Antiplasmodial activity of synthetic ellipticine derivatives and an isolated analog

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

Please use this identifier to cite or link to this item: https://repositorio.inpa.gov.br/handle/1/17604

Title:	Antiplasmodial activity of synthetic ellipticine derivatives and an isolated analog
Authors:	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
Keywords:	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
Issue Date:	2014
metadata.dc.publisher.journal:	Bioorganic and Medicinal Chemistry Letters
metadata.dc.relation.ispartof:	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.
metadata.dc.identifier.doi:	10.1016/j.bmcl.2014.04.070
Appears in Collections:	Artigos

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