Perturbation of the EphA2-EphrinA1 System in Human Prostate Cancer Cells by Colonic (Poly)phenol Catabolites - INRAE - Institut national de recherche pour l’agriculture, l’alimentation et l’environnement Access content directly
Journal Articles Journal of Agricultural and Food Chemistry Year : 2012

Perturbation of the EphA2-EphrinA1 System in Human Prostate Cancer Cells by Colonic (Poly)phenol Catabolites

Abstract

The Eph tyrosine kinase receptors and their ephrin ligands play a central role in human cancer as their deregulated expression induces tumorigenesis with aggressive phenotypes. To evaluate their potential contribution to EphA2-ephrinA1 modulation, several colonic catabolites of dietary (poly)phenolics, known to be generated in vivo, were screened using an ELISA-based binding assay. Some of the catabolites inhibited the binding in a dose-dependent manner (IC50 values from 0.26 to 43 mu M). Functional studies on prostate adenocarcinoma cells revealed that pyrogallol and protocatechuic acid specifically antagonized ephrinA1-Fc-induced EphA2 phosphorylation at concentrations that were not cytotoxic. The active concentrations of pyrogallol appear to be close to what can be reached in vivo under physiological conditions. Finally, because of the roles played by the Eph-ephrin system not only in cancer development but also in neurodegeneration and diabetes, pyrogallol and protocatechuic acid are candidates for more detailed functional studies to elucidate their role in these pathophysiological processes.
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hal-02652527 , version 1 (29-05-2020)

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Massimiliano Tognolini, Carmine Giorgio, Iftiin Hassan Mohamed, Elisabetta Barocelli, Luca Calani, et al.. Perturbation of the EphA2-EphrinA1 System in Human Prostate Cancer Cells by Colonic (Poly)phenol Catabolites. Journal of Agricultural and Food Chemistry, 2012, 60 (36), pp.8877 - 8884. ⟨10.1021/jf205305m⟩. ⟨hal-02652527⟩
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