Bilsel S, Yalçin A S, Taga Y, Emerk K
Department of Biochemistry, Faculty of Medicine, Marmara University, Haydarpaşa-Istanbul, Turkey.
Thromb Res. 1990 Jun 1;58(5):455-60. doi: 10.1016/0049-3848(91)90250-z.
Defibrotide is a profibrinolytic and antithrombotic drug which seems to modulate endothelial cell function. In this study, a method for radioactive labeling of the drug and its interaction with cultured endothelial cells is proposed. 3H-Acetic anhydride was used to label defibrotide. Endothelial cells obtained by collagenase treatment of human umbilical cord veins were cultured in 24-welled plastic culture dishes. Binding experiments were carried out by incubating cell cultures with media containing various concentrations of labeled defibrotide. Our results showed that labeled defibrotide has a KL value of 4.2 micrograms/ml for endothelial cells. Although the presence of a specific transporter is possible, the high molecular weight of the fraction used suggests that the interaction is binding to a specific receptor.
去纤苷是一种具有促纤溶和抗血栓作用的药物，似乎能调节内皮细胞功能。在本研究中，提出了一种对该药物进行放射性标记及其与培养的内皮细胞相互作用的方法。使用3H-乙酸酐对去纤苷进行标记。通过用胶原酶处理人脐静脉获得的内皮细胞，在24孔塑料培养皿中培养。通过将细胞培养物与含有不同浓度标记去纤苷的培养基孵育来进行结合实验。我们的结果表明，标记的去纤苷对内皮细胞的KL值为4.2微克/毫升。尽管可能存在特定的转运体，但所用组分的高分子量表明这种相互作用是与特定受体的结合。
