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Systematic Exploration of Natural and Synthetic Flavonoids for the Inhibition of Staphylococcus aureus Biofilms
Pharmaceutical Sciences, Department of Biosciences, Abo Akademi University, Artillerigatan 6A, 3rd Floor, Biocity, Turku FI-20520, Finland
Center for Biofilm Engineering, Montana State University, Bozeman, MT 59717, USA
Division of Pharmaceutical Biology, Faculty of Pharmacy, University of Helsinki, Viikinkaari 5E, P.O. Box 56, Helsinki FI-00014, Finland
* Author to whom correspondence should be addressed.
Received: 14 August 2013; in revised form: 3 September 2013 / Accepted: 10 September 2013 / Published: 25 September 2013
Abstract: When single-cell (or suspended) bacteria switch into the biofilm lifestyle, they become less susceptible to antimicrobials, imposing the need for anti-biofilms research. Flavonoids are among the most extensively studied natural compounds with an unprecedented amount of bioactivity claims. Most studies focus on the antibacterial effects against suspended cells; fewer reports have researched their anti-biofilm properties. Here, a high throughput phenotypic platform was utilized to screen for the inhibitory activity of 500 flavonoids, including natural and synthetic derivatives, against Staphylococcus aureus biofilms. Since discrepancies among results from earlier antibacterial studies on flavonoids had been noted, the current study aimed to minimize sources of variations. After the first screen, flavonoids were classified as inactive (443), moderately active (47) or highly active (10). Further, exclusion criteria combining bioactivity and selectivity identified two synthetic flavans as the most promising. The body of data reported here serves three main purposes. First, it offers an improved methodological workflow for anti-biofilm screens of chemical libraries taking into account the (many times ignored) connections between anti-biofilm and antibacterial properties. This is particularly relevant for the study of flavonoids and other natural products. Second, it provides a large and freely available anti-biofilm bioactivity dataset that expands the knowledge on flavonoids and paves the way for future structure-activity relationship studies and structural optimizations. Finally, it identifies two new flavans that can successfully act on biofilms, as well as on suspended bacteria and represent more feasible antibacterial candidates.
Keywords: flavonoids; flavanones; flavans; Staphylococcus aureus; biofilms; antibacterial; bioactivity; chalcones; flavones
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MDPI and ACS Style
Manner, S.; Skogman, M.; Goeres, D.; Vuorela, P.; Fallarero, A. Systematic Exploration of Natural and Synthetic Flavonoids for the Inhibition of Staphylococcus aureus Biofilms. Int. J. Mol. Sci. 2013, 14, 19434-19451.
Manner S, Skogman M, Goeres D, Vuorela P, Fallarero A. Systematic Exploration of Natural and Synthetic Flavonoids for the Inhibition of Staphylococcus aureus Biofilms. International Journal of Molecular Sciences. 2013; 14(10):19434-19451.
Manner, Suvi; Skogman, Malena; Goeres, Darla; Vuorela, Pia; Fallarero, Adyary. 2013. "Systematic Exploration of Natural and Synthetic Flavonoids for the Inhibition of Staphylococcus aureus Biofilms." Int. J. Mol. Sci. 14, no. 10: 19434-19451.