Transgenic rats carrying human c-Ha-ras proto-oncogene (Hras128 rats) have been shown to be highly susceptible to induction of tumors. We have found an early induction of tongue tumors in Hras128 rats treated with 4-nitroquinoline 1-oxide (4NQO). 4NQO was administered to the Hras128 and wild-type Sprague-Dawley (SD) rats for 4 and 8 weeks, respectively. The experiment was terminated at 14 (Hras...

The cyclooxygenase-2 (COX-2) isoenzyme is a key target for COX-2-selective non-steroidal anti-inflammatory drugs (NSAIDs). An important difference in binding of nimesulide compared with non-selective NSAIDs appears to involve the amino acid at position 523 of the enzyme. Replacement of valine with isoleucine at this position provides access to a binding site that is larger in COX-2 than in COX-...

Diet-induced changes in the lipid composition of mitochondrial membranes have been shown to influence physiological processes. However, the modulation effect of diet on mitochondrially-active drugs has not yet received the deserved attention. Our hypothesis is that modulation of membrane dynamics by diet impacts drug-effects on liver mitochondrial functioning. In a previous work, we have shown ...

Trypanosoma cruzi infection and nonsteroidal anti-inflammatory drugs inhibit colorectal carcinogenesis by mechanisms not completely known and metallothionein proteins (MTs) may be involved in this process. Sixty-six male Wistar rats weighing 90 to 120 g were randomly divided into seven groups (GI to GVII). GI, GII and GIII animals were subcutaneously infected with 200,000 trypomastigote forms o...

In this study, the anti-inflammatory activity of indomethacin, diclofenac, meloxicam and nimesulide were investigated on sunny and rainy days. Parallel to these experiments, the question of whether endogenous adrenaline and cortisol (corticosterone in rats) are factors that affect medicinal activity of these anti-inflammatory drugs on sunny and rainy days was examined. Our experimental results ...

Cyclooxygenase (COX) isoenzyme is known to play an important role in the pathophysiology of Parkinson's disease. The present study evaluated the neuroprotective effect of nimesulide, a preferential COX-2-inhibitor against 1-methyl-4-phenyl-1,2,3,6-tertahydropyridine (MPTP)-model of Parkinson's disease. Intrastriatal administration of MPTP (32 micromol in 2 microl) produced a significant decreas...

OBJECTIVE To determine the influence of allopurinol and nimesulide in the protection of the pancreas from acute ischemia-reperfusion (I/R) injury. MATERIALS AND METHODS A total of 30 rabbits were divided into 3 groups, group A: acute I/R only; group B: allopurinol (30 mg/kg) was administered intravenously 10 minutes before ischemia; group C: nimesulide (50 mg/kg) was given intraperitoneally 2...

The efficacy and safety of Nimulid (Nimesulide) and Diclofenac was evaluated in a double blind randomized diclofenac controlled trial in patients suffering from osteoarthritis of the knee joint. Out of 141 patients, 71 (42 mates, 29female) received Nimulid 100 mg. BD and 70 patients (40 male, 30 female) received Diclofenac 75 mg BD. There was no statistically significant difference in the age, ...

As a part of our ongoing effort to explore drug induced lipid peroxidation in relation to drug-induced toxicity, this study was undertaken to determine whether nonsteroidal anti-inflammatory drugs (NSAIDs), namely, diclofenac sodium, ibuprofen, flurbiprofen, paracetamol, nimesulide, celecoxib and indomethacin are involved in oxidative/antioxidative processes by determining malondialdehyde (MDA)...

Membrane viscosity is a key parameter in cell physiology, cell function, and cell signaling. The most common methods to measure changes in membrane viscosity are fluorescence recovery after photobleaching (FRAP) and fluorescence anisotropy. Recent interest in a group of viscosity sensitive fluorophores, termed molecular rotors, led to the development of the highly membrane-compatible (2-carboxy...