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目的 :研究滨蒿内酯 (scoparone ,Scop)对离体大鼠主动脉平滑肌张力的影响。方法 :通过测定离体血管环张力变化 ,观察Scop对主动脉平滑肌的舒张作用及与苯肾上腺素 (PE)、普萘洛尔 (Prop)和氯化钾 (KCl)之间的相互作用。结果 :Scop舒张离体主动脉平滑肌 ,并且对内皮完整 (EC +)标本的舒张作用明显大于去内皮 (EC - )标本 ,半抑制浓度 (IC50 )分别为 (10 0± 0 4 ) μmol/L(CE +)与 (83 2± 0 8) μmol/L(EC - ) (P <0 0 1) ;Scop使PE量效曲线下移 ,呈非竞争性抑制 ,亲和力指数 (PD2 )分别为 4 93± 0 0 5 (EC +)与 2 94± 0 14 (EC - ) ;Prop(1μmol/L)对Scop舒张血管平滑肌作用无影响 ;Scop不能抑制Prop所致血管平滑肌收缩 ;Scop对血管平滑肌的依内钙及依外钙性收缩均有明显抑制作用。结论 :Scop可舒张离体大鼠主动脉平滑肌 ,此作用与内皮细胞的功能有一定关系。Scop抑制血管平滑肌依内钙与依外钙性收缩可能是Scop舒张血管平滑肌的主要机制
Objective: To study the effect of scoparone (Scop) on the tension of isolated rat aortic smooth muscle. METHODS: By measuring the changes in the tension of isolated blood vessel rings, the relaxation effects of Scop on aorta smooth muscle and the interactions with phenylephrine (PE), propranolol (Prop) and potassium chloride (KCl) were observed. RESULTS: Scops attenuated isolated aortic smooth muscle and showed a significantly greater relaxant effect on endothelium-intact (EC+) specimens than did deendothelial (EC-) specimens. The half-inhibitory concentration (IC50) was (10 0 ± 0 4) μmol/L, respectively. (CE +) and (83 2 ± 0 8) μmol/L (EC - ) (P <0 01); Scops shifts down the PE dose-response curve, showing no competitive inhibition, with an affinity index (PD2) of 4 93± 0 0 5 (EC +) and 2 94± 0 14 (EC − ); Prop (1 μmol/L) had no effect on the effect of Scoop on vascular smooth muscle; Scop could not inhibit Prop-induced vascular smooth muscle contraction; Scop on vascular smooth muscle Intra-calcium and extravasated calcium contractions all have significant inhibitory effects. Conclusion :Scop can relax isolated rat aortic smooth muscle. This effect is related to the function of endothelial cells. Scop inhibition of vascular smooth muscle ingrowth calcium and epilepsy calcium contraction may be the main mechanism of Scop vascular smooth muscle relaxation