The 2-arylpropionic acid derivatives or "profens" are an important group of non-steroidal anti-inflammatory drugs (NSAIDs) that have been used for the symptomatic treatment of various forms of arthritis. These compounds are chiral and the majority of them are still marketed as racemate although it is know that the S form is the principal effective in the COX inhibition. However, recent findings suggest that certain pharmacological effect of 2-arylpropionic acids cannot be attributed exclusively to the S (+) enantiomer. To obtain further insights into the pharmacological effect of profen, the present study investigated the influence of racemic and pure enantiomers, of flurbiprofen on the production of nitric oxide (NO) and glycosaminoglycans (GAGs), key molecules involved in cartilage destruction. The culture of human articular cartilage stimulated by interleukin -betaznnwich play an important role in the degradatation of cartilage, has been established, as a profit experimental model, for reproducing the mechanisms involved in the pathophysiology of arthritic diseases. Our results show that mainly S (+) flurbiprofen decrease, at therapeutic concentrations, the IL-1-beta induced cartilage destruction.
Different in vitro activity of flurbiprofen and its enantiomers on human articular cartilage
NICOLOSI G
2003
Abstract
The 2-arylpropionic acid derivatives or "profens" are an important group of non-steroidal anti-inflammatory drugs (NSAIDs) that have been used for the symptomatic treatment of various forms of arthritis. These compounds are chiral and the majority of them are still marketed as racemate although it is know that the S form is the principal effective in the COX inhibition. However, recent findings suggest that certain pharmacological effect of 2-arylpropionic acids cannot be attributed exclusively to the S (+) enantiomer. To obtain further insights into the pharmacological effect of profen, the present study investigated the influence of racemic and pure enantiomers, of flurbiprofen on the production of nitric oxide (NO) and glycosaminoglycans (GAGs), key molecules involved in cartilage destruction. The culture of human articular cartilage stimulated by interleukin -betaznnwich play an important role in the degradatation of cartilage, has been established, as a profit experimental model, for reproducing the mechanisms involved in the pathophysiology of arthritic diseases. Our results show that mainly S (+) flurbiprofen decrease, at therapeutic concentrations, the IL-1-beta induced cartilage destruction.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
