Anti-angiogenic activity of auraptene

The objective of this research was to test the in vitro anti-angiogenic activity of auraptene, a coumarin from citrus peel oil. We tested the ability of auraptene to inhibit in vitro angiogenesis using vascular endothelial growth factor (VEGF)-induced human umbilical endothelial cells (HUVEC) growth stimulation. Auraptene was applied at concentrations between 0 μM and 1μM to HUVEC in the presence of 10 ng/mL of VEGF at 37 oC in a 5% CO2 humidified incubator for 6h. The viability, migration, and invasion of HUVEC in the presence of auraptene were evaluated by the CellTiter 96® AQueous One Solution Cell Proliferation assay and Boyden Chamber, respectively. Our results indicated that auraptene at 50 to 500 nM dosedependently inhibited VEGF-induced in vitro angiogenesis. In vitro tube formation was also reduced to less than 20% of that of the control in the presence of 500 nM of auraptene. The viability of HUVEC exposed to 500 nM auraptene for 72 h was reduced to about 15 % of that of untreated cells. Auraptene at 500 nM thus inhibited VEGF-induced HUVEC migration and invasion. This is the first report that supports the use of auraptene as an inhibitor of angiogenesis. Our results may help to explain the inhibitory activity of this bioactive compound against cancer cell growth and proliferation.