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Topics {✒️}

jian-gang shen & jian-ping chen vascular endothelial-growth-factor receptor-2 full size image jian-ping chen mda-mb-231 cell line mda-mb-231 xenograft model possess anti-cancer properties article download pdf strong π–π interactions avidin–biotin–hrp complex existing endothelium-lined vessels including p-erk/erk inhibited neo-vessel formation exerts anti-angiogenesis effects hai-bin luo mba-md-231 tumor growth suppress tumor-induced angiogenesis 3 mg/ml cortisone acetate de-po yang mba-md-231 tumor volumes mda-mb-231 xenografts sun yat-sen university values represent means ± sd dose dependently suppressed exert anti-angiogenesis effects pbs-soaked cotton swab vitro anti-proliferative activities poly-glu-tyr substrate dcfh-da staining assay serum-free medium supplemented full access fresh serum-free medium dose dependently suppress vivo anti-angiogenesis effects receptor tyrosine kinases multiple molecular targets atp-binding region lies 20 ng/ml human vegf yu-ling chen ellagic acid-treated group dietary-derived phenolic compound support tumor growth deparaffinized tumor sections vegfr-2/ellagic acid complex ellagic acid/vegfr-2 complex vegf-stimulated p-vegfr2 decreased mmps activity percent kinase activity ligand-binding site based multiple signal pathways

Questions {❓}

• Miller KD (2004) Recent translational research: antiangiogenic therapy for breast cancer—where do we stand?

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         description: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.
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      headline:Ellagic acid, a phenolic compound, exerts anti-angiogenesis effects via VEGFR-2 signaling pathway in breast cancer
      description: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.
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         Anti-angiogenesis
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         Molecular docking
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         Oncology
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