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Trypanocidal activity of copalic acid and their synthetics derivatives

Grant number: 12/16168-5
Support type:Regular Research Grants
Duration: March 01, 2013 - February 28, 2015
Field of knowledge:Health Sciences - Pharmacy
Principal Investigator:Sérgio de Albuquerque
Grantee:Sérgio de Albuquerque
Home Institution: Faculdade de Ciências Farmacêuticas de Ribeirão Preto (FCFRP). Universidade de São Paulo (USP). Ribeirão Preto , SP, Brazil

Abstract

Neglected tropical diseases (NTDs) affect more than 1 billion people worldwide. Chagas' disease is one of the major NTDs and remains such a public health problem, where thousands of people are infected and others remain at risk of infection. There is no effective drug against the parasite, Trypanosoma cruzi and the existing drugs have severe side effects and low efficacy. Because this problem the researchers have intensified the search for new therapeutic tools against the parasite. Studies carried out in several countries report that many compounds isolated of vegetal species, such as the terpenes and their synthetic derivatives have been described as antiparasitic agents, with high efficiency and selectivity against T. cruzi. This project proposes the evaluation of trypanocidal activity of the copalic acid, obtained by organic extraction of copaiba oil (commercially available), and derivatives obtained by partial synthesis, in an attempt to potentiate the biological activity of the natural product. The substances will be assayed in vitro and in vivo for the characterization of the trypanocidal activity. The biological assays will be carried out experimentally by in vitro protocols, on amastigotes, trypomastigotes and epimastigotes forms of T. cruzi and in vivo protocols on experimentally infected animals, observing the effects of the compounds against two different strains of the parasite. The parasites will be quantified both in the blood, by hemocytometer as in tissue by qPCR. (AU)