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具有选择性抗菌活性的白藜芦醇-席夫碱杂化化合物:合成、生物活性及计算研究

Resveratrol-Schiff Base Hybrid Compounds with Selective Antibacterial Activity: Synthesis, Biological Activity, and Computational Study.

作者信息

Sánchez-González Rodrigo, Leyton Patricio, Aguilar Luis F, Reyna-Jeldes Mauricio, Coddou Claudio, Díaz Katy, Mellado Marco

机构信息

Instituto de Química, Facultad de Ciencias, Pontificia Universidad Católica de Valparaíso, Valparaíso 2373223, Chile.

Departamento de Ciencias Biomédicas, Facultad de Medicina, Universidad Católica del Norte, Coquimbo 1781421, Chile.

出版信息

Microorganisms. 2022 Jul 22;10(8):1483. doi: 10.3390/microorganisms10081483.

Abstract

Nowadays, antimicrobial resistance is a serious concern associated with the reduced efficacy of traditional antibiotics and an increased health burden worldwide. In response to this challenge, the scientific community is developing a new generation of antibacterial molecules. Contributing to this effort, and inspired by the resveratrol structure, five new resveratrol-dimers (9a−9e) and one resveratrol-monomer (10a) were synthetized using 2,5-dibromo-1,4-diaminobenzene (8) as the core compound for Schiff base bridge conformation. These compounds were evaluated in vitro against pathogenic clinical isolates of Pseudomonas aeruginosa, Staphylococcus aureus, Bacillus sp., and Listeria monocytogenes. Antibacterial activity measurements of resveratrol-Schiff base derivatives (9a−9e) and their precursors (4−8) showed high selectivity against Listeria monocytogenes, being 2.5 and 13.7 times more potent than chloramphenicol, while resveratrol showed an EC50 > 320 µg/mL on the same model. Moreover, a prospective mechanism of action for these compounds against L. monocytogenes strains was proposed using molecular docking analysis, finding a plausible inhibition of internalin C (InlC), a surface protein relevant in bacteria−host interaction. These results would allow for the future development of new molecules for listeriosis treatment based on compound 8.

摘要

如今,抗菌药物耐药性是一个严重问题,与传统抗生素疗效降低以及全球健康负担增加相关。为应对这一挑战,科学界正在研发新一代抗菌分子。在此过程中,受白藜芦醇结构启发,以2,5 - 二溴 - 1,4 - 二氨基苯(8)为席夫碱桥构象的核心化合物,合成了五种新的白藜芦醇二聚体(9a−9e)和一种白藜芦醇单体(10a)。对这些化合物针对铜绿假单胞菌、金黄色葡萄球菌、芽孢杆菌属和单核细胞增生李斯特菌的临床致病分离株进行了体外评估。白藜芦醇 - 席夫碱衍生物(9a−9e)及其前体(4−8)的抗菌活性测量结果显示,它们对单核细胞增生李斯特菌具有高选择性,其效力分别比氯霉素高2.5倍和13.7倍,而白藜芦醇在同一模型上的EC50 > 320 µg/mL。此外,通过分子对接分析提出了这些化合物针对单核细胞增生李斯特菌菌株的潜在作用机制,发现它们可能抑制内化素C(InlC),这是一种在细菌与宿主相互作用中起重要作用的表面蛋白。这些结果将有助于未来基于化合物8开发用于治疗李斯特菌病的新分子。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7374/9330556/b69d2b03a1f7/microorganisms-10-01483-g001.jpg

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