Vistusertib improves pulmonary inflammation and fibrosis by modulating inflammatory/oxidative stress mediators via suppressing the mTOR signalling

Inflamm Res. 2024 Jul;73(7):1223-1237. doi: 10.1007/s00011-024-01894-5. Epub 2024 May 24.

Abstract

Introduction: Inflammation and oxidative stress are key factors in the development of pulmonary fibrosis (PF) by promoting the differentiation of fibroblasts through modulating various pathways including Wnt/β-catenin, TGF-β and mTOR signalling.

Objective and methods: This study aimed to evaluate the effects and elucidate the mechanisms of vistusertib (VSB) in treating pulmonary inflammation/fibrosis, specifically by targeting the mTOR pathway using various in vitro and in vivo models.

Results: Lipopolysaccharide (LPS)-induced inflammation model in macrophages (RAW 264.7), epithelial (BEAS-2B) and endothelial (HMVEC-L) cells revealed that treatment with VSB significantly reduced the IL-6, TNF-α, CCL2, and CCL7 expression. TGF-β induced differentiation was also significantly reduced upon VSB treatment in fibrotic cells (LL29 and DHLF). Further, bleomycin-induced inflammation and fibrosis models demonstrated that treatment with VSB significantly ameliorated the severe inflammation, and lung architectural distortion, by reducing the inflammatory markers expression/levels, inflammatory cells and oxidative stress indicators. Further, fibrosis model results exhibited that, VSB treatment significantly reduced the α-SMA, collagen and TGF-β expressions, improved the lung architecture and restored lung functions.

Conclusion: Overall, this study uncovers the anti-inflammatory/anti-fibrotic effects of VSB by modulating the mTOR activation. Although VSB was tested for lung fibrosis, it can be tested for other fibrotic disorders to improve the patient's survival and quality of life.

Keywords: Collagen deposition; Lung fibroblast; Lung inflammatory cells; mTOR inhibitor.

MeSH terms

  • Animals
  • Anti-Inflammatory Agents / pharmacology
  • Anti-Inflammatory Agents / therapeutic use
  • Bleomycin*
  • Cell Line
  • Cytokines / metabolism
  • Humans
  • Lipopolysaccharides
  • Lung* / drug effects
  • Lung* / metabolism
  • Lung* / pathology
  • Male
  • Mice
  • Mice, Inbred C57BL
  • Oxidative Stress* / drug effects
  • Pneumonia* / chemically induced
  • Pneumonia* / drug therapy
  • Pneumonia* / metabolism
  • Pneumonia* / pathology
  • Pulmonary Fibrosis* / chemically induced
  • Pulmonary Fibrosis* / drug therapy
  • Pulmonary Fibrosis* / metabolism
  • RAW 264.7 Cells
  • Signal Transduction* / drug effects
  • TOR Serine-Threonine Kinases* / metabolism

Substances

  • TOR Serine-Threonine Kinases
  • Bleomycin
  • Lipopolysaccharides
  • Cytokines
  • Anti-Inflammatory Agents
  • mTOR protein, mouse