Edelfosine (ET-18-OCH3) a Promising Alkylphospholipid against Resistant Trichomonas vaginalis

Edelfosine (ET-18-OCH3) is an alkylphospholipid with an analogous structure to miltefosine. Both molecules are active against kinetoplastids (Leishmania spp., Trypanosoma cruzi and Trypanosoma brucei). However, its trichomonacidal effect has never been studied. For this purpose, edelfosine has been...

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Autores: Ibáñez Escribano, Alexandra, Escario García-Trevijano, José Antonio, Mollinedo García, Faustino, Gómez Barrio, Alicia
Tipo de recurso: artículo
Fecha de publicación:2017
País:España
Institución:Universidad Complutense de Madrid (UCM)
Repositorio:Docta Complutense
Idioma:inglés
OAI Identifier:oai:docta.ucm.es:20.500.14352/19276
Acceso en línea:https://hdl.handle.net/20.500.14352/19276
Access Level:acceso abierto
Palabra clave:579
Microbiología (Farmacia)
3302.03 Microbiología Industrial
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spelling Edelfosine (ET-18-OCH3) a Promising Alkylphospholipid against Resistant Trichomonas vaginalisIbáñez Escribano, AlexandraEscario García-Trevijano, José AntonioMollinedo García, FaustinoGómez Barrio, Alicia579Microbiología (Farmacia)3302.03 Microbiología IndustrialEdelfosine (ET-18-OCH3) is an alkylphospholipid with an analogous structure to miltefosine. Both molecules are active against kinetoplastids (Leishmania spp., Trypanosoma cruzi and Trypanosoma brucei). However, its trichomonacidal effect has never been studied. For this purpose, edelfosine has been evaluated in vitro for its ability to inhibit proliferation of the common sexually transmitted parasite Trichomonas vaginalis following a standardized fluorimetric procedure. The results show an IC50 = 19.8 µM against metronidazole-sensitive isolates and a remarkable IC50 = 7.6 µM against the metronidazole-resistant IR78. This enhanced effect against the resistant isolate suggests another possible mode of action in comparison with the reference drug. Moreover, T. vaginalis exhibits a different growth rate due to the metabolic modifications according to its resistant trait. These results are in consonance with the trichomonacidal effect observed by other authors using the analog miltefosine against resistant samples, provoking membrane alterations and apoptosis. It is estimated that 2.5–10% of clinical cases of trichomonosis are produced by resistant isolates. The absence of pharmacological alternatives to the unique two 5-nitroimidazole drugs approved by the FDA makes necessary the incorporation of novel trichomonacidal drugs with a different mode of action. Taken together, our results, in consonance with previous reports, suggest the promising use of these alkylphospholipids as an alternative trichomonacidal drug against resistant cases.MDPIUniversidad Complutense de Madrid20172017-10-1920172017-10-19journal articlehttp://purl.org/coar/resource_type/c_6501info:eu-repo/semantics/articleapplication/pdfhttps://hdl.handle.net/20.500.14352/19276reponame:Docta Complutenseinstname:Universidad Complutense de Madrid (UCM)Inglésengopen accesshttp://purl.org/coar/access_right/c_abf2Atribución 3.0 Españahttps://creativecommons.org/licenses/by/3.0/es/info:eu-repo/semantics/openAccessoai:docta.ucm.es:20.500.14352/192762026-06-02T12:44:21Z
dc.title.none.fl_str_mv Edelfosine (ET-18-OCH3) a Promising Alkylphospholipid against Resistant Trichomonas vaginalis
title Edelfosine (ET-18-OCH3) a Promising Alkylphospholipid against Resistant Trichomonas vaginalis
spellingShingle Edelfosine (ET-18-OCH3) a Promising Alkylphospholipid against Resistant Trichomonas vaginalis
Ibáñez Escribano, Alexandra
579
Microbiología (Farmacia)
3302.03 Microbiología Industrial
title_short Edelfosine (ET-18-OCH3) a Promising Alkylphospholipid against Resistant Trichomonas vaginalis
