Abstract：
BACKGROUND: Paulownia tomentosa Steud. (P. tomentosa) is a medium-sized tree traditionally used in Chinese folk medicine for the treatment of infectious diseases. It is a rich source of prenylated phenolic compounds that have been extensively studied for their promising biological activities.
OBJECTIVE: Due to the increasing development of antibiotic resistance, our study investigated plant-derived natural products from the fruits of P. tomentosa that could control Staphylococcus aureus infections with novel targets/modes of action and reduce antimicrobial resistance.
METHODS: The ethanolic extract was fractionated and detected by liquid chromatography. The antistaphylococcal effects of the plant formulations were studied in detail in vitro by various biological methods, including microdilution methods for minimum inhibitory concentration (MIC), the checkerboard titration technique for synergy assay, fluorescence measurements for membrane disruption experiments, autoinducer-2-mediated bioassay for quorum sensing inhibition, and counting of colony-forming units for relative adhesion. Morphology was examined by transmission electron microscopy.
RESULTS: Total ethanolic extract and chloroform fraction showed MICs of 128 and 32 μg/mL, respectively. Diplacol, diplacone, and 3\'-O-methyl-5\'-hydroxydiplacone inhibited S. aureus growth in the range of 8-16 μg/mL. Synergistic potential was shown in combination with mupirocin and fusidic acid. The ethanolic extract and the chloroform fraction destroyed the cell membranes by 91.61% and 79.46%, respectively, while the pure compounds were less active. The ethanolic extract and the pure compounds reduced the number of adhered cells to 47.33-10.26% compared to the untreated control. All tested plant formulations, except diplacone, inhibited quorum sensing of S. aureus. Transmission electron microscopy showed deformation of S. aureus cells.
CONCLUSIONS: The products from the fruit of P. tomentosa showed antimicrobial properties against S. aureus alone and in combination with antibiotics. By affecting intracellular targets, geranylated flavonoids proposed novel approaches in the control of staphylococcal infections.
OBJECTIVE: Due to the increasing development of antibiotic resistance, our study investigated plant-derived natural products from the fruits of P. tomentosa that could control Staphylococcus aureus infections with novel targets/modes of action and reduce antimicrobial resistance.
METHODS: The ethanolic extract was fractionated and detected by liquid chromatography. The antistaphylococcal effects of the plant formulations were studied in detail in vitro by various biological methods, including microdilution methods for minimum inhibitory concentration (MIC), the checkerboard titration technique for synergy assay, fluorescence measurements for membrane disruption experiments, autoinducer-2-mediated bioassay for quorum sensing inhibition, and counting of colony-forming units for relative adhesion. Morphology was examined by transmission electron microscopy.
RESULTS: Total ethanolic extract and chloroform fraction showed MICs of 128 and 32 μg/mL, respectively. Diplacol, diplacone, and 3\'-O-methyl-5\'-hydroxydiplacone inhibited S. aureus growth in the range of 8-16 μg/mL. Synergistic potential was shown in combination with mupirocin and fusidic acid. The ethanolic extract and the chloroform fraction destroyed the cell membranes by 91.61% and 79.46%, respectively, while the pure compounds were less active. The ethanolic extract and the pure compounds reduced the number of adhered cells to 47.33-10.26% compared to the untreated control. All tested plant formulations, except diplacone, inhibited quorum sensing of S. aureus. Transmission electron microscopy showed deformation of S. aureus cells.
CONCLUSIONS: The products from the fruit of P. tomentosa showed antimicrobial properties against S. aureus alone and in combination with antibiotics. By affecting intracellular targets, geranylated flavonoids proposed novel approaches in the control of staphylococcal infections.
摘要：
背景：泡桐.(P.tomentosa）是一种中等大小的树，传统上用于中国民间医学，用于治疗传染病。它是异戊二烯化酚类化合物的丰富来源，因其有前途的生物活性而被广泛研究。
目的：由于抗生素耐药性的增加，我们的研究调查了植物来源的天然产物，这些产物可以用新的靶标/作用模式控制金黄色葡萄球菌感染，并降低抗菌素耐药性。
方法：将乙醇提取物分级分离并通过液相色谱法检测。通过各种生物学方法在体外详细研究了植物制剂的抗葡萄球菌作用，包括最小抑制浓度（MIC）的微量稀释方法，用于协同分析的棋盘滴定技术，膜破裂实验的荧光测量，用于群体感应抑制的自诱导物-2-介导的生物测定，并计算相对粘附的菌落形成单位。通过透射电子显微镜检查形态学。
结果：总乙醇提取物和氯仿部分显示出128和32μg/ml的MIC，分别。Diplacol,Diplacone,和3'-O-甲基-5'-羟基双取代酮在8-16μg/ml的范围内抑制金黄色葡萄球菌的生长。与莫匹罗星和夫西地酸组合显示出协同潜力。乙醇提取物和氯仿部分破坏细胞膜91.61%和79.46%，分别,而纯化合物的活性较低。与未处理的对照相比,乙醇提取物和纯化合物将粘附细胞的数量减少至47.33-10.26%。五种经过测试的植物配方，除了Diplacone,抑制金黄色葡萄球菌的群体感应。透射电镜显示金黄色葡萄球菌细胞变形。
结论：来自番茄果实的产品显示出单独抗金黄色葡萄球菌以及与抗生素组合的抗微生物特性。通过影响细胞内靶标，香叶黄酮提出了控制葡萄球菌感染的新方法。
目的：由于抗生素耐药性的增加，我们的研究调查了植物来源的天然产物，这些产物可以用新的靶标/作用模式控制金黄色葡萄球菌感染，并降低抗菌素耐药性。
方法：将乙醇提取物分级分离并通过液相色谱法检测。通过各种生物学方法在体外详细研究了植物制剂的抗葡萄球菌作用，包括最小抑制浓度（MIC）的微量稀释方法，用于协同分析的棋盘滴定技术，膜破裂实验的荧光测量，用于群体感应抑制的自诱导物-2-介导的生物测定，并计算相对粘附的菌落形成单位。通过透射电子显微镜检查形态学。
结果：总乙醇提取物和氯仿部分显示出128和32μg/ml的MIC，分别。Diplacol,Diplacone,和3'-O-甲基-5'-羟基双取代酮在8-16μg/ml的范围内抑制金黄色葡萄球菌的生长。与莫匹罗星和夫西地酸组合显示出协同潜力。乙醇提取物和氯仿部分破坏细胞膜91.61%和79.46%，分别,而纯化合物的活性较低。与未处理的对照相比,乙醇提取物和纯化合物将粘附细胞的数量减少至47.33-10.26%。五种经过测试的植物配方，除了Diplacone,抑制金黄色葡萄球菌的群体感应。透射电镜显示金黄色葡萄球菌细胞变形。
结论：来自番茄果实的产品显示出单独抗金黄色葡萄球菌以及与抗生素组合的抗微生物特性。通过影响细胞内靶标，香叶黄酮提出了控制葡萄球菌感染的新方法。
