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Previously we reported the identification of a new oxepin-containing diketopiperazine-type marine fungal metabolite, named protuboxepin A which showed antiproliferative activity in several cancer cell lines. In this study we elucidated the mechanism by which protuboxepin A induces cancer cell growth inhibition. Here we report that protuboxepin A induced round-up morphology, M phase arrest, and an increase in the subG(1) population in tumor cells in a dose dependent manner. Our investigations revealed that protuboxepin A directly binds to α,β-tubulin and stabilizes tubulin polymerization thus disrupting microtubule dynamics. This disruption leads to chromosome misalignment and metaphase arrest which induces apoptosis in cancer. Overall, we identified protuboxepin A as a microtubule-stabilizing agent which has a distinctly different chemical structure from previously reported microtubule inhibitors. These results indicate that protuboxepin A has a potential of being a new and effective anti-cancer drug. Crown Copyright © 2012. Published by Elsevier Ltd. All rights reserved.


Yukihiro Asami, Jae-Hyuk Jang, Nak-Kyun Soung, Long He, Dong Oh Moon, Jong Won Kim, Hyuncheol Oh, Makoto Muroi, Hiroyuki Osada, Bo Yeon Kim, Jong Seog Ahn. Protuboxepin A, a marine fungal metabolite, inducing metaphase arrest and chromosomal misalignment in tumor cells. Bioorganic & medicinal chemistry. 2012 Jun 15;20(12):3799-806

PMID: 22595423

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