Fungal Transformation and Schistosomicidal Effects of Pimaradienoic Acid

Wiley - Tập 9 Số 8 - Trang 1465-1474 - 2012
Thiago S. Porto1, Ademar Alves da Silva Filho1, Lizandra Guidi Magalhães1, Raquel Alves dos Santos1, Niege Araçari Jacometti Cardoso Furtado2, Nilton Syogo Arakawa3, Suraia Said2, Dionéia Camilo Rodrigues de Oliveira2, Luiz Elídio Gregório2, Vanderlei Rodrigues4, Rodrigo Cássio Sola Veneziani1, Sérgio Ricardo Ambrósio1
1Núcleo de Pesquisa em Ciências Exatas e Tecnológicas, Universidade de Franca, Franca, SP, Brazil, (phone: +55-16-37118878)
2Faculdade de Ciências Farmacêuticas de Ribeirão Preto, Universidade de São Paulo, Ribeirão Preto, SP, Brazil
3Instituto de Pesquisa e Desenvolvimento da Universidade do Vale do Paraíba, São José dos Campos, SP, Brazil
4Faculdade de Medicina de Ribeirão Preto, Universidade de São Paulo – Ribeirão Preto/SP, Brazil

Tóm tắt

AbstractThe 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 μM. 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.

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Wiley

Tập 9 Số 8

1465-1474

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