Biotransformation studies of trypanocidal agent grandisin by endophytic fungi

• Grant number: 05/04003-8
• Support Opportunities: Scholarships in Brazil - Scientific Initiation
• Start date: January 01, 2006
• End date: August 31, 2007
• Field of knowledge: Health Sciences - Pharmacy
• Principal Investigator: Ivone Carvalho
• Grantee: Michelle Verza
• Host Institution: Faculdade de Ciências Farmacêuticas de Ribeirão Preto (FCFRP). Universidade de São Paulo (USP). Ribeirão Preto , SP, Brazil

Abstract

The tropical illnesses constitute a serious problem for the countries of the third World. In the case of the of Chagas, it has a register in order of 20 million the infects. The only chemoprophylatic agent in use for the elimination of the parasite in the blood is the gentian violet. Grandisin is a lignan isolated from Virola surinamensis (Myristicaceae) whose extract presented strong trypanocidal activity, but is known that it is very lipofilic, and it shows low biodisponibility. Owing to the great diversity of the fungi and its potential in generating metabolite products of therapeutic interest, the aim of this work is the study of the biotransformation of grandisin with the purpose to generate metabolites with balanced polarity, as products of O-demethylation and also any others produced, to increase its biodisponibility and get an effective activity in vivo. The progression of reactions will be performed by HPLC and TLC. The structure of the metabolite will be determined by NMR, IR and Mass spectroscopy.