Hypoxia mimetic activity of VCE-004.8, a cannabidiol quinone derivative: implications for multiple sclerosis therapy

Journal of Neuroinflammation
Carmen NavarreteEduardo Muñoz

Abstract

Multiple sclerosis (MS) is characterized by a combination of inflammatory and neurodegenerative processes variously dominant in different stages of the disease. Thus, immunosuppression is the goal standard for the inflammatory stage, and novel remyelination therapies are pursued to restore lost function. Cannabinoids such as 9Δ-THC and CBD are multi-target compounds already introduced in the clinical practice for multiple sclerosis (MS). Semisynthetic cannabinoids are designed to improve bioactivities and druggability of their natural precursors. VCE-004.8, an aminoquinone derivative of cannabidiol (CBD), is a dual PPARγ and CB2 agonist with potent anti-inflammatory activity. Activation of the hypoxia-inducible factor (HIF) can have a beneficial role in MS by modulating the immune response and favoring neuroprotection and axonal regeneration. We investigated the effects of VCE-004.8 on the HIF pathway in different cell types. The effect of VCE-004.8 on macrophage polarization and arginase 1 expression was analyzed in RAW264.7 and BV2 cells. COX-2 expression and PGE2 synthesis induced by lipopolysaccharide (LPS) was studied in primary microglia cultures. The efficacy of VCE-004.8 in vivo was evaluated in two murine models of MS ...Continue Reading

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Citations

Jul 30, 2019·Frontiers in Immunology·Giada MondanelliUrsula Grohmann
Apr 28, 2020·Expert Opinion on Drug Discovery·Paula Morales, Nadine Jagerovic
Mar 21, 2020·Acta Neuropathologica Communications·Sabela Rodríguez-LorenzoHelga E de Vries
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Apr 4, 2021·International Journal of Molecular Sciences·Carmen NavarreteEduardo Muñoz
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Datasets Mentioned

BETA
SR144528

Methods Mentioned

BETA
PMA
transfection
Assay
PCR
ELISA
FCS

Software Mentioned

Incucyte FLR
IncuCyte
ImageJ
GraphPad Prism

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