In Vitro Anti-<i>Trypanosoma cruzi</i> Activity of Halophytes from Southern Portugal Reloaded: A Special Focus on Sea Fennel (<i>Crithmum maritimum</i> L.)

Marine halophytes are an outstanding reservoir of natural products and several species have anti-infectious traditional uses. However, reports about their potential use against neglected tropical ailments, such as Chagas disease, are scarce. This work evaluated for the first time the in vitro anti-&...

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Autores principales:	Catarina G. Pereira, Carolina Borsoi Moraes, Caio H. Franco, Clarissa Feltrin, Raphaël Grougnet, Euzébio Guimarães Barbosa, Michele Panciera, Carlos Roque D. Correia, Maria João Rodrigues, Luísa Custódio
Formato:	article
Lenguaje:	EN
Publicado:	MDPI AG 2021
Materias:	Marine halophytes Chagas disease <i>Trypanosoma cruzi</i> neglected tropical diseases <i>Crithmum maritimum</i> falcarindiol Botany QK1-989
Acceso en línea:	https://doaj.org/article/2a6d57c8fffe49b39b1b3c0696afffa5
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spelling	oai:doaj.org-article:2a6d57c8fffe49b39b1b3c0696afffa52021-11-25T18:44:02ZIn Vitro Anti-<i>Trypanosoma cruzi</i> Activity of Halophytes from Southern Portugal Reloaded: A Special Focus on Sea Fennel (<i>Crithmum maritimum</i> L.)10.3390/plants101122352223-7747https://doaj.org/article/2a6d57c8fffe49b39b1b3c0696afffa52021-10-01T00:00:00Zhttps://www.mdpi.com/2223-7747/10/11/2235https://doaj.org/toc/2223-7747Marine halophytes are an outstanding reservoir of natural products and several species have anti-infectious traditional uses. However, reports about their potential use against neglected tropical ailments, such as Chagas disease, are scarce. This work evaluated for the first time the in vitro anti-<i>Trypanosoma cruzi</i> activity of extracts from the aromatic and medicinal species <i>Helichrysum italicum</i> subsp. <i>picardii</i> (Boiss. & Reut.) Franco (Asteraceae, everlasting) and <i>Crithmum maritimum</i> L. (Apiaceae, sea fennel). For that purpose, decoctions, tinctures, and essential oils from everlasting’s flowers and sea fennel’s stems, leaves, and flowers were tested against intracellular amastigotes of two <i>T. cruzi</i> strains. The extract from the sea fennel flower decoction displayed significant anti-trypanosomal activity and no toxicity towards the host cell (EC<sub>50</sub> = 17.7 µg/mL, selectivity index > 5.65). Subsequent fractionation of this extract afforded 5 fractions that were re-tested in the same model of anti-parasitic activity. Fraction <b>1</b> was the most active and selective (EC<sub>50</sub> = 0.47 μg/mL, selectivity index = 59.6) and was submitted to preparative thin-layer chromatography. One major compound was identified, falcarindiol, which was likely the one responsible for the observed anti-trypanosomal activity. This was confirmed using a commercially sourced molecule. Target-fishing studies showed falcarindiol as a ligand of <i>T. cruzi</i> spermidine synthase, pointing to a potential enzyme-inhibiting anti-trypanosomal mechanism of action. Overall, this work shows that sea fennel can provide effective anti-parasitic molecule(s) with potential pharmacological applications in the treatment of CD.Catarina G. PereiraCarolina Borsoi MoraesCaio H. FrancoClarissa FeltrinRaphaël GrougnetEuzébio Guimarães BarbosaMichele PancieraCarlos Roque D. CorreiaMaria João RodriguesLuísa CustódioMDPI AGarticleMarine halophytesChagas disease<i>Trypanosoma cruzi</i>neglected tropical diseases<i>Crithmum maritimum</i>falcarindiolBotanyQK1-989ENPlants, Vol 10, Iss 2235, p 2235 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	Marine halophytes Chagas disease <i>Trypanosoma cruzi</i> neglected tropical diseases <i>Crithmum maritimum</i> falcarindiol Botany QK1-989
