LYG-202, a Newly Synthesized Flavonoid, Exhibits Potent Anti-angiogenic Activity In Vitro and In Vivo

被引：21
作者：
Chen, Yan [1 ]
Lu, Na [1 ]
Ling, Yun [1 ]
Wang, Ling [1 ]
You, Qidong [1 ]
Li, Zhiyu [1 ]
Guo, Qinglong [1 ]
机构：
[1] China Pharmaceut Univ, Jiangsu Key Lab Carcinogenesis & Intervent, Nanjing 210009, Peoples R China
来源：
JOURNAL OF PHARMACOLOGICAL SCIENCES | 2010年 / 112卷 / 01期
基金：
中国国家自然科学基金;
关键词：
flavonoid; angiogenesis; human umbilical vein endothelial cell (HUVEC); vascular endothelial growth factor (VEGF); KDR/Flk-1 (VEGFR-2); ENDOTHELIAL GROWTH-FACTOR; INDUCED TYROSINE PHOSPHORYLATION; SIGNALING PATHWAYS; VEGF; INHIBITION; MECHANISMS; KDR/FLK-1; RECEPTOR;
D O I：
10.1254/jphs.09213FP
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
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.
引用
收藏
页码：37 / 45
页数：9
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