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基于 1H-NMR 波谱技术检测药物对曼氏血吸虫雄性成虫代谢轮廓的影响

Drug effects on metabolic profiles of Schistosoma mansoni adult male parasites detected by 1H-NMR spectroscopy.

机构信息

Institute of Biochemistry and Cell Biology, National Research Council, Campus A. Buzzati-Traverso, Monterotondo (Rome) Italy.

Department of Chemical Science and Technologies, University of Rome Tor Vergata, Rome, Italy.

出版信息

PLoS Negl Trop Dis. 2020 Oct 12;14(10):e0008767. doi: 10.1371/journal.pntd.0008767. eCollection 2020 Oct.

Abstract

Schistosomiasis is one of the most devastating neglected tropical parasitic diseases caused by trematodes of the genus Schistosoma. Praziquantel (PZQ) is today the only drug used in humans and animals for the treatment of schistosomiasis but unfortunately it is poorly effective on larval and juvenile stages of the parasite. Therefore, it is urgent the discovery of new drug targets and compounds. We have recently showed that the anti-anginal drug perhexiline maleate (PHX) is very active on multiple developmental stages of Schistosoma mansoni in vitro. It is well known that PHX impacts the lipid metabolism in mammals, but the final target on schistosomes still remains unknown. The aim of this study was to evaluate the ability of 1H nuclear magnetic resonance (NMR) spectroscopy in revealing metabolic perturbations due to PHX treatment of S. mansoni adult male worms. The effects of PHX were compared with the ones induced by vehicle and gambogic acid, in order to detect different metabolic profiles and specificity of the PHX action. Remarkably a list of metabolites associated to PHX-treatment was identified with enrichment in several connected metabolic pathways including also the Kennedy pathway mediating the glycerophospholipid metabolism. Our study represents the first 1H-NMR metabolomic approach to characterize the response of S. mansoni to drug treatment. The obtained "metabolic fingerprint" associated to PHX treatment could represent a strategy for displaying cellular metabolic changes for any given drug and to compare compounds targeting similar or distinct biochemical pathways.

摘要

血吸虫病是由血吸虫属吸虫引起的最具破坏性的被忽视的热带寄生虫病之一。吡喹酮(PZQ)是目前唯一用于治疗血吸虫病的人类和动物药物,但不幸的是,它对寄生虫的幼虫和幼体阶段效果不佳。因此,迫切需要发现新的药物靶点和化合物。我们最近表明,抗心绞痛药物马来酸丙炔苯丙胺(PHX)在体外对曼氏血吸虫的多个发育阶段非常有效。众所周知,PHX 会影响哺乳动物的脂质代谢,但寄生虫的最终靶点仍然未知。本研究旨在评估 1H 核磁共振(NMR)光谱在揭示 PHX 处理曼氏血吸虫成虫引起的代谢紊乱方面的能力。将 PHX 的作用与载体和藤黄酸的作用进行了比较,以检测 PHX 作用的不同代谢谱和特异性。值得注意的是,我们确定了一组与 PHX 处理相关的代谢物,这些代谢物在包括介导甘油磷脂代谢的 Kennedy 途径在内的几个相关代谢途径中富集。我们的研究代表了第一个用于表征曼氏血吸虫对药物治疗反应的 1H-NMR 代谢组学方法。与 PHX 处理相关的获得的“代谢指纹”可以代表一种用于显示任何给定药物的细胞代谢变化的策略,并比较针对相似或不同生化途径的化合物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/21f9/7580944/fbafdce107dd/pntd.0008767.g001.jpg

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