MECHANISM OF ACTION OF MACROCYCLIC ANTIBIOTIC FILIPIN ON CELL AND LIPID MEMBRANES
Keywords:
polyene antibiotics (PA), filipin, bilayer lipid membranes (BLM), ionic channels, filipin-cholesterol complexes, conductivity of membranesAbstract
The mechanism of action of macrolide pentaene antibiotic filipin on cell and bilayer lipid membranes was investigated. The sterol hypothesis of the filipin mechanism of action is confirmed experimentally. The data of filipin action on bilayer lipid membranes (BLM) are presented. Single ionic channels with conductance of 15—20 pS were showed on cholesterol-containing membranes
by the action of filipin at low concentration (1•10-8 M). Combined ionic channels of filipin and amphotericin B with conductance of 25—30 pS, that by1.5—2 times lower than of the clean filipin channels and by 5 times more than of the clean amphotericin B channels were discovered. The selectivity of filipin channels is mainly cationic. The potential of the penetrating ion on 10-fold
gradient is +18 mV. It is shown the practical aspects of filipin application in medicine and pharmacology.
