FK506, an immunosuppressor, was reported to have the ability to suppress catabolic responses in primary human chondrocytes. However, immunosuppressive function of FK506 limited its use in cartilage osteoarthritis treatment. The purpose of this study was to evaluate the ability of FK506’s isomer, GPI-1046 in protecting against cartilage degeneration.
1ng/ml IL-1β was added to the medium of SW1353 to conduct osteoarthritis model. For treatment group, 0, 1, 10, 100, 200, and 500mM GPI-1046 were added to the medium. 10ug/ml FK506 was used as positive control. Cell viability was conducted. 24 and 48 hours later, QPCR and western blot were conducted to evaluate the protective effect of GPI-1046.
Cell viability results showed that GPI-1046 had no obvious cytotoxicity. QPCR showed GPI-1046 up-regulated the expression of collagen type II and SOX 9, down-regulated the expression of MMP1, 3, 13. Western blot demonstrated that cartilage protection ability of GPI-1046 was even better than FK506.
GPI-1046 has the potential of protect against cartilage degeneration.