RT info:eu-repo/semantics/article
T1 Ursolic Acid Derivatives as Potential Agents Against Acanthamoeba Spp.
A1 Sifaoui, Ines
A1 Rodríguez Expósito, Rubén L.
A1 Reyes Batlle, María
A1 Rizo Liendo, Aitor
A1 Piñero Barroso, José Enrique
A1 López Bazzocchi, Isabel
A1 Lorenzo Morales, Jacob
A1 Jiménez Díaz, Ignacio Antonio
K1 ursolic acid derivatives
K1 Acanthamoeba
K1 chemotherapy
K1 programmed cell death
AB The current chemotherapy of Acanthamoeba keratitis relies on few drugs with low potentialand limited e cacy, for all this there is an urgent need to identify new classes of anti-Acanthamoebaagents. In this regard, natural products play an important role in overcoming the current need andmedicinal chemistry of natural products represents an attractive approach for the discovery anddevelopment of new agents. Ursolic acid, a natural pentacyclic triterpenoid compound, possesses abroad spectrum of activities including anti-Acanthamoeba. Herein, we report on the development bychemical transformation of an ursolic acid-based series of seven compounds (2–8), one of them reportedfor the first time. The structure-activity relationship (SAR) analysis of their anti-Acanthamoeba activityrevealed that acylation/ether formation or oxidation enhances their biological profile, suggestingthat the hydrophobic moiety contributes to activity, presumably by increasing the a nity and/or cellmembrane permeability. These ursolic acid derivatives highlight the potential of this source as a goodbase for the development of novel therapeutic agents against Acanthamoeba infections.
YR 2019
FD 2019
LK http://riull.ull.es/xmlui/handle/915/36071
UL http://riull.ull.es/xmlui/handle/915/36071
LA en
DS Repositorio institucional de la Universidad de La Laguna
RD 21-may-2024