Department of Pharmacology, School of Basic Medical Science, Ningxia Medical University, Yinchuan 750004, Ningxia, China.
Biomed Environ Sci. 2009 Aug;22(4):327-32. doi: 10.1016/S0895-3988(09)60063-5.
To determine whether matrine, a kind of traditional Chinese medicinal alkaloid, can relax the aortic smooth muscles isolated from guinea pigs and to investigate the mechanism of its relaxant effects.
Phenylephrine or potassium chloride concentration-dependent relaxation response of aortic smooth muscles to matrine was studied in the precontracted guinea pigs.
Matrine (1 x 10(-4) mol/L -3.3 x 10(3) mol/L) relaxed the endothelium-denuded aortic rings pre-contracted sub-maximally with phenylephrine, in a concentration-dependent manner, and its pre-incubation (3.3 x 10(-3) mol/L) produced a significant rightward shift in the phenylephrine dose-response curve, but had no effects on the potassium chloride-induced contraction. The anti-contractile effect of matrine was not reduced by the highly selective ATP-dependent K+ channel blocker glibenclamide (10(-5) mol/L), either by the non-selective K+ channel blocker tetraethylammonium (10(-3) mol/L), or by the beta-antagonist propranolol (10(-5) mol/L). In either "normal" or "Ca(2+)-free" bathing medium, the phenylephrine-induced contraction was attenuated by matrine (3.3 x 10(-3) mol/L), indicating that the vasorelaxation was due to inhibition of intracellular and extracellular Ca2+ mobilization.
Matrine inhibits phenylephrine-induced contractions by inhibiting activation of alpha-adrenoceptor and interfering with the release of intracellular Ca2+ and the influx of extracellular Ca2+.
确定苦参碱(一种传统的中药生物碱)是否可以松弛豚鼠离体主动脉平滑肌,并探讨其舒张作用的机制。
研究了苦参碱对预先收缩的豚鼠主动脉平滑肌对苯肾上腺素或氯化钾浓度依赖性松弛反应的影响。
苦参碱(1 x 10(-4) mol/L-3.3 x 10(3) mol/L)浓度依赖性地松弛了预先用苯肾上腺素最大程度收缩的去内皮主动脉环,并预先孵育(3.3 x 10(-3) mol/L)导致苯肾上腺素剂量反应曲线显著右移,但对氯化钾诱导的收缩没有影响。苦参碱的抗收缩作用不受高度选择性的 ATP 依赖性 K+通道阻滞剂格列本脲(10(-5) mol/L)、非选择性的 K+通道阻滞剂四乙铵(10(-3) mol/L)或β-拮抗剂普萘洛尔(10(-5) mol/L)的影响。无论是在“正常”还是“无钙”灌流液中,苦参碱(3.3 x 10(-3) mol/L)均可减弱苯肾上腺素引起的收缩,表明血管舒张是由于抑制细胞内和细胞外 Ca2+动员。
苦参碱通过抑制α-肾上腺素受体的激活和干扰细胞内 Ca2+的释放以及细胞外 Ca2+的内流来抑制苯肾上腺素引起的收缩。