9种黄酮类化合物对肿瘤细胞的抑制活性及构效关系研究  

Inhibition effects of nine flavonoids on human cancer cells and their structure-activity relationship analysis

作　　者：程亚涛[1] 徐昕[1] 王鹏龙[1] 绪扩[1] 周燊[1] 李强[1] 雷海民[1] 

机构地区：[1]北京中医药大学中药学院,北京100102

出　　处：《西北药学杂志》2014年第2期187-190,共4页Northwest Pharmaceutical Journal

基　　金：国家自然科学基金项目(No.81173519);北京中医药大学创新团队资助项目(2011-CXTD-15)

摘　　要：目的研究9种黄酮类化合物对3种肿瘤细胞的增殖抑制作用及构效关系。方法采用四甲基偶氮唑蓝(MTT)法体外检测黄酮化合物对Bel-7402(人肝癌细胞)、Hela(人宫颈癌细胞)和HT-29(人结肠癌细胞)3种癌细胞模型的抗肿瘤活性。结果 9种黄酮化合物对3种肿瘤细胞具有抑制作用,其中木犀草素活性最显著(IC50:12.81,19.02,19.69),通过对9种黄酮化合物IC50值对比,发现黄酮母核、2,3位双键、5-OH和3′,4′-OH的存在对抑制肿瘤细胞的增殖具有显著的作用。结论黄酮化合物对肿瘤细胞的增殖抑制作用与其结构有一定的相关性,为以后黄酮化合物及其衍生物的研究提供参考。Objective To study the anti-cancer activity and structure-activity relationship of nine flavonoids .Methods The prolifera-tion inhibition of nine flavonoids was investigated on three cancer cell lines （Bel-7402 ,Hela ,HT-29） by MTT assay .Results A-mong the nine flavonoids ,luteolin exhibited the highest proliferation inhibition（IC50 =12 .81 ,19 .02 ,19 .69） .The final result dis-played that their anticancer activities were related to the position of hydroxyl groups ,double bond of C-ring and parent structure ;5-OH ,3′,4′-OH and double bond between position 2 and 3 can enhance the inhibitory effect .Conclusions The study demonstra-ted the proliferation inhibition effects of flavonoids had relationship with their structures .These findings may be benefit for fur-ther researches on the design of flavonoids derivatives with antitumor effect .

关 键 词：黄酮化合物 抗肿瘤 构效关系 

分 类 号：R914.2[医药卫生—药物化学]