Sandy Gerschler , Sandra Maaß , Philip Gerth , Lukas Schulig , Toni Wildgrube , Jan Rockstroh , Martina Wurster , Karen Methling , Dörte Becher , Michael Lalk , Christian Schulze , Sebastian Guenther , Nadin Schultze
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Specific fractions of flavonoids and naphthoquinones, as well as individual substances like 7-methyljuglone and 2″-<em>O</em>-galloylhyperoside, are analyzed. Results show that naphthoquinones appear to act via central regulatory proteins such as OmpR and alter the stress response while flavonoids likely affect biofilm formation by creating an iron-poor environment through iron complexation and additionally influence polyamine balance, reducing intracellular spermidine levels. Further investigations including assays for iron complexation and analysis of polyamines confirmed the proteomic data. Safety evaluations through cytotoxicity tests in 3D cell cultures and the <em>Galleria mellonella in vivo</em> model confirm the safety of the extracts used. 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引用次数: 0
摘要
在复湿泥炭地成功地可持续栽培著名药用植物紫菜,不仅保护了自然种群,而且为该植物的可持续药用利用提供了基础。芥菜类黄酮和萘醌类生物活性化合物对多重耐药的产esbl大肠杆菌菌株显示出生物膜抑制特性,开辟了新的治疗可能性。本研究通过蛋白质组学分析探讨了这些化合物在生物膜抑制中的分子机制。分析了黄酮类化合物和萘醌的特定组分,以及7-甲基核桃苷和2″- o -没食子酰基金丝桃苷等个别物质。结果表明,萘醌似乎通过OmpR等中心调节蛋白起作用并改变应激反应,而黄酮类化合物可能通过铁络合产生缺铁环境来影响生物膜的形成,另外还影响多胺平衡,降低细胞内亚精胺水平。进一步的研究包括铁络合和多胺分析证实了蛋白质组学数据。通过在3D细胞培养物和mellonella体内模型中进行细胞毒性测试进行的安全性评估证实了所使用提取物的安全性。这些发现突出表明,芥菜是一种有前途的新型植物药物。
Drosera rotundifolia L. as E. coli biofilm inhibitor: Insights into the mechanism of action using proteomics/metabolomics and toxicity studies
The successful sustainable cultivation of the well-known medicinal plant sundew on rewetted peatlands not only leads to the preservation of natural populations, but also provides a basis for the sustainable pharmaceutical use of the plant. The bioactive compounds of sundew, flavonoids and naphthoquinones, show biofilm-inhibiting properties against multidrug-resistant, ESBL-producing E. coli strains and open up new therapeutic possibilities.
This study investigates the molecular mechanisms of these compounds in biofilm inhibition through proteomic analyses. Specific fractions of flavonoids and naphthoquinones, as well as individual substances like 7-methyljuglone and 2″-O-galloylhyperoside, are analyzed. Results show that naphthoquinones appear to act via central regulatory proteins such as OmpR and alter the stress response while flavonoids likely affect biofilm formation by creating an iron-poor environment through iron complexation and additionally influence polyamine balance, reducing intracellular spermidine levels. Further investigations including assays for iron complexation and analysis of polyamines confirmed the proteomic data. Safety evaluations through cytotoxicity tests in 3D cell cultures and the Galleria mellonella in vivo model confirm the safety of the extracts used. These findings highlight sundew as a promising candidate for new phytopharmaceuticals.