Formation of an Antibacterial Metabolite from a New Macrolide Compound 23-O-Benzyl-5-mycaminosyl-tylonolide (TMC-101), by a Hepatic Microsomal Drug-Metabolizing Enzyme System
スポンサーリンク
概要
- 論文の詳細を見る
Upon incubation of 23-O-benzyl-5-mycaminosyl-tylonolide (TMC-101) with liver microsomes in the presence of an nicotinamide adenine dinucleotide phosphate-generating system, at least four metabolites were formed : two of them were also formed by an enzyme (s) in rat serum. One of the metabolites formed by liver microsomes possessed antibacterial activity comparable to TMC-101 as examined by bioautography using Micrococcus luteus ATCC 9341 as a tester strain. Incubation of TMC-101 with rat serum degraded most of the parent compound and did not form the active metabolite. The capacity of liver microsomes to produce the active metabolite was increased by pretreatment of rats with 3-methylcholanthrene, phenobarbital and polychlorinated biphenyl. The metabolite with the antibacterial activity was estimated not to be formed by the N-demethylation of TMC-101,and was chemically unstable.
- 公益社団法人日本薬学会の論文
著者
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KITADA Mitsukazu
Division of Pharmacy, Chiba University Hospital
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KAMATAKI Tetsuya
Division of Drug Metabolism, Faculty of Pharmaceuti-cal Sciences, Hokkaido University
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Kamataki T
Hokkaido Univ. Sapporo Jpn
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Kamataki Tetsuya
Department Of Pharmacology School Of Medicine Keio University:department Of Analytical Biochemistry
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NAKURA Hironori
Division of Analytical Biochemistry, Faculty of Pharmaceutical Sciences, Hokkaido University
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OHI Hiroaki
Division of Analytical Biochemistry, Faculty of Pharmaceutical Sciences, Hokkaido University
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MIURA Toshiaki
Division of Analytical Biochemistry, Faculty of Pharmaceutical Sciences, Hokkaido University
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FUJIWARA Tatsuro
Division of Analytical Biochemistry, Faculty of Pharmaceutical Sciences, Hokkaido University
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ISHIZONE Hiroyuki
Division of Analytical Biochemistry, Faculty of Pharmaceutical Sciences, Hokkaido University
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YOKOI Tsuyoshi
Division of Analytical Biochemistry, Faculty of Pharmaceutical Sciences, Hokkaido University
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Miura Toshiaki
Division Of Analytical Biochemistry Faculty Of Pharmaceutical Sciences Hokkaido University:explorato
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Miura Toshiaki
Department Of Applied Physics And Applied Mechanics Institute Of Industrial Science University Of To
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Kamataki Tetsuya
Division Of Analytical Biochemistry Faculty Of Pharmaceutical Sciences Hokkaido University
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Fujiwara Tatsuro
Division Of Analytical Biochemistry Faculty Of Pharmaceutical Sciences Hokkaido University:explorato
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Kitada Mitsukazu
Division Of Analytical Biochemistry Faculty Of Pharmaceutical Sciences Hokkaido University
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Ohi Hiroaki
Division Of Analytical Biochemistry Faculty Of Pharmaceutical Sciences Hokkaido University:explorato
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Yokoi Tsuyoshi
Division Of Analytical Biochemistry Faculty Of Pharmaceutical Sciences Hokkaido University:explorato
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Komori Masayuki
Division Of Analytical Biochemistry Faculty Of Pharmaceutical Sciences Hokkaido University
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Nakura Hironori
Division Of Analytical Biochemistry Faculty Of Pharmaceutical Sciences Hokkaido University:explorato
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Ishizone Hiroyuki
Division Of Analytical Biochemistry Faculty Of Pharmaceutical Sciences Hokkaido University:explorato
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Kamataki Tetsuya
Lab. Drug Metab. Fac. Pharm. Sci. Hokkaido University
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