阿司匹林共轭胆酸衍生物抗多种微生物感染和炎症。

IF 3.4 4区 医学 Q2 CHEMISTRY, MEDICINAL
ChemMedChem Pub Date : 2025-09-14 DOI:10.1002/cmdc.202500174
Sayed M Safwan, Devashish Mehta, Varsha Saini, Dolly Jain, Nikhil K Chourasiya, Amit Arora, Steffi Khatol, Mohit Singh, Vikas Verma, Avinash Bajaj
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引用次数: 0

摘要

由于传统抗生素的治疗效果有限,治疗由革兰氏阳性和革兰氏阴性细菌引起的伤口感染以及相关炎症仍然具有挑战性。利用胆酸衍生物的阳离子性、疏水性和结构适应性等独特性质,设计并合成了一种基于胆酸的新型阿司匹林衍生的易溶两亲化合物(amphiphile 1)。研究表明,两亲体1通过与细菌膜的脂壁酸和脂多糖等关键成分相互作用,发挥细菌膜干扰物的作用。研究发现,两亲体1可以降解源自革兰氏阳性菌和革兰氏阴性菌的单微生物和多微生物预先形成的生物膜。动物研究表明,以水凝胶为基础的两亲体1递送可有效减轻细菌感染并解决细菌相关炎症。总的来说,这些发现强调了两亲体1是解决多微生物感染挑战的假定治疗剂。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Aspirin-Conjugated Cholic Acid Derivative Combats Polymicrobial Infections and Inflammation.

Treating wound infections caused by Gram-positive and Gram-negative bacteria, along with associated inflammation, remains challenging due to the limited therapeutic efficacy of conventional antibiotics. Leveraging the unique properties of cholic acid derivatives, such as their cationic nature, hydrophobicity, and structural adaptability, a novel aspirin-derived facile amphiphile based on cholic acid (amphiphile 1) is designed and synthesized. The investigations reveal that the amphiphile 1 functions as a bacterial membrane disruptor through interacting with key components such as lipoteichoic acid and lipopolysaccharide of bacterial membranes. It is observed that amphiphile 1 can degrade both monomicrobial and polymicrobial preformed biofilms originating from Gram-positive and Gram-negative bacteria. Animal studies demonstrate that hydrogel-based delivery of amphiphile 1 effectively mitigates bacterial infections and resolves bacterial-associated inflammation. Collectively, these findings underscore that amphiphile 1 is a putative therapeutic agent for addressing the challenges of polymicrobial infections.

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来源期刊
ChemMedChem
ChemMedChem 医学-药学
CiteScore
6.70
自引率
2.90%
发文量
280
审稿时长
1 months
期刊介绍: Quality research. Outstanding publications. With an impact factor of 3.124 (2019), ChemMedChem is a top journal for research at the interface of chemistry, biology and medicine. It is published on behalf of Chemistry Europe, an association of 16 European chemical societies. ChemMedChem publishes primary as well as critical secondary and tertiary information from authors across and for the world. Its mission is to integrate the wide and flourishing field of medicinal and pharmaceutical sciences, ranging from drug design and discovery to drug development and delivery, from molecular modeling to combinatorial chemistry, from target validation to lead generation and ADMET studies. ChemMedChem typically covers topics on small molecules, therapeutic macromolecules, peptides, peptidomimetics, and aptamers, protein-drug conjugates, nucleic acid therapies, and beginning 2017, nanomedicine, particularly 1) targeted nanodelivery, 2) theranostic nanoparticles, and 3) nanodrugs. Contents ChemMedChem publishes an attractive mixture of: Full Papers and Communications Reviews and Minireviews Patent Reviews Highlights and Concepts Book and Multimedia Reviews.
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