Butein inhibited the IL-1β-induced inflammatory mediators in human osteoarthritis chondrocytes. Butein inhibited the IL-1β-induced degradation of type II collagen and SOX-9 in human osteoarthritis chondrocytes. Butein inhibited the IL-1β-induced IκB-α degradation, NF-kB p65 activation and NF-κB p65 nuclear translocation in human osteoarthritis chondrocytes. Butein attenuated the arthritis in mice osteoarthritis models.