Abstract
In the past decade substantial progress has been made in understanding the organization and biological activity of amphotericin B (AmB) in the presence of sterols in lipid environments. This review concentrates mainly on interactions of AmB with lipids and sterols, AmB channel formation in membranes, AmB aggregation, AmB modifications important for understanding its biological activity, and AmB models explaining its mechanism of action. Most of the reviewed studies concern monolayers at the water–gas interface, monolayers deposited on a solid substrate by use of the Langmuir–Blodgett technique, micelles, vesicles, and multi-bilayers. Liposomal AmB formulations and drug delivery are intentionally omitted, because several reviews dedicated to this subject are already available.
Highlights
Amphotericin B (AmB) is a macrolide polyene antifungal antibiotic (Gallis et al 1990; AbuSalah 1996; Hartsel and Bolard 1996; Carrillo-Munoz et al 2006; Cereghetti and Carreira 2006)
amphotericin B (AmB) can initiate in-plane ergosterol redistribution, which is not observed for cholesterol. This is in accordance with an H1 NMR study which shows that AmB, in the presence of ergosterol, interacts more strongly with the aliphatic lipid chains, whereas this is not observed for lipids containing cholesterol (Gabrielska et al 2006)
Several studies suggest the antifungal activity of AmB is related to the presence of ergosterol, the main sterol of fungal cells
Summary
Amphotericin B (AmB) is a macrolide polyene antifungal antibiotic (Gallis et al 1990; AbuSalah 1996; Hartsel and Bolard 1996; Carrillo-Munoz et al 2006; Cereghetti and Carreira 2006). This dynamic molecular study confirmed that AmB forms dimers in lipid bilayers with and without sterols, but in the presence of ergosterol AmB–AmB interaction is less favorable (Neumann et al 2013a). Yang et al (2013) measured the effect of AmB on pore formation in membranes containing ergosterol by use of fluorescent dyes of known average diameter.
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