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http://ir.nhri.org.tw/handle/3990099045/6221
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| Title: | NBM-HD-1: A novel histone deacetylase inhibitor with anticancer activity |
| Authors: | Huang, WJ;Liang, YC;Chuang, SE;Chi, LL;Lee, CY;Lin, CW;Chen, AL;Huang, JS;Chiu, CJ;Lee, CF;Huang, CY;Chen, CN |
| Contributors: | National Institute of Cancer Research |
| 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. |
| Date: | 2012-01 |
| Relation: | Evidence-based Complementary and Alternative Medicine. 2012 Jan;2012:Article ID 781417. |
| Link to: | http://dx.doi.org/10.1155/2012/781417 |
| Cited Times(WOS): | https://www.webofscience.com/wos/woscc/full-record/WOS:000298614100001 |
| Cited Times(Scopus): | http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=84855182267 |
| Appears in Collections: | [莊雙恩] 期刊論文
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| SCP84855182267.pdf | | 1707Kb | Adobe PDF | 754 | View/Open |
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