An ion conductor derived from spermine and cholic acid
An ion conductor derived from spermine and cholic acid
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DOI：
10.1021/ja0056466
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发表时间：
2000-12-27
影响因子：
15
通讯作者：
Regen, SL
中科院分区：
文献类型：
--
作者：
Bandyopadhyay, P;Janout, V;Regen, SL
在本文中，我们表明，两个自然发生的产品，精胺和胆酸的缩合，产生一个离子导体（1）对磷脂酰胆碱（PC）双层膜的不同厚度具有高选择性。使用这种类型的共轭物的潜力，从抗菌的角度来看，利用双层厚度的细微差异，简要讨论。在跨膜合成离子载体（即离子导体）的设计兴趣在最近几年有所加强。这种兴趣的一部分来源于这样一种概念，即离子导体可能导致新的抗生素类别，这些抗生素对耐药性不太敏感。促进Na+穿过PC双层流动的甾醇基离子导体的一个实例是衍生自23，24-双降-5-胆烯酸和1，17-二氨基-3，6，9，12，15-五氧杂十七烷的缀合物，即2. 4
In this paper we show that condensation of two naturally occurring products, spermine and cholic acid, yields an ion conductor (1) having high selectivity toward phosphatidylcholine (PC) bilayers of varying thickness. The potential for using conjugates of this type, to exploit subtle differences in bilayer thicknesses from an antimicrobial standpoint, is briefly discussed.Interest in the design of membrane-spanning synthetic ionophores (ie, ion conductors) has intensified in recent years. 1 Part of this interest stems from the notion that ion conductors may lead to new classes of antibiotics that are less susceptible toward resistance. 2, 3 One example of a sterol-based ion conductor, which promotes the flow of Na+ across PC bilayers, is a conjugate derived from 23, 24-bisnor-5-cholenic acid and 1, 17-diamino-3, 6, 9, 12, 15-pentaoxaheptadecane, ie, 2. 4