Adv Pharm Bull. 2020;10(1): 119-124.
doi: 10.15171/apb.2020.015
PMID: 32002370
PMCID: PMC6983991
Scopus ID: 85084153971
  Abstract View: 412
  PDF Download: 285

Research Article

Toxicity and Anti-promastigote Activity of Benzoxazinoid Analogs Against Leishmania (Viannia) braziliensis and Leishmania (Leishmania) infantum

Gilberto de Sousa 1 ORCID logo, William Gustavo Lima 2 ORCID logo, Flávio José dos Santos 3 ORCID logo, Francisco A. Macías 4 ORCID logo, José María González Molinillo 4 ORCID logo, Rafael Gonçalves Teixeira-Neto 1 ORCID logo, João Máximo de Siqueira 3 ORCID logo, Eduardo Sérgio da Silva 1* ORCID logo

1 Laboratório de Parasitologia e Doenças Parasitárias, Campus Centro-Oeste Dona Lindu, Universidade Federal de São João Del-Rei (UFSJ), Divinopolis, MG, Brazil.
2 Laboratório de Microbiologia Médica, Campus Centro-Oeste Dona Lindu, Universidade Federal de São João Del-Rei (UFSJ), Divinopolis, MG, Brazil.
3 Laboratório de Farmacognosia/Química de Produtos Naturais, Campus Centro-Oeste Dona Lindu, Universidade Federal de São João Del-Rei (UFSJ), Divinopolis, MG, Brazil.
4 Allelopathy Group, Department of Organic Chemistry, Institute of Biomolecules (INBIO), Campus CEIA3, School of Science, University of Cadiz, Puerto Real (Cádiz), Spain.


Purpose: Here, we aim to evaluate the antileishmanial activity of compounds with a benzoxazinoid (BX) skeleton, previously synthesized by our group, against Leishmania (Viannia) braziliensis and Leishmania (Leishmania) infantum promastigotes.

Methods: Anti-promastigote activity, as well as cytotoxicity, were determined using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) colorimetric assays. The selectivity index (SI) for each compound was calculated using a ratio of the cytotoxicity of compounds and the geometric mean (GM) of antileishmanial concentrations to each species tested. The comparisons between groups were carried out using a t test or analysis of variance (one-way ANOVA). A P value of less than 0.05 was considered significant.

Results: All the compounds tested were active, with IC50 falling between 92±6.19 µg/mL and 238±6.57 µg/mL for L. braziliensis, and 89±6.43 µg/mL and 188±3.58 µg/mL against L. infantum. Bex2, Bex3, Pyr1, Pyr2, and Pyr4 were compounds that showed activity similar to the drug Glucantime®, exhibited low cytotoxicity against splenic hamster cells (CC50 raging between >400 and 105.7±2.26 µg/mL) and had favorable selectivity indices (SI 1.12 to 3.96).

Conclusion: The analogs in question are promising prototypes for the pharmaceutical development of novel, safer and more effective leishmanicidal agents.

Keywords: Benzoxazinone core, Leishmanicidal agents, Neglected disease, Pharmacology, Pyridoxazinone core, Splenic hamster cells
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Submitted: 30 Jan 2019
Revision: 25 Jun 2019
Accepted: 02 Sep 2019
ePublished: 11 Dec 2019
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