1. Academic Validation
  2. LYG-202, a newly synthesized flavonoid, exhibits potent anti-angiogenic activity in vitro and in vivo

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

  • J Pharmacol Sci. 2010;112(1):37-45. doi: 10.1254/jphs.09213fp.
Yan Chen 1 Na Lu Yun Ling Ling Wang Qidong You Zhiyu Li Qinglong Guo
Affiliations

Affiliation

  • 1 Jiangsu Key Laboratory of Carcinogenesis and Intervention (China Pharmaceutical University), People's Republic of China.
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 VEGFR2/KDR/Flk-1/VEGFR2/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.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-115436
    98.01%, Anti-Angiogenic/Antitumor Agent