New benzimidazole derivative compounds with in vitro fasciolicidal properties
[EN] Background: Control of the zoonotic food-borne parasite Fasciola hepatica remains a major challenge in humans and livestock. It is estimated that annual economic losses due to fasciolosis can reach US$3.2 billion in agriculture and livestock. Moreover, the wide distribution of drug-resistant pa...
| Autores: | , , , , , , , , , |
|---|---|
| Tipo de recurso: | artículo |
| Estado: | Versión publicada |
| Fecha de publicación: | 2024 |
| País: | España |
| Institución: | Universidad de León |
| Repositorio: | BULERIA. Repositorio Institucional de la Universidad de León |
| OAI Identifier: | oai:buleria.unileon.es:10612/25802 |
| Acceso en línea: | https://parasitesandvectors.biomedcentral.com/articles/10.1186/s13071-024-06224-6 https://hdl.handle.net/10612/25802 |
| Access Level: | acceso abierto |
| Palabra clave: | Sanidad animal Veterinaria Fasciola hepatica Benzimidazole Anthelmintic resistance Zoonotic disease 2401.12 Parasitología Animal 3109.08 Farmacología |
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oai:buleria.unileon.es:10612/25802 |
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New benzimidazole derivative compounds with in vitro fasciolicidal propertiesValderas García, EloraCastilla Gómez de Agüero, VerónicaGonzález del Palacio, LauraGalli, GiulioEscala, NereaRuiz Somacarrera, MartaGonzález Warleta, MartaOlmo, Esther delBalaña Fouce, RafaelMartínez Valladares, MaríaSanidad animalVeterinariaFasciola hepaticaBenzimidazoleAnthelmintic resistanceZoonotic disease2401.12 Parasitología Animal3109.08 Farmacología[EN] Background: Control of the zoonotic food-borne parasite Fasciola hepatica remains a major challenge in humans and livestock. It is estimated that annual economic losses due to fasciolosis can reach US$3.2 billion in agriculture and livestock. Moreover, the wide distribution of drug-resistant parasite populations and the absence of a vaccine threaten sustainable control, reinforcing the need for novel flukicides. Methods: The present work analyses the flukicidal activity of a total of 70 benzimidazole derivatives on different stages of F. hepatica. With the aim to select the most potent ones, and screenings were first performed on eggs at decreasing concentrations ranging from 50 to 5 µM and then on adult worms at 10 µM. Only the most effective compounds were also evaluated using a resistant isolate of the parasite. Results: After the first screenings at 50 and 10 µM, four hit compounds (BZD31, BZD46, BZD56, and BZD59) were selected and progressed to the next assays. At 5 µM, all hit compounds showed ovicidal activities higher than 71% on the susceptible isolate, but only BZD31 remained considerably active (53%) when they were tested on an albendazol-resistant isolate, even with values superior to the reference drug, albendazole sulfoxide. On the other hand, BZD59 displayed a high motility inhibition when tested on adult worms from an albendazole-resistant isolate after 72 h of incubation. Conclusions: BZD31 and BZD59 compounds could be promising candidates for the development of fasciolicidal compounds or as starting point for the new synthesis of structure-related compoundsSIFinancial support came from PID2020-119035RB-100 funded by MCIN/AEI/10.13039/501100011033 and, by “ERDF A way of making Europe”. EVG was funded by European Union Next Generation EU/PRTR (Margarita Salas Grant for the training of young doctors); VCGA and LGDP are recipients of Junta de Castilla y León (JCyL) grants (LE082-18, LE096-20, respectively); GG was funded by PRE2021-096909, grant funded by MCIN/AEI/10.13039/501100011033 and, by “ESF Investing in your future”BioMed CentralSanidad AnimalFacultad de Veterinaria2024info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionhttps://parasitesandvectors.biomedcentral.com/articles/10.1186/s13071-024-06224-6https://hdl.handle.net/10612/25802reponame:BULERIA. Repositorio Institucional de la Universidad de Leóninstname:Universidad de LeónIngléshttp://creativecommons.org/licenses/by/4.0/info:eu-repo/semantics/openAccessoai:buleria.unileon.es:10612/258022026-06-24T12:43:27Z |
| dc.title.none.fl_str_mv |
New benzimidazole derivative compounds with in vitro fasciolicidal properties |
| title |
New benzimidazole derivative compounds with in vitro fasciolicidal properties |
| spellingShingle |
New benzimidazole derivative compounds with in vitro fasciolicidal properties Valderas García, Elora Sanidad animal Veterinaria Fasciola hepatica Benzimidazole Anthelmintic resistance Zoonotic disease 2401.12 Parasitología Animal 3109.08 Farmacología |
