5-Nitroindazole derivatives as potential therapeutic alternatives against Acanthamoeba castellanii

Amoebas of the genus Acanthamoeba are distributed worldwide, including species with a high pathogenic ca- pacity for humans. In a similar way to what occurs with other parasitic protozoa, the available treatments show variable effectiveness in addition to high toxicity, which demands the development...

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Autores: Martín-Escolano, Rubén, Pérez-Cordón, Gregorio, Arán, Vicente J., Marín, Clotilde, Sánchez-Moreno, Manuel, Rosales, María José
Tipo de recurso: artículo
Estado:Versión publicada
Fecha de publicación:2022
País:España
Institución:Consejo Superior de Investigaciones Científicas (CSIC)
Repositorio:DIGITAL.CSIC. Repositorio Institucional del CSIC
OAI Identifier:oai:digital.csic.es:10261/271678
Acceso en línea:http://hdl.handle.net/10261/271678
Access Level:acceso abierto
Palabra clave:Acanthamoeba castellanii
Amoebicidal
Chlorhexidine digluconate
5-nitroindazole derivatives
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spelling 5-Nitroindazole derivatives as potential therapeutic alternatives against Acanthamoeba castellaniiMartín-Escolano, RubénPérez-Cordón, GregorioArán, Vicente J.Marín, ClotildeSánchez-Moreno, ManuelRosales, María JoséAcanthamoeba castellaniiAmoebicidalChlorhexidine digluconate5-nitroindazole derivativesAmoebas of the genus Acanthamoeba are distributed worldwide, including species with a high pathogenic ca- pacity for humans. In a similar way to what occurs with other parasitic protozoa, the available treatments show variable effectiveness in addition to high toxicity, which demands the development of new treatments. Positive results of 5-nitroindazole derivatives against several protozoa parasites suggest that these compounds may be a promising tool for the development of efficient antiparasitic drugs. In the present work we have evaluated the in vitro activity of ten 5-nitroindazole derivatives against Acanthamoeba castellanii trophozoites and cysts. To that end, AlamarBlue Assay Reagent® was used to determine the activity against trophozoites compared to the reference drug chlorhexidine digluconate. Cytotoxicity of the compounds was evaluated using Vero cells. The activity on cysts was evaluated by light microscopy and using a Neubauer chamber to quantifying cysts and presence of trophozoites, as an indication of cyst. Our results showed the effectiveness of the 5-nitroindazole derivatives tested against both trophozoites and cysts of A. castellani highlighting 5-nitroindazole derivative 8 which showed a 80% activity on cysts, which is higher than that of the reference drug. Moreover, 5-nitroindazole derivatives 8, 9 and 10 were more effective on trophozoites than the reference drug showing IC50 values lower than 5 μM. Taking together these results, these 5-nitroindazole derivatives specially compound 8, might be a promising alternative for the development of more efficient treatments against A. castellani infection.This work was supported by the Spanish MINECO, FEDER funds of the E. U. [CTQ2013–14892 and 2010-CSD2010–00065]; the Unidad de Excelencia MDM [2015–0038]; and the Generalitat Valenciana (PROMETEO II 2015–002). R.M.-E. is grateful for the fellowship from the Alfonso Martín Escudero FoundatioPeer reviewedElsevierMinisterio de Economía, Industria y Competitividad (España)European CommissionGeneralitat ValencianaConsejo Superior de Investigaciones Científicas [https://ror.org/02gfc7t72]202220222022info:eu-repo/semantics/articlehttp://purl.org/coar/resource_type/c_6501Publisher's versioninfo:eu-repo/semantics/publishedVersionhttp://hdl.handle.net/10261/271678reponame:DIGITAL.CSIC. Repositorio Institucional del CSICinstname:Consejo Superior de Investigaciones Científicas (CSIC)Ingléshttps://doi.org/10.1016/j.actatropica.2022.106538Síinfo:eu-repo/semantics/openAccessoai:digital.csic.es:10261/2716782026-05-22T06:33:51Z
dc.title.none.fl_str_mv 5-Nitroindazole derivatives as potential therapeutic alternatives against Acanthamoeba castellanii
title 5-Nitroindazole derivatives as potential therapeutic alternatives against Acanthamoeba castellanii
spellingShingle 5-Nitroindazole derivatives as potential therapeutic alternatives against Acanthamoeba castellanii
Martín-Escolano, Rubén
Acanthamoeba castellanii
Amoebicidal
Chlorhexidine digluconate
5-nitroindazole derivatives
title_short 5-Nitroindazole derivatives as potential therapeutic alternatives against Acanthamoeba castellanii
title_full 5-Nitroindazole derivatives as potential therapeutic alternatives against Acanthamoeba castellanii
title_fullStr 5-Nitroindazole derivatives as potential therapeutic alternatives against Acanthamoeba castellanii
title_full_unstemmed 5-Nitroindazole derivatives as potential therapeutic alternatives against Acanthamoeba castellanii
title_sort 5-Nitroindazole derivatives as potential therapeutic alternatives against Acanthamoeba castellanii
dc.creator.none.fl_str_mv Martín-Escolano, Rubén
Pérez-Cordón, Gregorio
Arán, Vicente J.
