Synthesis, characterization and biological activity of a gold(I) triazenide complex against chronic myeloid leukemia cells and biofilm producing microorganisms

Autor: Melise Silveira Nunes, Litiérri Razia Garzon, Roberta Filipini Rampelotto, Maísa Kräulich Tizotti, Rosiéli Martini, Aline Locatelli, Marcelo Barbosa, Manfredo Hörner, Rosmari Hörner
Jazyk: angličtina
Rok vydání: 2018
Předmět:
Zdroj: Brazilian Journal of Pharmaceutical Sciences, Vol 53, Iss 4 (2018)
Druh dokumentu: article
ISSN: 2175-9790
DOI: 10.1590/s2175-97902017000400191
Popis: 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.
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