摘要
细胞色素P450酶(CYP450s)是肝脏、肠道中参与大多数临床药物I相代谢的最重要的代谢酶家族。近年来有临床报道显示,糖尿病状态下,肝脏CYP450s酶的活性与表达发生改变。本文对CYP3A、CYP2E1、CYP1A2等多种CYP450s酶亚型在糖尿病状态下功能与表达发生的改变进行了评述,分析了种属差异、糖尿病类型以及病程对CYP450s酶活性的影响,并总结了糖尿病状态下因CYP450s酶活性改变造成的药物代谢的变化及药物不良反应。此外,CYP450s酶活性的改变可进一步引发内源性物质代谢改变,加剧胰岛素抵抗等,本文进一步阐述了CYP450s酶活性改变对糖尿病病情发展产生的影响。
Cytochrome P450s （CYP450s） is one of the most important phase-I drug-metabolizing enzyme family that participates in the metabolism of most clinical drugs in liver and intestine. Accumulative evidences have reported that the activities and expressions of hepatic CYP450s exhibited significant alterations under diabetic condition. This article summarizes the induction or inhibition of different isoforms of CYP450s, including CYP3A, CYP2E1 and CYP1A2, in clinical or experimental diabetic conditions, and analyzes the impact of species difference, types and progression of diabetes on CYP450s activity. The article further lists the altered pharmaco- kinetic behaviors as well as adverse drug effects due to alteration of CYP450s in reported diabetic cases. The cor- relations between the altered metabolism of endocrines, the aggravation of insulin resistance, and the alteration of CYP450s activity are illustrated to shed more light on the pathogenesis of diabetes.
出处
《中国药科大学学报》
CAS
CSCD
北大核心
2014年第2期153-160,共8页
Journal of China Pharmaceutical University
基金
国家自然科学基金面上项目资助(No.81373482)
国家自然科学青年基金资助项目(No.81102503)
中央高校基本科研业务费专项基金重点项目资助(No.ZD2014YX0026)~~
