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Antileishmanial activity of isolated triterpenoids from Pourouma guianensis

2004; Elsevier BV; Volume: 11; Issue: 2-3 Linguagem: Inglês

10.1078/0944-7113-00381

1618-095X

Eduardo Caio Torres-Santos, Danilo de Paiva Lopes, Rodrigo Cardoso de Oliveira, J. P. P. Carauta, Camila Alves Bandeira Falcão, Maria Auxiliadora Coelho Kaplan, Bartira Rossi‐Bergmann,

Research on Leishmaniasis Studies

The inhibiting activity of triterpenoids isolated from the methanolic extract of Pourouma guianensis (Moraceae) leaves is described for promastigotes and intracellular amastigotes of Leishmania amazonensis. Whereas the fractions containing apigenin, friedelin, epi-friedelinol, arjunolic acid, hyptatic acid B, stigmasterol and sitosterol were of no or relatively low inhibitory activity, fractions containing tormentic acid, 2α,3β-dihydroxyursan-12-en-28-oic acid, 2α,3β-dihydroxyolean-12-en-28-oic acid, oleanolic acid and ursolic acid were very potent in inhibiting promastigote growth at 100 μg/ml. Of the eleven isolated compounds, however, only ursolic acid and oleanolic acid showed high activity against intracellular amastigotes (IC50 value = 27 μg/ml and 11 μg/ml, respectively), which was superior to the control drug Glucantime (IC50 value = 83 μg/ml). The antileishmanial activity of oleanolic acid was directed against the parasite and not due to activation of nitric oxide intermediates by macrophages, but this triterpenoid also significantly inhibited the phagocytic capacity of those cells at concentrations above 40 μg/ml, indicating a cytotoxic effect. These results indicate that Pourouma guianensis contains many triterpenoids and some, such as ursolic and oleanolic acids, may serve as lead compounds for new antileishmanial drugs, but chemical modifications may be necessary to avoid unselective cytotoxicity.