonen, Eeva Moilanen Source Type: journals

Incorporating Physiological and Biochemical Mechanisms into Pharmacokinetic–Pharmacodynamic Models: A Conceptual Framework*Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract: The aim of this conceptual framework paper is to contribute to the further development of the modelling of effects of drugs or toxic agents by an approach which is based on the underlying physiology and pathology of the biological processes. In general, modelling of data has the purpose (1) to describe experimental data, (2a) to reduce the amount of data resulting from an experiment, e.g. a clinical trial and (2b) to obtain the most relevant parameters, (3) to test hypotheses and (4) to make predictions within the boundaries of experimental conditions, e.g. range of doses tested (interpolation) and out of the bou...
Source: Basic and Clinical Pharmacology and Toxicology - July 21, 2009 Category: Drugs & Pharmacology Authors: Svein G. Dahl, Leon Aarons, Ursula Gundert-Remy, Mats O. Karlsson, Yves-Jacques Schneider, Jean-Louis Steimer, Iñaki F. Trocóniz Source Type: journals

Human Exposure to Triclosan via Toothpaste does not change CYP3A4 Activity or Plasma Concentrations of Thyroid HormonesEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract: Triclosan is an antibacterial compound commonly used in cosmetics and personal care products for everyday use. As previously shown, triclosan is found in the plasma, urine and milk from large parts of different human populations. Recent studies have revealed that triclosan is able to activate the human pregnane X receptor in vitro and thus possibly affecting metabolism of drugs in humans via the induction of CYP3A4. Besides, triclosan has been shown to affect thyroid hormonal levels in rats in vivo. In the present study, we investigated if an everyday exposure to triclosan via triclosan-containing toothpaste for ...
Source: Basic and Clinical Pharmacology and Toxicology - July 20, 2009 Category: Drugs & Pharmacology Authors: Mats Allmyr, Georgios Panagiotidis, Erik Sparve, Ulf Diczfalusy, Gunilla Sandborgh-Englund Source Type: journals

Role of Endocannabinoid System in the Ventral Hippocampus of Rats in the Modulation of Anxiety-Like BehavioursEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract: The effects of unilateral intra-ventral hippocampus injection of URB597, a fatty acid amid hydrolase inhibitor, and AM251, a selective CB1 receptor antagonist, on anxiety-related behaviours using elevated plus-maze test of anxiety were evaluated in the present study. Possible involvement of GABAergic system in those effects of URB597 was also evaluated. Injection of URB597 at the doses of 0.01, 0.1 and 1 [mu]g/rat showed significant anxiogenic-like effects at 0.1 and 1 [mu]g/rat. However, intra-ventral hippocampus injection of AM251 at the doses of 0.001, 0.01 and 0.1 [mu]g/rat did not produce any significant eff...
Source: Basic and Clinical Pharmacology and Toxicology - July 14, 2009 Category: Drugs & Pharmacology Authors: Ali Roohbakhsh, Samaneh Keshavarz, Parisa Hasanein, Mohammad Ebrahim Rezvani, Akbar Hajizadeh Moghaddam Source Type: journals

The Role of Human CYP2C8 and CYP2C9 Variants in Pioglitazone Metabolism In VitroEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract: The cytochrome P450 enzyme CYP2C8 appears to have a major role in pioglitazone metabolism. The present study was conducted to further clarify the role of individual CYPs and of the CYP2C8/9 polymorphisms in the primary metabolism of pioglitazone in vitro. Pioglitazone (2[ndash]400 [mu]M) was incubated with isolated cytochrome P450 enzymes or human liver microsomes, some of them carrying either the CYP2C8*3/*3 genotype (and also the CYP2C9*2/*2 genotype) or the CYP2C8*1/*1 genotype (five samples each). The formation of the primary pioglitazone metabolite M-IV was monitored by HPLC. Enzyme kinetics were estimated a...
Source: Basic and Clinical Pharmacology and Toxicology - July 14, 2009 Category: Drugs & Pharmacology Authors: Eugen Muschler, Jawahar Lal, Alexander Jetter, Anke Rattay, Ulrich Zanger, Gregor Zadoyan, Uwe Fuhr, Julia Kirchheiner Source Type: journals

In Vitro Protective Effect of Hypericum androsaemum Extract Against Oxygen and Nitrogen Reactive SpeciesEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract: Hypericum androsaemum L. (Gutiferae) is a medicinal plant growing in Western Europe that has been used in traditional medicine in the prevention or treatment of liver diseases. Oxidative stress and nitrosative stress are common pathogenetic mechanisms contributing to initiation and progression of hepatic damage in several liver disorders. In the present study, an ethanol:water (4:6) extract from H. androsaemum branches and leaves were evaluated for its putative in vitro scavenging effects on 1,1-diphenyl-2-picrylhydrazil radical, on reactive oxygen species, namely HO[bull], O2[bull][minus], ROO[bull], 1O2 and H2O...
Source: Basic and Clinical Pharmacology and Toxicology - July 14, 2009 Category: Drugs & Pharmacology Authors: Isabel F. Almeida, Eduarda Fernandes, José L.F.C. Lima, Paulo Cardoso Costa, Maria Fernanda Bahia Source Type: journals

