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2'-Hydroxyflavanone activity in vitro and in vivo against wild-type and antimony-resistant Leishmania amazonensis

BACKGROUND: To overcome the current problems in leishmaniasis chemotherapy, natural products have become an interesting alternative over the past few decades. Flavonoids have been studied as promising family of compounds for leishmaniasis treatment. 2’-Hydroxyflavanone (2HF) is a flavanone, a class...

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Autores principales: Gervazoni, Luiza F. O., Gonçalves-Ozório, Gabriella, Almeida-Amaral, Elmo E.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Public Library of Science 2018
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6283348/
https://www.ncbi.nlm.nih.gov/pubmed/30521527
http://dx.doi.org/10.1371/journal.pntd.0006930
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author Gervazoni, Luiza F. O.
Gonçalves-Ozório, Gabriella
Almeida-Amaral, Elmo E.
author_facet Gervazoni, Luiza F. O.
Gonçalves-Ozório, Gabriella
Almeida-Amaral, Elmo E.
author_sort Gervazoni, Luiza F. O.
collection PubMed
description BACKGROUND: To overcome the current problems in leishmaniasis chemotherapy, natural products have become an interesting alternative over the past few decades. Flavonoids have been studied as promising family of compounds for leishmaniasis treatment. 2’-Hydroxyflavanone (2HF) is a flavanone, a class of flavonoid that has shown promising results in cancer studies. In this study, we demonstrated the effects of 2HF in vitro and in vivo against wild-type and antimony-resistant Leishmania amazonensis promastigotes. METHODOLOGY/PRINCIPAL FINDINGS: 2HF was effective against promastigotes and the intracellular amastigote form, decreasing the infection index in macrophages infected with wild-type and antimony-resistant promastigotes, but it was not toxic to macrophages. In silico analysis indicated 2HF as a good oral candidate for leishmaniasis treatment. In vivo, 2HF was able to reduce the lesion size and parasite load in a murine model of cutaneous leishmaniasis using wild-type and antimony-resistant promastigotes, demonstrating no cross-resistance with antimonials. CONCLUSIONS/SIGNIFICANCE: Taken together, these results suggest 2HF as a potential candidate for leishmaniasis chemotherapy for cutaneous leishmaniasis caused by both wild-type and antimony-resistant Leishmania species by oral administration. Furthermore, studies should be conducted to determine the ideal dose and therapeutic regimen.
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spelling pubmed-62833482018-12-20 2'-Hydroxyflavanone activity in vitro and in vivo against wild-type and antimony-resistant Leishmania amazonensis Gervazoni, Luiza F. O. Gonçalves-Ozório, Gabriella Almeida-Amaral, Elmo E. PLoS Negl Trop Dis Research Article BACKGROUND: To overcome the current problems in leishmaniasis chemotherapy, natural products have become an interesting alternative over the past few decades. Flavonoids have been studied as promising family of compounds for leishmaniasis treatment. 2’-Hydroxyflavanone (2HF) is a flavanone, a class of flavonoid that has shown promising results in cancer studies. In this study, we demonstrated the effects of 2HF in vitro and in vivo against wild-type and antimony-resistant Leishmania amazonensis promastigotes. METHODOLOGY/PRINCIPAL FINDINGS: 2HF was effective against promastigotes and the intracellular amastigote form, decreasing the infection index in macrophages infected with wild-type and antimony-resistant promastigotes, but it was not toxic to macrophages. In silico analysis indicated 2HF as a good oral candidate for leishmaniasis treatment. In vivo, 2HF was able to reduce the lesion size and parasite load in a murine model of cutaneous leishmaniasis using wild-type and antimony-resistant promastigotes, demonstrating no cross-resistance with antimonials. CONCLUSIONS/SIGNIFICANCE: Taken together, these results suggest 2HF as a potential candidate for leishmaniasis chemotherapy for cutaneous leishmaniasis caused by both wild-type and antimony-resistant Leishmania species by oral administration. Furthermore, studies should be conducted to determine the ideal dose and therapeutic regimen. Public Library of Science 2018-12-06 /pmc/articles/PMC6283348/ /pubmed/30521527 http://dx.doi.org/10.1371/journal.pntd.0006930 Text en © 2018 Gervazoni et al http://creativecommons.org/licenses/by/4.0/ This is an open access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0/) , which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.
spellingShingle Research Article
Gervazoni, Luiza F. O.
Gonçalves-Ozório, Gabriella
Almeida-Amaral, Elmo E.
2'-Hydroxyflavanone activity in vitro and in vivo against wild-type and antimony-resistant Leishmania amazonensis
title 2'-Hydroxyflavanone activity in vitro and in vivo against wild-type and antimony-resistant Leishmania amazonensis
title_full 2'-Hydroxyflavanone activity in vitro and in vivo against wild-type and antimony-resistant Leishmania amazonensis
title_fullStr 2'-Hydroxyflavanone activity in vitro and in vivo against wild-type and antimony-resistant Leishmania amazonensis
title_full_unstemmed 2'-Hydroxyflavanone activity in vitro and in vivo against wild-type and antimony-resistant Leishmania amazonensis
title_short 2'-Hydroxyflavanone activity in vitro and in vivo against wild-type and antimony-resistant Leishmania amazonensis
title_sort 2'-hydroxyflavanone activity in vitro and in vivo against wild-type and antimony-resistant leishmania amazonensis
topic Research Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6283348/
https://www.ncbi.nlm.nih.gov/pubmed/30521527
http://dx.doi.org/10.1371/journal.pntd.0006930
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