The Eph tyrosine kinase receptors and their ephrin ligands play a central role in several human cancers and their deregulated expression or function promotes tumorigenesis, inducing aggressive tumor phenotypes. Green tea extracts (GTE) have been recently found to inhibit Eph-kinase phosphorylation. In order to evaluate the potential contribution of edible and medicinal plants on EphA2-ephrinA1 modulation, 133 commercially available plant extracts used as food supplements, essential and fixed oils were screened with an ELISA-based binding assay. Nine plant extracts, rich of polyphenols, reversibly inhibited binding in a dose-dependent manner (IC₅₀ 0.83-24 μg/ml). Functional studies on PC3 prostate adenocarcinoma cells revealed that active extracts antagonized ephrinA1-Fc-induced EphA2-phosphorylation at non-cytotoxic concentrations (IC₅₀ 0.31-11.3 μg/ml) without interfering with EGF-induced EGFR activation, suggesting a specific effect. These findings could furnish an interesting starting point regarding the potential relationship between diet, edible plant secondary metabolites and Eph-ephrin system, suggesting their possible involvement in cancer development modulation.
Polyphenol rich botanicals used as food supplements interfere with EphA2-ephrinA1 system / HASSAN MOHAMED, Iftiin; Giorgio, Carmine; Bruni, Renato; Flammini, Lisa; Barocelli, Elisabetta; D., Rossi; Domenichini, Giuseppe; F., Poli; Tognolini, Massimiliano. - In: PHARMACOLOGICAL RESEARCH. - ISSN 1043-6618. - 64(2011), pp. 464-470. [10.1016/j.phrs.2011.06.008]
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