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尿苷二磷酸葡萄糖醛酸转移酶1A1(UGT1A1)是一种重要的Ⅱ相代谢酶,不仅介导了大量临床药物、非药外源物的代谢清除,同时还在维系机体内源性物质代谢平衡中发挥着至关重要的作用。UGT1A1表达/功能的改变不仅会引起药物/中药-药物相互作用,还可导致内源性物质的代谢紊乱,引发高胆红素血症、胆红素脑病及肝损伤等毒副作用。目前已发现多种临床药物及中药成分等外源物可调控UGT1A1的活性。该文结合国内外在药物代谢及毒理学相关领域新近研究进展,综述了不同类型中药化学成分(如黄酮类、香豆素类、生物碱类等)对UGT1A1表达调控及活性作用,包括中药化学成分对UGT1A1酶活性的抑制作用和中药化学成分对UGT1A1酶的诱导作用。该文能够为UGT1A1介导的中药-药物相互作用提供深入的理解和一定的参考,有助于未来指导临床上中药制剂的合理使用。
Uridine diphosphate glucuronosyltransferase 1A1 (UGT1A1) is an important Phase II metabolic enzyme that not only mediates the metabolic clearance of a large number of clinical drugs, non-drug exogenous substances, but also maintains the body’s metabolism of endogenous substances Balance plays a crucial role. UGT1A1 expression / function changes will not only lead to drug / drug-drug interactions, but also lead to metabolic disorders of endogenous substances, triggering hyperbilirubinemia, bilirubin encephalopathy and liver injury and other toxic side effects. It has been found that a variety of clinical drugs and traditional Chinese medicine and other foreign substances can regulate the activity of UGT1A1. In this paper, we reviewed the recent progress in the field of drug metabolism and toxicology at home and abroad, and reviewed the regulation of UGT1A1 expression and its biological activity by different types of traditional Chinese medicine (flavonoids, coumarins, alkaloids, etc.) Inhibition of UGT1A1 Enzyme Activity and Induction of UGT1A1 Enzyme by Chinese Herbs. This article can provide a deep understanding and some references for the UGT1A1-mediated traditional Chinese medicine-drug interaction and help to guide the rational use of traditional Chinese medicine preparations in the future.