"In vitro" differences among (R) and (S) enantiomers of profens in their activities related to articular pathophysiology.

Abstract—An important group of non steroidal antinflammatory drugs (NSAIDs), which have beenused for the symptomatic treatment of various forms of arthritis, are the 2-arylpropionic acidderivatives, Fprofens_. By virtue of a chiral carbon atom on the propionic acid side chain, they existas enantiomeric pairs. Whereas the S (+) enantiomer could be represented as an effective, butunselective COX inhibitor, the R (j) enantiomer could be much less active in this respect. However,recent findings suggest that certain pharmacological effects of profens cannot be attributedexclusively to the S (+) enantiomer. To obtain further insights into the pharmacological effects ofprofens, this study investigated the influence of pure enantiomers (S), (R), and racemic flurbiprofenand ketoprofen on the production of NO, MMP-3, PGE2, ROS and GAGs, key molecules involvedin cartilage destruction. Our results show that (S) flurbiprofen and ketoprofen decrease, at 1- and10-mM concentrations, the interleukin-1b induced cartilage destruction.