Unsymmetrically substituted imidazolium salts: synthesis, characterization and antimicrobial activity

ABSTRACT Unsymmetrically substituted imidazolium salts were synthesized and characterized using 1H-NMR and 13C-NMR. The antimicrobial activities of the salts were evaluated using the agar-well diffusion method against 14 bacteria and five yeasts. The minimal inhibitory concentrations (MIC) against seven bacteria and one yeast were also determined. Among the test compounds applied, 1, 2, 3, 6 and 11 showed activities against Micrococcus luteus ATCC 9341, Staphylococcus aureus ATCC 25923, Staphylococcus epidermidis ATCC 12228, Bacilllus cereus ATCC 11778, Bacillus subtilis ATCC 6633, Bacillus thuringiensis, Listeria monocytogenes ATCC 19112 and Candida trophicalis. However, compounds 1, 2 and 3 showed the highest antimicrobial activities against Micrococcus luteus ATCC 9341, Stapylococcus aureus ATCC 25923, Staphylococcus epidermidis ATCC 12228, Bacilllus cereus ATCC 11778 and Bacillus subtilis ATCC 6633 with inhibition zones of 14-20 mm. In addition, compound 6 have only demonstrated activities against Candida trophicalis while compounds 4, 5, 7, 8, 9, 10, 12, 13 and 14 had no effect on test microorganisms.

Angiotensin II receptor blocker attenuates overexpression of vascular endothelial growth factor in diabetic podocytes

VEGF expressed in glomerular podocytes, is known to increase vascular permeability to macromolecules. Angiotensin II can stimulate the release of VEGF, and the protective effects of angiotensin II antagonist against diabetic glomerular injury suggest that the angiotensin II-induced VEGF is an important pathogenetic mechanism in the development of proteinuria during diabetic nephropathy although this mechanism is not fully understood. In this study, the changes of VEGF expression was examined in the experimental diabetic nephropathy to determine whether these changes were modified by renoprotective intervention by blockers of angiotensin II receptors. The streptozotocin- induced diabetic rats were treated with L-158,809, a blocker of angiotensin II receptors, for 12 weeks. Age-matched rats with L-158,809 served as controls. RT-PCR and immunohistochemistry were used to assess and quantify gene and protein expression of VEGF. A progressive increase in urinary protein excretion was observed in diabetic rats. Glomerular VEGF expression was significantly higher in diabetic rats than in the control groups, with a significant reduction in glomerular VEGF expression and proteinuria in L-158,809- treated diabetic rats. VEGF mRNA was also significantly higher in diabetic kidneys than in the control groups, with a significant reduction in VEGF mRNA in L-158,809-treated diabetic kidneys. These results demonstrates that VEGF expression is significantly increased in diabetic podocytes, and angiotensin II receptor antagonist attenuated these changes in VEGF expression and prevented the development of proteinuria in vivo. Attenuation of increased VEGF expression in podocytes could contribute to the renoprotective effects of angiotensin II receptor antagonists in diabetic nephropathy.

Efecto de la restricción alimentaria sobre el metabolismo del antichagásico benznidazol y enzimas relacionadas / Effect of food restriction on the metabolism of the antichagasic benznidazole and related enzymes

Se estudió el efecto de la restricción alimentaria al 50 por ciento sobre enzimas que participan en el metabolismo reductivo del antichagásico benznidazol. Ratas machos recién destetadas fueron sometidas a restricción dietaria al 50 por ciento, durante 28 días, sacrificadas y medida la actividad nitrorreductásica in vitro, de enzimas microsomales hepáticas sobre benznidazol. La actividad nitrorreductásica sobre benznidazol fue significativamente menor en los animales con dieta restringida que en aquellos alimentados ad libitum

Seguimiento post-terapia de pacientes con Paracoccidioidomicosis tratados con Itraconazol / Following post-therapy of patients with Paracoccidiodomycosis treatment with Itraconazol

Se hizo un seguimiento post-terapia de 11 pacientes con paracoccidioidomicosis tratados con Itraconazol; todos ellos fueron evaluados por 12 meses y 4 por periodos mayores (24-48 meses). Durante el tiempo de observacion ninguno de los pacientes recayo ni ocurrieron muertes como consecuencia de la micosis. La evolucion clinica y radiologica fue satisfactoria, persistiendo en la post-terapia solo aquellas manifestaciones debidas a procesos cicatriciales (disnea, fibrosis). En general las pruebas serologicas mostraron reduccion en los titulos de anticuerpos, en comparacion con los resultados iniciales. Los hallazgos anteriores sugieren que el Itraconazol constituye un adecuado tratamiento para la paracoccidioidomicosis

Trypsin and chymotryosin inhinitor of Vigna unguiculata seeds - involvement of tyrosyls in its interaction with proteases

When trypsin and chymotrypsin inhibitor of Vigna unguiculata seeds (black-eyed pea trypsin and chymotrypsin inhibitor, BTCI) combines with ß-trysin, 4.0, 1.5, 5.0, 5.8, and 6.6 tyrosyl residues are shield from reaction with N-acetylimidazole, at reagent/protein molar ratios of 60, 120, 200, 350 and 500, respectively. This may result from the presence of tyrosyl residues in the zone of contact between enzyme and inhibitor. In the interaction of BTCI and alpha-chymotrypsin, only 0.6 tyrosyl residues are shielded from the reaction with N-acetylimidazole, at a 500-fold reagent molar excess