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Mepacrine decreases lung leak in rats given interleukin-1 intratracheally

Y M Lee1, B M Hybertson, L S Terada

  • 1Webb-Waring Institute for Biomedical Research and the Department of Medicine at the University of Colorado Health Sciences Center, Denver, USA.

Insights

Phospholipase A2 (PLA2) metabolites contribute to acute lung injury. Inhibiting PLA2 with mepacrine reduced lung leak and neutrophil accumulation in rats, suggesting PLA2 plays a key role in pulmonary vascular injury.

Area of Science:

  • Pulmonary Medicine
  • Inflammation Research
  • Biochemistry

Background:

  • Acute lung injury involves neutrophil infiltration and vascular leakage.
  • Interleukin-1 (IL-1) is implicated in initiating inflammatory responses in the lungs.
  • Phospholipase A2 (PLA2) enzymes generate lipid mediators that can influence inflammation.

Purpose of the Study:

  • To investigate the role of phospholipase A2 (PLA2) metabolites in acute lung leak induced by IL-1.
  • To determine if inhibiting PLA2 activity can mitigate IL-1-induced pulmonary inflammation and vascular permeability in rats.

Main Methods:

  • Administered IL-1 intratracheally to rats to induce lung injury.
  • Used mepacrine, a PLA2 inhibitor, to assess its effects on lung inflammation.
  • Measured lung PLA2 activity, phospholipid content, vascular permeability (leak index), lung weight gain, and protein concentration in bronchoalveolar lavage fluid.
  • Assessed neutrophil accumulation and cytokine-induced neutrophil chemoattractant (CINC) levels.
  • Evaluated neutrophil adhesion to endothelial cells in vitro.

Main Results:

  • IL-1 administration significantly increased lung PLA2 activity, phospholipid content, lung leak, weight gain, and protein leakage.
  • Mepacrine treatment significantly reduced these IL-1-induced effects, including decreased PLA2 activity, leak, and weight gain.
  • Mepacrine also reduced neutrophil accumulation in the lungs but did not affect CINC levels.
  • In vitro, mepacrine inhibited the adhesion of neutrophils to IL-1-stimulated endothelial cells.

Conclusions:

  • PLA2 activity is a significant contributor to the acute neutrophil-dependent lung leak and vascular permeability induced by IL-1.
  • Inhibition of PLA2 by mepacrine effectively mitigates IL-1-induced pulmonary vascular injury and neutrophil retention.
  • These findings highlight PLA2 as a potential therapeutic target for managing acute lung inflammation and injury.

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