Apigenin suppresses the expression of VEGF, an important factor for angiogenesis, in endothelial cells via degradation of HIF-1α protein

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Abstract

Apigenin, a plant-derived flavone, is a potent inhibitor of cell proliferation and angiogenesis, but the mechanisms leading to the pathological anti-angiogenic effects of apigenin are still unclear. In this study, we found that apigenin inhibited the hypoxia-induced expression of vascular endothelial growth factor (VEGF) mRNA in human umbilical artery endothelial cells. Apigenin also suppressed the expression of erythropoietin mRNA, which is a typical hypoxia-inducible gene, via the degradation of hypoxia-inducible factor 1 (HIF-1) α. We investigated the effect of apigenin on the interaction of HIF-1α with heat shock protein 90 (Hsp90), which is reported to be important for the stabilization of HIF-1α, and found that VEGF expression was inhibited via degradation of HIF-1α through interference with the function of Hsp90. © 2004 Published by Elsevier B.V. on behalf of the Federation of European Biochemical Societies.

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Osada, M., Imaoka, S., & Funae, Y. (2004). Apigenin suppresses the expression of VEGF, an important factor for angiogenesis, in endothelial cells via degradation of HIF-1α protein. FEBS Letters, 575(1–3), 59–63. https://doi.org/10.1016/j.febslet.2004.08.036

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