Please use this identifier to cite or link to this item: https://www.arca.fiocruz.br/handle/icict/14517
Title: Norfloxacin and N-Donor Mixed-Ligand Copper(II) Complexes: Synthesis, Albumin Interaction, and Anti-Trypanosoma cruzi Activity
Authors: Martins, Darliane A.
Gouvea, Ligiane R.
Muniz, Gabriel S. Vignoli
Louro, Sonia R.W.
Batista, Denise da Gama Jaen
Soeiro, Maria de Nazaré C.
Teixeira, Letícia R.
Affilliation: Universidade Federal de Minas Gerais. Departamento de Química. Belo Horizonte, MG, Brasil.
Universidade Federal de Minas Gerais. Departamento de Química. Belo Horizonte, MG, Brasil.
Pontifíıcia Universidade Católica do Rio de Janeiro. Departamento de Física. Rio de Janeiro, RJ, Brasil.
Pontifíıcia Universidade Católica do Rio de Janeiro. Departamento de Física. Rio de Janeiro, RJ, Brasil.
Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ, Brasil
Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ, Brasil
Universidade Federal de Minas Gerais. Departamento de Química. Belo Horizonte, MG, Brasil.
Abstract: Copper(II) complexes with the first-generation quinolone antibacterial agent norfloxacin containing a nitrogen donor heterocyclic ligand 2,2󸀠-bipyridine (bipy) or 1,10-phenanthroline (phen)were prepared and characterized by IR, EPR spectra,molar conductivity, and elemental analyses.The experimental data suggest that norfloxacin was coordinated to copper(II) through the carboxylato and ketone oxygen atoms. The interaction of the copper(II) complexes with bovine serum albumin (BSA) and human serum albumin (HSA) was investigated using fluorescence quenching of the tryptophan residues and copper(II) EPR spectroscopy. The results of fluorescence titration revealed that copper(II) complexes have a moderate ability to quench the intrinsic fluorescence of the albumins through a static quenching mechanism. EPR experiments showed that BSA and HSA Cu(II) sites compete with NOR for Cu(II)-bipy and Cu(II)-phen to form protein mixed-ligand complexes. Copper(II) complexes, together with the corresponding ligands, were evaluated for their trypanocidal activity in vitro against Trypanosoma cruzi, the causative agent of Chagas disease. The tests performed using bloodstream trypomastigotes showed that the Cu(II)-N-donor precursors and the metal complexes were more active than the free fluoroquinolone.
Keywords: Chagas disease
Trypanosoma cruzi protozoa
Norfloxacin
Anti-Trypanosoma cruzi Activity
keywords: Norfloxacino
Doença de Chagas
Trypanosoma cruzi
Albuminas
Issue Date: 2016
Publisher: Hindawi Publishing Corporation
Citation: MARTINS, Darliane A. et al. Norfloxacin and N-Donor Mixed-Ligand Copper(II) Complexes: Synthesis, Albumin Interaction, and Anti-Trypanosoma cruzi Activity. Bioinorganic Chemistry and Applications, v.2016, Article ID5027404, 11p, 2016.
DOI: 10.1155/2016/5027404
Copyright: open access
Appears in Collections:IOC - Artigos de Periódicos

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