Effect of Fusidic Acid and Some Nitrogen-Containing Derivatives on Liposomal and Mitochondrial Membranes

The paper assesses the membranotropic action of the natural antibiotic fusidic acid (FA) and its derivatives. It was found that a FA analogue with ethylenediamine moiety (derivative 2), in contrast to native FA and 3,11-dioxime analogue (derivative 1), is able to increase the mobility of the lipid bilayer in the zone of lipid headgroups, as well as to induce permeabilization of lecithin liposome membranes. A similar effect of derivative 2 is also observed in the case of rat liver mitochondrial membranes. We noted a decrease in the microviscosity of the mitochondrial membrane and nonspecific permeabilization of organelle membranes in the presence of this agent, which was accompanied by a decrease in mitochondrial Delta psi and OXPHOS efficiency. This led to a reduction in mitochondrial calcium retention capacity. The derivatives also reduced the production of H2O2 by mitochondria. The paper considers the relationship between the structure of the tested compounds and the observed effects.

Automated summary

This paper assesses the membranotropic action of fusidic acid and its derivatives. The authors found that a derivative with ethylenediamine moiety can increase the mobility of lipid bilayer and induce permeabilization of liposome membranes. A similar effect was observed in rat liver mitochondrial membranes. Moreover, the derivatives reduced mitochondrial Delta psi and OXPHOS efficiency, leading to a decrease in mitochondrial calcium retention capacity.