The current report focuses on purification, structural and functional characterization of Cerastategrin from Cerastes cerastes venom, a novel basic disintegrin (pI 8.36) with 128 amino acid residues and a molecular weight of 13 835.25 Da measured by MALDI-MSMS. The 3D structure of Cerastategrin is organized as α-helix (13%), β-strand (15%) and disordered structure (30%) and presents homologies with several snake venom disintegrins. Structural modeling shows that Cerastategrin presents an RGD motif that connects specifically to integrin receptors. Cerastategrin exhibits the inhibition of ADP induced platelets with an IC₅₀ of 0.88 µg/mL and shows in vivo long stable anticoagulation effect 24 h post-injection of increasing doses ranging from 0.2 to 1 mg/kg, therefore, Cerastategrin maintained irreversibly the blood incoagulable. Moreover, Cerastategrin decreases the amount of bounded αIIbβ3 and reduced significantly the quantity of externalized P-Selectin. Cerastategrin acts as a molecule targeting specifically the receptor α_IIbβ₃; therefore, it behaves as a potent platelet activation inhibitor. As a new peptide with promising pharmacological properties, Cerastategrin could have a potential therapeutical effect in the vascular pathologies and may be a new effective treatment approach.

本报告的重点是从Cerastes cerastes毒液中的Cerastategrin的纯化，结构和功能表征，这是一种具有128个氨基酸残基，分子量为13835.25 Da的新型碱性双整合素（pI 8.36），通过MALDI-MSMS测定。Cerastategrin的3D结构组织为α-螺旋（13％），β-链（15％）和无序结构（30％），并呈现出与几种蛇毒双整合素的同源性。结构建模表明，Cerastategrin具有一个RGD基序，该基团专门连接至整联蛋白受体。Cerastategrin具有IC ₅₀抑制ADP诱导的血小板的作用浓度为0.88 µg / mL，并且在注射剂量从0.2到1 mg / kg的注射后24小时内显示出体内长期稳定的抗凝作用，因此，Cerastategrin不可逆地保持了血液的可凝结性。此外，Cerastategrin减少了结合的αIIbβ3的量，并显着减少了外化P-选择素的量。Cerastategrin充当分子靶向特异性α受体_IIB β ₃ ; 因此，它起着有效的血小板活化抑制剂的作用。Cerastategrin作为一种具有良好药理作用的新型肽，可能在血管病理学中具有潜在的治疗作用，并且可能是一种新的有效治疗方法。