The anti-inflammatory effects of 1,6-anhydro-3,4-dideoxy-2-furfuryl-beta-D-threo-3-enopyranose (MT2221) were investigated using animal models and compared with the effects of dexamethasone (DEX) and cyclosporin A (CYA). MT2221 inhibited carrageenan-induced acute inflammation and adjuvant arthritis in rats, as well as the delayed-type hypersensitive response and collagen-induced arthritis (CIA) in mice. However, it seemed that this compound was more effective against murine CIA than upon the other inflammation models. The MT2221 mode of action differed from those of conventional non-steroidal anti-inflammatory drugs (NSAIDs) and disease modifying anti-rheumatic drugs (DMARDs). All of these drugs are effective against acute inflammation or adjuvant arthritis models, but not against murine CIA. DEX and CYA did inhibit murine CIA, but in other animal models, their mode of action differed from that of MT2221. Moreover, allograft transplantation in mice showed that MT2221 slightly prolonged the allograft survival time. These results suggest that MT2221 has not only anti-inflammatory but also immunosuppressive effects based upon a novel mechanism of action that is different from NSAIDs, DMARDs, DEX and CYA.