title_full Edelfosine (ET-18-OCH3) a Promising Alkylphospholipid against Resistant Trichomonas vaginalis
title_fullStr Edelfosine (ET-18-OCH3) a Promising Alkylphospholipid against Resistant Trichomonas vaginalis
title_full_unstemmed Edelfosine (ET-18-OCH3) a Promising Alkylphospholipid against Resistant Trichomonas vaginalis
title_sort Edelfosine (ET-18-OCH3) a Promising Alkylphospholipid against Resistant Trichomonas vaginalis
dc.creator.none.fl_str_mv Ibáñez Escribano, Alexandra
Escario García-Trevijano, José Antonio
Mollinedo García, Faustino
Gómez Barrio, Alicia
author Ibáñez Escribano, Alexandra
author_facet Ibáñez Escribano, Alexandra
Escario García-Trevijano, José Antonio
Mollinedo García, Faustino
Gómez Barrio, Alicia
author_role author
author2 Escario García-Trevijano, José Antonio
Mollinedo García, Faustino
Gómez Barrio, Alicia
author2_role author
author
author
dc.contributor.none.fl_str_mv Universidad Complutense de Madrid
dc.subject.none.fl_str_mv 579
Microbiología (Farmacia)
3302.03 Microbiología Industrial
topic 579
Microbiología (Farmacia)
3302.03 Microbiología Industrial
description Edelfosine (ET-18-OCH3) is an alkylphospholipid with an analogous structure to miltefosine. Both molecules are active against kinetoplastids (Leishmania spp., Trypanosoma cruzi and Trypanosoma brucei). However, its trichomonacidal effect has never been studied. For this purpose, edelfosine has been evaluated in vitro for its ability to inhibit proliferation of the common sexually transmitted parasite Trichomonas vaginalis following a standardized fluorimetric procedure. The results show an IC50 = 19.8 µM against metronidazole-sensitive isolates and a remarkable IC50 = 7.6 µM against the metronidazole-resistant IR78. This enhanced effect against the resistant isolate suggests another possible mode of action in comparison with the reference drug. Moreover, T. vaginalis exhibits a different growth rate due to the metabolic modifications according to its resistant trait. These results are in consonance with the trichomonacidal effect observed by other authors using the analog miltefosine against resistant samples, provoking membrane alterations and apoptosis. It is estimated that 2.5–10% of clinical cases of trichomonosis are produced by resistant isolates. The absence of pharmacological alternatives to the unique two 5-nitroimidazole drugs approved by the FDA makes necessary the incorporation of novel trichomonacidal drugs with a different mode of action. Taken together, our results, in consonance with previous reports, suggest the promising use of these alkylphospholipids as an alternative trichomonacidal drug against resistant cases.
publishDate 2017
dc.date.none.fl_str_mv 2017
2017-10-19
2017
2017-10-19
dc.type.none.fl_str_mv journal article
http://purl.org/coar/resource_type/c_6501
dc.type.openaire.fl_str_mv info:eu-repo/semantics/article
format article
dc.identifier.none.fl_str_mv https://hdl.handle.net/20.500.14352/19276
url https://hdl.handle.net/20.500.14352/19276
dc.language.none.fl_str_mv Inglés
eng
language_invalid_str_mv Inglés
language eng
dc.rights.none.fl_str_mv open access
http://purl.org/coar/access_right/c_abf2
Atribución 3.0 España
https://creativecommons.org/licenses/by/3.0/es/
dc.rights.openaire.fl_str_mv info:eu-repo/semantics/openAccess
rights_invalid_str_mv open access
http://purl.org/coar/access_right/c_abf2
Atribución 3.0 España
https://creativecommons.org/licenses/by/3.0/es/
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv application/pdf
dc.publisher.none.fl_str_mv MDPI
publisher.none.fl_str_mv MDPI
dc.source.none.fl_str_mv reponame:Docta Complutense
instname:Universidad Complutense de Madrid (UCM)
instname_str Universidad Complutense de Madrid (UCM)
reponame_str Docta Complutense
collection Docta Complutense
repository.name.fl_str_mv
repository.mail.fl_str_mv
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