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Chemical & Pharmaceutical Bulletin

Jie Liang, Yun-Xiang Tang, Xiang-Zheng Tang, Hua-Jv Liang, Yamin Gao, Cuiting Fang, Tian-Yu Zhang, Ming Yan
A series of m-amido bromophenol derivatives were designed and synthesized. The compounds were found to potently inhibit the growth of Mycobacterium tuberculosis H37Ra. They also exhibited moderate inhibitory activity against Mycobacterium tuberculosis H37Rv and multidrug-resistant strains. The compounds did not show inhibitory activity against normal Gram-positive and Gram-negative bacteria. Moderate cytotoxicities and good metabolic stability were observed for the selected compounds. The results demonstrated meta-amido bromophenols as a new class of antitubercular agents with good potentials...
January 26, 2019: Chemical & Pharmaceutical Bulletin
Junjie Ma, Xin Ni, Yali Gao, Kun Huang, Yu Wang, Jiaan Liu, Guowei Gong
A series of semicarbazone derivatives bearing phenyl moiety were synthesized and evaluated for the vitro anticancer activities in four human cancer cell lines (HT29, SK-N-SH, MDA-MB-231 and MKN45). Biological evaluation led to the identification of 11q and 11s, which showed excellent anticancer activities against tested cancer cell lines with IC50 values ranging from 0.32 to 1.57 μM, respectively, while exhibiting weak cytotoxicity on the normal cells (HUVEC). Flow cytometric assay for cell cycle and apoptosis revealed that 11q and 11s caused an arrest in the Sub-G1 cell cycle and inhibited proliferation of cancer cells by inducing apoptosis in a dose-dependent manner...
January 24, 2019: Chemical & Pharmaceutical Bulletin
Waree Limwikrant, Tharahpi Aung, Kotchaphan Chooluck, Satit Puttipipatkhachorn, Keiji Yamamoto
In this study, we aimed to investigate the effects of stabilizers and processing parameters on the size reduction of alpha-mangostin (AMG) using high-pressure homogenization (HPH). The solubility of AMG in various stabilizers was studied. Selected stabilizers were used to prepare AMG suspensions by HPH under different conditions. After HPH, the particle size of AMG suspensions with stabilizers significantly decreased to microns. Percent size reduction efficiency of all AMG suspensions with each stabilizer increased with the increase in the number of homogenization cycles...
January 18, 2019: Chemical & Pharmaceutical Bulletin
Si-Peng Wu, Dan Li, Ning Wang, Jin-Cai Hou, Li Zhao
Yiqi Tongluo Granule (YQTL) is a kind of proprietary Chinese medicine, manufactured by China Shineway Pharmaceutical Group Ltd, under the authority of China Food and Drug Administration (CFDA) treating cardiovascular and cerebrovascular diseases such as ischemic stroke in China, however the underlying mechanism of YQTL on treating ischemic stroke has not been revealed. This study is aimed to evaluate the protective effect of YQTL on cerebral ischemia reperfusion (I/R) injury and inquire into its underlying mechanisms...
December 28, 2018: Chemical & Pharmaceutical Bulletin
Xuanhao Li, Xiaobo Wang, Daoxin Hong, Shangyu Zeng, Jinsong Su, Gang Fan, Yi Zhang
Rhodiola is widely consumed in traditional folk medicine and nutraceuticals. To establish a procedure for the hydrogen nuclear magnetic resonance (1 H-NMR) spectroscopic fingerprinting of secondary metabolites from three different Rhodiola species, the variation among three Rhodiola species were studied using 1 H-NMR metabolomics combined with multivariate data analysis. Gene expression programming (GEP) was used to generate a formula to distinguish Rhodiola crenulata from two other Rhodiola species. Finally, high-performance liquid chromatography (HPLC) was used to demonstrate the results...
