Fungal Transformation and Schistosomicidal Effects of Pimaradienoic Acid

Author(s):Show less -

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]

Affiliation

^[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

• Document type: Journal article
• Source: CHEMISTRY & BIODIVERSITY; v. 9, n. 8, p. 1465-1474, AUG 2012.
• Web of Science Citations: 12

Abstract

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)

• FAPESP's process: 07/54762-8 - Obtaining structural analogues of pimaradienoic acid through the process of fungal biotransformation and study of the effect of these metabolites on the activity of the TcDHODH enzyme and on the contraction of the vascular smooth muscle of the aorta artery of mice
• Grantee: Sergio Ricardo Ambrosio
• Support Opportunities: BIOTA-FAPESP Program - Young Investigators Grants
• FAPESP's process: 08/07696-2 - Studies on the biotransformation of two fungal diterpene class of pimaranos by Aspergillus ochraceus and biological evaluation of the metabolites obtained.
• Grantee: Thiago Sousa Porto
• Support Opportunities: Scholarships in Brazil - Master