RESUMO
Five new oxoprotoberberine alkaloids, miliusacunines A-E (1-5), along with nine known compounds, 6-14, were isolated from an acetone extract of the leaves and twigs of Miliusa cuneata. Their structures were elucidated by spectroscopic analysis. All isolated compounds were evaluated for their cytotoxicities against the KB and Vero cell lines and for antimalarial activities against the Plasmodium falciparum strains TM4 and K1 (a sensitive and a multi-drug-resistant strain, respectively). Compound 1 showed in vitro antimalarial activity against the TM4 strain, with an IC50 value of 19.3 ± 3.4 µM, and compound 2 demonstrated significant activity against the K1 strain, with an IC50 value of 10.8 ± 4.1 µM. Both compounds showed no discernible cytotoxicity to the Vero cell line at the concentration levels evaluated.
Assuntos
Alcaloides/isolamento & purificação , Alcaloides/farmacologia , Annonaceae/química , Antimaláricos/isolamento & purificação , Antimaláricos/farmacologia , Malária/tratamento farmacológico , Plasmodium falciparum/efeitos dos fármacos , Alcaloides/química , Animais , Antimaláricos/química , Chlorocebus aethiops , Relação Dose-Resposta a Droga , Humanos , Células KB , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular , Folhas de Planta/química , Plasmodium berghei , Células VeroRESUMO
One new p-quinonoid aporphine alkaloid, obtusipetadione (1), and eleven known compounds (2-12) were isolated from the acetone extract of the twigs of Dasymaschalon obtusipetalum. Their structures were elucidated by spectroscopic methods. The cytotoxic and antimalarial activities of the isolated compounds were evaluated. Compound 1 showed significant in vitro antiplasmodial activity against the P. falciparum strains TM4 and K1 (multidrug resistant strain) with IC50 values of 2.46 ± 0.12 and 1.38 ± 0.99 µg/mL, respectively with no cytotoxicity. Compound 9 had more modest antiplasmodial activity, but significant cytotoxicity.
