尿苷二磷酸葡萄糖醛酸转移酶1A1（UGT1A1）是哺乳动物体内分布的一种重要的Ⅱ相代谢酶，其不仅介导了大量临床药物、毒物的代谢清除，还是机体参与内源性毒性物质胆红素代谢清除的唯一代谢酶。药物或食品中的化学成分对UGT1A1的强烈抑制会引发多种不良反应，如药物/草药-药物相互作用、高胆红素血症、肝功能异常及神经毒性等。近年来，研究发现许多草药提取物及其化学成分可通过强效抑制UGT1A1引发药物-草药相互作用等不良反应。结合药物代谢及药物毒理学相关领域的新近研究进展，系统总结了UGT1A1抑制剂筛选与评价常用方法，以及中草药化学成分对UGT1A1抑制作用的研究进展。上述信息对于临床安全合理的使用中草药，尤其是在中西药联用或中药方剂使用过程中尽可能避免因UGT1A1抑制引发的不良反应，具有重要指导意义。

UDP-glucuronosyltransferase 1A1 (UGT1A1) is a key conjugative enzyme distributed in mammalian tissues. UGT1A1 is crucial for the detoxification of many clinical drugs and toxins, and is also the sole physiologically relevant enzyme participating in the metabolic elimination of bilirubin, an endogenous toxic metabolite. Strong inhibition on the catalytic activity of UGT1A1 by therapeutic drugs or chemical constitutes in herb or foods could trigger clinical adverse reactions, such as drug/herb-drug interactions, hyperbilirubinemia, hepatotoxicity and neurotoxicity. Recently, herb extracts and their chemical ingredients have been reported to exhibit strong inhibitory effects on UGT1A1 and may cause several adverse reactions. This review systemically summarizes the currently used methods for the screening and characterization of UGT1A1 inhibitors, and the inhibitory effects of herb extracts and their constitutes on UGT1A1, on the basis of the recent advances in the fields of drug metabolism and drug toxicology. All information and knowledge presented in this review will be very helpful for the reasonable and safety usage of Chinese Herbal Medicines in clinic, especially for avoiding the occurrence of adverse reactions via UGT1A1 inhibition when herb medicines were used combined with clinical drugs.

国家自然科学基金（81773687，81703606，81573501,81473181）；国家重点研发计划（2017YFC1700200，2017YFC1702000）；国家科技重大专项（2017ZX09101004）；新疆生产建设兵团科技攻关与成果转化项目（2016AD008）