【摘要】 采用四唑盐(MTT)比色法、白细胞弹性蛋白酶抑制剂筛选模型及二氢乳清酸脱氢酶抑制剂筛选模型对从玉竹中分离出的4个高异黄酮类化合物进行生物活性评价,探讨化合物结构与其活性之间的构效关系.高异黄酮类化合物1～4对肿瘤细胞K562,A549和HCT-15具有细胞毒性,IC50为7～35μg/mL;化合物1～4对人白细胞弹性蛋白酶有抑制作用,IC50分别为13.1,70.4,13.8,55.2μg/mL;化合物2,4对二氢乳清酸脱氢酶有一定的抑制作用,IC50分别为10.0,11.1μg/mL.高异黄酮类化合物的生物活性与其取代基的类型及位置有关.更多还原

【Abstract】 MTT assays were used to explore the inhibiting effect of the homoisoflavanones on cancer cell.Two high throughput screening modeles were established,one for screening human leukocyte elastase(HLE) inhibitor and the other for dihydroorotate dehydrogenase(DHODH) inhibitor from nature product.Compound 1~4 showed inhibitory activity on K562,A549 and HCT-15 cancer cell with IC50 from 7 to 35 μg/mL.Compound 1~4 showed inhibitory activity against HLE with IC50 of 13.1,70.4,13.8,55.2 μg/mL,respectively.Compound 2 and 4 showed inhibitory activity against DHODH with IC50 10.0,11.1 μg/mL,respectively.The location and type of substituent group affect biological activity of homoisoflavanones.更多还原