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新型单羰基姜黄素类似物的合成及抗肿瘤活性研究
引用本文:周代营,田宇光,杜志云,赵肃清,郑希,张焜.新型单羰基姜黄素类似物的合成及抗肿瘤活性研究[J].华南师范大学学报(自然科学版),2014,46(3):82-0.
作者姓名:周代营  田宇光  杜志云  赵肃清  郑希  张焜
作者单位:1.1.广东食品药品职业学院
基金项目:国家自然科学基金项目(B0207&21272043);广州市第一批菁英计划留学项目(11YB02)
摘    要:采用氮烷基化、羟基保护、醛酮缩合三步反应合成了8个新型单羰基姜黄素类似物,结构经质谱、核磁共振氢谱和核磁共振碳谱等手段进行确认。并采用MTT染色法体外检测所合成的8个单羰基姜黄素类似物对人肺癌细胞H1299,结肠癌细胞HT-29,人体胰腺癌细胞BxPC-3和人前列腺癌细胞PC-3的抗癌活性。半数抑制浓度IC50值结果显示:所合成的8个姜黄素类似物对四种细胞均有较强的抑制作用,其中化合物A6在四种细胞中的半数抑制浓度IC50均在0.65 μM以下,抗癌活性比姜黄素提高了40倍以上。

关 键 词:抗肿瘤活性
收稿时间:2014-01-17

Synthesis and Anti-tumor Properties of Mono-carbonyl Curcumin Analogues
Zhou Daiying;Tian Yuguang;Du Zhiyun;Zhao Suqing;Zheng Xi;Zhang.Synthesis and Anti-tumor Properties of Mono-carbonyl Curcumin Analogues[J].Journal of South China Normal University(Natural Science Edition),2014,46(3):82-0.
Authors:Zhou Daiying;Tian Yuguang;Du Zhiyun;Zhao Suqing;Zheng Xi;Zhang
Institution:Zhou Daiying;Tian Yuguang;Du Zhiyun;Zhao Suqing;Zheng Xi;Zhang Kun;Guangdong Food and Drug Vocational College;Guangdong University of Technology;
Abstract:Eight Mono-carbonyl curcumin analogues were synthesized by three-step reaction of alkylation, hydroxyl protection, aldehyde ketone condensation. Their structures were characterized by 1H NMR and ESI-MS techniques. Then all the compounds were synthesized and evaluated for their effects on cultured prostate cancer PC-3 cells, pancreas cancer BxPC-3 cells, colon cancer HT-29 cells and lung cancer H1299 cells. These compounds exhibited potent inhibitory effects on the growth of cultured PC-3, BxPC-3, HT-29 and H1299 cells. The IC50 for A6 was lower than 0.65μM in all four cell lines, and A6 was 40-fold more active than curcumin.
Keywords:
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