Background:
Various phenolic phytochemical extracts have been claimed to exhibit different types
of biological activity, including anti-inflammatory, anti-oxidative and anti-carcinogenic activity. Carnosol and
carnosic acid, extracts of rosemary, are among these phenolic compounds.
Materials and Methods:
CHARMm-based molecular docking was performed to estimate the possible molecular
interactions of both carnosic acid and carnosol with the COX-2 active binding site. An MTT assay was used to
evaluate HEp-2 cell viability after incubation for 48 hours with low or high concentrations of carnosol, carnosic
acid or their combination. The levels of COX-2 were measured in cell lysate by the quantitative indirect ELISA
technique.
Results:
Docking revealed favourable negative binding energies as well as binding interactions of both carnosic
acid and carnosol within the binding site of the COX-2 receptor. Carnosic acid showed more favourable binding
potential than carnosol. One-way ANOVA and Bonferroni’s post hoc tests revealed significant differences in
cytotoxicity among cells treated with different concentrations of the rosemary extracts (P< 0.001). ELISA revealed
significant reductions in COX-2 protein levels in HEp-2 cells treated with either carnosic acid (-1.42-
fold) or carnosol (-3.16-fold) compared to control cells.
Conclusion:
Both rosemary extracts, carnosol and carnosic acid, exert potential cytotoxic effects on the HEp-2
cell line via inhibition of the COX-2 pathway. The combination of carnosol and carnosic acid exerts a stronger
cytotoxic effect than either compound alone.
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