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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Authors | Yan Chen, Na Lu, Yun Ling, Ling Wang, Qidong You, Zhiyu Li, Qinglong Guo |
Journal | Journal of pharmacological sciences
(J Pharmacol Sci)
Vol. 112
Issue 1
Pg. 37-45
( 2010)
ISSN: 1347-8648 [Electronic] Japan |
PMID | 20093787
(Publication Type: Comparative Study, Journal Article, Research Support, Non-U.S. Gov't)
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Chemical References |
- Angiogenesis Inhibitors
- Flavones
- Flavonoids
- LYG 202
- Piperazines
- Vascular Endothelial Growth Factor A
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Topics |
- 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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