title: Study of the antimalarial properties of hydroxyethylamine derivatives using green fluorescent protein transformed Plasmodium berghei.
abstract: A rapid decrease in parasitaemia remains the major goal for new antimalarial drugs and thus, in vivo models must provide precise results concerning parasitaemia modulation. Hydroxyethylamine comprise an important group of alkanolamine compounds that exhibit pharmacological properties as proteases inhibitors that has already been proposed as a new class of antimalarial drugs. Herein, it was tested the antimalarial property of new nine different hydroxyethylamine derivatives using the green fluorescent protein (GFP)-expressing Plasmodium berghei strain. By comparing flow cytometry and microscopic analysis to evaluate parasitaemia recrudescence, it was observed that flow cytometry was a more sensitive methodology. The nine hydroxyethylamine derivatives were obtained by inserting one of the following radical in the para position: H, 4Cl, 4-Br, 4-F, 4-CH3, 4-OCH3, 4-NO2, 4-NH2 and 3-Br. The antimalarial test showed that the compound that received the methyl group (4-CH3) inhibited 70% of parasite growth. Our results suggest that GFP-transfected P. berghei is a useful tool to study the recrudescence of novel antimalarial drugs through parasitaemia examination by flow cytometry. Furthermore, it was demonstrated that the insertion of a methyl group at the para position of the sulfonamide ring appears to be critical for the antimalarial activity of this class of compounds.
authors.affiliation: Centro de Desenvolvimento Tecnológico em Saúde, Centro de Desenvolvimento Tecnológico em Saúde-Fiocruz, Rio de Janeiro, RJ, Brasil.
authors.forename: Mariana Conceição
authors.initials: MC
authors.lastname: Souza
authors.affiliation: Centro de Desenvolvimento Tecnológico em Saúde, Centro de Desenvolvimento Tecnológico em Saúde-Fiocruz, Rio de Janeiro, RJ, Brasil.
authors.forename: Tatiana Almeida
authors.initials: TA
authors.lastname: Padua
authors.affiliation: Centro de Desenvolvimento Tecnológico em Saúde, Centro de Desenvolvimento Tecnológico em Saúde-Fiocruz, Rio de Janeiro, RJ, Brasil.
authors.forename: Natalia Domingos
authors.initials: ND
authors.lastname: Torres
authors.affiliation: Centro de Desenvolvimento Tecnológico em Saúde, Centro de Desenvolvimento Tecnológico em Saúde-Fiocruz, Rio de Janeiro, RJ, Brasil.
authors.forename: Maria Fernanda de Souza
authors.initials: MF
authors.lastname: Costa
authors.affiliation: Centro de Desenvolvimento Tecnológico em Saúde, Centro de Desenvolvimento Tecnológico em Saúde-Fiocruz, Rio de Janeiro, RJ, Brasil.
authors.forename: Victor
authors.initials: V
authors.lastname: Facchinetti
authors.affiliation: Centro de Desenvolvimento Tecnológico em Saúde, Centro de Desenvolvimento Tecnológico em Saúde-Fiocruz, Rio de Janeiro, RJ, Brasil.
authors.forename: Claudia Regina Brandão
authors.initials: CR
authors.lastname: Gomes
authors.affiliation: Centro de Desenvolvimento Tecnológico em Saúde, Centro de Desenvolvimento Tecnológico em Saúde-Fiocruz, Rio de Janeiro, RJ, Brasil.
authors.forename: Marcus Vinícius Nora
authors.initials: MV
authors.lastname: Souza
authors.affiliation: Centro de Desenvolvimento Tecnológico em Saúde, Centro de Desenvolvimento Tecnológico em Saúde-Fiocruz, Rio de Janeiro, RJ, Brasil.
authors.forename: Maria das Graças
authors.initials: Md
authors.lastname: Henriques
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000627:therapeutic use*; D004195:Disease Models, Animal; D005434:Flow Cytometry; D049452:Green Fluorescent Proteins; D066298:In Vitro Techniques; D008288:Malaria / Q000188:drug therapy* / Q000469:parasitology; D051379:Mice; D018512:Parasitemia / Q000188:drug therapy* / Q000469:parasitology; D010962:Plasmodium berghei / Q000187:drug effects*; D051381:Rats
chemical_list: D000962:Antimalarials; D049452:Green Fluorescent Proteins