Synthetic hydraphile channels of appropriate length kill Escherichia coli
Synthetic hydraphile channels of appropriate length kill Escherichia coli
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DOI：
10.1021/ja017052o
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发表时间：
2002-08-07
影响因子：
15
通讯作者：
Gokel, GW
中科院分区：
文献类型：
--
作者：
Leevy, WM;Donato, GM;Gokel, GW
冠醚为基础的合成阳离子传导通道称为亲水显示明确的磷脂囊泡中的离子电渗活性。这些化合物显示出对细菌E有活性。杆菌进行纸片扩散测定以评估不同亲液衍生物的毒性。进行液体培养试验以定量细胞活性对通道长度的依赖性。有人提出，亲水性是有毒的细菌作为一个结果，在膜通道的形成。发现杀菌活性至少取决于功能性中央中继和适当通道长度的存在。据推测，亲水物插入到双层中并破坏细胞的渗透平衡，导致细胞死亡。
Crown ether-based synthetic cation conducting channels called hydraphiles show clear ionophoretic activity in phospholipid vesicles. These compounds are shown to be active against the bacteriumE. coli. Disk diffusion assays were performed to assess the toxicity of different hydraphile derivatives. Liquid culture tests were conducted to quantitate the dependence of bacterical activity on channel length. It is proposed that hydraphiles are toxic to bacteria as a result of channel formation in the membrane. The bactericidal activity is found to depend at least on the presence of a functional central relay and proper channel length. It is speculated that hydraphiles insert into the bilayer and disrupt the cell's osmotic balance, leading to cell death.