The binding and mode of internalization of conventional
sodium heparin and a low molecular weight heparin (LHG) by human umbilical vein endothelial cells (HUVEC) in culture were studied. The binding and/or internalization of [
35S] LHG to HUVEC was lower than those of [
35S] heparin when incubation was carried out at 37°C, whereas at 4°C both
35S labeled ligands bound to HUVEC similarly. When HUVEC were exposed to fluoresceinated heparin, the staining pattern suggested that heparin enters HUVEC by receptor-mediated pathway. But intracellular fluorescent punctate vesicles were relatively few when exposed to fluoresceinated LHG. The
reduction of anti-Xa activity in culture medium when LHG was added was smaller than that of heparin. Thus, the uptake by cellular compartments such as endothelial cells was suggested to contribute to the pharmacokinetics of both LHG and heparin.
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