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外排泵抑制作用及由及其香豆素类化合物介导的耐药性调节。 (原文表述不太完整准确,翻译可能会稍显生硬,推测原文可能有缺失部分信息)

Efflux Pump Inhibition and Resistance Modulation in by and Its Coumarins.

作者信息

Šimunović Katarina, Solnier Julia, Alperth Fabian, Kunert Olaf, Smole Možina Sonja, Bucar Franz

机构信息

Department of Pharmacognosy, Institute of Pharmaceutical Sciences, University of Graz, Beethovenstraße 8, 8010 Graz, Austria.

Department of Food Science and Technology, Biotechnical Faculty, University of Ljubljana, Jamnikarjeva 101, 1000 Ljubljana, Slovenia.

出版信息

Antibiotics (Basel). 2021 Sep 5;10(9):1075. doi: 10.3390/antibiotics10091075.

Abstract

Antibiotic resistance is a growing problem and may become the next major global health crisis if no timely actions are taken. Mycobacterial infections are widespread and, due to antibiotic resistance, also hard to treat and a major cause of mortality. Natural compounds have the potential to increase antibiotic effectiveness due to their resistance modulatory and antimicrobial effects. In this study, extracts, fractions, and isolated compounds were investigated regarding their antimicrobial and resistance-modulatory effects as well as efflux pump inhibition in   extracts were found to have anti-mycobacterial potential and resistance modulating effects on ethidium bromide activity. The major antibacterial effect was attributed to ostruthin, and we found that the more lipophilic the substrate, the greater the antimicrobial effect. Imperatorin caused potent modulatory effects by interfering with the action of the major LfrA efflux pump in . The plant has a complex effect on including antibacterial, efflux pump inhibition, resistance modulation, and membrane permeabilization, and its major constituents, ostruthin and imperatorin, have a distinct role in these effects. This makes and its coumarins promising therapeutics to consider in the fight against drug-resistant mycobacteria.

摘要

抗生素耐药性是一个日益严重的问题,如果不及时采取行动,可能会成为下一个重大的全球健康危机。分枝杆菌感染广泛存在,并且由于抗生素耐药性,也难以治疗,是导致死亡的主要原因。天然化合物由于其耐药性调节和抗菌作用,有可能提高抗生素的有效性。在本研究中,对提取物、馏分和分离出的化合物的抗菌和耐药性调节作用以及在[具体实验对象]中的外排泵抑制作用进行了研究。发现提取物具有抗分枝杆菌潜力,并对溴化乙锭活性有耐药性调节作用。主要的抗菌作用归因于蛇床素,并且我们发现底物的亲脂性越强,抗菌作用越大。欧前胡素通过干扰[具体菌株]中主要的LfrA外排泵的作用而产生有效的调节作用。该植物对[具体实验对象]具有复杂的作用,包括抗菌、外排泵抑制、耐药性调节和膜通透性增加,其主要成分蛇床素和欧前胡素在这些作用中发挥着不同的作用。这使得该植物及其香豆素类化合物有望成为对抗耐药分枝杆菌的治疗药物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fc12/8472667/4c3861a55862/antibiotics-10-01075-g001.jpg

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