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BP-M345, a New Diarylpentanoid with Promising Antimitotic Activity.


ABSTRACT: Previously, we reported the in vitro growth inhibitory effect of diarylpentanoid BP-M345 on human cancer cells. Nevertheless, at that time, the cellular mechanism through which BP-M345 exerts its growth inhibitory effect remained to be explored. In the present work, we report its mechanism of action on cancer cells. The compound exhibits a potent tumor growth inhibitory activity with high selectivity index. Mechanistically, it induces perturbation of the spindles through microtubule instability. As a consequence, treated cells exhibit irreversible defects in chromosome congression during mitosis, which induce a prolonged spindle assembly checkpoint-dependent mitotic arrest, followed by massive apoptosis, as revealed by live cell imaging. Collectively, the results indicate that the diarylpentanoid BP-M345 exerts its antiproliferative activity by inhibiting mitosis through microtubule perturbation and causing cancer cell death, thereby highlighting its potential as antitumor agent.

SUBMITTER: Novais P 

PROVIDER: S-EPMC8659070 | biostudies-literature | 2021 Nov

REPOSITORIES: biostudies-literature

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BP-M345, a New Diarylpentanoid with Promising Antimitotic Activity.

Novais Pedro P   Silva Patrícia M A PMA   Moreira Joana J   Palmeira Andreia A   Amorim Isabel I   Pinto Madalena M   Cidade Honorina H   Bousbaa Hassan H  

Molecules (Basel, Switzerland) 20211125 23


Previously, we reported the in vitro growth inhibitory effect of diarylpentanoid BP-M345 on human cancer cells. Nevertheless, at that time, the cellular mechanism through which BP-M345 exerts its growth inhibitory effect remained to be explored. In the present work, we report its mechanism of action on cancer cells. The compound exhibits a potent tumor growth inhibitory activity with high selectivity index. Mechanistically, it induces perturbation of the spindles through microtubule instability.  ...[more]

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