2-Chloroacetamidine, a novel immunomodulator, suppresses antigen-induced mouse airway inflammation

Allergy. 2015 Sep;70(9):1130-8. doi: 10.1111/all.12651. Epub 2015 Jun 2.

Abstract

Background: Citrullination is a presently under-recognized posttranslational protein modification catalyzed by PAD enzymes. Immune responses to citrullinated neo-epitopes are identified in a growing number of inflammatory and autoimmune diseases. However, the involvement of hypercitrullination in the pathogenesis of bronchial asthma is still unknown.

Methods: As main experimental tool, we examined the effect of 2-chloroacetamidine (2CA), a PAD enzyme inhibitor, on OVA-immunized and airway-challenged BALB/c mice; a commonly used model of allergic airway inflammation. We also measured the effect of 2CA on ex vivo lymphocytes and cell lines.

Results: In vivo, 2CA dramatically suppressed lung tissue hypercitrullination, inflammatory cell recruitment, and airway-Th2 cytokine secretion. 2CA also suppressed systemic OVA-specific and total IgE production dramatically, effectively preventing de novo and diminishing established disease without measurably impacting general immunocompetence. In vitro, 2CA markedly inhibited the proliferation of mouse and human T cells with cell cycle block and apoptosis during a limited, postactivation phase.

Conclusions: 2CA acts as narrow-spectrum immunosuppressant that selectively targets lymphocyte populations involved in active inflammatory tissue lesions. If hypercitrullination is generated in patients with asthma, 2CA may represent a novel disease modulator for human asthmatics/allergic diseases.

Keywords: T cell; animal model; asthma; protein citrullination.

MeSH terms

  • Amidines / pharmacology*
  • Animals
  • Antigens / immunology*
  • Apoptosis / drug effects
  • Asthma / drug therapy
  • Asthma / genetics
  • Asthma / immunology*
  • Asthma / metabolism
  • Bronchoalveolar Lavage Fluid / cytology
  • Bronchoalveolar Lavage Fluid / immunology
  • Cell Cycle / drug effects
  • Cell Line
  • Disease Models, Animal
  • Disease Progression
  • Enzyme Activation
  • Gene Expression
  • Humans
  • Hydrolases / antagonists & inhibitors
  • Hydrolases / genetics
  • Hydrolases / metabolism
  • Immunologic Factors / pharmacology*
  • Immunosuppressive Agents / pharmacology*
  • Lymphocyte Activation / drug effects
  • Lymphocyte Activation / immunology
  • Mice
  • Protein-Arginine Deiminases
  • T-Lymphocyte Subsets / immunology
  • T-Lymphocyte Subsets / metabolism
  • Th2 Cells / immunology
  • Th2 Cells / metabolism

Substances

  • 2-chloroacetamidine
  • Amidines
  • Antigens
  • Immunologic Factors
  • Immunosuppressive Agents
  • Hydrolases
  • Protein-Arginine Deiminases