4.5 Article

The novel agent ophiobolin O induces apoptosis and cell cycle arrest of MCF-7 cells through activation of MAPK signaling pathways

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 22, Issue 1, Pages 579-585

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.10.079

Keywords

Ophiobolin O; Breast cancer; MAPK signaling pathway; Apoptosis; Cell cycle arrest

Funding

  1. Ministry of Science and Technology of China [2010CB833804]

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Ophiobolin O is a natural compound that has been isolated from Aspergillus ustus 094102. This is the first study to demonstrate the anti-proliferative effect of ophiobolin O in human breast cancer MCF-7 cells. The results of present study show that ophiobolin O induced cycle G(0)/G(1) phase arrest in MCF-7 cells using a cell cycle analysis. In addition, we demonstrated that ophiobolin O reduced the viability of human breast cancer MCF-7 cells in a time- and dose-dependent manner and efficiently induced apoptosis in MCF-7 cells using the Annexin V/PI binding assay. Ophiobolin O also caused the activation of JNK (c-Jun NH2-terminal kinase), p38 MAPK (mitogen activated protein kinase) and ERK (extracellular signal-regulated kinase) as well as the degradation of Bcl-2 phosphorylation (Ser70). Bax protein expression was not changed in ophiobolin O-treated cells. Taken together, ophiobolin O may be considered as a novel therapeutic agent in breast cancer. Crown Copyright (C) 2011 Published by Elsevier Ltd. All rights reserved.

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