HDAC1 inhibition by MS-275 in mesothelial cells limits cellular invasion and promotes MMT reversal

Sci Rep. 2018 May 31;8(1):8492. doi: 10.1038/s41598-018-26319-2.

Abstract

Peritoneal fibrosis is a pathological alteration of the peritoneal membrane occurring in a variety of conditions including peritoneal dialysis (PD), post-surgery adhesions and peritoneal metastases. The acquisition of invasive and pro-fibrotic abilities by mesothelial cells (MCs) through induction of MMT, a cell-specific form of EMT, plays a main role in this process. Aim of this study was to evaluate possible effects of histone deacetylase (HDAC) inhibitors, key components of the epigenetic machinery, in counteracting MMT observed in MCs isolated from effluent of PD patients. HDAC inhibitors with different class/isoform selectivity have been used for pharmacological inhibition. While the effect of other inhibitors was limited to a partial E-cadherin re-expression, MS-275, a HDAC1-3 inhibitor, promoted: (i) downregulation of mesenchymal markers (MMP2, Col1A1, PAI-1, TGFβ1, TGFβRI) (ii) upregulation of epithelial markers (E-cadherin, Occludin), (iii) reacquisition of an epithelial-like morphology and (iv) marked reduction of cellular invasiveness. Results were confirmed by HDAC1 genetic silencing. Mechanistically, MS-275 causes: (i) increase of nuclear histone H3 acetylation (ii) rescue of the acetylation profile on E-cadherin promoter, (iii) Snail functional impairment. Overall, our study, pinpointing a role for HDAC1, revealed a new player in the regulation of peritoneal fibrosis, providing the rationale for future therapeutic opportunities.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aged
  • Aged, 80 and over
  • Benzamides / pharmacology*
  • Cadherins / metabolism
  • Cell Movement / drug effects
  • Epithelial Cells / cytology
  • Epithelial Cells / metabolism
  • Epithelial-Mesenchymal Transition / drug effects*
  • Female
  • Histone Deacetylase 1 / antagonists & inhibitors*
  • Histone Deacetylase 1 / genetics
  • Histone Deacetylase 1 / metabolism
  • Histone Deacetylase Inhibitors / pharmacology*
  • Humans
  • Kidney Failure, Chronic / metabolism
  • Kidney Failure, Chronic / pathology
  • Male
  • Middle Aged
  • Peritoneal Dialysis
  • Peritoneum / cytology
  • Pyridines / pharmacology*
  • RNA Interference
  • RNA, Small Interfering / metabolism
  • Snail Family Transcription Factors / metabolism
  • Transforming Growth Factor beta1 / metabolism

Substances

  • Benzamides
  • Cadherins
  • Histone Deacetylase Inhibitors
  • Pyridines
  • RNA, Small Interfering
  • SNAI1 protein, human
  • Snail Family Transcription Factors
  • Transforming Growth Factor beta1
  • entinostat
  • HDAC1 protein, human
  • Histone Deacetylase 1