Aspidosperma (Apocynaceae) plant cytotoxicity and activity towards
malaria parasites. Part II: experimental studies with Aspidosperma
ramiflorum in vivo and in vitro |
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Authors: | Anna CC Aguiar Ananda C Cunha Isabela Penna Ceravolo Regina A Correia Gon?alves Arildo JB Oliveira Antoniana Ursine Krettli |
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Institution: | 1.Fundação Oswaldo Cruz, Centro de Pesquisas René Rachou, Belo Horizonte, MG, Brasil;2.Universidade Federal de Minas Gerais, Faculdade de Medicina, Belo Horizonte, MG, Brasil;3.Universidade Estadual de Maringá, Departamento de Farmácia, Programa de Pós-Graduação em Ciências Farmacêuticas, Maringá, PR, Brasil |
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Abstract: | Several species of Aspidosperma plants are used to treat diseases in
the tropics, including Aspidosperma ramiflorum, which acts against
leishmaniasis, an activity that is experimentally confirmed. The species, known as
guatambu-yellow, yellow peroba,
coffee-peroba andmatiambu, grows in the Atlantic
Forest of Brazil in the South to the Southeast regions. Through a guided
biofractionation of A. ramiflorum extracts, the plant activity
against Plasmodium falciparum was evaluated in vitro for toxicity
towards human hepatoma G2 cells, normal monkey kidney cells and nonimmortalised human
monocytes isolated from peripheral blood. Six of the seven extracts tested were
active at low doses (half-maximal drug inhibitory concentration < 3.8 µg/mL); the
aqueous extract was inactive. Overall, the plant extracts and the purified compounds
displayed low toxicity in vitro. A nonsoluble extract fraction and one purified
alkaloid isositsirikine (compound 5) displayed high selectivity indexes (SI) (= 56
and 113, respectively), whereas compounds 2 and 3 were toxic (SI < 10). The
structure, activity and low toxicity of isositsirikine in vitro are described here
for the first time in A. ramiflorum, but only the neutral and
precipitate plant fractions were tested for activity, which caused up to 53%
parasitaemia inhibition of Plasmodium berghei in mice with
blood-induced malaria. This plant species is likely to be useful in the further
development of an antimalarial drug, but its pharmacological evaluation is still
required. |
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Keywords: | Aspidosperma ramiflorum ethnopharmacology antimalarials P falciparum medicinal plants |
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