Use este identificador para citar ou linkar para este item: https://repositorio.inpa.gov.br/handle/1/17604
Título: Antiplasmodial activity of synthetic ellipticine derivatives and an isolated analog
Autor: Montoia, Andréia
Silva, Luiz Francisco Rocha e
Torres, Zelina Estevam dos Santos
Costa, David Siqueira
Henrique, Marycleuma Campos
Lima, Emerson Silva
Vasconcellos, Marne Carvalho de
Souza, Rita C.Z.
Costa, Mônica Regina Farias
Grafov, Andrèi Andriy
Grafova, Iryna A.
Eberlin, M. N.
Tadei, Wanderli Pedro
Amorim, Rodrigo C.N.
Pohlit, Adrian Martin
Palavras-chave: 2 Methyl 1,2,3,4 Tetrahydroellipticine
3,4 Dihydroellipticine
7 Nitroellipticine
7,8,9 Tribromoellipticine
7,9 Dibromoellipticine
9 Bromoellipticine
9 Hydroxyellipticine
9 Methoxyellipticine
9 Nitroellipticine
Antimalarial Agent
Chloroquine
Ellipticine
Ellipticine Derivative
Olivacine
Unclassified Drug
Antimalarial Agent
Chloroquine
Ellipticine
Ellipticine Derivative
2 Methyl 1,2,3,4 Tetrahydroellipticine
7 Nitroellipticine
7,9 Dibromoellipticine
9 Nitroellipticine
Antimalarial Agent
Chloroquine
Ellipticine
Ellipticine Derivative
Olivacine
Quinine Sulfate
Antimalarial Activity
Aspidosperma
Aspidosperma Vargasii
Bark
Bromination
Controlled Study
Drug Cytotoxicity
Drug Effect
Drug Isolation
Drug Potency
Fetus
Human
Human Cell
Ic 50
In Vitro Study
Lung Fibroblast
Medicinal Plant
Nitration
Nonhuman
Plasmodium Berghei
Plasmodium Falciparum
Animals
Chemical Structure
Chemistry
Disease Model
Drug Effects
Fibroblast
Mouse
Synthesis
Animals Cell
Animals Experiment
Animals Model
Antiplasmodial Activity
Aspidosperma
Aspidosperma Vargasii
Carbon Nuclear Magnetic Resonance
Drug Structure
Drug Synthesis
Macrophage
Malaria
Malaria Control
Mass Spectrometry
Parasitemia
Proton Nuclear Magnetic Resonance
Aspidosperma
Plasmodium Falciparum
Animal
Antimalarials
Aspidosperma
Chloroquine
Disease Models, Animals
Ellipticines
Fibroblasts
Humans
Mice
Molecular Structure
Plant Bark
Plasmodium Falciparum
Data do documento: 2014
Revista: Bioorganic and Medicinal Chemistry Letters
É parte de: Volume 24, Número 12, Pags. 2631-2634
Abstract: Ellipticine has been shown previously to exhibit excellent in vitro antiplasmodial activity and in vivo antimalarial properties that are comparable to those of the control drug chloroquine in a mouse malaria model. Ellipticine derivatives and analogs exhibit antimalarial potential however only a few have been studied to date. Herein, ellipticine and a structural analog were isolated from Aspidosperma vargasii bark. A-ring brominated and nitrated ellipticine derivatives exhibit good in vitro inhibition of Plasmodium falciparum K1 and 3D7 strains. Several of the compounds were found not to be toxic to human fetal lung fibroblasts. 9-Nitroellipticine (IC50 = 0.55 μM) exhibits greater antiplasmodial activity than ellipticine. These results are further evidence of the antimalarial potential of ellipticine derivatives. © 2014 Elsevier Ltd. All rights reserved.
DOI: 10.1016/j.bmcl.2014.04.070
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