2026-06-29T02:33:32Zhttps://docta.ucm.es/rest/oai/requestoai:docta.ucm.es:20.500.14352/1188912025-05-23T17:44:49Zcom_20.500.14352_14col_20.500.14352_15
Dehydrohispanolone derivatives attenuate the inflammatory response through the modulation of inflammasome activation
Heras Polo, Beatriz De Las
González Cofrade, Laura
Cuadrado Berrocal, Irene
Oramas-Royo, Sandra
Amesty, Angel
Hortelano, Sonsoles
Estevez-Braun, Ana
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
2025-03-21T11:35:37Z
2025-03-21T11:35:37Z
2025-03-21T11:35:37Z
2020
journal article
https://hdl.handle.net/20.500.14352/118891
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10.1021/acs.jnatprod.0c00200
eng
RTI2018-094356-BC21
Pro ID 2017010071
PI17/00012
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.
http://creativecommons.org/licenses/by-nc-nd/4.0/
open access
Attribution-NonCommercial-NoDerivatives 4.0 International
ACS Publications