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目的为寻找活性高的肽类血小板聚集抑制剂,我们合成了RGD(Arg-Gly-Asp)肽类似物-RGDPe(Ac-Arg-Gly-Asp-NHCH2CH2C6H5),以验证其体外抗血小板聚集活性。方法以人血为标本,采用比浊法测定血小板聚集和同位素标记方法测定其竞争性抑制125I标记的纤维蛋白原(Fgn)与血小板糖蛋白(GP)Ⅱb/Ⅲa结合的能力,并与Sigma公司合成的RGDS(阳性对照)和生理盐水(阴性对照)比较。结果RGDPe抑制125I-Fgn与活化血小板GPⅡb/Ⅲa结合的IC50=3.64±0.55×10-5M(RGDS:6.03±1.24×10-5M),抗ADP诱导的血小板聚集IC50=76.42±55.42μM(RGDS:114.67±40.55μM)。结论RGDPe有较强的抑制血小板聚集活性,可能在体内有预防血栓形成功效。
OBJECTIVE To find an active peptide aggregation inhibitor, we synthesized RGD (Arg-Gly-Asp) peptide analogue-RGDPe (Ac-Arg-Gly-Asp-NHCH2CH2C6H5) to verify the anti-platelet aggregation activity in vitro. Methods Using human blood as sample, the ability of 125I-labeled fibrinogen (Fgn) to bind to platelet glycoprotein (GP) Ⅱb / Ⅲa was determined by turbidimetric platelet aggregation and isotope labeling. The synthetic RGDS (positive control) and saline (negative control) were compared. Results The IC50 of RGDPe for inhibiting 125I-Fgn binding to activated platelet GPⅡb / Ⅲa was 3.64 ± 0.55 × 10-5M (RGDS: 6.03 ± 1.24 × 10-5M), and the anti-ADP-induced platelet aggregation IC50 = 76.42 ± 55.42 μM (RGDS: 114.67 ± 40.55 μM). Conclusion RGDPe has a strong inhibition of platelet aggregation activity, may have the effect of preventing thrombosis in vivo.