Department of Chemistry, Temple University , Philadelphia, Pennsylvania 19122, United States.
Center for Oral Biology, University of Rochester School of Medicine and Dentistry , Rochester New York 14642, United States.
J Am Chem Soc. 2017 May 31;139(21):7188-7191. doi: 10.1021/jacs.7b03879. Epub 2017 May 17.
The oral microbiome is a dynamic environment inhabited by both commensals and pathogens. Among these is Streptococcus mutans, the causative agent of dental caries, the most prevalent childhood disease. Carolacton has remarkably specific activity against S. mutans, causing acid-mediated cell death during biofilm formation; however, its complex structure limits its utility. Herein, we report the diverted total synthesis and biological evaluation of a rationally designed library of simplified analogs that unveiled three unique biofilm phenotypes further validating the role of natural product synthesis in the discovery of new biological phenomena.
口腔微生物组是一个动态的环境,栖息着共生菌和病原体。其中包括变形链球菌,它是导致龋齿的病原体,也是最常见的儿童疾病。Carolacton 对变形链球菌具有显著的特异性活性,在生物膜形成过程中引起酸介导的细胞死亡;然而,其复杂的结构限制了它的实用性。在此,我们报告了一种经过合理设计的简化类似物文库的定向全合成及生物学评价,该文库揭示了三种独特的生物膜表型,进一步验证了天然产物合成在发现新生物学现象中的作用。