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Evidence-Based Complementary and Alternative Medicine
Volume 2012, Article ID 781417, 11 pages
http://dx.doi.org/10.1155/2012/781417
Research Article

NBM-HD-1: A Novel Histone Deacetylase Inhibitor with Anticancer Activity

1Graduate Institute of Pharmacognosy, College of Medicine, Taipei Medical University, Taipei 110, Taiwan
2School of Medical Laboratory Science and Biotechnology, College of Medicine, Taipei Medical University, Taipei 100, Taiwan
3National Institute of Cancer Research, National Health Research Institutes, Miaoli County, Zhunan 350, Taiwan
4New Drug Research and Development Center, NatureWise Biotech & Medicals Corporation, Nankang, Taipei 115, Taiwan

Received 14 June 2011; Revised 11 August 2011; Accepted 11 August 2011

Academic Editor: Vassya Bankova

Copyright © 2012 Wei-Jan Huang et al. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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.