Molecular structure-function relationship of dietary polyphenols for inhibiting VEGF-induced VEGFR-2

Ana Cerezo, Mark Winterbone, Christina Moyle, Paul Needs, and Paul Kroon

apples_green_teaThe Polyphenols and Health Group, led by Dr Paul Kroon, from the Institute of Food Research (UK), and Ana Cerezo from Nutrición y Bromatología, Facultad de Farmacia (Universidad de Sevilla, ES) have shown that some polyphenols bind directly with vascular endothelial growth factor (VEGF), which inhibits atherosclerosis and, therefore, progression of cardiovascular disease (CVD).

VEGF-EGCGVEGF was treated with different polyphenols to determine inhibition levels, using human umbilical vein endothelial cells (HUVECs) as model, and establish concentrations that would be relevant to dietary intake. Binding and affinity sites of VEGF were predicted using in-silico modelling.

Intakes of dietary polyphenols are inversely associated with CVD risk, and development of CVD involves the growth of new blood vessels (angiogenesis) arising from, amongst other factors, VEGF activity. Thus, if the VEGF activity can be reduced, some aspects of atherosclerosis will be inhibited, limiting progress of CVD.

To ensure the results were relevant to human health, the polyphenols chosen are commonly consumed in the diet and the results demonstrate that these polyphenols interact with VEGF at physiologically concentrations. Understanding this interaction better is essential for polyphenol-rich foods to obtain a positive opinion from EFSA in any health claims dossier.

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Figure 1: VEGF (green and blue) interaction with a polyphenol (grey)

Figure 2: Apples and green tea


  1. Inhibition was strongly associated with the presence of a galloyl, hydroxyl and catechol groups at specific positions on flavones and flavonols
  2. Potency was strongly correlated to binding affinities for the VEGF receptor VEGFR-2
  3. Inhibition was physiologically relevant at concentrations likely to be achieved through dietary intake