Anti-human immunodeficiency virus type 1 agent alpha-hydroxy glycineamide enters the target cells via a mechanism of passive diffusion.

摘要: Objectives Alpha-hydroxy glycineamide (αHGA) is the active antiviral metabolite of tri-peptide glycyl-prolyl-glycine-amide (GPG-NH2). αHGA inhibits replication HIV-1 in vitro by interfering with capsid formation. It has also an effect on viral gp160 envelope protein. Since drug transport important aspect function, we investigated mechanism [14C] uptake a human T cell line. Methods H9 cells were incubated defined amounts radiolabelled for definite time durations. After harvesting and removal material, radioactivity associated was assayed. Experiments designed to address metabolic inhibitors, temperature extra unlabelled compound as potential competitor cellular αHGA. Key findings Uptake into H9 time- dose-dependent. The properties showed low dependency (Q10 < 2). Moreover not inhibited increasing concentrations cold competitors. There no known NaN3 NaF. Conclusions Kinetic analysis uptake, inhibition studies, saturation studies Q10 value indicate that enters passive diffusion.