Anticancer Activity of MPT0E028, a Novel Potent Histone Deacetylase Inhibitor, in Human Colorectal Cancer HCT116 Cells In Vitro and In Vivo 英文参考文献.docVIP

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Anticancer Activity of MPT0E028, a Novel Potent Histone Deacetylase Inhibitor, in Human Colorectal Cancer HCT116 Cells In Vitro and In Vivo 英文参考文献.doc

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

AnticancerActivityofMPT0E028,aNovelPotentHistone DeacetylaseInhibitor,inHumanColorectalCancer HCT116CellsInVitroandInVivo Han-LinHuang1.,Hsueh-YunLee2.,An-ChiTsai3,Chieh-YuPeng5,Mei-JungLai2,Jing-ChiWang3, Shiow-LinPan3,4*,Che-MingTeng1*,Jing-PingLiou2* 1PharmacologicalInstitute,CollegeofMedicine,NationalTaiwanUniversity,Taipei,Taiwan,2SchoolofPharmacy,CollegeofPharmacy,TaipeiMedicalUniversity,Taipei, Taiwan, 3Institute of Biotechnology and Pharmaceutical Research, National Health Research Institutes, Zhunan Town, Miaoli County, Taiwan, 4Department of Pharmacology,TaipeiMedicalUniversity,Taipei,Taiwan,5SchoolofChineseMedicine,CollegeofChineseMedicine,ChinaMedicalUniversity,Taichung,Taiwan 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, wedemonstrated that MPT0E028,a novel N-hydroxyacrylamide- derivedHDACinhibitor,inhibitedhumancolorectalcancerHCT116cellgrowthinvitroandinvivo.TheresultsofNCI-60 screening showed that MPT0E028 inhibited proliferation in both solid and hematological tumor cell lines at micromolar concentrations,andwasespeciallypotentinHCT116cells.MPT0E028hadastrongerapoptoticactivityandinhibitedHDACs activitymorepotentlythanSAHA,thefirsttherapeuticHDACinhibitorprovedbyFDA.Invivomurinemodel,thegrowthof HCT116tumorxenograftwasdelayedandinhibitedaftertreatmentwithMPT0E028inadose-dependentmanner.Basedon invivostudy,MPT0E028showedstrongeranti-cancerefficacythanSAHA.Nosignificantbodyweightdifferenceorother adverseeffectswereobservedinbothMPT0E028-andSAHA-treatedgroups.Takentogether,ourresultsdemonstratethat MPT0E028hasseveralpropertiesandispotentialasapromisinganti-cancertherapeuticdrug. Citation:HuangH-L,LeeH-Y,TsaiA-C,PengC-Y,LaiM-J,etal.(2012)AnticancerActivityofMPT0E028,aNovelPotentHistoneDeacetylaseInhibitor,inHuman ColorectalCancerHCT116CellsInVitroandInVivo.PLoSONE7(8):e43645.doi:10.1371/journal.pone.0043645 Editor:Man