Marín, Clotilde
Sánchez-Moreno, Manuel
Rosales, María José
author Martín-Escolano, Rubén
author_facet Martín-Escolano, Rubén
Pérez-Cordón, Gregorio
Arán, Vicente J.
Marín, Clotilde
Sánchez-Moreno, Manuel
Rosales, María José
author_role author
author2 Pérez-Cordón, Gregorio
Arán, Vicente J.
Marín, Clotilde
Sánchez-Moreno, Manuel
Rosales, María José
author2_role author
author
author
author
author
dc.contributor.none.fl_str_mv Ministerio de Economía, Industria y Competitividad (España)
European Commission
Generalitat Valenciana
Consejo Superior de Investigaciones Científicas [https://ror.org/02gfc7t72]
dc.subject.none.fl_str_mv Acanthamoeba castellanii
Amoebicidal
Chlorhexidine digluconate
5-nitroindazole derivatives
topic Acanthamoeba castellanii
Amoebicidal
Chlorhexidine digluconate
5-nitroindazole derivatives
description Amoebas of the genus Acanthamoeba are distributed worldwide, including species with a high pathogenic ca- pacity for humans. In a similar way to what occurs with other parasitic protozoa, the available treatments show variable effectiveness in addition to high toxicity, which demands the development of new treatments. Positive results of 5-nitroindazole derivatives against several protozoa parasites suggest that these compounds may be a promising tool for the development of efficient antiparasitic drugs. In the present work we have evaluated the in vitro activity of ten 5-nitroindazole derivatives against Acanthamoeba castellanii trophozoites and cysts. To that end, AlamarBlue Assay Reagent® was used to determine the activity against trophozoites compared to the reference drug chlorhexidine digluconate. Cytotoxicity of the compounds was evaluated using Vero cells. The activity on cysts was evaluated by light microscopy and using a Neubauer chamber to quantifying cysts and presence of trophozoites, as an indication of cyst. Our results showed the effectiveness of the 5-nitroindazole derivatives tested against both trophozoites and cysts of A. castellani highlighting 5-nitroindazole derivative 8 which showed a 80% activity on cysts, which is higher than that of the reference drug. Moreover, 5-nitroindazole derivatives 8, 9 and 10 were more effective on trophozoites than the reference drug showing IC50 values lower than 5 μM. Taking together these results, these 5-nitroindazole derivatives specially compound 8, might be a promising alternative for the development of more efficient treatments against A. castellani infection.
publishDate 2022
dc.date.none.fl_str_mv 2022
2022
2022
dc.type.none.fl_str_mv info:eu-repo/semantics/article
http://purl.org/coar/resource_type/c_6501
Publisher's version
info:eu-repo/semantics/publishedVersion
format article
status_str publishedVersion
dc.identifier.none.fl_str_mv http://hdl.handle.net/10261/271678
url http://hdl.handle.net/10261/271678
dc.language.none.fl_str_mv Inglés
language_invalid_str_mv Inglés
dc.relation.none.fl_str_mv https://doi.org/10.1016/j.actatropica.2022.106538
Sí
dc.rights.none.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.publisher.none.fl_str_mv Elsevier
publisher.none.fl_str_mv Elsevier
dc.source.none.fl_str_mv reponame:DIGITAL.CSIC. Repositorio Institucional del CSIC
instname:Consejo Superior de Investigaciones Científicas (CSIC)
instname_str Consejo Superior de Investigaciones Científicas (CSIC)
reponame_str DIGITAL.CSIC. Repositorio Institucional del CSIC
collection DIGITAL.CSIC. Repositorio Institucional del CSIC
repository.name.fl_str_mv
repository.mail.fl_str_mv
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