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一类新型合成三环类黄酮的抗菌活性及作用机制探讨

Antibacterial activity and proposed action mechanism of a new class of synthetic tricyclic flavonoids.

作者信息

Babii C, Bahrin L G, Neagu A-N, Gostin I, Mihasan M, Birsa L M, Stefan M

机构信息

Faculty of Biology, Biology Department, The Alexandru Ioan Cuza University of Iasi, Iasi, Romania.

Faculty of Chemistry, The Alexandru Ioan Cuza University of Iasi, Iasi, Romania.

出版信息

J Appl Microbiol. 2016 Mar;120(3):630-7. doi: 10.1111/jam.13048. Epub 2016 Feb 9.

DOI:10.1111/jam.13048
PMID:26744255
Abstract

AIMS

This study reports on the inhibitory and bactericidal properties of a new synthetized flavonoid.

METHODS AND RESULTS

Tricyclic flavonoid 1 has been synthesized through a two-step reaction sequence. The antimicrobial effects were tested using the minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) assays. Also DNA fragmentation assay, fluorescence microscopy and SEM were used to study the mechanism of action. Our tested flavonoid displayed a strong antimicrobial activity with MIC and MBC values as low as 0·24 μg ml(-1) against Staphylococcus aureus and 3·9 μg ml(-1) against Escherichia coli. Flavonoid 1 displayed antimicrobial properties, causing not only the inhibition of bacterial growth, but also killing bacterial cells. The mechanism of action is related to the impairment of the cell membrane integrity and to cell agglutination.

CONCLUSIONS

Tricyclic flavonoid 1 was found to have a stronger antibacterial effect at lower concentrations than those described in the earlier reports.

SIGNIFICANCE AND IMPACT OF THE STUDY

Based on the strong antimicrobial activity observed, this new tricyclic flavonoid has a good potential for the design of new antimicrobial agents.

摘要

目的

本研究报告一种新合成黄酮类化合物的抑菌和杀菌特性。

方法与结果

通过两步反应序列合成了三环黄酮1。使用最低抑菌浓度(MIC)和最低杀菌浓度(MBC)测定法测试抗菌效果。还采用DNA片段化测定、荧光显微镜和扫描电子显微镜研究其作用机制。我们测试的黄酮类化合物表现出强大的抗菌活性,对金黄色葡萄球菌的MIC和MBC值低至0·24μg/ml,对大肠杆菌的MIC和MBC值低至3·9μg/ml。黄酮1具有抗菌特性,不仅能抑制细菌生长,还能杀死细菌细胞。其作用机制与细胞膜完整性受损和细胞凝集有关。

结论

发现三环黄酮1在较低浓度下比早期报告中描述的具有更强的抗菌作用。

研究的意义和影响

基于观察到的强大抗菌活性,这种新的三环黄酮类化合物在设计新型抗菌剂方面具有良好潜力。

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