TY - JOUR
T1 - Trypanocidal activity of South American Vernonieae (Asteraceae) extracts and its sesquiterpene lactones
AU - Sosa, Andrea
AU - Salamanca Capusiri, Efraín
AU - Amaya, Susana
AU - Bardón, Alicia
AU - Giménez-Turba, Alberto
AU - Vera, Nancy
AU - Borkosky, Susana
N1 - Publisher Copyright:
© 2020 Informa UK Limited, trading as Taylor & Francis Group.
PY - 2021
Y1 - 2021
N2 - Chagas disease is caused by Trypanosoma cruzi and affects the poorest population in the Americas. Fourteen plant extracts and seventeen sesquiterpene lactones from the tribe Vernonieae (Asteraceae), were evaluated for the first time against T. cruzi. Cytotoxicity employing HeLa cells was also assessed. The best results were obtained with leaves and flowers rinse extracts from Vernonanthura nebularum (E-1 and E-3) and Elephantopus mollis (E-11 and E-13), with IC50 values <2 µg/mL, being E-1 the most active (IC50 = 0.8 µg/mL). Additionally, these extracts displayed a good selectivity (SI > 10). The most active sesquiterpene lactones, isolated from the extracts, were 2 (2-methoxy-2,5-epoxy-8-methacryloxygermacra-3Z,11(13)-dien-6,12-olide) and 6 (2-ethoxy-2,5-epoxy-8-angeloxygermacra-3Z,11(13)-dien-6,12-olide) from V. nebularum and 12 (8α-methacryloxyhirsutinolide 13-O-acetate) from V. pinguis, with IC50 of 1.5, 2.1 and 2.0 µM, respectively. These compounds showed SI values >14, better than those of the reference drug nifurtimox. Plants living in South American ecosystems could become a potential source of trypanocidal agents.
AB - Chagas disease is caused by Trypanosoma cruzi and affects the poorest population in the Americas. Fourteen plant extracts and seventeen sesquiterpene lactones from the tribe Vernonieae (Asteraceae), were evaluated for the first time against T. cruzi. Cytotoxicity employing HeLa cells was also assessed. The best results were obtained with leaves and flowers rinse extracts from Vernonanthura nebularum (E-1 and E-3) and Elephantopus mollis (E-11 and E-13), with IC50 values <2 µg/mL, being E-1 the most active (IC50 = 0.8 µg/mL). Additionally, these extracts displayed a good selectivity (SI > 10). The most active sesquiterpene lactones, isolated from the extracts, were 2 (2-methoxy-2,5-epoxy-8-methacryloxygermacra-3Z,11(13)-dien-6,12-olide) and 6 (2-ethoxy-2,5-epoxy-8-angeloxygermacra-3Z,11(13)-dien-6,12-olide) from V. nebularum and 12 (8α-methacryloxyhirsutinolide 13-O-acetate) from V. pinguis, with IC50 of 1.5, 2.1 and 2.0 µM, respectively. These compounds showed SI values >14, better than those of the reference drug nifurtimox. Plants living in South American ecosystems could become a potential source of trypanocidal agents.
KW - Asteraceae
KW - Hela cells
KW - Trypanosoma cruzi
KW - Vernonieae
KW - antiparasitic
KW - sesquiterpene lactones
UR - http://www.scopus.com/inward/record.url?scp=85082316565&partnerID=8YFLogxK
U2 - 10.1080/14786419.2020.1739682
DO - 10.1080/14786419.2020.1739682
M3 - Artículo
C2 - 32182147
AN - SCOPUS:85082316565
SN - 1478-6419
VL - 35
SP - 5224
EP - 5228
JO - Natural Product Research
JF - Natural Product Research
IS - 23
ER -