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Title: In vivo and in vitro antimalarial activity of 4-nerolidylcatechol
Authors: 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
Keywords: 4 Nerolidylcatechol
Antimalarial Agent
Catechol Derivative
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
Growth Inhibition
Human Cell
In Vitro Study
In Vivo Study
Microbial Growth
Piper Peltatum
Plasmodium Berghei
Plasmodium Falciparum
Treatment Response
Disease Models, Animals
Malaria, Falciparum
Plasmodium Berghei
Plasmodium Falciparum
Piper Peltatum
Plasmodium Berghei
Plasmodium Falciparum
Issue Date: 2011
metadata.dc.publisher.journal: Phytotherapy Research
metadata.dc.relation.ispartof: Volume 25, Número 8, Pags. 1181-1188
Abstract: 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.
metadata.dc.identifier.doi: 10.1002/ptr.3424
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