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暴露胆碱单元的抗菌纳米组装杯[4]芳烃抑制革兰氏阴性菌的生物膜形成和运动性

Antibacterial Nanoassembled Calix[4]arene Exposing Choline Units Inhibits Biofilm and Motility of Gram Negative Bacteria.

作者信息

Consoli Grazia Maria Letizia, Granata Giuseppe, Ginestra Giovanna, Marino Andreana, Toscano Giovanni, Nostro Antonia

机构信息

Institute of Biomolecular Chemistry-C.N.R., Catania 95126, Italy.

Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, Messina 98122, Italy.

出版信息

ACS Med Chem Lett. 2022 May 10;13(6):916-922. doi: 10.1021/acsmedchemlett.2c00015. eCollection 2022 Jun 9.

Abstract

The high incidence of antibiotic resistance and biofilm-associated infections is still a major cause of morbidity and mortality and triggers the need for new antimicrobial drugs and strategies. Nanotechnology is an emerging approach in the search for novel antimicrobial agents. The aim of this study was to investigate the inherent antibacterial effects of a self-assembling amphiphilic choline-calix[4]arene derivative () against Gram negative bacteria. showed activity against and , including antibiotic-resistant strains, and affected the bacterial biofilm and motility. The activity is likely related to the amphipathicity and cationic surface of nanoassembly that can establish large contact interactions with the bacterial surface. appears to be a promising candidate in the search for novel nanosized nonconventional antimicrobials.

摘要

抗生素耐药性和生物膜相关感染的高发生率仍然是发病和死亡的主要原因,并引发了对新型抗菌药物和策略的需求。纳米技术是寻找新型抗菌剂的一种新兴方法。本研究的目的是研究一种自组装两亲性胆碱杯[4]芳烃衍生物()对革兰氏阴性菌的固有抗菌作用。对和显示出活性,包括抗生素耐药菌株,并影响细菌生物膜和运动性。该活性可能与纳米组装体的两亲性和阳离子表面有关,其可与细菌表面建立大量接触相互作用。在寻找新型纳米尺寸非常规抗菌剂方面似乎是一个有前景的候选者。

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