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Chalcone-3 Inhibits the Proliferation of Human Breast Cancer MDA-MB-231 Cell Line
Novrita Padauleng1,2, Mustofa Mustofa3, Tutik Dwi Wahyuningsih4
1Doctoral Program, Faculty of Medicine, Public Health and Nursing (FKKMK), Universitas Gadjah Mada, Yogyakarta, Indonesia.
Objective:
Chalcone-3 has been shown to be cytotoxic and selective against luminal subtype breast cancer cell lines, which are suspected to occur through the mechanism of epidermal growth factor receptors (EGFR) inhibition. However, the cytotoxic effect has never been tested on cell strains from patients with triple negative breast cancer (TNBC), where EGFR expression is known to increase. This study aimed to identify the role of chalcone-3 in one of the downstream targets of EGFR as an antiproliferative agent.
Methods:
Chalcone-3 was examined for its effect on proliferation in human breast cancer MDA-MB-231 cell lines. The percentage of proliferation inhibition was analyzed using methyl-thiazol tetrazolium assay. Flow cytometry was used to analyze the population of cell cycle distribution and the expression of cyclin-D1 and pEGFR.
Results:
Chalcone-3 inhibited the proliferation of MDA-MB-231 cells in a dose and time-dependent manner with an IC50 value of 17.98±6.36 µg/mL by inducing cell cycle arrest at the G2/M phase. Flow cytometry assays showed that chalcone-3 significantly reduced the expression of pEGFR and cyclin-D1, contributing to cell cycle arrest.
Conclusion:
Chalcone-3 might have potential as an anti-proliferative drug to treat TNBC.
Insights
Chalcone-3 effectively inhibits triple-negative breast cancer (TNBC) cell proliferation by reducing pEGFR and cyclin-D1 expression, suggesting its potential as an anti-cancer drug.
Area of Science:
- Oncology
- Molecular Biology
- Pharmacology
Background:
- Chalcone-3 exhibits cytotoxicity against luminal breast cancer subtypes via epidermal growth factor receptor (EGFR) inhibition.
- Triple-negative breast cancer (TNBC) shows increased EGFR expression, necessitating investigation of chalcone-3's efficacy in this subtype.
Purpose of the Study:
- To evaluate chalcone-3's antiproliferative role in TNBC.
- To investigate chalcone-3's effect on downstream EGFR targets in breast cancer cells.
Main Methods:
- Methyl-thiazol tetrazolium assay to determine proliferation inhibition percentage.
- Flow cytometry to analyze cell cycle distribution and expression of cyclin-D1 and phosphorylated EGFR (pEGFR).
Main Results:
- Chalcone-3 demonstrated dose- and time-dependent inhibition of MDA-MB-231 cell proliferation (IC50: 17.98±6.36 µg/mL).
- Chalcone-3 induced G2/M phase cell cycle arrest.
- Significant reduction in pEGFR and cyclin-D1 expression was observed, correlating with cell cycle arrest.
Conclusions:
- Chalcone-3 exhibits potential as an antiproliferative agent for TNBC treatment.
- Targeting EGFR downstream pathways with chalcone-3 warrants further investigation for TNBC therapy.
