RT Journal Article
T1 Isomeric O-methyl cannabidiolquinones with dual BACH1/NRF2 activity.
A1 Casares, Laura
A1 Unciti-Broceta, Juan Diego
A1 Prados, Maria Eugenia
A1 Caprioglio, Diego
A1 Mattoteia, Daiana
A1 Higgins, Maureen
A1 Apendino, Giovanni
A1 Dinkova-Kostova, Albena T
A1 Muñoz, Eduardo
A1 de la Vega, Laureano
K1 Cannabidiol derivative/ NRF2/ BACH1/ HMOX1/ neurodegenerative diseases
K1 Mice
K1 NF-E2-related factor 2
K1 Neurodegenerative diseases
K1 Oxidative stress
AB Oxidative stress and inflammation in the brain are two key hallmarks of neurodegenerative diseases (NDs) such as Alzheimer's, Parkinson's, Huntington's and multiple sclerosis. The axis NRF2-BACH1 has anti-inflammatory and anti-oxidant properties that could be exploited pharmacologically to obtain neuroprotective effects. Activation of NRF2 or inhibition of BACH1 are, individually, promising therapeutic approaches for NDs. Compounds with dual activity as NRF2 activators and BACH1 inhibitors, could therefore potentially provide a more robust antioxidant and anti-inflammatory effects, with an overall better neuroprotective outcome. The phytocannabinoid cannabidiol (CBD) inhibits BACH1 but lacks significant NRF2 activating properties. Based on this scaffold, we have developed a novel CBD derivative that is highly effective at both inhibiting BACH1 and activating NRF2. This new CBD derivative provides neuroprotection in cell models of relevance to Huntington's disease, setting the basis for further developments in vivo.
PB Elsevier
YR 2020
FD 2020-08-22
LK http://hdl.handle.net/10668/16178
UL http://hdl.handle.net/10668/16178
LA en
NO Casares L, Unciti-Broceta JD, Prados ME, Caprioglio D, Mattoteia D, Higgins M, et al. Isomeric O-methyl cannabidiolquinones with dual BACH1/NRF2 activity. Redox Biol. 2020 Oct;37:101689
DS RISalud
RD Apr 19, 2025