天然植物活性成分通过转录因子调节UGT的研究进展  

Active Phytochemicals: Regulation of UDP-glucuronosyltransferases Via Transcription Factors

作　　者：詹志坤 侯楚祺 刘文钦 唐斓[1] Zhan zhikun;Hou chuqi;Liuqin;Tang Lan(School of Pharmaceutical Sciences,Southern Medical University,Guangzhou 510515,China)

机构地区：[1]南方医科大学药学院,广州510515

出　　处：《世界科学技术-中医药现代化》2019年第2期168-181,共14页Modernization of Traditional Chinese Medicine and Materia Medica-World Science and Technology

基　　金：广东省科技厅科技计划项目重点项目(2016B020237005):基于代谢分析的创新药物研发风险控制技术平台;负责人:刘叔文

摘　　要：尿苷二磷酸葡萄糖醛酸转移酶能催化诱变剂,内源性和包括草药中的植物活性物质在内的外源性物质与辅因子尿苷二磷酸葡萄糖醛酸结合。作为药理活性分子的前体,植物化学物质已经受到越来越多的关注。在中药和常见药物的使用中,植物化学物质对UGT的表达应该没有显著的影响。然而,大量的植物化学物质可以通过调控各种转录因子影响UGT基因表达,并诱导药物间的相互作用。本文总结了植物化学物质通过13个关键转录因子AhR、CAR、PXR、PPARα、LXR、FXR、Nrf2、HNF1α、HNF3α、HNF4α、ERα、AR、NF-kB调节人UGT基因表达的当前研究进展,并对其潜在的机制进行了讨论。UDP-glucuronosyltransferases(UGTs)catalyze the glucuronidation of mutagens,endobiotics,and xenobiotics,including active phytochemicals from herbal medicine.Phytochemicals have been given increasing attention as precursors for pharmacologically active molecules.In the consumption of herbal products and conventional drugs,phytochemicals should be neutral in terms of their effects on UGT expression.However,numerous phytochemicals could affect the gene expression of UGTs via regulating kinds of transcription factors and could induce herb–drug interactions.This paper summarized the research progress on the regulation of UGTs expressed in humans by phytochemicals via 13 key transcriptional factors,namely,AhR,CAR,PXR,PPARα,LXR,FXR,Nrf2,HNF1α,HNF3α,HNF4α,ERα,AR,and NF-kB.The potential mechanisms were also discussed.

关 键 词：尿苷二磷酸葡萄糖醛酸转移酶 植物化学物质 转录因子 基因调节 

分 类 号：R282-71[医药卫生—中药学]