Spiramine N-6属粉花秀线菊植物中提取分离的二十碳二萜生物碱.本实验采用Born,Shen和Hamburger等方法分别观察了spiramine N-6在体外和体内对兔血小板聚集功能的影响.应用荧光分光光度法测定其对血小板5-羟色胺释放反应的作用,同时评价spiramine N-6对激活的血小板与中性粒细胞之间粘附反应的影响.结果表明:spiramineN-6在体外选择性抑制血小板活化因子(PAF)诱导的血小板聚集,并呈量效关系,其IC50=26μmol/L,对花生四烯酸(AA)或腺苷二磷酸(ADP)引起的血小板聚集无明显作用;spiramine N-6静注后明显抑制PAF、AA和ADP诱导的血小板聚集.Spiramine N-6呈浓度依赖性减少AA和PAF引起血小板5-羟色胺的释放,其IC50分别为64.7和33.5 μmol/Lo Spiramine N-6明显阻抑激活的血小板与中性粒细胞间的粘附率,其IC50为78.6μmol/L.结果提示spiramine N-6作为二十碳二萜生物碱具有较强的抗血小板和阻抑血小板-中性粒细胞相互作用的生物活性.%Spiramine N-6, a C20-skeleton diterpenoid alkaloid, was isolated from Spiraea japonica L.f. In thispaper,the effects of spiramine N-6 were investigated on plate let aggregation in vitro and in vivo,platelet serotoninrelease, and on the binding of thrombin-stimulated platelets to neutrophils by use of the methods of Bom, Shen, andHamburger, respectively. The results showed that spiramine N-6 in vitro significantly inhibited platelet activatingfactor (PAF)-induced platelet aggregation in a concentration-dependent manner while had no influence on plateletaggregation induced by arachidonic acid (AA) or adenosine diphosphate (ADP) .The medium inhibitoryconcentration (IC50) on PAF was 26μmol/L. Intravenous spiramine N-6 markedly suppressed platelet aggregationinduced by ADP, AA, or PAF.Spiramine N-6 also decreased serotonin release from platelets activated by AA andPAF,obtaining the IC50 values of 64.7 and 33.5 μmol/L.Spiramine N-6 decreased the binding between thrombin-stimulated platelets and neutrophils with an IC50 of 78.6 μmol/L. It is suggested that spiramine N-6 inhibitedplatelet aggregation in vitro and in vivo, decreased serotonin release from platelet, and suppressed the binding ofactivated platelets to neutrophils.
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