RESUMO
Water solutions of adriblastin, dactinomycin, rosevin, methotrexate, cisplatin, sarcolysine, rubomycin, cyclophosphamide, 5-fluorouracil or ftorafur were combined with dextran ferrite. The obtained compositions were injected i.p. to BDF1 mice 24 hours after they were inoculated with one million of murine P388 leukemic cells. Antitumor activity was fully retained for each of these agents in combination with dextran ferrite.
Assuntos
Antineoplásicos/administração & dosagem , Complexo Ferro-Dextran/administração & dosagem , Leucemia P388/tratamento farmacológico , Animais , Cisplatino/administração & dosagem , Ciclofosfamida/administração & dosagem , Dactinomicina/administração & dosagem , Daunorrubicina/administração & dosagem , Doxorrubicina/administração & dosagem , Combinação de Medicamentos , Fluoruracila/administração & dosagem , Melfalan/administração & dosagem , Metotrexato/administração & dosagem , Camundongos , Tegafur/administração & dosagemRESUMO
Derivatives of antitumour anthracycline antibiotics containing N-methylurea moiety in the carbohydrate ring were obtained by the interaction of methyl isocyanate with daunorubicin, doxorubicin, carminomycin and daunorubicin derivatives, substituted at C-13 or C-14 positions. N-Nitrosation of these compounds yielded modified anthracycline antibiotics containing the N-methyl-N-nitrosourea substituent at C-3' position. Alkaline degradation of these derivatives produced, through corresponding isocyanates cyclic 3'-N,4'-carbonylderivatives. In these anthracycline derivatives with sugar cycles conjugated with oxazoline-2-ones the predominant conformations of sugar ring has changed from 1C4 to 4C1, 2,5B, or B0,3 (shown by 1H NMR spectroscopy). It was demonstrated, both in vitro and in vivo, that introduction of methylurea or cytotoxic methylnitrosourea moieties does not potentiate antimicrobial, cytotoxic or antitumour properties of these compounds.
Assuntos
Antibióticos Antineoplásicos/síntese química , Daunorrubicina/síntese química , Leucemia P388/tratamento farmacológico , Leucemia Experimental/tratamento farmacológico , Metilnitrosoureia/síntese química , Compostos de Metilureia/síntese química , Animais , Divisão Celular/efeitos dos fármacos , Fenômenos Químicos , Química , Daunorrubicina/farmacologia , Masculino , Camundongos , Relação Estrutura-AtividadeRESUMO
Evidences on the antileukemic effect of L-lysine alpha-oxidase from Trichoderma sp. are presented. It is inferred that enzyme needs detail studying as a potential chemotherapeutic drug both in experimental and clinical research.