Joint-protective effects of compound K, a major ginsenoside metabolite, in rheumatoid arthritis: in vitro evidence

Rheumatol Int. 2013 Aug;33(8):1981-90. doi: 10.1007/s00296-013-2664-9. Epub 2013 Jan 31.

Abstract

Regulatory expression of matrix metalloproteinases (MMPs) and osteoclastogenesis is implicated in the process of joint destruction in rheumatoid arthritis (RA). Although several reports suggested the anti-arthritic effects of ginseng saponins, it has not been investigated whether the most absorbable ginsenoside, compound K (CK), has a joint-protective action. We here investigated the effect of CK (0-5 μM) on TNF-α-induced MMP-1, MMP-3, and MMP-13 and TIMP-1 production from RA fibroblast-like synoviocytes (FLS) and determined the inhibitory effect of CK on osteoclastogenesis from RAW264.7 cells co-cultured with RA-FLS and from human CD14+ monocytes. The effect of CK on NF-κB, nuclear factor of activated T cells c1 (NFATc1), and mitogen-activated protein kinases pathways were evaluated using immunoblotting or specific inhibitors. CK significantly inhibited MMP-1 and MMP-3 productions from RA-FLS in a concentration-dependent manner through suppressing the JNK and ERK pathways. In the co-culture system of TNF-α-stimulated RA-FLS and RAW264.7 cells, CK dose-dependently reduced receptor activator of NF-κB ligand (RANKL) expression in the RA-FLS and inhibited the formation of tartrate-resistant acid phosphatase (TRAP)-positive osteoclast-like cells. Furthermore, CK significantly inhibited soluble RANKL-induced osteoclastogenesis or osteoclast activity in RAW264.7 cells and human CD14+ monocytes through inhibition of RANKL-induced IκBα degradation and NFATc1 expression. In conclusion, our results increase the understanding of the molecular mechanisms of the joint-protective effects of CK in RA. The characteristic actions of CK provide in vitro evidence for its potential utility in RA therapy.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Arthritis, Rheumatoid / drug therapy*
  • Arthritis, Rheumatoid / metabolism
  • Arthritis, Rheumatoid / pathology
  • Female
  • Ginsenosides / pharmacology*
  • Ginsenosides / therapeutic use
  • Humans
  • Male
  • Matrix Metalloproteinases / metabolism
  • Synovial Membrane / drug effects*
  • Synovial Membrane / metabolism
  • Synovial Membrane / pathology
  • Tissue Inhibitor of Metalloproteinase-1 / metabolism
  • Tumor Necrosis Factor-alpha / pharmacology

Substances

  • Ginsenosides
  • Tissue Inhibitor of Metalloproteinase-1
  • Tumor Necrosis Factor-alpha
  • ginsenoside M1
  • Matrix Metalloproteinases