Introduction/Background Epithelial ovarian cancer is a prevalent cancer type in women causing significant mortality rates worldwide, and remains incurable especially in advanced stages due to chemoresistance and drug-associated side effects. To address this issue, identifying novel chemotherapeutic agents with fewer side effects and enhanced anti-cancer activity is crucial. In this study, we examined a collection of chalcone analogues, which are precursors of flavonoids, to evaluate their potential as anti-cancer agents against ovarian cancer cells. Our aim is to identify novel agents that could overcome chemoresistance and improve the efficacy of ovarian cancer treatment.
Methodology In order to investigate the potential cytotoxic activity of 17 novel chalcone derivatives, we performed SRB assay on four different cell lines, including both ovarian cancer and non-tumorigenic cells. Through the application of the SRB assay, chalcone derivatives exhibiting promising efficacy against ovarian cancer cells were selected for further analysis. To further characterize the underlying cell death mechanisms, we employed various experimental approaches, including PI staining, Annexin-V staining, and western blot analysis.
Results Our study revealed that out of the 17 chalcone derivatives, 3 chalcones derivatives exhibited potent activity against ovarian cancer cells, with low IC50 values. After further investigation of the mode of action of these compounds, these derivatives were also found to induce apoptotic cell death, cause DNA damage through phosphorylation of H2AX, and affect the cell cycle in ovarian cancer cells causing sub-G1 increase.
Conclusion In conclusion, our findings suggest that the new chalcones have potential as chemotherapeutic agents in the treatment of ovarian cancer. Further research is needed to thoroughly investigate their efficacy and safety profiles, and to identify the specific mechanisms by which they induce apoptotic cell death, and cell cycle effects on ovarian cancer cells. These promising results warrant further investigation and development of these chalcones as potential therapeutic agents for ovarian cancer.
Disclosures Author(s) declare no conflict of interest.
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