新型大豆异黄酮磺酸酯抑制血管平滑肌细胞增殖活性研究

摘要

To find compounds that have strong inhibition to the growth of vascular smooth muscle cells,effect of novel soybean isoflavone sulfonate on the proliferation of vascular smooth muscle cell was investigated in vitro with MMT method. The results showed that the inhibition rate on the proliferation of vascular smooth muscle cell was 56.06% in the 10-7 mol/L of the novel daidzein sulfonate (P <0.05) ,and it increased by about 1000 times compared with that of lead compound daidzein. The structure-activity relationship studies indicated that after the benzene sulfonate modification ,its spatial structure and charge distribution were change,as well as its polarizability ,from 26. 51 to 54.12 ,which was easier for drugs to reach the cell membrane and act with target precisely,thus enhance the drug efficacy.%为了寻找对血管平滑肌细胞异常增殖有较强抑制作用的化合物,本文用MMT法考察新型大豆苷元磺酸酯体外抑制血管平滑肌细胞增殖活性.结果表明:该大豆苷元磺酸酯对血管平滑肌细胞增殖在10-7 mol/L时有抑制作用(P＜0.05),该浓度下的抑制率为56.06％,与先导化合物大豆苷元相比活性提高约1000倍.构效关系研究表明,大豆苷元经苯磺酸酯修饰,改变分子的空间结构、分子的可极化率从26.51增加到54.12,改变了药物的电荷分布,更有利于药物通过细胞膜到达靶标和与靶标更精确作用而导致药物药理作用大大增强.药理实验与构效关系研究初步表明,该大豆苷元磺酸酯有进一步研究价值.