nbm-hd-1: a novel histone deacetylase inhibitor with anticancer activity
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2012
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Abstract
HDAC inhibitors (HDACis) have been developed as promising anticancer agents in recent years. In this study, we synthesized and characterized a novel HDACi, termed NBM-HD-1. This agent was derived from the semisynthesis of propolin G, isolated from Taiwanese green propolis (TGP), and was shown to be a potent suppressor of tumor cell growth in human breast cancer cells (MCF-7 and MDA-MB-231) and rat glioma cells (C6), with an IC50 ranging from 8.5 to 10.3 μM. Western blot demonstrated that levels of p21(Waf1/Cip1), gelsolin, Ac-histone 4, and Ac-tubulin markedly increased after treatment of cancer cells with NBM-HD-1. After NBM-HD-1 treatment for 1–4 h, p-PTEN and p-AKT levels were markedly decreased. Furthermore, we also found the anticancer activities of NBM-HD-1 in regulating cell cycle regulators. Treatment with NBM-HD-1, p21(Waf1/Cip1) gene expression had markedly increased while cyclin B1 and D1 gene expressions had markedly decreased. On the other hand, we found that NBM-HD-1 increased the expressions of tumor-suppressor gene p53 in a dose-dependent manner. Finally, we showed that NBM-HD-1 exhibited potent antitumor activity in a xenograft model. In conclusion, this study demonstrated that this compound, NBM-HD-1, is a novel and potent HDACi with anticancer activity in vitro and in vivo.
| Reference Key |
huang2012evidence-basednbm-hd-1:
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| Authors | ;Wei-Jan Huang;Yu-Chih Liang;Shuang-En Chuang;Li-Ling Chi;Chi-Yun Lee;Chia-Wei Lin;Ai-Ling Chen;Jing-Shi Huang;Chun-Jung Chiu;Cheng-Feng Lee;Chung-Yang Huang;Chia-Nan Chen |
| Journal | ACS applied materials & interfaces |
| Year | 2012 |
| DOI |
10.1155/2012/781417
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| URL | |
| Keywords |
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