Pharmacokinetics and tissue distribution of pterostilbene in the rat. Issue 11 (22nd August 2014)

• Record Type: Journal Article
• Authors: Azzolini, Michele; La Spina, Martina; Mattarei, Andrea; Paradisi, Cristina; Zoratti, Mario; Biasutto, Lucia
• Is Part Of: Molecular nutrition & food research. Volume 58:Issue 11(2014:Nov.)
• Page Start: 2122
• Page End: 2132
• Publication Date: 2014-08-22
• Subjects: Food -- Biotechnology -- Periodicals; Food -- Microbiology -- Periodicals; Nutrition -- Periodicals; Food -- Toxicology -- Periodicals; Nutrition -- Periodicals; Food Microbiology -- Periodicals; Food Technology -- Periodicals; Molecular Biology -- Periodicals; 664.0705
• DOI: 10.1002/mnfr.201400244
• Languages: English
• ISSNs: 1613-4125

Abstract

<abstract abstract-type="main"> <title> <x xml:space="preserve">Abstract</x> </title> <sec id="mnfr2248-sec-0010" sec-type="section"> <title>Scope</title> <p>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.</p> </sec> <sec id="mnfr2248-sec-0020" sec-type="section"> <title>Methods and results</title> <p>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<sub>Pt</sub>/AUC<sub>Pt‐S</sub> ∼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<sub>Pt</sub>/AUC<sub>Pt‐S</sub> ∼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.</p> </sec> <sec id="mnfr2248-sec-0030" sec-type="section"> <title>Conclusion</title> <p>AUC<sub>Pt</sub> 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.</p> </sec> </abstract>