Ⅱ相代谢及其酶的研究进展

摘要/Abstract

摘要： 以结合反应为特征的Ⅱ相药物代谢是机体处置药物重要环节,主要包括葡萄糖醛酸化、乙酰化、甲基化、谷胱甘肽化、硫酸化等结合反应。不同基团对应的结合反应均由多个同类基因或超基因家族介导催化完成。Ⅱ相代谢反应都具有各自不同的反应特征与各自不同的功能意义。Ⅱ相药物代谢酶活性受联合用药影响会导致临床药物相互作用,其基因多态性一方面会影响内源性物质的代谢,可能导致某些疾病发生率升高,同时也会影响外源性物质的代谢,引起药物疗效的改变或毒性反应的发生。

关键词: Ⅱ相代谢, Ⅱ相代谢酶, 药物代谢

Abstract: Phase Ⅱ drug-metabolizing reaction, characterized by the conjugation reaction, is an important way of body drug disposition. Glucuronidation, acetylation, methylation, glutathione conjugation reaction, and sulphation represent different conjugation reactions and are catalyzed by some similar genes or gene superfamily respectively. All these phase Ⅱ metabolic reactions have their own different characteristics and functional significance. Drug induced significant change of phase Ⅱ drug metabolizing enzyme activity may lead to clinical drug interactions. The genetic polymorphisms of phase Ⅱdrug metabolizing enzymes will affect the metabolism of endogenous substances, which may lead to the increased incidence of certain diseases, and these polymorphisms also affect the metabolism of exogenous substances, causing toxicity or changes in drug efficacy.

Key words: Phase Ⅱ reaction, Phase Ⅱ metabolism enzyme, Drug metabolism

中图分类号:

R969

石淑亚, 王连生. Ⅱ相代谢及其酶的研究进展[J]. 中国临床药理学与治疗学, 2014, 19(1): 82-89.

SHI Shu-ya, WANG Lian-sheng. Progress in research of phase Ⅱ metabolisms and their enzymes[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2014, 19(1): 82-89.

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