Delwaide P A
Rev Med Liege. 1998 Nov;53(11):700-10.
The hepatic cytochrome P450 enzymes (CYP450) play a prominent part in the metabolism of drugs, toxicants and some endogenous compounds. After a brief recall of their biochemical properties, the recent nomenclature is proposed. They are members of a large superfamily with various functions; the specialization of 3 families, CYP1, CYP2, CYP3 towards the metabolism of foreign and artificial compounds gives way to some evolutive considerations. Three main features are characteristic: these enzymes are poorly selective as a matter of substrates; some display genetic polymorphism; some are highly inducible. The mechanism of induction is detailed for CYP1A1. The consequences in pharmacotherapy are deduced: the CYP450 are the main cause of the variability in pharmacokinetics, of drug interactions and of drug adverse events of type II. Their implication in carcinogenesis, although controversial, deserves attention and requires further studies.
肝脏细胞色素P450酶(CYP450)在药物、毒物及一些内源性化合物的代谢过程中发挥着重要作用。在简要回顾其生化特性之后,介绍了最新的命名法。它们是具有多种功能的大型超家族成员;CYP1、CYP2、CYP3这三个家族对外源性和人工合成化合物代谢的特异性引发了一些进化方面的思考。有三个主要特征:这些酶作为底物的选择性较差;一些表现出遗传多态性;一些具有高度可诱导性。详细阐述了CYP1A1的诱导机制。由此推断出在药物治疗中的后果:CYP450是药代动力学变异性、药物相互作用及II型药物不良事件的主要原因。它们在致癌作用中的影响虽然存在争议,但值得关注并需要进一步研究。