December 5, 2018: Chemical & Pharmaceutical Bulletin
Shalom P de O Assis, Moara T da Silva, Filipe Torres da Silva, Mirella P Sant'Anna, Carolina M B de Albuquerque Tenório, Caroline F Brito Dos Santos, Caíque S M da Fonseca, Gustavo Seabra, Vera L M Lima, Ronaldo N de Oliveira
Phthalimido-alkyl-1H-1,2,3-triazole derivatives 3a-d and 4a-d were efficiently synthesized using 1,3-dipolar cycloaddition reaction. Anti-inflammatory activity and toxicity studies were performed. The results demonstrated that all the tested compounds reduced carrageenan-induced paw edema and indicated no lethality for toxicity against Artemia salina and acute toxicity in vivo (LD50 up to 1 g kg -1 ). Furthermore, the structure of phthalimide linked to phenyl group proved to be more active than the compounds containing benzothiazole moiety...
2019: Chemical & Pharmaceutical Bulletin
Elizabeth Mary Mathew, Sudheer Moorkoth, Pankaj D Rane, Leslie Lewis, Pragna Rao
25-Hydroxyvitamin D (25-(OH)D) deficiency is recently been described as one of the multiple factors responsible for pediatric seizures. 25-Hydroxyvitamin D3 and 25-Hydroxyvitamin D2 are the well-known markers to determine Vitamin D status. In this work we report the development of a sensitive and cost effective HPLC technique for the quantification of the vitamin D metabolites from dried blood spot samples (DBS). The metabolites were extracted using acetonitrile-methanol-0.1% formic acid (60 : 20 : 20 (v/v)) and analyzed on an Acclaim C18 column (150 × 4...
2019: Chemical & Pharmaceutical Bulletin
Masafumi Okawa, Ryo Akahoshi, Kyoko Kawasaki, Daisuke Nakano, Ryota Tsuchihashi, Junei Kinjo, Toshihiro Nohara
Two new triterpene glycosides, 24-deoxyoxytrogenin 3-O-α-L-rhamnopyranosyl (1→2)[β-D-glucopyranosyl]-β-D-galactopyranosyl (1→2)-β-D-glucuronopyranoside and sophoradiol 3-O-α-L-rhamnopyranosyl (1→2)-β-D-glucuronopyranosyl (1→2)-β-D-glucuronopyranoside with four known glycosides were isolated from a Chinese natural medicine, the roots of Uraria crinita (L.) DESV. Their structures were determined by chemical and spectral methods.
2019: Chemical & Pharmaceutical Bulletin
Huijie Liu, Xuejuan Wang, Hanlin Yang, Yan Zhao, Shengping Ji, Hui Ma, Yiting Zhou, Yanjie Wang, Hongan Zhang, Wenyan Jiang, Chunyan Fang, Lingjun Feng, Xuejian Wang
Aminopeptidase N, also known as CD13, is a transmembrance protease with many functions. CD13 is involved in inflammatory diseases and cancers. A convenient and reliable laboratory test method for detecting the suppressing effects of enzyme activity would be useful for study of CD13 inhibitors. Porcine CD13 (pCD13) was traditionally considered an enzyme source but has significant practical disadvantages. pCD13 is not a human source, and the accuracy and reliability of experimental results are greatly reduced...
2019: Chemical & Pharmaceutical Bulletin
Noriyasu Hada, Yuna Umeda, Hiromi Kumada, Yoshinori Shimazaki, Kimiaki Yamano, Frank Schweizer, Naohiro Oshima, Tadahiro Takeda, Fumiyuki Kiuchi
Stereocontrolled syntheses of biotin-labeled oligosaccharide portions containing the non reducing end oligosaccharides of glycosphingolipids from Ascaris suum have been accomplished. Galα1→3GalNAcβ1→OR (1), Galβ1→3Galα1→3GalNAcβ1→OR (2), Galβ1→6Galα1→3GalNAcβ1→OR (3), Galβ1→6(Galβ1→3)Galα1→3GalNAcβ1→OR (4) and GlcNAcβ1→6Galβ1→6(Galβ1→3)Galα1→3GalNAcβ1→OR (5) (R = biotinylated probe) were synthesized by stepwise condensation (1-4) and block synthesis (5) using 5-(methoxycarbonylpentyl) 2-O-benzoyl-3-O-2-napthylmethyl-4,6-O-di-tert-butylsilylene-α-D-galactopyranosyl-(1→3)-4,6-O-benzylidene-2-deoxy-2-phthalimido-β-D-galactopyranoside (12) as a common precursor...
