Exp Mol Med.  2006 Oct;38(5):502-508.

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

• Yi EY
• Park SY
• Song HS
• Son MJ
• Yi KY
• Yoo SE
• Kim YJ

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.

Keyword

angiogenesis; angiogenesis inhibitors; fibroblast growth factor 2; neoplasms

MeSH Terms

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