In vitro and in vivo anti-malarial activity of plants from the Brazilian Amazon
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...
| Autor principal: | Lima, Renata Braga Souza |
|---|---|
| Outros Autores: | 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 |
| Grau: | Artigo |
| Idioma: | English |
| Publicado em: |
Malaria Journal
2020
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| Acesso em linha: |
https://repositorio.inpa.gov.br/handle/1/15871 |
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oai:repositorio:1-15871 |
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oai:repositorio:1-15871 In vitro and in vivo anti-malarial activity of plants from the Brazilian Amazon 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 Alcohol Anacardic Acid Andropogon Leucostachyus Extract Chloroform Chloroquine Clidemia Bullosa Extract Croton Cajucara Extract Derris Floribunda Extract Guarana Extract Methanol 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 Adult Andropogon Andropogon Leucostachyus Animals Cell Animals Experiment Animals Model Antimalarial Activity Antimalarial Drug Resistance Brazilian Cell Viability Clidemia Bullosa Controlled Study Croton Croton Cajucara Derris Derris Floribunda Drug Cytotoxicity Drug Screening Drug Selectivity Drug Synthesis Enzyme-linked Immunosorbent Assay Fabaceae Fibroblast Culture Human Human Cell Ic 50 In Vitro Study In Vivo Study Macrophage Malpighiaceae Medicinal Plant Melanoma Cell Line Melastomataceae Miconia Nervosa Mouse Nonhuman Parasitemia Parkia Nitida Plant Leaf Plasmodium Berghei Infection Plasmodium Falciparum Plasmodium Falciparum K1 Plasmodium Falciparum W2 Stigmaphyllon Sinuatum Varietas Xylopia Xylopia Amazonica Zanthoxylum Zanthoxylum Djalma Batistae Animals Bagg Albino Mouse Brasil Cell Culture Cell Survival Chemistry Disease Model Drug Effects Drug Sensitivity Isolation And Purification Malaria Plant Plasmodium Berghei Treatment Outcome Animal Antimalarials Brasil Cell Survival Cells, Cultured Disease Models, Animals Humans Inhibitory Concentration 50 Malaria Mice, Inbred Balb C Parasitemia Parasitic Sensitivity Tests Plant Extracts Plants Plasmodium Berghei Plasmodium Falciparum Treatment Outcome 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. 2020-05-19T20:34:02Z 2020-05-19T20:34:02Z 2015 Artigo https://repositorio.inpa.gov.br/handle/1/15871 10.1186/s12936-015-0999-2 en Volume 14, Número 1 Attribution-NonCommercial-NoDerivs 3.0 Brazil http://creativecommons.org/licenses/by-nc-nd/3.0/br/ application/pdf Malaria Journal |
| institution |
Instituto Nacional de Pesquisas da Amazônia - Repositório Institucional |
| collection |
INPA-RI |
| language |
English |
| topic |
Alcohol Anacardic Acid Andropogon Leucostachyus Extract Chloroform Chloroquine Clidemia Bullosa Extract Croton Cajucara Extract Derris Floribunda Extract Guarana Extract Methanol 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 Adult Andropogon Andropogon Leucostachyus Animals Cell Animals Experiment Animals Model Antimalarial Activity Antimalarial Drug Resistance Brazilian Cell Viability Clidemia Bullosa Controlled Study Croton Croton Cajucara Derris Derris Floribunda Drug Cytotoxicity Drug Screening Drug Selectivity Drug Synthesis Enzyme-linked Immunosorbent Assay Fabaceae Fibroblast Culture Human Human Cell Ic 50 In Vitro Study In Vivo Study Macrophage Malpighiaceae Medicinal Plant Melanoma Cell Line Melastomataceae Miconia Nervosa Mouse Nonhuman Parasitemia Parkia Nitida Plant Leaf Plasmodium Berghei Infection Plasmodium Falciparum Plasmodium Falciparum K1 Plasmodium Falciparum W2 Stigmaphyllon Sinuatum Varietas Xylopia Xylopia Amazonica Zanthoxylum Zanthoxylum Djalma Batistae Animals Bagg Albino Mouse Brasil Cell Culture Cell Survival Chemistry Disease Model Drug Effects Drug Sensitivity Isolation And Purification Malaria Plant Plasmodium Berghei Treatment Outcome Animal Antimalarials Brasil Cell Survival Cells, Cultured Disease Models, Animals Humans Inhibitory Concentration 50 Malaria Mice, Inbred Balb C Parasitemia Parasitic Sensitivity Tests Plant Extracts Plants Plasmodium Berghei Plasmodium Falciparum Treatment Outcome |
