Dados do Trabalho

Título

ASSESSMENT OF THE ANTI-LEISHMANIA ACTIVITY OF QUINOLINE-DERIVED COMPOUNDS IN Leishmania infantum

Introdução

Leishmaniasis is the most important neglected tropical disease by the World Health Organization (WHO). Current treatment involves highly toxic drugs such as pentavalent antimonials, Amphotericin B (AmB), and miltefosine. Given this context, it becomes imperative to search for new molecules capable of treating leishmaniasis without exerting such significant toxicity. Natural products from the quinoline class have been identified as new targets exhibiting antimalarial, antibacterial, anticancer, and antipsychotic activities. Studies report that the activity of quinoline derivatives in Leishmania also relates to interference in electron transport, inhibiting the functioning of the mitochondrial respiratory chain and production of lethal oxidative radicals, as well as the inhibition of genes from the cysteine protease family, which are important for the parasite's virulence. 

Objetivo (s)

In this study, we aimed to evaluate the anti-Leishmania activity of quinoline-derived compounds on promastigote forms of L. infantum, to obtain the values of half-maximal inhibitory concentration, representing 50% inhibition of promastigote growth (IC50), and to investigate the cytotoxic effect of the compounds on human erythrocytes. 

Material e Métodos

In this study, all compounds were tested at concentrations ranging from 0.78 to 100 µM in triplicate. The purpose was to obtain the cell viability rate in the promastigote forms of the parasite using the MTT colorimetric method (3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide). The hemolytic rates of the compounds in human erythrocytes were also evaluated through the half-maximal hemolytic concentration (HC50). Amphotericin B was used as a positive control reference. This study was approved by the Ethics Committee for Research in Humans of the Lauro Wanderley University Hospital/UFPB (CAAE: 17813013.8.0000.5183).

Resultados e Conclusão

The tested compound CQ41 exhibited significant anti-Leishmania activity against promastigote forms of L. infantum, yielding an IC50 value of 2.176 µM. Additionally, we observed low hemolytic activity of this compound, with average erythrocyte lysis percentages below 2%. Furthermore, future studies with the compound may strengthen these present results. This potential activity can be considered a significant advancement in the study of this class of derivatives, making it a promising candidate for the development of new in vivo research investment.

Palavras Chave

biological activity; biosynthetic compounds; treatment