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目的为了进一步提高小檗碱的抗肿瘤活性,对小檗碱进行了烷基化,为开发新抗肿瘤药物奠定基础。方法以盐酸小檗碱为起始原料,经格氏试剂烷基化及溴代反应,合成一系列8-烷基-13-溴代-盐酸小檗碱,经UV、IR1、H-NMR和元素分析进行结构鉴定。用四甲基偶氮唑盐(MTT)法观测产物对人肝癌细胞HepG2增殖能力的影响。结果 发现该细胞对目标产物的敏感性与碳链长度有很大关系,其中8-辛基-13-溴代盐酸小檗碱对该细胞的敏感性最强,在浓度为32μg/mL时抑制率为96.82%,IC50为3.33μg/mL。结论从IC50可知在8个碳原子以内,随着溴代小檗碱侧链的增长,抗癌活性增强。
Objective To further improve the anti-tumor activity of berberine, alkylating berberine and laying the foundation for the development of new anticancer drugs. Methods Berberine hydrochloride was used as starting material to synthesize a series of 8-alkyl-13-bromo-hydrochloric berberine by alkylation of Grignard reagent and bromination reaction. The compounds were characterized by UV, IR1, H-NMR and Elemental analysis for structural identification. The effect of the product on the proliferation of HepG2 cells was observed by MTT assay. The results showed that the sensitivity of the cells to the target product has a great relationship with the length of the carbon chain. Among them, 8-octyl-13-bromo-berberine hydrochloride is the most sensitive to this cell and inhibited at a concentration of 32 μg / mL The rate was 96.82% and the IC50 was 3.33 μg / mL. Conclusion From IC50, it is known that within 8 carbon atoms, the anti-cancer activity is enhanced with the increase of the side chain of bromo-berberine.