论文部分内容阅读
体外和体内试验证明,AP921总黄酮对PAF诱导的血小板聚集有明显的抑制作用,静注AP921血小板聚集有效抑制量后,兔全血PAF浓度无显著改变。对乙酸乙酯相提取物行硅胶层析,获得3种结晶化合物。药效监测发现,化合物Ⅱ对PAF诱导的血小板聚集有明显的抑制作用。经红外光谱、核磁共振谱和质谱分析,确定其分子结构为高圣草素-7-O-β-D-葡萄糖甙,PAF受体结合竞争抑制试验表明,高圣草素-7-O-β-D-葡萄糖甙具有与PAF竞争受体的作用,其IC50为8.0×10-7mol/L。研究证实AP921为一种新的PAF拮抗剂
In vitro and in vivo tests showed that total flavonoids AP921 PAF-induced platelet aggregation was significantly inhibited, intravenous injection of AP921 platelet aggregation effective inhibition, rabbit whole blood PAF concentration was not significantly changed. The ethyl acetate extract was subjected to silica gel chromatography to obtain three kinds of crystalline compounds. Efficacy monitoring found that compound Ⅱ significantly inhibited PAF-induced platelet aggregation. The results of IR, 1HNMR and MS showed that the molecular structure of the compound was as follows: HH, -7-O-β-D-glucoside and PAF receptor binding inhibition test. β-D-glucoside has the effect of competing with PAF for receptor with IC50 of 8.0 × 10-7mol / L. The study confirmed that AP921 is a new PAF antagonist