Kreander K, Vuorela P, Tammela P
Drug Discovery and Development Technology Center, Faculty of Pharmacy, University of Helsinki, Finland.
Folia Microbiol (Praha). 2005;50(6):487-93. doi: 10.1007/BF02931435.
A rapid and simple microdilution technique on 96-well microplate based on turbidimetry was optimized and validated for screening of antimicrobial activity against erythromycin-resistant bacterial strains of Streptococcus pyogenes and Staphylococcus simulans isolated from Finnish patients. Using S. pyogenes ATCC 12351 as reference strain the developed method was evaluated by reproducibility measurements and using parameters typically employed for screening methods, i.e. signal-to-background, signal-to-noise and a screening-window coefficient, the Z' factor. The method was further used for screening a group of natural compounds and their synthetic derivatives against resistant bacterial strains. Of these, octyl and dodecyl gallates, and usnic and ursolic acids were the most active. The described method is a rapid, homogeneous, cost-effective and easy-to-perform system for screening of new potential antimicrobial agents in drug discovery.
基于比浊法的96孔微孔板快速简便微量稀释技术,经优化和验证后用于筛选对从芬兰患者中分离出的耐红霉素化脓性链球菌和模仿葡萄球菌菌株的抗菌活性。以化脓性链球菌ATCC 12351作为参考菌株,通过重复性测量以及使用筛选方法通常采用的参数,即信号背景比、信噪比和筛选窗口系数Z'因子,对所开发的方法进行了评估。该方法还进一步用于筛选一组天然化合物及其合成衍生物对耐药菌株的抗菌活性。其中,没食子酸辛酯和十二烷基酯以及松萝酸和熊果酸活性最强。所描述的方法是一种快速、均相、经济高效且易于操作的系统,用于在药物研发中筛选新的潜在抗菌剂。