中药成分对肝脏尿苷二磷酸葡萄糖醛酸转移酶的体外作用研究进展  

Research progress on in vitro effects of traditional Chinese medicine ingredients on liver UDP-glucuronosyltransferases

作　　者：闫媛 李慧慧 彭佩瑾 安广涛 邓秀平 刘志东[1,2,3] 祁东利[1,2] YAN Yuan;LI Hui-hui;PENG Pei-jin;AN Cuang-lao;DENG iu-ping;LIU Zhi-dog;QI Dong-li(State Key Laboratory of Component-based Chinese Medicine,Tianjin University of Traditional Chinese Medicine,Tianjin 301617,China;Engineering Research Center of Modern Chinese Medicine Discovery and Preparation Technique,Ministry of Education,Tianjin University of Traditional Chinese Medicine,Tianjin 301617,China;School of Chinese Materia Medica,Tianjin University of Traditional Chinese Medicine,Tianjin 301617,China;Nanjing Healthnice Pharmaceutical Technology Co.,Ltd.,Nanjing 210031,China)

机构地区：[1]天津中医药大学组分中药国家重点实验室,天津301617 [2]天津中医药大学现代中药发现与制剂技术教育部工程研究中心,天津301617 [3]天津中医药大学中药学院,天津301617 [4]南京海纳医药科技股份有限公司,江苏南京210031

出　　处：《中国中药杂志》2024年第20期5397-5409,共13页China Journal of Chinese Materia Medica

基　　金：国家中药标准化项目(ZYBZH-C-JS-35)。

摘　　要：尿苷二磷酸葡萄糖醛酸转移酶(UDP-glucuronosyltransferases, UGTs)是人体内最主要的Ⅱ相代谢酶,参与体内各种化学物质的葡萄糖醛酸化反应。中药成分影响药物代谢酶UGTs的活性,经该酶代谢的药物发生血药浓度波动,在临床上会引起代谢药物的血药浓度升高或降低,引起“中药-中药”“中药-化药”相互作用,导致用药安全性问题、影响药物疗效等,因此,探究中药成分对UGTs活性的作用至关重要。重组人UGTs单酶法和肝微粒体孵育法可靠且有效,常被用于研究中药成分对肝脏UGTs的作用。目前,已有许多文献报道多种中药成分对UGTs活性存在诱导或抑制作用,但尚未对其进行系统总结,该文综述了中药单体成分、中药提取物和中成药对重组人UGTs或肝微粒体UGTs的体外作用,以期为中药在临床上的合理安全使用提供参考;从UGTs介导的药物-药物相互作用角度,阐明已有的中药经典药对及配伍禁忌原理,为发掘新的药物配伍奠定基础。UDP-glucuronosyltransferases(UGTs)are the main phaseⅡmetabolizing enzymes in the human body,participating in the glucuronidation of various chemicals in the body.Traditional Chinese medicine(TCM)ingredients affect the activities of UGTs in-volved in drug metabolism,and the fluctuations in the blood concentrations of drugs metabolized by UGTs will lead to the risk of TCM-TCM or TCM-chemical drug interaction,which will cause drug safety problems and affect drug efficacy.Therefore,it is essential to ex-plore the effect of TCM ingredients on the activities of UGTs.The recombinant human UGTs method and liver microsomal incubation method are reliable and effective,and they are thus often used to study the effects of TCM ingredients on UGTs in the liver.Studies have reported that different TCM ingredients can induce or inhibit the activities of UGTs,while the systematical review remains to be carried out.This paper reviews the effects of different ingredients and extracts of TCM and Chinese patent medicines on recombinant human UGTs or liver microsomal UGTs,aiming to provide reference for the rational and safe use of TCM in clinical practice.From the perspective of drug-drug interaction mediated by UGTs,the exacting classical drug pairs and incompatibility principles of traditional Chinese medicine were clarified,which laid the foundation for exploring new drug compatibility.

关 键 词：尿苷二磷酸葡萄糖醛酸转移酶(UGTs) 中药 重组人UGTs 肝微粒体 

分 类 号：R285[医药卫生—中药学]