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Title

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

Pages

  119-124

Abstract

 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 μ g/mL and 238± 6. 57 μ g/mL for L. braziliensis, and 89 ± 6. 43 μ g/mL and 188 ± 3. 58 μ g/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 μ g/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.

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    APA: Copy

    Lima, William Gustavo, Lima, William Gustavo, dos Santos, Flavio Jose, Macias, Francisco A., Teixeira Neto, Rafael Goncalves, de Siqueira, Joao Maximo, & da Silva, Eduardo Sergio. (2020). Toxicity and Anti-promastigote Activity of Benzoxazinoid Analogs Against Leishmania (Viannia) braziliensis and Leishmania (Leishmania) infantum. ADVANCED PHARMACEUTICAL BULLETIN, 10(1), 119-124. SID. https://sid.ir/paper/753216/en

    Vancouver: Copy

    Lima William Gustavo, Lima William Gustavo, dos Santos Flavio Jose, Macias Francisco A., Teixeira Neto Rafael Goncalves, de Siqueira Joao Maximo, da Silva Eduardo Sergio. Toxicity and Anti-promastigote Activity of Benzoxazinoid Analogs Against Leishmania (Viannia) braziliensis and Leishmania (Leishmania) infantum. ADVANCED PHARMACEUTICAL BULLETIN[Internet]. 2020;10(1):119-124. Available from: https://sid.ir/paper/753216/en

    IEEE: Copy

    William Gustavo Lima, William Gustavo Lima, Flavio Jose dos Santos, Francisco A. Macias, Rafael Goncalves Teixeira Neto, Joao Maximo de Siqueira, and Eduardo Sergio da Silva, “Toxicity and Anti-promastigote Activity of Benzoxazinoid Analogs Against Leishmania (Viannia) braziliensis and Leishmania (Leishmania) infantum,” ADVANCED PHARMACEUTICAL BULLETIN, vol. 10, no. 1, pp. 119–124, 2020, [Online]. Available: https://sid.ir/paper/753216/en

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