| spellingShingle |
Alcohol Anacardic Acid Andropogon Leucostachyus Extract Chloroform Chloroquine Clidemia Bullosa Extract Croton Cajucara Extract Derris Floribunda Extract Guarana Extract Methanol 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 Adult Andropogon Andropogon Leucostachyus Animals Cell Animals Experiment Animals Model Antimalarial Activity Antimalarial Drug Resistance Brazilian Cell Viability Clidemia Bullosa Controlled Study Croton Croton Cajucara Derris Derris Floribunda Drug Cytotoxicity Drug Screening Drug Selectivity Drug Synthesis Enzyme-linked Immunosorbent Assay Fabaceae Fibroblast Culture Human Human Cell Ic 50 In Vitro Study In Vivo Study Macrophage Malpighiaceae Medicinal Plant Melanoma Cell Line Melastomataceae Miconia Nervosa Mouse Nonhuman Parasitemia Parkia Nitida Plant Leaf Plasmodium Berghei Infection Plasmodium Falciparum Plasmodium Falciparum K1 Plasmodium Falciparum W2 Stigmaphyllon Sinuatum Varietas Xylopia Xylopia Amazonica Zanthoxylum Zanthoxylum Djalma Batistae Animals Bagg Albino Mouse Brasil Cell Culture Cell Survival Chemistry Disease Model Drug Effects Drug Sensitivity Isolation And Purification Malaria Plant Plasmodium Berghei Treatment Outcome Animal Antimalarials Brasil Cell Survival Cells, Cultured Disease Models, Animals Humans Inhibitory Concentration 50 Malaria Mice, Inbred Balb C Parasitemia Parasitic Sensitivity Tests Plant Extracts Plants Plasmodium Berghei Plasmodium Falciparum Treatment Outcome Lima, Renata Braga Souza In vitro and in vivo anti-malarial activity of plants from the Brazilian Amazon |
| topic_facet |
Alcohol Anacardic Acid Andropogon Leucostachyus Extract Chloroform Chloroquine Clidemia Bullosa Extract Croton Cajucara Extract Derris Floribunda Extract Guarana Extract Methanol 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 Adult Andropogon Andropogon Leucostachyus Animals Cell Animals Experiment Animals Model Antimalarial Activity Antimalarial Drug Resistance Brazilian Cell Viability Clidemia Bullosa Controlled Study Croton Croton Cajucara Derris Derris Floribunda Drug Cytotoxicity Drug Screening Drug Selectivity Drug Synthesis Enzyme-linked Immunosorbent Assay Fabaceae Fibroblast Culture Human Human Cell Ic 50 In Vitro Study In Vivo Study Macrophage Malpighiaceae Medicinal Plant Melanoma Cell Line Melastomataceae Miconia Nervosa Mouse Nonhuman Parasitemia Parkia Nitida Plant Leaf Plasmodium Berghei Infection Plasmodium Falciparum Plasmodium Falciparum K1 Plasmodium Falciparum W2 Stigmaphyllon Sinuatum Varietas Xylopia Xylopia Amazonica Zanthoxylum Zanthoxylum Djalma Batistae Animals Bagg Albino Mouse Brasil Cell Culture Cell Survival Chemistry Disease Model Drug Effects Drug Sensitivity Isolation And Purification Malaria Plant Plasmodium Berghei Treatment Outcome Animal Antimalarials Brasil Cell Survival Cells, Cultured Disease Models, Animals Humans Inhibitory Concentration 50 Malaria Mice, Inbred Balb C Parasitemia Parasitic Sensitivity Tests Plant Extracts Plants Plasmodium Berghei Plasmodium Falciparum Treatment Outcome |
| description |
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. |
| format |
Artigo |
| author |
Lima, Renata Braga Souza |
| author2 |
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 |
| author2Str |
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 |
| title |
In vitro and in vivo anti-malarial activity of plants from the Brazilian Amazon |
| title_short |
In vitro and in vivo anti-malarial activity of plants from the Brazilian Amazon |
| title_full |
In vitro and in vivo anti-malarial activity of plants from the Brazilian Amazon |
| title_fullStr |
In vitro and in vivo anti-malarial activity of plants from the Brazilian Amazon |
| title_full_unstemmed |
In vitro and in vivo anti-malarial activity of plants from the Brazilian Amazon |
| title_sort |
in vitro and in vivo anti-malarial activity of plants from the brazilian amazon |
| publisher |
Malaria Journal |
| publishDate |
2020 |
| url |
https://repositorio.inpa.gov.br/handle/1/15871 |
| _version_ |
1787142939224309760 |
| score |
11.755432 |