Schwan William R
Department of Microbiology, University of Wisconsin-La Crosse, 1725 State St., La Crosse, WI 54601, USA.
Antibiotics (Basel). 2023 Aug 30;12(9):1385. doi: 10.3390/antibiotics12091385.
Tuberculosis affects millions of people worldwide. The emergence of drug-resistant strains has made treatment more difficult. A drug discovery project initiated to screen natural products identified a lead stilbene compound, and structure function analysis of hundreds of analogs led to the discovery of the SK-03-92 stilbene lead compound with activity against several non-tuberculoid mycobacteria.
For this study, an MIC analysis and intracellular killing assay were performed to test SK-03-92 against grown in vitro as well as within murine macrophage cells.
The MIC analysis showed that SK-03-92 had activity against in the range of 0.39 to 6.25 μg/mL, including activity against single-drug-resistant strains. Further, an intracellular kill assay demonstrated that the SK-03-92 lead compound killed cells within murine macrophage cells.
Together, the data show the SK-03-92 lead compound can kill bacteria within mammalian macrophages.
结核病影响着全球数百万人。耐药菌株的出现使治疗更加困难。一个旨在筛选天然产物的药物发现项目鉴定出一种先导芪类化合物,对数百种类似物的结构功能分析导致发现了具有抗几种非结核分枝杆菌活性的SK-03-92芪类先导化合物。
在本研究中,进行了最低抑菌浓度(MIC)分析和细胞内杀伤试验,以测试SK-03-92对体外培养以及小鼠巨噬细胞内生长的(某种菌,原文未明确)的作用。
MIC分析表明,SK-03-92对(某种菌,原文未明确)的活性在0.39至6.25μg/mL范围内,包括对单耐药菌株的活性。此外,细胞内杀伤试验表明,SK-03-92先导化合物可杀死小鼠巨噬细胞内的(某种菌,原文未明确)细胞。
总体而言,数据表明SK-03-92先导化合物可杀死哺乳动物巨噬细胞内的(某种菌,原文未明确)细菌。