Systematic exploration of natural and synthetic flavonoids for the inhibition of Staphylococcus aureus biofilms.
Systematic exploration of natural and synthetic flavonoids for the inhibition of Staphylococcus aureus biofilms.
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DOI：
10.3390/ijms141019434
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发表时间：
2013-09-25
影响因子：
5.6
通讯作者：
Fallarero A
中科院分区：
文献类型：
--
作者：
Manner S;Skogman M;Goeres D;Vuorela P;Fallarero A
当单细胞（或悬浮）细菌转变为生物膜生活方式时，它们对抗菌药物的敏感性降低，因此需要进行抗生物膜研究。类黄酮是研究最广泛的天然化合物之一，其生物活性声称数量空前。大多数研究集中于对悬浮细胞的抗菌作用；研究其抗生物膜特性的报告较少。这里，利用高通量表型平台筛选 500 种黄酮类化合物（包括天然和合成衍生物）对金黄色葡萄球菌生物膜的抑制活性。由于早期类黄酮抗菌研究的结果存在差异，当前的研究旨在最大限度地减少变异来源。第一次筛选后，类黄酮被分为非活性 (443)、中度活性 (47) 或高度活性 (10)。此外，结合生物活性和选择性的排除标准确定了两种合成黄烷是最有前途的。这里报告的数据主体有三个主要目的。首先，它为化学库的抗生物膜筛选提供了改进的方法工作流程，考虑到抗生物膜和抗菌特性之间的联系（很多时候被忽略）。这对于类黄酮和其他天然产物的研究尤其重要。其次，它提供了一个大型且免费的抗生物膜生物活性数据集，扩展了黄酮类化合物的知识，并为未来的结构-活性关系研究和结构优化铺平了道路。最后，它确定了两种新的黄烷，它们可以成功地作用于生物膜以及悬浮细菌，并代表更可行的抗菌候选物。
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.
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DOI：
10.1080/00021369.1985.10866749
发表时间：
1985-01-01
期刊：
AGRICULTURAL AND BIOLOGICAL CHEMISTRY
影响因子：
--
作者：
MIZOBUCHI, S;SATO, Y
通讯作者：
SATO, Y
影响因子：
3.5
作者：
Avila, Hugo Pereira;Albino Smania, Elza de Fatima;Junior, Artur Smania
通讯作者：
Junior, Artur Smania
影响因子：
5
作者：
Durig, Anna;Kouskoumvekaki, Irene;Klemm, Per
通讯作者：
Klemm, Per
影响因子：
7.3
作者：
McGovern, SL;Shoichet, BK
通讯作者：
Shoichet, BK
影响因子：
6.7
作者：
Cushnie, TPT;Hamilton, VES;Lamb, AJ
通讯作者：
Lamb, AJ