Objective. Osteoarthritis (OA) and Rheumatoid Arthritis (RA), however different in pathophysiology, share the degradative process. In the aim to develop new drugs with selective inhibiting action towards the enzymes responsible for the extracellular matrix damage, scientific research is focused on two main branches: 1) development of new drugs with specific inhibiting action towards MMPs; 2) study of the pharmacologic profile of drugs, currently used during therapy of rheumatic diseases, in order to identify a possible inhibiting action towards the degradative enzymes. Methods. The interaction between Indomethacin or Meloxicam and collagenase activity from human synovial fluids was studied by using a fluorogenic substrate. Results. In experimental conditions Indomethacin did not show any activity against collagenase activity, when used at the therapeutical plasmatic or synovial fluid concentrations. On the other hand, Meloxicam caused a 53% reduction of collagenase activity. Conclusions. According to our studies, NSAIDs could downregulate the activity of enzymes responsible for the degradation of the extracellular matrix.

L'inibizione delle metalloproteasi quale possibile nuovo approccio per il trattamento delle malattie reumatiche

BARRACCHINI, ANNALISA;PANTALEONI, Giancarlo;AMICOSANTE, Gianfranco;
2000-01-01

Abstract

Objective. Osteoarthritis (OA) and Rheumatoid Arthritis (RA), however different in pathophysiology, share the degradative process. In the aim to develop new drugs with selective inhibiting action towards the enzymes responsible for the extracellular matrix damage, scientific research is focused on two main branches: 1) development of new drugs with specific inhibiting action towards MMPs; 2) study of the pharmacologic profile of drugs, currently used during therapy of rheumatic diseases, in order to identify a possible inhibiting action towards the degradative enzymes. Methods. The interaction between Indomethacin or Meloxicam and collagenase activity from human synovial fluids was studied by using a fluorogenic substrate. Results. In experimental conditions Indomethacin did not show any activity against collagenase activity, when used at the therapeutical plasmatic or synovial fluid concentrations. On the other hand, Meloxicam caused a 53% reduction of collagenase activity. Conclusions. According to our studies, NSAIDs could downregulate the activity of enzymes responsible for the degradation of the extracellular matrix.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11697/103090
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