Gypenoside inhibits interleukin-1β-induced inflammatory response in human osteoarthritis chondrocytes

J Biochem Mol Toxicol. 2017 Sep;31(9). doi: 10.1002/jbt.21926. Epub 2017 Apr 19.


Gypenoside (GP), the main active ingredient of Gynostemma pentaphyllum, possesses a variety of pharmacological capacities including anti-inflammation, anti-oxidation, and anti-tumor. However, the effects of GP on IL-1β-stimulated human osteoarthritis (OA) chondrocytes are still unknown. Therefore, this study aimed to investigate the anti-inflammatory effects of GP on IL-1β-stimulated human OA chondrocytes and explore the possible mechanism. Our results showed that GP dose-dependently inhibited IL-1β-induced NO and PGE2 production in human OA chondrocytes. In addition, treatment of GP inhibited the expression of MMP3 and MMP13, which was increased by IL-1β. Finally, we found that pretreatment of GP obviously suppressed NF-κB activation in IL-1β-stimulated human OA chondrocytes. Taken together, the results demonstrated that GP has chondro-protective effects, at least in part, through inhibiting the activation of NF-κB signaling pathway in human OA chondrocytes. Thus, these findings suggest that GP may be considered as an alternative therapeutic agent for the management of OA patients.

Keywords: NF-κB signaling pathway; gypenoside (GP) (OA); inflammation; osteoarthritis.

MeSH terms

  • Aged
  • Cells, Cultured
  • Chondrocytes / metabolism*
  • Chondrocytes / pathology
  • Female
  • Gynostemma
  • Humans
  • Inflammation / metabolism
  • Inflammation / pathology
  • Interleukin-1beta / metabolism*
  • Male
  • Matrix Metalloproteinase 13 / biosynthesis
  • Matrix Metalloproteinase 3 / biosynthesis
  • Middle Aged
  • NF-kappa B / metabolism
  • Osteoarthritis / metabolism*
  • Osteoarthritis / pathology
  • Plant Extracts / pharmacology
  • Signal Transduction / drug effects*


  • IL1B protein, human
  • Interleukin-1beta
  • NF-kappa B
  • Plant Extracts
  • gypenoside
  • MMP13 protein, human
  • Matrix Metalloproteinase 13
  • MMP3 protein, human
  • Matrix Metalloproteinase 3