异紫堇碱及其类似物的抗癌活性研究  

Research on anticancer activity of isocorydine and its derivatives

作　　者：闫倩[1,2] 李如霞[1,3] 辛爱一 柳军玺[1] 李文广[3] 邸多隆[1] 

机构地区：[1]中国科学院兰州化学物理研究所中国科学院西北特色植物资源化学重点实验室甘肃省天然药物重点实验室,甘肃兰州730000 [2]中国科学院大学,北京100049 [3]兰州大学基础医学院,甘肃兰州730000

出　　处：《中国中药杂志》2017年第16期3152-3158,共7页China Journal of Chinese Materia Medica

基　　金：国家自然科学基金项目(21672225)

摘　　要：采用天然产物化学研究手段,从秃疮花和云南地不容中分离得到部分异紫堇碱类生物碱,并对异紫堇碱进行化学结构修饰得到异紫堇碱类似物,采用MTT法考察了异紫堇碱类似物对3种人癌细胞株的细胞生长抑制活性。结果表明异紫堇碱及其类似物均具有一定的抗癌活性,结合异紫堇碱及其类似物的单晶衍射结构与EGFR分子对接模拟,从立体化学结构、化合物不同取代基位置以及芳香环电子云密度等角度探讨了该类化合物具有抗癌活性的构效关系。Isocorydine and its analogs were extracted from Dicranostigma leptopodum and Stephania yunnanensis through the method of natural products chemistry. Its derivatives were prepared by chemical structure modifications from isocorydine. MTT method was used to study the inhibitory effect of those compounds on the growth of HepG2,He La and MGC-803 cancer cell lines in vitro. The results showed that isocorydine and its analogs all have the growth inhibition for those cancer cell lines. This paper investigated the structure-activity relationship of isocorydine and its derivatives with anticancer activity in the aspect of stereochemical structure,functional groups positions of the compounds and the electron density of aromatic rings based on the single crystal diffraction structure and the molecular docking of EGFR and isocorydine.

关 键 词：阿朴啡类生物碱 抗癌活性 构效关系 异紫堇碱 

分 类 号：R284[医药卫生—中药学] R285[医药卫生—中医学]