Vollaro Adriana, Esposito Anna, Antonaki Eleni, Iula Vita Dora, D'Alonzo Daniele, Guaragna Annalisa, De Gregorio Eliana
Department of Molecular Medicine and Medical Biotechnology, University of Naples Federico II, Via S. Pansini 5, 80131 Naples, Italy.
Department of Chemical Sciences, University of Naples Federico II, Via Cintia, 80126 Naples, Italy.
Microorganisms. 2020 Mar 25;8(4):468. doi: 10.3390/microorganisms8040468.
In this work, the antibacterial activity of deflazacort and several of its synthetic precursors was tested against a panel of bacterial pathogens responsible for most drug-resistant infections including spp., , , , , and spp. The derivative of deflazacort, PYED-1 (pregnadiene-11-hydroxy-16α,17α-epoxy-3,20-dione-1) showed the best antibacterial activity in a dose-dependent way. We focused on the action of PYED-1 against cells. PYED-1 exhibited an additive antimicrobial effect with gentamicin and oxacillin against the methicillin-resistant isolate 00717. In addition to its antimicrobial effect PYED-1 was found to repress the expression of several virulence factors of , including toxins encoded by the (alpha-haemolysin), (beta-haemolysin), (leucotoxins E-D), and (staphylococcal enterotoxin A) genes, and cell surface factors (fibronectin-binding protein B) and capC (capsule biosynthesis protein C)). The expression levels of autolysin isaA (immunodominant staphylococcal antigen) were also increased.
在这项研究中，对去氟可特及其几种合成前体针对一组导致大多数耐药性感染的细菌病原体进行了抗菌活性测试，这些病原体包括 菌属、 菌属、 菌属、 菌属、 菌属和 菌属。去氟可特的衍生物PYED-1（孕二烯-11-羟基-16α,17α-环氧-3,20-二酮-1）呈剂量依赖性地表现出最佳抗菌活性。我们重点研究了PYED-1对 细胞的作用。PYED-1与庆大霉素和苯唑西林对耐甲氧西林 分离株00717表现出相加抗菌作用。除了其抗菌作用外，还发现PYED-1可抑制 的几种毒力因子的表达，包括由 基因（α-溶血素）、 基因（β-溶血素）、 基因（白细胞毒素E-D）和 基因（葡萄球菌肠毒素A）编码的毒素，以及细胞表面因子（纤连蛋白结合蛋白B）和capC（荚膜生物合成蛋白C）。自溶素isaA（免疫显性葡萄球菌抗原）的表达水平也有所增加。
