Biopolym. Cell. 2026; 42(3):210-220.
https://doi.org/10.7124/bc.000BBB
Molecular Biomedicine
Cytotoxicity of new platinum complexes based on 3-(2-pyridyl)-1,2,4-triazole derivatives against squamous cell carcinoma
1Yeshchenko M. O., 1, 2Virych P. A., 1Kostovskyi M. S., 1Raspertova I. V., 1Khomenko D. M., 1, 2Virych P. A.
  1. Taras Shevchenko National University of Kyiv
    64, Volodymyrska Str., Kyiv, Ukraine, 01601
  2. State Institution “O.S. Kolomiychenko Institute of Otolaryngology of National Academy of Medical Science of Ukraine”
    3, Zoologichna Str., Kyiv, Ukraine, 08702, 03680

Abstract

Platinum complexes are one of the key elements of anti-tumor chemotherapy. Currently, the efforts are focused on the development of novel Pt-complexes based on ligands of various chemical nature. The aim of the research was to study the anticancer activity of new platinum complexes based on ligands 2-(5-ethyl-1-methyl-1H-1,2,4-triazol-3-yl)pyridine (L6) and benzyl (2-(5-benzyl-1-methyl-1H-1,2,4-triazol-3-yl)pyridine (L12). Methods. The cytotoxicity of the Pt(L6) Cl2 and Pt(L12)Cl2 complexes against the Hep-2 and MAEC cells was assessed. The catalytic activities of lactate dehydrogenase (LDH), succinate dehydrogenase (SDH), and glucose-6-phosphate dehydrogenase (G6PD) were determined using the nitroblue tetrazolium assay. The intracellular ROS level was determined by the 2',7'-dichlorofluorescein diacetate, and the mitochondrial potential (ΔΨm) was determined by Rhodamine 123. Results. The calculated EC50 for Pt(L12)Cl2 against Hep-2 cells was 9.12±0.33 μM. The LDH activity was decreased in both Hep-2 and MAEC cells, but no changes in the SDH activity were detected in Hep-2 cells. In Hep-2 cells, the treatment with the Pt(L12)Cl2 complex resulted in decrease in G6PD activity, whereas the Pt(L6)Cl2 complex induced increase. An increase in the ΔΨm and ROS was observed in Hep-2 cell. Conclusions. The Pt complexes have a cytotoxic effect on Hep-2 cells by reducing the activity of LDH, but without affecting SDH. Intracellular ROS level was changed weak, but ΔΨm was increased.
Keywords: platinum complexes, cancer, reactive oxygen species, mitochondrial membrane potential, lactate dehydrogenase, succinate dehydrogenase
Full text: (PDF, in English)

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