Bestatin is a potent inhibitor of aminopeptidases. The Ki values for bestatin against leucyl aminopeptidase, tripeptide aminopeptidase, cytosol alanyl aminopeptidase, leukotriene A4 hydrolase, aminopeptidase B and nardilysin were 1nM, 0.5μM, 14nM, 0.17μM, 1μM and 15μM, respectively[3]. Pre-incubation of human leukocyte LTA4 hydrolase with 1, 10, or 100μM bestatin resulted in 20%, 50%, and 90% inhibition of [3H]LTA4 labeling of LTA4 hydrolase, respectively. Bestatin inhibited LTB4 formation by LTA4 hydrolase in a dose-dependent manner with 50% inhibition of activity at 10μM[4]. In human umbilical vein endothelial cells (HUVECs), bestatin at 1-100mg/ml inhibited the Ala-MCA-hydrolysing activity of cells in a dose-dependent manner. Bestatin at the same concentration range also resulted in the formation of shorter branching structures in HUVECs compared to the controls. In C57BL/6 mice implanted with B16-BL6 melanoma cells into the dorsal side, intraperitoneal administration of bestatin (50 or 100 mg/kg/day) for 5 days significantly reduced the number of vessels oriented towards the tumor mass without affecting the tumor volume[1].
作用机制
Bestatin is a potent aminopeptidase inhibitor. It competes with the substrates via binding to the catalytic site of the enzyme[3].
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