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The assessment of the cytotoxic activity of 2-(1,1-dimethyl-1H-benzo[e]indolin-2-yl)-5,6,7-trichloro-1,3-tropolone against the human glioblastoma U87 MG cell line

https://doi.org/10.37748/2686-9039-2025-6-2-1

EDN: hejatt

Abstract

Purpose of the study. To study the cytotoxic effect of 2-(1,1-dimethyl-1H-benzo[e]indolin-2-yl)-5,6,7-trichloro-1,3-tropolone (JO-122 (2)) on the U87 MG cell line.

Materials and methods. The investigation of the cytotoxic effect of synthesized tropolone JO-122 (2) was performed using the standard MTT colorimetric assay on the human glioblastoma cell line U87 MG. Test substance samples were prepared by sequential twofold dilutions of the original stock solution with concentrations of 24 μM. Temozolomide was used as a reference drug, and its tested doses fell in the range of 250 to 0.4883 μM. Incubation time after the addition of the substances were 24, 48, and 72 hours. The statistical processing of the obtained data was carried out using Microsoft Excel 2013 and Statistica 10 software.

Results. The cytotoxic effect of 2-(1,1-dimethyl-1H-benzo[e]indolin-2-yl)-5,6,7-trichloro-1,3-tropolone on the U87 MG cell line was investigated in the study. The assessment of cytotoxicity showed that at all investigated doses of tropolone, there was a statistically significant inhibition of cell growth in the U87 MG cell line. After 24, 48, and 72 hours, the necessary minimum concentration of JO-122 (2) for suppressing tumor cell growth was 3 μM, 0.0469 μM, and 0.1875 μM, respectively.

The comparison drug showed less pronounced suppression of tumor cell growth compared to tropolone. For an incubation time of 24 hours, no significant decrease in cell viability was observed in any of the tested concentrations. The minimum concentration of Temozolomide required to inhibit U87 MG cell culture growth was obtained after 72 hours and was 3.9063 μM.

Conclusion. The conducted research demonstrated that both substances exhibited concentration-dependent toxicity towards the human glioblastoma cell line. However, tropolone JO-122 (2) showed a more pronounced ability to suppress the growth of the U87 MG cell line.

About the Authors

D. V. Khodakova
National Medical Research Centre for Oncology
Russian Federation

Darya V. Khodakova – junior researcher at the testing Laboratory Center, National Medical Research Centre for Oncology, Rostov-on-Don, Russian Federation

ORCID: https://orcid.org/0000-0003-3753-4463, SPIN: 8718-3983, AuthorID: 1056414, ResearcherID: MCK-3167-2025, Scopus Author ID: 57221463056


Competing Interests:

the authors declare that there are no obvious and potential conflicts of interest associated with the publication of this article



N. S. Kuznetsova
National Medical Research Centre for Oncology
Russian Federation

Natalia S. Kuznetsova – MD, oncologist, National Medical Research Center for Oncology, Rostov-on-Don, Russian Federation

ORCID: https://orcid.org/0000-0002-2337-326X, SPIN: 8553-3081, AuthorID: 920734


Competing Interests:

the authors declare that there are no obvious and potential conflicts of interest associated with the publication of this article



S. Yu. Filippova
National Medical Research Centre for Oncology
Russian Federation

Svetlana Yu. Filippova – Researcher at the Laboratory of Cellular Technologies, National Medical Research Center for Oncology, Rostov-on-Don, Russian Federation

ORCID: https://orcid.org/0000-0002-4558-5896, SPIN: 9586-2785, AuthorID: 878784, ResearcherID: AAH-4408-2020, Scopus Author ID: 5718961884


Competing Interests:

the authors declare that there are no obvious and potential conflicts of interest associated with the publication of this article



A. S. Goncharova
National Medical Research Centre for Oncology
Russian Federation

Anna S. Goncharova – Cand. Sci. (Biol.), head of testing Laboratory Center, National Medical Research Centre for Oncology, Rostov-on-Don, Russian Federation

ORCID: https://orcid.org/0000-0003-0676-0871, SPIN: 7512-2039, AuthorID: 553424, Scopus Author ID: 57215862139


Competing Interests:

the authors declare that there are no obvious and potential conflicts of interest associated with the publication of this article



A. V. Galina
National Medical Research Centre for Oncology
Russian Federation

Anastasia V. Galina – junior researcher at the testing Laboratory Center, National Medical Research Centre for Oncology, Rostov-on-Don, Russian Federation

ORCID: https://orcid.org/0000-0001-7823-3865, SPIN: 9171-4476, AuthorID: 1071933, Scopus Author ID: 57221460594


Competing Interests:

the authors declare that there are no obvious and potential conflicts of interest associated with the publication of this article



S. V. Gurova
National Medical Research Centre for Oncology
Russian Federation

Sofya V. Gurova – junior researcher at the testing Laboratory Center, National Medical Research Centre for Oncology, Rostov-on-Don, Russian Federation

ORCID: https://orcid.org/0000-0002-9747-8515, SPIN: 5413-6901, AuthorID: 1147419


Competing Interests:

the authors declare that there are no obvious and potential conflicts of interest associated with the publication of this article



E. A. Gusakov
National Medical Research Centre for Oncology
Russian Federation

Evgeniy A. Gusakov – Cand. Sci. (Chem.), Researcher at the Research Institute of Physical and Organic Chemistry, Southern Federal University, Rostov-on-Don, Russian Federation

ORCID: https://orcid.org/0000-0001-7593-1334, SPIN: 1690-9488, AuthorID: 789745, Scopus Author ID: 55180460600


Competing Interests:

the authors declare that there are no obvious and potential conflicts of interest associated with the publication of this article



Yu. A. Sayapin
National Medical Research Centre for Oncology
Russian Federation

Yurii A. Sayapin – Cand. Sci. (Chem.), Head of the Laboratory of Physical and Organic Chemistry, Federal Research Center at the Southern Scientific Center of the Russian Academy of Sciences, Rostov-on-Don, Russian Federation

ORCID: https://orcid.org/0000-0002-3180-1762, SPIN: 4877-3959, AuthorID: 121929


Competing Interests:

the authors declare that there are no obvious and potential conflicts of interest associated with the publication of this article



E. E. Rostorguev
National Medical Research Centre for Oncology
Russian Federation

Eduard E. Rostorguev – MD, Head of the Department of Neuro-Oncology, National Medical Research Center for Oncology, Rostov-on-Don, Russian Federation

ORCID: https://orcid.org/0000-0003-2937-0470, SPIN: 8487-9157, AuthorID: 794808, Scopus Author ID: 57196005138


Competing Interests:

the authors declare that there are no obvious and potential conflicts of interest associated with the publication of this article



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Khodakova D.V., Kuznetsova N.S., Filippova S.Yu., Goncharova A.S., Galina A.V., Gurova S.V., Gusakov E.A., Sayapin Yu.A., Rostorguev E.E. The assessment of the cytotoxic activity of 2-(1,1-dimethyl-1H-benzo[e]indolin-2-yl)-5,6,7-trichloro-1,3-tropolone against the human glioblastoma U87 MG cell line. South Russian Journal of Cancer. 2025;6(2):6-13. https://doi.org/10.37748/2686-9039-2025-6-2-1. EDN: hejatt

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