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色酮衍生物CM3a通过抑制细胞黏附有效根除生物膜。

Chromone Derivatives CM3a Potently Eradicate Biofilms by Inhibiting Cell Adherence.

作者信息

Zhan Qing, Xu Yanlei, Zhan Lingling, Wang Bingjie, Guo Yinjuan, Wu Xiaocui, Ai Wenxiu, Song Zengqiang, Yu Fangyou

机构信息

Jiangxi Provincial Key Laboratory of Preventive Medicine, School of Public Health, Nanchang University, Nanchang, 330006, People's Republic of China.

Department of Laboratory Medicine, The First Affiliated Hospital of Wenzhou Medical University, Wenzhou, 325000, People's Republic of China.

出版信息

Infect Drug Resist. 2021 Mar 11;14:979-986. doi: 10.2147/IDR.S301483. eCollection 2021.

DOI:10.2147/IDR.S301483
PMID:33737820
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7961208/
Abstract

INTRODUCTION

The ability of to form biofilms is associated with high mortality and treatment costs. Established biofilms cannot be eradicated by many conventional antibiotics due to the development of antibiotic tolerance by . Here we report the synthesis and biological characterization of novel small-molecule compounds with antibiofilm activity. Chromone 5-maleimide substitution compounds (CM3a) showed favorable antibacterial activity against .

METHODS

CM3A with antibacterial activity was synthesized and screened. The minimum inhibitory concentration (MIC) of CM3a were determined by the broth microdilution method. Biofilm eradication assay and colony count methods were used to investigate the effect of CM3a on biofilm disruption and killing. Changes in biofilm architecture when subjected to CM3a, were visualized using confocal laser scanning microscopy (CLSM). CCK-8 assay and survival rate of larvae were used to test the toxicity of CM3a.

RESULTS

The minimum inhibitory concentration (MIC) of CM3a against was about 26.4 μM. Biofilm staining and laser scanning confocal microscopy analysis showed that CM3a eradicated biofilms by reducing the viability of the constituent bacterial cells. On the other hand, CM3a showed negligible toxicity against mouse alveolar epithelial cells and larvae.

CONCLUSION

Chromone derivatives CM3a has therapeutic potential as a safe and effective compound for the treatment of infection.

摘要

引言

形成生物膜的能力与高死亡率和治疗成本相关。由于[细菌名称]产生抗生素耐受性，已形成的生物膜无法被许多传统抗生素根除。在此，我们报告了具有抗生物膜活性的新型小分子化合物的合成及生物学特性。色酮5-马来酰亚胺取代化合物（CM3a）对[细菌名称]显示出良好的抗菌活性。

方法

合成并筛选具有抗菌活性的CM3A。采用肉汤微量稀释法测定CM3a的最低抑菌浓度（MIC）。使用生物膜根除试验和菌落计数方法研究CM3a对[细菌名称]生物膜破坏和杀灭的效果。使用共聚焦激光扫描显微镜（CLSM）观察CM3a作用后生物膜结构的变化。采用CCK-8法和[细菌名称]幼虫存活率测试CM3a的毒性。

结果

CM3a对[细菌名称]的最低抑菌浓度（MIC）约为26.4μM。生物膜染色和激光扫描共聚焦显微镜分析表明，CM3a通过降低组成细菌细胞的活力来根除[细菌名称]生物膜。另一方面，CM3a对小鼠肺泡上皮细胞和[细菌名称]幼虫显示出可忽略不计的毒性。

结论

色酮衍生物CM3a作为一种安全有效的化合物，在治疗[细菌名称]感染方面具有治疗潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/18dd/7961208/5207e044d49d/IDR-14-979-g0006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/18dd/7961208/c560d6535642/IDR-14-979-g0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/18dd/7961208/ad4bcbf150b3/IDR-14-979-g0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/18dd/7961208/6f5cf38cc6b9/IDR-14-979-g0003.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/18dd/7961208/78615d462205/IDR-14-979-g0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/18dd/7961208/5207e044d49d/IDR-14-979-g0006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/18dd/7961208/c560d6535642/IDR-14-979-g0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/18dd/7961208/ad4bcbf150b3/IDR-14-979-g0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/18dd/7961208/6f5cf38cc6b9/IDR-14-979-g0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/18dd/7961208/a06fdfa7593d/IDR-14-979-g0004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/18dd/7961208/78615d462205/IDR-14-979-g0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/18dd/7961208/5207e044d49d/IDR-14-979-g0006.jpg

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