Fungal Transformation and Schistosomicidal Effects of Pimaradienoic Acid

Autor(es):Mostrar menos -

Porto, Thiago S. ^[1] ; da Silva Filho, Ademar A. ^[1] ; Magalhaes, Lizandra G. ^[1] ; dos Santos, Raquel A. ^[1] ; Furtado, Niege A. J. C. ^[2] ; Arakawa, Nilton S. ^[3] ; Said, Suraia ^[2] ; de Oliveira, Dioneia C. R. ^[2] ; Gregorio, Luiz E. ^[2] ; Rodrigues, Vanderlei ^[4] ; Veneziani, Rodrigo C. S. ^[1] ; Ambrosio, Sergio R. ^[1]

Afiliação do(s) autor(es)

^[1] Univ Franca, Nucleo Pesquisa Ciencias Exatas & Tecnol, Franca, SP - Brazil

^[2] Univ Sao Paulo, Fac Ciencias Farmaceut Ribeirao Preto, Ribeirao Preto, SP - Brazil

^[3] Univ Vale Paraiba, Inst Pesquisa & Desenvolvimento, Sao Jose Dos Campos, SP - Brazil

^[4] Univ Sao Paulo, Fac Med Ribeirao Preto, Ribeirao Preto, SP - Brazil

• Tipo de documento: Artigo Científico
• Fonte: CHEMISTRY & BIODIVERSITY; v. 9, n. 8, p. 1465-1474, AUG 2012.
• Citações Web of Science: 12

Resumo

The schistosomicidal effects of pimaradienoic acid (PA) and two derivatives, obtained by fungal transformation in the presence of Aspergillus ochraceus, were investigated. PA was the only compound with antischistosomal activity among the three diterpenes studied, with the ability to significantly reduce the viability of the parasites at concentrations ranging from 25 to 100 mu M. PA also promoted morphological alterations of the tegument of Schistosoma mansoni, separated all the worm couples, and affected the production and development of eggs. Moreover, this compound was devoid of toxicity toward human fibroblasts. In a preliminary in vivo experiment, PA at a dose of 100 mg/kg significantly diminished the number of parasites in infected Balb/c mice. Taken together, these results show that PA may be potentially employed in the discovery of novel schistosomicidal agents, and that diterpenes are an important class of natural compounds for the investigation of agents capable of fighting the parasite responsible for human schistosomiasis. (AU)

• Processo FAPESP: 07/54762-8 - Obtenção de análogos estruturais do ácido pimaradienóico através do processo de biotransformação fúngica e estudo do efeito destes metabólitos sobre a atividade da enzima TcDHODH e sobre a contração da musculatura lisa vascular de artéria aorta de ratos
• Beneficiário: Sergio Ricardo Ambrosio
• Modalidade de apoio: Auxílio à Pesquisa - Programa BIOTA - Jovens Pesquisadores
• Processo FAPESP: 08/07696-2 - Estudos sobre a biotransformação fúngica de dois diterpenos da classe dos pimaranos por Aspergillus ochraceus e avaliação biológica dos metabólitos obtidos.
• Beneficiário: Thiago Sousa Porto
• Modalidade de apoio: Bolsas no Brasil - Mestrado