title: Xanthohumol uptake and intracellular kinetics in hepatocytes, hepatic stellate cells, and intestinal cells.
abstract: Xanthohumol (XN) is the major prenylated chalcone of hops and hence an ingredient of beer. Despite many advances in understanding of the pharmacology of XN, one largely unresolved issue is its low bioavailability in the human organism. Also, not much is known about its actual concentrations and pharmacokinetics in liver and intestinal cells. Therefore, the uptake, intracellular distribution, and kinetics of XN were studied in various cell types, namely, hepatocellular carcinoma cells (HuH-7), hepatic stellate cells (HSC), primary cultured hepatocytes, and colorectal adenocarcinoma cells (Caco-2). Fluorescent microscopy allowed for the first time visualization and tracing of the uptake and intracellular distribution of XN. A rapid accumulation of XN concentrations that were up to >60-fold higher than the concentration present in the ambient culture medium was observed. Fluorescence recovery after photobleaching experiments revealed that most XN molecules are bound to cellular proteins, which may alter properties of cellular factors.
authors.affiliation: Institute of Virology, Helmholtz Zentrum München - German Research Center for Environmental Health, Ingolstädter Landstrasse 1, Neuherberg, Germany.
authors.forename: Horst
authors.initials: H
authors.lastname: Wolff
authors.forename: Magdalena
authors.initials: M
authors.lastname: Motyl
authors.forename: Claus
authors.initials: C
authors.lastname: Hellerbrand
authors.forename: Jörg
authors.initials: J
authors.lastname: Heilmann
authors.forename: Birgit
authors.initials: B
authors.lastname: Kraus
mesh_terms: D001682:Biological Availability; D018938:Caco-2 Cells; D006528:Carcinoma, Hepatocellular; D045744:Cell Line, Tumor; D002478:Cells, Cultured; D005419:Flavonoids / Q000493:pharmacokinetics*; D055166:Hepatic Stellate Cells / Q000378:metabolism*; D022781:Hepatocytes / Q000378:metabolism*; D006801:Humans; D027582:Humulus / Q000737:chemistry; D007413:Intestinal Mucosa / Q000378:metabolism*; D007700:Kinetics; D008113:Liver Neoplasms; D011427:Propiophenones / Q000493:pharmacokinetics*
chemical_list: D005419:Flavonoids; D011427:Propiophenones; C104536:xanthohumol