| Author | Martins, Darliane A. | |
| Author | Gouvea, Ligiane R. | |
| Author | Batista, Denise da Gama Jean | |
| Author | Silva, Patrícia Bernardino da | |
| Author | Louro, Sonia R. W. | |
| Author | Soeiro, Maria de Nazaré C. | |
| Author | Teixeira, Letícia R. | |
| Access date | 2016-09-06T15:56:13Z | |
| Available date | 2016-09-06T15:56:13Z | |
| Document date | 2012 | |
| Citation | MARTINS, Darliane A. et al. Copper(II)–fluoroquinolone complexes with antiTrypanosoma cruzi activity and DNA binding ability. Biometals, v.25, n.5, p.951-960, Oct. 2012. | pt_BR |
| ISSN | 0966-0844 | pt_BR |
| URI | https://www.arca.fiocruz.br/handle/icict/15703 | |
| Language | eng | pt_BR |
| Publisher | Springer Verlag | pt_BR |
| Rights | restricted access | |
| Subject in Portuguese | Fluoroquinolones | pt_BR |
| Subject in Portuguese | Trypanosoma cruzi | pt_BR |
| Title | Copper(II)-fluoroquinolone complexes with anti-Trypanosoma cruzi activity and DNA binding ability | pt_BR |
| Type | Article | |
| DOI | 10.1007/s10534-012-9565-3 | |
| Abstract | Copper(II) complexes of fluoroquinolone antibacterial agents levofloxacin (LEV) and sparfloxacin (SPAR), containing or not a nitrogen donor heterocyclic ligand, 2,2'-bipyridine (bipy) or 1,10-phenathroline (phen), were prepared and characterized. The complexes are of the type [CuCl(2)(H(2)O)(L)], [CuCl(bipy)(L)]Cl and [CuCl(2)(phen)(L)], where L = LEV or SPAR. The data suggest that LEV and SPAR act as zwitterionic bidentade ligands coordinated to Cu(II) through the carboxylate and ketone oxygen atoms. The electron paramagnetic resonance spectra of the [CuCl(bipy)(L)]Cl and [CuCl(2)(phen)(L)] complexes (L = LEV and SPAR) in aqueous and DMSO solutions indicate mixture of mononuclear and binuclear forms. The Cu(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 assays performed against bloodstream trypomastigotes showed that all complexes were more active than their corresponding ligands. Complexes [CuCl(2)(phen)(LEV)] and [CuCl(2)(phen)(SPAR)] were revealed, among all studied compounds, to be the most active with IC(50) = 1.6 and 4.7 μM, respectively, both presenting a superior effect than benznidazole. The interactions of fluoroquinolones and their Cu(II) complexes with calf-thymus DNA were investigated. These compounds showed binding properties towards DNA, with moderated binding constants values, suggesting that this structure may represent a parasite target. | pt_BR |
| Affilliation | Universidade Federal de Minas Gerais. Departamento de Química. Belo Horizonte, MG, Brasil. | pt_BR |
| Affilliation | Universidade Federal de Minas Gerais. Departamento de Química. Belo Horizonte, MG, Brasil. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ, Brasil. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ, Brasil. | pt_BR |
| Affilliation | Pontifícia Universidade Católica do Rio de Janeiro. Departamento de Física. Rio de Janeiro, RJ, Brasil. | pt_BR |
| Affilliation | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Biologia Celular. Rio de Janeiro, RJ, Brasil. | pt_BR |
| Affilliation | Universidade Federal de Minas Gerais. Departamento de Química. Belo Horizonte, MG, Brasil. | pt_BR |
| Subject | Fluoroquinolones | pt_BR |
| Subject | Copper(II) complexes | pt_BR |
| Subject | Anti-T. cruzi activity | pt_BR |
| Subject | UV–Vis spectroscopy | pt_BR |
| Subject | Interaction with calf-thymus DNA | pt_BR |
| e-ISSN | 1572-8773 | |
| Embargo date | 2030-01-01 | |
