In vivo and in vitro antimalarial activity of 4-nerolidylcatechol
4-Nerolidylcatechol (4-NC) isolated from Piper peltatum L. (Piperaceae) was evaluated for in vitro antiplasmodial activity against Plasmodium falciparum (cultures of both standard CQR (K1) and CQS (3D7) strains and two Amazonian field isolates) and for in vivo antimalarial activity using the Plasmod...
| Autor principal: | Silva, Luiz Francisco Rocha e |
|---|---|
| Outros Autores: | Pinto, Ana Cristina da Silva, Pohlit, Adrian Martin, Quignard, Etienne Louis Jacques, Vieira, Pedro Paulo Ribeiro, Tadei, Wanderli Pedro, Chaves, Francisco Célio Maia, Samonek, Jean Francisco, Lima, Carlos Alberto Jatoba, Costa, Mônica Regina Farias, Alecrim, Maria das Graças Costa, Andrade Neto, Valter Ferreira de |
| Grau: | Artigo |
| Idioma: | English |
| Publicado em: |
Phytotherapy Research
2020
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| Acesso em linha: |
https://repositorio.inpa.gov.br/handle/1/18169 |
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oai:repositorio:1-18169 |
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oai:repositorio:1-18169 In vivo and in vitro antimalarial activity of 4-nerolidylcatechol Silva, Luiz Francisco Rocha e Pinto, Ana Cristina da Silva Pohlit, Adrian Martin Quignard, Etienne Louis Jacques Vieira, Pedro Paulo Ribeiro Tadei, Wanderli Pedro Chaves, Francisco Célio Maia Samonek, Jean Francisco Lima, Carlos Alberto Jatoba Costa, Mônica Regina Farias Alecrim, Maria das Graças Costa Andrade Neto, Valter Ferreira de 4 Nerolidylcatechol Antimalarial Agent Catechol Derivative Chloroquine Unclassified Drug Animals Cell Animals Experiment Animals Model Antimalarial Activity Blood Sampling Concentration (parameters) Controlled Study Drug Determination Drug Dose Comparison Drug Inhibition Drug Metabolism Drug Structure Female Growth Inhibition Human Human Cell In Vitro Study In Vivo Study Malaria Microbial Growth Mouse Nonhuman Piper Peltatum Piperaceae Plasmodium Berghei Plasmodium Falciparum Treatment Response Animal Antimalarials Brasil Catechols Disease Models, Animals Female Malaria Malaria, Falciparum Mice Piper Plasmodium Berghei Plasmodium Falciparum Murinae Mus Piper Peltatum Piperaceae Plasmodium Berghei Plasmodium Falciparum 4-Nerolidylcatechol (4-NC) isolated from Piper peltatum L. (Piperaceae) was evaluated for in vitro antiplasmodial activity against Plasmodium falciparum (cultures of both standard CQR (K1) and CQS (3D7) strains and two Amazonian field isolates) and for in vivo antimalarial activity using the Plasmodium berghei-murine model. 4-NC exhibits significant in vitro and moderate in vivo antiplasmodial activity. 4-NC administered orally and subcutaneously at doses of 200, 400 and 600 mg/kg/day suppressed the growth of P. berghei by up to 63% after four daily treatments (days 1-4). Also, 4-NC exhibited important in vitro antiplasmodial activity against both standard and field P. falciparum strains in which 50% inhibition of parasite growth (IC 50) was produced at concentrations of 0.05-2.11 μg/mL and depended upon the parasite strain. Interestingly, healthy (non-infected) mice that received 4-NC orally presented (denatured) blood plasma which exhibited significant in vitro activity against P. falciparum. This is evidence that mouse metabolism allows 4-NC or active metabolites to enter the blood. Further chemical and pharmacological studies are necessary to confirm the potential of 4-NC as a new antimalarial prototype. Copyright © 2011 John Wiley & Sons, Ltd. 2020-06-15T21:52:15Z 2020-06-15T21:52:15Z 2011 Artigo https://repositorio.inpa.gov.br/handle/1/18169 10.1002/ptr.3424 en Volume 25, Número 8, Pags. 1181-1188 Restrito Phytotherapy Research |
| institution |
Instituto Nacional de Pesquisas da Amazônia - Repositório Institucional |
| collection |
INPA-RI |
| language |
English |
| topic |
4 Nerolidylcatechol Antimalarial Agent Catechol Derivative Chloroquine Unclassified Drug Animals Cell Animals Experiment Animals Model Antimalarial Activity Blood Sampling Concentration (parameters) Controlled Study Drug Determination Drug Dose Comparison Drug Inhibition Drug Metabolism Drug Structure Female Growth Inhibition Human Human Cell In Vitro Study In Vivo Study Malaria Microbial Growth Mouse Nonhuman Piper Peltatum Piperaceae Plasmodium Berghei Plasmodium Falciparum Treatment Response Animal Antimalarials Brasil Catechols Disease Models, Animals Female Malaria Malaria, Falciparum Mice Piper Plasmodium Berghei Plasmodium Falciparum Murinae Mus Piper Peltatum Piperaceae Plasmodium Berghei Plasmodium Falciparum |
