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  • 标题:p-NITROPHENYL VINYL ETHER, A NOVEL SUBSTRATE FOR THE ASSAY OF CYTOCHROME P-450 DEPENDENT OLEFINIC EPOXIDATION IN HEPATIC MICROSOMES
  • 本地全文:下载
  • 作者:MASAKAZU ISOBE ; TOMOMICHI SONE ; EIGO TAKABATAKE
  • 期刊名称:Biological and Pharmaceutical Bulletin
  • 印刷版ISSN:0918-6158
  • 电子版ISSN:1347-5215
  • 出版年度:1985
  • 卷号:8
  • 期号:8
  • 页码:614-622
  • DOI:10.1248/bpb1978.8.614
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要:p-Nitrophenyl vinyl ether (NPVE) was metabolized to p-nitrophenol and glycolaldehyde via an epoxide by rat hepatic microsomes. The cofactor requirment and effects of monooxygenase inhibitors indicated that the oxidative metabolism of NPVE was mediated by microsomal cytochrome P-450. Epoxide hydrolase plays a minor role, because a strong epoxide hydrolase inhibitor, 3, 3, 3-trichloropropene oxide, showed a weak inhibitory effect on the p-nitrophenol formation. The epoxy intermediate is so labile that the hydrolysis of the epoxide proceeds mostly nonenzymically even at a neutral pH. Induction experiments suggested that NPVE was susceptible to a wide varieties of cytochrome P-450 species. Thus, a convenient and sensitive method for the assay of olefinic epoxidase activity in hepatic microsomes was developed with NPVE as a substrate.
  • 关键词:hepatic metabolism
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