新型酯类苦参碱衍生物的合成与体外抗肿瘤活性

Synthesis and in vitro anti-tumor activities of novel matrine ester derivatives

目的:合成苦参碱衍生物并研究其体外抗肿瘤活性。方法:以槐果碱为原料,设计合成了12个酯类衍生物,采用MTT法测试所合成化合物的体外抗肿瘤活性。结果:目标化合物结构经元素分析、1H-NMR和MS确证。体外抗肿瘤结果显示,化合物3 l的活性优于参照药物美法仑,3 f～k的活性弱于美法仑但优于苦参碱,3a～e没有生物活性。结论:苯环和氮芥基团的引入可使苦参碱抗肿瘤活性增强。

Objective： To synthesize matrine derivatives and evaluate their in vitro anti-tumor activities.Methods： Twelve novel matrine ester derivatives were synthesized utilizing sophocarpine as starting material,and their in vitro anti-tumor activities were tested with MTT reduction assay.Results： The structures of target compounds were characterized by elemental analysis,1H-NMR and MS.The results of in vitro anti-tumor activities showed that compound 3l possessed higher activity than the reference drug melphalan.The activities of compounds 3f^k were between melphalan and matrine.Compounds 3a^e did not show the biological activities.Conclusion： Incorporating phenyl and nitrogen mustard to matrine can enhance its in vitro anti-tumor activities.