2019: Chemical & Pharmaceutical Bulletin
Yue-Juan Zhang, Xiao-Long Liu, Wen-Ming Wang, Cheng Chen, Mu-Han Zhao, Ke-Wu Yang
Superbug infection caused by metallo-β-lactamases (MβLs) is a global public health threat. Previous studies reported that the thioesters specifically inhibited the B3 subclass MβL L1. In this work, nine amino acid thioesters 1-9 were synthesized, the activity evaluation revealed that all of these molecules exhibited broad-spectrum inhibitory efficacy against ImiS, IMP-1, NDM-1, and L1, with IC50 values range of 0.02-54.9 µM (except 5 and 7 on NDM-1), and 1 was found to be the best inhibitor with IC50 range of 0...
2019: Chemical & Pharmaceutical Bulletin
Toshinori Suzuki, Hiroki Ota, Yuma Namba, Toshifumi Fujino
When a neutral solution of a nucleoside mixture was irradiated with UV light having wavelength longer than 300 nm, addition of salicylic acid to the solution greatly accelerated the reaction of thymidine. The UV light irradiation of thymidine solution in the presence of salicylic acid resulted in four major product peaks in HPLC. All the products were identified as isomers of cyclobutane thymidine dimers by MS and NMR. The cyclobutane thymidine dimers were generated from thymidine almost exclusively. UV irradiation with the longer wavelength of 350 nm induced almost no reaction...
2019: Chemical & Pharmaceutical Bulletin
Zhi-Gang Sun, Yun-Jie Xu, Jian-Fei Xu, Qi-Xing Liu, Yu-Shun Yang, Hai-Liang Zhu
Broadened antibacterial activity was introduced to rhodanine derivatives targeting Mycobacterial tuberculosis enoyl-acyl carrier protein reductase (Mtb InhA) by recruiting feature of xacins to bring DNA Gyrase B inhibitory capability. This is significant for preventing further bacterial injections in the tuberculosis treatment. The most potent compound Cy14 suggested comparable bioactivity (IC50  = 3.18 µM for Mtb InhA; IC50  = 10 nM for DNA Gyrase B) with positive controls. Structure-activity relationship discussion and molecular docking model revealed the significance of rhodanine moiety and derived methoxyl on meta-position, pointing out orientations for future modification...
2019: Chemical & Pharmaceutical Bulletin
Kazunori Inaba, Toshiharu Oie, Hiroko Otake, Takeshi Kotake, Noriaki Nagai
The evaluation of the dissolution profile of hypnotic drugs is important to promote switching from original products to generic products by removing distrust in generic hypnotics. In this study, we investigated differences in the dissolution profiles between original and generic products (GE-D, GE-S, and GE-T) in commercially available zolpidem tartrate (ZOL) products using the HPLC method using a connected microdialysis probe (microdialysis-HPLC method). Although the degree of hardness and the disintegration time were not different among the original, GE-S, and GE-T, GE-D was 1...
