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Sci China B ; 36(10): 1216-23, 1993 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-8136034

RESUMO

Making use of the fact that the combination of a drug substance with DNA may inhibit the duplication, synthesis and proliferation of DNA and the consistency of the in vivo and in vitro interactions, the authors worked out a preliminary screening method for testing complex agents as potential antitumor drugs using ethidium bromide as a fluorescence probe. In this report, the method was applied for in vitro testing fourteen synthesized palladium(II)/phenanthroline/amino acid/chloride complexes as potential non-platinum antitumor agents. The fluorimetric screening method was compared with methylene blue tube test and trypan blue dye exclusion assay. All three methods gave agreeable results. Among the complexes tested, [Pd(phen)(lys)]Cl, [Pd(phen)(arg)]Cl and [Pd(phen)(pro)]Cl showed antineoplastic ratios for animal tumor S-180 56%, 50% and 48%, respectively, in accordance with the order of their binding constants with DNA, 7.96 x 10(6), 4.52 x 10(6) and 1.0 x 10(6), respectively. The test results show that fluorimetric method is simple, cheap and rapid, suitable for preliminary screening of antitumor complexes.


Assuntos
Antineoplásicos/farmacologia , Compostos Organometálicos/farmacologia , Paládio/farmacologia , Animais , Antineoplásicos/uso terapêutico , Ensaios de Seleção de Medicamentos Antitumorais , Feminino , Masculino , Camundongos , Transplante de Neoplasias , Compostos Organometálicos/uso terapêutico , Paládio/uso terapêutico , Sarcoma 180/tratamento farmacológico
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