title: Determination of cyanidin 3-glucoside in rat brain, liver and kidneys by UPLC/MS-MS and its application to a short-term pharmacokinetic study.
abstract: Anthocyanins 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.
authors.affiliation: University of Trieste, Department of Life Sciences, via L. Giorgieri 1, 34127 Trieste, Italy.
authors.forename: Stefano
authors.initials: S
authors.lastname: Fornasaro
authors.affiliation: University of Trieste, Department of Life Sciences, via L. Giorgieri 1, 34127 Trieste, Italy.
authors.forename: Lovro
authors.initials: L
authors.lastname: Ziberna
authors.affiliation: Fondazione Edmund Mach (FEM), Department of Food Quality and Nutrition, Research and Innovation Centre, via E. Mach 1, 38010 San Michele all'Adige, Italy.
authors.forename: Mattia
authors.initials: M
authors.lastname: Gasperotti
authors.affiliation: University of Trieste, Department of Life Sciences, via L. Giorgieri 1, 34127 Trieste, Italy.
authors.forename: Federica
authors.initials: F
authors.lastname: Tramer
authors.affiliation: Fondazione Edmund Mach (FEM), Department of Food Quality and Nutrition, Research and Innovation Centre, via E. Mach 1, 38010 San Michele all'Adige, Italy.
authors.forename: Urška
authors.initials: U
authors.lastname: Vrhovšek
authors.affiliation: Fondazione Edmund Mach (FEM), Department of Food Quality and Nutrition, Research and Innovation Centre, via E. Mach 1, 38010 San Michele all'Adige, Italy.
authors.forename: Fulvio
authors.initials: F
authors.lastname: Mattivi
authors.affiliation: University of Trieste, Department of Life Sciences, via L. Giorgieri 1, 34127 Trieste, Italy.
authors.forename: Sabina
authors.initials: S
authors.lastname: Passamonti
mesh_terms: D000818:Animals; D000872:Anthocyanins / Q000008:administration & dosage / Q000737:chemistry / Q000378:metabolism* / Q000493:pharmacokinetics*; D001682:Biological Availability; D001921:Brain / Q000378:metabolism*; D002851:Chromatography, High Pressure Liquid; D005960:Glucosides / Q000008:administration & dosage / Q000737:chemistry / Q000378:metabolism* / Q000493:pharmacokinetics*; D007668:Kidney / Q000378:metabolism*; D008099:Liver / Q000378:metabolism*; D008297:Male; D015394:Molecular Structure; D051381:Rats; D053719:Tandem Mass Spectrometry; D014018:Tissue Distribution
chemical_list: D000872:Anthocyanins; D005960:Glucosides; C462279:cyanidin-3-O-beta-glucopyranoside