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A novel fluorescent probe for the detection of AmpC beta-lactamase and the application in screening beta-lactamase inhibitors
Spectrochimica Acta Part A: Molecular and Biomolecular Spectroscopy ( IF 4.3 ) Pub Date : 2020-03-14 , DOI: 10.1016/j.saa.2020.118257
Pan Yu , Jia-Ning Yang , Jin-Wu Yan , Zhi-Zhong Meng , W. David Hong , Adam P. Roberts , Stephen A. Ward , Lei Zhang , Shan Li

The rapid detection of β-lactamases (Blas) and effective screening of Bla inhibitors are critically important and urgent for solving antibiotic resistance and improving precision medicine. Here a novel fluorescent probe CDC-559 was designed and synthesized, which can be used for the selective and direct detection of AmpC Blas. More importantly, it can realize screening the Bla inhibitors with sulbactam sodium and tazobactam as model compounds, and the half-maximal inhibitory concentration are 0.279 μM and 0.053 μM, respectively. CDC-559 can be applied not only to examine the resistance of the strains, but also to categorize its mode of action specifically, which is consistent with the essential result of the Blas. The research suggests that CDC-559 probe features its tremendous potential in the rapid detection of AmpC Blas as well as the strains with AmpC-encoded gene, which is instructive in promoting better antibiotic stewardship practices and developments.



中文翻译:

一种用于检测AmpCβ-内酰胺酶的新型荧光探针及其在筛选β-内酰胺酶抑制剂中的应用

快速检测β-内酰胺酶(Blas)和有效筛选Bla抑制剂对于解决抗生素耐药性和改善精密医学至关重要。本文设计并合成了新型荧光探针CDC-559,可用于AmpC Blas的选择性和直接检测。更重要的是,它可以实现以舒巴坦钠和他唑巴坦为模型化合物筛选Bla抑制剂,其最大半数抑制浓度分别为0.279μM和0.053μM。CDC-559不仅可以用于检查菌株的抗性,而且可以特别地对其作用方式进行分类,这与Blas的基本结果一致。研究表明,CDC-559 该探针在快速检测AmpC Blas以及带有AmpC编码基因的菌株中具有巨大的潜力,这对促进更好的抗生素管理实践和开发具有指导意义。

更新日期:2020-03-16
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