5-Loxin is a compound extracted from an ancient herb that might be considered as a potent lipooxygenase inhibitor. The results observed in a preliminary trial suggest a highly intriguing clinically relevant symptomatic effect contrasting with a poor bioavailability of this compound. Moreover, in this trial, a statistically significant decrease in matrix metalloproteinase enzyme serum level suggests that, in addition to the observed symptomatic effect, such a compound might have a disease modifying effect in osteoarthritis. Further studies are required both to confirm the symptomatic efficacy and acceptable safety profile and to evaluate the potential chondromodulating effect of this compound.