五环三萜衍生物的合成和对α-葡萄糖苷酶的抑制活性  

Synthesis and inhibitory activity against α-glycosidase of pentacyclic triterpenes

作　　者：陈磊[1,2] 杨小生 杨娟[2] 叶林虎[2] 郝小江[2] 

机构地区：[1]贵州大学生命科学学院,贵阳550025 [2]贵州省、中国科学院天然产物化学重点实验室,贵阳550002

出　　处：《中国药科大学学报》2010年第3期222-225,共4页Journal of China Pharmaceutical University

基　　金：国家自然科学基金资助项目(No.30973620);贵州省科技计划资助项目(No.2008-7004)~~

摘　　要：对天然产物进行结构修饰和在天然产物中分离得到的齐墩果酸和熊果酸型五环三萜衍生物,经过理化性质和光谱数据确定化合物的结构,并对α-葡萄糖苷酶抑制活性进行测定。体外活性测试表明,天然存在的和从熊果酸和齐墩果酸结构衍生的三萜化合物对α-葡萄糖苷酶均有不同程度的抑制作用,其中化合物1a和1b活性较好。因此,对五环三萜化合物进行结构衍生,可以发现高活性α-葡萄糖苷酶抑制活性化合物。The structures of ursolic acid and oleanolic acid related compound,including natural products and synthetic derivatives of ursolic acid and oleanolic acid,were identified by physical and spectral analyses,or literature data.The inhibitory activity of the triterpene compounds against α-glycosidase were evaluated.The in vitro results showed that the test pentacyclic triterpenes exhibited diverse inhibitory activity against α-glycosidase.Within this series of compounds,1a and 1b had better inhibitory activity than that of the others.It is possible that highly active compounds with α-glycosidase inhibition activity would be found through structural modification of pentacyclic triterpenes.

关 键 词：五环三萜 衍生物 Α-葡萄糖苷酶 抑制活性 

分 类 号：TQ460.31[化学工程—制药化工]