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[中药化学成分对尿苷二磷酸葡萄糖醛酸转移酶1A1表达及活性调控作用的研究进展]

[Advances in research on regulatory effects of chemical ingredients of traditional Chinese medicine on UDP-glucuronosyltransferase 1A1 expression and activity].

作者信息

Xin Hong, Xu Wei

机构信息

Department of Integrated Traditional Chinese and Western Medicine, First Affiliated Hospital of Harbin Medical University, Harbin 150001, China.

出版信息

Zhongguo Zhong Yao Za Zhi. 2017 Feb;42(3):428-432. doi: 10.19540/j.cnki.cjcmm.2017.0008.

Abstract

Uridine 5'-diphosphate-glucuronosyltransferase1A1(UGT1A1) is a major phase Ⅱ metabolism enzyme, responsible for glucuronidation and elimination of drugs and endogenous compounds, playing a vital role in sustaining endogenous metabolism balance. Therefore, changes in UGT1A1 expression/functional can not only cause adverse clinical drug/herbs-drug interactions, but also lead to metabolic disorder of endogenous substances, causing high blood bilirubin, bilirubin encephalopathy and liver injury, as well as other side effects. To date, many studies have found that a variety of clinical medicines and medicinal ingredients can regulate UGT1A1 activity. This article would summarize the advances in research on drug metabolism and toxicology in domestic and foreign literature, and investigate the regulatory effects of different types of traditional Chinese medicine(TCM) ingredients(such as flavonoids, coumarins, alkaloids) on UGT1A1 expression and activity, including inhibitory effect of TCM chemical ingredients on UGT1A1 and effect of TCM chemical ingredients on UGT1A1. It is hoped that this review could provide depth understanding and certain reference for the interaction between chemical ingredients of TCM and UGT1A1, which is of great significance to guide the rational clinical use in future.

摘要

尿苷5'-二磷酸葡萄糖醛酸基转移酶1A1(UGT1A1)是一种主要的Ⅱ相代谢酶,负责药物和内源性化合物的葡萄糖醛酸化及消除,在维持内源性代谢平衡中发挥着至关重要的作用。因此,UGT1A1表达/功能的改变不仅会导致不良的临床药物/草药-药物相互作用,还会引起内源性物质的代谢紊乱,导致高胆红素血症、胆红素脑病和肝损伤以及其他副作用。迄今为止,许多研究发现多种临床药物和药用成分可调节UGT1A1活性。本文将总结国内外文献中关于药物代谢和毒理学的研究进展,并探讨不同类型的中药成分(如黄酮类、香豆素类、生物碱类)对UGT1A1表达和活性的调节作用,包括中药化学成分对UGT1A1的抑制作用以及中药化学成分对UGT1A1的影响。希望本综述能够为中药化学成分与UGT1A1之间的相互作用提供深入的理解和一定的参考,这对指导未来临床合理用药具有重要意义。

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