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Title

Antiprotozoal activities of marine polyether triterpenoids

AuthorsDíaz-Marrero, Ana R. CSIC ORCID; López-Arencibia, Atteneri; Bethencout-Estrella, Carlos J.; Cen-Pacheco, Francisco; Sifaoui, Ines; Hernández Creus, Alberto; Duque-Ramírez, María Clara; Souto, María L.; Hernández Daranas, Antonio CSIC ORCID ; Lorenzo-Morales, Jacob; Piñero, José E.; Fernández, José J.
KeywordsLeishmanicidal
Trypanocidal
Trypanosoma
Marine polyether
Marine natural products
Oxasqualenoids
Kinetoplastids
Laurencia
Leishmania
Issue Date11-Sep-2019
PublisherElsevier
CitationBioorganic Chemistry 92: 103276 (2019)
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 IC 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 IC 5.40 µM against Leishmania amazonensis, turned to be non-toxic against the murine macrophage cell line J774A.1 (CC > 100). These values are comparable with the reference compound miltefosine IC 6.48 ± 0.24 and CC 72.19 ± 3.06 μM, suggesting that this substance could be scaffold for development of new antikinetoplastid drugs.
Publisher version (URL)https://doi.org/10.1016/j.bioorg.2019.103276
URIhttp://hdl.handle.net/10261/193206
DOI10.1016/j.bioorg.2019.103276
Identifiersdoi: 10.1016/j.bioorg.2019.103276
e-issn: 1090-2120
issn: 0045-2068
Appears in Collections:(IPNA) Artículos

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