Leão Patrícia Virna Sales, Ferreira Ana Laura da Silva, Oliveira Felipe Araújo de Alcântara, Mesquita Avilnete Belém de Souza, Lima-Net José de Sousa, Gutierrez Stanley Juan Chavéz, Nogueira Carlos Emídio Sampaio, Cruz-Martins Natália, Arcanjo Daniel Dias Rufino, Barreto Humberto Medeiros, Lima Ferreira Josie Haydée
Laboratory of Research in Microbiology, Department of Parasitology and Microbiology, Federal University of Piaui, Teresina, Piauí, Brazil.
Department of Pharmacy, Federal University of Piauí, Teresina, Piauí, Brazil.
Evid Based Complement Alternat Med. 2023 Apr 8;2023:1780838. doi: 10.1155/2023/1780838. eCollection 2023.
is an important opportunistic pathogen that causes serious health-related infections, especially in intensive care units. The present study aimed to investigate the antimicrobial activity of Riparin-B (Rip-B) alone and in association with norfloxacin against multidrug-resistant clinical isolates of . For this, the minimum inhibitory concentrations were determined by the microdilution method. For the evaluation of resistance-modulating activity, MIC values for antibiotics were determined in the presence or absence of subinhibitory concentrations of Rip-B or chlorpromazine (CPZ). The AdeABC-AdeRS efflux system genes from these isolates were detected by PCR. Docking studies were also carried out to evaluate the interaction of Riparin-B and the AdeABC-AdeRS efflux system. The study was conducted from 2017 to 2019. The results showed that Rip-B showed weak intrinsic activity against the strains tested. On the other hand, Rip-B was able to modulate norfloxacin's response against strains that express efflux pump-mediated resistance. Docking studies provided projections of the interaction between Rip-B and EtBr with the AdeB protein, suggesting that Rip-B acts by competitive inhibition with the drug. Results found by in vitro and in silico assays suggest that Rip-B, in combination with norfloxacin, has the potential to treat infections caused by multidrug-resistant with efflux pump resistance.
是一种重要的机会致病菌，可引起严重的健康相关感染，尤其是在重症监护病房。本研究旨在调查瑞帕林 - B（Rip - B）单独以及与诺氟沙星联合对多重耐药临床分离株的抗菌活性。为此，采用微量稀释法测定最低抑菌浓度。为评估耐药调节活性，在存在或不存在亚抑菌浓度的Rip - B或氯丙嗪（CPZ）的情况下测定抗生素的MIC值。通过PCR检测这些分离株中的AdeABC - AdeRS外排系统基因。还进行了对接研究以评估瑞帕林 - B与AdeABC - AdeRS外排系统的相互作用。该研究于2017年至2019年进行。结果表明，Rip - B对所测试的菌株显示出较弱的内在活性。另一方面，Rip - B能够调节诺氟沙星对表达外排泵介导耐药性的菌株的反应。对接研究提供了Rip - B和溴化乙锭与AdeB蛋白之间相互作用的预测，表明Rip - B通过与药物的竞争性抑制起作用。体外和计算机模拟分析结果表明，Rip - B与诺氟沙星联合有潜力治疗由具有外排泵耐药性的多重耐药引起的感染。
