斑蝥素衍生物的设计合成及体外抗肿瘤活性与刺激性毒性研究  

Design,Synthesis,Anti-tumor Activity and Excitant Toxicity of Cantharidin Derivatives

作　　者：陈农[1] 李贺敏[1] 彭国平[1] 郑云枫[1] 李存玉[1] 蒋颖[1] 

机构地区：[1]南京中医药大学药学院,江苏南京210029

出　　处：《长春中医药大学学报》2013年第1期25-28,共4页Journal of Changchun University of Chinese Medicine

基　　金：康缘中医药科技创新基金(HZ1006KY);南京中医药大学中药学一级学科开放课题资助(2011ZYX3-008)

摘　　要：目的:设计斑蝥素衍生物合成路线,寻找低毒有效的新型斑蝥素衍生物。方法:以呋喃和顺丁烯二酸酐为初始原料经多步合成斑蝥素衍生物,其结构经1HNMR和IR确证;并分别通过家兔眼刺激性实验方法和MTT法,以去甲斑蝥素(NCTD)为对照,考查衍生物的刺激性毒性和体外抗癌活性。结果:合成得到3种斑蝥素衍生物a,b和c,药理结果表明化合物a,b和c均对肿瘤细胞株有一定的抑制作用,且他们的刺激性毒性顺序为:a>NCTD>c>b。结论:合成路线简易可行,得到的衍生物刺激性毒性很小,有进一步研究的价值。objective：To design synthetic route of cantharidin derivatives and look for novel low toxic effective can- tharidin derivatives, methods： Cantharidin derivatives were synthesized through several steps using furan and maleic anhy- dride as the starting material, all compounds were confirmed by 1 H NMR and IR. ; With norcanthadin （NCTD） as control sample, excitant toxicity was investigated by eye irritation of experimental methods and antitumor activity in vitro was investi- gated by MTF. results： Three cantharidin derivatives a,b and c was obtained;each derivative have certain inhibition on tu- mor cell line ; excitant toxicity order was ： a 〉 NCTD 〉 c 〉 b. conclusion： The synthetic route was simple and feasible, the ex- citant toxicity of obtained derivatives was small and had the the value of further study.

关 键 词：斑蝥素衍生物 合成 抗癌活性 刺激性毒性 新西兰白兔 

分 类 号：R285.5[医药卫生—中药学]