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Effect of 1,4-Dioxane Solvent on β-Glucuronidation Using Methyl 1,2,3,4-Tetra-O-acetyl-β-D-glucuronate as the Glycosyl Donor
Chem Pharm Bull (Tokyo). 2024;72(4):408-412. doi: 10.1248/cpb.c24-00068.ABSTRACTA facile and selective β-D-glucuronidation of alcohols, such as (-)-menthol, cholestanol, (+)- and (-)-borneols, and 2-adamantanol, using commercially available methyl 1,2,3,4-tetra-O-acetyl-β-D-glucuronate as the glycosyl donor and trimethylsilyl bis(trifluoromethanesulfonyl)imide (Tf2NTMS) (0.5 equivalent) as the activator in 1,4-dioxane at 60 °C gave products in moderate yields. The addition of MS4A increased the β : α ratios of D-glucuronides when cholestanol, (+)-borneol, and 2-adamantanol were used as the acceptor substrate.PMID:3865...
Source: Chemical and Pharmaceutical Bulletin - April 24, 2024 Category: Drugs & Pharmacology Authors: Tetsuya Kajimoto Tianqi Du Kimiyoshi Kaneko Yasuyuki Matsushima Tsuyoshi Miura Source Type: research

In Vitro and in Vivo Study of a Photostable Quinone Compound with Enhanced Therapeutic Efficacy against Chagas Disease
In this study, we elucidated the structure of the light-induced degradation products of compound 2 and probed the correlation between the quinone ring's substituents and its susceptibility to light. Our findings led to the discovery of quinones with significantly enhanced light stability, some of which exhibiting antitrypanosomal activity. The most promising compound was evaluated for drug efficacy in a mouse model of Chagas disease, revealing where a notable reduction in blood parasitemia.PMID:38644164 | DOI:10.1248/cpb.c24-00116 (Source: Chemical and Pharmaceutical Bulletin)
Source: Chemical and Pharmaceutical Bulletin - April 21, 2024 Category: Drugs & Pharmacology Authors: Yutaka Suto Nagisa Inoue Mohammed Suliman Omer Tagod Yoko Onizuka Tomoya Nobuta Mayumi Ishii Daniel Ken Inaoka Kayoko Kanamitsu Noriyuki Yamagiwa Junko Nakajima-Shimada Source Type: research

Discovery of a Novel Lidocaine Metabolite by Human Liver Microsome and Identification of Microbial Species Which Produces the Same Metabolite
In this study, we identified an unknown metabolite of the anaesthetic drug lidocaine, which is metabolised by HLM. By screening for lidocaine metabolic activity in five types of foods (blue cheese, shiitake mushroom, natto, yoghurt, and dry yeast), we found that bacteria isolated from natto reproduced the lidocaine metabolic reaction that occurs in HLM. A fraction containing the unknown lidocaine metabolite was prepared through mass cultivation of a Bacillus subtilis standard strain, ethyl acetate extraction, open column chromatography, and HPLC purification. We identified the unknown metabolite as 3-(2,6-dimethylphenyl)-1...
Source: Chemical and Pharmaceutical Bulletin - April 21, 2024 Category: Drugs & Pharmacology Authors: Sho Hori Hikari Taniguchi Sota Yoshimura Kanako Takeda Ryusei Yamashita Atsushi Kimishima Kazuo Harada Source Type: research

Discovery and Structure-Activity Relationship of a Ryanodine Receptor 2 Inhibitor
Chem Pharm Bull (Tokyo). 2024;72(4):399-407. doi: 10.1248/cpb.c24-00114.ABSTRACTRyanodine receptor 2 (RyR2) is a large Ca2+-release channel in the sarcoplasmic reticulum (SR) of cardiac muscle cells. It serves to release Ca2+ from the SR into the cytosol to initiate muscle contraction. RyR2 overactivation is associated with arrhythmogenic cardiac disease, but few specific inhibitors have been reported so far. Here, we identified an RyR2-selective inhibitor 1 from the chemical compound library and synthesized it from glycolic acid. Synthesis of various derivatives to investigate the structure-activity relationship of each s...
Source: Chemical and Pharmaceutical Bulletin - April 21, 2024 Category: Drugs & Pharmacology Authors: Ryosuke Ishida Xi Zeng Nagomi Kurebayashi Takashi Murayama Shuichi Mori Hiroyuki Kagechika Source Type: research

