基于UGM靶标的贵州药用植物抗结核分枝杆菌化合物构建及类似物研究  

Research of anti-Mycobacterium tuberculosis compounds and their analogues from Guizhou characteristic medicinal plants based on UGM targets

作　　者：娄华勇 傅建 潘卫东 LOU Huayong;FU Jian;PAN Weidong(Natural Products Research Center of Guizhou Province,Guiyang 550014,Guizhou,China;State Key Laboratory of Functions and Applications of Medicinal Plants,Guizhou Medical University,Guiyang 550014,Guizhou,China;College of Pharmacy,Guizhou University of Traditional Chinese Medicine,Guiyang 550025,Guizhou,China)

机构地区：[1]贵州省天然产物研究中心,贵州贵阳550014 [2]贵州医科大学省部共建药用植物功效与利用国家重点实验室,贵州贵阳550014 [3]贵州中医药大学药学院,贵州贵阳550025

出　　处：《贵州医科大学学报》2023年第6期621-626,633,共7页Journal of Guizhou Medical University

基　　金：国家自然科学基金(32060100,81903517);贵州省科技厅项目(黔科合基础-ZK[2021]534);贵阳市高层次创新型青年科技人才(筑科合同[2021]43-10)。

摘　　要：本文回顾性总结了潘卫东研究员项目团队有关二磷酸尿苷-半乳糖变异酶(UGM)探针设计、新型抑制剂的开发及新型筛选技术等方面的研究成果,明确了UGM反应机理,系统构建了贵州特色药用植物的抗结核分枝杆菌天然小分子化合物库,并从中发现了天然产物来源的UGM抑制剂,从而突破了当前UGM抑制剂成药性不佳的瓶颈,证实UGM存在变构位点,为贵州中药民族药的资源开发拓展了新思路。Objective The study presents a systematic review concerning a novel anti-tubercolosis agents targeting UDP-Galactopyranose mutase(UGM)by Professor Weidong Pan's team from Guizhou China and Chinese academy of sciences,which achieved some original research results based on UGM for probe design,new inhibitor development and novel screening techniques:including the confirmation of the mechanism of UGM reaction,systematical construction of anti-tuberculosis natural products sources from medicinal plants of Guizhou and helpful resources for further research and development of new UGM inhibitor drugs.Moreover,some key scientific problems on UGM research were solved,which confirmed the existence of allosteric sites in UGM.The research results greatly promoted the development of related fields and expanded new conception for the resource development of traditional Chinese medicine and ethnic medicine in Guizhou China.

关 键 词：结核分枝杆菌 二磷酸尿苷-半乳糖变异酶 药用植物 抑制剂 结构修饰 先导化合物 

分 类 号：R37[医药卫生—病原生物学]