异甜菊醇衍生物的生物活性及构效关系研究进展  

Research Advances in Biological Activities and Structure-activity Relationship of Isosteviol Derivatives

作　　者：王婷婷[1] 陈莉[1] 

机构地区：[1]中国药科大学天然药物化学教研室,江苏南京210009

出　　处：《药学进展》2013年第4期152-160,共9页Progress in Pharmaceutical Sciences

基　　金：2011年中国药科大学中央高校基本科研业务费专项基金(No.JKY2011042)

摘　　要：异甜菊醇因具有贝叶烷四环二萜类的特征性骨架,并具有抗高血压、调血脂、降血糖、保护心脑细胞、抑菌、抗炎及抗肿瘤等广泛生物活性,且其制备原料甜菊苷廉价易得、安全低毒,故以其为先导物,通过化学合成和微生物转化,对其结构进行修饰与改造,发现具更高活性的异甜菊醇衍生物,已成为广受药学研究者关注的热点。综述近年来异甜菊醇衍生物的生物活性及构效关系研究进展。The diterpene isosteviol, bearing distinctive tetracylic skeleton of kanrene, exhibits wide biological activities including anti-hypertension, controlling blood lipid, reducing blood glucose, protecting heart-brain cells, antibacterium, antiinflammation, anticancer and so on. Besides, stevioside as the starting material is readily available, cheap and safe. Therefore, it has become a hot spot to discover highly active derivatives through structural modification of isosteviol via chemical synthesis and microbial transformation, of which the application in the development of related drugs prospects well. The recent advances in the research on biological activities and structure-activity relationship of isoteviol derivatives were reviewed.

关 键 词：异甜菊醇 衍生物 化学合成 微生物转化 结构修饰 生物活性 构效关系 

分 类 号：R284[医药卫生—中药学] R285[医药卫生—中医学]