LYG-202,a newly synthesized flavonoid,exhibits potent anti-angiogenic activity in vitro and in vivo

Lyg-202 (c25h30n2o5) is a newly synthesized flavonoid that has been confirmed to possess an antitumor effect,but the mechanism is unclear. our present study was performed to identify the anti-angiogenic activity of this novel compound in vitro and in vivo. lyg-202 inhibited vascular endothelial growth factor (vegf) stimulated migration and tube formation of human umbilical vein endothelial cells and arrested microvessel outgrowth from rat aortic rings in vitro. meanwhile,lyg-202 suppressed the neovascularization of chicken chorioallantoic membrane in vivo. mechanistic studies revealed that lyg-202 suppressed the vegf-induced tyrosine phosphorylation of kdr/flk-1 (vegfr-2) as well as its downstream protein kinases activation,by decreasing phosphorylated forms of serine/threonine kinase akt,extracellular signal-regulated kinase,and p38 mitogen-activated protein kinase. lyg-202 exerts anti-angiogenic activity both in vitro and in vivo,and these results suggest that it deserves further investigation as a promising anti-tumor angiogenesis compound. ©2010 the japanese pharmacological society.