These tools will no longer be maintained as of December 31, 2024. Archived website can be found here. PubMed4Hh GitHub repository can be found here. Contact NLM Customer Service if you have questions.


Pubmed for Handhelds

PUBMED FOR HANDHELDS

Search MEDLINE/PubMed

  • Title: Interaction of the macrolide azithromycin with phospholipids. I. Inhibition of lysosomal phospholipase A1 activity.
    Author: Van Bambeke F, Montenez JP, Piret J, Tulkens PM, Courtoy PJ, Mingeot-Leclercq MP.
    Journal: Eur J Pharmacol; 1996 Oct 24; 314(1-2):203-14. PubMed ID: 8957238.
    Abstract:
    Azithromycin, the first clinically developed dicationic macrolide antibiotic, displays an exceptional accumulation in lysosomes of cultured cells. In fibroblasts incubated with 50 mg/l (66.6 microM), it induces a distinct phospholipidosis as evidenced by biochemical and ultrastructural criteria, which strikingly resembles alterations described previously with gentamicin, a pentacationic aminoglycoside antibiotic which inhibits the lysosomal catabolism of phospholipids. We show that both drugs inhibit, in an equimolar manner, the activity of phospholipase A1 (assayed for phosphatidylcholine, included in negatively charged liposomes), in a way consistent with the model of 'charge neutralization' proposed already for gentamicin (Mingeot-Leclercq et al., 1988, Biochem. Pharmacol. 37, 591). Both drugs bind to negatively charged liposomes. Yet, in spite of this binding, azithromycin does not induce aggregation or fusion of negatively charged vesicles, under conditions in which gentamicin (or spermine, a fully hydrophilic polycation) causes a massive aggregation, and bis(beta-diethylaminoethylether)hexestrol (a dicationic amphiphile) causes fusion. The molecular interactions of azithromycin with acidic phospholipids are further examined in a companion paper.
    [Abstract] [Full Text] [Related] [New Search]