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Endothelium-independent vasorelaxation by leonurine, a plant alkaloid purified from Chinese motherwort.

机译:益母草碱是一种不依赖内皮的血管舒张作用,这是一种从中国益母草中提纯的植物生物碱。

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摘要

Leonurine, a plant alkaloid present in Chinese motherwort, induced concentration- dependent and endothelium-independent relaxation of phenylephrine (PE)- pretreated rat aortic arterial rings. The IC50 values for leonurine were 86.4+/-10.4 and 85.9+/-17.2 microM in the presence and absence of endothelium respectively. It inhibited the responses of aortic smooth muscle to PE in Ca2+ free medium containing 100 microM EGTA, suggesting a possible action on the release of intracellular Ca2+. Leonurine is not a specific alpha-adrenoceptor blocker, since it also caused a concentration-dependent inhibition of vascular contractile responses to KCl with an IC50 value of 96.4+/-13.4 microM, suggesting that leonurine also blocks the L-type Ca2+-channel. In addition, leonurine relaxed the aortic contraction induced by prostaglandin F2alpha (PGF2alpha). These inhibitory effects of leonurine were reversible and did not affect the resting tension. In conclusion, these findings suggest that leonurine is an effective inhibitor of vascular smooth tone, probably acting by inhibiting the Ca2+ influx and the release of intracellular Ca2+.
机译:益母草中存在的植物生物碱益母草碱可引起去氧肾上腺素(PE)预处理的大鼠主动脉环的浓度依赖性和内皮依赖性松弛。在有和没有内皮的情况下,leonurine的IC50值分别为86.4 +/- 10.4和85.9 +/- 17.2 microM。在含有100 microM EGTA的不含Ca2 +的培养基中,它抑制了主动脉平滑肌对PE的反应,表明可能对释放细胞内Ca2 +具有作用。益母草嘌呤不是特异性的α-肾上腺素受体阻滞剂,因为它也引起浓度依赖性的对KCl的血管收缩反应的抑制,IC50值为96.4 +/- 13.4 microM,这表明益母草嘌呤还可以阻断L型Ca2 +通道。此外,Leonurine缓解了前列腺素F2alpha(PGF2alpha)诱导的主动脉收缩。精氨酸的这些抑制作用是可逆的,并且不影响静息张力。总之,这些发现表明,精氨酸是血管平滑肌的有效抑制剂,可能通过抑制Ca2 +内流和细胞内Ca2 +的释放而起作用。

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