title: 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.
authors.affiliation: Institute of Chemistry/Organic and Bioorganic Chemistry, University of Graz, Heinrichstrasse 28, A-8010 Graz, Austria.
authors.forename: Simone
authors.initials: S
authors.lastname: Kosol
authors.forename: Evelyne
authors.initials: E
authors.lastname: Schrank
authors.forename: Mirjana Bukvić
authors.initials: MB
authors.lastname: Krajačić
authors.forename: Gabriel E
authors.initials: GE
authors.lastname: Wagner
authors.forename: N Helge
authors.initials: NH
authors.lastname: Meyer
authors.forename: Christoph
authors.initials: C
authors.lastname: Göbl
authors.forename: Gerald N
authors.initials: GN
authors.lastname: Rechberger
authors.forename: Klaus
authors.initials: K
authors.lastname: Zangger
authors.forename: Predrag
authors.initials: P
authors.lastname: Novak
mesh_terms: D000900:Anti-Bacterial Agents / Q000737:chemistry*; D017963:Azithromycin / Q000737:chemistry; D004058:Diffusion; D018942:Macrolides / Q000737:chemistry*; D009682:Magnetic Resonance Spectroscopy; D008567:Membranes, Artificial; D008823:Micelles; D008958:Models, Molecular; D018716:Molecular Mimicry; D010718:Phosphatidylserines / Q000737:chemistry; D054466:Phospholipases A1 / Q000737:chemistry; D010767:Phosphorylcholine / Q000031:analogs & derivatives / Q000737:chemistry; D012967:Sodium Dodecyl Sulfate / Q000737:chemistry; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D018942:Macrolides; D008567:Membranes, Artificial; D008823:Micelles; D010718:Phosphatidylserines; D010767:Phosphorylcholine; D012967:Sodium Dodecyl Sulfate; C028810:dodecylphosphocholine; D017963:Azithromycin; D054466:Phospholipases A1