dc.contributor | Facultad de Veterinaria | es_ES |
dc.contributor.author | Reguera Torres, Rosa María | |
dc.contributor.author | Álvarez Velilla, Raquel | |
dc.contributor.author | Domínguez Asenjo, Bárbara | |
dc.contributor.author | Gutiérrez Corbo, María del Camino | |
dc.contributor.author | Balaña Fouce, Rafael | |
dc.contributor.author | Cushman, Mark | |
dc.contributor.author | Pérez Pertejo, Maria Yolanda | |
dc.contributor.other | Toxicologia | es_ES |
dc.date | 2019-11-09 | |
dc.date.accessioned | 2024-01-26T10:00:09Z | |
dc.date.available | 2024-01-26T10:00:09Z | |
dc.identifier.citation | Reguera, R. M., Álvarez-Velilla, R., Domínguez-Asenjo, B., Gutiérrez-Corbo, C., Balaña-Fouce, R., Cushman, M., & Pérez-Pertejo, Y. (2019). Antiparasitic effect of synthetic aromathecins on Leishmania infantum. BMC veterinary research, 15(1), 405. https://doi.org/10.1186/s12917-019-2153-9 | es_ES |
dc.identifier.other | https://bmcvetres.biomedcentral.com/articles/10.1186/s12917-019-2153-9 | es_ES |
dc.identifier.uri | https://hdl.handle.net/10612/17836 | |
dc.description.abstract | [EN} Background Canine leishmaniasis is a zoonotic disease caused by Leishmania infantum, being the dogs one of the major reservoirs of human visceral leishmaniasis. DNA topology is a consolidated target for drug discovery. In this regard, topoisomerase IB – one of the enzymes controlling DNA topology – has been poisoned by hundreds of compounds that increase DNA fragility and cell death. Aromathecins are novel molecules with a multiheterocyclic ring scaffold that have higher stability than camptothecins. Results Aromathecins showed strong activity against both forms of L. infantum parasites, free-living promastigotes and intra-macrophagic amastigotes harbored in ex vivo splenic explant cultures obtained from infected BALB/c mice. However, they prevented the relaxation activity of leishmanial topoisomerase IB weakly, which suggests that the inhibition of topoisomerase IB partially explains the antileishmanial effect of these compounds. The effect of aromathecins was also studied against a strain resistant to camptothecin, and results suggested that the trafficking of these compounds is not through the ABCG6 transporter. Conclusions Aromathecins are promising novel compounds against canine leishmaniasis that can circumvent potential resistances based on drug efflux pumps. | es_ES |
dc.language | eng | es_ES |
dc.publisher | BMC | es_ES |
dc.rights | Attribution-NonCommercial-NoDerivatives 4.0 Internacional | * |
dc.rights.uri | http://creativecommons.org/licenses/by-nc-nd/4.0/ | * |
dc.subject | Veterinaria | es_ES |
dc.subject.other | Leishmania | es_ES |
dc.subject.other | DNA-Topoisomerase IB | es_ES |
dc.subject.other | Camptothecin | es_ES |
dc.subject.other | Aromathecins | es_ES |
dc.title | Antiparasitic effect of synthetic aromathecins on Leishmania infantum | es_ES |
dc.type | info:eu-repo/semantics/article | es_ES |
dc.identifier.doi | 10.1186/s12917-019-2153-9 | |
dc.description.peerreviewed | SI | es_ES |
dc.relation.projectID | info:eu-repo/grantAgreement/AEI/ Programa Estatal de I+D+i Orientada a los Retos de la Sociedad / SAF2017-83575-R/ES/ AUTOVIA A LOS LISOSOMAS: DIRIGIENDO A MACROFAGOS INFECTADOS // | es_ES |
dc.rights.accessRights | info:eu-repo/semantics/openAccess | es_ES |
dc.identifier.essn | 1746-6148 | |
dc.journal.title | BMC Veterinary Research | es_ES |
dc.volume.number | 15 | es_ES |
dc.issue.number | 1 | es_ES |
dc.page.initial | 405 | es_ES |
dc.type.hasVersion | info:eu-repo/semantics/publishedVersion | es_ES |
dc.subject.unesco | 3109 Ciencias Veterinarias | es_ES |
dc.subject.unesco | 32 Ciencias Médicas | es_ES |
dc.description.project | This research had the financial support of: Ministerio de Economía y Competitividad (MINECO, AEI, FEDER, UE) [MINECO: AGL2016–79813-C2-1R, SAF2017–83575-R]. Junta de Castilla y León cofinanced by FEDER UE [LE020P17, Grant UIC108]. The funding body does not participate in the design of the study; collection, analysis and interpretation of data and in writing the manuscript. | es_ES |