Trypanocidal activity of South American Vernonieae (Asteraceae) extracts and its sesquiterpene lactones

Andrea Sosa; Efraín Salamanca Capusiri; Susana Amaya; Alicia Bardón; Alberto Giménez-Turba; Nancy Vera; Susana Borkosky

doi:10.1080/14786419.2020.1739682

Trypanocidal activity of South American Vernonieae (Asteraceae) extracts and its sesquiterpene lactones

Andrea Sosa, Efraín Salamanca Capusiri, Susana Amaya, Alicia Bardón, Alberto Giménez-Turba, Nancy Vera, Susana Borkosky

Research output: Contribution to journal › Article › peer-review

4 Scopus citations

Abstract

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.

Original language	English
Pages (from-to)	5224-5228
Number of pages	5
Journal	Natural Product Research
Volume	35
Issue number	23
DOIs	https://doi.org/10.1080/14786419.2020.1739682
State	Published - 2021

Bibliographical note

Funding Information:
This work was supported by CONICET [Grant PIP-533] and SCAIT, UNT [Grant PIUNT D 552-2]. The authors would like to thank Biochemists C. Palma and C. Condo Montero (IIFB-UMSA) for their help with biological assays and LISA (UNT-CONICET) for the spectroscopic determinations.

Publisher Copyright:
© 2020 Informa UK Limited, trading as Taylor & Francis Group.

Keywords

Asteraceae
Hela cells
Trypanosoma cruzi
Vernonieae
antiparasitic
sesquiterpene lactones

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10.1080/14786419.2020.1739682

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title = "Trypanocidal activity of South American Vernonieae (Asteraceae) extracts and its sesquiterpene lactones",

abstract = "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.",

keywords = "Asteraceae, Hela cells, Trypanosoma cruzi, Vernonieae, antiparasitic, sesquiterpene lactones",

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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

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

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DO - 10.1080/14786419.2020.1739682

M3 - Artículo

C2 - 32182147

AN - SCOPUS:85082316565

VL - 35

SP - 5224

EP - 5228

JO - Natural Product Research

JF - Natural Product Research

SN - 1478-6419

IS - 23

ER -

Trypanocidal activity of South American Vernonieae (Asteraceae) extracts and its sesquiterpene lactones

Abstract

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Keywords

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