海洋化合物Tartrolon E作用于……的无性和早期有性阶段。 （原文此处不完整）
The Marine Compound Tartrolon E Targets the Asexual and Early Sexual Stages of .
作者信息
Cotto-Rosario Alexis, Miller Emma Y D, Fumuso Fernanda G, Clement Jason A, Todd Matthew J, O'Connor Roberta M
机构信息
Department of Veterinary Microbiology and Pathology, Washington State University, Pullman, WA 99164, USA.
Department of Veterinary and Biomedical Sciences, University of Minnesota, St. Paul, MN 55108, USA.
出版信息
Microorganisms. 2022 Nov 15;10(11):2260. doi: 10.3390/microorganisms10112260.
New therapeutic agents for cryptosporidiosis are a critical medical need. The marine organic compound, tartrolon E (trtE), is highly effective against multiple apicomplexan parasites, including . Understanding the mechanism of action of trtE is required to advance in the drug development pipeline. Here, we validate using Nluc parasites for the study of trtE and pinpoint the life stage targeted by trtE. Results show that trtE kills Nluc and wild type with equal efficiency, confirming the use of the Nluc to study this compound. Results revealed that trtE kills the parasite within an hour of treatment and while the compound has no effect on viability of sporozoites, trtE does inhibit establishment of infection. Targeting treatment at particular life cycle stages demonstrated that trtE is effective against asexual of the parasite but has reduced efficacy against mature sexual stages. Gene expression analysis shows that trtE inhibits the early sexual stage of the parasite. Results from these studies will aid the development of trtE as a therapeutic for cryptosporidiosis.
新型隐孢子虫病治疗药物是一项迫切的医学需求。海洋有机化合物tartrolon E（trtE）对包括……在内的多种顶复门寄生虫具有高效作用。为推进药物研发进程，需要了解trtE的作用机制。在此，我们验证了使用表达纳米荧光素酶（Nluc）的寄生虫来研究trtE，并确定trtE靶向的生命阶段。结果表明，trtE以相同效率杀死表达Nluc的寄生虫和野生型寄生虫，证实了使用表达Nluc的寄生虫来研究该化合物。结果显示，trtE在处理一小时内杀死寄生虫，虽然该化合物对子孢子活力没有影响，但trtE确实抑制感染的建立。针对特定生命周期阶段进行治疗表明，trtE对寄生虫的无性阶段有效，但对成熟有性阶段的疗效降低。基因表达分析表明，trtE抑制寄生虫的早期有性阶段。这些研究结果将有助于trtE作为隐孢子虫病治疗药物的开发。
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