Formoterol synergy with des-ciclesonide inhibits IL-4 expression in IgE/antigen-induced mast cells by inhibiting JNK activation

Eur J Pharmacol. 2015 Aug 15:761:161-7. doi: 10.1016/j.ejphar.2015.05.008. Epub 2015 May 19.

Abstract

Inhaled corticosteroid (ICS) therapy in combination with long-acting β-adrenergic agonists (LABA) is the most important treatment for allergic asthma, although the mechanism still remains unclear. However, mast cells play a central role in the pathogenesis of asthma. In this study, we explored the sole or synergetic effects of des-ciclesonide (ICS) and formoterol (LABA) on the cytokines IL-4 and IL-13 and on histamine release from mast cells (RBL-2H3 cells). We found that des-ciclesonide (0.1, 1 and 10nM) and formoterol (0.1, 1 and 10μM) alone attenuated DNP-BSA-induced IL-4 and IL-13 production, respectively, in a concentration-dependent manner in DNP-IgE-sensitized mast cells. Des-ciclesonide (0.2nM) and formoterol (1μM) alone also reduced histamine production. However, the combination of des-ciclesonide (0.2nM) and formoterol (1μM) had a synergistic inhibition effect on IL-4 mRNA expression and protein production but not IL-13 and histamine release. The JNK inhibitor SP600125 (10μM) inhibited antigen-induced mRNA expression and protein production of IL-4. Des-ciclesonide and formoterol alone inhibited the activation of JNK in a concentration-dependent manner, and the combination of des-ciclesonide (0.2nM) and formoterol (1μM) exhibited greater inhibition effect compared with des-ciclesonide (0.2nM) or formoterol (1μM) alone. Taken together, these synergistic effects on mast cells might provide the rationale for the development of the most recent ICS/LABA combination approved for asthma therapy.

Keywords: Ciclesonide; Combination; Formoterol; IL-4; Mast cells.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adrenal Cortex Hormones / pharmacology*
  • Adrenergic beta-2 Receptor Agonists / pharmacology*
  • Animals
  • Cell Line, Tumor
  • Dinitrophenols / immunology*
  • Dose-Response Relationship, Drug
  • Drug Synergism
  • Drug Therapy, Combination
  • Enzyme Activation
  • Formoterol Fumarate / pharmacology*
  • Gene Expression Regulation
  • Histamine Release / drug effects
  • Immunoglobulin E / immunology*
  • Interleukin-13 / metabolism
  • Interleukin-4 / genetics
  • Interleukin-4 / metabolism*
  • JNK Mitogen-Activated Protein Kinases / antagonists & inhibitors
  • JNK Mitogen-Activated Protein Kinases / metabolism*
  • Mast Cells / drug effects*
  • Mast Cells / enzymology
  • Mast Cells / immunology
  • Phosphorylation
  • Pregnenediones / pharmacology*
  • Protein Kinase Inhibitors / pharmacology
  • RNA, Messenger / metabolism
  • Rats
  • Serum Albumin, Bovine / immunology*
  • Signal Transduction / drug effects

Substances

  • Adrenal Cortex Hormones
  • Adrenergic beta-2 Receptor Agonists
  • Dinitrophenols
  • Interleukin-13
  • Pregnenediones
  • Protein Kinase Inhibitors
  • RNA, Messenger
  • dinitrophenyl-bovine serum albumin
  • Interleukin-4
  • Serum Albumin, Bovine
  • Immunoglobulin E
  • desisobutyrylciclesonide
  • JNK Mitogen-Activated Protein Kinases
  • Formoterol Fumarate