title: A novel histone deacetylase inhibitor Chidamide induces G0/G1 arrest and apoptosis in myelodysplastic syndromes.
abstract: Chidamide as a newly designed and synthesized histone deacetylase inhibitor induces an antitumor effect in various cancer, and it has been used in several clinical trials such as peripheral T cell lymphoma (PTCL). Here we demonstrate that Chidamide was able to increase the acetylation levels of histone H3 and decrease HDAC activity in MDS cell lines(SKM-1,MUTZ-1)and AML cell line(KG-1). In vitro, at low concentration (<250nM) of Chidamide inhibited cell proliferation and delayed G0/G1 cell cycle progression by down-regulating CDK2 and regulating p-P53 and P21 protein expression. Meanwhile,it also induced cell apoptosis by down-regulating Bcl-2 and up-regulating cleaved Caspase-3 and Bax protein expression.The results of the present study demonstrates the potential utility of Chidamide for the treatment of Myelodysplastic syndromes.
authors.affiliation: Department of Hematology, Tianjin Medical University General Hospital, Tianjin, PR China.
authors.forename: Zhaoyun
authors.initials: Z
authors.lastname: Liu
authors.affiliation: Department of Hematology, Tianjin Medical University General Hospital, Tianjin, PR China.
authors.forename: Kai
authors.initials: K
authors.lastname: Ding
authors.affiliation: Department of Hematology, Tianjin Medical University General Hospital, Tianjin, PR China.
authors.forename: Lijuan
authors.initials: L
authors.lastname: Li
authors.affiliation: Department of Hematology, Tianjin Medical University General Hospital, Tianjin, PR China.
authors.forename: Hui
authors.initials: H
authors.lastname: Liu
authors.affiliation: Department of Hematology, Tianjin Medical University General Hospital, Tianjin, PR China.
authors.forename: Yihao
authors.initials: Y
authors.lastname: Wang
authors.affiliation: Department of Hematology, Tianjin Medical University General Hospital, Tianjin, PR China.
authors.forename: Chunyan
authors.initials: C
authors.lastname: Liu
authors.affiliation: Department of Hematology, Tianjin Medical University General Hospital, Tianjin, PR China. Electronic address: florai@sina.com.
authors.forename: Rong
authors.initials: R
authors.lastname: Fu
mesh_terms: D000107:Acetylation / Q000187:drug effects; D000631:Aminopyridines / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects*; D001549:Benzamides / Q000494:pharmacology*; D002460:Cell Line; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D059585:G1 Phase Cell Cycle Checkpoints / Q000187:drug effects*; D056572:Histone Deacetylase Inhibitors / Q000494:pharmacology*; D006657:Histones / Q000378:metabolism; D006801:Humans; D009190:Myelodysplastic Syndromes / Q000473:pathology*; D016192:Resting Phase, Cell Cycle / Q000187:drug effects*
chemical_list: D000631:Aminopyridines; D001549:Benzamides; D056572:Histone Deacetylase Inhibitors; D006657:Histones; C547816:N-(2-amino-5-fluorobenzyl)-4-(N-(pyridine-3-acrylyl)aminomethyl)benzamide
keywords: Apoptosis; Cell cycle; Chidamide; HDAC inhibitor; Myelodysplastic syndrome