Study of crystal and molecular structure of synthetic riparin derivatives with effects against Schistosoma mansoni

• Grant number: 14/20297-0
• Support Opportunities: Scholarships in Brazil - Scientific Initiation
• Start date: December 01, 2014
• End date: May 31, 2015
• Field of knowledge: Physical Sciences and Mathematics - Physics - Atomic and Molecular Physics
• Principal Investigator: Ana Carolina Mafud
• Grantee: Thiago Israel Rubio
• Host Institution: Instituto de Física de São Carlos (IFSC). Universidade de São Paulo (USP). São Carlos , SP, Brazil

Abstract

Schistosomiasis is caused by worms of genus Schistosoma. It has become one of the worst neglected diseases on the planet, affecting more than 200 million people in poor neighborhoods without sanitation, being the most fatal verminose worldwide. Schistosomiasis treatment and control are dependent upon a single drug, praziquantel, which is on the market for over three decades. Due to its continuous use in monotherapy, conducted throughout this time, evidence of drug resistance was evaluated. Therefore, new chemotherapies are urgently needed. Riparins are alkaloids extracted from Aniba riparia fruit, which show pharmacological activity and low toxicity. In this sense, new riparins derivatives were designed and synthesized, and their in vitro effects against adult worms of Schistosoma mansoni were evaluated. This project aims to determine riparins A, B, C and D crystal structures by X-Ray Diffraction and analyze their similarities with praziquantel in order to establish structure-activity relationships between these compounds in schistosomiasis treatment.