Blocking ion channels induced by antifungal lipopeptide syringomycin E with amide-linked local anesthetics

The effects of the amide-linked (lidocaine (LDC), mepivacaine (MPV), prilocaine (PLC)) and ester-bound local anesthetics (benzocaine (BZC), procaine (PRC), and tetracaine (TTC)) on the pore-forming activity of the antifungal lipopeptide syringomycin E (SRE) in lipid bilayers were studied. Independen...

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Bibliographic Details
Published in:Scientific reports 2018-08, Vol.8 (1), p.11543-10, Article 11543
Main Authors: Zakharova, Anastasiia A., Efimova, Svetlana S., Schagina, Ludmila V., Malev, Valery V., Ostroumova, Olga S.
Format: Article
Language:English
Subjects:
119/118
631/45/269
631/45/287/1189
631/57/2270/1140
Anesthetics
Binding sites
Conductance
Humanities and Social Sciences
Ion channels
Lidocaine
Lipid bilayers
Lipid composition
Local anesthesia
Local anesthetics
Membranes
multidisciplinary
Potassium chloride
Prilocaine
Science
Science (multidisciplinary)
Tetracaine
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Summary:The effects of the amide-linked (lidocaine (LDC), mepivacaine (MPV), prilocaine (PLC)) and ester-bound local anesthetics (benzocaine (BZC), procaine (PRC), and tetracaine (TTC)) on the pore-forming activity of the antifungal lipopeptide syringomycin E (SRE) in lipid bilayers were studied. Independently on electrolyte concentration in the membrane bathing solution the observed changes in conductance of SRE channels agreed with the altered membrane dipole potential under the action of ester-bound local anesthetics. Effects of aminoamides in diluted and concentrated solutions were completely different. At 0.1 M KCl (pH 7.4) the effects of amide-linked anesthetics were in accordance with changes in the membrane surface potential, while at 2 M KCl aminoamides blocked ion passage through the SRE channels, leading to sharp reductions in pore conductance at negative voltages and 100-fold decreases in the channel lifetimes. The effects were not practically influenced by the membrane lipid composition. The interaction cooperativity implied the existence of specific binding sites for amide-bound anesthetics in SRE channels.
ISSN:2045-2322
2045-2322
DOI:10.1038/s41598-018-30077-6