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Endothelium-Independent Vasorelaxant Effects of Hydroalcoholic Extract from Nigella sativa Seed in Rat Aorta: The Roles of Ca2+ and K+ Channels

机译:大鼠主动脉Nigella sativa种子中乙醇提取物的内皮依赖性血管舒张作用:Ca2 +和K +通道的作用

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摘要

Objective. The aim of this study was to elucidate the mechanism(s) responsible for the vasorelaxant effect of Nigella sativa (N. sativa). Methods. The activity of different concentrations of N. sativa extract was evaluated on contractile responses of isolated aorta to KCl and phenylephrine (PE). Results. The extract (2–14 mg/mL) induced a concentration dependent relaxation both in endothelium-intact and endothelium-denuded aortic rings precontracted by PE (10−6 M) and KCl (6 × 10−2 M). Extract reduced PE- and KCl-induced contractions in presence of cumulative concentrations of calcium (10−5–10−2 M) significantly. L-NAME and indomethacin had no effect on vasorelaxation effect of extract in PE-induced contraction. Diltiazem and heparin reduced significantly this vasorelaxation at a concentration of 14 mg/mL of extract; however, N. sativa-induced relaxation was not affected by ruthenium red. Tetraethylammonium chloride reduced the extract-induced relaxation in concentrations of 2–6 mg/mL of extract significantly but glibenclamide reduced this relaxative effect in all concentrations of extract. Conclusions. The inhibitory effect of N. sativa seed extract on the contraction induced by PE and KCl was endothelium-independent. This relaxation was mediated mainly through the inhibition of Ca2+ and KATP channels and also intracellular calcium release.
机译:目的。这项研究的目的是阐明造成Nigella sativa(N. sativa)的血管舒张作用的机制。方法。根据离体主动脉对KCl和去氧肾上腺素(PE)的收缩反应评估了不同浓度的紫花苜蓿提取物的活性。结果。提取物(2–14 mg / mL)在PE(10 -6 M)和KCl(6×10 −2 M)。在钙的累积浓度(10 −5 –10 −2 M)存在的情况下,提取物可减少PE和KCl引起的收缩。 L-NAME和消炎痛对PE引起的收缩中提取物的血管舒张作用没有影响。地尔硫卓和肝素在提取物浓度为14μmg/ mL时能显着降低血管舒张作用。然而,紫花苜蓿诱导的松弛不受钌红的影响。氯化四乙铵在2–6μmg / mL的提取物浓度下可显着降低提取物诱导的弛豫,但格列苯脲在所有浓度的提取物中均会降低这种弛豫作用。结论。苜蓿种子提取物对PE和KCl诱导的收缩的抑制作用与内皮无关。这种放松主要是通过抑制Ca 2 + 和KATP通道以及细胞内钙的释放来介导的。

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