Revista Cubana de Plantas Medicinales
versão On-line ISSN 1028-4796
GALVIS, Jhon H et al. Assessment of the in vitro leishmanicide activity of Annona cherimolioides extracts. Rev Cubana Plant Med [online]. 2010, vol.15, n.4, pp. 209-218. ISSN 1028-4796.
INTRODUCTION: the use of our flora allows a approach to search of new substances with a high level of bioactivity characteristic of the Annonaceae family where it is reported a series of secondary metabolites very promissory to attack these pathogens. OBJECTIVE: to assess the leishmanicidal activity on intracellular amastigotes of Leishmania (V) panamensis and the toxic activity on human macrophages and Artemia salina. METHODS: it was applied the column chromatography and the preparative layer chromatography for extraction and isolation of alkaloids present in the stem bark of Annona cherimolioides Triana & Planch. Alkaloid extracts and fractions were assessed to determine the leishmanicidal activity by flow cytometry as well as cytotoxic activity on the U937 cellular line and on the peritoneal macrophages of hamster. The in vivo cytotoxic activity was assessed on Artemia salina. RESULTS: a purifying compound was obtained in which the presence of an aporphine nucleus was determined by 1-H nuclear magnetic resonance and spectrophotometry. There wasn't activity against the Leishmania parasites. The crude extract showed the highest toxicity on Artemia salina whereas the purifying compound showed a moderate toxicity on the U937 cell line. DISCUSSION: there was a selective cytotoxic activity against tumoral cells (U397 cell line) compared to toxicity seen in the primary culture (non-tumoral). Due to the cytotoxicity showed on the above cell line, it was impossible to determine the effective concentration of extracts against intracellular amastigotes, thus it is necessary to continue the assessments of in vitro systems using non-tumoral cells.
Palavras-chave : alkaloids; leishmanicide activity; Annona cherimolioides; cytotoxicity.