Diterpenoids from Azorella compacta (Umbelliferae) active on Trypanosoma cruzi

Diterpenoids from Azorella compacta (Umbelliferae) active on Trypanosoma cruzi

Autor Araya, Jorge E Google Scholar
Neira, Iván Google Scholar
Silva, Solange da Autor UNIFESP Google Scholar
Mortara, Renato Arruda Autor UNIFESP Google Scholar
Manque, Patricio Google Scholar
Cordero, Esteban Mauricio Autor UNIFESP Google Scholar
Sagua, Hernán Google Scholar
Loyola, Alberto Google Scholar
Bórquez, Jorge Google Scholar
Morales, Glauco Google Scholar
González, Jorge Google Scholar
Instituição Universidad de Antofagasta Departamento de Tecnología Médica Unidad de Parasitología
Universidad de Antofagasta Departamento de Química Laboratorio de Productos Naturales
Universidade Federal de São Paulo (UNIFESP)
Resumo The anti-Trypanosoma cruzi activity of natural products isolated from Azorella compacta was evaluated, with particular emphasis on their effect against intracellular amastigotes. Five diterpenoids from A. compacta derived from mulinane and azorellane were isolated and identified. Only two products, named azorellanol (Y-2) and mulin-11,3-dien-20-oic acid (Y-5), showed trypanocidal activity against all stages of T. cruzi including intracellular amastigotes. At 10 µM, these compounds displayed a strong lytic activity. It ranged from 88.4 ± 0.6 to 99.0 ± 1 % for all strains and stages evaluate, with an IC50 /18 h values of 20-84 µM and 41-87 µM, respectively. The development of intracellular amastigotes was also inhibited by nearly 60% at 25 µM. The trypanocidal molecules Y-2 and Y-5 did show different degrees of cytotoxicity depending on the cell line tested, with an IC50 /24 h ranging from 33.2 to 161.2 µM. We evaluated the effect of diterpenoids against intracellular T. cruzi forms by immunofluorescent identification of a specific membrane molecular marker (Ssp-4 antigen) of the T. cruzi amastigote forms. The accuracy and reproducibility of the measurements were found to be outstanding when examined by confocal microscopy.
Palavra-chave Trypanosoma cruzi
intracellular amastigotes
lysis
diterpenoids
Azorella compacta
chemotherapy
confocal microscopy
Idioma Inglês
Data de publicação 2003-04-01
Publicado em Memórias do Instituto Oswaldo Cruz. Instituto Oswaldo Cruz, Ministério da Saúde, v. 98, n. 3, p. 413-418, 2003.
ISSN 0074-0276 (Sherpa/Romeo)
Publicador Instituto Oswaldo Cruz, Ministério da Saúde
Extensão 413-418
Fonte http://dx.doi.org/10.1590/S0074-02762003000300022
Direito de acesso Acesso aberto Open Access
Tipo Artigo
SciELO S0074-02762003000300022 (estatísticas na SciELO)
Endereço permanente http://repositorio.unifesp.br/handle/11600/1680

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