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基于胆汁酸的抗菌剂的最新进展。

Recent Progress in Bile Acid-Based Antimicrobials.

机构信息

School of Materials Science and Engineering, South China University of Technology, Guangzhou 510641, China.

National Engineering Research Center for Tissue Restoration and Reconstruction, South China University of Technology, Guangzhou 510006, China.

出版信息

Bioconjug Chem. 2021 Mar 17;32(3):395-410. doi: 10.1021/acs.bioconjchem.0c00642. Epub 2021 Mar 8.

Abstract

With the emergence of drug-resistant bacteria and the formation of biofilms by bacteria and fungi, microbial infections gradually threaten global health. Natural antimicrobial peptides (AMPs) have low susceptibility for developing resistance due to the membrane targeted mechanism, but instability and high manufacturing cost limit their applications in clinic. Bile acids, a group of steroids in the human body, with high stability, biocompatibility, and inherent facial amphiphilic structure similar to the characteristics of AMPs, have been applied to the biological field, such as drug delivery systems, self-healing hydrogels, antimicrobials, and so on. In this review, we mainly focus on the different classes of bile acid-based antimicrobials in recent years. Various designs and methods for the preparation of unimolecular antimicrobials with bile acid skeletons are first introduced, including coupling of primary amine, quaternary ammonium, and amino acid units with bile acid skeletons. Some representative oligomeric antimicrobials, including dimers of bile acids, are summarized. Finally, macromolecular antimicrobials bearing some positive charges at the main chain or side chain and interaction mechanisms of these bile acid-based antimicrobials are discussed.

摘要

随着耐药菌的出现以及细菌和真菌形成生物膜,微生物感染逐渐威胁到全球健康。天然抗菌肽(AMPs)由于其靶向膜的作用机制,不易产生耐药性,但不稳定性和高制造成本限制了它们在临床上的应用。胆汁酸是人体中的一组甾体,具有高稳定性、生物相容性和与 AMPs 特征相似的固有两亲性结构,已被应用于生物领域,如药物传递系统、自修复水凝胶、抗菌剂等。在这篇综述中,我们主要关注近年来不同类型的基于胆汁酸的抗菌剂。首先介绍了具有胆汁酸骨架的单分子抗菌剂的各种设计和制备方法,包括与胆汁酸骨架偶联的伯胺、季铵和氨基酸单元。总结了一些有代表性的低聚物抗菌剂,包括胆汁酸二聚体。最后,讨论了带有主链或侧链正电荷的高分子抗菌剂和这些基于胆汁酸的抗菌剂的相互作用机制。

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