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氯喹类似物PQI08001/06的体内外抗疟作用及毒理学评价

In vivo and in vitro antimalarial effect and toxicological evaluation of the chloroquine analogue PQUI08001/06.

作者信息

Reis Patricia Alves, Pais Karla Ceodaro, Pereira Monica Farah, Douradinha Bruno, Costa Natália Ferreira, Kaiser Carlos Roland, Bozza Patricia Torres, Areas André Luiz Lisboa, Zalis Mariano Gustavo, de Lima Ferreira Marcelle, de Souza Marcos Vinícius Nora, da Silva Frutuoso Valber, de Castro-Faria-Neto Hugo Caire

机构信息

Laboratório de Imunofarmacologia, Instituto Oswaldo Cruz, Avenida Brasil 4365, Manguinhos, RJ, Brazil.

Instituto de Tecnologia em Fármacos (Farmanguinhos), Fundação Oswaldo Cruz, Avenida Brasil 4365, Manguinhos, RJ, 21040-360, Brazil.

出版信息

Parasitol Res. 2018 Nov;117(11):3585-3590. doi: 10.1007/s00436-018-6057-6. Epub 2018 Aug 25.

DOI:10.1007/s00436-018-6057-6
PMID:30145706
Abstract

Antimalarial interventions mostly rely upon drugs, as chloroquine. However, plasmodial strains resistant to many drugs are constantly reported, leading to an expansion of malaria cases. Novel approaches are required to circumvent the drug resistance issue. Here, we describe the antimalarial potential of the chloroquine analogue 2-[[2-[(7-chloro-4-quinolinyl)amino]ethyl]amino] ethanol (PQUI08001/06). We observed that PQUI08001/06 treatment reduces parasitemia of both chloroquine-resistant and -sensitive strains of Plasmodium falciparum in vitro and P. berghei in vivo. Our data suggests that PQUI08001/06 is a potential antimalarial therapeutic alternative approach that could also target chloroquine-resistant plasmodial strains.

摘要

抗疟干预措施大多依赖于药物,如氯喹。然而,不断有对多种药物耐药的疟原虫菌株被报道,这导致疟疾病例增加。需要新的方法来解决耐药问题。在此,我们描述了氯喹类似物2-[[2-[(7-氯-4-喹啉基)氨基]乙基]氨基]乙醇(PQUI08001/06)的抗疟潜力。我们观察到,PQUI08001/06处理在体外可降低恶性疟原虫氯喹耐药和敏感菌株以及体内伯氏疟原虫的寄生虫血症。我们的数据表明,PQUI08001/06是一种潜在的抗疟治疗替代方法,也可针对氯喹耐药的疟原虫菌株。

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