Preprint Article Version 1 Preserved in Portico This version is not peer-reviewed

Аntiproliferative, Pro-apoptotic Activity and Tubulin Dynamics Modulation of 1H-Benzimidazole-2-Yl Hydrazones in Human Breast Cancer Cell Line Mda-Mb-231

Denitsa Yancheva
* ORCID logo ,
Maria Argirova
,
Irina Georgieva
ORCID logo ,
Vanya Milanova
,
Maya Guncheva
ORCID logo ,
Nadya Hristova-Avakumova
,
Miroslav Rangelov
,
Nadezhda Todorova
,
Rumiana Tzoneva
*
Version 1 : Received: 19 March 2024 / Approved: 20 March 2024 / Online: 21 March 2024 (02:16:43 CET)

How to cite: Yancheva, D.; Argirova, M.; Georgieva, I.; Milanova, V.; Guncheva, M.; Hristova-Avakumova, N.; Rangelov, M.; Todorova, N.; Tzoneva, R. Аntiproliferative, Pro-apoptotic Activity and Tubulin Dynamics Modulation of 1H-Benzimidazole-2-Yl Hydrazones in Human Breast Cancer Cell Line Mda-Mb-231. Preprints 2024, 2024031210. https://doi.org/10.20944/preprints202403.1210.v1 Yancheva, D.; Argirova, M.; Georgieva, I.; Milanova, V.; Guncheva, M.; Hristova-Avakumova, N.; Rangelov, M.; Todorova, N.; Tzoneva, R. Аntiproliferative, Pro-apoptotic Activity and Tubulin Dynamics Modulation of 1H-Benzimidazole-2-Yl Hydrazones in Human Breast Cancer Cell Line Mda-Mb-231. Preprints 2024, 2024031210. https://doi.org/10.20944/preprints202403.1210.v1

Abstract

(1) Background: In this work, a series of benzimidazole derivatives containing colchicine-like and cathechol-like moieties with methyl group substitution in the benzimidazole ring were evaluated for their in vitro antiproliferative, pro-apoptotic and antioxidative activity against highly invasive breast cancer cell line MDA-MB-231 and related impairment of tubulin dynamics; (2) Methods: MTT assay was used to evaluate the antiproliferative activity. In vitro tubulin polymerization assay as well as docking analysis was applied to prove the alterations in tubulin polymerization. Immunofluorescent and DAPI staining reveal the pro-apoptotic potential of benzimidazole derivatives and the effect on tubulin’s dynamics in living cells. The antioxidant activity was evaluated by scavenging of H2O2 and hypochlorite ion and ortho-phenanthroline tests; (3) Results: The compounds containing colchicine-like moiety displayed significant growth inhibitory effect against cancer cell line as was highlighted the role of methyl functional group on the tubulin aggregation and blockage of mitosis. All compounds showed an ability to scavenge H2O2, while the compounds with cathecol-like moiety were more effective against hypochlorite ion and chelation of iron; (4) Conclusions: The benzimidazole derivative containing colchicine-like moiety and methyl group substitution in benzimidazole ring is a potential antiproliferative and microtubule destabilizing agent.

Keywords

benzimidazole-2-yl hydrazones; tubulin polymerization; mitotic blockage; cytotoxicity; oxidative stress; MDA-MB-231 cells

Subject

Biology and Life Sciences, Life Sciences

Copyright: This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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