title: Pharmacokinetics and tissue distribution of pterostilbene in the rat.
abstract: METHODS
  Pterostilbene (Pt) is emerging as an important health-promoting natural compound. Pharmacokinetic studies so far have focused on plasma levels, while Pt distribution in tissues is most relevant for biological action. This study determined tissue distribution of Pt and its major metabolite, pterostilbene-4'-sulfate (Pt-S), in rats after oral administration.
  
  
  RESULTS
  Upon intravenous (iv) administration (88 μmol/kg), Pt was cleared from blood with a half-life of 1.8 ± 0.3 h. Oral administration (same dose) resulted in moderate Pt bioavailability (∼35%) and in an increased abundance of Pt-S in blood (AUC(Pt)/AUC(Pt-S) ∼0.75 and ∼0.05 after iv or oral administration, respectively). Pt-S was the major species in all organs except the brain, where intact Pt was predominant (AUC(Pt)/AUC(Pt-S) ∼5). Both Pt and Pt-S peaked in all tissues at approximately 2 h. The highest levels (∼200 nmoles/g for Pt-S and 40 nmoles/g for Pt) were measured in the liver, the lowest (≤7 nmol/g) in skeletal muscles and testes.
  
  
  CONCLUSIONS
  AUC(Pt) was ∼2- to ∼25-fold higher in tissues than in blood; this may explain its bioactivity despite barely detectable blood levels. Of particular interest is the high fraction of nonmetabolized Pt in the brain, given the reports of its activity at the level of the central nervous system.
authors.affiliation: Department of Biomedical Sciences, University of Padova, Padova, Italy.
authors.forename: Michele
authors.initials: M
authors.lastname: Azzolini
authors.forename: Martina
authors.initials: M
authors.lastname: La Spina
authors.forename: Andrea
authors.initials: A
authors.lastname: Mattarei
authors.forename: Cristina
authors.initials: C
authors.lastname: Paradisi
authors.forename: Mario
authors.initials: M
authors.lastname: Zoratti
authors.forename: Lucia
authors.initials: L
authors.lastname: Biasutto
mesh_terms: D061605:Administration, Intravenous; D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D002138:Calibration; D002851:Chromatography, High Pressure Liquid; D004305:Dose-Response Relationship, Drug; D006207:Half-Life; D008099:Liver / Q000187:drug effects / Q000378:metabolism; D008297:Male; D051381:Rats; D017208:Rats, Wistar; D013267:Stilbenes / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D014018:Tissue Distribution
chemical_list: D013267:Stilbenes; C107773:pterostilbene
keywords: Area under the curve; LC; Pharmacokinetics; Pterostilbene; Tissue distribution