TY - JOUR
T1 - Drimanes from Drimys brasiliensis with leishmanicidal and antimalarial activity
AU - Claudino, Vanessa Duarte
AU - da Silva, Kesia Caroline
AU - Filho, Valdir Cechinel
AU - Yunes, Rosendo Augusto
AU - Monache, Franco Delle
AU - Giménez, Alberto
AU - Salamanca, Efrain
AU - Gutierrez-Yapu, David
AU - Malheiros, Angela
PY - 2013/4
Y1 - 2013/4
N2 - This paper evaluates CHCl3 and CH3OH extracts of the stem bark, branches and leaves of Drimys brasiliensis and drimane sesquiterpenes isolated from the stem bark against strains of Leishmania amazonensis and Leishmania braziliensis promastigotes and Plasmodium falciparum trophozoites. All of the extracts and compounds were tested in cell lines in comparison with reference standards and cell viability was determined by the XTT method. The CHCl3 and CH3OH extracts from the stem bark and branches yielded promising results against two strains of Leishmania, with 50% inhibitory concentrations (IC50) values ranging from 39-100 μg/mL. The CHCl3 extract of the stem bark returned IC50 values of 39 and 40.6 μg/mL for L. amazonensis and L. braziliensis, respectively. The drimanes were relatively effective: 1-β-(p-coumaroyloxy)-polygodial produced IC50 values of 5.55 and 2.52 μM for L. amazonensis and L. braziliensis, respectively, compared with 1-β-(p-methoxycinnamoyl)-polygodial, which produced respective IC50 values of 15.85 and 17.80 μM. The CHCl3 extract demonstrated activity (IC50 of 3.0 μg/mL) against P. falciparum. The IC50 values of 1-β-(p-cumaroyloxyl)-polygodial and 1-β-(p-methoxycinnamoyl)-polygodial were 1.01 and 4.87 μM, respectively, for the trophozoite strain. Therefore, the results suggest that D. brasiliensis is a promising plant from which to obtain new and effective antiparasitic agents.
AB - This paper evaluates CHCl3 and CH3OH extracts of the stem bark, branches and leaves of Drimys brasiliensis and drimane sesquiterpenes isolated from the stem bark against strains of Leishmania amazonensis and Leishmania braziliensis promastigotes and Plasmodium falciparum trophozoites. All of the extracts and compounds were tested in cell lines in comparison with reference standards and cell viability was determined by the XTT method. The CHCl3 and CH3OH extracts from the stem bark and branches yielded promising results against two strains of Leishmania, with 50% inhibitory concentrations (IC50) values ranging from 39-100 μg/mL. The CHCl3 extract of the stem bark returned IC50 values of 39 and 40.6 μg/mL for L. amazonensis and L. braziliensis, respectively. The drimanes were relatively effective: 1-β-(p-coumaroyloxy)-polygodial produced IC50 values of 5.55 and 2.52 μM for L. amazonensis and L. braziliensis, respectively, compared with 1-β-(p-methoxycinnamoyl)-polygodial, which produced respective IC50 values of 15.85 and 17.80 μM. The CHCl3 extract demonstrated activity (IC50 of 3.0 μg/mL) against P. falciparum. The IC50 values of 1-β-(p-cumaroyloxyl)-polygodial and 1-β-(p-methoxycinnamoyl)-polygodial were 1.01 and 4.87 μM, respectively, for the trophozoite strain. Therefore, the results suggest that D. brasiliensis is a promising plant from which to obtain new and effective antiparasitic agents.
KW - Drimane sesquiterpenes
KW - Drimys
KW - Leishmaniasis
KW - Malaria
UR - http://www.scopus.com/inward/record.url?scp=84875445603&partnerID=8YFLogxK
U2 - 10.1590/0074-0276108022013002
DO - 10.1590/0074-0276108022013002
M3 - Artículo
AN - SCOPUS:84875445603
SN - 0074-0276
VL - 108
SP - 140
EP - 144
JO - Memorias do Instituto Oswaldo Cruz
JF - Memorias do Instituto Oswaldo Cruz
IS - 2
ER -