13-乙酰甲氨基取代苦参碱衍生物的合成及其体外抗肝纤维化活性  

Synthesis and in vitro antifibrosis activities of 13-acetylmethylaminomatrine derivatives

作　　者：付奔 吴茂诚[1] 丁力[1] 吴秋业[1] 赵庆杰[1] 郭忠武[1] 

机构地区：[1]第二军医大学药学院有机化学教研室,上海200433

出　　处：《药学服务与研究》2017年第2期102-104,共3页Pharmaceutical Care and Research

基　　金：国家自然科学基金(21502225;81102490)

摘　　要：目的:合成13-乙酰甲氨类取代基苦参碱衍生物,并研究该类化合物的体外抗肝纤维化活性。方法:以M19为先导化合物,将侧链酰化后引入不同的脂肪胺芳胺基团,合成一系列目标化合物,其结构均通过1 H-NMR和MS确证。用MTT比色法测定目标化合物体外对大鼠肝星状细胞(T6)和人肝星状细胞(LX-2)增殖的抑制作用。结果:所有目标化合物对T6和LX-2的增殖均有一定的抑制作用,部分化合物抑制T6和LX-2增殖的活性优于对照药M19。结论:引入不同的脂肪胺芳胺侧链的苦参碱衍生物具有一定的体外抗肝纤维化活性。Objective： To synthesize a series of 13-acetylmethylaminomatrine derivatives and evaluate their anti/ibrosis ac- tivities in vitro. Methods： M19 was used as the lead compound,aliphatic amines and aromatic amines were introduced into the matrine,and a series of title compounds were synthesized. The structure of target compounds were confirmed by 1H-NMR and MS spectrometries. Their antifibrosis activities against rat hepatic stellate cell （T6） and human hepatic stellate cell （LX-2） were evaluated in vitro by MTT assay. Results： All the target compounds exhibited certain inhibitory activities against T6 and LX-2, some of which showed more potent antifibrosis activities as compared with the control drug M19. Conclusion： The matrine derivatives with aeetylmethylamino side chain have potent antifibrosis activities in vitro.

关 键 词：苦参碱 衍生物 化学合成 抗肝纤维化 体外活性 

分 类 号：R914.5[医药卫生—药物化学]