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