白杨素衍生物的合成及其活性研究

Synthesis and Biological Evaulation of Chrysin Derivatives

合成白杨素衍生物并对其进行活性评价。以5,7-二羟基黄酮为原料,通过取代、水解、酰胺缩合反应合成白杨素的衍生物,然后采用MTT比色法测定白杨素及白杨素衍生物对EC109(食管癌)、HepG2(肝癌)、SW480(结肠癌)、Hela(宫颈癌)细胞增殖抑制作用。合成的白杨素衍生物对HepG2、SW480肿瘤细胞的IC50值比白杨素的IC50值低。该衍生物对HepG2、SW480肿瘤细胞的抗癌活性较白杨素有一定程度的提高。

Chrysin derivate was synthesized to evaluate its biological activities.5,7-dihydroxyflavone as raw material and with the chemical methods of substitution reaction,hydrolysis and amide condensation reaction,the chrysin was synthesized,and then its antiproliferative activities against human cancer cell EC109,HepG2,SW480,and Hela were evaluated.The anti-caner activities against HepG2,SW480 of chrysin derivate manifestly increased,compared with chrysin.Compound 3 displayed better of anti-cancer activities than chrysin against HepG2,SW480.