Roxatidine Attenuates Degradation of Extracellular Matrix

Biomed Pharmacother. 2017 Nov:95:1156-1160. doi: 10.1016/j.biopha.2017.08.130. Epub 2017 Sep 15.

Abstract

Degradation of extracellular matrix such as type II collagen and aggrecan induced by proinflammatory cytokines has been considered as an important hallmark of Osteoarthritis (OA). Roxatidine is a licensed specific competitive H (2) -receptor antagonist used for the treatment of gastric and duodenal ulcers. The pharmacological function of roxatidine on Osteoarthritis (OA) remains unknown. In the current study, we report that roxatidine attenuated TNF-α- induced degradation of type II collagen by suppressing the expression of MMP-3 and MMP-13 in human chondrosarcoma cell line SW1353 cells. In addition, roxatidine ameliorated TNF-α- induced reduction of aggrecan by inhibiting the expression of ADAMTS-4 and ADAMTS-5. Notably, results indicate that roxatidine ameliorated TNF-α- induced the phosphorylations of IKK, IκBα, and NF-κB p65 as well as nuclear translocation of NF-κB p65 and the transcriptional activity of NF-κB, suggesting that roxatidine abolished the activation of NF-κB signaling pathway. Our findings implicate that roxatidine might be considered as an anti-osteoarthritic agent.

Keywords: Aggrecan; B p65; NF-κ Osteoarthritis; Roxatidine; Type II collagen.

MeSH terms

  • ADAMTS Proteins / metabolism
  • Cell Line, Tumor
  • Collagen Type II / metabolism
  • Extracellular Matrix / drug effects
  • Extracellular Matrix / metabolism*
  • Humans
  • Matrix Metalloproteinase 13 / metabolism
  • Matrix Metalloproteinase 3 / metabolism
  • Nitric Oxide / metabolism
  • Nitric Oxide Synthase Type II / metabolism
  • Piperidines / chemistry
  • Piperidines / pharmacology*
  • Transcription Factor RelA / metabolism
  • Tumor Necrosis Factor-alpha / pharmacology

Substances

  • Collagen Type II
  • Piperidines
  • Transcription Factor RelA
  • Tumor Necrosis Factor-alpha
  • Nitric Oxide
  • Nitric Oxide Synthase Type II
  • ADAMTS Proteins
  • MMP13 protein, human
  • Matrix Metalloproteinase 13
  • MMP3 protein, human
  • Matrix Metalloproteinase 3
  • roxatidine acetate