Chemical Modification of Recombinant Human Granulocyte Colony-Stimulating Factor by Polyethylene Glycol Increases its Biological Activity in vivo

抄録

Recombinant human granulocyte colony-stimulating factor (rHuG-CSF) produced in Escherichia coil was chemically modified by polyethylene glycol (PEG) of molecular weights 4, 500 or 10, 000. The neutrophils observed at 32 hours after intravenous injection of the rHuG-CSF modified with PEG (4, 500) or PEG (10, 000) to mice were, respectively, 2.5 times and 5 times more than that observed after the injection of the un-modified rHuG-CSF. These results show that the covalent attachment of PEG to rHuG-CSF enhanced its pharmacological activity in vivo and that the modification with the larger PEG molecule is more effective to enhance the in vivo activity of rHuG-CSF.