Published in:
01-12-2005
“In Vitro” Differences among (R) and (S) Enantiomers of Profens in their Activities Related to Articular Pathophysiology
Authors:
A. M. Panico, V. Cardile, B. Gentile, F. Garufi, S. Avondo, S. Ronsisvalle
Published in:
Inflammation
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Issue 4-6/2005
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Abstract
An important group of non steroidal antinflammatory drugs (NSAIDs), which have been used for the symptomatic treatment of various forms of arthritis, are the 2-arylpropionic acid derivatives, ‘profens’. By virtue of a chiral carbon atom on the propionic acid side chain, they exist as enantiomeric pairs. Whereas the S (+) enantiomer could be represented as an effective, but unselective COX inhibitor, the R (−) enantiomer could be much less active in this respect. However, recent findings suggest that certain pharmacological effects of profens cannot be attributed exclusively to the S (+) enantiomer. To obtain further insights into the pharmacological effects of profens, this study investigated the influence of pure enantiomers (S), (R), and racemic flurbiprofen and ketoprofen on the production of NO, MMP-3, PGE2, ROS and GAGs, key molecules involved in cartilage destruction. Our results show that (S) flurbiprofen and ketoprofen decrease, at 1- and 10-μM concentrations, the interleukin-1β induced cartilage destruction.