大鼠肝细胞色素P450s对尼古丁的代谢
Nicotine metabolism by rat hepatic cytochrome P450s.
作者信息
Nakayama H, Okuda H, Nakashima T, Imaoka S, Funae Y
机构信息
Department of Pharmacology, Nara Medical University, Kashihara, Japan.
出版信息
Biochem Pharmacol. 1993 Jun 22;45(12):2554-6. doi: 10.1016/0006-2952(93)90238-r.
Many kinds of cytochrome P450s were purified from rat hepatic microsomes, and their role in the metabolization of nicotine in a reconstituted system examined. Of four phenobarbital-inducible P450s, P450 2B1 had the highest nicotine oxidation activity and P450 2B2 showed a low rate of nicotine oxidation, whereas P450 2C6 and 3A2 had no detectable activity toward nicotine. Among eleven other purified cytochrome P450s tested, P450 2C11 had high nicotine oxidation activity and P450 1A2 and 2D1 showed low catalytic activity toward nicotine. The other cytochrome P450s, P450 1A1, 2A1, 2A2, 2C7, 2C12, 2C13, 2E1 and 4A1, had no detectable nicotine oxidation activity. Based on these results, participation of cytochrome P450s in nicotine metabolism in human and animal livers is discussed.
从大鼠肝微粒体中纯化出多种细胞色素P450，并在重组系统中检测了它们在尼古丁代谢中的作用。在四种苯巴比妥诱导的P450中，P450 2B1具有最高的尼古丁氧化活性，P450 2B2的尼古丁氧化速率较低，而P450 2C6和3A2对尼古丁没有可检测到的活性。在测试的其他11种纯化的细胞色素P450中，P450 2C11具有高尼古丁氧化活性，P450 1A2和2D1对尼古丁显示出低催化活性。其他细胞色素P450，P450 1A1、2A1、2A2、2C7、2C12、2C13、2E1和4A1，没有可检测到的尼古丁氧化活性。基于这些结果，讨论了细胞色素P450在人和动物肝脏尼古丁代谢中的参与情况。
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