2'-Hydroxyflavanone activity in vitro and in vivo against wild-type and antimony-resistant Leishmania amazonensis.
<h4>Background</h4>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)...
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| Format: | Article |
| Language: | English |
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Public Library of Science (PLoS)
2018-12-01
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| Series: | PLoS Neglected Tropical Diseases |
| Online Access: | https://doi.org/10.1371/journal.pntd.0006930 |
| _version_ | 1818575965291282432 |
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| author | Luiza F O Gervazoni Gabriella Gonçalves-Ozório Elmo E Almeida-Amaral |
| author_facet | Luiza F O Gervazoni Gabriella Gonçalves-Ozório Elmo E Almeida-Amaral |
| author_sort | Luiza F O Gervazoni |
| collection | DOAJ |
| description | <h4>Background</h4>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.<h4>Methodology/principal findings</h4>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.<h4>Conclusions/significance</h4>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. |
| first_indexed | 2024-12-15T00:48:01Z |
| format | Article |
| id | doaj.art-eee32b1720a344cb8431a7cd7e5a35d0 |
| institution | Directory Open Access Journal |
| issn | 1935-2727 1935-2735 |
| language | English |
| last_indexed | 2024-12-15T00:48:01Z |
| publishDate | 2018-12-01 |
| publisher | Public Library of Science (PLoS) |
| record_format | Article |
| series | PLoS Neglected Tropical Diseases |
| spelling | doaj.art-eee32b1720a344cb8431a7cd7e5a35d02022-12-21T22:41:30ZengPublic Library of Science (PLoS)PLoS Neglected Tropical Diseases1935-27271935-27352018-12-011212e000693010.1371/journal.pntd.00069302'-Hydroxyflavanone activity in vitro and in vivo against wild-type and antimony-resistant Leishmania amazonensis.Luiza F O GervazoniGabriella Gonçalves-OzórioElmo E Almeida-Amaral<h4>Background</h4>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.<h4>Methodology/principal findings</h4>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.<h4>Conclusions/significance</h4>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.https://doi.org/10.1371/journal.pntd.0006930 |
| spellingShingle | Luiza F O Gervazoni Gabriella Gonçalves-Ozório Elmo E Almeida-Amaral 2'-Hydroxyflavanone activity in vitro and in vivo against wild-type and antimony-resistant Leishmania amazonensis. PLoS Neglected Tropical Diseases |
| 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 |
| url | https://doi.org/10.1371/journal.pntd.0006930 |
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