麦角甾醇体外抗血小板聚集作用

摘要

Objective To evaluate the anti-platelet aggregation effect of ergosterol in vitro and explore the preliminary mechanism. Methods The anti-platelet aggregation activity of ergosterol was assessed in vitro on rabbit platelet aggregation. Different inducers, ADP ( 4 μmol?L-1 ) , collagen ( 4 μg?mL-1 ) , arachidonic acid ( AA, 1 mmol?L-1 ) and thrombin (0.5 U?mL-1), and blockers (ozagrel, dipyridamole, clopidogrel and aspirin) were applied to observe the potential targets of ergosterol, platelet aggregation induced by ADP (0, 1, 2, 4, 6μmol?L-1) or fibrinogen (0, 1, 2, 4, 6, 10 mg?mL-1). Results Ergosterol exhibited an obvious anti-platelet aggregation effect in vitro with IC50 values on different inducers ( ADP, collagen, AA and thrombin) of (19.3±0.8), (23.4±1.2), (26.7±0.7), (32.9±1.5) μmol?L-1, respectively. Conclusion Ergosterol can significantly inhibit aggregation and activation of platelet. It provides experimental basis for full exploration of ergosterol and development of novel anti-platelet aggregation drugs.%目的 研究麦角甾醇的抗血小板聚集作用及机制.方法 采用家兔体外血小板聚集实验方法,观察麦角甾醇对二磷酸腺苷(4μmol?L-1)、胶原蛋白(4μg?mL-1)、花生四烯酸(1 mmol?L-1)和凝血酶(0.5 U?mL-1)诱导体外血小板聚集的抑制活性?麦角甾醇与奥扎格雷、双嘧达莫、氯吡格雷和阿司匹林联合应用体外抗二磷酸腺苷(0,1,2,4,6μmol?L-1)与纤维蛋白原(0,1,2,4,6,10 mg?mL-1)诱导血小板聚集作用.结果 麦角甾醇对各诱导剂二磷酸腺苷、胶原蛋白、花生四烯酸、凝血酶抑制作用的半数抑制浓度(IC50值)分别为(19.3±0.8),(23.4±1.2),(26.7±0.7),(32.9±1.5)μmol?L-1.麦角甾醇抑制二磷酸腺苷及纤维蛋白原诱导聚集作用的协同相关性的线性最佳为双嘧达莫与氯吡格雷.结论 麦角甾醇能显著抑制血小板聚集及其功能活化,为麦角甾醇资源的充分开发及研制新的抗血小板聚集药物提供实验依据.