尿苷二磷酸葡萄糖醛酸轉(zhuǎn)移酶(UGT)是人體重要的II相代謝酶,代謝藥物的同時(shí)也代謝許多重要的內(nèi)源性物質(zhì),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(duì)許多內(nèi)源性物質(zhì)的代謝是滅活和清除這些內(nèi)源性物質(zhì)的關(guān)鍵步驟,能夠防止內(nèi)源性物質(zhì)累積引發(fā)的毒性反應(yīng),或及時(shí)終止內(nèi)源性激素的信號(hào)防止腫瘤的發(fā)生。然而,內(nèi)源性物質(zhì)對(duì)UGT酶也會(huì)產(chǎn)生影響,特別是在一些生理病理?xiàng)l件下,某些內(nèi)源性物質(zhì)能夠抑制UGT酶活性,影響其參與的代謝反應(yīng)。將就內(nèi)源性物質(zhì)和UGT酶的相互作用做一綜述,以引起人們對(duì)UGT酶和內(nèi)源性物質(zhì)相互作用的關(guān)注。關(guān)鍵詞:藥物代謝;尿苷二磷酸葡萄糖醛酸轉(zhuǎn)移酶;內(nèi)源性物質(zhì)

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.