Uptake of suramin by human microvascular endothelial cells.
We have demonstrated for the first time that suramin is taken up by human dermal microvascular endothelial (HMEC-1) cells by an active process involving the caveolae system. The uptake of suramin was time-dependent and reduced by more than 90% when incubated in the presence of albumin or at 4 degrees C. Suramin uptake was also inhibited when incubated in the presence of filipin and digitonin, both potent cholesterol-binding agents, but not in the presence of probenecid. The [3H]suramin taken up by the HMEC-1 cells was located primarily within the nucleus, followed by the cytoplasmic fraction. The presence of suramin in these cellular compartments suggests that this drug may act through intracellular mechanisms.
Gagliardi
A R
AR
Veterans Affairs Medical Center and the Department of Obstetrics and Gynecology, University of Kentucky Medical Center, Lexington 40536-0305, USA.
Taylor
M F
MF
Collins
D C
DC
D000970:Antineoplastic Agents / Q000493:pharmacokinetics*; D002478:Cells, Cultured; D004730:Endothelium, Vascular / Q000378:metabolism*; D006801:Humans; D012709:Serum Albumin / Q000494:pharmacology; D013498:Suramin / Q000493:pharmacokinetics*
D000970:Antineoplastic Agents; D012709:Serum Albumin; D013498:Suramin