Literature DB >> 30145706

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

Patricia Alves Reis1, Karla Ceodaro Pais2,3, Monica Farah Pereira1, Bruno Douradinha4, Natália Ferreira Costa2, Carlos Roland Kaiser3, Patricia Torres Bozza1, André Luiz Lisboa Areas5, Mariano Gustavo Zalis5, Marcelle de Lima Ferreira2,3, Marcos Vinícius Nora de Souza2, Valber da Silva Frutuoso1, Hugo Caire de Castro-Faria-Neto1.   

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.

Entities:  

Keywords:  Antimalarial drug; Chloroquine; Chloroquine resistance; Malaria; Plasmodium

Mesh:

Substances:

Year:  2018        PMID: 30145706     DOI: 10.1007/s00436-018-6057-6

Source DB:  PubMed          Journal:  Parasitol Res        ISSN: 0932-0113            Impact factor:   2.289


  19 in total

1.  Mutations in the P. falciparum digestive vacuole transmembrane protein PfCRT and evidence for their role in chloroquine resistance.

Authors:  D A Fidock; T Nomura; A K Talley; R A Cooper; S M Dzekunov; M T Ferdig; L M Ursos; A B Sidhu; B Naudé; K W Deitsch; X Z Su; J C Wootton; P D Roepe; T E Wellems
Journal:  Mol Cell       Date:  2000-10       Impact factor: 17.970

Review 2.  From methylene blue to chloroquine: a brief review of the development of an antimalarial therapy.

Authors:  Kristine Krafts; Ernst Hempelmann; Agnieszka Skórska-Stania
Journal:  Parasitol Res       Date:  2012-03-13       Impact factor: 2.289

3.  High-level chloroquine resistance of Plasmodium berghei is associated with multiple drug resistance and loss of reversal by calcium antagonists.

Authors:  D F Platel; F Mangou; J Tribouley-Duret
Journal:  Int J Parasitol       Date:  1998-04       Impact factor: 3.981

4.  Quinoline antimalarials decrease the rate of beta-hematin formation.

Authors:  Timothy J Egan; Kanyile K Ncokazi
Journal:  J Inorg Biochem       Date:  2005-07       Impact factor: 4.155

5.  The antimalarial activity of N-benzyloxydihydrotriazines. I. The activity of clociguanil (BRL 50216) against rodent malaria, and studies on its mode of action.

Authors:  D J Knight; W Peters
Journal:  Ann Trop Med Parasitol       Date:  1980-08

6.  Complex polymorphisms in an approximately 330 kDa protein are linked to chloroquine-resistant P. falciparum in Southeast Asia and Africa.

Authors:  X Su; L A Kirkman; H Fujioka; T E Wellems
Journal:  Cell       Date:  1997-11-28       Impact factor: 41.582

7.  Chloroquine transport via the malaria parasite's chloroquine resistance transporter.

Authors:  Rowena E Martin; Rosa V Marchetti; Anna I Cowan; Susan M Howitt; Stefan Bröer; Kiaran Kirk
Journal:  Science       Date:  2009-09-25       Impact factor: 47.728

8.  Simple and inexpensive fluorescence-based technique for high-throughput antimalarial drug screening.

Authors:  Martin Smilkstein; Nongluk Sriwilaijaroen; Jane Xu Kelly; Prapon Wilairat; Michael Riscoe
Journal:  Antimicrob Agents Chemother       Date:  2004-05       Impact factor: 5.191

9.  Human malaria parasites in continuous culture.

Authors:  W Trager; J B Jensen
Journal:  Science       Date:  1976-08-20       Impact factor: 47.728

Review 10.  A systematic review and meta-analysis of evidence for correlation between molecular markers of parasite resistance and treatment outcome in falciparum malaria.

Authors:  Stéphane Picot; Piero Olliaro; Frédérique de Monbrison; Anne-Lise Bienvenu; Ric N Price; Pascal Ringwald
Journal:  Malar J       Date:  2009-05-04       Impact factor: 2.979

View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.