Circulating Free Fatty Acids do not Contribute to the Acute Systemic Inflammatory Response. An Experimental Study in Porcine EndotoxaemiaEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
This study was designed to study the pro-inflammatory effects of two free fatty acid concentrations during acute endotoxaemia and controlled comparable levels of plasma glucose and insulin. Twenty pigs were anaesthetized and mechanically ventilated. Pigs were randomized to two different, constant Intralipid® infusion rates, throughout observation. All pigs were administered continuous intravenous infusion of endotoxin and subjected to controlled levels of p-glucose (4.5 mmol/l) and insulin by use of a hyperinsulinaemic euglycaemic clamp. Changes in circulating tumour necrosis factor-[alpha] (TNF-[alpha]), interleukin (IL)...
Source: Basic and Clinical Pharmacology and Toxicology - July 13, 2009 Category: Drugs & Pharmacology Authors: Mads Buhl, Jakob Gjedsted, Asger Granfeldt, Pernille Ø. Larsen, Michelle Chew, Niels Møller, Else Tønnesen Source Type: journals

New Haemolytic Potential Assay on an Alternative Insect ModelEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract: A new screening test of a haemolytic potential is presented on Spodoptera larvae in vivo. The assay was evaluated using phenylhydrazine, the well-known xenobiotic which induces haemolysis in mammals. Haemocyte disintegration causes changes in total haemocyte counts and differentials. It is shown that only qualitative evaluation of panoptically stained haemolymph smears is sufficient, fast and cheap to detect haemolytic potential. The presented assay also prevents unneeded, non-ethical use of vertebrates. (Source: Basic and Clinical Pharmacology and Toxicology)
Source: Basic and Clinical Pharmacology and Toxicology - July 12, 2009 Category: Drugs & Pharmacology Authors: Josef Berger Source Type: journals

Immunological Response to (1,4)-α-d-Glucan in the Lung and Spleen of Endotoxin-Stimulated Juvenile RatsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract: We investigated the effects of (1,4)-[alpha]-D-glucan ([alpha]-DG), a novel immune stimulatory drug from Tinospora cordifolia, on the concentration of pro- and anti-inflammatory cytokines (interleukin [IL]-1[beta], IL-6, tumour necrosis factor-[alpha] [TNF-[alpha]], [gamma]-interferon [IFN-[gamma]] and IL-10) in the lung and spleen of endotoxin-stimulated juvenile rats. Experimental groups (n = 16/group) included controls with an intraperitoneal injection of saline, endotoxaemic rats with a non-lethal dose of 10 mg/kg Escherichia coli endotoxin, and endotoxaemic rats treated with two doses of 10 mg/kg [alpha]-DG,...
Source: Basic and Clinical Pharmacology and Toxicology - July 12, 2009 Category: Drugs & Pharmacology Authors: Ectis A. Velazquez, Dai Kimura, Dan Torbati, Cheppail Ramachandran, Balagangadhar R. Totapally Source Type: journals

Mercury Exposure Increases Circulating Net Matrix Metalloproteinase (MMP)-2 and MMP-9 ActivitiesEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract: Mercury (Hg) exposure causes health problems that may result from increased oxidative stress and matrix metalloproteinase (MMP) levels. We investigated whether there is an association between the circulating levels of MMP-2, MMP-9, their endogenous inhibitors (the tissue inhibitors of metalloproteinases; TIMPs) and the circulating Hg levels in 159 subjects environmentally exposed to Hg. Blood and plasma Hg were determined by inductively coupled plasma-mass spectrometry (ICP-MS). MMP and TIMP concentrations were measured in plasma samples by gelatin zymography and ELISA respectively. Thiobarbituric acid-reactive s...
Source: Basic and Clinical Pharmacology and Toxicology - July 6, 2009 Category: Drugs & Pharmacology Authors: Anna L. B. Jacob-Ferreira, Carlos J. S. Passos, Alceu A. Jordão, Myriam Fillion, Donna Mergler, Mélanie Lemire, Raquel F. Gerlach, Fernando Barbosa Jr, Jose E. Tanus-Santos Source Type: journals

Progression of Lipid Peroxidation Measured as Thiobarbituric Acid Reactive Substances, Damage to DNA and Histopathological Changes in the Liver of Rats Subjected to a Methionine–Choline-Deficient DietEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract: Methionine[ndash]choline-deficient diet represents a model for the study of the pathogenesis of steatohepatitis. Male rats were divided into three groups, the first group receiving a control diet and the other two groups receiving a methionine[ndash]choline-deficient diet for 1 month (MCD1) and for 2 months (MCD2), respectively. The livers of the animals were collected for the determination of vitamin E, thiobarbituric acid reactive substances (TBARS), GSH concentration, DNA damages, and for histopathological evaluation. The hepatic TBARS and GSH content was higher (P < 0.05) in the groups receiving the experimen...
Source: Basic and Clinical Pharmacology and Toxicology - July 5, 2009 Category: Drugs & Pharmacology Authors: Alceu Afonso Jordao, Marcia Elena Zanutto, Fernanda Aparecida Domenici, Guilherme Vannucchi Portari, Andréa Oliveira Cecchi, Sergio Zucoloto, Helio Vannucchi Source Type: journals

Antinociceptive Activity of a New Benzofuranone Derived from a ChalconeEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract: Chalcones represent an important group of natural or synthetic compounds with a variety of biological activities including antinociceptive and anti-inflammatory ones. The aim of this work was the synthesis of a new benzofuranone compound and evaluation of its antinociceptive potential in mice. The new benzofuranone 4 was synthesized from chalcone 3. The antinociceptive activity of 4 was determined by writhing, formalin, capsaicin, and glutamate and hot-plate tests. Compound 4 caused potent and dose-related inhibition against the writhing test with ID50 6.1 (5.1[minus]7.6) [mu]mol/kg, i.p., being about 15 times mo...
Source: Basic and Clinical Pharmacology and Toxicology - July 4, 2009 Category: Drugs & Pharmacology Authors: Pâmela Padaratz, Mauricio Fracasso, Fátima de Campos-Buzzi, Rogério Corrêa, Rivaldo Niero, Franco Delle Monache, Valdir Cechinel-Filho Source Type: journals