AM251, a cannabinoid receptor 1 antagonist, prevents human fibroblasts differentiation and collagen deposition induced by TGF-β – An in vitro study

Previous studies showed that cannabinoid 1 receptor (CB1) is linked with skin fibrosis and scar tissue formation in mice. Therefore, the topical use of cannabinoids may have a role in the prevention or treatment of local fibrotic and wound healing diseases as hypertrophic scars or keloids. In this s...

Full description

Saved in:
Bibliographic Details
Published in:European journal of pharmacology 2021-02, Vol.892, p.173738-173738, Article 173738
Main Authors: Correia-Sá, Inês B., Carvalho, Cláudia M., Serrão, Paula V., Machado, Vera A., Carvalho, Sofia O., Marques, Marisa, Vieira-Coelho, Maria A.
Format: Article
Language:English
Subjects:
Actins - metabolism
Adult
AM251
Cannabinoid Receptor Antagonists - pharmacology
CB1 receptors
Cell Differentiation - drug effects
Cells, Cultured
Collagen - metabolism
Female
Fibroblasts
Fibroblasts - drug effects
Fibroblasts - metabolism
Fibroblasts - pathology
Fibrosis
Humans
Middle Aged
Myofibroblasts - drug effects
Myofibroblasts - metabolism
Myofibroblasts - pathology
Piperidines - pharmacology
Pyrazoles - pharmacology
Receptor, Cannabinoid, CB1 - antagonists & inhibitors
Receptor, Cannabinoid, CB1 - metabolism
Signal Transduction
Skin
TGF-β
Transforming Growth Factor beta1 - pharmacology
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:Previous studies showed that cannabinoid 1 receptor (CB1) is linked with skin fibrosis and scar tissue formation in mice. Therefore, the topical use of cannabinoids may have a role in the prevention or treatment of local fibrotic and wound healing diseases as hypertrophic scars or keloids. In this study, we asked whether CB1 activation or inactivation would change fibroblast differentiation into myofibroblast and collagen deposition in skin human fibroblast. Primary cultures of adult human fibroblasts were obtained from abdominal human skin. Cells were stimulated with transforming growth factor-beta (TGF-β, 10ng/ml) and treated with a CB1 selective agonist (arachidonyl-2-chloroethylamide, ACEA 1 μM) and an antagonist (AM251 1, 5 and 10 μM). Alpha-smooth muscle actin (α-SMA) was quantified using Immunocytochemistry and Western Blot. Collagen was quantified with Sirius Red staining assay. Significance was assessed by One-way ANOVA. P 
ISSN:0014-2999
1879-0712
DOI:10.1016/j.ejphar.2020.173738