[关键词]
[摘要]
巴西苏木红素为中药苏木的主要活性成分之一。利用体外血管舒缩试验以及血管平滑肌细胞试验,从分子生物学角度对巴西苏木红素舒血管效应及其机制进行了研究。结果表明,巴西苏木红素主要通过影响K+通道,抑制膜去极化,进而使血管舒张。这种效应与阻断5-HT 受体有关。同时还与调控胞内Ca2+浓度,影响钙调蛋白,下调MLCP 有关。这一过程中cAMP、PKA 和PGI2 也受巴西苏木红素影响并参与了调控。
[Key word]
[Abstract]
Brazilein is one of the active ingredients of a Chinese medicine Caesalpinia sappan L. This study was aimed to test the vasodilator effect of brazilein on vascular smooth muscle cells in vitro from the perspective of molecular biology. The results showed that brazilein mainly acted through the influence of potassium ion channels,reducing membrane depolarization in order to affect the vessel relaxation. This effect can be influenced by blocking 5 -HT receptor, and, simultaneously, correlating with the regulation of intracellular calcium ion concentration, affecting calmodulin and downregulating MLCP. In addition, the alterations of cAMP, PKA and PGI2 were involved in the pharmacological process of brazilein.
[中图分类号]
[基金项目]
科学技术部国家“十二五”计划“重大新药创制”科技重大专项(2012ZX09102201-008):国家一类中药新药巴西苏木红素注射剂的研究,负责人:杜力军。