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AIM: To study the effects of benznidazole (Bz), a drug used in the chemotherapy of the acute and the intermedi-ate phase of Chagas’ disease, on the colon of rats. METHODS: Sprague Dawley male rats received Bz 100 mg/kg ig. After 24 h colons were examined by electron microscopy. Concentrations of Bz in colonic tissue were measured by HPLC. Bz nitroreduction was followed by the decrease in the drug concentration using spectropho-tometry and HPLC or by covalent binding to proteins of reactive products formed under in vivo and in vitro con-ditions. RESULTS: Colon mucosa of Bz-treated rats showed intense ultrastructural alterations: abundant mucus secretion at the level of the Goblet cells and dilatation of the endoplasmic reticulum and the Golgi apparatus in ep-ithelial cells. The concentration of Bz in tissue was (59±18) and (93±14) nmol/g (protein) 1 and 3 h after o-ral administration to rats, respectively. Colonic micro-somes anaerobically activated Bz in the presence of NADPH. This activating nitrored
AIM: To study the effects of benznidazole (Bz), a drug used in the chemotherapy of the acute and the intermedia- ate phase of Chagas’ disease, on the colon of rats. METHODS: Sprague Dawley male rats received Bz 100 mg / kg After 24 h colons were examined by electron microscopy. Concentrations of Bz in colonic tissue were measured by HPLC. Bz nitroreduction was followed by the decrease in the drug concentration using spectropho-tometry and HPLC or by covalent binding to proteins of reactive products formed under vivo and in vitro con-ditions. RESULTS: Colon mucosa of Bz-treated rats showed intense ultrastructural alterations: abundant mucus secretion at the level of the Goblet cells and dilatation of the endoplasmic reticulum and the Golgi apparatus in ep-ithelial cells. The concentration of Bz in tissue was (59 ± 18) and (93 ± 14) nmol / g (protein) 1 and 3 h after o-ral administration to rats, respectively. Colonic micro-somes anaerobically activated Bz in presence of NADPH This a ctivating nitrored