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Fernandes FR, Ferreira WA, Campos MA, et al. Amphiphilic Antimony(V) Complexes for Oral Treatment of Visceral Leishmaniasis. Antimicrob Agents Chemother. 2013;57(9):4229-4236doi: 10.1128/AAC.00639-13.
Fernandes, F. R., Ferreira, W. A., Campos, M. A., Ramos, G. S., Kato, K. C., Almeida, G. G., Corrêa, J. D., Melo, M. N., Demicheli, C., & Frézard, F. (2013). Amphiphilic Antimony(V) Complexes for Oral Treatment of Visceral Leishmaniasis. Antimicrobial agents and chemotherapy, 57(9), 4229-4236. https://doi.org/10.1128/AAC.00639-13
Fernandes, Flaviana R, et al. "Amphiphilic Antimony(V) Complexes for Oral Treatment of Visceral Leishmaniasis." Antimicrobial agents and chemotherapy vol. 57,9 (2013): 4229-4236. doi: https://doi.org/10.1128/AAC.00639-13
Fernandes FR, Ferreira WA, Campos MA, Ramos GS, Kato KC, Almeida GG, Corrêa JD, Melo MN, Demicheli C, Frézard F. Amphiphilic Antimony(V) Complexes for Oral Treatment of Visceral Leishmaniasis. Antimicrob Agents Chemother. 2013 Sep;57(9):4229-4236. doi: 10.1128/AAC.00639-13. Epub 2013 Jun 24. PMID: 23796930; PMCID: PMC3754332.
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Antimicrob Agents Chemother. 2013 Sep;57(9):4229-4236. doi: 10.1128/AAC.00639-13. Epub 2013 Jun 24.

Amphiphilic Antimony(V) Complexes for Oral Treatment of Visceral Leishmaniasis.

Antimicrobial agents and chemotherapy

Flaviana R Fernandes, Weverson A Ferreira, Mariana A Campos, Guilherme S Ramos, Kelly C Kato, Gregório G Almeida, José D Corrêa, Maria N Melo, Cynthia Demicheli, Frédéric Frézard

Affiliations

  1. Departamento de Fisiologia e Biofísica, Instituto de Ciências Biológicas.
  2. Departamento de Química, Instituto de Ciências Exatas.
  3. Departamento de Parasitologia, Instituto de Ciências Biológicas.
  4. Departamento de Morfologia, Instituto de Ciências Biológicas, Universidade Federal de Minas Gerais, Pampulha, Belo Horizonte, Minas Gerais, Brazil.
  5. Departamento de Fisiologia e Biofísica, Instituto de Ciências Biológicas [email protected].

PMID: 23796930 PMCID: PMC3754332 DOI: 10.1128/AAC.00639-13

Abstract

The need for daily parenteral administration is an important limitation in the clinical use of pentavalent antimonial drugs against leishmaniasis. In this study, amphiphilic antimony(V) complexes were prepared from alkylmethylglucamides (L8 and L10, with carbon chain lengths of 8 and 10, respectively), and their potential for the oral treatment of visceral leishmaniasis (VL) was evaluated. Complexes of Sb and ligand at 1:3 (SbL8 and SbL10) were obtained from the reaction of antimony(V) with L8 and L10, as evidenced by elemental and electrospray ionization-tandem mass spectrometry (ESI-MS) analyses. Fluorescence probing of hydrophobic environment and negative-staining transmission electron microscopy showed that SbL8 forms kinetically stabilized nanoassemblies in water. Pharmacokinetic studies with mice in which the compound was administered by the oral route at 200 mg of Sb/kg of body weight indicated that the SbL8 complex promoted greater and more sustained Sb levels in serum and liver than the levels obtained for the conventional antimonial drug meglumine antimoniate (Glucantime [Glu]). The efficacy of SbL8 and SbL10 administered by the oral route was evaluated in BALB/c mice infected with

Copyright © 2013, American Society for Microbiology. All Rights Reserved.

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