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天然与合成双重活性化合物的抗菌与抗氧化活性。

Antibacterial and antioxidant activities for natural and synthetic dual-active compounds.

机构信息

Department of Chemistry "G. Ciamician", University of Bologna, Via Selmi 2, 40126, Bologna, Italy.

Department of Chemistry "G. Ciamician", University of Bologna, Via Selmi 2, 40126, Bologna, Italy.

出版信息

Eur J Med Chem. 2018 Oct 5;158:91-105. doi: 10.1016/j.ejmech.2018.09.009. Epub 2018 Sep 5.

Abstract

Antimicrobial resistance is widely recognized as a grave threat to global health in the 21st century, since the past decades have seen a dramatic increase in human-pathogenic bacteria that are resistant to one or multiple antibiotics. New antimicrobial agents are urgently required, particularly in the treatment of chronic infections such as cystic fibrosis, often associated with persistent colonization by drug-resistant pathogens and epithelial damage by pulmonary oxidative stress. In such events, it would be favourable to find agents that could have antioxidant and antibacterial activities combined in one molecule. The discovery of compounds that can show a dual-target activity considerably increased in the last years, reflecting the growing confidence that this new approach could lead to better therapeutic solutions for complex multigenic diseases. The aim of this review is to report those natural and synthetic compounds displaying significant antioxidant and antibacterial activities. In recent years there has been a growing attention on plant-derived antimicrobials as an alternative to antibiotics, for their efficacy and low tendency in developing bacterial resistance. Moreover, it was found that some natural products could enhance the activity of common antibiotics displaying a synergistic effect. We then report some selected synthetic compounds with an in-built capacity to act on two targets or with the combination in a single structure of two pharmacophores with antioxidant and antibacterial activities. Recent literature instances were screened and the most promising examples of dual-active antibacterial-antioxidant molecules were highlighted.

摘要

抗菌药物耐药性是 21 世纪全球健康面临的重大威胁,因为过去几十年中,人类致病菌对抗生素的耐药性急剧增加。迫切需要新的抗菌药物,特别是在治疗囊性纤维化等慢性感染方面,此类感染通常与耐药病原体的持续定植和肺部氧化应激引起的上皮损伤有关。在这种情况下,找到一种能够将抗氧化和抗菌活性结合在一个分子中的药物将是有利的。近年来,能够表现出双重靶向活性的化合物的发现大大增加,这反映出人们越来越相信这种新方法可以为复杂的多基因疾病带来更好的治疗解决方案。本文旨在报告那些具有显著抗氧化和抗菌活性的天然和合成化合物。近年来,植物来源的抗菌药物作为抗生素的替代品越来越受到关注,因为它们具有疗效好、细菌耐药性低的特点。此外,人们发现一些天然产物可以增强常见抗生素的活性,表现出协同作用。然后,我们报告了一些具有内在双重作用靶点能力的合成化合物,或者在一个结构中结合了具有抗氧化和抗菌活性的两个药效团。对最近的文献进行了筛选,并突出了具有双重活性的抗菌-抗氧化分子的最有前途的例子。

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