Dissertação
Avaliação da atividade biológica de triazenos inéditos complexados com Au(I)
Fecha
2013-03-22Registro en:
KEMPFER, Cláudia Barbisan. EVALUATION OF BIOLOGICAL ACTIVITY OF UNPUBLISHED TRIAZENES COMPLEXED WITH Au (I). 2013. 86 f. Dissertação (Mestrado em Farmacologia) - Universidade Federal de Santa Maria, Santa Maria, 2013.
Autor
Kempfer, Cláudia Barbisan
Institución
Resumen
The Triazenes are compounds with proven antibacterial and cytotoxic activity.
Variations in the chemical structure such as complexation with metals like gold (I) can confer
different biological activities. The antineoplastic temozolomide and dacarbazine are examples
of commercially available triazenes used in the treatment of solid tumors and acute leukemias.
In this study, the following compounds were synthesized triazenes complexed with novel gold
(I): 1) [1,3-Bis (2-fluorophenyl) triazenido] (triphenylphosphine) gold (I); 2) [1,3-Bis (2-
chlorophenyl) triazenido] (triphenylphosphine) gold (I) 3) [1,3-Bis (2-bromophenyl)
triazenido] (triphenylphosphine) gold (I), 4) [1,3-Bis (2-iodophenyl) triazenido]
(triphenylphosphine ) gold (I). Cytotoxicity of these compounds was evaluated by the MTT
colorimetric assay of cell culture effecting bone marrow of patients with different types of
leukemia, in addition to controlling patient without the disease. For the analysis of the
antimicrobial activity was utilized quantitative methodology of microdilution with the
determination of minimum inhibitory concentration (MIC). To determine the activity of
nuclease cleavage assays were performed in double-stranded plasmid DNA using the method
of electrophoresis in agarose gel. The results showed a considerable activity against different
types of leukemia (acute myeloid leukemia, chronic myeloid leukemia, acute lymphoblastic
leukemia, chronic lymphocytic leukemia) with a small IC50 value of 0.0057 μmol mL-1 for
compound 4 in cells of acute myeloid leukemia, all the active compounds in different types of
leukemia but not so selective. The antibacterial activity was higher against gram-positive
bacteria mainly in different strains of Staphylococcus aureus (MIC value of equal to 16
ug/ml). Any of the four compounds analyzed in this study was able to cleave the plasmid
DNA. Thus, all tested triazenes have biological potential, or may be the subject of further
studies as alternatives to anticancer and antimicrobial drugs existent.