尿苷二磷酸葡萄糖醛酸转移酶的调控及其介导的中药-药物相互作用研究进展  

Research progress of regulation of UDP-glucuronosyltransferases and herb-drug interaction

作　　者：周楠 李婷婷[2] 陈西敬 ZHOU Nan;LI Tingting;CHEN Xijing(School of Basic Medicine and Clinical Pharmacy,China Pharmaceutical University,Nanjing 211198,China;School of Pharmacy,China Pharmaceutical University,Nanjing 211198,China)

机构地区：[1]中国药科大学基础医学与临床药学学院,江苏南京211198 [2]中国药科大学药学院,江苏南京211198

出　　处：《药学研究》2022年第6期394-399,共6页Journal of Pharmaceutical Research

基　　金：国家自然科学基金(No.81503150);中央高校基本科研业务专项资金资助(No.2632019ZD05)。

摘　　要：尿苷二磷酸葡萄糖醛酸转移酶(UGT)催化的葡萄糖醛酸化反应是的是Ⅱ相代谢中重要的代谢反应之一,对于维持内源性化合物如胆红素、胆汁酸的动态平衡和药物、致癌物等外源性化合物的处置过程起着至关重要的作用。尿苷二磷酸葡萄糖醛酸转移酶的表达和酶活性受多维机制的调控。深入研究其调控网络以及尿苷二磷酸葡萄糖醛酸转移酶介导的相关中药-药物相互作用,对于临床更安全、有效的使用中药提供了指导。因此,本文总结了尿苷二磷酸葡萄糖醛酸转移酶的转录前、转录水平、翻译后修饰等分子调节机制,以及由尿苷二磷酸葡萄糖醛酸转移酶介导的中药-药物相互作用相关的研究进展。The glucuronidation reaction catalyzed by uridine diphosphate glucuronyltransferases(UGT)is the most important metabolic reaction in phaseⅡmetabolism,which plays a role in maintaining the homeostasis of endogenous compounds such as bilirubin and bile acids and disposal process of exogenous compounds such as drug and carcinogens.The expression and enzymatic activities of UGTs are regulated by multidimensional mechanisms and various factors.An in-depth study of its regulatory network and herb-drug interactions mediated by UGT provides guidance for safer and more effective clinical use of herb.Therefore,this article summarized the molecular regulation mechanisms of UGT such as epigenetic modifications,transcriptional level,and posttranslational modification,as well as UGT-mediated herb-drug interactions.

关 键 词：尿苷二磷酸葡萄糖醛酸转移酶 中药-药物相互作用 中药 

分 类 号：R969.2[医药卫生—药理学]