title: Evaluation of PPARα activation by known blueberry constituents.
abstract: 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.
  
  
  CONCLUSIONS
  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.
authors.affiliation: U.S. Department of Agriculture, Agricultural Research Service, Natural Products Utilization Research Unit, University, MS, 38677, USA.
authors.forename: Agnes M
authors.initials: AM
authors.lastname: Rimando
authors.affiliation: University of Mississippi, National Center for Natural Products Research, School of Pharmacy, University of Mississippi, University, MS, 38677, USA.
authors.forename: Shabana I
authors.initials: SI
authors.lastname: Khan
authors.affiliation: U.S. Department of Agriculture, Agricultural Research Service, Natural Products Utilization Research Unit, University, MS, 38677, USA.
authors.forename: Cassia S
authors.initials: CS
authors.lastname: Mizuno
authors.affiliation: Auburn University, Department of Nutrition, Dietetics and Hospitality Management, 260 Lem Morrison Drive, Auburn, AL, 36849, USA.
authors.forename: Guang
authors.initials: G
authors.lastname: Ren
authors.affiliation: Auburn University, Department of Nutrition, Dietetics and Hospitality Management, 260 Lem Morrison Drive, Auburn, AL, 36849, USA.
authors.forename: Suresh T
authors.initials: ST
authors.lastname: Mathews
authors.affiliation: U.S. Department of Agriculture, Agricultural Research Service, Western Regional Research Center, 800 Buchanan St, Albany, CA, 94710, USA.
authors.forename: Hyunsook
authors.initials: H
authors.lastname: Kim
authors.affiliation: U.S. Department of Agriculture, Agricultural Research Service, Western Regional Research Center, 800 Buchanan St, Albany, CA, 94710, USA.
authors.forename: Wallace
authors.initials: W
authors.lastname: Yokoyama
mesh_terms: D000818:Animals; D000872:Anthocyanins / Q000737:chemistry / Q000494:pharmacology*; D029798:Blueberry Plants / Q000737:chemistry*; D002392:Catechin / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology*; D002460:Cell Line; D006224:Cricetinae; D006801:Humans; D047493:PPAR alpha / Q000378:metabolism*; D011485:Protein Binding; D000077185:Resveratrol; D013267:Stilbenes / Q000494:pharmacology
chemical_list: D000872:Anthocyanins; D047493:PPAR alpha; D013267:Stilbenes; D002392:Catechin; D000077185:Resveratrol
keywords: PPARα; anthocyanin; blueberry; catechin; pterostilbene; resveratrol