异斯特维醇的结构修饰及其衍生物的生物活性研究进展  

Research progress on the structural modification of isosteviol and the biological activities of its derivatives

作　　者：赵丽君 杨有福 王统盛 张艳丽[1,2] 吴亚 ZHAO Li-jun;YANG You-fu;WANG Tong-sheng;ZHANG Yan-li;WU Ya(College of Medicine,Henan University of Chinese Medicine,Zhengzhou 450046,China;The Engineering and Technology Center for Chinese Medicine Development of Henan Province,Zhengzhou 450046,China)

机构地区：[1]河南中医药大学药学院,河南郑州450046 [2]河南省中药开发工程技术研究中心,河南郑州450046

出　　处：《药学学报》2025年第1期22-36,共15页Acta Pharmaceutica Sinica

基　　金：国家自然科学基金资助项目(21402044);河南省科技攻关项目(202102310474)。

摘　　要：异斯特维醇是天然产物甜菊糖苷在酸性条件下水解得到的四环二萜类化合物,具有多种药理活性,例如抗肿瘤、降糖、降脂、抗炎和抗菌等。由于异斯特维醇本身具有水溶性低、活性不高、生物利用度低等缺点,导致了其成药性能较差。为了克服这些缺点,学者们对其进行了大量的结构修饰与改造,发现了许多结构新颖、活性优良的异斯特维醇衍生物。本文综述了近年来异斯特维醇的结构修饰、生物活性、构效关系及微生物转化的相关研究进展,以期为异斯特维醇及其衍生物类新药开发提供参考。Isosteviol is a tetracyclic diterpenoid compound obtained by hydrolysis of natural stevia glycoside under acidic conditions.It has many pharmacological activities,such as anti-tumor,hypoglycemic,anti-inflammatory and antibacterial.Due to its low water solubility,low activity and low bioavailability,isosteviol has poor performance.In order to overcome these shortcomings,scholars have obtained a large number of isosteviol derivatives with novel structures and excellent activity.In this paper,we review the recent progress in the research on the structure modification,biological activity,structure-activity relationship and microbial transformation of isosteviol,in order to provide a reference for the development of new drugs of isosteviol and its derivatives.

关 键 词：异斯特维醇 衍生物 结构修饰 微生物转化 生物活性 构效关系 

分 类 号：R914[医药卫生—药物化学]