新型大豆苷元磺酸酯抑制血管平滑肌细胞增殖活性

Inhibition effects of novel daidzein sulfonate on the proliferation of vascular smooth muscle cells

关键词:  大豆苷元  磺酸酯衍生物  血管平滑肌细胞  构效关系

Key words:  daidzein  sulfonate derivate  vascular smooth muscle cell  construction effect relation

摘要:

为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，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 6 mol/L时有抑制作用（P＜0.05），该浓度下的抑制率为64.62%，与先导化合物大豆苷元相比活性提高约100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40.32，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药理研究价值。

Abstract:

To find compounds that have a strong inhibitory effect to the proliferation of vascular smooth muscle cells，inhibition effects of novel daidzein sulfonate on the proliferation of vascular smooth muscle cells were investigated in vitro with MMT method. The result showed that its inhibiting rate on the proliferation of vascular smooth muscle cells was 64.62% in the 10 6 mol/L of the novel daidzein sulfonate(P＜0.05)，and it increased by about 100 fold compared with the inhibiting rate of lead compound daidzein. The construction effect relations studies indicated，its spatial structure and charge distribution were changed，its polarizability increased from 26.51 to 54.12，and these factors were more beneficial to the arrival at the target through the cell membrane and action more precisely with the target that led its pharmacological action to enhance greatly after its beautification of benzene sulfonate.