Perturbation of the EphA2–EphrinA1 system in human prostate cancer cells by colonic (poly)phenol catabolites

Tognolini, M. et al. (2012) Perturbation of the EphA2–EphrinA1 system in human prostate cancer cells by colonic (poly)phenol catabolites. Journal of Agricultural and Food Chemistry, 60(36), pp. 8877-8884. (doi: 10.1021/jf205305m)

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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 μM). 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.

Item Type:Articles
Glasgow Author(s) Enlighten ID:Borges, Dr Gina and Crozier, Professor Alan
Authors: Tognolini, M., Giorgio, C., Hassan Mohamed, I., Barocelli, E., Calani, L., Reynaud, E., Dangles, O., Borges, G., Crozier, A., Brighenti, F., and Del Rio, D.
College/School:College of Medical Veterinary and Life Sciences > School of Medicine, Dentistry & Nursing
Journal Name:Journal of Agricultural and Food Chemistry
Publisher:American Chemical Society
ISSN (Online):1520-5118
Published Online:12 March 2012

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