| spellingShingle |
4 Nerolidylcatechol Antimalarial Agent Catechol Derivative Chloroquine Unclassified Drug Animals Cell Animals Experiment Animals Model Antimalarial Activity Blood Sampling Concentration (parameters) Controlled Study Drug Determination Drug Dose Comparison Drug Inhibition Drug Metabolism Drug Structure Female Growth Inhibition Human Human Cell In Vitro Study In Vivo Study Malaria Microbial Growth Mouse Nonhuman Piper Peltatum Piperaceae Plasmodium Berghei Plasmodium Falciparum Treatment Response Animal Antimalarials Brasil Catechols Disease Models, Animals Female Malaria Malaria, Falciparum Mice Piper Plasmodium Berghei Plasmodium Falciparum Murinae Mus Piper Peltatum Piperaceae Plasmodium Berghei Plasmodium Falciparum Silva, Luiz Francisco Rocha e In vivo and in vitro antimalarial activity of 4-nerolidylcatechol |
| topic_facet |
4 Nerolidylcatechol Antimalarial Agent Catechol Derivative Chloroquine Unclassified Drug Animals Cell Animals Experiment Animals Model Antimalarial Activity Blood Sampling Concentration (parameters) Controlled Study Drug Determination Drug Dose Comparison Drug Inhibition Drug Metabolism Drug Structure Female Growth Inhibition Human Human Cell In Vitro Study In Vivo Study Malaria Microbial Growth Mouse Nonhuman Piper Peltatum Piperaceae Plasmodium Berghei Plasmodium Falciparum Treatment Response Animal Antimalarials Brasil Catechols Disease Models, Animals Female Malaria Malaria, Falciparum Mice Piper Plasmodium Berghei Plasmodium Falciparum Murinae Mus Piper Peltatum Piperaceae Plasmodium Berghei Plasmodium Falciparum |
| description |
4-Nerolidylcatechol (4-NC) isolated from Piper peltatum L. (Piperaceae) was evaluated for in vitro antiplasmodial activity against Plasmodium falciparum (cultures of both standard CQR (K1) and CQS (3D7) strains and two Amazonian field isolates) and for in vivo antimalarial activity using the Plasmodium berghei-murine model. 4-NC exhibits significant in vitro and moderate in vivo antiplasmodial activity. 4-NC administered orally and subcutaneously at doses of 200, 400 and 600 mg/kg/day suppressed the growth of P. berghei by up to 63% after four daily treatments (days 1-4). Also, 4-NC exhibited important in vitro antiplasmodial activity against both standard and field P. falciparum strains in which 50% inhibition of parasite growth (IC 50) was produced at concentrations of 0.05-2.11 μg/mL and depended upon the parasite strain. Interestingly, healthy (non-infected) mice that received 4-NC orally presented (denatured) blood plasma which exhibited significant in vitro activity against P. falciparum. This is evidence that mouse metabolism allows 4-NC or active metabolites to enter the blood. Further chemical and pharmacological studies are necessary to confirm the potential of 4-NC as a new antimalarial prototype. Copyright © 2011 John Wiley & Sons, Ltd. |
| format |
Artigo |
| author |
Silva, Luiz Francisco Rocha e |
| author2 |
Pinto, Ana Cristina da Silva Pohlit, Adrian Martin Quignard, Etienne Louis Jacques Vieira, Pedro Paulo Ribeiro Tadei, Wanderli Pedro Chaves, Francisco Célio Maia Samonek, Jean Francisco Lima, Carlos Alberto Jatoba Costa, Mônica Regina Farias Alecrim, Maria das Graças Costa Andrade Neto, Valter Ferreira de |
| author2Str |
Pinto, Ana Cristina da Silva Pohlit, Adrian Martin Quignard, Etienne Louis Jacques Vieira, Pedro Paulo Ribeiro Tadei, Wanderli Pedro Chaves, Francisco Célio Maia Samonek, Jean Francisco Lima, Carlos Alberto Jatoba Costa, Mônica Regina Farias Alecrim, Maria das Graças Costa Andrade Neto, Valter Ferreira de |
| title |
In vivo and in vitro antimalarial activity of 4-nerolidylcatechol |
| title_short |
In vivo and in vitro antimalarial activity of 4-nerolidylcatechol |
| title_full |
In vivo and in vitro antimalarial activity of 4-nerolidylcatechol |
| title_fullStr |
In vivo and in vitro antimalarial activity of 4-nerolidylcatechol |
| title_full_unstemmed |
In vivo and in vitro antimalarial activity of 4-nerolidylcatechol |
| title_sort |
in vivo and in vitro antimalarial activity of 4-nerolidylcatechol |
| publisher |
Phytotherapy Research |
| publishDate |
2020 |
| url |
https://repositorio.inpa.gov.br/handle/1/18169 |
| _version_ |
1787143191154130944 |
| score |
11.755432 |