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DOI: 10.1055/s-0037-1608112
Isolation of potent tripanocidal compounds – primin and miconidin – through a bioguided study of Miconia wildenowii
Publication History
Publication Date:
24 October 2017 (online)
Trypanosoma cruzi affects about 8 to 9 million people all over the world, leading to approximately 14,000 deaths annually, therefore considered one of the most troublesome disease among those known like neglected. The demand for more effective medicines against T. cruzi parasites has rised, leading to search for new compounds mainly natural products plant derivatives. From a screening of crude extracts of different species of plants, Miconia wildenowii, an endemic Brazilian rainforest specie, presented high biological activity against epimastigote forms, strain Y, of T. cruzi. Then, its crude extract was partitioned into hexane, ethyl acetate and mixture ethanol: water. The three fractions were submitted to the same anti-epimastigote assay showing that the ethyl acetate fraction was the most active. This fraction was subjected to silica gel column chromatography and eluted with a gradient of solvents like hexane, ethyl acetate and methanol by gradually increasing the polarity, yielding 12 subfractions. These also were evaluated against T. cruzi epimastigotes forms in which three of them presented higher antichagasic activity. HPLC-UV-DAD profile of these active subfractions exposed the same two compounds. Isolation was performed in the same equipament and identification could be made by NMR and mass data of the compounds, in comparison with data on literature, characterized as primin and miconidin. The anti-epimastigote assay with both primin (EC50 = 2,59µM) and miconidin (EC50 = 5,70µM) showed that they are more efficient than the reference drug benznidazole (EC50 = 9,46µM). Both isolated compounds presented cytotoxic effects only in higher concentration, evidencing the anti-chagasic potential of them.
FAPEMIG, FINEP, CAPES and CNPq.
Paucar R. et al. Curr Med Chem. 2016;23:3154 – 3170.