Ⅱ相代谢及其酶的研究进展

Progress in research of phase Ⅱ metabolisms and their enzymes

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。

Phase Ⅱ drug-metabolizing reac tion, characterized by the conjugation reaction, is an important way of body drug disposition. Glucuronidation, acetylation, methylation, glu- tathione conjugation reaction, and sulphation re- present different conjugation reactions and are catalyzed by some similar genes or gene super- family respectively. All these phase Ⅱ metabolic reactions have their own different characteristics and functional significance. Drug induced signifi- cant change of phaseⅡ drug metabolizing en- zyme activity may lead to clinical drug interae-tions. The genetic polymorphisms of phaseⅡ drug metabolizing enzymes will affect the metab- olism of endogenous substances, which may lead to the increased incidence of certain diseases, and these polymorphisms also affect the metabo- lism of exogenous substances, causing toxicity or changes in drug efficacy.