Anandamide induced PPARγ transcriptional activation and 3T3-L1 preadipocyte differentiation
Abstract
We investigated the effects of anandamide on peroxisome proliferator-activated receptor gamma (PPARgamma) activity. In two different transactivation systems using either full-length or only the ligand binding domain of PPARgamma, we showed that anandamide, but not palmitoylethanolamide induced transcriptional activation of PPARgamma in a dose dependent manner with an EC50 of 8 microM. In addition, competition binding experiments showed that anandamide but not palmitoylethanolamide binds directly to PPAR-ligand binding domain. We also found that anandamide treatment induced 3T3-L1 fibroblast differentiation into adipocytes. Indeed, anandamide induced triglyceride droplet accumulation and the expression of PPARgamma responsive genes such as CCAAT enhancer binding protein alpha (C-EBPalpha), aP2, PerilipinA and Acrp30. Furthermore, the PPARgamma antagonist (GW9662) inhibited the anandamide-induced 3T3-L1 differentiation confirming that this is a PPARgamma-mediated process. Altogether, these data indicate that anandamide binds PPARgamma and induces cellular PPARgamma signaling.
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AEA can also activate the PPARγ receptor.
“AEA can also activate the peroxisome proliferator receptor-γ (PPARγ) receptor.32”
From Cannabinoids as Pharmacotherapies for Neuropathic Pain: From the Bench to the Bedside (2009) · cites this paper as [32]
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- Authors
- Bouaboula, M., Hilairet, S., Marchand, J., Fajas, L., Fur, G. L., & Casellas, P.
- Affiliations
- Sanofi (France) (FR)
- Corresponding author
- Casellas, Pierre
- Venue
- European Journal of Pharmacology
- Publisher
- Elsevier BV
- Published
- 2005-07
- Volume
- 517
- Issue
- 3
- Pages
- 174-181
- ISSN
- 0014-2999 (ISSN-L)
- OpenAlex
- W2061169432
- Cited by
- 298
- References
- 43
- Citations by year
- 2026: 4 · 2025: 8 · 2024: 9 · 2023: 10 · 2022: 7 · 2021: 25 · 2020: 14 · 2019: 14 · 2018: 15 · 2017: 13 · 2016: 14 · 2015: 16 · 2014: 19 · 2013: 17 · 2012: 17
- FWCI
- 5.92
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- European Journal of Pharmacology (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Peroxisome Proliferator-Activated Receptors
- Health Sciences › Nursing › Nutrition and Dietetics › Fatty Acid Research and Health
- Health Sciences › Medicine › Pharmacology › Cannabis and Cannabinoid Research
- Keywords
- anandamide, PPARγ, transcriptional activation, adipogenesis, palmitoylethanolamide, GW9662, C/EBPα, AP-2, perilipin, adiponectin, endocannabinoids, triglyceride accumulation
- MeSH terms
- Perilipin-1, Pioglitazone, Troglitazone, Anilides, Animals, Arachidonic Acids, Binding Sites, Binding, Competitive, Carrier Proteins, Cell Differentiation, Cell Line, Chlorocebus aethiops, Chromans, Dose-Response Relationship, Drug, Fibroblasts, HeLa Cells, Humans, Luciferases, Phosphoproteins, Plasmids, Recombinant Fusion Proteins, Transfection, Blotting, Western, Transcriptional Activation, Gene Expression, Adipocytes, COS Cells, Reverse Transcriptase Polymerase Chain Reaction, CCAAT-Enhancer-Binding Protein-alpha, Intercellular Signaling Peptides and Proteins, 3T3-L1 Cells, Thiazolidinediones, PPAR gamma, Mice, Adiponectin, Polyunsaturated Alkamides, Cannabinoid Receptor Modulators, Endocannabinoids
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