RT info:eu-repo/semantics/article
T1 Antiprotozoal activities of marine polyether triterpenoids.
A1 López Arencibia, Atteneri
A1 Díaz-Marrero, Ana R
AD 
A1 Bethencourt Estrella, Carlos Javier
A1 Cen-Pacheco, Francisco
A1 Sifaoui, Inés
A1 Hernández Creus, Alberto
A1 Duque-Ramírez, María Clara
A1 Souto Suárez, María Luisa
A1 Hernández Daranas, Antonio
A1 Lorenzo Morales, Jacob
A1 Piñero Barroso, José Enrique
A1 Fernández Castro, José Javier
K1 Marine natural products
K1 Marine polyether
K1 Oxasqualenoids
K1 Kinetoplastids
K1 Laurencia
K1 Leishmania
K1 Leishmanicidal
K1 Trypanosoma
K1 Trypanocidal
AB Chagas 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.
SN 0045-2068
YR 2019
FD 2019
LK http://riull.ull.es/xmlui/handle/915/35812
UL http://riull.ull.es/xmlui/handle/915/35812
LA en
NO Díaz-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
DS Repositorio institucional de la Universidad de La Laguna
RD 24-nov-2024