目的 設(shè)計合成甘草次酸-苦參堿復(fù)合物,并對其體外抗腫瘤活性進(jìn)行研究.方法 以槐果堿、18α-甘草次酸和18β-甘草次酸為原料,經(jīng)過加成、氧化、酯化縮合等反應(yīng)合成目標(biāo)化合物甘草次酸-苦參堿復(fù)合物,并采用MTT法對其進(jìn)行體外抗腫瘤活性研究.結(jié)果 設(shè)計并合成了目標(biāo)產(chǎn)物甘草次酸-苦參堿復(fù)合物,利用MS和¹H-NMR確證了結(jié)構(gòu);體外活性實驗中,甘草次酸-苦參堿復(fù)合物的抗腫瘤活性明顯高于甘草次酸及苦參堿,并優(yōu)于對照藥美法侖.結(jié)論 甘草次酸-苦參堿復(fù)合物具有良好的抗腫瘤活性,尤其對肝癌細(xì)胞生長產(chǎn)生較好的抑制作用,值得進(jìn)一步進(jìn)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.

天津市衛(wèi)生局科技基金資助項目(2012KZ058)