Anticancer activity of MPT0E028, a novel potent histone deacetylase inhibitor, in human colorectal cancer HCT116 cells in vitro and in vivo

Han-Lin Huang, Hsueh Yun Lee, An-Chi Tsai, Chieh-Yu Peng, Mei-Jung Lai, Jing-Chi Wang, Shiow Lin Pan, Che-Ming Teng, Jing Ping Liou

Research output: Contribution to journalArticle

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Abstract

Recently, histone deacetylase (HDAC) inhibitors have emerged as a promising class of drugs for treatment of cancers, especially subcutaneous T-cell lymphoma. In this study, we demonstrated that MPT0E028, a novel N-hydroxyacrylamide-derived HDAC inhibitor, inhibited human colorectal cancer HCT116 cell growth in vitro and in vivo. The results of NCI-60 screening showed that MPT0E028 inhibited proliferation in both solid and hematological tumor cell lines at micromolar concentrations, and was especially potent in HCT116 cells. MPT0E028 had a stronger apoptotic activity and inhibited HDACs activity more potently than SAHA, the first therapeutic HDAC inhibitor proved by FDA. In vivo murine model, the growth of HCT116 tumor xenograft was delayed and inhibited after treatment with MPT0E028 in a dose-dependent manner. Based on in vivo study, MPT0E028 showed stronger anti-cancer efficacy than SAHA. No significant body weight difference or other adverse effects were observed in both MPT0E028-and SAHA-treated groups. Taken together, our results demonstrate that MPT0E028 has several properties and is potential as a promising anti-cancer therapeutic drug.

Original languageEnglish
Article numbere43645
JournalPLoS One
Volume7
Issue number8
DOIs
Publication statusPublished - Aug 22 2012

Fingerprint

HCT116 Cells
histone deacetylase
Histone Deacetylase Inhibitors
colorectal neoplasms
Colorectal Neoplasms
neoplasms
therapeutics
in vivo studies
lymphoma
Tumors
Neoplasms
drug therapy
cell growth
T-lymphocytes
animal models
adverse effects
cell lines
screening
T-cells
T-Cell Lymphoma

ASJC Scopus subject areas

  • Agricultural and Biological Sciences(all)
  • Biochemistry, Genetics and Molecular Biology(all)
  • Medicine(all)

Cite this

Anticancer activity of MPT0E028, a novel potent histone deacetylase inhibitor, in human colorectal cancer HCT116 cells in vitro and in vivo. / Huang, Han-Lin; Lee, Hsueh Yun; Tsai, An-Chi; Peng, Chieh-Yu; Lai, Mei-Jung; Wang, Jing-Chi; Pan, Shiow Lin; Teng, Che-Ming; Liou, Jing Ping.

In: PLoS One, Vol. 7, No. 8, e43645, 22.08.2012.

Research output: Contribution to journalArticle

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