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.
AuthorsYan Chen, Na Lu, Yun Ling, Ling Wang, Qidong You, Zhiyu Li, Qinglong Guo
JournalJournal of pharmacological sciences (J Pharmacol Sci) Vol. 112 Issue 1 Pg. 37-45 ( 2010) ISSN: 1347-8648 [Electronic] Japan
PMID20093787 (Publication Type: Comparative Study, Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Angiogenesis Inhibitors
  • Flavones
  • Flavonoids
  • LYG 202
  • Piperazines
  • Vascular Endothelial Growth Factor A
  • Angiogenesis Inhibitors (chemical synthesis, pharmacology)
  • Animals
  • Cell Movement (drug effects, physiology)
  • Cells, Cultured
  • Chickens
  • Endothelial Cells (cytology, drug effects, physiology)
  • Flavones (chemical synthesis, pharmacology)
  • Flavonoids (chemical synthesis, pharmacology)
  • Humans
  • Microtubules (drug effects, physiology)
  • Piperazines (chemical synthesis, pharmacology)
  • Rats
  • Rats, Sprague-Dawley
  • Vascular Endothelial Growth Factor A (antagonists & inhibitors, physiology)

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