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Trypanocidal activity of pimarane diterpenes from Viguiera arenaria (Asteraceae)
Author(s) -
Ambrósio Sérgio R.,
Arakawa Nilton S.,
Esperandim Viviane R.,
de Albuquerque Sérgio,
Da Costa Fernando B.
Publication year - 2008
Publication title -
phytotherapy research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.019
H-Index - 129
eISSN - 1099-1573
pISSN - 0951-418X
DOI - 10.1002/ptr.2512
Subject(s) - asteraceae , derivatization , diterpene , pharmacognosy , trypanosoma cruzi , stereochemistry , terpenoid , biology , in vitro , traditional medicine , biological activity , chemistry , botany , biochemistry , organic chemistry , high performance liquid chromatography , medicine , parasite hosting , world wide web , computer science
Five structurally related pimarane diterpenes isolated from the roots of Viguiera arenaria and a further compound obtained by chemical derivatization were evaluated in vitro against the trypomastigote forms of Trypanosoma cruzi . The natural compound ent ‐15‐pimarene‐8 β ,19‐diol and the derivative ent ‐8(14),15‐pimaradiene‐3 β ‐acetoxy showed the highest trypanocidal activity, displaying IC 50 values of 116.5 ± 1.21 and 149.3 ± 1.07 µM, respectively, while the positive control, violet gentian, showed an IC 50 of 76 µM. Based on the results, it can be concluded that minor structural differences among the tested diterpenes influence significantly the trypanocidal activity, thus bringing new perspectives to the establishment of structure‐activity relationships among this type of metabolites to the treatment of Chagas' disease. Copyright © 2008 John Wiley & Sons, Ltd.