dianas 9 (1) González-Cofrade etal 2020 Anti-inflammatory activity of labdanediol-derived diterpenes.

dianas 9(1) > González-Cofrade etal

dianas | Vol 9 Num 1 | marzo 2020 | e202003c01

Anti-inflammatory activity of labdanediol-derived diterpenes.

1. Departamento de Farmacología, Farmacognosia y Botánica, Facultad de Farmacia, Universidad Complutense de Madrid.  2. Instituto Universitario de Bio-Orgánica "Antonio González". Universidad de La Laguna, Tenerife, Spain.  3. Unidad de Terapias Farmacológicas, Instituto de Investigaciones en Enfermedades Raras (IIER), Instituto de Salud Carlos III (ISCIII), Majadahonda, Madrid, España.


V Congreso de Señalización Celular, SECUAH 2020.
16-18 de marzo, 2020. Universidad de Alcalá. Alcalá de Henares, Madrid. España.


Inflammation is a protective physiological response triggered by microbial infection or tissue injury with a key role in the pathogenesis of several chronic diseasease, due to the up-regulation and overproduction of proinflammatory mediators and the dysregulation of the NLRP3 inflammasome. Terpenes are bioactive natural products with great therapeutic potential. In this work, a series of ten novel labdanes derivatives (LB1-LB10) from the diterpene labdanediol isolated from Oxylobus glanduliferus was synthetized and evaluated for anti-inflammatory potential in lipopolysaccharide (LPS)-treated J774A.1 macrophages. Inhibitory effects of the non-toxic compounds on nitric oxide (NO) release were evaluated. Labdanediol derivative LB5 was selected as the most active inhibitor (IC50= 10 µM). LB5 also significantly inhibited the protein expression of Nitric Oxide Synthase-2 (NOS-2) and Cyclooxygenase-2 (COX-2) enzymes and the gene expression at the transcriptional level of NOS-2, COX-2 and inflammatory cytokines (IL-6, TNFα). Regulation of NLRP3 inflammasome pathway seems not to be involved in the anti-inflammatory activity of these compounds, as IL-1β levels in LPS/ATP-stimulated macrophages were not significantly reduced by treatment with these derivatives. In summary, we have identified a novel labdanediol derivative (LB5) with potential anti-inflammatory activity so it can be considered as a promising starting point for the development of new anti-inflamatory agents. Further experiments will be performed to elucidate the molecular mechanisms involved.

Citation: González-Cofrade, Laura; Cuadrado, Irene; Estévez-Braun, Ana; Hortelano, Sonsoles; de las Heras, Beatriz (2020) Anti-inflammatory activity of labdanediol-derived diterpenes. Proceedings of the V Congreso de Señalización Celular, SECUAH 2020. 16-18 de marzo, 2020. Universidad de Alcalá. Alcalá de Henares, Madrid. España. dianas 9 (1): e202003c01. ISSN 1886-8746 (electronic) journal.dianas.e202003c01 http://www3.uah.es/dianas?e202003c01. URI http://hdl.handle.net/10017/15181. DOI https://doi.org/10.37536/DIANAS.2020.9.1.80

Copyright: © González-Cofrade L, Cuadrado I, Estévez-Braun A, Hortelano S, de-las-Heras B. Some rights reserved. This is an open-access work licensed under a Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International License. http://creativecommons.org/licenses/by-nc-nd/4.0/

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