Evaluation of 2',4'-dihydroxy-3,4,5-trimethoxychalcone as antimitotic agent that induces mitotic catastrophe in MCF-7 breast cancer cells.

Toxicol Lett

Centro de Química Medicinal da Universidade do Porto (CEQUIMED-UP), Rua de Jorge Viterbo Ferreira 228, 4050-313 Porto, Portugal; Laboratório de Química Orgânica e Farmacêutica, Departamento de Ciências Químicas, Faculdade de Farmácia, Universidade do Porto, Rua de Jorge Viterbo Ferreira 228, 4050-313 Porto, Portugal; Centro Interdisciplinar de Investigação Marinha e Ambiental (CIIMAR/CIMAR), Universidade do Porto, Rua dos Bragas 289, 4050-123, Porto, Portugal. Electronic address:

Published: September 2014

We previously reported the synthesis and the anti-proliferative action of 2',4'-dihydroxy-3,4,5-trimethoxychalcone. Here we reported its mechanism of action on MCF-7 cells. The compound induced aberrant spindles, and arrested cells at metaphase/anaphase boundary with accumulation of checkpoint proteins Mad2, Bub1 and BubR1. Live cell imaging revealed that the compound sustained a prolonged mitotic arrest, followed by massive cell death. The results indicate that 2',4'-dihydroxy-3,4,5-trimethoxychalcone exerts its anti-proliferative activity by affecting microtubules and causing mitotic catastrophe, and thus has the potential for antitumor activity.

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http://dx.doi.org/10.1016/j.toxlet.2014.06.016DOI Listing

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