This article is devoted to the research of biological activity and physical and chemical properties of macrolactone polyene antibiotics (PA) with different hydrophilic and hydrophobic parts of molecules at the interaction with bilayer lipid membranes (BLM). Physical and chemical parameters of ion channels such selectivity and conductivity inducing by PA are influenced even by small changes in the number of double bonds, hydroxyl and carbonyl groups in molecule of these compounds. It was found that higher number of double bonds in the molecule of PA leads the higher biological activity of antibiotics. Among of the different PA there are used amphotericin B, levorin A, nystatin and filipin in the our experiments. There is comparative analysis of single ion channels of above mentioned PA and hybrid ion channels formed of PA with various ion channels in cholesterol containing phospholipid membranes. It makes possibilities for the targeted synthesis of new generation antibiotics.
polyene antibiotics (PA), bilayer lipid membranes (BLM), membrane activity, conductivity, selectivity, ion channels
1. Borowski E. Novel approaches in the rational design of antifungal agents of low toxicity. Farmaco., 2000, vol. 55, pp. 206-208.
2. Mueller P., Rudin D.O., Tien H.T., Wescott W.C. Methods for formation of single bimolecular lipid membrane in aqueous solution. J. Phys. Chem., 1963, vol. 67, pp. 534-535.
3. Folch J., Leese M., Sloan-Stanley G.H. A simple method for the isolation and purification of total lipids from animal tissues. J. Bio. Chem., 1957, vol. 226, pp. 4997-509.
4. Kasumov H.M. Struktura i membrannaya funkciya polienovyh makroolidnyh antibiotikov. Monografiya. Baku-Elm, Moskva: Nauka, 2009, 511 s. @@[Kasumov Kh.M. Structure and membrane function of polyene macrolide antibiotics. Monograph. Baku-Elm, Moscow: Nauka, 2009, 511 r. (In Russ.)]
5. Samedova A.A., Taghi-zade T.P., Kasumov Kh.M. Dependence of ion channel properties formed by polyene antibitoics molecules on the lactone ring structure. Russian J. Of Bioorganic Chemistry, 2018, vol. 44, no. 3, pp. 337-345.
6. Ibragimova V, H., Alieva I.N., Kasumov H.M. Effekt levorina A2, vvodimogo s odnoy storony lipidnyh membran. Biologicheskie membrany, t. 23, № 6, s. 493-502. @@[Ibragimova V.Kh., Aliyeva I.N., Kasumov Kh.M. Effect of levorin A2 added by one side of lipid membranes. Biological membranes, vol. 23, no. 6, pr 493-502. (In Russ.)]
