KR-31831, a new synthetic anti-ischemic agent, inhibits in vivo and in vitro angiogenesis.

Abstract

Angiogenesis is considered to be an integral process to the growth and spread of solid tumors. Anti-angiogenesis therapy recently has been found to be one of the most promising anti-cancer therapeutic strategies. In this study, we provide several lines of evidences showing that KR-31831, a new benzopyran derivative, has anti-angiogenic activities. KR-31831 inhibited the proliferation, migration, invasion and tube formation of bovine aortic endothelial cells (BAECs), and suppressed the release of matrix metalloproteinase-2 (MMP-2) of BAECs. KR-31831 also inhibited in vivo angiogenesis in mouse Matrigel plug assay. Furthermore, the mRNA expressions of basic fibroblast growth factor (bFGF), fibroblast growth factor receptor-2 (FGFR-2), and vascular endothelial growth factor receptor-2 (VEGFR-2) were decreased by KR-31831. Taken together, these results suggest that KR-31831 acts as a novel angiogenesis inhibitor and might be useful for treating hypervascularized cancers.

• Authors: Eui-Yeun Yi, Shi-Young Park, Hyun Seok Song, Myung Jin Son, Kyu-Yang Yi, Sung-En Yoo, Yung-Jin Kim
• Journal: Experimental & molecular medicine (Exp Mol Med) Vol. 38 Issue 5 Pg. 502-8 (Oct 31 2006) ISSN: 1226-3613 [Print] United States
• PMID: 17079866 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Angiogenesis Inhibitors
• Benzopyrans
• Imidazoles
• KR 31831
• Fibroblast Growth Factor 2
• Receptor, Fibroblast Growth Factor, Type 2
• Vascular Endothelial Growth Factor Receptor-2
• Matrix Metalloproteinase 2

Topics

• Angiogenesis Inhibitors (pharmacology, therapeutic use)
• Animals
• Benzopyrans (pharmacology, therapeutic use)
• Cattle
• Cell Movement (drug effects)
• Cells, Cultured
• Endothelial Cells (drug effects)
• Fibroblast Growth Factor 2 (metabolism)
• Imidazoles (pharmacology, therapeutic use)
• In Vitro Techniques
• Ischemia (drug therapy)
• Male
• Matrix Metalloproteinase 2 (metabolism)
• Mice
• Mice, Inbred C57BL
• Models, Biological
• Neovascularization, Pathologic (drug therapy)
• Neovascularization, Physiologic (drug effects)
• Receptor, Fibroblast Growth Factor, Type 2 (metabolism)
• Vascular Endothelial Growth Factor Receptor-2 (metabolism)