Farmaci antiflogistici steroidei

does not catalyze the reverse reaction . the conversion of XMP to IMP. Unlike other bacteria, M. tuberculosis harbors three IMPDH-like genes, designated as Mt-guaB1, Mt-guaB2 and Mt-guaB3 respectively. Of the three putative IMPDH’s, we previously confirmed that Mt-GuaB2 was the only functional ortholog by characterizing the enzyme kinetically. Using an in silico approach based on designed scaffolds, a series of novel classes of inhibitors was identified. The inhibitors possess good activity against M. tuberculosis with MIC values in the range of to mg mL21 . Among the identified ligands, two inhibitors have nanomolar Ki s against the Mt-GuaB2 enzyme.

8 LA MEDICINA BIOLOGICA OTTOBRE - DICEMBRE 3 TAB. 6 Audiometria dopo 9 giorni. FIG. 7 Rappresentazione grafica di Tab. 6. VALUTAZIONE DELLA FUNZIONE UDITIVA AUDIOMETRIA DOPO 9 GIORNI nessun miglioramento del deficit uditivo 9 (11,1%) 8 (,5%) miglioramento >% della funzione uditiva 48 (59,3%) 24 (29,6%) 47 (61,8%) 21 (27,7%) 9 8 nessun miglioramento del deficit uditivo miglioramento > % della funzione uditiva TAB. 7 Audiometria dopo 18 giorni. FIG. 8 Rappresentazione grafica di Tab. 7. VALUTAZIONE DELLA FUNZIONE UDITIVA AUDIOMETRIA DOPO 18 GIORNI nessun miglioramento del deficit uditivo miglioramento >% della funzione uditiva 6 (7,4%) 45 (55,5%) (37,1%) 12 (15,8%) 61 (8,3%) 3 (3,9%) nessun miglioramento del deficit uditivo miglioramento > % della funzione uditiva 3 TAB. 8 Timpanometria dopo 9 giorni. FIG. 9 Rappresentazione grafica di Tab. 8. VALUTAZIONE DELLA FUNZIONE UDITIVA TIMPANOMETRIA DOPO 9 GIORNI nessun miglioramento del deficit uditivo 7 (8,6%) 5 (6,6%) miglioramento >% della funzione uditiva 49 (6,5%) 25 (,9%) 48 (63,1%) 23 (,3%) 7 5 nessun miglioramento del deficit uditivo miglioramento > % della funzione uditiva TAB. 9 Timpanometria dopo 18 giorni. FIG. Rappresentazione grafica di Tab. 9. VALUTAZIONE DELLA FUNZIONE UDITIVA TIMPANOMETRIA DOPO 18 GIORNI nessun miglioramento del deficit uditivo miglioramento >% della funzione uditiva 5 (6,2%) 44 (54,3%) 32 (39,5%) (13,1%) 62 (81,6%) 4 (5,3%) nessun miglioramento del deficit uditivo miglioramento > % della funzione uditiva

A panel of non-steroidal anti-inflammatory drugs commonly used for therapeutic purposes was assessed for their effects on the respiratory burst of isolated human polymorphonuclear neutrophils. Cells were stimulated with opsonised yeast and the production of reactive oxygen species was measured by amplified chemiluminescence with luminol and lucigenin which are two luminogenic agents measuring different cellular events. A special attention was devoted to the establishment of dose–effect curves and calculation of ED 50 . Some of the drugs tested (acemetacine, diclofenac, flufenamic acid and niflumic acid) were able to decrease both luminol and lucigenin chemiluminescence in a dose-dependent manner reflecting an inhibitory effect on the respiratory burst. The most potent derivative was flufenamic acid (ED 50 8 and 78 μ M, respectively, with luminol and lucigenin), followed by diclofenac (21 and 98 μ M), niflumic acid (97 and 227 μ M) and acemetacine (585 and 427 μ M). In contrast, several other drugs (flurbiprofen, ibuprofen, ketoprofen, piroxicam) stimulated both luminol and lucigenin chemiluminescence, suggesting a pro-oxidant activity. Acetylsalicylic acid (up to 1250 μ M) was a modest inhibitor (maximum 25% inhibition) showing no dose-dependant effect and tolmetin (up to 125 μ M) had no significant effect in both systems. The results were in agreement using both luminogenic agents, except for indomethacin, naproxen and tenoxicam which showed different kinds of effects. The unspecific and complex nature of the measurement systems used did not allow to give a complete mechanistic interpretation of the results, but the comparison with literature data gave some pertinent explanations for both anti- and pro-oxidant effects.

Farmaci antiflogistici steroidei

farmaci antiflogistici steroidei

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