1,720,964 research outputs found
INTERAZIONE DELLO SHOCK ELETTRICO, DEL DIGIUNO E DELLA PERFUSIONE CON ENKEFALINE, CON L'ANALGESIA DA NAFTILORFINE CON ANELLO ETEROCICLICO (NAE)
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L’inibizione delle metalloproteasi: applicazioni terapeutiche nelle patologie reumatiche
No full textPurpose: Matrix metalloproteinases (MMPs) play an important role in the degradation of articular cartilage in several diseases, including osteorthritis and rheumatoid arthritis. Aiming at developing new drugs with selective inhibiting action against enzyme damaging the extracellular matrix, research is mainly directed towards the: 1) development of new drugs with specific inhibitory effect on MMPs; 2) better understanding of the pharmacologic profile of drugs already used in the treatment of rheumatic diseases, in order to identify those having an inhibiting action on degradative enzymes. Materials and Methods: The interaction between rifamycins and collagenase type XI were studied using a fluorogenic substrate MOCAc-Pro-Leu-Gly-Leu-A2pr(Dnp)-Ala-Arg-NH2. Results: In our experimental conditions rifamycins showed a marked inhibition capacity with a IC50 ranging from 13 to 20.7 μM. This inhibition was reversible after extensive dialysis. Conclusions: Our results indicate that the effects of rifamycins in rheumatoid arthritis may correlate to the inhibitory activity of these molecules on collagenase activity
Meloxicam and Indomethacin activity on human matrix metalloproteinases in synovial fluid
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MMPs activities and cytokine expression during nimesulide therapy in a patient affected by osteoarthritis
No full textBackground: We present the case of a man affected by generalized osteoarthritis (OA). Case Report: After 2-month therapy with nimesulide a significative reduction of the activity in synovial fluid (SF) was observed for matrix metalloproteinases (MMP-1 and MMP-3), and an increase of immunoregulatory cytokines (IL-4 and IL-10). Our results emphasize the role of MMPs in the pathogenesis of OA. Conclusion: We describe the first examination and correlation of the effects of an NSAID, nimesulide on SF MMPs and cytokines in OA. Further studies on effects of this, and other NSAIDs, on a broader variety of SF and synovial cytokines may help to predict long-term effects of NSAIDs on progression of OA
Nimesulide e Collagenasi: inibizione dell'attività enzimatica "in vitro"
No full textIrreparable degradation of the extracellular matrix is a hallmark of severe inflammatory arthritis. In view of the central role that collagenase plays both in normal and pathological catabolism of the extracellular matrix, it is of interest to carry out detailed kinetic studies on this enzyme in order to check the effect showed by some NSAIDs like nimesulide, sodium meclophenamate and acetaminophen. The interaction between NSAIDs and collagenase 'in vitro' was studied by using a fluorogenic substrate MOCAc- Pro-Leu-Gly-Leu-A2pr(Dnp)-Ala-Arg-NH 2. After cleavage of the probe by collagenase the increased fluorescence, due to the removal of the NH 2- terminal dinitrophenyl group, was monitored and related to the enzyme activity. The presence of nimesulide induced a marked inhibition of the enzyme activity with an IC 50 of 1,90 μM and a K(i) of 0,83 μM. These concentrations was lower of the effective level of the drug found in the synovial fluid of patients receiving normal therapeutical dosage. Conversely, in the same experimental conditions, sodium meclophenamate gave lower inhibitory activity than nimesulide, showing an IC 50 = 26,80 μM and K(i) = 21,80 μM and acetaminophen did not affected the enzyme at all. These results support the hypothesis that nimesulide 'in vivo' may exert its antiinflammatory activity also via the inhibition of collagen degradation
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