Universidade Federal do Vale do São Francisco, Petrolina, Pernambuco 56300-000, Brazil.
Universidade Federal de Viçosa, Viçosa, Minas Gerais 36570-900, Brazil.
J Appl Microbiol. 2024 Apr 1;135(4). doi: 10.1093/jambio/lxae072.
The purpose was to evaluate the antimicrobial activity of highly soluble polypyrrole (Hs-PPy), alone or combined with oxacillin, as well as its antibiofilm potential against methicillin-resistant Staphylococcus aureus strains. Furthermore, the in silico inhibitory mechanism in efflux pumps was also investigated.
Ten clinical isolates of methicillin-resistant Staphylococcus aureus (MRSA) and two reference strains were used. Antimicrobial activity was determined by broth microdilution, and the combination effect with oxacillin was evaluated by the checkerboard assay. The biofilm formation capacity of MRSA and the interference of Hs-PPy were evaluated. The inhibitory action of Hs-PPy on the efflux pump was evaluated in silico through molecular docking. Hs-PPy showed activity against the isolates, with inhibitory action between 62.5 and 125 µg ml-1 and bactericidal action at 62.5 µg ml-1, as well as synergism in association with oxacillin. The isolates ranged from moderate to strong biofilm producers, and Hs-PPy interfered with the formation of this structure, but not with mature biofilm. There was no in silico interaction with the efflux protein EmrD, the closest homolog to NorA.
Hs-PPy interferes with biofilm formation by MRSA, has synergistic potential, and is an efflux pump inhibitor.
评估高溶解性聚吡咯（Hs-PPy）单独或与苯唑西林联合的抗菌活性，以及其针对耐甲氧西林金黄色葡萄球菌（MRSA）菌株的抗生物膜潜力。此外，还研究了其对外排泵的抑制作用的计算机制。
使用了 10 株临床分离的耐甲氧西林金黄色葡萄球菌（MRSA）和 2 株参考菌株。通过肉汤微量稀释法测定抗菌活性，并通过棋盘试验评估与苯唑西林的联合作用。评估了 MRSA 的生物膜形成能力和 Hs-PPy 的干扰作用。通过分子对接计算方法评估了 Hs-PPy 对外排泵的抑制作用。Hs-PPy 对分离株具有活性，其抑制作用在 62.5 和 125μg/ml 之间，杀菌作用在 62.5μg/ml，与苯唑西林联合具有协同作用。分离株的生物膜生成能力从中度到强，Hs-PPy 干扰了该结构的形成，但不干扰成熟的生物膜。与 NorA 最接近的同源物 EmrD 外排蛋白没有计算上的相互作用。
Hs-PPy 干扰 MRSA 生物膜的形成，具有协同作用，并且是外排泵抑制剂。
