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Evaluation of PPARα activation by known blueberry constituents

Agnes M Rimando, Shabana I Khan, Cassia S Mizuno, Guang Ren, Suresh T Mathews, Hyunsook Kim, Wallace Yokoyama
Journal of the science of food and agriculture 2016 v.96 no.5 pp. 1666-1671
epicatechin, hamsters, pterostilbene, hepatoma, fenofibrate, low density lipoprotein cholesterol, luciferase, benzophenones, correlation, dose response, molecular models, gene expression, amino acids, gene expression regulation, anthocyanins, transcription factors, messenger RNA, pomace, rats, resveratrol, catechin, diet, liver, ligands, chenodeoxycholic acid, agonists, blueberries
BACKGROUND: Anthocyanins are known to have hypolipidemic properties. It was deemed necessary to determine whether major blueberry anthocyanins and catechins are ligands for the transcription factor peroxisome proliferator activated receptor alpha isoform (PPARα), and compare activation with known PPARα agonistic constituents, pterostilbene and resveratrol. It was also considered important to investigate the effect of pterostilbene on PPARα gene expression, and relate results with hepatic mRNA PPARα expression up‐regulation observed previously in hamsters fed a diet supplemented with blueberry peels extract (BBX). RESULTS: The anthocyanins and catechins did not activate PPARα. Only pterostilbene exhibited a dose‐dependent activation of PPARα in H4IIEC3 cells. The resveratrol responses were lower than those of pterostilbene. Pterostilbene significantly and dose‐dependently (at 10, 20 and 50 µmol L⁻¹) increased PPARα gene expression and the effect at 10 µmol L⁻¹ was greater than 100 and 200 µmol L⁻¹ of fenofibrate. Analysis of BBX showed levels of pterostilbene and resveratrol at 418 and 2381 ng g⁻¹, respectively. CONCLUSION: Anthocyanins and catechins do not appear to contribute to the up‐regulation of hepatic PPARα expression observed in hamsters. While pterostilbene and resveratrol demonstrated PPARα activation, their levels in BBX do not seem to be at efficacious concentrations. These stilbenes may contribute to the up‐regulation of PPARα expression by acting synergistically with each other or with other constituents in BBX. © 2015 Society of Chemical Industry