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中国临床药理学与治疗学 ›› 2011, Vol. 16 ›› Issue (5): 579-585.

• 综述与讲座 • 上一篇    下一篇

细胞色素P450酶诱导/抑制的研究方法及在药物研究中的应用

卜明华1,2, 张颖1, 刘建勋1, 刘东春2   

  1. 1中国中医科学院西苑医院实验研究中心,北京 100091;
    2沈阳药科大学中药学院,沈阳 110016,辽宁
  • 收稿日期:2011-02-15 修回日期:2011-03-12 发布日期:2011-07-08
  • 通讯作者: 张颖,女,副研究员,研究方向:药代动力学。Tel:010-62835641 E-mail:zhyingde@sina.com
  • 作者简介:卜明华,女,硕士研究生,研究方向:生药学。Tel:010-62835641 E-mail:bmh113@126.com
  • 基金资助:
    国家自然科学基金项目(30701101)

Research approaches of CYP450s' induction/inhibition and their application on drug development

BU Ming-hua1,2, ZHANG Ying 1 , LIU Jian-xun1 , LIU Dong-chun2   

  1. 1Research Center, Xiyuan Hospital, China Academy of Chinese Medical Sciences, Beijing 100091, China;
    2College of Traditional Chinese Medicine, Shenyang Pharmaceutical University, Shenyang 110016, Liaoning, China
  • Received:2011-02-15 Revised:2011-03-12 Published:2011-07-08

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。

关键词: 细胞色素P450酶, 诱导/抑制, 研究方法, 药物开发, 天然产物

Abstract: 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.

Key words: Cytochrome P450, Induction/inhibition, Research approaches, Drug development, Natural products

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