KR-31831, a new synthetic anti-ischemic agent, inhibits in vivo and in vitro angiogenesis.
- Author:
Eui Yeun YI
1
;
Shi Young PARK
;
Hyun Seok SONG
;
Myung Jin SON
;
Kyu Yang YI
;
Sung En YOO
;
Yung Jin KIM
Author Information
1. Department of Molecular Biology, Pusan National University, Busan, Korea. yjinkim@pusan.ac.kr
- Publication Type:Original Article ; In Vitro ; Research Support, Non-U.S. Gov't
- Keywords:
angiogenesis;
angiogenesis inhibitors;
fibroblast growth factor 2;
neoplasms
- MeSH:
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
- From:Experimental & Molecular Medicine
2006;38(5):502-508
- CountryRepublic of Korea
- Language:English
-
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.