藤黄酸衍生物的合成及抗肿瘤活性研究  

Synthesis and Bioevaluation of Gambogic Acid Derivatives as Antitumor Agents

作　　者：张生烈[1,2] 李乾[1,2] 张磊[1,2] 孙昊鹏[1,2] 尤启冬[1,2,3] 

机构地区：[1]天然药物活性组分与药效国家重点实验室、中国药科大学,南京210009 [2]中国药科大学药物化学教研室,南京210009 [3]江苏省肿瘤发生与干预重点实验室、中国药科大学,南京210009

出　　处：《有机化学》2012年第8期1450-1458,共9页Chinese Journal of Organic Chemistry

基　　金：国家自然科学基金(No.90713038);重大新药创制科技重大专项(No.2009ZX09501-003)资助项目~~

摘　　要：以藤黄酸为原料,经过C-32位选择性环氧化、高碘酸氧化、甲基化、Jones氧化、不同条件的酯化、酰胺化等反应步骤,合成了17个藤黄酸衍生物.所有目标化合物的结构均通过核磁共振谱、红外光谱和质谱证实,并采用MTT比色法对所合成的目标化合物进行了体外抗肿瘤细胞生物活性测试.结果表明,化合物5,7,8,13对人肝癌细胞(HepG2)、人结肠癌细胞(HCT-116)的增殖抑制活性显著强于藤黄酸.eventeen new compounds were synthesized from gambogic acid（GA） with the structural modification of C-32.The reaction steps included selective epoxidation,periodate oxidation,methylation,Jones oxidation,different conditions of esterification,amidation,etc.The structures of target compounds were confirmed by NMR,IR and MS/ESI techniques.Their antitumor activities were evaluated in vitro by MTT assay.The results showed that compounds 5,7,8 and 13 were more potent than GA to human hepatoma cells（HepG2） and colon carcinoma cells（HCT-116）.

关 键 词：藤黄酸 衍生物 合成 抗肿瘤 生物活性 

分 类 号：R284.1[医药卫生—中药学] R285[医药卫生—中医学]