Ursolic Acid Derivatives as Potential Agents Against Acanthamoeba Spp.

The current chemotherapy of Acanthamoeba keratitis relies on few drugs with low potential and limited e cacy, for all this there is an urgent need to identify new classes of anti-Acanthamoeba agents. In this regard, natural products play an important role in overcoming the current need and medicinal...

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Autores: Sifaoui, Ines, Rodríguez Expósito, Rubén L., Reyes Batlle, María, Rizo Liendo, Aitor, Piñero Barroso, José Enrique, López Bazzocchi, Isabel, Lorenzo Morales, Jacob, Jiménez Díaz, Ignacio Antonio
Tipo de documento: artigo
Estado:Versão publicada
Data de publicação:2019
País:España
Recursos:Universidad de La Laguna (ULL)
Repositório:RIULL. Repositorio Institucional de la Universidad de La Laguna
OAI Identifier:oai:riull.ull.es:915/36071
Acesso em linha:http://riull.ull.es/xmlui/handle/915/36071
Access Level:Acceso aberto
Palavra-chave:ursolic acid derivatives
Acanthamoeba
chemotherapy
programmed cell death
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spelling Ursolic Acid Derivatives as Potential Agents Against Acanthamoeba Spp.Sifaoui, InesRodríguez Expósito, Rubén L.Reyes Batlle, MaríaRizo Liendo, AitorPiñero Barroso, José EnriqueLópez Bazzocchi, IsabelLorenzo Morales, JacobJiménez Díaz, Ignacio Antonioursolic acid derivativesAcanthamoebachemotherapyprogrammed cell deathThe current chemotherapy of Acanthamoeba keratitis relies on few drugs with low potential and limited e cacy, for all this there is an urgent need to identify new classes of anti-Acanthamoeba agents. In this regard, natural products play an important role in overcoming the current need and medicinal chemistry of natural products represents an attractive approach for the discovery and development of new agents. Ursolic acid, a natural pentacyclic triterpenoid compound, possesses a broad spectrum of activities including anti-Acanthamoeba. Herein, we report on the development by chemical transformation of an ursolic acid-based series of seven compounds (2–8), one of them reported for the first time. The structure-activity relationship (SAR) analysis of their anti-Acanthamoeba activity revealed that acylation/ether formation or oxidation enhances their biological profile, suggesting that the hydrophobic moiety contributes to activity, presumably by increasing the a nity and/or cell membrane permeability. These ursolic acid derivatives highlight the potential of this source as a good base for the development of novel therapeutic agents against Acanthamoeba infections.202420242019info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionhttp://riull.ull.es/xmlui/handle/915/36071reponame:RIULL. Repositorio Institucional de la Universidad de La Lagunainstname:Universidad de La Laguna (ULL)InglésPathogens 2019, 8, 130;Attribution-NonCommercial-NoDerivatives 4.0 Internacionalhttp://creativecommons.org/licenses/by-nc-nd/4.0/info:eu-repo/semantics/openAccessoai:riull.ull.es:915/360712026-06-22T13:13:57Z
dc.title.none.fl_str_mv Ursolic Acid Derivatives as Potential Agents Against Acanthamoeba Spp.
title Ursolic Acid Derivatives as Potential Agents Against Acanthamoeba Spp.
spellingShingle Ursolic Acid Derivatives as Potential Agents Against Acanthamoeba Spp.
Sifaoui, Ines
ursolic acid derivatives
Acanthamoeba
chemotherapy
programmed cell death
title_short Ursolic Acid Derivatives as Potential Agents Against Acanthamoeba Spp.
title_full Ursolic Acid Derivatives as Potential Agents Against Acanthamoeba Spp.
title_fullStr Ursolic Acid Derivatives as Potential Agents Against Acanthamoeba Spp.
title_full_unstemmed Ursolic Acid Derivatives as Potential Agents Against Acanthamoeba Spp.
title_sort Ursolic Acid Derivatives as Potential Agents Against Acanthamoeba Spp.
dc.creator.none.fl_str_mv Sifaoui, Ines
Rodríguez Expósito, Rubén L.
Reyes Batlle, María
Rizo Liendo, Aitor
Piñero Barroso, José Enrique
López Bazzocchi, Isabel
Lorenzo Morales, Jacob
Jiménez Díaz, Ignacio Antonio
author Sifaoui, Ines
author_facet Sifaoui, Ines
Rodríguez Expósito, Rubén L.
Reyes Batlle, María
Rizo Liendo, Aitor
Piñero Barroso, José Enrique
López Bazzocchi, Isabel
Lorenzo Morales, Jacob
Jiménez Díaz, Ignacio Antonio
author_role author
author2 Rodríguez Expósito, Rubén L.
Reyes Batlle, María
Rizo Liendo, Aitor
Piñero Barroso, José Enrique
López Bazzocchi, Isabel
Lorenzo Morales, Jacob
Jiménez Díaz, Ignacio Antonio
author2_role author
author
author
author
author
author
author
dc.subject.none.fl_str_mv ursolic acid derivatives
Acanthamoeba
chemotherapy
programmed cell death
topic ursolic acid derivatives
Acanthamoeba
chemotherapy
programmed cell death
description The current chemotherapy of Acanthamoeba keratitis relies on few drugs with low potential and limited e cacy, for all this there is an urgent need to identify new classes of anti-Acanthamoeba agents. In this regard, natural products play an important role in overcoming the current need and medicinal chemistry of natural products represents an attractive approach for the discovery and development of new agents. Ursolic acid, a natural pentacyclic triterpenoid compound, possesses a broad spectrum of activities including anti-Acanthamoeba. Herein, we report on the development by chemical transformation of an ursolic acid-based series of seven compounds (2–8), one of them reported for the first time. The structure-activity relationship (SAR) analysis of their anti-Acanthamoeba activity revealed that acylation/ether formation or oxidation enhances their biological profile, suggesting that the hydrophobic moiety contributes to activity, presumably by increasing the a nity and/or cell membrane permeability. These ursolic acid derivatives highlight the potential of this source as a good base for the development of novel therapeutic agents against Acanthamoeba infections.
publishDate 2019
dc.date.none.fl_str_mv 2019
2024
2024
dc.type.none.fl_str_mv info:eu-repo/semantics/article
info:eu-repo/semantics/publishedVersion
format article
status_str publishedVersion
dc.identifier.none.fl_str_mv http://riull.ull.es/xmlui/handle/915/36071
url http://riull.ull.es/xmlui/handle/915/36071
dc.language.none.fl_str_mv Inglés
language_invalid_str_mv Inglés
dc.relation.none.fl_str_mv Pathogens 2019, 8, 130;
dc.rights.none.fl_str_mv Attribution-NonCommercial-NoDerivatives 4.0 Internacional
http://creativecommons.org/licenses/by-nc-nd/4.0/
info:eu-repo/semantics/openAccess
rights_invalid_str_mv Attribution-NonCommercial-NoDerivatives 4.0 Internacional
http://creativecommons.org/licenses/by-nc-nd/4.0/
eu_rights_str_mv openAccess
dc.source.none.fl_str_mv reponame:RIULL. Repositorio Institucional de la Universidad de La Laguna
instname:Universidad de La Laguna (ULL)
instname_str Universidad de La Laguna (ULL)
reponame_str RIULL. Repositorio Institucional de la Universidad de La Laguna
collection RIULL. Repositorio Institucional de la Universidad de La Laguna
repository.name.fl_str_mv
repository.mail.fl_str_mv
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score 15,812429

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