Tag Archives: genotoxicity

Effects of pyrrolidinedione-thiazolidinone hybrid molecules on the genotoxicity in vitro

30.07.2026   Uncategorized

N. Finiuk1,2*, O. Klyuchivska1, R. Lesyk2,3, R. Stoika1

1Department of Regulation of Cell Proliferation and Apoptosis,
Institute of Cell Biology, National Academy of Sciences of Ukraine, Lviv, Ukraine;
2Molecular Design Center, Danylo Halytsky Lviv National Medical University, Lviv, Ukraine;
3Department of Pharmaceutical, Organic and Bioorganic Chemistry,
Danylo Halytsky Lviv National Medical University, Lviv, Ukraine;
*e-mail: nataliyafiniuk@gmail.com

Received: 25 May 2026; Revised: 17 July 2026;
Accepted: 27 July 2026; Available on-line:  04 August 2026

Background. Pyrrolidinedione-thiazolidinone hybrid molecules represent a promising class of anticancer candidates; however, a comprehensive evaluation of their genotoxic and mutagenic safety profile is essential before further preclinical development. Objectives. This work aimed to investigate the genotoxic potential of pyrrolidinedione-thiazolidinone hybrid molecules Les-6287 and Les-6294 that possessed antineoplastic activity. Methods. The mutagenic potential was evaluated using the Ames bacterial reverse mutation test with Salmonella typhimurium strains TA98 and TA100 in the presence and absence of metabolic activation (S9 fraction). The effects at the chromosomal level were assessed using the Allium cepa anaphase-telophase chromosome aberration assay. Primary DNA strand break induction was quantified using the alkaline comet assay. Results. Les-6287 and Les-6294 at 10 and 100 µM concentrations do not produce a mutagenic activity exceeding 1.6 in either S. typhimurium strain TA98 or TA100, with or without S9-mediated metabolic activation. In the A. cepa anaphase-telophase assay treatment with Les-6287 and Les-6294 did not result in a statistically significant elevation in chromosomal aberration frequency relative to the negative control (2.8%), with observed values ranging from 3.3% to 4.3% across all tested concentrations. No significant alterations in the mitotic index were recorded. The alkaline comet assay revealed no significant increase in primary DNA damage, with percent tail DNA of 1.3-1.9% in treated peripheral blood mononuclear cells. Conclusion. Pyrro­lidinedione-thiazolidinone hybrid molecules Les-6287 and Les-6294 at concentrations up to 100 µM do not pose a genotoxic or mutagenic risk under the tested experimental conditions. Further targeted safety assessments are needed prior to progressing Les-6287 and Les-6294 to preclinical evaluation as candidate antitumor agents.

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Functions of metallothioneins and a system of antioxidant defense under the effect of Co- and Zn-containing nanocomposites on crucian carp (Carassius auratus gibelio)

26.10.2015   Uncategorized   No comments

H. I. Falfushynska1,2, L. L. Gnatyshyna1, O. O. Turta1, O. B. Stoliar1,
N. E. Mitina3, O. S. Zaichenko3, R. S. Stoika4

1Volodymyr Hnatiuk Ternopil National Pedagogical University, Ukraine;
2I. Ya. Horbachevski Ternopil State Medical University, Ukraine;
e-mail: halynka.f@gmail.com;
3Lviv Polytechnic National University, Ukraine;
4Institute of Cell Biology, National Academy of Sciences of Ukraine, Lviv

The effect of metal-nanocomposites (Me-NC) of cobalt and zinc (Co- and Zn-NC, correspondingly) synthecized on the basis of vinylpyrrolidone (PS) on the metal-accumulative proteins with antioxidant potential metallothioneins (MT) in crucian carp (Carassius auratus gibelio) was studied­. Fish was subjected to the effect of Co-NC, Zn-NC, Co2+, Zn2+ or polymer carrier (PC) in the concentrations correspondent to 50 µg×Co/l or 100 µg×Zn/l during 14 days. It was shown that the MTs response is highly specific for the nature of metal, both in ion and Me-NC form: the effect of Co and Co-NC provoked the elevation of total MT concentration (MT-SH) and activation of antioxidant defence, whereas Zn and Zn-NC induced the decrease of the concentration of MT-SH and the inhibition of antioxidant defense. All the exposures provoked the decrease of the concentration of immunoreactive chelating MT form (MTi) and reduced glutathione, activation of anaerobiosys and Mn-superoxide dismutase, and also decrease of the concentration of proteins and lipids oxidative injury products. It was accompanied by the increase of the content of erythrocytes with nuclear abnormalities but did not cause the decrease of choline esterase activity. According to the rate of MT-SH and MTi concentrations, antioxidant potential of MTs is determined by its apoform. Our data indicate that partial biodegradation of Me-NC occurs in the organism of crucian carp.

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C(60) fullerene prevents genotoxic effects of doxorubicin in human lymphocytes in vitro

20.05.2015   Uncategorized   No comments

K. S. Afanasieva1, S. V. Prylutska1, A. V. Lozovik1, K. I. Bogutska1, A. V. Sivolob1,
Yu. I. Prylutskyy1, U. Ritter2, P. Scharff2

1Taras Shevchenko National University of Kyiv, Ukraine;
е-mail: prylut@ukr.net;
2Technical University of Ilmenau, Institute of Chemistry
and Biotechnology, Ilmenau, Germany 

The self-ordering of C60  fullerene, doxorubicin and their mixture precipitated from aqueous solutions was investigated using atomic-force microscopy. The results suggest the complexation between the two compounds. The genotoxicity of doxorubicin in complex with C60  fullerene (С60+Dox) was evaluated in vitro with comet assay using human lymphocytes. The obtained results show that the C60  fullerene prevents the toxic effect of Dox in normal cells and, thus, С60+Dox complex might be proposed for biomedical application.

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