Characterization of Quin-C1 for its anti-inflammatory property in a mouse model of bleomycin-induced lung injury

Acta Pharmacol Sin. 2011 May;32(5):601-10. doi: 10.1038/aps.2011.4. Epub 2011 Apr 18.

Abstract

Aim: To study the in vivo effects of Quin-C1, a highly specific agonist for formyl peptide receptor 2 (FPR2/ALX), in a mouse model of bleomycin (BLM)-induced lung injury.

Methods: Male ICR mice were injected intratracheally with BLM (d 0), and intraperitoneally with Quin-C1 (0.2 mg/d) or vehicle between d 1 and d 28, during which pulmonary inflammation was monitored. A similar regimen was carried out between d 5 and d 28 to differentiate anti-inflammatory from anti-fibrotic effects. During the treatment, leukocyte numbers in bronchoalveolar lavage fluid (BALF) were counted, and FPR2/ALX transcripts, tumor necrosis factor α (TNF-α), interleukin-1β (IL-1β), the mouse keratinocyte-derived chemokine (KC), transforming growth factor β1 (TGF-β1) and C-X-C motif chemokine 10 (CXCL10) expression levels in the lung tissue were also measured. Both hydroxyproline content and histological changes were examined on d 28 to assess the severity of lung fibrosis.

Results: BLM caused a significant increase in expression levels of all the selected cytokines and chemokines, as well as a thickening of the alveolar wall. Treatment with Quin-C1 significantly reduced the neutrophil and lymphocyte counts in BALF, diminished expression of TNF-α, IL-1β, KC, and TGF-β1, and decreased collagen deposition in lung tissue. The treatment also lowered the content of lung hydroxyproline. Quin-C1 did not ameliorate lung fibrosis when the treatment was started 5 d after the BLM challenge, suggesting that the protection may be attributed to its anti-inflammatory effects. Exposure to BLM or BLM plus Quin-C1 did not change the level of FPR2/ALX transcripts (mFpr1, mFpr2, and Lxa4r) in the lung tissue.

Conclusion: The results demonstrate an anti-inflammatory role for Quin-C1 in bleomycin-induced lung injury, which may be further explored for therapeutic applications.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Inflammatory Agents / pharmacology*
  • Benzamides / pharmacology*
  • Bleomycin / toxicity
  • Chemokines / drug effects
  • Chemokines / metabolism
  • Cytokines / drug effects
  • Cytokines / metabolism
  • Disease Models, Animal
  • Fibrosis
  • Inflammation / drug therapy*
  • Inflammation / physiopathology
  • Lung Injury / drug therapy*
  • Lung Injury / physiopathology
  • Male
  • Mice
  • Mice, Inbred ICR
  • Quinazolines / pharmacology*
  • Receptors, Formyl Peptide / agonists
  • Time Factors

Substances

  • 4-butoxy-N-(2-(4-methoxy-phenyl)-4-oxo-1,4-dihydro-2H-quinazolin-3-yl)-benzamide
  • Anti-Inflammatory Agents
  • Benzamides
  • Chemokines
  • Cytokines
  • Quinazolines
  • Receptors, Formyl Peptide
  • formyl peptide receptor 2, mouse
  • Bleomycin