Therapeutic effects of histone deacetylase inhibitors in a murine asthma model

Inflamm Res. 2016 Dec;65(12):995-1008. doi: 10.1007/s00011-016-0984-4. Epub 2016 Aug 26.

Abstract

Objective and design: To investigate the therapeutic effects of various HDAC inhibitors on the development of chronic allergic airway disease in mice with airway inflammation, airway remodeling, and airway hyperresponsiveness.

Subjects: Wild-type BALB/C mice (N = 72).

Treatment: Tubastatin A HCl [TSA, a selective histone deacetylase 6 (HDAC6) inhibitor], PCI-34051 (a selective HDAC8 inhibitor), and givinostat (a broad-spectrum HDAC inhibitor that inhibits class I and class II HDACs and several pro-inflammatory cytokines).

Methods: Mice were divided into six groups: control, asthma, dexamethasone (positive control), TSA, PCI-34051, and givinostat (n = 12 per group). Twenty-four hours after OVA nebulization, airway hyperresponsiveness, inflammation, and remodeling were assessed.

Results: The chronic asthma mouse model produced typical airway inflammation, airway remodeling, and airway hyperresponsiveness. Administration of PCI-34051 and dexamethasone reduced the eosinophilic inflammation and airway hyperresponsiveness in asthma to reduce the airway remodeling. Treatment with Tubastatin A HCl reduced airway inflammation and was associated with decreased IL-4, IL-5 and total inflammatory cell count, as well as goblet cell metaplasia and subepithelial fibrosis; however, this outcome was not as effective as that with dexamethasone. TGF-β1 expression in the cytoplasm of airway epithelium of mice in the Tubastatin A HCl group was reduced and expression of α-SMA in the airway smooth muscle was also decreased.

Conclusions: The results suggested that treatment with HDAC inhibitors can reduce airway inflammation, airway remodeling, and airway hyperresponsiveness in chronic allergic airway disease in mice.

Keywords: Airway hyperresponsiveness; Airway inflammation; Bronchial asthma; Histone deacetylase.

MeSH terms

  • Actins / metabolism
  • Airway Remodeling / drug effects
  • Animals
  • Anti-Asthmatic Agents / pharmacology
  • Anti-Asthmatic Agents / therapeutic use*
  • Asthma / drug therapy*
  • Asthma / metabolism
  • Asthma / pathology
  • Asthma / physiopathology
  • Bronchial Hyperreactivity / drug therapy
  • Bronchial Hyperreactivity / metabolism
  • Bronchial Hyperreactivity / pathology
  • Bronchial Hyperreactivity / physiopathology
  • Bronchoalveolar Lavage Fluid / cytology
  • Bronchoalveolar Lavage Fluid / immunology
  • Collagen / metabolism
  • Cytokines / metabolism
  • Disease Models, Animal
  • Female
  • Histone Deacetylase Inhibitors / pharmacology
  • Histone Deacetylase Inhibitors / therapeutic use*
  • Hydroxamic Acids / pharmacology
  • Hydroxamic Acids / therapeutic use
  • Indoles / pharmacology
  • Indoles / therapeutic use
  • Lung / drug effects
  • Lung / metabolism
  • Mice
  • Mice, Inbred BALB C
  • Transforming Growth Factor beta1 / metabolism

Substances

  • Actins
  • Anti-Asthmatic Agents
  • Cytokines
  • Histone Deacetylase Inhibitors
  • Hydroxamic Acids
  • Indoles
  • PCI 34051
  • Transforming Growth Factor beta1
  • tubastatin A
  • Collagen