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<h2> Characterization of the Interactions between Fluoroquinolone Antibiotics and Lipids: a Multitechnique Approach</h2> <strong> Hayet Bensikaddour<sup> </sup>, Nathalie Fa<sup> </sup>, Ingrid Burton<sup> <img src="http://www.biophysj.org/math/dagger.gif" alt="{dagger}"></sup>, Magali Deleu<sup> <img src="http://www.biophysj.org/math/Dagger.gif" alt="{ddagger}"></sup>, Laurence Lins<sup> <img src="http://www.biophysj.org/math/sect.gif" alt="§"></sup>, André Schanck<sup> ¶</sup>, Robert Brasseur<sup> ¶</sup>, Yves F. Dufrêne<sup> <img src="http://www.biophysj.org/math/dagger.gif" alt="{dagger}"></sup>, Erik Goormaghtigh<sup> \|\|</sup> and Marie-Paule Mingeot-Leclercq<sup> </sup></strong> <p> <sup></sup> Université Catholique de Louvain, Faculty of Medicine, Unité de Pharmacologie Cellulaire et Moléculaire, Brussels, Belgium; <sup><img src="http://www.biophysj.org/math/dagger.gif" alt="{dagger}"></sup> Université Catholique de Louvain, Faculty of Agronomy, Unité de Chimie des Interfaces, Louvain-la-Neuve, Belgium; <sup><img src="http://www.biophysj.org/math/Dagger.gif" alt="{ddagger}"></sup> Faculté Universitaire des Sciences Agronomiques de Gembloux, Unité de Chimie Biologique Industrielle, and <sup><img src="http://www.biophysj.org/math/sect.gif" alt="§"></sup> Centre de Biophysique Moléculaire Numérique, Faculté Universitaire des Sciences Agronomiques de Gembloux, Gembloux, Belgium; <sup>¶</sup> Université Catholique de Louvain, Louvain-la-Neuve, Faculty of Sciences, Unité de Chimie Structurale et des Mécanismes Réactionnels, Belgium; and <sup>\|\|</sup> Université Libre de Bruxelles, Faculty of Sciences, Unité de Structure et Fonction des Membranes Biologiques, Brussels, Belgium </p> <p> An Open Access Article : <em>Biophysical Journal</em> 94:3035-3046 (2008). </p> <p> </p> <h3> <strong>Abstract</strong> </h3> <p> Probing drug/lipid interactions at the molecular level represents<sup></sup>an important challenge in pharmaceutical research and membrane<sup></sup>biophysics. Previous studies showed differences in accumulation<sup></sup>and intracellular activity between two fluoroquinolones, ciprofloxacin<sup></sup>and moxifloxacin, that may actually result from their differential<sup></sup>susceptibility to efflux by the ciprofloxacin transporter. In<sup></sup>view of the critical role of lipids for the drug cellular uptake<sup></sup>and differences observed for the two closely related fluoroquinolones,<sup></sup>we investigated the interactions of these two antibiotics with<sup></sup>lipids, using an array of complementary techniques. Moxifloxacin<sup></sup>induced, to a greater extent than ciprofloxacin, an erosion<sup></sup>of the DPPC domains in the DOPC fluid phase (atomic force microscopy)<sup></sup>and a shift of the surface pressure-area isotherms of DOPC/DPPC/fluoroquinolone<sup></sup>monolayer toward lower area per molecule (Langmuir studies).<sup></sup>These effects are related to a lower propensity of moxifloxacin<sup></sup>to be released from lipid to aqueous phase (determined by phase<sup></sup>transfer studies and conformational analysis) and a marked decrease<sup></sup>of all-<em>trans</em> conformation of acyl-lipid chains of DPPC (determined<sup></sup>by ATR-FTIR) without increase of lipid disorder and change in<sup></sup>the tilt between the normal and the germanium surface (also<sup></sup>determined by ATR-FTIR). All together, differences of ciprofloxacin<sup></sup>as compared to moxifloxacin in their interactions with lipids<sup></sup>could explain differences in their cellular accumulation and<sup></sup>susceptibility to efflux transporters. <br> </p>
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