8-烷基黄连碱同系物的合成及体外降糖作用  

Synthesis and in vitro glucose-lowering effect of 8-alkyl-coptisine

作　　者：蒋小飞[1,2] 李学刚[1] 汤琳[1] 叶小利[3] 

机构地区：[1]西南大学药学院药用资源化学研究所,重庆400716 [2]重庆三峡学院化学与环境工程学院,重庆404100 [3]西南大学生命科学学院,重庆400715

出　　处：《中草药》2011年第4期640-644,共5页Chinese Traditional and Herbal Drugs

基　　金：重庆市科委重大专项"黄连综合开发利用"资助项目(CSTC2008AA5021);重庆市科委攻关项目"平抑舒降糖胶囊对不同症侯糖尿病疗效及安全性研究"资助(CSTC2010AC5007);科技部新药创制项目"黄连治疗糖尿病型高血脂并发症中药新药研究"资助(2010ZX09401-306-3-10)

摘　　要：目的合成8-烷基黄连碱同系物并研究其在体外对细胞糖代谢的影响。方法采用与人肝细胞表型相似的HepG2细胞,检测24 h后培养液中葡萄糖消耗量,用MTT法观察细胞增殖情况。结果 8-烷基黄连碱同系物在葡萄糖浓度为10 mmol/L时可使HepG2细胞的葡萄糖消耗量有不同程度的增加,其中以8-己基黄连碱最为显著。8-烷基黄连碱同系物对HepG2细胞增殖有显著的抑制作用。结论首次合成8-烷基黄连碱同系物。8-烷基黄连碱同系物随着其烷基碳链的延长,细胞的葡萄糖消耗量先是增大,当8位烷基链碳原子数超过6时,葡萄糖消耗量逐渐减小。8-已基黄连碱是具有一定潜力的降血糖先导化合物。Objective To investigate the effect of 8-alkyl-coptisine on glycometabolism in vitro.Methods HepG2 cells similar to human hepatic cells were used to test the glucose consumption（GC） in cultural solution in 24 h and MTT assay was used to monitor the proliferation of HepG2 cells.Results The results indicated that 8-alkyl-coptisine could increase the amounts of GC of HepG2 cells.In glucose concentration（10 mmol/L）,8-hexyl-coptisine was the most significant.8-Alkyl-coptisine had notable inhibition in proliferation of HepG2 cells.Conclusion 8-Alkyl-coptisine was successfully synthesized.GC could increase as the length of the aliphatic chain increases firstly and the GC could decrease when the length of the aliphatic chain exceeds six atoms.8-Hexyl-coptisine is a potential hypoglycemic leading compound.

关 键 词：8-烷基黄连碱 合成 HEPG2细胞 葡萄糖消耗 8-烷基黄连碱同系物 

分 类 号：R284.1[医药卫生—中药学]