such as "Introduction", "Conclusion"..etc
* Université Catholique de Louvain, Faculty of Medicine, Unité de Pharmacologie Cellulaire et Moléculaire, Brussels, Belgium; Université Catholique de Louvain, Faculty of Agronomy, Unité de Chimie des Interfaces, Louvain-la-Neuve, Belgium; Faculté Universitaire des Sciences Agronomiques de Gembloux, Unité de Chimie Biologique Industrielle, and Centre de Biophysique Moléculaire Numérique, Faculté Universitaire des Sciences Agronomiques de Gembloux, Gembloux, Belgium; ¶
Université Catholique de Louvain, Louvain-la-Neuve, Faculty of
Sciences, Unité de Chimie Structurale et des Mécanismes Réactionnels,
Belgium; and || Université Libre de Bruxelles, Faculty of Sciences, Unité de Structure et Fonction des Membranes Biologiques, Brussels, Belgium
An Open Access Article : Biophysical Journal 94:3035-3046 (2008).
Probing drug/lipid interactions at the molecular level representsan important challenge in pharmaceutical research and membranebiophysics. Previous studies showed differences in accumulationand intracellular activity between two fluoroquinolones, ciprofloxacinand moxifloxacin, that may actually result from their differentialsusceptibility to efflux by the ciprofloxacin transporter. Inview of the critical role of lipids for the drug cellular uptakeand differences observed for the two closely related fluoroquinolones,we investigated the interactions of these two antibiotics withlipids, using an array of complementary techniques. Moxifloxacininduced, to a greater extent than ciprofloxacin, an erosionof the DPPC domains in the DOPC fluid phase (atomic force microscopy)and a shift of the surface pressure-area isotherms of DOPC/DPPC/fluoroquinolonemonolayer toward lower area per molecule (Langmuir studies).These effects are related to a lower propensity of moxifloxacinto be released from lipid to aqueous phase (determined by phasetransfer studies and conformational analysis) and a marked decreaseof all-trans conformation of acyl-lipid chains of DPPC (determinedby ATR-FTIR) without increase of lipid disorder and change inthe tilt between the normal and the germanium surface (alsodetermined by ATR-FTIR). All together, differences of ciprofloxacinas compared to moxifloxacin in their interactions with lipidscould explain differences in their cellular accumulation andsusceptibility to efflux transporters.
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