Use este identificador para citar ou linkar para este item: http://repositorio.inpa.gov.br/handle/123/4782
Título: Biological activity of neoergeolide and isobrucein B isolated from the Amazonian medicinal plant Picrolemma sprucei (Simaroubaceae)
Autor(es): Ellen Cristina Costa da Silva
Bruno Coêlho Cavalcanti
Rodrigo C N Amorim
Jorcilene F. Lucena
Dulcimar Silva Quadros
Wanderli Pedro Tadei
Raquel C. Montenegro
Leticia Veras Costa-Lotufo
Cláudia Pessoa
Manoel Odorico Moraes
Rita de Cássia Saraiva Nunomura
Márcia Rubia S Melo
Valter F de Andrade-Neto
Luiz Francisco Rocha Silva
Pedro Paulo R Vieira
Adrian Martin Pohlit
Sergio Massayoshi Nunomura
Assunto: cytotoxicity
Antimalarial
larvicidal
ISSN: 1678-8060
Revista: Memórias do Instituto Oswaldo Cruz
Volume: 104
Resumo: In the present study, in vitro techniques were used to investigate a range of biological activities of known natural quassinoids isobrucein B (1) and neosergeolide (2), known semi-synthetic derivative 1,12-diacetylisobrucein B (3), and a new semi-synthetic derivative, 12-acetylneosergeolide (4). These compounds were evaluated for general toxicity toward the brine shrimp species Artemia franciscana, cytotoxicity toward human tumour cells, larvicidal activity toward the dengue fever mosquito vector Aedes aegypti, haemolytic activity in mouse erythrocytes and antimalarial activity against the human malaria parasite Plasmodium falciparum. Compounds 1 and 2 exhibited the greatest cytotoxicity against all the tumor cells tested (IC50 = 5-27 µg/L) and against multidrug-resistant P. falciparum K1 strain (IC50 = 1.0-4.0 g/L) and 3 was only cytotoxic toward the leukaemia HL-60 strain (IC50 = 11.8 µg/L). Quassinoids 1 and 2 (LC50 = 3.2-4.4 mg/L) displayed greater lethality than derivative 4 (LC50 = 75.0 mg/L) toward A. aegypti larvae, while derivative 3 was inactive. These results suggest a novel application for these natural quassinoids as larvicides. The toxicity toward A. franciscana could be correlated with the activity in several biological models, a finding that is in agreement with the literature. Importantly, none of the studied compounds exhibited in vitro haemolytic activity, suggesting specificity of the observed cytotoxic effects. This study reveals the biological potential of quassinoids 1 and 2 and to a lesser extent their semi-synthetic derivatives for their in vitro antimalarial and cytotoxic activities.
URI: http://repositorio.inpa.gov.br/handle/123/4782
ISSN: 1678-8060
DOI: https://dx.doi.org/10.1590/S0074-02762009000100008
Aparece nas coleções:Coordenação de Tecnologia e Inovação (COTI)

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