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共价键合的多壁碳纳米管-寡聚乙撑利奈唑胺缀合物的合成及其对细菌菌株的抗菌活性。

Synthesis of covalent bonding MWCNT-oligoethylene linezolid conjugates and their antibacterial activity against bacterial strains.

作者信息

Alatorre-Barajas José A, Alcántar-Zavala Eleazar, Gil-Rivas M Graciela, Estrada-Zavala Edgar, Ochoa-Terán Adrián, Gochi-Ponce Y, Montes-Ávila Julio, Cabrera Alberto, Trujillo-Navarrete Balter, Rivera-Lugo Yazmin Yorely, Alonso-Núñez Gabriel, Reynoso-Soto Edgar A, Medina-Franco J L

机构信息

Centro de Graduados e Investigación en Química, Tecnológico Nacional de México/ IT de Tijuana Tijuana B. C. Mexico

Facultad de Ciencias Químico Biológicas, Universidad Autónoma de Sinaloa Culiacán Sin Mexico.

出版信息

RSC Adv. 2021 Aug 31;11(46):28912-28924. doi: 10.1039/d1ra04691h. eCollection 2021 Aug 23.

DOI:10.1039/d1ra04691h
PMID:35478546
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9038137/
Abstract

Nowadays, infectious diseases caused by drug-resistant bacteria have become especially important. Linezolid is an antibacterial drug active against clinically important Gram positive strains; however, resistance showed by these bacteria has been reported. Nanotechnology has improved a broad area of science, such as medicine, developing new drug delivery and transport systems. In this work, several covalently bounded conjugated nanomaterials were synthesized from multiwalled carbon nanotubes (MWCNTs), a different length oligoethylene chain ( ), and two linezolid precursors (4 and 7), and they were evaluated in antibacterial assays. Interestingly, due to the intrinsic antibacterial activity of the amino-oligoethylene linezolid analogues, these conjugated nanomaterials showed significant antibacterial activity against various tested bacterial strains in a radial diffusion assay and microdilution method, including Gram negative strains as (11 mm, 6.25 μg mL) and (14 mm, ≤0.78 μg mL), which are not inhibited by linezolid. The results show a significant effect of the oligoethylene chain length over the antibacterial activity. Molecular docking of amino-oligoethylene linezolid analogs shows a more favorable interaction of the -7 analog in the PTC of .

摘要

如今，由耐药细菌引起的传染病变得尤为重要。利奈唑胺是一种对临床上重要的革兰氏阳性菌株有活性的抗菌药物；然而，已有报道称这些细菌会产生耐药性。纳米技术在医学等广泛的科学领域取得了进展，开发了新的药物递送和运输系统。在这项工作中，由多壁碳纳米管（MWCNT）、不同长度的低聚乙烯链（ ）和两种利奈唑胺前体（4和7）合成了几种共价键合的共轭纳米材料，并在抗菌试验中对它们进行了评估。有趣的是，由于氨基 - 低聚乙烯利奈唑胺类似物的固有抗菌活性，这些共轭纳米材料在径向扩散试验和微量稀释法中对各种测试细菌菌株表现出显著的抗菌活性，包括利奈唑胺无法抑制的革兰氏阴性菌株，如 （11毫米，6.25微克/毫升）和 （14毫米，≤0.78微克/毫升）。结果表明低聚乙烯链长度对抗菌活性有显著影响。氨基 - 低聚乙烯利奈唑胺类似物的分子对接显示 -7类似物在 的PTC中有更有利的相互作用。

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