新型姜黄素衍生物的合成及其抗癌活性研究  

Synthesis and Anti-tumor Evaluation of New Curcumin Derivants

作　　者：林锦璇[1] 王鹏龙[2] 褚福浩[2] 徐昕[2] 绪扩[2] 程亚涛[2] 李国梁[2] 龚晏[2] 雷海民[2] 张宇忠[1] 

机构地区：[1]北京中医药大学基础医学院,北京100029 [2]北京中医药大学中药学院,北京100102

出　　处：《中国实验方剂学杂志》2014年第7期113-117,共5页Chinese Journal of Experimental Traditional Medical Formulae

基　　金：国家自然科学基金项目(81173519);北京中医药大学创新团队项目(2011-CXTD-15);北京中医药大学自主课题项目(2013-JYBZZ-XS-040)

摘　　要：目的:研究新型姜黄素衍生物的合成及其体外抗癌活性。方法:以"十全大补丸"方中抗癌活性成分为原料,利用拼合原理,设计、合成姜黄素衍生物,并采用四甲基偶氮唑蓝(MTT)法体外检测姜黄素衍生物在HT-29(人结肠癌细胞)、Bel7402(人肝癌细胞)、HepG2(人肝癌细胞)、Hela(人宫颈癌细胞)4种癌细胞模型的抗癌活性和对正常细胞MDCK(犬肾上皮细胞)的毒性。结果:发现化合物4和CU-T能明显抑制4种人源性癌细胞的增殖,二者体外抗癌活性(IC50)与顺铂相似,显著高于姜黄素;且对MDCK细胞的毒性明显小于顺铂。结论:以拼合原理为指导,进一步验证了从经典方药中发现高效、低毒的抗癌先导化合物的研究思路是可行的。Objective： To study the synthesis and in vitro anti-cancer activity of new curcumin derivatives. Method： Three new curcumin derivatives were synthesized using anti-tumor ingredients of Shiquandabu Wan as starting materials. Our idea was enlightened by the ‘combination principle’ in drug discovery. The curcumin derivatives anti-tumor activities were evaluated on the HT-29, Bel-7402, HepG2 and Hela human cancer cell lines and their toxicities were evaluated on MDCK （madin-darby canine kidney cell lines）. Result： Compound 4 and CU-T displayed more antiproliferative activities on these cancer cells than their starting materials; IC50 values were similar to DDP＇s, while curcumin derivatives showed much lower toxicity on MDCK cell than DDP. Conclusion： It is feasible to discover high-effect and low-toxicity lead compounds from classic formulas via combination principle.

关 键 词：姜黄素 衍生物 拼合原理 中医药 抗肿瘤 

分 类 号：R284.1[医药卫生—中药学]