ArticleThe Journal of membrane biology2003
The macrolide antibiotic azithromycin interacts with lipids and affects membrane organization and fluidity: studies on Langmuir-Blodgett monolayers, liposomes and J774 macrophages.
Article in The Journal of membrane biology, 2003. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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Who cites it
21 citing papers in PubMed, 52 citations in OpenAlex.
- The Synergistic Armory: A Global Genome-Wide Association Study Reveals the Integrated Mechanisms of Azithromycin Resistance inInternational journal of molecular sciences · 2026Article
- Design of chitosan-coated CeORSC medicinal chemistry · 2025Article
- The Non-Antibacterial Effects of Azithromycin and Other Macrolides on the Bronchial Epithelial Barrier and Cellular Differentiation.International journal of molecular sciences · 2025Article
- Monitoring membranes: The exploration of biological bilayers with second harmonic generation.Chemical physics reviews · 2022Review
- Interaction of a Phospholipid and a Coagulating Protein: Potential Candidate for Bioelectronic Applications.ACS omega · 2022Article
- Azithromycin in viral infections.Reviews in medical virology · 2021Review
- Azithromycin: The First Broad-spectrum Therapeutic.European journal of medicinal chemistry · 2020Review
- Azithromycin: The First Broad-spectrum Therapeutic.Journal of translational autoimmunity · 2020Review
- A How-To Guide for Mode of Action Analysis of Antimicrobial Peptides.Frontiers in cellular and infection microbiology · 2020Review
- Proteomics-Based Mechanistic Investigation ofFrontiers in microbiology · 2019Article
- Azithromycin-Induced Changes to Bacterial Membrane Properties MonitoredACS medicinal chemistry letters · 2018Article
- Membrane Interactions of Phytochemicals as Their Molecular Mechanism Applicable to the Discovery of Drug Leads from Plants.Molecules (Basel, Switzerland) · 2015Review
- Macrolides rapidly inhibit red blood cell invasion by the human malaria parasite, Plasmodium falciparum.BMC biology · 2015Article
- Azithromycin distinctively modulates classical activation of human monocytes in vitro.British journal of pharmacology · 2012Article
- Crohn's disease: evidence for involvement of unregulated transcytosis in disease etio-pathogenesis.World journal of gastroenterology · 2011Review
- Article
- Label-free detection of drug-membrane association using ultraviolet-visible sum-frequency generation.Journal of the American Chemical Society · 2009Article
- Article
- Effect of fengycin, a lipopeptide produced by Bacillus subtilis, on model biomembranes.Biophysical journal · 2008Article
- Influence on mitochondria and cytotoxicity of different antibiotics administered in high concentrations on primary human osteoblasts and cell lines.Antimicrobial agents and chemotherapy · 2007Article
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Authors and funding
7 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The macrolide antibiotic azithromycin was shown to markedly inhibit endocytosis. Here we investigate the interaction of azithromycin with biomembranes and its effects on membrane biophysics in relation to endocytosis. Equilibrium dialysis and 31P NMR revealed that azithromycin binds to lipidic model membranes and decreases the mobility of phospholipid phosphate heads. In contrast, azithromycin had no effect deeper in the bilayer, based on fluorescence polarization of TMA-DPH and DPH, compounds that, respectively, explore the interfacial and hydrophobic domains of bilayers, and it did not induce membrane fusion, a key event of vesicular trafficking. Atomic force microscopy showed that azithromycin perturbed lateral phase separation in Langmuir-Blodgett monolayers, indicating a perturbation of membrane organization in lateral domains. The consequence of azithromycin/ phospholipid interaction on membrane endocytosis was next evaluated in J774 macrophages by using three tracers with different insertion preferences inside the biological membranes and intracellular trafficking: C6-NBD-SM, TMA-DPH and N-Rh-PE. Azithromycin differentially altered their insertion into the plasma membrane, slowed down membrane trafficking towards lysosomes, as evaluated by the rate of N-Rh-PE self-quenching relief, but did not affect bulk membrane internalization of C6-NBD-SM and TMA-DPH. Azithromycin also decreased plasma membrane fluidity, as shown by TMA-DPH fluorescence polarization and confocal microscopy after labeling by fluorescent concanavalin A. We conclude that azithromycin directly interacts with phospholipids, modifies biophysical properties of membrane and affects membrane dynamics in living cells. This antibiotic may therefore help to elucidate the physico-chemical properties underlying endocytosis.
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