A novel histone deacetylase inhibitor Chidamide induces G0/G1 arrest and apoptosis in myelodysplastic syndromes

作者：Liu, Zhaoyun; Ding, Kai; Li, Lijuan; Liu, Hui; Wang, Yihao; Liu, Chunyan; Fu, Rong^*

来源：Biomedicine & Pharmacotherapy, 2016, 83: 1032-1037.

DOI：10.1016/j.biopha.2016.08.023

• Chidamide
• HDAC inhibitor
• Myelodysplastic syndrome
• Cell cycle
• Apoptosis

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 (<250 nM) 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.

• 出版日期2016-10
• 单位天津医科大学