cGAS/STING pathway modulation in polyhexamethyleneguanidine phosphate-induced immune dysregulation and pulmonary fibrosis using human monocytic cells (THP-1) and male C57BL/6 mice

J Toxicol Environ Health A. 2025 Feb 16;88(4):162-174. doi: 10.1080/15287394.2024.2432020. Epub 2024 Nov 28.

Abstract

Polyhexamethyleneguanidine phosphate (PHMG), a widely used antimicrobial agent, has been implicated in humidifier disinfectant-associated lung injuries (HDLI). PHMG exposure suppressed interferon regulatory factor 3 (IRF3) activation and interferon-β (IFN-β) expression induced by a cGAS agonist or a STING agonist in human monocytic cells (THP-1), which are known to transition to alveolar macrophages during pulmonary fibrosis development. However, the mechanisms underlying PHMG-induced pulmonary toxicity in lung remain unclear. Thus, it was of interest to investigate the effects of PHMG on the innate immune system in male C57BL/6 mouse, focusing on the cyclic GMP-AMP synthase (cGAS)/stimulator of interferon genes (STING) pathway and potential role in pulmonary fibrosis. Intratracheal administration of PHMG (1 or 2 mg/kg) in mice resulted in lung fibrosis, as evidenced by H&E staining with Szapiel scoring, Masson's trichrome staining with Ashcroft scoring, and increased mRNA levels of TGF-β and collagen type I. Interestingly, lower dose of PHMG enhanced IFN-β production in the lungs, whereas higher dose decreased IFN-β levels, indicating a biphasic effect that initially promotes inflammation but ultimately impairs host defense mechanisms, leading to pulmonary fibrosis. Our findings demonstrate the critical role of the cGAS/STING pathway in PHMG-induced mouse lung injury and suggest that targeting this pathway might serve as a potential therapeutic strategy for treating pulmonary fibrosis.

Keywords: Biocide; cGAS/STING; disinfectant; immune dysregulation; pulmonary fibrosis; type I interferons.

MeSH terms

  • Animals
  • Guanidines* / pharmacology
  • Humans
  • Male
  • Membrane Proteins* / genetics
  • Membrane Proteins* / metabolism
  • Mice
  • Mice, Inbred C57BL*
  • Monocytes / drug effects
  • Nucleotidyltransferases* / metabolism
  • Pulmonary Fibrosis* / chemically induced
  • Signal Transduction / drug effects
  • THP-1 Cells

Substances

  • Nucleotidyltransferases
  • Membrane Proteins
  • Guanidines
  • polyhexamethyleneguanidine
  • Sting1 protein, mouse
  • STING1 protein, human
  • cGAS protein, human
  • cGAS protein, mouse