The anticancer effects of Levonorgestrel on human esophageal squamous carcinoma cells

Abstract Drug repositioning is a better way to cancer drug discovery. As a common used oral contraceptive, Levonorgestrel (LNG) was found to play important anticancer roles in several cancers, but its role in human esophageal squamous cell carcinoma (ESCC) was little known. Using ESCC cell line of Ec1 and human normal esophageal epithelial cell line of Het-1A, this study was aim to investigate the effect and molecular mechanism of LNG on the ESCC. The results showed that LNG inhibit the cell proliferation; LNG also induced the cell apoptosis of ESCC related to mitochondrial apoptotic pathway for its disruption of mitochondrial capacity and upregulation of cleaved-Caspase 3 and the declining of the ratio of Bcl-2/Bax; LNG can inhibit the cell migration of ESCC with the E-cadherin overexpression. The anticancer effect of LNG on ESCC mainly associated with Wnt/β-catenin signaling pathway through up-regulation the phosphorylation level of β-catenin. At last, the study declared that LNG combined with cisplatin (CDDP) significantly suppressed the proliferation of Ec1. In conclusions, the LNG serves as efficient anticancer drug in ESCC cells and maybe used for drug repositioning to adjunctive therapy ESCC.