CYTOTOXICITY OF ARENOBUFAGIN AND ITS DERIVATIVES AGAINST MCF-7 CELLS

«Farmatsiya» · № 5/2026 · с. 57–63

Mukhamedov Nurkhodja Ramazanovich, E. Sipos, Khakimov Makhmudjon Sobir ugli, Kayumov Muzaffar Bakhadirovich, Yashinov Ansor Sharofiddin ugli, Tashmukhamedov Mugrajitdin Salakhovich, Mirzaakhmedov Sharafitdin Yashinovich

Institute of Bioorganic Chemistry, Academy of Sciences of the Republic of Uzbekistan, Tashkent, Uzbekistan
Department of Pharmacology, Faculty of Pharmacy, University of Debrecen, Debrecen, Hungary
Department of Biotechnology, Tashkent Institute of Chemical Technology, Tashkent, Uzbekistan

Abstract

Arenobufagin is a bufadienolide with potent antitumor activity against a variety of human cancer cell lines. In the present study, the cytotoxic activity of arenobufagin and seven newly synthesized derivatives was evaluated against MCF-7 human breast cancer cells using the MTT assay. Cells were exposed to the tested compounds at concentrations of 10, 50, and 300 nM for 24 h. Arenobufagin and the derivatives Ar-004, Ar-007, Ar-008, and Ar-015 exhibited pronounced concentration-dependent cytotoxicity, whereas Ar-014 showed only moderate activity. In contrast, Ar-005 and Ar-011 demonstrated little or no cytotoxic effect under the experimental conditions. The obtained results indicate that structural modification of arenobufagin markedly influences its cytotoxic activity against MCF-7 cells. These findings provide useful preliminary information for the biological evaluation of newly synthesized arenobufagin derivatives and may contribute to the identification of promising lead compounds for further anticancer studies.

Keywords: arenobufagin; bufadienolides; MCF-7 cells; breast cancer; cytotoxicity; MTT assay.

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