Bufalin inhibits endothelial cell proliferation and angiogenesis in vitro.

We have investigated the effects of bufalin, one of the prominent components in Chinese toad venom, on proliferation of bovine aortic endothelial (BAE) cells and tube formation in three-dimensional type I collagen matrix. In the present study, bufalin potently inhibited the formation of capillary-like tubular networks in a dose-dependent manner. Bufalin also inhibited the proliferation of BAE cells at the same concentration (5 nM) that the tube formation was inhibited. As a potent inhibitor of endothelial cell proliferation, bufalin specifically prevented the entry of BAE cells into the G0/G1 phase of a cell cycle. These findings suggest that in vitro angioinhibitory action of bufalin may be induced by the proliferation inhibition of endothelial cells through the arrest at the G2/M phase of a cell cycle.