Oregano: a source for peroxisome proliferator-activated receptor gamma antagonists.
Peroxisome proliferator-activated receptors (PPARs) are drug targets for several perturbations of metabolic syndrome, defined as the coexistence of obesity, hyperglycemia, hypertension, and hyper/dyslipidemia. In this study, PPAR activation by oregano (e.g., Origanum vulgare) and its components was tested. Oregano extracts bind but do not transactivate PPARgamma, and binding affinity differs among different oregano extracts. The extracts contain PPARgamma antagonists (e.g., quercetin, luteolin, rosmarinic acid, and diosmetin), selective PPARgamma modulators (e.g., naringenin and apigenin), and PPARgamma agonists (e.g., biochanin A). Oregano extract and isolated compounds in the extract antagonize rosiglitazone-mediated DRIP205/TRAP220 recruitment to PPARgamma, pointing to oregano extracts as putative food supplements for weight reduction. Rosmarinic acid and biochanin A, PPARalpha agonists, may ameliorate the lipid profile. By endothelial nitric oxide synthase activation, oregano extract could prevent atherosclerosis. The results warrant further investigation of oregano extract for its potential to prevent and ameliorate metabolic syndrome and its complications.
Mueller
Monika
M
Christian Doppler Laboratory for Receptor Biotechnology, Department of Biotechnology, University of Natural Resources and Applied Life Sciences, Vienna, Austria.
Lukas
Brigitte
B
Novak
Johannes
J
Simoncini
Tommaso
T
Genazzani
Andrea Riccardo
AR
Jungbauer
Alois
A
D000818:Animals; D002478:Cells, Cultured; D042783:Endothelial Cells / Q000187:drug effects / Q000378:metabolism; D006801:Humans; D051379:Mice; D041681:NIH 3T3 Cells; D019001:Nitric Oxide Synthase / Q000378:metabolism; D031341:Origanum / Q000737:chemistry*; D047495:PPAR gamma / Q000037:antagonists & inhibitors* / Q000378:metabolism; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology*
D047495:PPAR gamma; D010936:Plant Extracts; D019001:Nitric Oxide Synthase