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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 ,并且不影响血浆正常的凝血功能
OBJECTIVE To find RGD peptide derivatives with higher activity and more stable antithrombotic effect, we designed and synthesized AoGDW peptide and investigated its in vitro anti-platelet aggregation activity, stability and its effect on plasma coagulation function. Methods ① The turbidimetric method was used to determine the inhibitory effect of AoGDW peptide on human platelet aggregation and its stability in plasma. ② the use of coagulation analyzer to determine its effect on plasma coagulation. Results The 50% inhibitory concentration (IC50) of AoGDW peptides on platelet aggregation was (47 ± 25) μmol / L, which was significantly lower than that of the negative control group and the positive control group (P <0.01). Incubation in plasma for 3 h still retained 10% activity. In addition, the indicators of coagulation activity thromboplastin time (TT), prothrombin time (PT), activated partial thromboplastin time (APTT) were within the normal range. Conclusion AoGDW peptide has a strong and stable inhibition of platelet aggregation in vitro and does not affect the normal plasma coagulation function