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.