Ellagic acid, a phenolic compound, exerts anti-angiogenesis effects via VEGFR-2 signaling pathway in breast cancer

N Wang, ZY Wang, SL Mo, TY Loo, DM Wang… - Breast cancer research …, 2012 - Springer
N Wang, ZY Wang, SL Mo, TY Loo, DM Wang, HB Luo, DP Yang, YL Chen, JG Shen
Breast cancer research and treatment, 2012Springer
Anti-angiogenesis targeting VEGFR-2 has been considered as an important strategy for
cancer therapy. Ellagic acid is a naturally existing polyphenol widely found in fruits and
vegetables. It was reported that ellagic acid interfered with some angiogenesis-dependent
pathologies. Yet the mechanisms involved were not fully understood. Thus, we analyzed its
anti-angiogenesis effects and mechanisms on human breast cancer utilizing in-vitro and in-
vivo methodologies. The in-silico analysis was also carried out to further analyze the …
Abstract
Anti-angiogenesis targeting VEGFR-2 has been considered as an important strategy for cancer therapy. Ellagic acid is a naturally existing polyphenol widely found in fruits and vegetables. It was reported that ellagic acid interfered with some angiogenesis-dependent pathologies. Yet the mechanisms involved were not fully understood. Thus, we analyzed its anti-angiogenesis effects and mechanisms on human breast cancer utilizing in-vitro and in-vivo methodologies. The in-silico analysis was also carried out to further analyze the structure-based interaction between ellagic acid and VEGFR-2. We found that ellagic acid significantly inhibited a series of VEGF-induced angiogenesis processes including proliferation, migration, and tube formation of endothelial cells. Besides, it directly inhibited VEGFR-2 tyrosine kinase activity and its downstream signaling pathways including MAPK and PI3K/Akt in endothelial cells. Ellagic acid also obviously inhibited neo-vessel formation in chick chorioallantoic membrane and sprouts formation of chicken aorta. Breast cancer xenografts study also revealed that ellagic acid significantly inhibited MDA-MB-231 cancer growth and P-VEGFR2 expression. Molecular docking simulation indicated that ellagic acid could form hydrogen bonds and aromatic interactions within the ATP-binding region of the VEGFR-2 kinase unit. Taken together, ellagic acid could exert anti-angiogenesis effects via VEGFR-2 signaling pathway in breast cancer.
Springer
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