Drug Research Program, Division of Pharmaceutical Biosciences, Faculty of Pharmacy, University of Helsinki, Helsinki, Finland.
Drug Research Program, Division of Pharmaceutical Chemistry and Technology, Faculty of Pharmacy, University of Helsinki, Helsinki, Finland.
Biofouling. 2021 Aug;37(7):791-807. doi: 10.1080/08927014.2021.1971655. Epub 2021 Aug 30.
Antibacterial screenings are most commonly targeted at planktonic bacteria but less effort is dedicated to the exploration of agents acting on biofilms. Here, a natural compounds library was screened against using a 384-well plate platform to identify compounds preventing biofilm formation. Five structurally diverse hits were selected for follow-up studies: honokiol, tschimganidin, ferutinin, oridonin and deoxyshikonin. The compounds were evaluated against different bacterial species for their capacity to prevent and disrupt biofilms. The development of resistance and cytotoxicity were also investigated. Ferutinin displayed the best antibacterial activity, with a minimum inhibitory, bactericidal and biofilm preventive concentration of 25 µM against . It efficiently disrupted pre-formed biofilms (over 5-log reduction of viable cells) and reduced biofilm formation on a catheter in the presence of neutrophils. This work provides new information on the antibacterial activity of five natural compounds and identified ferutinin as a promising candidate against biofilms.
抗菌筛选最常用于浮游细菌，但对作用于生物膜的制剂的探索较少。在这里，使用 384 孔板平台对天然化合物库进行了筛选，以鉴定防止生物膜形成的化合物。选择了五个结构不同的命中物进行后续研究：厚朴酚、茨希曼宁、费鲁替尼、冬凌草素和去氧地锦草素。评估了这些化合物对不同细菌物种的能力，以防止和破坏生物膜。还研究了耐药性和细胞毒性的发展。费鲁替尼显示出最好的抗菌活性，对 的最小抑菌、杀菌和生物膜预防浓度为 25µM。它有效地破坏了预先形成的生物膜（活细胞减少超过 5 个对数），并在中性粒细胞存在的情况下减少导管上的生物膜形成。这项工作提供了关于五种天然化合物的抗菌活性的新信息，并确定费鲁替尼是一种有前途的针对 生物膜的候选药物。
