芳香基苦参碱衍生物的合成及抗肿瘤活性  

A Study on the Synthesis and Anti-tumour Activity of Matrine Derivatives with Aryl

作　　者：韦星船[1] 郑成[1] 何雄[1] 郑希 姚惠珍[3] 霍梦月[1] 段彦飞[1] 

机构地区：[1]广州大学化学化工学院,广东广州510006 [2]美国Rutgers大学Susan Lehman Cullman肿瘤研究所,美国新泽西08854 [3]广州医学院药学实验中心,广东广州510182

出　　处：《精细化工》2013年第8期936-939,共4页Fine Chemicals

基　　金：广东省科技计划项目(2011B050400028);广州市科技计划项目(12C32011623)~~

摘　　要：分别以茴香醛、黎芦醛、3,4,5-三甲氧基苯甲醛、2,3,4-三甲氧基苯甲醛为原料,在氢化钠的作用下,与苦参碱发生Claisen-Schimidt缩合反应合成了4个芳香基苦参碱衍生物;采用MTT法测试目标化合物对人结肠癌细胞株HT-29,人胰腺癌细胞株PANC-1的增殖抑制活性。结果表明,合成的芳香基苦参碱衍生物的IC50值分别为27.8、18.0、9.05、13.2μmol/L,苦参碱的IC50值为28.6μmol/L,4个苦参碱衍生物的抗肿瘤活性较苦参碱有所提高。Four matrine derivatives were synthesized by Claisen-Schimidt condensation in which matrine reacted respectively with anisaldehyde, veratrum aldehyde, 3,4,5-trimethoxy-benzaldehyd and 2,3,4- trimethoxy-benzaldehyde in sodium hydride solution. The most suitable conditions for the synthesis were ascertained by an orthogonal experiment. The inhibitory effects of these compounds were determined by the MTF assay on the growth of HT -29 cells and PANC - 1 cells. The results show that the ICs0 of matrine derivative is 27.8μmol/L, 18.0μmol/L, 9.05 μmol/L and 13.2 μmol/L respectively, and the IC50 of matrine is 28.6μmoL/L. The four matrine derivatives synthesized have better anticaneer activity than matrine.

关 键 词：苦参碱 苦参碱衍生物 抗肿瘤活性 医药与日化原料 

分 类 号：R979.1[医药卫生—药品]