Cytotoxic Effect of Tideglusib on Human Fibroblasts: An In Vitro Study

Abstract

Aim: This study evaluated the cytotoxic effect of different concentrations of Tideglusib as a GSK-3 inhibitor drug on human fibroblasts.Materials and methods: Fibroblasts were cultivated and incubated under 5% CO2 and 95% humidity at 37oC for one day to achieve maturity and confluent growth. In the experimental group, cultures were subjected to different concentrations (500 nM/mL, 250 nM/mL, 125 nM/mL, 62.50 nM/mL, and 31.25 nM/mL and 15.60 nM/mL) of Tideglusib drug dissolved in Dimethyl sulfoxide (DMSO). In the positive control group, cell cultures were supplemented with equivalent volumes of DMSO solution. For negative control group, medium only was used without addition of Tideglusib or DMSO. For evaluation of cytotoxicity, Methyl Thiazol Tetrazolium (MTT) assay was used. Viability percentage was determined for each group and cytotoxicity responses were scored as: severe cytotoxic ≤30%, moderate cytotoxic 30%-60%, mild cytotoxic 60%-90%, and non-cytotoxic ≥90%. Data were statistically analyzed by One-way ANOVA followed by Tukey’s post hoc test.Results: Treatment with Tideglusib drug at the concentrations of 500, 250, 125, 62.50 nM/mL showed severe cytotoxic effects on fibroblasts and significantly decreased the percentage of cell viability when compared to the positive control (P<0.001). Treatment with 31.25 nM/mL and 15.60 nM/mL Tideglusib showed moderate and mild cytotoxic effects, respectively, and significantly decreased the percentage of cell viability when compared to the positive control (P<0.001). Conclusion: Tideglusib showed a dose-dependent cytotoxic impact on fibroblast viability. Lower doses of Tideglusib, beginning at 31.25 nM/mL, resulted in cell viability rate of more than 50%.