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.
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)
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
Cantharidin derivatives
Synthesis
Antitumor activity
Excitant toxicity
New zealand white rabbits
