The Properties of Ion Channels in Lipid Membranes Modified by the Aromatic Antibiotic Levorin А2

Abstract

It has been shown that the main components of levorin A, that is, A0, A1, A2, or A3, that contain an aromatic group increase the permeability of membranes in the series A3 > A2 > A1 > A0 when they are on the same side of the membrane. All levorin components have cationic selectivity. The most studied levorin, А2, promotes the almost ideal permeability of membranes to potassium ions. The membrane potential for a ten-fold change in the KCl concentration gradient is 56 ± 2 mV. It has been shown that the injection of the same concentration of levorin А2 into one side of the membrane and then, after achieving the typical membrane permeability, into the other side of the membrane generates a two-fold increase in the total membrane permeability. This means that independent levorin-induced conductive semi-pores are formed on each side of the membrane. It has been found that the injection of levorin А2 only into one side of the membrane enhances the membrane permeability to monosaccharides and other neutral molecules. The presence of levorin А2 in cholesterol-, ergosterol-, and stigmasterol-containing phospholipid membranes has been shown to lead to the single-channel conductivity of typical ion channels of 0.2–0.5 pS. The properties of these channels have been studied. The levorin channels exist in two states, open and closed. Most of the time, the channel remains in the open state in the KBr solution. In solutions of different salts of the same concentration, the conductivity value of the levorin channels is approximately the same (0.4–0.5 pS). An increase in the dimethyl sulfoxide concentration in aqueous solutions facilitates the transition of polyene antibiotic molecules from dispersed to monomolecular form. The molecules of polyene antibiotics in the associated form exhibit high membrane activity.