RESUMEN
Reactions of amphotericin B, a polyene macrolide antibiotic, with acyl perfluorides resulted in formation of its N-perfluoroacyl derivatives. Physicochemical and medicobiological properties of the derivatives were studied. The biological study revealed that the acute toxity (LD50) of the derivatives was 2 times as low as that of the starting antibiotic. The derivatives showed high antifungal activity against a great number of the test cultures.
Asunto(s)
Anfotericina B/análogos & derivados , Antibacterianos/farmacología , Fluorocarburos/farmacología , Anfotericina B/biosíntesis , Anfotericina B/farmacología , Antibacterianos/biosíntesis , Fenómenos Químicos , Química Física , Fluorocarburos/metabolismo , Dosificación Letal Mediana , Pruebas de Sensibilidad MicrobianaRESUMEN
Reactions of amphotericin B, a polyenic macrolide antibiotic, with aromatic aldehydes and H3PO2 resulted in formation of its new hydrophosphoryl derivatives. Physico-chemical and biological properties of the compounds were investigated. The biological studies showed that the hydrophosphoryl derivatives of amphotericin B were low toxic and had antifungal and antiviral activities.
Asunto(s)
Anfotericina B/análogos & derivados , Antibacterianos/síntesis química , Antifúngicos/síntesis química , Antivirales/síntesis química , Anfotericina B/síntesis química , Anfotericina B/farmacología , Animales , Antibacterianos/farmacología , Antibacterianos/toxicidad , Antifúngicos/farmacología , Antifúngicos/toxicidad , Antivirales/farmacología , Antivirales/toxicidad , Dosificación Letal Mediana , Masculino , Ratones , Pruebas de Sensibilidad Microbiana , Estructura Molecular , Fosforilación , Espectrofotometría , Relación Estructura-ActividadRESUMEN
A lung pneumocystosis model has been developed in white non-inbred rats (83 animals). The pathological process develops during 1 month versus 2-3 months in other models. Pathomorphology is in principle similar to human pneumocystosis. Bauer's method appeared to be the simplest and adequate for the detection of mature pneumocysts in the lung sections among many other methods used.
Asunto(s)
Pneumocystis/aislamiento & purificación , Neumonía por Pneumocystis/patología , Animales , Niño , Cortisona/efectos adversos , Modelos Animales de Enfermedad , Humanos , Pulmón/citología , Pulmón/microbiología , Masculino , RatasRESUMEN
Dehydrogenase activity of the tissue form cells of C. albicans during the infection process in albino mice with and without amphotericin B treatment was studied. The strength of the metabolic reactions resulting in accumulation of ATP was evident from the activity of 4 main enzymes, i.e. succinate dehydrogenase, lactate dehydrogenase, alcohol dehydrogenase and glucose-6-phosphate dehydrogenase. The enzymatic activity was determined by the tetrasol method based on formation of diphormazan. Investigation of the fungal cells 10 minutes after the infection showed that preliminary intravenous or intraperitoneal administration of amphotericin B did not change the activity of the tissue forms. The cytochemical characteristics of the fungal cells remained the same as that in the untreated animals. Six hours after infection of the animals treated with amphotericin B administered intravenously the fungus vegetation decreased from 52 to 38 per cent, while in the animals treated with amphotericin B administered intraperitoneally it was suppressed completely. Simultaneously the energy metabolism was also suppressed, the activity of alcohol dehydrogenase being suppressed most significantly. The activity of this enzyme in the cells of C. albicans isolated from the animals treated with the antibiotic administered intraperitoneally was 14 times lower than that in the cells of the culture isolated from the control animals.