Department of Chemistry, Fudan University, 220 Handan Road, Shanghai 200433 (China).
Angew Chem Int Ed Engl. 2014 Apr 25;53(18):4578-81. doi: 10.1002/anie.201311249. Epub 2014 Mar 28.
Three new artificial transmembrane channel molecules have been designed and synthesized by attaching positively charged Arg-incorporated tripeptide chains to pillar[5]arene. Fluorescent and patch-clamp experiments revealed that voltage can drive the molecules to insert into and leave from a lipid bilayer and thus switch on and off the transport of K(+) ions. One of the molecules was found to display antimicrobial activity toward Bacillus subtilis with half maximal inhibitory concentration (IC50 ) of 10 μM which is comparable to that of natural channel-forming peptide alamethicin.
三种新型人工跨膜通道分子通过将带正电荷的 Arg 整合三肽链连接到[5]柱芳烃上而设计和合成。荧光和膜片钳实验表明，电压可以驱动分子插入和离开脂质双层，从而打开和关闭 K(+)离子的运输。其中一种分子被发现对枯草芽孢杆菌具有抗菌活性，其半最大抑制浓度（IC50）为 10 μM，与天然通道形成肽短杆菌素相当。
