Bernardi Thierry, Badel Stéphanie, Mayer Pascal, Groelly Jérome, de Frémont Pierre, Jacques Béatrice, Braunstein Pierre, Teyssot Marie-Laure, Gaulier Christelle, Cisnetti Federico, Gautier Arnaud, Roland Sylvain
Biofilm Control SAS, Biopôle Clermont-Limagne, 63360 Saint-Beauzire (France).
ChemMedChem. 2014 Jun;9(6):1140-4. doi: 10.1002/cmdc.201402012. Epub 2014 Apr 11.
A set of molecules including a majority of metal-N-heterocyclic carbene (NHC) complexes (metal=Ag, Cu, and Au) and azolium salts were evaluated by high-throughput screening of their activity against biofilm formation associated with pathogenic bacteria. The anti-planktonic effects were compared in parallel. Representative biofilm-forming strains of various genera were selected (Listeria, Pseudomonas, Staphylococcus, and Escherichia). All the compounds were tested at 1 mg L(-1) by using the BioFilm Ring Test. An information score (IS, sum of the activities) and an activity score (AS, difference between anti-biofilm and anti-planktonic activity) were determined from normalized experimental values to classify the most active molecules against the panel of bacterial strains. With this method we identified lipophilic Ag(I) and Cu(I) complexes possessing aromatic groups on the NHC ligand as the most efficient at inhibiting biofilm formation.
通过高通量筛选，对一组包含大多数金属-N-杂环卡宾（NHC）配合物（金属 = 银、铜和金）和唑盐的分子进行了评估，以检测它们对与病原菌相关的生物膜形成的活性。同时并行比较了它们的抗浮游菌效果。选择了各属代表性的生物膜形成菌株（李斯特菌、假单胞菌、葡萄球菌和大肠杆菌）。所有化合物均使用生物膜环试验在1 mg L(-1) 的浓度下进行测试。根据归一化实验值确定信息得分（IS，活性总和）和活性得分（AS，抗生物膜活性与抗浮游菌活性之差），以对针对该组细菌菌株的最具活性的分子进行分类。通过这种方法，我们确定了在NHC配体上具有芳基的亲脂性Ag(I)和Cu(I)配合物在抑制生物膜形成方面最为有效。
