Division of Pharmaceutical Biology, Faculty of Pharmacy, P. O. Box 56 (Biocenter 1), FIN-00014 University of Helsinki, Finland.
Z Naturforsch C J Biosci. 2011 Nov-Dec;66(11-12):562-70. doi: 10.1515/znc-2011-11-1205.
We report the antimicrobial activity of formylchromones. These compounds are remote structural analogues of nalidixic acid and quinolone antibiotics, and their activity was investigated by a simple micro-scale method designed for the determination of minimal inhibitory concentrations (MIC) of drug candidates and antibiotics against aerobic bacteria and yeasts. Minimal bactericidal and fungicidal concentrations (MBC and MFC, respectively) were also determined in connection with the MIC determinations. The results obtained were compared with those obtained using classical agar diffusion methodology. In the MIC method, deep-well micro-titration plates are used, covered by silicone sealing mats that allow diffusion of oxygen to the wells. The appropriate broth is pipetted into the wells, followed by a standardized microbial suspension (except for sterile controls) and a dilution series of the test substance or control antibiotic or a mere control solvent. The use of white non-transparent polypropylene plates allows easy visual inspection of microbial growth. For the MBC and MFC methods, samples are taken from all wells that contain a test substance or control antibiotic and do not display growth in the MIC test. The samples are streaked on agar plates, the liquid is allowed to absorb into the agar, and finally the microbes are spread all over the plate with a bent rod. Colony counts are compared with that of the untreated microbial suspension at the beginning of the MIC test. The MIC method is suitable for high-throughput screening.
我们报告了甲酰基色酮的抗菌活性。这些化合物是萘啶酸和喹诺酮类抗生素的远程结构类似物，其活性通过一种简单的微尺度方法进行了研究，该方法旨在确定候选药物和抗生素对需氧细菌和酵母菌的最小抑菌浓度 (MIC)。还与 MIC 测定一起确定了最小杀菌和最小抑菌浓度 (MBC 和 MFC)。将获得的结果与使用经典琼脂扩散方法学获得的结果进行了比较。在 MIC 方法中，使用深孔微量滴定板，并用硅酮密封垫覆盖，以允许氧气扩散到孔中。将适当的肉汤吸到孔中，然后加入标准化的微生物悬浮液（无菌对照除外）和测试物质或对照抗生素的稀释系列，或者仅进行对照溶剂处理。使用白色不透明的聚丙烯板可轻松目视检查微生物的生长。对于 MBC 和 MFC 方法，从所有含有测试物质或对照抗生素且在 MIC 测试中未显示生长的孔中取样。将样品划线接种在琼脂平板上，让液体吸收到琼脂中，最后用弯曲的棒将微生物散布在平板上。将菌落计数与 MIC 测试开始时未经处理的微生物悬浮液的菌落计数进行比较。MIC 方法适用于高通量筛选。
