地奥司明诱导大鼠离体股静脉平滑肌收缩装置对Ca2+敏感性增加。
Diosmin-induced increase in sensitivity to Ca2+ of the smooth muscle contractile apparatus in the rat isolated femoral vein.
作者信息
Savineau J P, Marthan R
机构信息
Laboratoire de Physiologie, Université de Bordeaux II, France.
出版信息
Br J Pharmacol. 1994 Apr;111(4):978-80. doi: 10.1111/j.1476-5381.1994.tb14838.x.
Abstract
The effect of diosmin, a flavone derivative, on the Ca2+ sensitivity of the venous contractile apparatus was investigated in chemically (beta-escin) skinned strips from the rat isolated femoral vein. Diosmin (0.5-10 microM) shifted to the left the concentration-response curve to Ca2+ (0.05-5 microM). The maximal effect was observed in the presence of 1 microM diosmin which increased the contractile response evoked by 0.15 microM Ca2+ from 26.3% to 78.9% of the maximal Ca(2+)-induced response. This work demonstrates that the venotonic action of diosmin involves an increase in the Ca2+ sensitivity of the contractile apparatus. Such a mechanism of action could represent a new and important means of therapeutic control of vasomotor activity.
摘要
在大鼠离体股静脉的化学（β-七叶皂苷）去皮肌条中，研究了黄酮衍生物地奥司明对静脉收缩装置Ca2+敏感性的影响。地奥司明（0.5 - 10微摩尔）使Ca2+（0.05 - 5微摩尔）的浓度-反应曲线向左移动。在1微摩尔地奥司明存在下观察到最大效应，它使0.15微摩尔Ca2+诱发的收缩反应从最大Ca(2+)诱导反应的26.3%增加到78.9%。这项研究表明，地奥司明的静脉张力作用涉及收缩装置Ca2+敏感性的增加。这种作用机制可能代表了一种新的、重要的血管运动活性治疗控制手段。
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