文献类型：期刊文章

作　　者：杨博威[1] 梁丹琳[1] 魏雄[1] 孟祥豹[1] 李中军[1,2]

机构地区：[1]北京大学医学部药学院天然药物及仿生药物国家重点实验室化学生物学系,北京100191 [2]江西师范大学国家单糖化学合成工程技术研究中心,江西南昌330022

出　　处：《Journal of Chinese Pharmaceutical Sciences》

基　　金：The National Research Foundation for the Doctoral Program of Higher Education of China(Grant No.20130001110058)

年　　份：2017

卷　　号：26

期　　号：8

起止页码：556-565

语　　种：中文

收录情况：CAB、CAS、CSCD、CSCD2017_2018、DOAJ、EMBASE、IC、JST、SCOPUS、ZGKJHX、普通刊

摘　　要：Mangiferin is a natural plant polyphenol with a structure of xanthone C-glycoside and it displays a wide spectrum of pharmacological activities. Investigation of the metabolites of mangiferin is valuable in studying the mechanisms of its various pharmacological properties and developing novel drugs from the mangiferin derivatives. Among the metabolites of mangiferin, mangiferin-7-O-β-D-glucuronide has been reported as the phase Ⅱ metabolite of mangiferin. Herein we described the first semi-synthesis of mangiferin-7-O-β-D-glucuronide with the natural product mangiferin as the starting material. In this work, we adopted several regioselective protection procedures to distinguish the different hydroxyl groups in the structure of mangiferin, and we accomplished the glycosylation under the phase-transfer catalysis conditions. In this method, we efficiently synthesized the glucuronide derivative of mangiferin in 10 steps with highly regioselective protection.

关 键 词：Mangiferin-7-O-β-D-glucuronide  Semi-synthesis  Regioselective protection  Glycosylation  

分 类 号：R914]