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Title: R-(-)-{beta}-O-methylsynephrine, a natural product, inhibits VEGF-induced angiogenesis in vitro and in vivo

Journal Article · · Biochemical and Biophysical Research Communications
 [1]; ;  [2]
  1. Chemical Genomics Laboratory, Department of Biotechnology, Translational Research Center for Protein Function Control, College of Life Science and Biotechnology, Yonsei University, Seoul 120-749 (Korea, Republic of)
  2. Eskitis Institute, Griffith University, Brisbane, QLD 4111 (Australia)

Research highlights: {yields} R-(-)-{beta}-O-methylsynephrine (OMe-Syn) is a natural compound isolated from a plant of the Rutaceae family. {yields} OMe-Syn possesses lead-like physicochemical properties, conferring good solubility. {yields} OMe-Syn effectively inhibited VEGF-induced angiogenesis in vitro and in vivo. {yields} OMe-Syn could be a novel basis for a small molecule targeting angiogenesis. -- Abstract: 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.

OSTI ID:
22202730
Journal Information:
Biochemical and Biophysical Research Communications, Vol. 399, Issue 1; Other Information: Copyright (c) 2010 Elsevier Science B.V., Amsterdam, The Netherlands, All rights reserved.; Country of input: International Atomic Energy Agency (IAEA); ISSN 0006-291X
Country of Publication:
United States
Language:
English