尿苷二磷酸葡萄糖醛酸轉移酶(UGT)是人體重要的II相代謝酶,代謝藥物的同時也代謝許多重要的內(nèi)源性物質,如膽紅素、甲狀腺激素、雌激素、雄激素、膽汁酸和5-羥色胺等。該酶對許多內(nèi)源性物質的代謝是滅活和清除這些內(nèi)源性物質的關鍵步驟,能夠防止內(nèi)源性物質累積引發(fā)的毒性反應,或及時終止內(nèi)源性激素的信號防止腫瘤的發(fā)生。然而,內(nèi)源性物質對UGT酶也會產(chǎn)生影響,特別是在一些生理病理條件下,某些內(nèi)源性物質能夠抑制UGT酶活性,影響其參與的代謝反應。將就內(nèi)源性物質和UGT酶的相互作用做一綜述,以引起人們對UGT酶和內(nèi)源性物質相互作用的關注。關鍵詞:藥物代謝;尿苷二磷酸葡萄糖醛酸轉移酶;內(nèi)源性物質

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.