title: Interaction of 3H-defibrotide with cultured human umbilical vein endothelial cells.
abstract: 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.
authors.affiliation: Department of Biochemistry, Faculty of Medicine, Marmara University, Haydarpaşa-Istanbul, Turkey.
authors.forename: S
authors.initials: S
authors.lastname: Bilsel
authors.forename: A S
authors.initials: AS
authors.lastname: Yalçin
authors.forename: Y
authors.initials: Y
authors.lastname: Taga
authors.forename: K
authors.initials: K
authors.lastname: Emerk
mesh_terms: D001665:Binding Sites; D002478:Cells, Cultured; D004730:Endothelium, Vascular / Q000378:metabolism*; D005343:Fibrinolytic Agents / Q000378:metabolism; D006801:Humans; D007700:Kinetics; D011089:Polydeoxyribonucleotides / Q000378:metabolism*
chemical_list: D005343:Fibrinolytic Agents; D011089:Polydeoxyribonucleotides; C036901:defibrotide