NBM-HD-1: A novel histone deacetylase inhibitor with anticancer activity

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

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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 10.3M. 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 14h, 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.

Original languageEnglish
Article number781417
JournalEvidence-based Complementary and Alternative Medicine
Volume2012
DOIs
Publication statusPublished - 2012

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ASJC Scopus subject areas

  • Complementary and alternative medicine

Cite this

Huang, W. J., Liang, Y. C., Chuang, S. E., Chi, L. L., Lee, C. Y., Lin, C. W., Chen, A. L., Huang, J. S., Chiu, C. J., Lee, C. F., Huang, C. Y., & Chen, C. N. (2012). NBM-HD-1: A novel histone deacetylase inhibitor with anticancer activity. Evidence-based Complementary and Alternative Medicine, 2012, [781417]. https://doi.org/10.1155/2012/781417