Intra-articular injection of rebamipide prevents articular cartilage degeneration in murine post-traumatic osteoarthritis models.

Rebamipide is a protective drug used for gastric mucosal injuries, and it also exerts protective effects for a variety of other tissues. In this study, murine post-traumatic (PT) osteoarthritis (OA) models and human OA chondrocytes were used to examine the effects of rebamipide on articular cartilage degeneration. Male BALB/c mice were used. The knee ligaments were transected in both knees. Mice were injected with rebamipide into the knee joint every week. Human chondrocytes were stimulated with IL-1β, then treated with or without rebamipide. The levels of mRNA expression of COL2A, IL-1β, TNFα, NF-κB, MMP3, MMP13, ADAMTS5, TIMP3, FGF2, and TGFβ were estimated using real-time PCR. Histological scores were significantly better in the rebamipide 1 mg/mL and 10 mg/mL groups than in the control group. Rebamipide up-regulated the mRNA expressions of COL2A, TIMP3, TGFβ, and FGF2 in chondrocytes and down-regulated IL-1β, TNFα, NF-κB, MMP3, MMP13, and ADAMTS5. Intra-articular injection of rebamipide prevents articular cartilage degeneration for 6 weeks in murine models of OA . Rebamipide down-regulates inflammatory cytokines and catabolic factors and up-regulates anabolic factors in human chondrocytes . Rebamipide could be an important treatment for prevention of articular cartilage degeneration.