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

- 2′,4′-Dihydroxy-3,4,5-trimethoxychalcone disrupts spindle organization.
- 2′,4′-Dihydroxy-3,4,5-trimethoxychalcone induces sustained mitotic arrest.
- 2′,4′-Dihydroxy-3,4,5-trimethoxychalcone activates the spindle checkpoint.
- 2′,4′-Dihydroxy-3,4,5-trimethoxychalcone results in mitotic catastrophe.

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.