Objective: To investigate the in vitro and in vivo anticancer effects of a chalcone against KYSE-4 esophageal cancer cells.
Methods: A chalcone was synthesized via the molecular hybridization strategy based on the anticancer activity of chalcone and dithiocarbamate scaffolds. The anticancer effects of different concentrations of the chalcone derivative were compared in esophageal cancer cells.
Results: This chalcone displayed strong inhibitory effects on esophageal cancer cell growth with an IC50 of 1.06 μM in KYSE-4 cells. Analysis of the mechanism revealed that the derivative obviously inhibited KYSE-4 cell growth, migration, and invasion in a concentration-dependent manner. Furthermore, the compound regulated migration-related biomarkers (E-cadherin, N-cadherin, and Slug) and inhibited the Wnt/β-catenin pathway. According to western blotting, this chalcone suppressed the expression of proline-rich protein 11 (PRR11) in a concentration- and time-dependent manner.
Conclusions: This chalcone might be a leading candidate for suppressing the growth and metastasis of esophageal cancer by downregulating PRR11 expression and inhibiting Wnt/β-catenin signaling.
Keywords: Chalcone; PRR11; cell growth; epithelial–mesenchymal transition; esophageal cancer; invasion; metastasis; molecular hybridization.