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Volume 14
Issue 16
10.3390/cells14161299
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This is an early access version, the complete PDF, HTML, and XML versions will be available soon.
Article

Selective Anticancer Activity and Safety Profile of Chlorochalcones: Impact on Breast Cancer, Blood, and Endothelial Cells

by
Sylwia Cyboran-Mikołajczyk
1,*,
Karolina Matczak
2,
Teresa Kaźmierczak
1,
Natalia Trochanowska-Pauk
1,
Tomasz Walski
3,
Raghvendra Bohara
4,
Karol Bukowski
2,
Agnieszka Krawczyk-Łebek
5 and
Edyta Kostrzewa-Susłow
5
1
Department of Physics and Biophysics, Faculty of Biotechnology and Food Sciences, Wrocław University of Environmental and Life Sciences, Norwida 25 St., 50-375 Wrocław, Poland
2
Department of Medical Biophysics, Faculty of Biology and Environmental Protection, University of Lodz, Pomorska 141/143 St., 90-236 Lodz, Poland
3
Department of Biomedical Engineering, Faculty of Fundamental Problems of Technology, Wrocław University of Science and Technology, Wybrzeże Wyspiańskiego 27, 50-370 Wrocław, Poland
4
Centre for Interdisciplinary Research, D.Y. Patil Educational Society, Kolhapur 416006, India
5
Department of Food Chemistry and Biocatalysis, Wrocław University of Environmental and Life Sciences, Norwida 25 St., 50-375 Wrocław, Poland
*
Author to whom correspondence should be addressed.
Cells 2025, 14(16), 1299; https://doi.org/10.3390/cells14161299
Submission received: 16 July 2025 / Revised: 19 August 2025 / Accepted: 19 August 2025 / Published: 21 August 2025
(This article belongs to the Section Cellular Biophysics)
Versions Notes

Abstract

In the pursuit of novel anticancer therapies, assessing their selectivity and safety profile towards healthy cells is crucial. This study investigated chlorochalcones, derivatives of 2′-hydroxychalcone containing a chlorine atom, for their impact on human breast cancer cells (MCF-7 and MDA-MB-231), healthy blood cells (erythrocytes, peripheral blood mononuclear cells (PBMCs), platelets), and microvascular endothelial cells (HMEC-1). Our findings demonstrated that chlorochalcones did not detrimentally affect erythrocytes, showing no hemolysis or preserving osmotic resistance and transmembrane potential. They also exhibited minimal impact on normal PBMC viability and varying effects on platelet metabolic activity at therapeutic concentrations. Importantly, these derivatives displayed lower toxicity towards HMEC-1 endothelial cells than towards breast cancer cells, indicating a degree of selectivity. Chlorochalcones have high antiproliferative activity against cancer cells, primarily by inducing apoptosis with virtually no significant impact on cell cycle progression. Their mechanism of action involves the modulation of reactive oxygen species (ROS) levels and induction of mitochondrial dysfunction, including membrane depolarization and reduced mitochondrial mass. Biological activity, including toxicity and ROS modulation, is dependent on the position and number of chlorine atoms. In conclusion, this study highlights the ability of chlorochalcones to effectively target malignant cells while sparing normal circulatory and endothelial cells, thus positioning them as a promising class of candidates for further anticancer drug development.
Keywords: RBCs; leukocytes; PLTs; membrane potentials; HMEC-1; H2DCFDA; molecular mechanism; biological activity; aggregometry; toxicity; structure activity relationship RBCs; leukocytes; PLTs; membrane potentials; HMEC-1; H2DCFDA; molecular mechanism; biological activity; aggregometry; toxicity; structure activity relationship

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MDPI and ACS Style

Cyboran-Mikołajczyk, S.; Matczak, K.; Kaźmierczak, T.; Trochanowska-Pauk, N.; Walski, T.; Bohara, R.; Bukowski, K.; Krawczyk-Łebek, A.; Kostrzewa-Susłow, E. Selective Anticancer Activity and Safety Profile of Chlorochalcones: Impact on Breast Cancer, Blood, and Endothelial Cells. Cells 2025, 14, 1299. https://doi.org/10.3390/cells14161299

AMA Style

Cyboran-Mikołajczyk S, Matczak K, Kaźmierczak T, Trochanowska-Pauk N, Walski T, Bohara R, Bukowski K, Krawczyk-Łebek A, Kostrzewa-Susłow E. Selective Anticancer Activity and Safety Profile of Chlorochalcones: Impact on Breast Cancer, Blood, and Endothelial Cells. Cells. 2025; 14(16):1299. https://doi.org/10.3390/cells14161299

Chicago/Turabian Style

Cyboran-Mikołajczyk, Sylwia, Karolina Matczak, Teresa Kaźmierczak, Natalia Trochanowska-Pauk, Tomasz Walski, Raghvendra Bohara, Karol Bukowski, Agnieszka Krawczyk-Łebek, and Edyta Kostrzewa-Susłow. 2025. "Selective Anticancer Activity and Safety Profile of Chlorochalcones: Impact on Breast Cancer, Blood, and Endothelial Cells" Cells 14, no. 16: 1299. https://doi.org/10.3390/cells14161299

APA Style

Cyboran-Mikołajczyk, S., Matczak, K., Kaźmierczak, T., Trochanowska-Pauk, N., Walski, T., Bohara, R., Bukowski, K., Krawczyk-Łebek, A., & Kostrzewa-Susłow, E. (2025). Selective Anticancer Activity and Safety Profile of Chlorochalcones: Impact on Breast Cancer, Blood, and Endothelial Cells. Cells, 14(16), 1299. https://doi.org/10.3390/cells14161299

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