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Antileishmanial and cytotoxic activities of ionic surfactants compared to those of miltefosine.

Authors
  • Alonso, Lais1
  • Cardoso, Éder Jeferson Souza2
  • Gomes, Rodrigo Saar3
  • Mendanha, Sebastião Antônio2
  • Dorta, Miriam Leandro3
  • Alonso, Antonio4
  • 1 Instituto Federal Goiano, Trindade, GO, Brazil. , (Brazil)
  • 2 Instituto de Física, Universidade Federal de Goiás, Goiânia, GO, Brazil. , (Brazil)
  • 3 Instituto de Patologia Tropical e Saúde Publica, Departamento de Imunologia e Patologia Geral, Universidade Federal de Goiás, Goiânia, GO, Brazil. , (Brazil)
  • 4 Instituto de Física, Universidade Federal de Goiás, Goiânia, GO, Brazil. Electronic address: [email protected] , (Brazil)
Type
Published Article
Journal
Colloids and surfaces. B, Biointerfaces
Publication Date
Aug 05, 2019
Volume
183
Pages
110421–110421
Identifiers
DOI: 10.1016/j.colsurfb.2019.110421
PMID: 31401463
Source
Medline
Keywords
Language
English
License
Unknown

Abstract

Using the electron paramagnetic resonance (EPR) of spin-labeled stearic acid and a spin label chemically attached to the membrane proteins, the interaction of miltefosine (MIL) and the ionic surfactants sodium dodecyl sulfate (SDS, anionic), cetyltrimethylammonium chloride (CTAC, cationic) and N-hexadecyl-N,N-dimethyl-3-ammonio-1-propanesulfonate (HPS, zwitterionic) with the plasma membrane of Leishmania (L.) amazonensis promastigotes was studied. The spin-label EPR data indicated that the four compounds studied have the ability to increase the molecular dynamics of membrane proteins to a large extent. Compared to the other compounds, SDS produced the smallest increases in dynamics and demonstrated the lowest antileishmanial activity and cytotoxicity to J774.A1 macrophages. The activities of the other three compounds were not different from each other, but CTAC had a stronger activity against L. amazonensis promastigotes at higher cellular concentrations (> 1 × 109 cells/mL) and was the most effective against L. amazonensis-infected macrophages. However, CTAC was also the most cytotoxic to macrophages. By measuring the IC50/CC50 values for assays of different cell concentrations, we estimated the membrane-water partition coefficient (KM/W) as well as the concentrations in the membrane (cm50) and aqueous phase (cw50) of the compounds at their IC50/CC50. Compared to the other compounds, SDS showed the lowest value of KM/W and the highest value of cm50. In all experiments in this study, the data for the zwitterionic molecules HPS and MIL were not significantly different. Copyright © 2019 Elsevier B.V. All rights reserved.

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