||Nunes, Melise Silveira; Garzon, Litiérri Razia; Rampelotto, Roberta Filipini; Tizotti, Maísa Kräulich; Martini, Rosiéli; Locatelli, Aline; Barbosa, Marcelo; Hörner, Manfredo; Hörner, Rosmari.|
||Synthesis, characterization and biological activity of a gold(I) triazenide complex against chronic myeloid leukemia cells and biofilm producing microorganisms|
||Braz. J. Pharm. Sci. (Online);53(4):e00191, 2017. tab, graf, ilus.
||ABSTRACT The enhancement of anti-leukemia therapy and the treatment of infections caused by multidrug-resistant pathogens are major challenges in healthcare. Although a large arsenal of drugs is available, many of these become ineffective, and as a result, the discovery of new active substances occurs. Notably, triazenes (TZCs) have been consolidated as a promising class of compounds, characterized by significant biological activity, especially antiproliferative and antimicrobial properties. The aim of this study is the synthesis and characterization of a new triazenide complex of gold (I), as well as the in vitro assessment of its antiproliferative activity against the K562 cell line (Chronic Myeloid Leukemia), and antibacterial activity against bacterial isolates of biofilm-producing coagulase-negative staphylococci. The combination of TZC with gold metal tends to have a synergistic effect against all biofilm-producing isolates, with Minimum Inhibitory Concentration values (MIC) between 32 and 64 µg mL-1. It has also shown activity against K562 cell line, getting an IC50=4.96 µM. Imatinib mesylate (Glivec) was used as reference, with IC50=3.86 µM. To the best of our knowledge, this study represents the first report of the activity of a TZC complexed with gold ion in the oxidation state (I) against microorganisms that produce biofilm and K562 cells.|
Leucemia Mielogênica Crônica BCR-ABL Positiva/tratamento farmacológico
| Tipo de Publ:
||Técnicas In Vitro|
||BR40.1 - DBD - Divisão de Biblioteca e Documentacão do Conjunto das Químicas|