Identification of a Strigoterpenoid with Dual Nrf2 and Nf-κB Modulatory Activity

Federica Rogati; Estrella Millán; Giovanni Appendino; Alejandro Correa; Diego Caprioglio; Alberto Minassi; Eduardo Muñoz

doi:10.1021/acsmedchemlett.8b00604

Identification of a Strigoterpenoid with Dual Nrf2 and Nf-κB Modulatory Activity

ACS Med Chem Lett. 2019 Jan 8;10(4):606-610. doi: 10.1021/acsmedchemlett.8b00604. eCollection 2019 Apr 11.

Authors

Federica Rogati¹, Estrella Millán^{2

3

4}, Giovanni Appendino¹, Alejandro Correa^{2

3

4}, Diego Caprioglio¹, Alberto Minassi¹, Eduardo Muñoz^{2

3

4}

Affiliations

¹ Dipartimento di Scienze del Farmaco, Università del Piemonte Orientale, Via Bovio 6, Novara 28100, Italy.
² Maimonides Biomedical Research Institute of Córdoba, Avda Menendez Pidal s/n, 14004 Cordoba, Spain.
³ Department of Cellular Biology, Physiology and Immunology, University of Cordoba, Avda Menendez Pidal s/n, 14004 Cordoba, Spain.
⁴ University Hospital Reina Sofía, Avda Menendez Pidal s/n, 14004 Cordoba, Spain.

Abstract

The sesquiterpene-coumarin ether samarcandone provided a suitable framework to replace the apocarotenoid A-C ring system of strigol (1), replicating, after linking to a butenolide moiety, the activity of the natural phytohormone on Nrf2 and also showing potent NF-kB inhibitory activity, overall modulating two critical pathways of inflammation and cancer.