尿苷二磷酸葡萄糖醛酸转移酶与内源性物质的相互作用

尿苷二磷酸葡萄糖醛酸转移酶(UGT)是人体重要的II相代谢酶,代谢药物的同时也代谢许多重要的内源性物质,如胆红素、甲状腺激素、雌激素、雄激素、胆汁酸和5-羟色胺等。该酶对许多内源性物质的代谢是灭活和清除这些内源性物质的关键步骤,能够防止内源性物质累积引发的毒性反应,或及时终止内源性激素的信号防止肿瘤的发生。然而,内源性物质对UGT酶也会产生影响,特别是在一些生理病理条件下,某些内源性物质能够抑制UGT酶活性,影响其参与的代谢反应。将就内源性物质和UGT酶的相互作用做一综述,以引起人们对UGT酶和内源性物质相互作用的关注。关键词:药物代谢;尿苷二磷酸葡萄糖醛酸转移酶;内源性物质

Interaction of uridine diphosphate glucuronic acid transferase and endogenous substances

Uridine diphosphate glucuronic acid transferase (UGT) is an important phase II metabolism enzyme in human body, it metabolites many drugs and endogenous substances. For many endogenous substances, such as bilirubin, thyroid hormones, estrogens, et al, the UGT enzymes are the key enzymes for inactivated and remove endogenous substances. It can prevent toxic effects caused by accumulation. Its termination of endogenous hormone signal can prevent the occurrence of cancer. On the other hand, endogenous substances can affect the enzymes. In some physiological and pathological conditions, some of endogenous substances can inhibit UGT enzymes, and exert an influence on UGT enzymes involved metabolism. This article will make a review on the interaction of endogenous substances and UGT enzymes.