AoGDW肽体外抗血小板作用的研究

Studies about AoGDW′s antiplatelet action in vitro

目的 为寻找活性更高、作用更稳定的具有抗栓作用的RGD肽衍生物 ,我们设计合成了AoGDW肽 ,并研究其体外抗血小板聚集的活性、稳定性以及它对血浆凝血功能的影响。方法 ①采用比浊法测定AoGDW肽抑制人血小板聚集的活性以及在血浆中的稳定性。②利用血凝仪测定其对血浆凝血功能的影响。结果 AoGDW肽抑制血小板聚集的 5 0 %的抑制剂浓度 (IC50 )为 (4 7± 2 5 ) μmol/L ,与阴性对照组、阳性对照组相比 ,均为P <0 0 1。在血浆中孵育 3h仍保持 10 0 %的活性。另外血浆凝血功能各项指标凝血活酶时间 (TT)、凝血酶原时间 (PT)、活化部分凝血活酶时间 (APTT)均在正常范围内。结论 AoGDW肽在体外有较强的、稳定的抑制血小板聚集的作用 。

Objective To seek highly active,highly steady,highly specific RGD analog,the author designed and synthesized AoGDW peptide,then testified its activity,stability and effect on cruor of plasma.Methods Platelet aggregation was studied using aggregometer.Effect of AoGDW on cruor of plasma was testified by cruormeter.Results IC 50 value of inhibitor of platelet aggregation was (4 7±2 5) μmol/L, P <0 01,compared with NS or RGDS.AoGDW was achieved with improved plasma stability (100% activity after 3 h).TT,PT,APTT were normal after plasma preincubated with AoGDW.Conclusion AoGDW was a highly active,highly steady inhibitor of platelet aggregation and did not affect cruor of plasma.