短足蒿叶水醇提取物的研究局目前通过钙内流堵塞介导的抗痉挛活性

F. S. Monteiro, J. S. Costa, Lenivaldo Jorge Alves Martins, Cláudia Quintino Rocha, A. C. Borges, M. O. R. Borges
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引用次数: 5

摘要

目的:考虑到其他大戟科植物也具有抗痉挛活性,决定采用化学分类标准,对短足Arrabidaea brachypoda叶片的抗痉挛活性进行测定。方法:将大鼠空肠各节段悬浮于含有特定生理盐水溶液的玻璃桶中,在适当温度下,稳定期后,用收缩剂刺激,观察EHFAB的抑制或松弛作用。结果:EH-FAB中含有以芦丁为主的10种化合物,具有抑制离体大鼠空肠收缩的相位成分和放松紧张性成分的抗痉挛活性。为了评估抗痉挛作用的机制,我们绘制了CCh的累积曲线,其中由于控制曲线向右移位和最大收缩效应(Emax)降低,观察到非竞争性拮抗作用。之后,通过增加细胞外钾来评估钙和/或钾通道的参与,观察到EH-FAB放松了大鼠空肠,表明Ca2+通道的参与。为了证实这一假设,EH-FAB在Ca2+的自由去极化溶液中对Ca2+的累积曲线进行了测试,观察到随着Emax的减少,曲线向右移动。结论:EH-FAB在离体大鼠空肠中具有抗痉挛活性,并可能阻断Ca2+通过电压门控钙通道的流入,表明其治疗绞痛和/或腹泻的潜力。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Hydroalcoholic extract of leaves of Arrabidaea brachypoda (DC.) Bureau present antispasmodic activity mediated through calcium influx blockage
Aim: Since other species of the Bignoniaceae Family presented of antispasmodic activity, it was decided, by chemotaxonomic criterion, to determine the antispasmodic activity of the leaves of Arrabidaea brachypoda. Methodology: the segments of the rat jejunum were suspended in glass vats containing specific saline solution, at an appropriate temperature, and after stabilization period, were stimulated by a contractile agent to observe the inhibitory or relaxing effect of EHFAB. Results: EH-FAB showed the presence of 10 compounds, mainly rutin and it has an antispasmodic activity as it inhibits the phasic component and relaxes the tonic component of the contraction in isolated rat jejunum. To assess the mechanism of antispasmodic action, cumulative curves to the CCh were performed in which a non-competitive antagonism was observed, due to a displacement of the control curve to the right and reduction of the maximum contraction effect (Emax). Afterward, the participation of the calcium and/or potassium channels was evaluated by increasing the extracellular potassium, and it was observed that the EH-FAB relaxed the rat jejunum, suggesting the participation of the Ca2+ channels. To corroborate that hypothesis, the EH-FAB was tested against cumulative curves to Ca2+ in a free depolarizing solution of Ca2+, and it was observed that there was a shift of the curve to the right with a reduction in Emax. Conclusions: EH-FAB presents antispasmodic activity in isolated rat jejunum and it is suggested to block the influx of Ca2+ through voltage-gated calcium channels, signaling the therapeutic potential for the treatment of colic and/or diarrhea.
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