2019: Chemical & Pharmaceutical Bulletin
Hidehito Takano, Shinya Uchida, Yasuharu Kashiwagura, Shimako Tanaka, Akio Hakamata, Keiichi Odagiri, Naoki Inui, Hiroshi Watanabe, Noriyuki Namiki
Orally disintegrating tablets (ODTs), which are administered without water, are beneficial for elderly patients and patients with dysphagia. Masking the unpleasant taste of a drug is an important factor associated with adherence of patients consuming ODTs. We prepared cocoa powder-containing ODTs of bitter-tasting rebamipide (rebamipide chocolet) and evaluated their clinical palatability. We prepared rebamipide ODTs by adding a sweetener and 0, 2.5, 5, and 10% cocoa powder (Ch0-ODTs, Ch2.5-ODTs, Ch5-ODTs, and Ch10-ODTs, respectively)...
2019: Chemical & Pharmaceutical Bulletin
Kazuhiro Matsuura, Honami Kojima, Tamami Haraguchi, Miyako Yoshida, Satoshi Suzuki, Tatsuya Suzuki, Shuichi Ando, Takahiro Uchida
The purpose of this study was to prepare poly(lactide-co-glycolide) (PLGA) microspheres (MS) loaded with itraconazole (ITCZ) or miconazole (MCZ) under different evaporation temperatures (25 or 40°C) using an oil-in-water emulsion solvent evaporation method in order to evaluate the initial burst release of drug. Loading efficiencies were comparatively good and the diameters of prepared drug-loaded PLGA MS were around 20 µm in all formulations. The release rates of ITCZ-PLGA MS prepared at 40°C showed a significantly restricted release profile compared with the corresponding ITCZ-PLGA MS prepared at 25°C...
2019: Chemical & Pharmaceutical Bulletin
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2019: Chemical & Pharmaceutical Bulletin
Tomoyo Kamei, Yuta Kimura, Jyunichi Koyanagi, Kaori Matsumoto, Tetsuya Hasegawa, Masayuki Akimoto, Tamiko Takahashi
The absolute configuration of (+)-4-(6-methoxy-2-naphthyl)butan-2-ol ((+)-MNBO), a nabumetone metabolite, was determined using 1-fluoroindan-1-carboxylic acid (FICA). Both enantiomers of the FICA methyl esters were derivatized to diastereomeric esters of (+)-MNBO by an ester exchange reaction. The results of 1 H- and 19 F-NMR spectroscopy of the diastereomeric FICA esters of (+)-MNBO confirmed the absolute configuration of (+)-MNBO was (S).
2019: Chemical & Pharmaceutical Bulletin
Minoru Ozeki, Ayumi Hachino, Takashi Shigeta, Aya Niki, Natsuko Kobayashi, Hideki Mizutani, Akihiro Nakamura, Ayano Horie, Kenji Arimitsu, Tetsuya Kajimoto, Shinzo Hosoi, Hiroki Iwasaki, Naoto Kojima, Masayuki Yamashita, Ikuo Kawasaki
A facile and convenient synthesis of trisubstituted (E)-α,β-unsaturated esters was developed by improving our previously established method. The new method circumvented the separation of the intermediates, which have an activating group of the hydroxyl group in β-hydroxy esters, furnishing α,β-unsaturated esters in shorter steps than the previous method: an acetylation of β-hydroxy group and subsequent E1cB reaction proceeded in tandem. In addition, the new method can not only employ a diastereomeric mixture of the substrate for the E1cB reaction, it has a wide substrate scope as well, which would enable the synthesis of various trisubstituted (E)-α,β-unsaturated esters...
2019: Chemical & Pharmaceutical Bulletin
Kazuhiro Yamamoto, Akira Kotani, Yuzuru Hayashi, Hideki Hakamata
The present study proposes a method for the assessment of repeatability in supercritical fluid chromatography with electrochemical detection (SFC-ECD), based on the ISO 11843 part 7 (ISO 11843-7:2018) which can theoretically provide detection limits and standard deviation (S.D.) through the stochastic properties of baseline noise without repetitive measurements of real samples. On the baseline noise of SFC-ECD, large-amplitude and periodic noises with less than 0.05 Hz were observed, and the power spectrum of the baseline noise showed 1/f fluctuation (f = frequency)...
2019: Chemical & Pharmaceutical Bulletin
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