Institute of Materia Medica, Taishan Medical University, Middle of Changcheng Road, Taian, Shandong 271016, China.
J Ethnopharmacol. 2011 Sep 1;137(1):547-52. doi: 10.1016/j.jep.2011.06.013. Epub 2011 Jun 16.
Sophora flavescens (SF) is a known medicinal herb for the treatment of cardiovascular symptoms associated with arrhythmia in China. However, the pharmacological action mechanisms involved have not been well studied. The aim of the present study was to define effects of roots of SF on the vascular tension and responsible mechanisms in rat thoracic aorta.
Ethanol extract of the roots of SF (ESF) was examined for their vascular relaxant effect in isolated phenylephrine-precontracted rat thoracic aorta.
ESF (0.1-100 μg/ml) induced relaxation of the phenylephrine-precontracted aortic rings in a concentration-dependent manner. Endothelium-denudation abolished the ESF-induced vasorelaxation. Pretreatment of the endothelium-intact aortic rings with l-NAME, an inhibitor of nitric oxide synthase, and ODQ, an inhibitor of soluble guanylyl cyclase (sGC), inhibited ESF-induced vasorelaxation. ESF increased cGMP levels of the aortic rings in a concentration-dependent manner and the effect was blocked by l-NAME and ODQ. Inhibition of K(+) channels with glibenclamide and tetraethylammonium, cyclooxygenase inhibition with indomethacin, and β-adrenergic and muscarinic receptors blockade had no effect on the ESF-induced vasorelaxation.
These findings suggest that ESF relaxes vascular smooth muscle via endothelium-dependent NO-sGC-cGMP signaling pathway.
苦参(SF)是一种已知的草药,用于治疗中国与心律失常相关的心血管症状。然而,其涉及的药理作用机制尚未得到很好的研究。本研究旨在确定苦参根对大鼠胸主动脉血管张力的影响及其作用机制。
采用乙醇提取物苦参根(ESF),观察其对预先收缩的离体大鼠胸主动脉的血管舒张作用。
ESF(0.1-100μg/ml)浓度依赖性地诱导预先收缩的主动脉环松弛。内皮细胞剥脱消除了 ESF 诱导的血管舒张作用。预先用一氧化氮合酶抑制剂 l-NAME 和可溶性鸟苷酸环化酶(sGC)抑制剂 ODQ 处理内皮完整的主动脉环,抑制了 ESF 诱导的血管舒张作用。ESF 浓度依赖性地增加主动脉环中环鸟苷酸(cGMP)的水平,该作用被 l-NAME 和 ODQ 阻断。用格列本脲和四乙铵抑制 K+通道、用吲哚美辛抑制环氧化酶以及阻断β-肾上腺素能和毒蕈碱受体,均对 ESF 诱导的血管舒张作用无影响。
这些发现表明 ESF 通过内皮依赖性 NO-sGC-cGMP 信号通路舒张血管平滑肌。