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Icariin Regulates Cellular Functions and Gene Expression of Osteoarthritis Patient-Derived Human Fibroblast-Like Synoviocytes

Int J Mol Sci. 2017 Dec 8;18(12):2656. doi: 10.3390/ijms18122656.

Abstract

Synovial inflammation plays an important role in the pathogenesis and progress of osteoarthritis (OA). There is an urgent need to find safe and effective drugs that can reduce the inflammation and regulate the pathogenesis of cytokines of the OA disease. Here, we investigated the effect of icariin, the major pharmacological active component of herb Epimedium on human osteoarthritis fibroblast-like synoviocytes (OA-FLSs). The OA-FLSs were isolated from patients with osteoarthritis and cultured in vitro with different concentrations of icariin. Then, cell viability, proliferation, and migration were investigated; MMP14, GRP78, and IL-1β gene expression levels were detected via qRT-PCR. Icariin showed low cytotoxicity to OA-FLSs at a concentration of under 10 μM and decreased the proliferation of the cells at concentrations of 1 and 10 μM. Icariin inhibited cell migration with concentrations ranging from 0.1 to 1 μM. Also, the expression of three cytokines for the pathogenesis of OA which include IL-1β, MMP14 and GRP78 was decreased by the various concentrations of icariin. These preliminary results imply that icariin might be an effective compound for the treatment of OA disease.

Keywords: GRP78; MMP14; OA–FLSs; anti-inflammation; icariin; osteoarthritis.

MeSH terms

  • Cell Movement / drug effects
  • Cell Proliferation / drug effects
  • Cell Survival / drug effects
  • Cells, Cultured
  • Endoplasmic Reticulum Chaperone BiP
  • Fibroblasts / drug effects
  • Flavonoids / administration & dosage
  • Gene Expression Regulation / drug effects
  • Heat-Shock Proteins / genetics*
  • Humans
  • Inflammation / drug therapy*
  • Inflammation / genetics
  • Inflammation / pathology
  • Interleukin-1beta / genetics*
  • Matrix Metalloproteinase 14 / genetics*
  • Osteoarthritis / drug therapy*
  • Osteoarthritis / genetics
  • Osteoarthritis / pathology
  • Synovial Membrane / drug effects
  • Synovial Membrane / pathology
  • Synoviocytes / drug effects
  • Synoviocytes / pathology

Substances

  • Endoplasmic Reticulum Chaperone BiP
  • Flavonoids
  • HSPA5 protein, human
  • Heat-Shock Proteins
  • Interleukin-1beta
  • MMP14 protein, human
  • Matrix Metalloproteinase 14
  • icariin