丹参酮ⅡA磺酸钠和丹参素对猪冠状动脉平滑肌细胞钙激活钾通道的激活机制

Mechanisms of activation of sodium tanshinone ⅡA sulfonate and danshensu on calcium-activated potassium channels in porcine coronary artery smooth muscle cells

目的研究丹参酮ⅡA磺酸钠(DS-201)和丹参素(DS-182)的冠状动脉舒张作用除了已知的机制外,是否还与钙激活钾通道(KCa)有关。方法猪冠脉平滑肌细胞贴附式和内面向外式膜片钳单通道电流记录技术。结果DS-201和DS-182均可激活冠脉平滑肌细胞KCa,但DS-201在内面向外膜片方式下激活KCa;而DS-182在细胞贴附膜片方式下激活KCa。结论DS-201和DS-182激活KCa的作用机制不同。DS-201能直接激活KCa,而DS-182则可能需要一系列胞内过程。这种差异可能与二者的结构和溶解性质不同有关。

AIM To investigate whether one of the mechanisms of coronary vasodilation of sodium tanshinone II A sulfonate （DS-201） and danshensu （DS-182） is the activation of calcium-activated potassium （KCa） channels in coronary artery smooth muscle cells. METHODS The cell-attached and inside-out porcine coronary artery patch-clamp technique of smooth muscle cells. RESULTS Both DS-201 and DS-182 activated KCa channels. But DS-201 activated KCa channels in the inside-out configuration when DS-201 applied to the intracellular side of the patches; while DS182 in the cell-attached configuration, when DS182 applied to the extracellular side of the patches. CONCLUSION DS-201 and DS-182 activate Kca channels with different mechanisms. DS201 activates KCa channels directly; while DS-182 may activate KCa channels indirectly through the intracellular system, which probably results from their differences of structure and soluble properties.