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[甾醇在多烯抗生素与脂质膜相互作用中的作用]

[Role of sterols in the interaction of polyene antibiotics with lipid membranes].

作者信息

Feĭgin A M, Gnanik T, Pasechnik V I, Flerov M N, Bogoslovskiĭ N A

出版信息

Antibiotiki. 1981 Jul;26(7):522-6.

PMID:6267995
Abstract

The problem whether the membrane sterols are indirect acceptors of polyenic antibiotics or they play the role of substances providing conditions (at the expense of putting in order the membrane phospholipids) for formation of conductive complexes (ionic canals) from the antibiotic molecules is discussed. The comparative study on the ability of sterols of various structure (ergosterol, 7-dehydrocholesterol, cholesterol, 5 alpha-cholestan-3 beta-ol) to interact with the membrane phospholipids and to increase the sensitivity of such membranes to amphotericin B showed no correlation between the levels of these properties. The value of the changes in the cross elasticity module (E) of artificial bilayer lipid membranes from egg lecithin on introduction of the above sterols into their composition was used as the criterion for the interaction level. The absence of correlation between the above properties of the sterols indicated that the role of the sterols in interaction of polyenic antibiotics with the membranes could not be considered as the only effect of the sterols on putting in order the phospholipids, which confirmed the hypothesis on the acceptor function of the sterols with respect to polyenic antibiotics. The study of the effect of amphotericin B on the elastic properties of the cholesterol-containing bilayer membranes isolated from egg lecithin showed tha the values of the longitudinal and cross elasticity modules of the membranes did not change during introduction into the membranes of the ionic canals.

摘要

文中讨论了膜固醇是多烯抗生素的间接受体,还是它们起到了为抗生素分子形成传导复合物(离子通道)提供条件(通过使膜磷脂排列有序来实现)的物质的作用这一问题。对各种结构的固醇(麦角固醇、7-脱氢胆固醇、胆固醇、5α-胆甾烷-3β-醇)与膜磷脂相互作用以及增加此类膜对两性霉素B敏感性的能力进行的比较研究表明,这些特性的水平之间没有相关性。将上述固醇引入卵磷脂人工双层脂质膜的组成中后,膜的横向弹性模量(E)变化值被用作相互作用水平的标准。固醇的上述特性之间缺乏相关性表明,固醇在多烯抗生素与膜相互作用中的作用不能仅被视为固醇对磷脂排列有序的唯一影响,这证实了关于固醇对多烯抗生素受体功能的假说。对两性霉素B对从卵磷脂中分离出的含胆固醇双层膜弹性特性的影响的研究表明,在向膜中引入离子通道的过程中,膜的纵向和横向弹性模量值没有变化。

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