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中国临床药理学与治疗学 ›› 2020, Vol. 25 ›› Issue (6): 686-700.doi: 10.12092/j.issn.1009-2501.2020.06.012

• 综述与讲座 • 上一篇    下一篇

疾病状态下II相代谢酶表达和活性的研究进展

张钰, 彭英, 王广基, 孙建国   

  1. 中国药科大学药物代谢动力学重点实验室,南京 210009,江苏
  • 收稿日期:2020-05-08 出版日期:2020-06-26 发布日期:2020-07-09
  • 通讯作者: 孙建国,男,博士,研究员,研究方向:药物代谢动力学。Tel: 13915990907 E-mail: jgsun@cpu.edu.cn
  • 作者简介:张钰,女,硕士研究生,研究方向:药物代谢动力学。Tel:18012203663 E-mail:zhangyu0205com@sina.com
  • 基金资助:
    国家自然科学基金项目(81773987);国际合作重点项目(2017YFE0109600)

Advances in study of phase II metabolic enzyme expression and activity under diseases status

ZHANG Yu, PENG Ying, WANG Guangji, SUN Jianguo   

  1. Key Laboratory of Drug Metabolism and Pharmacokinetics, China Pharmaceutical University, Nanjing 210009, Jiangsu, China
  • Received:2020-05-08 Online:2020-06-26 Published:2020-07-09

摘要: 通常认为II相代谢为解毒和灭活过程,在药物代谢和解毒过程中酶催化的结合反应起着十分重要的作用。在疾病状态下,药物II相代谢酶的表达和活性也会发生改变。疾病对人体药物代谢酶的影响可能具有同工酶选择性。研究疾病状态下II相代谢酶的变化,有助于了解II相代谢酶的调节机制,对于进一步研究以指导临床合理用药及疾病的预防治疗有重要作用。本文综述了II相代谢酶的分布及功能,阐述了它们在肝脏疾病、消化道疾病、糖尿病、癌症、神经退行性疾病、妇科疾病及心血管疾病下表达/活性的变化,探讨不同疾病下及疾病进展中各种II相代谢酶表达与活性的变化及差异的产生原因。

关键词: II相代谢酶, 疾病, 基因表达, 酶活性

Abstract: Phase II metabolism is generally considered to be a process of detoxification and inactivation. The enzymatic binding reaction plays a very important role in the process of drug metabolism and detoxification. Under disease status, the expression and activity of drug phase II metabolic enzymes will also change. The effects of disease on human drug metabolism enzymes may be isozyme selective. Studying the changes of phase II metabolic enzymes under disease status is helpful for understanding the regulation mechanism of phase II metabolic enzymes, and has an important role in further research to guide clinical rational drug usage and disease prevention and treatment. This article reviewed the distribution and function of phase II metabolic enzymes, and described their changes in expression/activity in liver disease, digestive tract disease, diabetes, cancer, neurodegenerative disease, glynecological disease and cardiovascular disease. The changes and causes of various phase II metabolizing enzymes under different disease and disease progression were also discussed.

Key words: phase II metabolic enzyme, disease, gene expression, enzyme activity

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