Probing the Interactions of Macrolide Antibiotics with Membrane-Mimetics by NMR Spectroscopy

Abstract

Interactions of macrolide antibiotics with biological membranes contribute to their bioavailability but are also involved in the formation of phospholipidosis, which is caused by the inhibition of phospholipase A(1) activity. We determined the interaction strength and localization of macrolide antibiotics with membrane-mimetics. Macrolides bind to membrane-mimetics with the positively charged amino groups being close to the micelle surface and thereby protect the lipids from being degraded by phospholipase A(1) rather than inhibiting the enzyme.