Cytotoxic mechanism of tioconazole involves cell cycle arrest at mitosis through inhibition of microtubule assembly.

ABSTRACT: Tioconazole is one of the drugs used to treat topical mycotic infections. It exhibited severe toxicity during systemic administration; however, the molecular mechanism behind the cytotoxic effect was not well established. We employed HeLa cells as a model to investigate the molecular mechanism of its toxicity and discovered that tioconazole inhibited HeLa cell growth through mitotic block (37%). At the half-maximal inhibitory concentration (≈ 15 μM) tioconazole apparently depolymerized microtubules and caused defects in chromosomal congression at the metaphase plate. Tioconazole induced apoptosis and significantly hindered the migration of HeLa cells. Tioconazole bound to goat brain tubulin (K _d, 28.3 ± 0.5 μM) and inhibited the assembly of microtubules in the in vitro as

SUBMITTER: Sebastian J 

PROVIDER: S-EPMC8816991 | biostudies-literature | 2022 Feb

REPOSITORIES: biostudies-literature