LYG-202, a Newly Synthesized Flavonoid,Exhibits Potent Anti-angiogenic Activity In Vitro and In Vivo |
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Authors: | Yan Chen Na Lu Yun Ling Ling Wang Qidong You Zhiyu Li Qinglong Guo |
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Institution: | 1. Jiangsu Key Laboratory of Carcinogenesis and Intervention (China Pharmaceutical University), Nanjing 210009, People’s Republic of China |
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Abstract: | 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. |
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Keywords: | flavonoid angiogenesis human umbilical vein endothelial cell (HUVEC) vascular endothelial growth factor (VEGF) KDR/Flk-1 (VEGFR-2) |
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