IC50: 7.7, 13.7 and 10.4 μM for HepG2, SMMC-7721 and BEL-7402 cell line, respectively (after 24h treatment)

Salinomycin (Sal), which is a polyether ionophore antibiotic from Streptomyces albus, has been proven to be able to kill different types of human cancer cells, most likely via interfering with ABC drug transporters, the Wnt/β-catenin signaling pathway, or other pathways.

In vitro: Several hepatocellular carcinoma (HCC) cell lines were treated with Sal. Results showed that Sal inhibited proliferation and decreased PCNA levels. Cell cycle analysis showed that Sal caused cell cycle arrest in different phases. Sal induced apoptosis as characterized by an increase in the Bax/Bcl-2 ratio. Compared to control, β-catenin expression was down-regulated by Sal treatment significantly. The Ca2+ concentration in HCC cells was examined by flow cytometry and it was found that higher Ca2+ concentrations were observed in Sal treatment groups [1].

In vivo: The in vivo anti-tumor effect of Sal was verified using the hepatoma orthotopic tumor model and results showed that the liver tumor size in Sal-treated groups decreased. Immunohistochemistry and TUNEL staining also demonstrated that Sal could in vivo inhibit proliferation and induced apoptosis [1].

Clinical trial: N/A