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高圣草素-7-O-β-D-葡萄糖苷是从中草药槲寄生中提取分离的一种黄酮类化合物。已证实该化合物在体内外对血小板活化因子(PAF)诱导的人及兔血小板聚集有明显的抑制作用。本研究应用放射配体[3H]PAF与受体结合的抑制实验证实该化合物是在受体水平上阻断了PAF对血小板的活化作用。抑制呈剂量效应关系,化合物浓度的负对数与抑制率明显相关γ=0.985,P<0.05)。在浓度大于1×10~-5 mol·L~-1时,增加浓度,不能提高抑制率,提示抑制的饱和。抑制的IC50为8×10~-7 mol·L~-1。首次发现,高圣草素-7-O-β-D-葡萄糖苷通过阻断PAF受体而抑制PAF诱导的血小板聚集。
Hypertechin-7-O-β-D-glucoside is a flavonoid extracted from the Chinese herbal medicine mistletoe. This compound has been shown to significantly inhibit platelet aggregation induced by platelet-activating factor (PAF) in humans and rabbits both in vitro and in vivo. In the present study, inhibition of the binding of [3H] PAF to the receptor by radioligand was demonstrated to inhibit the activation of platelet by PAF at the receptor level. Inhibition showed a dose-response relationship, the negative logarithm of compound concentration and inhibition rate was significantly related to γ = 0.985, P <0.05). When the concentration is more than 1 × 10 -5 mol·L -1, increasing the concentration can not increase the inhibition rate, suggesting the inhibition of saturation. The IC50 of inhibition was 8 × 10 -7 mol·L -1. It was first found that ascorbic acid-7-O-β-D-glucoside inhibits PAF-induced platelet aggregation by blocking the PAF receptor.