Investigação química e farmacológica de espécies vegetais da região Amazônica contra a Malária

Abstract

Malaria is one of the most important parasitic infections of humans due to the high morbidity and mortality. Several drugs have been discovered, from medicinal plants, to act against this disease, among them quinine and artemisinin. With the goal of contributing to the research and to provide the discovery of new antimalarial compounds, were selected two plants of the Amazon region: the species Ampelozizyphus amazonicus known as Indian beer and Vismia cayennensis, known as Lacre. From his botanical parts, were prepared the hexane, chloroform and ethanolic extracts, which were subject to antimalarial schizontocidal liver (against Plasmodium. berghei) and erythrocytic (against Plasmodium. falciparum) tests. The pharmacological results for the specie A. amazonicus, indicate that chloroform and aqueous extracts of the root bark and stem displays an antimalarial activity in vitro against P. berghei with IC50 values between 19.6 and 39.9 μg/mL. The chloroform extract of the root bark was the most active against P. falciparum, through it was possible to isolate and identifity the betulinic acid as the substance most active with value of IC50= 2,56 to 3D7 and 3,76 μg/mL to Dd2. The high performance liquid chromatography allowed the quantification of this constituint in the extracts obtained, being possible to observe a correlation between the quantity of betulinic acid and antimalarial activity observed, thus extracts that showed the highest content of the triterpene were the most active. For samples of V. cayennensis, the chloroform extract was the only active with IC50 = 4.65 for 3D7 and 7.26 μg / mL for Dd2. An in vivo assay, in the hepatic phase, was only possible to identify an active extract, the dichloromethane extract of the stem bark of A. amazonicus. Of the active extracts 12 substances were isolated, being 9 of the specie A. amazonicus and 3 of V. cayennensis. In this context, the ethnopharmacological approach associated with the chemical profile, appear useful and promising tools in the search for new drugs, allowing to contribute significantly to the scientific knowledge of the antimalarial potential of the Amazon flora and thus, open perspectives for the development of new antimalarials