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(Referência obtida automaticamente do Web of Science, por meio da informação sobre o financiamento pela FAPESP e o número do processo correspondente, incluída na publicação pelos autores.)

A Nanostructured Lipid System as a Strategy to Improve the in Vitro Antibacterial Activity of Copper(II) Complexes

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Autor(es):
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da Silva, Patricia B. [1] ; Bonifacio, Bruna V. [1] ; Frem, Regina C. G. [2] ; Godoy Netto, Adelino V. [2] ; Mauro, Antonio E. [2] ; da Costa Ferreira, Ana M. [3] ; Lopes, Erica de O. [1] ; Raddi, Maria S. G. [1] ; Bauab, Tais M. [1] ; Pavan, Fernando R. [1] ; Chorilli, Marlus [1]
Número total de Autores: 11
Afiliação do(s) autor(es):
[1] Univ Estadual Paulista, Sch Pharmaceut Sci, UNESP, BR-14801902 Araraquara, SP - Brazil
[2] Univ Estadual Paulista, Inst Chem, UNESP, BR-14800060 Araraquara, SP - Brazil
[3] Univ Sao Paulo, Inst Chem, BR-05508900 Sao Paulo, SP - Brazil
Número total de Afiliações: 3
Tipo de documento: Artigo Científico
Fonte: Molecules; v. 20, n. 12, p. 22534-22545, DEC 2015.
Citações Web of Science: 6
Resumo

The aim of this study was to construct a nanostructured lipid system as a strategy to improve the in vitro antibacterial activity of copper( II) complexes. New compounds with the general formulae {[} CuX2( INH) 2] center dot nH(2)O ( X = Cl - and n = 1 ( 1); X = NCS - and n = 5 ( 2); X = NCO - and n = 4 ( 3); INH = isoniazid, a drug widely used to treat tuberculosis) derived from the reaction between the copper( II) chloride and isoniazid in the presence or absence of pseudohalide ions ( NCS - or NCO -) were synthesized and characterized by infrared spectrometry, electronic absorption spectroscopy, electron paramagnetic resonance ( EPR) spectroscopy, elemental analysis, melting points and complexometry with 2,2 1,2 1 1,2 1 1 1 -( Ethane- 1,2- diyldinitrilo) tetraacetic acid ( EDTA). The characterization techniques allowed us to confirm the formation of the copper( II) complexes. The Cu( II) complexes were loaded into microemulsion ( MEs) composed of 10% phase oil ( cholesterol), 10% surfactant {[} soy oleate and Brij (R) 58 ( 1: 2)] and 80% aqueous phase ( phosphate buffer pH = 7.4) prepared by sonication. The Cu( II) complex- loaded MEs displayed sizes ranging from 158.0 +/- 1.060 to 212.6 +/- 1.539 nm, whereas the polydispersity index ( PDI) ranged from 0.218 +/- 0.007 to 0.284 +/- 0.034. The antibacterial activity of the free compounds and those that were loaded into the MEs against Staphylococcus aureus ATCC (R) 25923 and Escherichia coli ATCC (R) 25922, as evaluated by a microdilution technique, and the cytotoxicity index ( IC50') against the Vero cell line ( ATCC (R) CCL- 81TM) were used to calculate the selectivity index ( SI). Among the free compounds, only compound 2 ( MIC 500 mu g/ mL) showed activity for S. aureus. After loading the compounds into the MEs, the antibacterial activity of compounds 1, 2 and 3 was significantly increased against E. coli ( MIC's 125, 125 and 500 mu g/ mL, respectively) and S. aureus ( MICs 250, 500 and 125- g/ mL, respectively). The loaded compounds were less toxic against the Vero cell line, especially compound 1 ( IC50 from 109.5 to 319.3 mu g/ mL). The compound 2- and 3- loaded MEs displayed the best SI for E. coli and S. aureus, respectively. These results indicated that the Cu( II) complex- loaded MEs were considerably more selective than the free compounds, in some cases, up to 40 times higher. (AU)

Processo FAPESP: 13/14957-5 - Investigação do potencial contra tuberculose de uma nova classe de compostos furoxânicos e compostos nanoestruturados de rutênio(II) e cobre(II)
Beneficiário:Fernando Rogério Pavan
Linha de fomento: Auxílio à Pesquisa - Apoio a Jovens Pesquisadores
Processo FAPESP: 13/09265-7 - Avaliação do potencial de sistemas lipídicos nanoestruturados para administração de compostos de Cu(II) aplicáveis na otimização da terapia da tuberculose
Beneficiário:Patrícia Bento da Silva
Linha de fomento: Bolsas no Brasil - Pós-Doutorado