Tranformações químicas no alcalóide natural piperina e avaliação tóxica sobre Trypanosoma cruzi

Abstract

This work is part of a research program aiming at the use of abundant natural products in the synthesis of new molecules with potential application as antiparasitic drugs. We describe herein an evaluation of trypanocida effects of the natural alkaloid piperine (isolated from Piper nigrum) and twelve synthetic derivatives against epimastigote and amastigote forms of the protozoan parasite Trypanosoma cruzi, the causative agent of the incurable human disease, Chagas' disease. Piperine was tested against T. cruzi epimastigotes showing a dose-dependent toxicity, with IC50 of 7.36 mM This preliminary result encouraged us to prepare a series of derivatives in order to determine the chemical features present in piperine responsible for the trypanocidal activity. The results obtained point to piperine and its derivatives as a suitable templates for the development of a new family of drugs with trypanocida activity.