SerpinA3N limits cartilage destruction in osteoarthritis by inhibiting macrophage-derived leucocyte elastase

Ann Rheum Dis. 2024 Nov 14;83(12):1781-1790. doi: 10.1136/ard-2024-225645.

Abstract

Objectives: Inflammatory mediators such as interleukin 6 (IL-6) are known to activate catabolic responses in chondrocytes during osteoarthritis (OA). This study aimed to investigate the role of a downstream target gene of IL-6, the serine protease inhibitor SerpinA3N, in the development of cartilage damage in OA.

Methods: RNA sequencing was performed in murine primary chondrocytes treated with IL-6, and identified target genes were confirmed in human and murine OA cartilage samples. Male cartilage-specific Serpina3n-deficient mice and control mice underwent meniscectomy (MNX) or sham surgery at 10 weeks of age. Intra-articular injections of SerpinA3N or sivelestat (an inhibitor of leucocyte elastase (LE), a substrate for SerpinA3N) were performed in wild-type mice after MNX. Joint damage was assessed 3-9 weeks after surgery by histology and micro-CT. The effect of sivelestat was assessed in cartilage explants exposed to macrophage-derived conditioned media.

Results: RNA sequencing revealed that SerpinA3N is a major target gene of IL-6 in chondrocytes. The expression of SerpinA3N is increased in OA cartilage. Conditional loss of SerpinA3N in chondrocytes aggravated OA in mice, while intra-articular injection of SerpinA3N limited joint damage. Chondrocytes did not produce serine proteases targeted by SerpinA3N. By contrast, macrophages produced LE on IL-6 stimulation. Sivelestat limited the cartilage catabolism induced by conditioned media derived from IL-6-stimulated macrophages. Additionally, an intra-articular injection of sivelestat is protected against OA in the MNX model.

Conclusions: SerpinA3N protects cartilage against catabolic factors produced by macrophages, including LE. SerpinA3N and LE represent new therapeutic targets to dampen cartilage damage in OA.

Keywords: Chondrocytes; Inflammation; Osteoarthritis.

MeSH terms

  • Acute-Phase Proteins
  • Animals
  • Cartilage, Articular* / drug effects
  • Cartilage, Articular* / metabolism
  • Cartilage, Articular* / pathology
  • Cells, Cultured
  • Chondrocytes* / drug effects
  • Chondrocytes* / metabolism
  • Chondrocytes* / pathology
  • Disease Models, Animal
  • Glycine / analogs & derivatives
  • Humans
  • Injections, Intra-Articular
  • Interleukin-6* / metabolism
  • Leukocyte Elastase / metabolism
  • Macrophages* / drug effects
  • Macrophages* / metabolism
  • Male
  • Meniscectomy
  • Mice
  • Mice, Knockout
  • Osteoarthritis / metabolism
  • Osteoarthritis / pathology
  • Osteoarthritis, Knee / metabolism
  • Osteoarthritis, Knee / pathology
  • Serpins / metabolism
  • Serpins / pharmacology
  • Sulfonamides / pharmacology

Substances

  • Interleukin-6
  • Serpina3n protein, mouse
  • Leukocyte Elastase
  • Serpins
  • sivelestat
  • Sulfonamides
  • Acute-Phase Proteins
  • Glycine