摘要
目的设计并合成甘草次酸C3、C30衍生物,并对其体外抗肿瘤活性进行研究。方法以甘草次酸为先导化合物,对其C3位羟基、C30位羧基进行结构修饰,并采用SRB法对目标化合物进行体外抗肿瘤活性研究。结果设计合成了12个新型甘草次酸衍生物,并利用MS、1H-NMR及元素分析确证了结构;体外实验中,目标化合物对MCF-7和A549肿瘤细胞的抑制活性均明显强于甘草次酸,其中化合物GA-I1、GA-I2和GA-II1对MCF-7和A549两种细胞表现出很好的抑制活性,明显高于对照药吉非替尼。结论甘草次酸衍生物具有良好的抗肿瘤活性,值得进一步研究。
Objective To design and synthesize glycyrrhetinic acid C3 and C30 derivatives and their antitumor activities in vitro. Methods Glycyrrhetinic acid was used as starting material to synthesize the target compounds by structural modification at C3 hydroxyl group, and C30 carboxyl group. The antitumor activities of the compounds were tested bySRBassay.Results Twelve novel glycyrrhetinic acid derivatives were synthesized and characterized by MS,1H-NMR, and elemental analysis. Thein vitro antitumor activity experiments showed that cytotoxic effects of target compounds against MCF-7 and A549 cells were higher than those of glycyrrhetinic acidin vitro. In which compoundsGA-I1,GA-I2, andGA-II1 had better cytotoxic effects against MCF-7 and A549 cells, and it was better than control drug gefitinib.Conclusion The target compounds glycyrrhetinic acid derivatives have good antitumor activities which could be a valuable candidate for further development.
出处
《现代药物与临床》
CAS
2015年第6期610-615,共6页
Drugs & Clinic
基金
国家自然科学基金资助项目(21372156)
辽宁省教育厅高等学校优秀人才支持计划资助项目(LR2013017)
沈阳市科技计划资助项目(F13-316-1-47)
关键词
甘草次酸
五环三萜类
结构改造
合成
抗肿瘤活性
glycyrrhetinic acid
pentacyclic trierpenoids
structure modification
synthesis
antitumor activity
