DJ-X-013 reduces LPS-induced inflammation, modulates Th17/ myeloid-derived suppressor cells, and alters NF-κB expression to ameliorate experimental colitis

Biomed Pharmacother. 2024 Oct:179:117379. doi: 10.1016/j.biopha.2024.117379. Epub 2024 Sep 9.

Abstract

Scope: Inflammatory bowel disease (IBD) is a chronic intestinal inflammatory condition of unknown etiology, although recent evidence suggests that it is caused by an excessive immune response to mucosal antigens. We determined the anti-inflammatory properties of novel compound DJ-X-013 in vitro in lipopolysaccharide (LPS)-induced macrophages and in an in vivo dextran sodium sulfate (DSS)-induced model of colitis.

Methods and results: To evaluate the anti-inflammatory properties of DJ-X-013, we used LPS-activated RAW 264.7 macrophages in vitro and a DSS-induced experimental model of colitis in vivo. We examine cellular morphology, and tissue architecture by histology, flow cytometry, RT-qPCR, multiplex, and immunoblot analysis to perform cellular and molecular studies. DJ-X-013 treatment altered cell morphology and expression of inflammatory cytokines in LPS-activated macrophages as compared to cells treated with LPS alone. DJ-X-013 also impeded the migration of RAW 264.7 macrophages by modulating cytoskeletal organization and suppressed the expression of NF-κB and inflammatory markers as compared to LPS alone. DJ-X-013 treatment improved body weight, and colon length and attenuated inflammation in the colon of DSS-induced colitis. Intriguingly, DSS-challenged mice treated with DJ-X-013 induced the numbers of myeloid-derived suppressor cells (MDSCs), dendritic cells (DCs), and natural killer T cells (NKT) in the colon lamina propria (LP) relative to DSS. DJ-X-013 also reduced the influx of neutrophils, TNF-α producing macrophages, restricted the number of Th17 cells, and suppressed inflammatory cytokines and NF-κB in the LP relative to DSS.

Conclusion: DJ-X-013 is proposed to be a therapeutic strategy for ameliorating inflammation and experimental colitis.

Keywords: Colitis; Cytoskeletal protein; Inflammation; MDSCs; Th17.

MeSH terms

  • Animals
  • Anti-Inflammatory Agents / pharmacology
  • Colitis* / chemically induced
  • Colitis* / drug therapy
  • Colitis* / immunology
  • Colitis* / pathology
  • Colon / drug effects
  • Colon / immunology
  • Colon / metabolism
  • Colon / pathology
  • Cytokines / metabolism
  • Dextran Sulfate*
  • Disease Models, Animal
  • Inflammation* / drug therapy
  • Inflammation* / pathology
  • Lipopolysaccharides*
  • Macrophages / drug effects
  • Macrophages / immunology
  • Macrophages / metabolism
  • Male
  • Mice
  • Mice, Inbred C57BL*
  • Myeloid-Derived Suppressor Cells* / drug effects
  • Myeloid-Derived Suppressor Cells* / immunology
  • Myeloid-Derived Suppressor Cells* / metabolism
  • NF-kappa B* / metabolism
  • RAW 264.7 Cells
  • Th17 Cells* / drug effects
  • Th17 Cells* / immunology
  • Th17 Cells* / metabolism

Substances

  • NF-kappa B
  • Lipopolysaccharides
  • Dextran Sulfate
  • Anti-Inflammatory Agents
  • Cytokines