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Title: | In vitro and in vivo anti-malarial activity of limonoids isolated from the residual seed biomass from Carapa guianensis (andiroba) oil production |
Authors: | Pereira, Tiago B. Silva, Luiz Francisco Rocha e Amorim, Rodrigo C.N. Melo, Márcia R.S. Zacardi de Souza, Rita C. Eberlin, M. N. Lima, Emerson Silva Vasconcellos, Marne Carvalho de Pohlit, Adrian Martin |
Keywords: | 6alpha Acetoxyepoxyazadiradione 6alpha Acetoxygedunin 6alpha Hydroxydeacetylgedunin 7 Deacetoxy 7 Oxogedunin Andirobin Antimalarial Agent Limonoid Plant Extract Unclassified Drug Antimalarial Agent Limonoid Plant Extract Animals Experiment Animals Model Antimalarial Activity Carapa Guianensis Controlled Study Dose Response Drug Cytotoxicity Drug Efficacy Drug Screening Fibroblast Human Human Cell Ic 50 In Vitro Study In Vivo Study Medicinal Plant Meliaceae Minimum Inhibitory Concentration Mouse Nonhuman Seed Plant Plasmodium Berghei Infection Plasmodium Falciparum Animals Bagg Albino Mouse Cell Line Chemistry Drug Effects Female Malaria Meliaceae Plasmodium Berghei Animal Antimalarials Cell Line Female Humans Inhibitory Concentration 50 Limonins Malaria Meliaceae Mice Mice, Inbred Balb C Plant Extracts Plasmodium Berghei Plasmodium Falciparum Seeds |
Issue Date: | 2014 |
metadata.dc.publisher.journal: | Malaria Journal |
metadata.dc.relation.ispartof: | Volume 13, Número 1 |
Abstract: | Background: Carapa guianensis is a cultivable tree used by traditional health practitioners in the Amazon region to treat several diseases and particularly symptoms related to malaria. Abundant residual pressed seed material (RPSM) results as a by-product of carapa or andiroba oil production. The objective of this study was to evaluate the in vitro and in vivo anti-malarial activity and cytotoxicity of limonoids isolated from C. guaianensis RPSM.Methods. 6-acetoxyepoxyazadiradione (1), andirobin (2), 6-acetoxygedunin (3) and 7-deacetoxy-7-oxogedunin (4) (all isolated from RPSM using extraction and chromatography techniques) and 6-hydroxy-deacetylgedunin (5) (prepared from 3) were evaluated using the micro test on the multi-drug-resistant Plasmodium falciparum K1 strain. The efficacy of limonoids 3 and 4 was then evaluated orally and subcutaneously in BALB/c mice infected with chloroquine-sensitive Plasmodium berghei NK65 strain in the 4-day suppressive test.Results: In vitro, limonoids 1-5 exhibited median inhibition concentrations (IC50) of 20.7-5.0 μM, respectively. In general, these limonoids were not toxic to normal cells (MRC-5 human fibroblasts). In vivo, 3 was more active than 4. At oral doses of 50 and 100 mg/kg/day, 3 suppressed parasitaemia versus untreated controls by 40 and 66%, respectively, evidencing a clear dose-response.Conclusion: 6-acetoxygedunin is an abundant natural product present in C. guianensis residual seed materials that exhibits significant in vivo anti-malarial properties. © 2014 Pereira et al.; licensee BioMed Central Ltd.x. |
metadata.dc.identifier.doi: | 10.1186/1475-2875-13-317 |
Appears in Collections: | Artigos |
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