Open Access
Apigenin induces apoptosis and impairs head and neck carcinomas EGFR/ErbB2 signaling
Laura Masuelli1,Laura Marzocchella1,Alessandro Quaranta1,Camilla Palumbo1,Giorgio Pompa1,Valerio Izzi1,Antonella Canini1,Andrea Modesti1,Fabio Galvano1,Roberto Bei1
Department of Experimental Medicine, University of Rome, Sapienza, Rome, Italy
DOI: 10.2741/3735 Volume 16 Issue 3, pp.1060-1068
Published: 01 January 2011
(This article belongs to the Special Issue Dietary approaches to prevent chronic-degenerative diseases)

The development of head and neck squamous cell carcinomas (HNSCCs) is a multistep process progressing from precancerous lesions to highly malignant tumors. A critical role in HNSCCs development and progression is played by EGFR family members including EGFR and ErbB2. The aim of this study was to investigate the effect of apigenin, a low molecular weight flavonoid contained in fruits and vegetables, on growth and survival and on EGFR/ErbB2 signaling in cell lines derived from HNSCCs of the tongue (CAL-27, SCC-15) or pharynx (FaDu). Using sulforhodamine B assay, FACS analysis and activated caspase-3 detection by immunofluorescence, we here demonstrate that apigenin dose-dependently inhibits survival and induces apoptosis of HNSCC cells. Further, by performing western blotting with antibodies specific for phosphorylated EGFR, ErbB2, Erk1/2 and Akt we demonstrate that apigenin reduces ligand-induced phosphorylation of EGFR and ErbB2 and impairs their downstream signaling. On the whole, our results suggest that apigenin properties might be exploited for chemoprevention and/or therapy of head and neck carcinomas.

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Laura Masuelli, Laura Marzocchella, Alessandro Quaranta, Camilla Palumbo, Giorgio Pompa, Valerio Izzi, Antonella Canini, Andrea Modesti, Fabio Galvano, Roberto Bei. Apigenin induces apoptosis and impairs head and neck carcinomas EGFR/ErbB2 signaling. Frontiers in Bioscience-Landmark. 2011. 16(3); 1060-1068.