Department of Microbiology and Molecular Genetics, Harvard Medical School, 200 Longwood Avenue, Boston, MA 02115, USA.
Int J Antimicrob Agents. 2010 Mar;35(3):292-6. doi: 10.1016/j.ijantimicag.2009.10.011. Epub 2009 Dec 23.
To gain insights into the cellular processes required for intracellular bacterial pathogenesis, we previously developed a generalisable screening approach to identify small molecule compounds that alter Listeria monocytogenes infection. In this report, a small molecule library enriched for compounds affecting neurological functions was screened and 68 compounds that disrupted L. monocytogenes infection of macrophages were identified. Many of these compounds were known antimicrobial agents, however 26 compounds were novel inhibitors of intracellular infection. Two of the compounds chosen for further study, the antipsychotic drug thioridazine and the calcium channel blocker bepridil, exhibited dose-dependent inhibition of vacuolar escape and intracellular replication of L. monocytogenes during infection of murine macrophages. These results suggest that clinically approved neurological drugs may provide a novel source of anti-infective agents that are suitable for development as therapeutics against intracellular bacterial infections.
为了深入了解细胞内细菌发病机制所需的细胞过程,我们之前开发了一种可推广的筛选方法,以鉴定改变李斯特菌感染的小分子化合物。在本报告中,筛选了富含影响神经系统功能的化合物的小分子文库,鉴定出 68 种破坏李斯特菌感染巨噬细胞的化合物。其中许多化合物是已知的抗菌剂,但是有 26 种化合物是新型的细胞内感染抑制剂。选择了两种化合物进一步研究,抗精神病药硫利达嗪和钙通道阻滞剂贝普地尔,在感染小鼠巨噬细胞时表现出对李斯特菌液泡逃逸和细胞内复制的剂量依赖性抑制作用。这些结果表明,临床批准的神经药物可能为抗感染药物提供新的来源,这些药物适合开发成为针对细胞内细菌感染的治疗方法。