RT Journal Article
T1 Dehydrohispanolone derivatives attenuate the inflammatory response through the modulation of inflammasome activation
A1 Heras Polo, Beatriz De Las
A1 González Cofrade, Laura
A1 Cuadrado Berrocal, Irene
A1 Oramas-Royo, Sandra
A1 Amesty, Angel
A1 Hortelano, Sonsoles
A1 Estevez-Braun, Ana
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 and18 are selective inhibitors of the NLRP3 inflammasome, reinforcing the previously demonstrated anti-inflammatory properties ofhispanolone derivatives
PB ACS Publications
YR 2020
FD 2020
LK https://hdl.handle.net/20.500.14352/118891
UL https://hdl.handle.net/20.500.14352/118891
LA eng
NO González-Cofrade L, Oramas-Royo S, Cuadrado I, Amesty Á, Hortelano S, Estevez-Braun A, et al. Dehydrohispanolone Derivatives Attenuate the Inflammatory Response through the Modulation of Inflammasome Activation. J Nat Prod 2020;83:2155–64. https://doi.org/10.1021/acs.jnatprod.0c00200.
NO Ministerio de Ciencia, Innovacion y Universidades (MICIU)
NO Agencia Canaria de Investigacion, ́Innovacion y Sociedad de la Informacion (ACIISI)
NO Instituto de Salud Carlos III
DS Docta Complutense
RD 7 jun 2025