Antikinetoplastid Activity of Sesquiterpenes Isolated from the Zoanthid <i>Palythoa aff. clavata</i>

Leishmaniasis and Chagas disease are neglected tropical diseases that cause problems in developing countries. The causative agents, <i>Leishmania</i> spp. and <i>Trypanosoma cruzi</i>, produce a clinical picture that can be fatal for the patient, such as Chagas heart disease,...

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Autores principales: Carlos J. Bethencourt-Estrella, Nathalia Nocchi, Atteneri López-Arencibia, Desirée San Nicolás-Hernández, María L. Souto, Blanca Suárez-Gómez, Ana R. Díaz-Marrero, José J. Fernández, Jacob Lorenzo-Morales, José E. Piñero
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spelling oai:doaj.org-article:1d4a2e353eff45508024a989a99682982021-11-25T18:39:17ZAntikinetoplastid Activity of Sesquiterpenes Isolated from the Zoanthid <i>Palythoa aff. clavata</i>10.3390/ph141110951424-8247https://doaj.org/article/1d4a2e353eff45508024a989a99682982021-10-01T00:00:00Zhttps://www.mdpi.com/1424-8247/14/11/1095https://doaj.org/toc/1424-8247Leishmaniasis and Chagas disease are neglected tropical diseases that cause problems in developing countries. The causative agents, <i>Leishmania</i> spp. and <i>Trypanosoma cruzi</i>, produce a clinical picture that can be fatal for the patient, such as Chagas heart disease, visceral leishmaniasis and megacolon, among others. Current treatments for these diseases are not very effective and highly toxic, since they require very prolonged treatments. The development of innovative, effective and safe drugs to fight infections caused by these parasites remains a challenge. For this reason, in recent years, there has been an increase in the search for new therapies. In this study, the antikinetoplastid activity of 13 sesquiterpene lactones obtained from <i>Palythoa aff. clavata</i> was screened against <i>L. amazonensis</i>, <i>L. donovani</i> and <i>T. cruzi</i>. The results revealed that the sesquiterpene lactones anhydroartemorin (<b>2</b>), <i>cis,trans</i>-costunolide-14-acetate (<b>3</b>) and 4-hydroxyarbusculin A (<b>11</b>) were the most selective against the kinetoplastid species studied. These molecules seem to induce the mechanisms involved in an apoptotic-like death or programmed cell death (PCD) in the kinetoplastids, and since they do not cause necrosis, the inflammatory events associated with this type of cell death will not be triggered.Carlos J. Bethencourt-EstrellaNathalia NocchiAtteneri López-ArencibiaDesirée San Nicolás-HernándezMaría L. SoutoBlanca Suárez-GómezAna R. Díaz-MarreroJosé J. FernándezJacob Lorenzo-MoralesJosé E. PiñeroMDPI AGarticlekinetoplastids<i>Trypanosoma</i><i>Leishmania</i>leishmanicidalChagastrypanocidalMedicineRPharmacy and materia medicaRS1-441ENPharmaceuticals, Vol 14, Iss 1095, p 1095 (2021)
institution DOAJ
collection DOAJ
language EN
topic kinetoplastids
<i>Trypanosoma</i>
<i>Leishmania</i>
leishmanicidal
Chagas
trypanocidal
Medicine
R
Pharmacy and materia medica
RS1-441
spellingShingle kinetoplastids
<i>Trypanosoma</i>
<i>Leishmania</i>
leishmanicidal
Chagas
trypanocidal
Medicine
R
Pharmacy and materia medica
RS1-441
Carlos J. Bethencourt-Estrella
Nathalia Nocchi
Atteneri López-Arencibia
Desirée San Nicolás-Hernández
María L. Souto
Blanca Suárez-Gómez
Ana R. Díaz-Marrero
José J. Fernández
Jacob Lorenzo-Morales
José E. Piñero
Antikinetoplastid Activity of Sesquiterpenes Isolated from the Zoanthid <i>Palythoa aff. clavata</i>
description Leishmaniasis and Chagas disease are neglected tropical diseases that cause problems in developing countries. The causative agents, <i>Leishmania</i> spp. and <i>Trypanosoma cruzi</i>, produce a clinical picture that can be fatal for the patient, such as Chagas heart disease, visceral leishmaniasis and megacolon, among others. Current treatments for these diseases are not very effective and highly toxic, since they require very prolonged treatments. The development of innovative, effective and safe drugs to fight infections caused by these parasites remains a challenge. For this reason, in recent years, there has been an increase in the search for new therapies. In this study, the antikinetoplastid activity of 13 sesquiterpene lactones obtained from <i>Palythoa aff. clavata</i> was screened against <i>L. amazonensis</i>, <i>L. donovani</i> and <i>T. cruzi</i>. The results revealed that the sesquiterpene lactones anhydroartemorin (<b>2</b>), <i>cis,trans</i>-costunolide-14-acetate (<b>3</b>) and 4-hydroxyarbusculin A (<b>11</b>) were the most selective against the kinetoplastid species studied. These molecules seem to induce the mechanisms involved in an apoptotic-like death or programmed cell death (PCD) in the kinetoplastids, and since they do not cause necrosis, the inflammatory events associated with this type of cell death will not be triggered.
format article
author Carlos J. Bethencourt-Estrella
Nathalia Nocchi
Atteneri López-Arencibia
Desirée San Nicolás-Hernández
María L. Souto
Blanca Suárez-Gómez
Ana R. Díaz-Marrero
José J. Fernández
Jacob Lorenzo-Morales
José E. Piñero
author_facet Carlos J. Bethencourt-Estrella
Nathalia Nocchi
Atteneri López-Arencibia
Desirée San Nicolás-Hernández
María L. Souto
Blanca Suárez-Gómez
Ana R. Díaz-Marrero
José J. Fernández
Jacob Lorenzo-Morales
José E. Piñero
author_sort Carlos J. Bethencourt-Estrella
title Antikinetoplastid Activity of Sesquiterpenes Isolated from the Zoanthid <i>Palythoa aff. clavata</i>
title_short Antikinetoplastid Activity of Sesquiterpenes Isolated from the Zoanthid <i>Palythoa aff. clavata</i>
title_full Antikinetoplastid Activity of Sesquiterpenes Isolated from the Zoanthid <i>Palythoa aff. clavata</i>
title_fullStr Antikinetoplastid Activity of Sesquiterpenes Isolated from the Zoanthid <i>Palythoa aff. clavata</i>
title_full_unstemmed Antikinetoplastid Activity of Sesquiterpenes Isolated from the Zoanthid <i>Palythoa aff. clavata</i>
title_sort antikinetoplastid activity of sesquiterpenes isolated from the zoanthid <i>palythoa aff. clavata</i>
publisher MDPI AG
publishDate 2021
url https://doaj.org/article/1d4a2e353eff45508024a989a9968298
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