Kincses Annamária, Ghazal Tasneem Sultan Abu, Veres Katalin, Spengler Gabriella, Hohmann Judit
Institute of Pharmacognosy, University of Szeged, Szeged, Hungary.
Department of Medical Microbiology, Albert Szent-Györgyi Health Center and Albert Szent-Györgyi Medical School, University of Szeged, Szeged, Hungary.
Pharm Biol. 2025 Dec;63(1):402-410. doi: 10.1080/13880209.2025.2511805. Epub 2025 Jun 2.
Antibiotic resistance in bacteria is a growing global problem, with biofilm formation and efflux pumps playing crucial roles in this issue.
This study explores the effects of phenolic compounds of against and methicillin-resistant (MRSA) strains by inhibiting biofilm formation and efflux pumps.
The methanolic extract of was fractionated guided by an antibiofilm assay, and the active fractions were analyzed by multistep chromatographic separation to yield five pure compounds. Their structures were then determined using 1D and 2D nuclear magnetic resonance spectroscopy. The minimum inhibitory concentrations of the extracts, fractions, and isolated compounds were determined the microdilution method in a 96-well plate. Antibiofilm activity was assessed using the crystal violet method, and the effect on efflux pumps was tested by a real-time ethidium bromide accumulation assay.
Arbutin (), apigenin 7--glucoside (), 6'-caffeoylarbutin (), rosmarinic acid (), and 2-deoxy-d-1,4-ribonolactone () were isolated from the aqueous methanolic extract. Compounds , , and reduced biofilm formation by 24.82%-42.98% at 100 µM, whereas only arbutin () moderately suppressed biofilm formation of MRSA (23.15 ± 1.56% at 50 µM). Arbutin also demonstrated efflux pump inhibitory activity against MRSA (relative fluorescence index of 0.49 at 100 µM).
The newly discovered natural antibiofilm agents show promise as candidates for treating biofilm-associated infections and combating antibiotic-resistant bacteria.
细菌中的抗生素耐药性是一个日益严重的全球性问题，生物膜形成和外排泵在这个问题中起着关键作用。
本研究通过抑制生物膜形成和外排泵，探讨酚类化合物对金黄色葡萄球菌和耐甲氧西林金黄色葡萄球菌（MRSA）菌株的影响。
以抗生物膜试验为指导，对[植物名称]的甲醇提取物进行分离，通过多步色谱分离对活性组分进行分析，得到五种纯化合物。然后使用一维和二维核磁共振光谱确定它们的结构。采用96孔板微量稀释法测定提取物、组分和分离化合物的最低抑菌浓度。使用结晶紫法评估抗生物膜活性，并通过实时溴化乙锭积累试验测试对外排泵的影响。
从甲醇水提取物中分离出熊果苷（）、芹菜素7 - [葡萄糖苷名称]（）、6'-咖啡酰熊果苷（）、迷迭香酸（）和2 - 脱氧 - d - 1,4 - 核糖内酯（）。化合物[具体化合物编号]、[具体化合物编号]和[具体化合物编号]在100 μM时可使金黄色葡萄球菌生物膜形成减少24.82% - 42.98%，而只有熊果苷（）在50 μM时适度抑制MRSA生物膜形成（23.15 ± 1.56%）。熊果苷还对MRSA表现出外排泵抑制活性（100 μM时相对荧光指数为0.49）。
新发现的天然抗生物膜剂有望成为治疗生物膜相关感染和对抗耐药细菌的候选药物。