spellingShingle	Marine halophytes Chagas disease <i>Trypanosoma cruzi</i> neglected tropical diseases <i>Crithmum maritimum</i> falcarindiol Botany QK1-989 Catarina G. Pereira Carolina Borsoi Moraes Caio H. Franco Clarissa Feltrin Raphaël Grougnet Euzébio Guimarães Barbosa Michele Panciera Carlos Roque D. Correia Maria João Rodrigues Luísa Custódio In Vitro Anti-<i>Trypanosoma cruzi</i> Activity of Halophytes from Southern Portugal Reloaded: A Special Focus on Sea Fennel (<i>Crithmum maritimum</i> L.)
description	Marine halophytes are an outstanding reservoir of natural products and several species have anti-infectious traditional uses. However, reports about their potential use against neglected tropical ailments, such as Chagas disease, are scarce. This work evaluated for the first time the in vitro anti-<i>Trypanosoma cruzi</i> activity of extracts from the aromatic and medicinal species <i>Helichrysum italicum</i> subsp. <i>picardii</i> (Boiss. & Reut.) Franco (Asteraceae, everlasting) and <i>Crithmum maritimum</i> L. (Apiaceae, sea fennel). For that purpose, decoctions, tinctures, and essential oils from everlasting’s flowers and sea fennel’s stems, leaves, and flowers were tested against intracellular amastigotes of two <i>T. cruzi</i> strains. The extract from the sea fennel flower decoction displayed significant anti-trypanosomal activity and no toxicity towards the host cell (EC<sub>50</sub> = 17.7 µg/mL, selectivity index > 5.65). Subsequent fractionation of this extract afforded 5 fractions that were re-tested in the same model of anti-parasitic activity. Fraction <b>1</b> was the most active and selective (EC<sub>50</sub> = 0.47 μg/mL, selectivity index = 59.6) and was submitted to preparative thin-layer chromatography. One major compound was identified, falcarindiol, which was likely the one responsible for the observed anti-trypanosomal activity. This was confirmed using a commercially sourced molecule. Target-fishing studies showed falcarindiol as a ligand of <i>T. cruzi</i> spermidine synthase, pointing to a potential enzyme-inhibiting anti-trypanosomal mechanism of action. Overall, this work shows that sea fennel can provide effective anti-parasitic molecule(s) with potential pharmacological applications in the treatment of CD.
format	article
author	Catarina G. Pereira Carolina Borsoi Moraes Caio H. Franco Clarissa Feltrin Raphaël Grougnet Euzébio Guimarães Barbosa Michele Panciera Carlos Roque D. Correia Maria João Rodrigues Luísa Custódio
author_facet	Catarina G. Pereira Carolina Borsoi Moraes Caio H. Franco Clarissa Feltrin Raphaël Grougnet Euzébio Guimarães Barbosa Michele Panciera Carlos Roque D. Correia Maria João Rodrigues Luísa Custódio
author_sort	Catarina G. Pereira
title	In Vitro Anti-<i>Trypanosoma cruzi</i> Activity of Halophytes from Southern Portugal Reloaded: A Special Focus on Sea Fennel (<i>Crithmum maritimum</i> L.)
title_short	In Vitro Anti-<i>Trypanosoma cruzi</i> Activity of Halophytes from Southern Portugal Reloaded: A Special Focus on Sea Fennel (<i>Crithmum maritimum</i> L.)
title_full	In Vitro Anti-<i>Trypanosoma cruzi</i> Activity of Halophytes from Southern Portugal Reloaded: A Special Focus on Sea Fennel (<i>Crithmum maritimum</i> L.)
title_fullStr	In Vitro Anti-<i>Trypanosoma cruzi</i> Activity of Halophytes from Southern Portugal Reloaded: A Special Focus on Sea Fennel (<i>Crithmum maritimum</i> L.)
title_full_unstemmed	In Vitro Anti-<i>Trypanosoma cruzi</i> Activity of Halophytes from Southern Portugal Reloaded: A Special Focus on Sea Fennel (<i>Crithmum maritimum</i> L.)
title_sort	in vitro anti-<i>trypanosoma cruzi</i> activity of halophytes from southern portugal reloaded: a special focus on sea fennel (<i>crithmum maritimum</i> l.)
publisher	MDPI AG
publishDate	2021
url	https://doaj.org/article/2a6d57c8fffe49b39b1b3c0696afffa5
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In Vitro Anti-<i>Trypanosoma cruzi</i> Activity of Halophytes from Southern Portugal Reloaded: A Special Focus on Sea Fennel (<i>Crithmum maritimum</i> L.)

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