文章基本信息

标题：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
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作者：Hironori NAKURA ; Hiroaki OHI ; Toshiaki MIURA 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：1991
卷号：14
期号：7
页码：377-383
DOI：10.1248/bpb1978.14.377
出版社：The Pharmaceutical Society of Japan
摘要：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.
关键词：antibacterial activity