人葡糖醛酸基转移酶介导的黄酮Ⅱ相代谢研究进展

PhaseⅡ metabolism of flavonoids mediated by human glucuronosyltransferase:an advanced research

人葡糖醛酸基转移酶(UGT)同工酶在黄酮类化合物Ⅱ相代谢反应中呈重要的作用。本综述总结了近年来国内外学者对黄酮类化合物Ⅱ相代谢中UGT的研究情况,包括各同工酶间的底物差异,结构-代谢活性关系,基因多态性的影响以及黄酮对UGT调控的研究。结果表明,人UGT1A1,1A3,1A8,1A9,1A10和2B15主要参与了广泛黄酮类化合物的葡醛酸结合反应,而UGT1A5,1A7和2B7对黄酮代谢的作用有待于进一步研究证明,UGT的基因多态性、结构-代谢关系、调控机制为生物黄酮的合理利用以及此类化合物的合理药物设计提供了重要的参考依据。

Glucuronosyltransferase （UGT） isoforms play an important role on phase Ⅱ metabolism of flavonoids. The advanced research of UGT on the phase Ⅱ metabolism of flavonoids by domestic and aboard scholars in recent years was summarized, including the substrate difference between each isozyme, the relationships between the chemical structures and metabolic activities, the influences of gene polymorphism and the regulation of flavonoids to UGT. The glueuronidation of flavonoids is mediated by human UGTIAI, IA3, IA8, IA9, IA10, 2B15, and the importances of UGT1AS, IAT, 2B7 to flavonoids metabolism are still on progress. The UGT gene polymorphism, strueture-metabolism relationships and regulation mechanism provide important references to the reasonable bioflavonoids development and rational flavonoid drug design.