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Study of the antimalarial properties of hydroxyethylamine derivatives using green fluorescent protein transformed Plasmodium berghei
Souza, Mariana Conceição; Padua, Tatiana Almeida; Torres, Natalia Domingos; Costa, Maria Fernanda de Souza; Facchinetti, Victor; Gomes, Claudia Regina Brandão; Souza, Marcus Vinícius Nora & Henriques, Maria das Graças
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.
Keywords
experimental malaria; novel antimalarial drugs; hydroxyethylamine
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