Miltefosine and BODIPY-labeled alkylphosphocholine with leishmanicidal activity: Aggregation properties and interaction with model membranes

Autor(es)

Barioni, Marina Berardi ^[1] ; Ramos, Ana Paula ^[2] ; Darbello Zaniquelli, Maria Elisabete ^[2] ; Acuna, Alberto Ulises ^[3] ; Ito, Amando Siuiti ^[1]

Afiliação do(s) autor(es)

^[1] Univ Sao Paulo, Fac Filosofia Ciencias & Letras Ribeirao Preto, Dept Fis, BR-14040901 Ribeirao Preto, SP - Brazil

^[2] Univ Sao Paulo, Fac Filosofia Ciencias & Letras Ribeirao Preto, Dept Quim, BR-14040901 Ribeirao Preto, SP - Brazil

^[3] CSIC, Inst Quim Fis Rocasolano, E-28006 Madrid - Spain

• Tipo de documento: Artigo Científico
• Fonte: Biophysical Chemistry; v. 196, p. 92-99, JAN 2015.
• Citações Web of Science: 8

Resumo

Miltefosine (hexadecylphosphocholine, MT) afforded successful oral treatment against human visceral and cutaneous leishmaniasis. Knowledge of MT aggregation in aqueous solutions and of its interaction with lipid membranes is important to understand pharmacokinetics, bioavailability and antiparasitic effects. Methods based on surface tension and fluorescence spectroscopy gave the value of 50 mu M for critical micelle concentration (CMC) in buffered water solution, and the value is influenced by salt content. Interaction between MT and lipid vesicles was monitored by fluorescence and the drug promotes only minor changes in the surface of the vesicles. At MT concentration below CMC, modifications in probe fluorescence are due to disordering effects promoted by the drug in the bilayer. Above the CMC, MT promoted large modifications in the vesicles as a whole, resulting in mixed aggregates containing lipids, drug and probe. Effects are less evident above thermal phase transition when the bilayer is in less ordered state. (C) 2014 Elsevier B.V. All rights reserved. (AU)

• Processo FAPESP: 10/08652-9 - Propriedades estruturais de membranas modelo em interação com compostos com ação anti-Leishmania
• Beneficiário: Marina Berardi Barioni
• Modalidade de apoio: Bolsas no Brasil - Doutorado
• Processo FAPESP: 09/54044-3 - EMU: aquisição de espectroscópio de correlação de fluorescência para medidas de correlação de fluorescência e obtenção de imagens por tempo de vida
• Beneficiário: Amando Siuiti Ito
• Modalidade de apoio: Auxílio à Pesquisa - Programa Equipamentos Multiusuários