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三嗪喹啉类化合物的抗血吸虫活性:体内疗效及其对曼氏血吸虫的作用机制。

Antischistosomal activity of trioxaquines: in vivo efficacy and mechanism of action on Schistosoma mansoni.

机构信息

Université de Perpignan Via Domitia, Perpignan, France.

出版信息

PLoS Negl Trop Dis. 2012;6(2):e1474. doi: 10.1371/journal.pntd.0001474. Epub 2012 Feb 14.

DOI:10.1371/journal.pntd.0001474
PMID:22348155
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3279339/
Abstract

Schistosomiasis is among the most neglected tropical diseases, since its mode of spreading tends to limit the contamination to people who are in contact with contaminated waters in endemic countries. Here we report the in vitro and in vivo anti-schistosomal activities of trioxaquines. These hybrid molecules are highly active on the larval forms of the worms and exhibit different modes of action, not only the alkylation of heme. The synergy observed with praziquantel on infected mice is in favor of the development of these trioxaquines as potential anti-schistosomal agents.

摘要

血吸虫病是最被忽视的热带病之一,因为其传播方式往往局限于在流行国家与受污染水接触的人群。在这里,我们报告三嗪喹啉类化合物的体外和体内抗血吸虫活性。这些杂交分子对蠕虫的幼虫形式具有高度活性,并表现出不同的作用模式,不仅是血红素的烷化作用。在感染小鼠中与吡喹酮的协同作用有利于这些三嗪喹啉类化合物作为潜在的抗血吸虫药物的开发。

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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/30b1/3279339/dc3222359b3b/pntd.0001474.g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/30b1/3279339/2967d17667a2/pntd.0001474.g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/30b1/3279339/f8597647861b/pntd.0001474.g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/30b1/3279339/912f0d607486/pntd.0001474.g010.jpg
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