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海风藤酮是从中药海风藤(Piperfutokadsura)中提取的一种木脂素。本文运用放射配基受体分析及血小板聚集观察海风藤酮的作用,发现海风藤酮特异性地抑制血小板活化因子(PAF)与洗涤的兔血小板结合,其ki为2×10-12mol/L,体外实验显示特异性地抑制PAF引起的血小板聚集,IC50为2.6μmol/L,而对APP、AA引起的血小板聚集无效。半体内实验表明,0.1mg/kg海风藤酮抑制PAF引起血小板聚集的作用,可维持2小时。静脉(71mg/kg,14.2mg/kg)及口服(80g/kg;120mg/kg)海风藤酮抑制大鼠体内血小板血栓形成,其抑制率分别为25.4%,38.2%,21.4%又34.6%以上结果表明,海风藤酮是一血小板活化因子的特异性受体拮抗剂。
Sea buckthorn is a lignan extracted from Piperfutokadsura. In this paper, the use of radio ligand receptor assay and platelet aggregation observation of the role of kelp, and found that kelp specifically inhibit platelet activating factor (PAF) and washed rabbit platelet binding, the ki of 2 × 10-12mol / L, In vitro experiments showed that PAF can specifically inhibit platelet aggregation induced by PAF with an IC50 of 2.6μmol / L, which is ineffective against platelet aggregation induced by APP and AA. Half in vivo experiments showed that 0.1mg / kg kremlifene PAF platelet aggregation inhibitory effect, can be maintained for 2 hours. The inhibitory rates of intravenous (71mg / kg, 14.2mg / kg) and oral (80g / kg; 120mg / kg) tylosin on platelet thrombosis in rats were 25.4%, 38.2%, 21 .4% and 34.6% The above results show that kelp is a platelet-activating factor-specific receptor antagonist.