Determination of cyanidin 3-glucoside in rat brain, liver and kidneys by UPLC/MS-MS and its application to a short-term pharmacokinetic study

• DOI: 10.1038/srep22815
• Publication Date: 2016-03-11T10:03:56Z
• Authors: Stefano Fornasaro; Lovro Ziberna; Mattia Gasperotti; Federica Tramer; Urška Vrhovšek; Fulvio Mattivi; Sabina Passamonti
• Keywords: Animals; Anthocyanins; Biological Availability; Brain; Chromatography, High Pressure Liquid; Glucosides; Kidney; Liver; Male; Molecular Structure; Rats; Tandem Mass Spectrometry; Tissue Distribution; Multidisciplinary; Male; Settore CHIM/01 - CHIMICA ANALITICA; 570; Cyanidin 3-glucoside; Tandem mass spectrometry; 610; Biological Availability; Metabolomic; Cianidina 3-glucoside; UPLC/MS-MS; Kidney; Article; Anthocyanins; 03 medical and health sciences; Farmacocinetica; Glucosides; Tandem Mass Spectrometry; UHPLC; Animals; Pharmacokinetics; flavonoid; Tissue Distribution; pharmacokinetic; Chromatography, High Pressure Liquid; Metabolomics; C3G; pharmacokinetics; UPLC/MS-MS; Blood-brain barrier; flavonoids; anthocyanins; Blood-brain barrier; Spettrometria di massa triplo quadrupolo; 0303 health sciences; Molecular Structure; Brain; C3G; anthocyanins; Rats; Antociani; Liver

AbstractAnthocyanins exert neuroprotection in various in vitro and in vivo experimental models. However, no details regarding their brain-related pharmacokinetics are so far available to support claims about their direct neuronal bioactivity as well as to design proper formulations of anthocyanin-based products. To gather this missing piece of knowledge, we intravenously administered a bolus of 668 nmol cyanidin 3-glucoside (C3G) in anaesthetized Wistar rats and shortly after (15 s to 20 min) we collected blood, brain, liver, kidneys and urine samples. Extracts thereof were analysed for C3G and its expected metabolites using UPLC/MS-MS. The data enabled to calculate a set of pharmacokinetics parameters. The main finding was the distinctive, rapid distribution of C3G in the brain, with an apparently constant plasma/brain ratio in the physiologically relevant plasma concentration range (19–355 nM). This is the first report that accurately determines the distribution pattern of C3G in the brain, paving the way to the rational design of future tests of neuroprotection by C3G in animal models and humans.