白藜芦醇衍生物的合成及抑制宫颈癌HeLa细胞肿瘤活性  

Synthesis and Anti-tumor Activities of Resveratrol Derivatives on Cervical Cancer HeLa Cells

作　　者：杜成[1] 任玉杰[1,2] 王庆伟[1] 金鹭[1] 

机构地区：[1]上海应用技术学院化学与环境工程学院,上海201418 [2]中国科学院上海有机化学研究所天然产物有机合成化学重点实验室,上海200032

出　　处：《有机化学》2013年第6期1279-1283,共5页Chinese Journal of Organic Chemistry

基　　金：上海市教委科研创新重点(No.12ZZ188);上海市科委(No.11430502500);上海高校特聘教授(东方学者)岗位计划(No.405ZK110060002)资助项目~~

摘　　要：以白藜芦醇、氯乙酰氯、对甲苯磺酰氯、对甲苯甲酰氯为原料,合成9种新的白藜芦醇衍生物,其结构经IR,1HNMR,13C NMR和HRMS所表征.用3-(4,5-二甲基噻唑-2)-2,5-二苯基四氮唑溴盐(MTT)法测试了目标化合物抑制宫颈癌HeLa细胞的肿瘤活性,结果表明:化合物4a,6a,7b,8b和11c对HeLa细胞的抑制活性比白藜芦醇高,其中化合物6a和8b的抑制效果最明显,其IC50值分别为22.7和18.0μmol/L,活性高于白藜芦醇(IC50=114μmol/L),且在150μmol/L浓度下对HeLa细胞的抑制率达95.5%和87.7%.Nine novel resveratrol derivatives were synthesized from resveratrol, chloroacetyl chloride, p-toluenesulfonyl chloride and p-methyl benzoyl chloride. These structures were confirmed by IR, 1H NMR, 13C NMR and HR-MS techniques. The target compounds were evaluated for their anti-tumor activities against cervical cancer HeLa cells by 3-（4,5-dimethylthi- azol-2-yl）-2,5-diphenyltetrazolium bromide （MTT） method, and the results indicated that compounds 4a, 6a, 7b, gb and lie of all the derivatives displayed better activities than resveratrol against HeLa cells, the compounds 6a and 8b displayed excellent inhibition effect, with IC50 values of 22.7 and 18.0 μmol/L, respectively, even higher than that of resveratrol （IC50=114 μmol/L）. The inhibitory ratio of compounds 6a and gb were 95.5% and 87.7% against HeLa cells at the concentration of 150 μmol/L.

关 键 词：白藜芦醇 衍生物 合成 HELA细胞 抗肿瘤活性 

分 类 号：R284[医药卫生—中药学] R285[医药卫生—中医学]