RT info:eu-repo/semantics/article
T1 Dehydrohispanolone derivatives attenuate the Inflammatory response through the modulation of Inflammasome activation
A1 Estévez Braun, Ana María
A1 González-Cofrade, Laura
A1 Oramas-Royo, Sandra M.
A1 Cuadrado, Irene
A1 Amesty Arrieta, Ángel Ernesto
A1 Hortelano, Sonsoles
A1 Heras, Beatriz de las
A2 Química Orgánica
A2 Grupo Quibionat; Instituto de Bio-Orgánica
AB The NLRP3 inflammasome plays a critical role in inflammation-mediated human diseases and represents a promising drug target for novel anti-inflammatory therapies. Hispanolone is a labdane diterpenoid isolated from the aerial parts of Ballota species.  This diterpenoid and some derivatives have demonstrated anti-inflammatory effects in classical inflammatory pathways. In the present study, a series of dehydrohispanolone derivatives (1-19) was synthesized and their anti-inflammatory activities toward NLRP3 inflammasome activation were evaluated. The structures of the dehydrohispanolone analogues produced were elucidated by NMR spectroscopy and mass spectrometry. Four derivatives significantly inhibited IL-1β secretion, with 15 and 18 being the most active (IC50 = 18.7 and 13.8 µM, respectively). Analysis of IL-1β and caspase-1 expression revealed that the new diterpenoids 15 and 18 are selective inhibitors of the NLRP3 inflammasome, reinforcing the previously demonstrated anti-inflammatory properties of hispanolone derivatives.
YR 2020
FD 2020
LK http://riull.ull.es/xmlui/handle/915/40673
UL http://riull.ull.es/xmlui/handle/915/40673
LA en
DS Repositorio institucional de la Universidad de La Laguna
RD 27-abr-2025