Exploring the Effectiveness of Carboxymethylated and Crosslinked Albizia Procera Gum in Diltiazem Hydrochloride Matrix Tablets: A Comparative Analysis
This study investigates the efficacy of modified Albizia procera gum as a release-retardant polymer in Diltiazem hydrochloride (DIL) matrix tablets. Carboxymethylated Albizia procera gum (CAP) and ionically crosslinked carboxymethylated Albizia procera gum (Ca-CAP) were utilized, with Ca-CAP synthesized via crosslinking CAP with calcium ions (Ca2+) using calcium chloride (CaCl2). FTIR analysis affirmed polymer compatibility, while Differential scanning calorimetry (DSC) and X-ray diffraction (XRD) assessed thermal behavior and crystallinity, respectively. Zeta potential analysis explored surface charge and electrostatic in...
Source: Chemical and Pharmaceutical Bulletin - April 21, 2024 Category: Drugs & Pharmacology Authors: Sudipta Mukherjee Jasmina Khanam Source Type: research

Comparison of Non-ephedrine Constituents from Ephedra Plants Cultivated in Japan
This study suggests that Ephedra plants have diverse non-ephedrine constituents.PMID:38631893 | DOI:10.1248/cpb.c24-00043 (Source: Chemical and Pharmaceutical Bulletin)
Source: Chemical and Pharmaceutical Bulletin - April 17, 2024 Category: Drugs & Pharmacology Authors: Kengo Hayashi Yuki Miyao Hina Matsui Takao Yamaura Ken Tanaka Mariko Baba Hiroaki Hayashi Source Type: research

Sustained Release Formulation of Hydroxypropyl- β-cyclodextrin Eye Drops Using Xanthan Gum
Chem Pharm Bull (Tokyo). 2024;72(4):381-384. doi: 10.1248/cpb.c24-00059.ABSTRACTBietti's crystalline dystrophy (BCD) is an autosomal recessive chorioretinal degeneration caused by mutations in the CYP4V2 gene. It is characterized by cholesterol accumulation and crystal-like deposits in the retinas. Hydroxypropyl-β-cyclodextrin (HP-β-CyD) exerts therapeutic effects against BCD by reducing lysosomal dysfunction and inhibiting cytotoxicity in induced pluripotent stem cell (iPSC)-RPE cells established from patient-derived iPS cells. However, the ocular retention of HP-β-CyD is low and needs to be improved. Therefore, this s...
Source: Chemical and Pharmaceutical Bulletin - April 14, 2024 Category: Drugs & Pharmacology Authors: Taishi Higashi Taito Goto Risako Onodera Tatsunori Hirotsu Hanako Ohashi Ikeda Keiichi Motoyama Source Type: research

A Method for the Tensile Strength Prediction of Tablets with Differing Powder Plasticities
The objective of this study was to quantitatively evaluate the relationship between the compression properties and tablet strength of powder mixtures. The compression properties of the powder mixtures with different plasticities were evaluated based on the force-displacement curves obtained from the powder compression tests. Heckel and compression energy analyses were performed to evaluate compression properties. During the compression energy analysis, the ratio of plastic deformation energy to elastic deformation energy (Ep/Ee) was assumed to be the plastic deformability of the powder. The quantitative relationship betwee...
Source: Chemical and Pharmaceutical Bulletin - April 10, 2024 Category: Drugs & Pharmacology Authors: Takeru Yano Atsushi Oshiro Shuji Ohsaki Hideya Nakamura Satoru Watano Source Type: research