Gargouil Y M, Perdrix L, Chapelain B, Gaborieau R
Départment de Biologie, Celle l'Evescault, France.
Int Angiol. 1989 Oct-Dec;8(4 Suppl):19-22.
The effect of Daflon 500 mg, consisting of 90% diosmin and 10% hesperidin, on bovine veins and lymphatic vessels was shown. The recording of mechanical tension on metacarpal vein rings demonstrated a dose-effect relationship with an ED50 of 0.5 X 10(-6) M. This effect observed on isolated organs, is close to the tonic effect of Daflon 500 mg observed in human. An effect was also observed as demonstrated by the depolarisation curve obtained after administration of solutions containing increasing concentrations of potassium. The curve was shifted to the right which may indicate a decrease in potassium permeability in the presence of Daflon 500 mg. On lymphatic vessels isolated from mesenterium, the main effect was an increase in the frequency of spontaneous response which could explain the effect of Daflon 500 mg on lymph flow as shown previously. This dose-effect relationship could be due to an increase in the sensitivity of receptors to some agonists. However, this effect could be pleiotropic. This pleiotropic effect could involve the stimulation by Daflon 500 mg of other cellular mechanisms such as phosphatidylinositol metabolism, or more directly, the pacemaker activity of the cells which govern spontaneous activity, pacemaker activity being under the control of membrane potassium permeability. Some evidence about the action of Daflon 500 mg on potassium permeability could also be shown on other tissues.
研究显示了由90%地奥司明和10%橙皮苷组成的500毫克微粒化纯化黄酮类药物（Daflon 500 mg）对牛静脉和淋巴管的作用。掌静脉环机械张力记录显示出剂量效应关系，半数有效剂量（ED50）为0.5×10⁻⁶ M。在离体器官上观察到的这种效应，与在人体中观察到的500毫克微粒化纯化黄酮类药物的强直性效应相近。给药含递增浓度钾的溶液后获得的去极化曲线也证实了一种效应。曲线右移，这可能表明在存在500毫克微粒化纯化黄酮类药物的情况下钾通透性降低。在从肠系膜分离出的淋巴管上，主要效应是自发反应频率增加，这可以解释先前所示的500毫克微粒化纯化黄酮类药物对淋巴流动的影响。这种剂量效应关系可能是由于受体对某些激动剂的敏感性增加。然而，这种效应可能具有多效性。这种多效性效应可能涉及500毫克微粒化纯化黄酮类药物对其他细胞机制的刺激，如磷脂酰肌醇代谢，或者更直接地说，涉及控制自发活动的细胞的起搏器活性，起搏器活性受膜钾通透性的控制。关于500毫克微粒化纯化黄酮类药物对钾通透性作用的一些证据也可以在其他组织上显示出来。
