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离子液体:新兴的抗菌剂。

Ionic Liquids: Emerging Antimicrobial Agents.

机构信息

Key Laboratory of Smart Drug Delivery of MOE, School of Pharmacy, Fudan University, Shanghai, 201203, China.

出版信息

Pharm Res. 2022 Oct;39(10):2391-2404. doi: 10.1007/s11095-022-03336-5. Epub 2022 Jul 25.

DOI:10.1007/s11095-022-03336-5
PMID:35879499
Abstract

Antimicrobial resistance has become a serious threat to global health. New antimicrobials are thus urgently needed. Ionic liquids (ILs), salts consisting of organic cations and anions with melting points less than 100°C, have been recently found to be promising in antimicrobial field as they may disrupt the bacterial wall and membrane and consequently lead to cell leakage and death. Different types of antimicrobial ILs are introduced in the review, including cationic, polymeric, and anionic ILs. Being the main type of the antimicrobial ILs, the review focuses on the structure and the antimicrobial mechanisms of cationic ILs. The quantitative structure-activity relationship (QSAR) models of the cationic ILs are also included. Increase in alkyl chain length and lipophilicity is beneficial to increase the antimicrobial effects of cationic ILs. Polymeric ILs are homopolymers of monomer ILs or copolymers of ILs and other monomers. They have great potential in the field of antibiotics as they provide stronger antimicrobial effects than the sum of the monomer ILs. Anionic ILs are composed of existing anionic antibiotics and organic cations, being capable to enhance the solubility and bioavailability of the original form. Nonetheless, the medical application of antimicrobial ILs is limited by the toxicity. The structural optimization aided by QSAR model and combination with existing antibiotics may provide a solution to this problem and expand the application range of ILs in antimicrobial field.

摘要

抗菌药物耐药性已成为全球健康的严重威胁,因此急需新的抗菌药物。最近发现,离子液体(ILs)作为一种有前途的抗菌物质,具有广阔的应用前景。ILs 是由熔点低于 100°C 的有机阳离子和阴离子组成的盐,它们可能破坏细菌的细胞壁和膜,从而导致细胞泄漏和死亡。本文综述了不同类型的抗菌 ILs,包括阳离子型、聚合型和阴离子型 ILs。阳离子型 ILs 作为主要的抗菌 ILs 类型,本文重点介绍了阳离子型 ILs 的结构和抗菌机制。还包括阳离子 ILs 的定量构效关系(QSAR)模型。烷基链长度和疏水性的增加有利于提高阳离子 ILs 的抗菌效果。聚合型 ILs 是单体 ILs 的均聚物或 ILs 和其他单体的共聚物。它们在抗生素领域具有巨大的潜力,因为它们提供的抗菌效果比单体 ILs 的总和更强。阴离子 ILs 由现有的阴离子抗生素和有机阳离子组成,能够提高原药的溶解度和生物利用度。然而,抗菌 ILs 的医学应用受到毒性的限制。QSAR 模型辅助的结构优化和与现有抗生素的结合可能为解决这一问题提供方案,并扩大 ILs 在抗菌领域的应用范围。

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