摘要
细胞色素P450(CYP450)在外源及内源物质的生物转化过程中发挥着至关重要的作用,是肝脏中重要的药物代谢酶。CYP450酶活性/含量的改变直接影响了经其代谢的药物在体内的有效量和作用时间,与药效和用药安全性有密切的联系。因此,了解药物对CYP450酶可能存在的诱导或抑制作用是药物研究过程中不可缺少的研究内容。本文综述了近年来研究CYP450酶诱导/抑制水平和机制的试验方法以及在药物、尤其是在天然产物研究中的应用。
Cytochrome P450（CYP450） is the most important enzyme family in liver which plays a crucial role in metabolism of the exogenous and endogenous substances.The change of CYP450s on activity or content is closely related with the effectiveness and safety of their substrate drugs through altering drugs＇ effective doses or response time.Therefore,it is an indispensable research during drug development to understand the potential induction or inhibition effects on CYP450 enzyme.This paper reviewed methodology development of degree evaluation,phenotype analysis and mechanistic investigation of CYP450 enzyme induction/inhibition,as well as their application mainly on natural products.
出处
《中国临床药理学与治疗学》
CAS
CSCD
2011年第5期579-585,共7页
Chinese Journal of Clinical Pharmacology and Therapeutics
基金
国家自然科学基金项目(30701101)
