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Leishmanicidal Evaluation of Tetrahydroprotoberberine and Spirocyclic Erythrina-Alkaloids

Leishmaniasis is one of the World’s most problematic diseases in developing countries. Traditional medicines to treat leishmaniasis have serious side effects, as well as significant parasite resistance problems. In this work, two alkaloids 1 and 2 were obtained from Corydalis govaniana Wall and seve...

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Autores principales: Callejon, Daniel R., Riul, Thalita B., Feitosa, Luis G. P., Guaratini, Thais, Silva, Denise B., Adhikari, Achyut, Shrestha, Ram L. (S.), Marques, Lucas M. M., Baruffi, Marcelo D., Lopes, João L. C., Lopes, Norberto P.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2014
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6271856/
https://www.ncbi.nlm.nih.gov/pubmed/24802983
http://dx.doi.org/10.3390/molecules19055692
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author Callejon, Daniel R.
Riul, Thalita B.
Feitosa, Luis G. P.
Guaratini, Thais
Silva, Denise B.
Adhikari, Achyut
Shrestha, Ram L. (S.)
Marques, Lucas M. M.
Baruffi, Marcelo D.
Lopes, João L. C.
Lopes, Norberto P.
author_facet Callejon, Daniel R.
Riul, Thalita B.
Feitosa, Luis G. P.
Guaratini, Thais
Silva, Denise B.
Adhikari, Achyut
Shrestha, Ram L. (S.)
Marques, Lucas M. M.
Baruffi, Marcelo D.
Lopes, João L. C.
Lopes, Norberto P.
author_sort Callejon, Daniel R.
collection PubMed
description Leishmaniasis is one of the World’s most problematic diseases in developing countries. Traditional medicines to treat leishmaniasis have serious side effects, as well as significant parasite resistance problems. In this work, two alkaloids 1 and 2 were obtained from Corydalis govaniana Wall and seven alkaloids 3–9, were obtained from Erythrina verna. The structures of the compounds were confirmed by mass spectrometry and 1D- and 2D-NMR spectroscopy. The leishmanicidal activity of compounds 1–9 against Leishmania amazonensis was tested on promastigote forms and cytotoxicity against J774 (macrophage cell line) was assessed in vitro. Compound 1 showed potent activity (IC(50) = 0.18 µg/mL), compared with the standard amphotericin B (IC(50) = 0.20 µg/mL). The spirocyclic erythrina-alkaloids showed lower leishmanicidal activity than dibenzoquinolizine type alkaloids.
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spelling pubmed-62718562018-12-21 Leishmanicidal Evaluation of Tetrahydroprotoberberine and Spirocyclic Erythrina-Alkaloids Callejon, Daniel R. Riul, Thalita B. Feitosa, Luis G. P. Guaratini, Thais Silva, Denise B. Adhikari, Achyut Shrestha, Ram L. (S.) Marques, Lucas M. M. Baruffi, Marcelo D. Lopes, João L. C. Lopes, Norberto P. Molecules Article Leishmaniasis is one of the World’s most problematic diseases in developing countries. Traditional medicines to treat leishmaniasis have serious side effects, as well as significant parasite resistance problems. In this work, two alkaloids 1 and 2 were obtained from Corydalis govaniana Wall and seven alkaloids 3–9, were obtained from Erythrina verna. The structures of the compounds were confirmed by mass spectrometry and 1D- and 2D-NMR spectroscopy. The leishmanicidal activity of compounds 1–9 against Leishmania amazonensis was tested on promastigote forms and cytotoxicity against J774 (macrophage cell line) was assessed in vitro. Compound 1 showed potent activity (IC(50) = 0.18 µg/mL), compared with the standard amphotericin B (IC(50) = 0.20 µg/mL). The spirocyclic erythrina-alkaloids showed lower leishmanicidal activity than dibenzoquinolizine type alkaloids. MDPI 2014-05-05 /pmc/articles/PMC6271856/ /pubmed/24802983 http://dx.doi.org/10.3390/molecules19055692 Text en © 2014 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/).
spellingShingle Article
Callejon, Daniel R.
Riul, Thalita B.
Feitosa, Luis G. P.
Guaratini, Thais
Silva, Denise B.
Adhikari, Achyut
Shrestha, Ram L. (S.)
Marques, Lucas M. M.
Baruffi, Marcelo D.
Lopes, João L. C.
Lopes, Norberto P.
Leishmanicidal Evaluation of Tetrahydroprotoberberine and Spirocyclic Erythrina-Alkaloids
title Leishmanicidal Evaluation of Tetrahydroprotoberberine and Spirocyclic Erythrina-Alkaloids
title_full Leishmanicidal Evaluation of Tetrahydroprotoberberine and Spirocyclic Erythrina-Alkaloids
title_fullStr Leishmanicidal Evaluation of Tetrahydroprotoberberine and Spirocyclic Erythrina-Alkaloids
title_full_unstemmed Leishmanicidal Evaluation of Tetrahydroprotoberberine and Spirocyclic Erythrina-Alkaloids
title_short Leishmanicidal Evaluation of Tetrahydroprotoberberine and Spirocyclic Erythrina-Alkaloids
title_sort leishmanicidal evaluation of tetrahydroprotoberberine and spirocyclic erythrina-alkaloids
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6271856/
https://www.ncbi.nlm.nih.gov/pubmed/24802983
http://dx.doi.org/10.3390/molecules19055692
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