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疟原虫二氢叶酸还原酶是三氯生抗疟作用的第二个酶靶标。

Plasmodium dihydrofolate reductase is a second enzyme target for the antimalarial action of triclosan.

机构信息

Cambridge Systems Biology Centre & Department of Biochemistry, University of Cambridge, Cambridge, UK.

Department of Structural and Functional Biology, Institute of Biology, UNICAMP, Campinas, SP, Brazil.

出版信息

Sci Rep. 2018 Jan 18;8(1):1038. doi: 10.1038/s41598-018-19549-x.

Abstract

Malaria, caused by parasites of the genus Plasmodium, leads to over half a million deaths per year, 90% of which are caused by Plasmodium falciparum. P. vivax usually causes milder forms of malaria; however, P. vivax can remain dormant in the livers of infected patients for weeks or years before re-emerging in a new bout of the disease. The only drugs available that target all stages of the parasite can lead to severe side effects in patients with glucose-6-phosphate dehydrogenase (G6PD) deficiency; hence, there is an urgent need to develop new drugs active against blood and liver stages of the parasite. Different groups have demonstrated that triclosan, a common antibacterial agent, targets the Plasmodium liver enzyme enoyl reductase. Here, we provide 4 independent lines of evidence demonstrating that triclosan specifically targets both wild-type and pyrimethamine-resistant P. falciparum and P. vivax dihydrofolate reductases, classic targets for the blood stage of the parasite. This makes triclosan an exciting candidate for further development as a dual specificity antimalarial, which could target both liver and blood stages of the parasite.

摘要

疟疾由疟原虫属寄生虫引起,每年导致超过 50 万人死亡,其中 90%是由恶性疟原虫引起的。间日疟原虫通常引起疟疾的较轻形式;然而,间日疟原虫可以在受感染患者的肝脏中潜伏数周或数年,然后在疾病的新一轮发作中重新出现。目前可用的靶向寄生虫所有阶段的唯一药物会导致葡萄糖-6-磷酸脱氢酶(G6PD)缺乏症患者出现严重的副作用;因此,迫切需要开发针对寄生虫血液和肝脏阶段的新药。不同的研究小组已经证明,三氯生,一种常见的抗菌剂,靶向疟原虫肝脏酶烯醇还原酶。在这里,我们提供了 4 条独立的证据线,证明三氯生特异性靶向野生型和抗疟药嘧啶耐药的恶性疟原虫和间日疟原虫二氢叶酸还原酶,这是寄生虫血液阶段的经典靶点。这使得三氯生成为进一步开发作为双重特异性抗疟药的一个令人兴奋的候选药物,它可以针对寄生虫的肝脏和血液阶段。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/069f/5773535/3d0f144854bf/41598_2018_19549_Fig1_HTML.jpg

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