Ormeloxifene inhibits the proliferation of cervical cancer cells by suppressing Wnt/β-catenin signaling

Background: Ormeloxifene, a non-steroidal selective estrogen receptor modulator used widely as an oral contraceptive, which was recently reported to play anti-cancer activity in various types of cancer. This study aimed to investigate the effect of Ormeloxifene on human cervical cancer HeLa cells and related mechanism. Material and methods: After treated with different doses of Ormeloxifene, cell viability was determined by MTT method, the cell cycle distribution and apoptosis were observed by flow cytometry (FCM), the expression of Wingless-type (Wnt), beta-catenin, glycogen synthase kinase (GSK)-3 beta and CyclinD1 was measured by Quantitative real-time PCR (QPCR) and Western blot analysis. Results: Ormeloxifene treatment significantly inhibited the proliferation, induced G1 arrest and apoptosis in human cervical cancer HeLa cells. More importantly, QPCR and Western blot showed that Ormeloxifene markedly down-regulated the expression levels of Wnt, beta-catenin, and cyclinD1, up-regulated the expression of GSK-3 beta in HeLa cells. Conclusion: Together, the results of this study reveal that Ormeloxifene significantly inhibits the proliferation of HeLa cell and is a potential drug for the treatment of cervical cancer.