摘要
采用氮烷基化、羟基保护、醛酮缩合的三步反应合成了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单羰基姜黄素类似物对肺癌细胞H1299、结肠癌细胞HT-29、胰腺癌细胞BxPC-3和前列腺癌细胞PC-3的抗肿瘤活性.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4种肿瘤细胞均有较强的抑制作用,其中化合物A6半数抑制浓度IC50均在0.65μmol/L以下,抗癌活性比姜黄素提高40倍以上.
Eight mono-carbonyl curcumin analogues were synthesized by a three-step reaction of alkylation,hydroxyl protection,and aldehyde ketone condensation. Their structures were characterized by1 H NMR and ESI-MS techniques. All the compounds were 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 inhibitory effects on the growth of cultured PC-3,BxPC-3,HT-29 and H1299 cells. The IC50 of compound A6 was lower than 0. 65μmol/L in all four cell lines,and A6 was 40-fold more active than curcumin.
出处
《华南师范大学学报（自然科学版）》
CAS
北大核心
2014年第3期82-86,共5页
Journal of South China Normal University(Natural Science Edition)
基金
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)
关键词
单羰基姜黄素类似物
合成
抗肿瘤活性
mono-carbonyl curcumin analogues
synthesis
anticancer activity
