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dc.contributor.authorLópez Arencibia, Atteneri 
dc.contributor.authorDíaz-Marrero, Ana R,
dc.contributor.authorBethencourt Estrella, Carlos Javier
dc.contributor.authorCen-Pacheco, Francisco
dc.contributor.authorSifaoui, Inés 
dc.contributor.authorHernández Creus, Alberto 
dc.contributor.authorDuque-Ramírez, María Clara
dc.contributor.authorSouto Suárez, María Luisa
dc.contributor.authorHernández Daranas, Antonio
dc.contributor.authorLorenzo Morales, Jacob 
dc.contributor.authorPiñero Barroso, José Enrique 
dc.contributor.authorFernández Castro, José Javier
dc.date.accessioned2024-01-29T21:06:20Z
dc.date.available2024-01-29T21:06:20Z
dc.date.issued2019
dc.identifier.issn0045-2068
dc.identifier.urihttp://riull.ull.es/xmlui/handle/915/35812
dc.descriptionDíaz-Marrero, A. R., López-Arencibia, A., Bethencout-Estrella, C. J., Cen-Pacheco, F., Sifaoui, I., Hernández Creus, A., Duque-Ramírez, M. C., Souto, M. L., Hernández Daranas, A., Lorenzo-Morales, J., Piñero, J. E., & Fernández, J. J. (2019). Antiprotozoal activities of marine polyether triterpenoids. Bioorganic chemistry, 92, 103276. https://doi.org/10.1016/j.bioorg.2019.103276
dc.description.abstractChagas disease and leishmaniasis are tropical neglected diseases caused by kinetoplastids protozoan parasites of Trypanosoma and Leishmania genera, and a public health burden with high morbidity and mortality rates in developing countries. Among difficulties with their epidemiological control, a major problem is their limited and toxic treatments to attend the affected populations; therefore, new therapies are needed in order to find new active molecules. In this work, sixteen Laurencia oxasqualenoid metabolites, natural compounds 1–11 and semisynthetic derivatives 12–16, were tested against Leishmania amazonensis, Leishmania donovani and Trypanosoma cruzi. The results obtained point out that eight substances possess potent activities, with IC50 values in the range of 5.40–46.45 µM. The antikinetoplastid action mode of the main metabolite dehydrothyrsiferol (1) was developed, also supported by AFM images. The semi-synthetic active compound 28-iodosaiyacenol B (15) showed an IC50 5.40 µM against Leishmania amazonensis, turned to be non-toxic against the murine macrophage cell line J774A.1 (CC50 > 100). These values are comparable with the reference compound miltefosine IC50 6.48 ± 0.24 and CC50 72.19 ± 3.06 μM, suggesting that this substance could be scaffold for development of new antikinetoplastid drugs.en
dc.format.mimetypeapplication/pdf
dc.language.isoenen
dc.relation.ispartofseriesBioorganic Chemistry, 92, (2019)
dc.rightsLicencia Creative Commons (Reconocimiento-No comercial-Sin obras derivadas 4.0 Internacional)
dc.rights.urihttps://creativecommons.org/licenses/by-nc-nd/4.0/deed.es_ES
dc.titleAntiprotozoal activities of marine polyether triterpenoids.
dc.typeinfo:eu-repo/semantics/article
dc.identifier.doi10.1016/j.bioorg.2019.103276
dc.subject.keywordMarine natural products
dc.subject.keywordMarine polyether
dc.subject.keywordOxasqualenoids
dc.subject.keywordKinetoplastids
dc.subject.keywordLaurencia
dc.subject.keywordLeishmania
dc.subject.keywordLeishmanicidal
dc.subject.keywordTrypanosoma
dc.subject.keywordTrypanocidal


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