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