RT info:eu-repo/semantics/article
T1 Phenolic and quinone methide nor-triterpenes as selective NLRP3 inflammasome inhibitors
A1 Estévez Braun, Ana María
A1 González-Cofrade, Laura
A1 Green, Jack P.
A1 Cuadrado, Irene
A1 Amesty Arrieta, Ángel Ernesto
A1 Oramas-Royo, Sandra M.
A1 Brough, David
A1 Hortelano, Sonsoles
A1 Heras, Beatriz de las
A2 Química Orgánica
A2 Grupo de Investigación Quibionat. Instituto Universitario de Bio-Orgánica
K1 Nor-friedelane triterpenes
K1 Maytenus retusa
K1 NLRP3 inflammasome
K1 ASC
K1 pyroptosis
K1 IL-1b
K1 macrophages
AB Dysregulated inflammasome activity, particularly of the NLRP3 inflammasome, is associated with the development of several inflammatory diseases. The study of molecules directly targeting NLRP3 is an emerging field in the discovery of new therapeutic compounds for the treatment of inflammatory disorders. Friedelane triterpenes are biologically active phytochemicals having a wide range of activities including anti-inflammatory effects. In this work, we evaluated the potential anti-inflammatory activity of phenolic and quinonemethide nor-triterpenes (1-11) isolated from Maytenus retusa and some semisynthetic derivatives (12-16) through inhibition of the NLRP3 inflammasome in macrophages. Among them, we found that triterpenes 6 and 14 were the most potent, showing markedly reduced caspase-1 activity, IL-1β secretion (IC50 = 1.15 µM and 0.19 µM, respectively), and pyroptosis (IC50 = 2.21 µM and 0.13 µM, respectively). Further characterization confirmed their selective inhibition of NLRP3 inflammasome in both canonical and non-canonical activation pathways with no effects on AIM2 or NLRC4 inflammasome activation.
YR 2023
FD 2023
LK http://riull.ull.es/xmlui/handle/915/40664
UL http://riull.ull.es/xmlui/handle/915/40664
LA en
DS Repositorio institucional de la Universidad de La Laguna
RD 13-nov-2025