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Published on: March 20, 2020
Novel Selenoesters as a Potential Tool in Triple-Negative Breast Cancer Treatment
Dominika Radomska1, Robert Czarnomysy1, Anna Szymanowska2
1Department of Synthesis and Technology of Drugs, Medical University of Bialystok, Kilinskiego 1, 15-089 Bialystok, Poland.
Abstract:
Disturbing cancer statistics, especially for breast cancer, are becoming a rationale for the development of new anticancer therapies. For the past several years, studies have been proving a greater role of selenium in the chemoprevention of many cancers than previously considered; hence, a trend to develop compounds containing this element as potential agents with anticancer activity has been set for some time. Therefore, our study aimed to evaluate the anticancer activity of novel selenoesters (EDA-71, E-NS-4) in MCF-7 and MDA-MB-231 human breast cancer cells. The assays evaluating proliferation and cell viability, and flow cytometer analysis of apoptosis/autophagy induction, changes in mitochondrial membrane potential, disruption of cell cycle phases, and protein activity of mTOR, NF-κB, cyclin E1/A2, and caspases 3/7, 8, 9, 10 were performed. The obtained results indicate that the tested selenoesters are highly cytotoxic and exhibit antiproliferative activity at low micromolar doses (<5 µM) compared with cisplatin. The most active compound—EDA-71—highly induces apoptosis, which proceeds via both pathways, as evidenced by the activation of all tested caspases. Furthermore, we observed the occurrence of autophagy (↓ mTOR levels) and cell cycle arrest in the S or G2/M phase (↓ cyclin E1, ↑ cyclin A2).
Insights
Novel selenoesters, EDA-71 and E-NS-4, show significant anticancer activity against human breast cancer cells. EDA-71 effectively induces apoptosis and autophagy, offering a promising new avenue for breast cancer therapy.
Area of Science:
- Oncology
- Medicinal Chemistry
- Molecular Biology
Background:
- Rising breast cancer incidence necessitates novel therapeutic strategies.
- Selenium compounds are increasingly recognized for their chemopreventive and anticancer potential.
- Developing new selenium-based agents is a key research trend.
Purpose of the Study:
- To evaluate the anticancer efficacy of novel selenoesters, EDA-71 and E-NS-4.
- To assess their activity in human breast cancer cell lines (MCF-7 and MDA-MB-231).
- To investigate the molecular mechanisms underlying their cytotoxic effects.
Main Methods:
- Cell proliferation and viability assays.
- Flow cytometry analysis for apoptosis, autophagy, and mitochondrial membrane potential.
- Cell cycle phase distribution analysis.
- Western blot analysis of key proteins (mTOR, NF-κB, cyclins, caspases).
Main Results:
- Both selenoesters demonstrated high cytotoxicity and antiproliferative effects at low micromolar concentrations (<5 µM), outperforming cisplatin.
- EDA-71 significantly induced apoptosis through both intrinsic and extrinsic pathways, activating all tested caspases.
- Autophagy was observed (indicated by decreased mTOR levels), alongside cell cycle arrest in the S or G2/M phase (decreased cyclin E1, increased cyclin A2).
Conclusions:
- Novel selenoesters, particularly EDA-71, possess potent anticancer properties against human breast cancer cells.
- These compounds induce apoptosis and autophagy, offering a promising therapeutic approach.
- Further investigation into selenoesters as breast cancer therapeutics is warranted.
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