| title_short |
New benzimidazole derivative compounds with in vitro fasciolicidal properties |
| title_full |
New benzimidazole derivative compounds with in vitro fasciolicidal properties |
| title_fullStr |
New benzimidazole derivative compounds with in vitro fasciolicidal properties |
| title_full_unstemmed |
New benzimidazole derivative compounds with in vitro fasciolicidal properties |
| title_sort |
New benzimidazole derivative compounds with in vitro fasciolicidal properties |
| dc.creator.none.fl_str_mv |
Valderas García, Elora Castilla Gómez de Agüero, Verónica González del Palacio, Laura Galli, Giulio Escala, Nerea Ruiz Somacarrera, Marta González Warleta, Marta Olmo, Esther del Balaña Fouce, Rafael Martínez Valladares, María |
| author |
Valderas García, Elora |
| author_facet |
Valderas García, Elora Castilla Gómez de Agüero, Verónica González del Palacio, Laura Galli, Giulio Escala, Nerea Ruiz Somacarrera, Marta González Warleta, Marta Olmo, Esther del Balaña Fouce, Rafael Martínez Valladares, María |
| author_role |
author |
| author2 |
Castilla Gómez de Agüero, Verónica González del Palacio, Laura Galli, Giulio Escala, Nerea Ruiz Somacarrera, Marta González Warleta, Marta Olmo, Esther del Balaña Fouce, Rafael Martínez Valladares, María |
| author2_role |
author author author author author author author author author |
| dc.contributor.none.fl_str_mv |
Sanidad Animal Facultad de Veterinaria |
| dc.subject.none.fl_str_mv |
Sanidad animal Veterinaria Fasciola hepatica Benzimidazole Anthelmintic resistance Zoonotic disease 2401.12 Parasitología Animal 3109.08 Farmacología |
| topic |
Sanidad animal Veterinaria Fasciola hepatica Benzimidazole Anthelmintic resistance Zoonotic disease 2401.12 Parasitología Animal 3109.08 Farmacología |
| description |
[EN] Background: Control of the zoonotic food-borne parasite Fasciola hepatica remains a major challenge in humans and livestock. It is estimated that annual economic losses due to fasciolosis can reach US$3.2 billion in agriculture and livestock. Moreover, the wide distribution of drug-resistant parasite populations and the absence of a vaccine threaten sustainable control, reinforcing the need for novel flukicides. Methods: The present work analyses the flukicidal activity of a total of 70 benzimidazole derivatives on different stages of F. hepatica. With the aim to select the most potent ones, and screenings were first performed on eggs at decreasing concentrations ranging from 50 to 5 µM and then on adult worms at 10 µM. Only the most effective compounds were also evaluated using a resistant isolate of the parasite. Results: After the first screenings at 50 and 10 µM, four hit compounds (BZD31, BZD46, BZD56, and BZD59) were selected and progressed to the next assays. At 5 µM, all hit compounds showed ovicidal activities higher than 71% on the susceptible isolate, but only BZD31 remained considerably active (53%) when they were tested on an albendazol-resistant isolate, even with values superior to the reference drug, albendazole sulfoxide. On the other hand, BZD59 displayed a high motility inhibition when tested on adult worms from an albendazole-resistant isolate after 72 h of incubation. Conclusions: BZD31 and BZD59 compounds could be promising candidates for the development of fasciolicidal compounds or as starting point for the new synthesis of structure-related compounds |
| publishDate |
2024 |
| dc.date.none.fl_str_mv |
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 |
https://parasitesandvectors.biomedcentral.com/articles/10.1186/s13071-024-06224-6 https://hdl.handle.net/10612/25802 |
| url |
https://parasitesandvectors.biomedcentral.com/articles/10.1186/s13071-024-06224-6 https://hdl.handle.net/10612/25802 |
| dc.language.none.fl_str_mv |
Inglés |
| language_invalid_str_mv |
Inglés |
| dc.rights.none.fl_str_mv |
http://creativecommons.org/licenses/by/4.0/ info:eu-repo/semantics/openAccess |
| rights_invalid_str_mv |
http://creativecommons.org/licenses/by/4.0/ |
| eu_rights_str_mv |
openAccess |
| dc.publisher.none.fl_str_mv |
BioMed Central |
| publisher.none.fl_str_mv |
BioMed Central |
| dc.source.none.fl_str_mv |
reponame:BULERIA. Repositorio Institucional de la Universidad de León instname:Universidad de León |
| instname_str |
Universidad de León |
| reponame_str |
BULERIA. Repositorio Institucional de la Universidad de León |
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BULERIA. Repositorio Institucional de la Universidad de León |
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