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Título
Antiparasitic effect of synthetic aromathecins on Leishmania infantum
Autor
Facultad/Centro
Área de conocimiento
Título de la revista
BMC Veterinary Research
Número de la revista
1
Cita Bibliográfica
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
Editorial
BMC
Fecha
2019-11-09
Resumen
[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.
Materia
Palabras clave
Peer review
SI
ID proyecto
- 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 //
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