Cilengitide, a small molecule antagonist, targeted to integrin αν inhibits proliferation and induces apoptosis of laryngeal cancer cells in vitro

Cilengitide is a chemical synthesis cyclopeptide containing RGD sequence, which can be used as a small molecule antagonist targeted to integrin alpha nu (ITGAV). The aim of present study was to investigate the effect on proliferation and cell apoptosis of the cilengitide in laryngeal cancer cells. In the study, we have treatmented the cultured cells of laryngeal cancer (Hep-2) with cilengitide. After the medication, the proliferation of the Hep-2 cells was detected by MTT assay, the expression of ITGAV was detected by RT-PCR and the activity of caspase-3 protein was detected by a specialized kit. RGD linear peptides (GRGDSP), non-RGD linear peptide (GRGESP), and 5-fluorouracil (5-Fu) were used as controls. Results showed that the proliferation of Hep-2 cells was signally inhibited by the cilengitide with a time and dose compliance. Its inhibition effect was significantly higher than that of 5-Fu and GRGDSP, but the GRGESP showed no obvious inhibitory effect. After intervene of cilengitide, the activity of caspase-3 protein of Hep-2 cells was significantly increased, and the expression of ITGAV was significantly decreased. 5-Fu significantly inhibited the proliferation of Hep-2 cells, but no significant changes of ITGAV expression were observed. In conclusion, cilengitide can significantly down-regulate ITGAV expression and inhibit cell proliferation in laryngeal cancer cells, it will also to induce cell apoptosis through caspase-3 pathway. Therefore, it could be as a kind of effective chemotherapy drugs that will be used in clinical treatment of the laryngeal cancer.