Anticancer Activity of MPT0E028, a Novel Potent Histone Deacetylase Inhibitor, in Human Colorectal Cancer HCT116 Cells In Vitro and In Vivo

• DOI: 10.1371/journal.pone.0043645
• Publication Date: 2012-08-22T17:28:45Z
• Authors: 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
• Keywords: Histone deacetylase inhibitor; Vorinostat; Growth inhibition

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