The activity of pyrazoline B compound in inhibiting proliferation of breast cancer cells with human epidermal growth factor receptor 2 overexpression

Introduction: This study aimed to evaluate the cytotoxicity and elucidate the mechanism of action of the chemical compound pyrazoline B in inhibiting the proliferation of MCF 7/HER-2 breast cancer cells. Material and methods: Pyrazoline B was synthesized at the Department of Chemistry, Faculty of Mathematics and Natural Sciences, Universitas Gadjah Mada. Cytotoxic activity against MCF 7/HER-2 cells was assessed using the MTT assay. Flow cytometry was used to analyse cell cycle arrest (G2/M phase), induction of apoptosis and necrosis, and the expression of PI3K, mTOR, and reactive oxygen species (ROS). Results: Pyrazoline B exhibited cytotoxicity with an IC₅₀ value of 16.42 µg/ml. All comparisons between treated and control cells were statistically significant (p < 0.001). Compared with the untreated control cells, G2/M phase accumulation increased by 19.10-20.80 (1.09-fold). Early apoptosis increased by 1.8-2.8 (1.56-fold), late apoptosis by 3.4-14.1 (4.15-fold), and late necrosis by 0.9-2.5 (2.78-fold). PI3K expression decreased by 98.2-85.0 (13.2 reduction), and mTOR expression by 99.6-98.3 (1.3 reduction). Reactive oxygen species levels increased by 34.2-49.2 (1.44-fold). Conclusions: Pyrazoline B inhibited cell cycle progression, induced apoptosis and necrosis, downregulated PI3K/ mTOR signalling, and elevated ROS levels in MCF 7/HER-2 cells compared with the untreated control cells. These findings suggest that pyrazoline B is a promising candidate for development as a novel anticancer agent. © Termedia Sp. z o.o. This is an Open Access article distributed under the terms of the Creative Commons Attribution-NonCommercial-ShareAlike 4.0 International (CC BY-NC-SA 4.0). License (http://creativecommons.org/licenses/by-nc-sa/4.0/)