Natural terpenoids from Ambrosia species are active in vitro and in vivo against human pathogenic trypanosomatids.

Among the natural compounds, terpenoids play an important role in the drug discovery process for tropical diseases. The aim of the present work was to isolate antiprotozoal compounds from Ambrosia elatior and A. scabra. The sesquiterpene lactone (STL) cumanin was isolated from A. elatior whereas two...

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Autores principales:	Valeria P Sülsen, Silvia I Cazorla, Fernanda M Frank, Laura C Laurella, Liliana V Muschietti, Cesar A Catalán, Virginia S Martino, Emilio L Malchiodi
Formato:	article
Lenguaje:	EN
Publicado:	Public Library of Science (PLoS) 2013
Materias:	Arctic medicine. Tropical medicine RC955-962 Public aspects of medicine RA1-1270
Acceso en línea:	https://doaj.org/article/1d4f04a4357741ff877eb22e148a1885
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spelling	oai:doaj.org-article:1d4f04a4357741ff877eb22e148a18852021-11-18T09:16:47ZNatural terpenoids from Ambrosia species are active in vitro and in vivo against human pathogenic trypanosomatids.1935-27271935-273510.1371/journal.pntd.0002494https://doaj.org/article/1d4f04a4357741ff877eb22e148a18852013-01-01T00:00:00Zhttps://www.ncbi.nlm.nih.gov/pmc/articles/pmid/24130916/?tool=EBIhttps://doaj.org/toc/1935-2727https://doaj.org/toc/1935-2735Among the natural compounds, terpenoids play an important role in the drug discovery process for tropical diseases. The aim of the present work was to isolate antiprotozoal compounds from Ambrosia elatior and A. scabra. The sesquiterpene lactone (STL) cumanin was isolated from A. elatior whereas two other STLs, psilostachyin and cordilin, and one sterol glycoside, daucosterol, were isolated from A. scabra. Cumanin and cordilin were active against Trypanosoma cruzi epimastigotes showing 50% inhibition concentrations (IC50) values of 12 µM and 26 µM, respectively. Moreover, these compounds are active against bloodstream trypomastigotes, regardless of the T. cruzi strain tested. Psilostachyin and cumanin were also active against amastigote forms with IC50 values of 21 µM and 8 µM, respectively. By contrast, daucosterol showed moderate activity on epimastigotes and trypomastigotes and was inactive against amastigote forms. We also found that cumanin and psilostachyin exhibited an additive effect in their trypanocidal activity when these two drugs were tested together. Cumanin has leishmanicidal activity with growth inhibition values greater than 80% at a concentration of 5 µg/ml (19 µM), against both L. braziliensis and L. amazonensis promastigotes. In an in vivo model of T. cruzi infection, cumanin was more active than benznidazole, producing an 8-fold reduction in parasitemia levels during the acute phase of the infection compared with the control group, and more importantly, a reduction in mortality with 66% of the animals surviving, in comparison with 100% mortality in the control group. Cumanin also showed nontoxic effects at the doses assayed in vivo, as determined using markers of hepatic damage.Valeria P SülsenSilvia I CazorlaFernanda M FrankLaura C LaurellaLiliana V MuschiettiCesar A CatalánVirginia S MartinoEmilio L MalchiodiPublic Library of Science (PLoS)articleArctic medicine. Tropical medicineRC955-962Public aspects of medicineRA1-1270ENPLoS Neglected Tropical Diseases, Vol 7, Iss 10, p e2494 (2013)
institution	DOAJ
collection	DOAJ
language	EN
topic	Arctic medicine. Tropical medicine RC955-962 Public aspects of medicine RA1-1270
spellingShingle	Arctic medicine. Tropical medicine RC955-962 Public aspects of medicine RA1-1270 Valeria P Sülsen Silvia I Cazorla Fernanda M Frank Laura C Laurella Liliana V Muschietti Cesar A Catalán Virginia S Martino Emilio L Malchiodi Natural terpenoids from Ambrosia species are active in vitro and in vivo against human pathogenic trypanosomatids.
description	Among the natural compounds, terpenoids play an important role in the drug discovery process for tropical diseases. The aim of the present work was to isolate antiprotozoal compounds from Ambrosia elatior and A. scabra. The sesquiterpene lactone (STL) cumanin was isolated from A. elatior whereas two other STLs, psilostachyin and cordilin, and one sterol glycoside, daucosterol, were isolated from A. scabra. Cumanin and cordilin were active against Trypanosoma cruzi epimastigotes showing 50% inhibition concentrations (IC50) values of 12 µM and 26 µM, respectively. Moreover, these compounds are active against bloodstream trypomastigotes, regardless of the T. cruzi strain tested. Psilostachyin and cumanin were also active against amastigote forms with IC50 values of 21 µM and 8 µM, respectively. By contrast, daucosterol showed moderate activity on epimastigotes and trypomastigotes and was inactive against amastigote forms. We also found that cumanin and psilostachyin exhibited an additive effect in their trypanocidal activity when these two drugs were tested together. Cumanin has leishmanicidal activity with growth inhibition values greater than 80% at a concentration of 5 µg/ml (19 µM), against both L. braziliensis and L. amazonensis promastigotes. In an in vivo model of T. cruzi infection, cumanin was more active than benznidazole, producing an 8-fold reduction in parasitemia levels during the acute phase of the infection compared with the control group, and more importantly, a reduction in mortality with 66% of the animals surviving, in comparison with 100% mortality in the control group. Cumanin also showed nontoxic effects at the doses assayed in vivo, as determined using markers of hepatic damage.
format	article
author	Valeria P Sülsen Silvia I Cazorla Fernanda M Frank Laura C Laurella Liliana V Muschietti Cesar A Catalán Virginia S Martino Emilio L Malchiodi
author_facet	Valeria P Sülsen Silvia I Cazorla Fernanda M Frank Laura C Laurella Liliana V Muschietti Cesar A Catalán Virginia S Martino Emilio L Malchiodi
author_sort	Valeria P Sülsen
title	Natural terpenoids from Ambrosia species are active in vitro and in vivo against human pathogenic trypanosomatids.
title_short	Natural terpenoids from Ambrosia species are active in vitro and in vivo against human pathogenic trypanosomatids.
title_full	Natural terpenoids from Ambrosia species are active in vitro and in vivo against human pathogenic trypanosomatids.
title_fullStr	Natural terpenoids from Ambrosia species are active in vitro and in vivo against human pathogenic trypanosomatids.
title_full_unstemmed	Natural terpenoids from Ambrosia species are active in vitro and in vivo against human pathogenic trypanosomatids.
title_sort	natural terpenoids from ambrosia species are active in vitro and in vivo against human pathogenic trypanosomatids.
publisher	Public Library of Science (PLoS)
publishDate	2013
url	https://doaj.org/article/1d4f04a4357741ff877eb22e148a1885
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Natural terpenoids from Ambrosia species are active in vitro and in vivo against human pathogenic trypanosomatids.

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