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In-Silico Analyses of Sesquiterpene-Related Compounds on Selected Leishmania Enzyme-Based Targets
Molecules 2014, 19(5), 5692-5703; doi:10.3390/molecules19055692
Article

Leishmanicidal Evaluation of Tetrahydroprotoberberine and Spirocyclic Erythrina-Alkaloids

1,2
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, 1
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 and 1,*
1 Pesquisa em Produtos Naturais e Sintéticos (NPPNS), Faculdade de Ciências Farmacêuticas de Ribeirão Preto (FCFRP), Universidade de São Paulo (USP), Av. Café s/n, 14040-903, Ribeirão Preto, SP, Brazil 2 Lychnoflora Pesquisa e Desenvolvimento em Produtos Naturais LTDA, Ribeirão Preto 14030-090, SP, Brazil 3 Departamento de Análises Clínicas, Faculdade de Ciências Farmacêuticas de Ribeirão Preto (FCFRP), Universidade de São Paulo (USP), Av. Café s/nº, 14040-903, Ribeirão Preto, SP, Brazil 4 Research Institute of Chemistry, ICCBS, University of Karachi, Karachi 75270, Pakistan 5 Amrit Science Campus, Tribhuvan University, Kathmandu, Nepal
* Author to whom correspondence should be addressed.
Received: 15 March 2014 / Revised: 22 April 2014 / Accepted: 25 April 2014 / Published: 5 May 2014
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Abstract

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 39, 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 19 against Leishmania amazonensis was tested on promastigote forms and cytotoxicity against J774 (macrophage cell line) was assessed in vitro. Compound 1 showed potent activity (IC50 = 0.18 µg/mL), compared with the standard amphotericin B (IC50 = 0.20 µg/mL). The spirocyclic erythrina-alkaloids showed lower leishmanicidal activity than dibenzoquinolizine type alkaloids.
Keywords: Leishmania amazonensis; spirocyclic erythrina-alkaloids; tetrahydro-protoberberine-type alkaloids; Corydalis govaniana; Erythrina verna Leishmania amazonensis; spirocyclic erythrina-alkaloids; tetrahydro-protoberberine-type alkaloids; Corydalis govaniana; Erythrina verna
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Callejon, D.R.; Riul, T.B.; Feitosa, L.G.P.; Guaratini, T.; Silva, D.B.; Adhikari, A.; Shrestha, R.L.; Marques, L.M.M.; Baruffi, M.D.; Lopes, J.L.C.; Lopes, N.P. Leishmanicidal Evaluation of Tetrahydroprotoberberine and Spirocyclic Erythrina-Alkaloids. Molecules 2014, 19, 5692-5703.

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