Discovery of isopenicin A, a meroterpenoid as a novel inhibitor of tubulin polymerization

Microtubules are involved in celluar processes of movement, intracellular trafficking and mitosis, thus microtubule-targeting agents have been widely used in cancer therapy. Herein, we report isopenicin A, a novel meroterpenoid isolated from the plant endophytic fungus of Penicillium sp. sh18, as a...

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Bibliographic Details
Published in:Biochemical and biophysical research communications 2020-04, Vol.525 (2), p.303-307
Main Authors: Chen, Lin, Fan, Dong-Mei, Tang, Jian-Wei, An, Tao, Li, Xue, Kong, Ling-Mei, Puno, Pema-Tenzin, Li, Yan
Format: Article
Language:English
Subjects:
Cancer
Endophytic fungus
Isopenicin A
Meroterpenoid
Microtubule
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Summary:Microtubules are involved in celluar processes of movement, intracellular trafficking and mitosis, thus microtubule-targeting agents have been widely used in cancer therapy. Herein, we report isopenicin A, a novel meroterpenoid isolated from the plant endophytic fungus of Penicillium sp. sh18, as a novel microtubule binding molecule that efficiently depolymerizes microtubule polymerization to evoke G2/M cell cycle arrest and subsequent cell apoptosis, contributing to proliferation inhibition of human tumor cell lines. The discovery of isopenicin A provides a new chemotype for discovery and development of promising microtubule inhibitors. •Identification of isopenicin A as a novel chemotype of microtubule inhibitor.•Isopenicin A induced G2/M cycle arrest and subsequent apoptosis.•Isopenicin A inhibited proliferation of three carcinoma cell lines.
ISSN:0006-291X
1090-2104
DOI:10.1016/j.bbrc.2020.02.026