Centro Singular de Investigación en Química Biolóxica e, Materiais Moleculares (CIQUS), Departamento de Química Orgánica, Universidade de Santiago de Compostela, 15782, Santiago de Compostela, Spain.
Department of Microbiology and Parasitology, Medical School, University of Santiago de Compostela, 15782, Santiago de Compostela, Spain.
Chemistry. 2021 Feb 10;27(9):3029-3038. doi: 10.1002/chem.202004127. Epub 2020 Nov 30.
A new class of amphipathic cyclic peptides, which assemble in bacteria membranes to form polymeric supramolecular nanotubes giving them antimicrobial properties, is described. The method is based on the use of two orthogonal clickable transformations to incorporate different hydrophobic or hydrophilic moieties in a simple, regioselective, and divergent manner. The resulting cationic amphipathic cyclic peptides described in this article exhibit strong antimicrobial properties with a broad therapeutic window. Our studies suggest that the active form is the nanotube resulted from the parallel stacking of the cyclic peptide precursors. Several techniques, CD, FTIR, fluorescence, and STEM, among others, confirm the nanotube formation.
一种新的两亲性环状肽类，在细菌膜中组装形成具有抗菌性能的聚合超分子纳米管，本文对此进行了描述。该方法基于使用两种正交点击反应，以简单、区域选择性和发散的方式将不同的疏水性或亲水性部分引入到环状肽中。本文所描述的阳离子两亲性环状肽具有很强的抗菌活性和较宽的治疗窗口。我们的研究表明，活性形式是环状肽前体平行堆积形成的纳米管。几种技术，如 CD、FTIR、荧光和 STEM 等，证实了纳米管的形成。
