R-(-)-beta-O-methylsynephrine, a natural product, inhibits VEGF-induced angiogenesis in vitro and in vivo.
R-(-)-beta-O-methylsynephrine (OMe-Syn) is an active compound isolated from a plant of the Rutaceae family. We conducted cell proliferation assays on various cell lines and found that OMe-Syn more strongly inhibited the growth of human umbilical vein endothelial cells (HUVECs) than that of other normal and cancer cell lines tested. In angiogenesis assays, it inhibited vascular endothelial growth factor (VEGF)-induced invasion and tube formation of HUVECs with no toxicity. The anti-angiogenic activity of OMe-Syn was also validated in vivo using the chorioallantonic membrane (CAM) assay in growing chick embryos. Expression of the growth factors VEGF, hepatocyte growth factor, and basic fibroblast growth factor was suppressed by OMe-Syn in a dose-dependent manner. Taken together, our results indicate that this compound could be a novel basis for a small molecule targeting angiogenesis.
Kim
Nam Hee
NH
Department of Biotechnology, Translational Research Center for Protein Function Control, Yonsei University, Seoul, Republic of Korea.
Pham
Ngoc Bich
NB
Quinn
Ronald J
RJ
Kwon
Ho Jeong
HJ
D020533:Angiogenesis Inhibitors / Q000494:pharmacology*; D000818:Animals; D001688:Biological Products / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002478:Cells, Cultured; D002642:Chick Embryo; D004730:Endothelium, Vascular / Q000166:cytology / Q000187:drug effects* / Q000378:metabolism; D004809:Ephedrine / Q000031:analogs & derivatives; D016222:Fibroblast Growth Factor 2 / Q000037:antagonists & inhibitors; D017228:Hepatocyte Growth Factor / Q000037:antagonists & inhibitors; D006801:Humans; D018919:Neovascularization, Physiologic / Q000187:drug effects*; D013578:Synephrine / Q000031:analogs & derivatives* / Q000494:pharmacology; D042461:Vascular Endothelial Growth Factor A / Q000037:antagonists & inhibitors / Q000494:pharmacology
D020533:Angiogenesis Inhibitors; D001688:Biological Products; D042461:Vascular Endothelial Growth Factor A; D016222:Fibroblast Growth Factor 2; D017228:Hepatocyte Growth Factor; C026055:oxilofrine; D004809:Ephedrine; D013578:Synephrine