Atividade antileishmania do eupomatenóide-5, substância isolada de folhas de Piper regnellii var. pallescens

• Ano de defesa: 2006
• Autor(a) principal: Vendrametto, Michele Cristina
• Tipo de documento: Dissertação
• Tipo de acesso: Acesso aberto
• Idioma: por
• Instituição de defesa: Universidade Estadual de Maringá; Brasil; Programa de Pós-Graduação em Ciências Farmacêuticas; UEM; Maringá,PR; Departamento de Farmácia e Farmacologia
• Palavras-chave em Português: Pariparoba; Piper regnellii var pallescens; Leishmania amazonensis; Atividade antileishmania; Eupomatóide-5; Plantas medicinais; Neolignanas; Fitofármaco; Citotoxidade; Ultraestrutura; Brasil.; Piper regnellii; Antileishmanial activity; Euupomatenoid-5; Neolignan; Medicinal plants; Cytotoxicity; Ultrastructure; Brazil.; Ciências da Saúde; Farmácia
• Link de acesso: http://repositorio.uem.br:8080/jspui/handle/1/1938

The main remedies recommended to the treatment of cutaneus and visceral leishmaniasis are derived from the pentavalents antimonials such as sodium estibogluconate (Pentostan®) and meglumine antimonial (Glucantime®), however they are far to be ideal drugs because they are not active when administered orally and need a long period for the treatment. Besides, the side effects can reveal the patients intolerance for this medicaments. Considering that leishmaniasis is endemic in various regions of Brazil, the quest for herbal remedies that are effective for the treatment of this illness is very important, thus the availability of this products could contribute to the its control. The aim of the present work was to invetigate the activity of eupomatenoid-5, isolated from leaves of Piper regnelli (Miq.) C. DC. var. pallescens (C. DC.) Yunck (Piperaceae), over promastigote and amastigote forms of Leishmania amazonensis strain MHOM/BR/75/Josefa. Toxicity of eupomatenoid-5 on J774G8 macrophages and its effect on host-parasite interaction was also evaluated The extraction process and fractionation of Piper regnellii var. pallescens leaves was realized by adsorption chromatography and the compound dihidrobenzofuranic neolignan (eupomatenoid-5) was isolated and characterized by RMN 1H, 13C spectroscopy, comparing to literature data. At µg/ml eupomatenoid-5 presented an inhibitory growth concentration of 50% against promastigotes after 72 h at 28ºC. Under these conditions, significative ultrastructural alterations of the protozoa were visualized through transmission electron microscopy. The toxicity of eupomatenoid-5 against macrophages cell cultures was observed at concentrations higher than the necessary to inhibit the protozoa growth. The effect of eupomatenoid-5 in the leishmania-macrophage interaction is higher when the parasites are treated before the interaction.