摘要
目的研究RGD(精氨酸-甘氨酸-天门冬氨酸)肽衍生物-AoGDW(ω-氨基辛酸-甘氨酸-天门冬氨酸-色氨酸)抑制血小板聚集的作用机制。方法采用双色荧光标记以及流式细胞技术检测AoGDW肽对CD41抗体与血小板GPⅡb/Ⅲa受体结合的抑制作用以及对血小板膜上P-选择素表达的影响。结果随着AoGDW肽浓度的增加,CD41抗体与活化血小板GPⅡb/Ⅲa受体结合率呈现下降趋势,相对于阴性对照组,P<0.01。但CD41抗体与静止血小板GPⅡb/Ⅲa受体的结合率以及CD62p抗体与静止血小板P选择素的结合率与阴性对照组相比,P>0.05。结论AoG-DW肽是通过占据血小板上纤维蛋白原的结合位点即活化的GPⅡb/Ⅲa受体而发挥抑制血小板聚集的作用,并且不具有活化血小板的作用,是一种选择性的GPⅡb/Ⅲa受体拮抗剂。
Aim To confirm the mechanism of AoGDW （ω-aminooctanoic acid-glycine-aspartic acid-tryptophan ） inhibiting platelet aggregation. Methods Effects of AoGDW on CD41 antibody binding to platelet GP Ⅱ b/Ⅲ a and the expression of P （ selectin were assessed by FCM （flow cytometric messurements） using two-color assay. Results AoGDW inhibited CD41 antibody binding to activated platelets in a concentration-dependent manner （ P 〈 0. 01 ） versus negative group,but did not inhibit the binding of CD41 antibody to resting platelets. P-selectin binding to CD62p was not affected by AoGDW in resting platelets. Conclusion AoGDW competitive inhibited fibrinogen binding to the activated platelet receptor glycoprotein GP Ⅱ b/Ⅲ a and had no effect on platelet activation. AoGDW peptide was a kind of inhibitor of selective platelet GP Ⅱ b/Ⅲ a receptor.
出处
《中国药理学通报》
CAS
CSCD
北大核心
2007年第5期626-629,共4页
Chinese Pharmacological Bulletin
基金
山西医科大学大学生创新基金资助项目(No200474)
