Epigenetic and Metabolic Reprogramming of Fibroblasts in Crohn's Disease Strictures Reveals Histone Deacetylases as Therapeutic Targets

J Crohns Colitis. 2024 Jun 3;18(6):895-907. doi: 10.1093/ecco-jcc/jjad209.

Abstract

Background and aims: No effective therapeutic intervention exists for intestinal fibrosis in Crohn's disease [CD]. We characterized fibroblast subtypes, epigenetic and metabolic changes, and signalling pathways in CD fibrosis to inform future therapeutic strategies.

Methods: We undertook immunohistochemistry, metabolic, signalling pathway and epigenetic [Transposase-Accessible Chromatin using sequencing] analyses associated with collagen production in CCD-18Co intestinal fibroblasts and primary fibroblasts isolated from stricturing [SCD] and non-stricturing [NSCD] CD small intestine. SCD/NSCD fibroblasts were cultured with TGFβ and valproic acid [VPA].

Results: Stricturing CD was characterized by distinct histone deacetylase [HDAC] expression profiles, particularly HDAC1, HDAC2, and HDAC7. As a proxy for HDAC activity, reduced numbers of H3K27ac+ cells were found in SCD compared to NSCD sections. Primary fibroblasts had increased extracellular lactate [increased glycolytic activity] and intracellular hydroxyproline [increased collagen production] in SCD compared to NSCD cultures. The metabolic effect of TGFβ stimulation was reversed by the HDAC inhibitor VPA. SCD fibroblasts appeared 'metabolically primed' and responded more strongly to both TGFβ and VPA. Treatment with VPA revealed TGFβ-dependent and TGFβ-independent Collagen-I production in CCD-18Co cells and primary fibroblasts. VPA altered the epigenetic landscape with reduced chromatin accessibility at the COL1A1 and COL1A2 promoters.

Conclusions: Increased HDAC expression profiles, H3K27ac hypoacetylation, a significant glycolytic phenotype and metabolic priming characterize SCD-derived as compared to NSCD fibroblasts. Our results reveal a novel epigenetic component to Collagen-I regulation and TGFβ-mediated CD fibrosis. HDAC inhibitor therapy may 'reset' the epigenetic changes associated with fibrosis.

Keywords: Collagen-I; Crohn’s disease; fibrosis; histone deacetylase; valproic acid.

MeSH terms

  • Cells, Cultured
  • Collagen Type I / genetics
  • Collagen Type I / metabolism
  • Crohn Disease* / drug therapy
  • Crohn Disease* / genetics
  • Crohn Disease* / metabolism
  • Crohn Disease* / pathology
  • Epigenesis, Genetic*
  • Fibroblasts* / drug effects
  • Fibroblasts* / metabolism
  • Fibrosis*
  • Histone Deacetylase 1 / genetics
  • Histone Deacetylase 1 / metabolism
  • Histone Deacetylase 2 / genetics
  • Histone Deacetylase 2 / metabolism
  • Histone Deacetylase Inhibitors* / pharmacology
  • Histone Deacetylases* / genetics
  • Histone Deacetylases* / metabolism
  • Humans
  • Metabolic Reprogramming
  • Signal Transduction / drug effects
  • Transforming Growth Factor beta* / metabolism
  • Valproic Acid* / pharmacology

Substances

  • Valproic Acid
  • Histone Deacetylases
  • Histone Deacetylase Inhibitors
  • HDAC7 protein, human
  • Transforming Growth Factor beta
  • HDAC1 protein, human
  • Histone Deacetylase 1
  • HDAC2 protein, human
  • Histone Deacetylase 2
  • Collagen Type I