[Mechanism of action of macrolide antibiotic filipin on cell and lipid membranes].

Abstract

The review deals with investigation of the mechanism of action of macrolide pentaene antibiotic filipin on cell and bilayer lipid membranes (BLM). The sterol hypothesis of the filipin mechanism of action is confirmed experimentally. The hemolytic and geneticocytological action of filipin, its action on virus infection and prion protein-associated diseases are discussed. The data on the mechanism of filipin action on BLM are presented. Filipin single ionic channels with conductance of 15-20 pS that is 3-4 times higher than that of the amphotericin channels were detected on cholesterol-containing membranes in filipin low concentration (1 x 10(-8) M) aqueous salt solution. Combined ionic channels of filipin and amphotericin B with conductance of 25-30 pS, that is 1.5-2 time lower than that of the clean filipin channels and 5 times higher that of the clean amphotericin B channels were also detected. The selectivity of filipin channels is mainly cationic. The potential of the penetrating ion on 10-fold gradient is +18 mV. The practical aspects of filipin application in biology, medicine and pharmacology are indicated.

• Authors: A A Samedova, Kh M Kasumov
• Journal: Antibiotiki i khimioterapiia = Antibiotics and chemoterapy [sic] (Antibiot Khimioter) Vol. 54 Issue 11-12 Pg. 44-52 ( 2009) ISSN: 0235-2990 [Print] Russia (Federation)
• PMID: 20583567 (Publication Type: English Abstract, Journal Article, Review)

Chemical References

• Anti-Bacterial Agents
• Ion Channels
• Membrane Lipids
• Filipin

Topics

• Animals
• Anti-Bacterial Agents (metabolism, pharmacology)
• Cell Membrane (metabolism)
• Cell Membrane Permeability (drug effects)
• Filipin (metabolism, pharmacology)
• Humans
• Ion Channels (metabolism)
• Membrane Lipids (metabolism)