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Title: In vitro and in vivo anti-malarial activity of plants from the Brazilian Amazon
Authors: Lima, Renata Braga Souza
Rocha Silva, Luiz F.
Melo, Márcia R.S.
Costa, Jacqueline S.
Picanço, Neila Soares
Lima, Emerson Silva
Vasconcellos, Marne Carvalho de
Boleti, Ana Paula de Araújo
Santos, Jakeline M.P.
Amorim, Rodrigo C.N.
Chaves, Francisco Célio Maia
Coutinho, Julia Penna
Tadei, Wanderli Pedro
Krettli, Antoniana Ursine
Pohlit, Adrian Martin
Keywords: Alcohol
Anacardic Acid
Andropogon Leucostachyus Extract
Clidemia Bullosa Extract
Croton Cajucara Extract
Derris Floribunda Extract
Guarana Extract
Miconia Nervosa Extract
Monoclonal Antibody
Parkia Nitida Extract
Plant Extract
Stigmaphyllon Sinuatum Extract
Unclassified Drug
Xylopia Amazonica Extract
Zanthoxylum Djalma Batistae Extract
Antimalarial Agent
Plant Extract
Andropogon Leucostachyus
Animals Cell
Animals Experiment
Animals Model
Antimalarial Activity
Antimalarial Drug Resistance
Cell Viability
Clidemia Bullosa
Controlled Study
Croton Cajucara
Derris Floribunda
Drug Cytotoxicity
Drug Screening
Drug Selectivity
Drug Synthesis
Enzyme-linked Immunosorbent Assay
Fibroblast Culture
Human Cell
Ic 50
In Vitro Study
In Vivo Study
Medicinal Plant
Melanoma Cell Line
Miconia Nervosa
Parkia Nitida
Plant Leaf
Plasmodium Berghei Infection
Plasmodium Falciparum
Plasmodium Falciparum K1
Plasmodium Falciparum W2
Stigmaphyllon Sinuatum
Xylopia Amazonica
Zanthoxylum Djalma Batistae
Bagg Albino Mouse
Cell Culture
Cell Survival
Disease Model
Drug Effects
Drug Sensitivity
Isolation And Purification
Plasmodium Berghei
Treatment Outcome
Cell Survival
Cells, Cultured
Disease Models, Animals
Inhibitory Concentration 50
Mice, Inbred Balb C
Parasitic Sensitivity Tests
Plant Extracts
Plasmodium Berghei
Plasmodium Falciparum
Treatment Outcome
Issue Date: 2015
metadata.dc.publisher.journal: Malaria Journal
metadata.dc.relation.ispartof: Volume 14, Número 1
Abstract: Background: The anti-malarials quinine and artemisinin were isolated from traditionally used plants (Cinchona spp. and Artemisia annua, respectively). The synthetic quinoline anti-malarials (e.g. chloroquine) and semi-synthetic artemisinin derivatives (e.g. artesunate) were developed based on these natural products. Malaria is endemic to the Amazon region where Plasmodium falciparum and Plasmodium vivax drug-resistance is of concern. There is an urgent need for new anti-malarials. Traditionally used Amazonian plants may provide new treatments for drug-resistant P. vivax and P. falciparum. Herein, the in vitro and in vivo antiplasmodial activity and cytotoxicity of medicinal plant extracts were investigated. Methods: Sixty-nine extracts from 11 plant species were prepared and screened for in vitro activity against P. falciparum K1 strain and for cytotoxicity against human fibroblasts and two melanoma cell lines. Median inhibitory concentrations (IC50) were established against chloroquine-resistant P. falciparum W2 clone using monoclonal anti-HRPII (histidine-rich protein II) antibodies in an enzyme-linked immunosorbent assay. Extracts were evaluated for toxicity against murine macrophages (IC50) and selectivity indices (SI) were determined. Three extracts were also evaluated orally in Plasmodium berghei-infected mice. Results: High in vitro antiplasmodial activity (IC50 = 6.4-9.9 μg/mL) was observed for Andropogon leucostachyus aerial part methanol extracts, Croton cajucara red variety leaf chloroform extracts, Miconia nervosa leaf methanol extracts, and Xylopia amazonica leaf chloroform and branch ethanol extracts. Paullinia cupana branch chloroform extracts and Croton cajucara red variety leaf ethanol extracts were toxic to fibroblasts and or melanoma cells. Xylopia amazonica branch ethanol extracts and Zanthoxylum djalma-batistae branch chloroform extracts were toxic to macrophages (IC50 = 6.9 and 24.7 μg/mL, respectively). Andropogon leucostachyus extracts were the most selective (SI >28.2) and the most active in vivo (at doses of 250 mg/kg, 71 % suppression of P. berghei parasitaemia versus untreated controls). Conclusions: Ethnobotanical or ethnopharmacological reports describe the anti-malarial use of these plants or the antiplasmodial activity of congeneric species. No antiplasmodial activity has been demonstrated previously for the extracts of these plants. Seven plants exhibit in vivo and or in vitro anti-malarial potential. Future work should aim to discover the anti-malarial substances present. © 2015 Lima et al.
metadata.dc.identifier.doi: 10.1186/s12936-015-0999-2
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