甘草次酸–苦参碱复合物的合成及其抗肿瘤活性研究  

Synthesis of glycyrrhetinic acid-matrine complexes and their antitumor activities

作　　者：张娜[1] 崔晓燕[1,2] 赵秀梅[1] 李冬冬[1] 代霖霖 陶遵威[1] 

机构地区：[1]天津市医药科学研究所,天津300020 [2]天津医科大学研究生院,天津300070

出　　处：《现代药物与临床》2014年第11期1199-1202,共4页Drugs & Clinic

基　　金：天津市卫生局科技基金资助项目(2012KZ058)

摘　　要：目的设计合成甘草次酸–苦参碱复合物,并对其体外抗肿瘤活性进行研究。方法以槐果碱、18α-甘草次酸和18β-甘草次酸为原料,经过加成、氧化、酯化缩合等反应合成目标化合物甘草次酸–苦参碱复合物,并采用MTT法对其进行体外抗肿瘤活性研究。结果设计并合成了目标产物甘草次酸–苦参碱复合物,利用MS和1H-NMR确证了结构;体外活性实验中,甘草次酸–苦参碱复合物的抗肿瘤活性明显高于甘草次酸及苦参碱,并优于对照药美法仑。结论甘草次酸–苦参碱复合物具有良好的抗肿瘤活性,尤其对肝癌细胞生长产生较好的抑制作用,值得进一步进行研究。Objective To design and synthesize glycyrrhetinic acid-matrine complexes, and to evaluate their antitumor activities in vitro. Methods Sophocarpine, 18α-glycyrrhetinic acid and 18β-glycyrrhetinic acid were used as starting materials to synthesize the target compounds glycyrrhetinic acid-matrine complexes by addition, oxidation, and esterification reactions. The antitumor activities in vitro were evaluated by MTT method. Results The target compounds glycyrrhetinic acid-matrine complexes were synthesized and characterized by MS and ^1H-NMR. The in vitro antitumor activity experiments showed that the antitumor activity of glycyrrhetinic acid-matrine complexes were higher than those of glycyrrhetinic acid and matrine in vitro, and were better than control drug melphalan. Conclusion The target compounds glycyrrhetinic acid-matrine complexes have good antitumor activities especially against hepatoma cells, which could be a valuable candidate for further development.

关 键 词：甘草次酸–苦参碱复合物 甘草次酸 苦参碱 合成 美法仑 抗肿瘤活性 

分 类 号：R914[医药卫生—药物化学] R966[医药卫生—药学]