Manzanelli Franco A, Clemente Camila M, Campagno Luciana P, Beltramo Dante M, Robledo Sara M, Ravetti Soledad, Garro Ariel G
Centro de Investigaciones y Transferencia de Villa María (CIT VM), Villa María, Argentina.
Departamento de Química Biológica, Facultad de Ciencias Exactas y Naturales, Universidad de Buenos Aires (FCEyN-UBA) e Instituto de Química Biológica de la Facultad de Ciencias Exactas y Naturales (IQUIBICEN) CONICET, Ciudad de Buenos Aires, Argentina.
Future Microbiol. 2025 Apr;20(5):395-407. doi: 10.1080/17460913.2025.2475639. Epub 2025 Mar 9.
To evaluate the antibacterial and antibiofilm activities of sodium ibuprofenate (NaI) and its hypertonic variant (NaIHS) against multidrug-resistant Gram-negative bacteria (MDR-GNB) and explore their potential to inhibit β-lactamase enzymes.
Antibacterial activity was assessed using minimum inhibitory concentration (MIC), minimum bactericidal concentration (MBC), and time-kill assays. Antibiofilm activity was evaluated by measuring bacterial viability and biomass reduction in preformed biofilms. Scanning electron microscopy (SEM) was used to observe membrane effects. Molecular docking and molecular dynamics simulations were conducted to analyze the binding affinity of ibuprofen to the active sites of β-lactamases (CTX-M-15, KPC-2, OXA-23).
NaI exhibited bactericidal activity at concentrations of 25-75 mm, with being the most susceptible. NaCl (≥0.5 M) enhanced bactericidal efficacy and lowered MBCs. Time-kill assays indicated rapid bacterial eradication within 2 hours, with NaIHS achieving similar results at lower concentrations. SEM confirmed membrane disruption. Both formulations reduced bacterial viability in biofilms, with NaIHS showing greater efficiency. studies suggest ibuprofen may inhibit β-lactamases, with enhanced interactions in saline environments.
Sodium ibuprofenate, particularly in its hypertonic form, demonstrates strong antibacterial, antibiofilm, and potential β-lactamase inhibitory activity, making it a promising candidate for treating MDR-GNB infections.
评估布洛芬钠（NaI）及其高渗变体（NaIHS）对多重耐药革兰氏阴性菌（MDR - GNB）的抗菌和抗生物膜活性，并探索其抑制β - 内酰胺酶的潜力。
使用最低抑菌浓度（MIC）、最低杀菌浓度（MBC）和时间 - 杀菌试验评估抗菌活性。通过测量成熟生物膜中细菌活力和生物量减少来评估抗生物膜活性。使用扫描电子显微镜（SEM）观察膜效应。进行分子对接和分子动力学模拟以分析布洛芬与β - 内酰胺酶（CTX - M - 15、KPC - 2、OXA - 23）活性位点的结合亲和力。
NaI在浓度为25 - 75 mM时表现出杀菌活性，其中[具体细菌名称未给出]最敏感。NaCl（≥0.5 M）增强了杀菌效果并降低了MBC。时间 - 杀菌试验表明在2小时内可快速根除细菌，NaIHS在较低浓度下也取得了类似结果。SEM证实了膜破坏。两种制剂均降低了生物膜中的细菌活力，NaIHS显示出更高的效率。[此处原文不完整，推测是相关研究]表明布洛芬可能抑制β - 内酰胺酶，在盐环境中相互作用增强。
布洛芬钠，特别是其高渗形式，表现出强大的抗菌、抗生物膜和潜在的β - 内酰胺酶抑制活性，使其成为治疗MDR - GNB感染的有前途的候选药物。
