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.

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)