Oleamide activates peroxisome proliferator-activated receptor gamma (PPARγ) in vitro.

Lipids in Health and Disease
Mauro DionisiAndrew J Bennett

Abstract

Oleamide (ODA) is a fatty acid primary amide first identified in the cerebrospinal fluid of sleep-deprived cats, which exerts effects on vascular and neuronal tissues, with a variety of molecular targets including cannabinoid receptors and gap junctions. It has recently been reported to exert a hypolipidemic effect in hamsters. Here, we have investigated the nuclear receptor family of peroxisome proliferator-activated receptors (PPARs) as potential targets for ODA action. Activation of PPARα, PPARβ and PPARγ was assessed using recombinant expression in Chinese hamster ovary cells with a luciferase reporter gene assay. Direct binding of ODA to the ligand binding domain of each of the three PPARs was monitored in a cell-free fluorescent ligand competition assay. A well-established assay of PPARγ activity, the differentiation of 3T3-L1 murine fibroblasts into adipocytes, was assessed using an Oil Red O uptake-based assay. ODA, at 10 and 50 μM, was able to transactivate PPARα, PPARβ and PPARγ receptors. ODA bound to the ligand binding domain of all three PPARs, although complete displacement of fluorescent ligand was only evident for PPARγ, at which an IC50 value of 38 μM was estimated. In 3T3-L1 cells, ODA, at 10 and 20 μM, induce...Continue Reading

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Citations

Jun 15, 2013·Oxidative Medicine and Cellular Longevity·Jie LiuCurtis D Klaassen
Apr 15, 2016·British Journal of Pharmacology·Saoirse Elizabeth O'Sullivan
Dec 13, 2013·Biomedicines·Izak S TaitJun Lu
Sep 16, 2020·Neurotoxicity Research·Ana Laura Torres-RománAlette Ortega-Gómez
Oct 15, 2020·Journal of Agricultural and Food Chemistry·Yu ZhangAnning Li

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Methods Mentioned

BETA
NMR
transfection
Assay
protein assay
competition binding

Software Mentioned

GraphPad Prism

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