Abstract: Purpose: Grape seed proanthocyanidins extract (GSPE) is considered to be an antitumor bioactivator. This study aims to explore the effectiveness of GSPE in inducing cell apoptosis in human esophageal cancer cell line ECA109 and to elucidate the underlying mechanism. Methods: ECA109 cells were treated with 10 μmol/L BAY11-7082 and GSPE at concentrations of 0, 25, 50, 100, 200, 400 μg/mL for 24 h. 3-(4,5-Dimethyl-2-thiazolyl)-2,5-diphenyl-2-H-tetrazolium bromide assay and flow cytometry were used respectively to measure cell proliferation and apoptosis; inflammatory cytokines and Bax/Bcl-2 were detected by enzyme-linked immunosorbent assay (ELISA) with double antibodies; the mRNA and protein expression of caspase-3 and nuclear factor-kappa B (NF-κB) signaling was detected by real-time polymerase chain reaction (qPCR) and Western blot. Results: GSPE at all concentrations tested could inhibit cell proliferation and induce apoptosis in ECA109 cells, increasing the apoptotic rate from 54.44% to 82.80%. ELISA results showed that GSPE and BAY11-7082 both could significantly inhibit the secretion of prostaglandin E2 (PGE2) and C reactive protein (CRP) (P < 0.05). The results of qPCR and Western blot showed that BAY11-7082 and GSPE could activate caspase-3 and suppress NF-κB signaling. Conclusion: GSPE can induce cell apoptosis and inhibit proliferation in ECA109 cells by inhibiting the production of inflammatory factors through suppressing NF-κB signaling pathway and activating caspase-3.

Key words: grape seed proanthocyanidins extract, human esophageal carcinoma, cell apoptosis, nuclear factor-kappa B signaling pathway