p-Nitrophenyl vinyl ether, a novel substrate for the assay of cytochrome P-450 dependent olefinic epoxidation in hepatic microsomes.
p-Nitrophenyl vinyl ether, a novel substrate for the assay of cytochrome P-450 dependent olefinic epoxidation in hepatic microsomes.
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对硝基苯基乙烯基醚，一种用于检测肝微粒体中细胞色素 P-450 依赖性烯属环氧化作用的新型底物。
DOI：
10.1248/bpb1978.8.614
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发表时间：
1985
期刊：
影响因子：
--
通讯作者：
E. Takabatake
中科院分区：
文献类型：
--
作者：
M. Isobe;T. Sone;E. Takabatake
对硝基苯基乙烯基醚（NPVE）在大鼠肝微粒体中通过环氧化物代谢为对硝基苯酚和乙醇醛。辅因子的需要和单加氧酶抑制剂的作用表明，NPVE的氧化代谢是由微粒体细胞色素P-450介导的。环氧化物水解酶起次要作用，因为强环氧化物水解酶抑制剂3，3，3-三氯环氧丙烷对对硝基苯酚的形成显示出弱抑制作用。环氧中间体是如此不稳定的环氧化物的水解进行大多nonenzymically即使在中性pH值。诱导实验表明，NPVE是敏感的细胞色素P-450种类繁多。因此，一个方便和灵敏的方法测定烯环氧酶活性的肝微粒体与NPVE作为底物。
p-Nitrophenyl vinyl ether (NPVE) was metabolized to p-nitrophenol and glycolaldehyde via an epoxide by rat hepatic microsomes. The cofactor requirement 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.
丙烯腈体外代谢为2-氰基环氧乙烷，与谷胱甘肽反应，与蛋白质和核酸不可逆结合。
影响因子：
11.2
作者：
Guengerich,FP;Geiger,LE;Hogy,LL;Wright,PL
通讯作者：
Wright,PL