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硝酮查耳酮和戊基咖啡酸酯对医院病原体的抗菌活性导致微生物黏附减少和生物膜形成减少。

Antimicrobial activity of nitrochalcone and pentyl caffeate against hospital pathogens results in decreased microbial adhesion and biofilm formation.

机构信息

a Department of Physiological Sciences , Piracicaba Dental School, University of Campinas , Piracicaba , SP , Brazil.

b Department of Chemistry and Environmental Sciences , Júlio de Mesquita Filho University , São Jose do Rio Preto , Brazil.

出版信息

Biofouling. 2019 Feb;35(2):129-142. doi: 10.1080/08927014.2019.1574763. Epub 2019 Apr 5.

Abstract

The present study investigated the antimicrobial, anti-adhesion and anti-biofilm activity of the modified synthetic molecules nitrochalcone (NC-E05) and pentyl caffeate (C5) against microorganisms which have a high incidence in hospital-acquired infections. The compounds were further tested for their preliminary systemic toxicity in vivo. NC-E05 and C5 showed antimicrobial activity, with minimum inhibitory concentrations (MICs) ranging between 15.62 and 31.25 μg ml. Treatment with NC-E05 and C5 at 1 × MIC and/or 10 × MIC significantly reduced mono or mixed-species biofilm formation and viability. At MIC/2, the compounds decreased microbial adhesion to HaCaT keratinocytes from 1 to 3 h (p < 0.0001). In addition, NC-E05 and C5 demonstrated low toxicity in vivo in the Galleria mellonella model at anti-biofilm concentrations. Thus, the chemical modification of these molecules proved to be effective in the proposed anti-biofilm activity, opening opportunities for the development of new antimicrobials.

摘要

本研究调查了经修饰的合成分子硝基查耳酮(NC-E05)和戊基咖啡酸酯(C5)对医院获得性感染中高发微生物的抗菌、抗黏附和抗生物膜活性。进一步测试了这些化合物的体内初步全身毒性。NC-E05 和 C5 表现出抗菌活性,最小抑菌浓度(MIC)范围在 15.62 至 31.25μg/ml 之间。用 1×MIC 和/或 10×MIC 的 NC-E05 和 C5 处理可显著降低单种或混合物种生物膜的形成和活力。在 MIC/2 时,化合物将微生物对 HaCaT 角质形成细胞的黏附从 1 小时减少到 3 小时(p<0.0001)。此外,NC-E05 和 C5 在抗生物膜浓度的大蜡螟模型中表现出低体内毒性。因此,这些分子的化学修饰在拟议的抗生物膜活性中被证明是有效的,为开发新的抗菌药物开辟了机会。

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