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新型富含阳离子氨基酸的短肽的探索:设计、固相肽合成、生物学评价及研究

Exploration of novel cationic amino acid-enriched short peptides: design, SPPS, biological evaluation and study.

作者信息

Chandole Prashant K, Pawar Tushar Janardan, Olivares-Romero José Luis, Tivari Sunil R, Garcia Lara Bianney, Patel Harun, Ahmad Iqrar, Delgado-Alvarado Enrique, Kokate Siddhant V, Jadeja Yashwantsinh

机构信息

Department of Chemistry, Marwadi University Rajkot-360003 Gujarat India

Red de Estudios Moleculares Avanzados, Instituto de Ecología A.C. Carretera Antigua a Coatepec 351 Xalapa 91073 Veracruz Mexico.

出版信息

RSC Adv. 2024 Jun 3;14(25):17710-17723. doi: 10.1039/d3ra08313f. eCollection 2024 May 28.

Abstract

Antimicrobial resistance (AMR) represents a critical challenge worldwide, necessitating the pursuit of novel approaches to counteract bacterial and fungal pathogens. In this context, we explored the potential of cationic amino acid-enriched short peptides, synthesized solid-phase methods, as innovative antimicrobial candidates. Our comprehensive evaluation assessed the antibacterial and antifungal efficacy of these peptides against a panel of significant pathogens, including , , , , , and . Utilizing molecular docking techniques, we delved into the molecular interactions underpinning the peptides' action against these microorganisms. The results revealed a spectrum of inhibitory activities, with certain peptide sequences displaying pronounced effectiveness across various pathogens. These findings underscore the peptides' potential as promising antimicrobial agents, with molecular docking offering valuable insights into their mechanisms of action. This study enriches antimicrobial peptide (AMP) research by identifying promising candidates for further refinement and development toward therapeutic application, highlighting their significance in addressing the urgent issue of AMR.

摘要

抗菌耐药性(AMR)是全球面临的一项严峻挑战,因此有必要寻求新的方法来对抗细菌和真菌病原体。在此背景下,我们探索了通过固相方法合成的富含阳离子氨基酸的短肽作为新型抗菌候选物的潜力。我们的综合评估测定了这些肽对一系列重要病原体的抗菌和抗真菌功效,这些病原体包括 、 、 、 、 以及 。利用分子对接技术,我们深入研究了这些肽作用于这些微生物的分子相互作用。结果揭示了一系列抑制活性,某些肽序列对多种病原体表现出显著的有效性。这些发现强调了这些肽作为有前景的抗菌剂的潜力,分子对接为其作用机制提供了有价值的见解。本研究通过鉴定有前景的候选物以进一步优化和开发用于治疗应用,丰富了抗菌肽(AMP)研究,突出了它们在解决AMR这一紧迫问题中的重要性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c43a/11145139/a72c4cf8af05/d3ra08313f-f8.jpg

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