Planta Med 2009; 75 - PE38
DOI: 10.1055/s-0029-1234599

Uptake of xanthohumol in human liver and intestinal cells

M Motyl 1, C Dorn 2, C Hellerbrand 2, J Heilmann 1, B Kraus 1
  • 1Pharmaceutical Biology, Institute of Pharmacy, University of Regensburg, 93042 Regensburg, Germany
  • 2Department of Internal Medicine I, University of Regensburg, 93042 Regensburg, Germany

Humulus lupulus L. (hops) has long been used in traditional medicine with sleep disturbances being the main indication. However, scientific evidence has accumulated over the past years pointing to the cancer preventive potential of selected constituents, i.e. xanthohumol (XN), a prenylated chalcone. The mechanisms of protection by XN have been proposed to be inhibition of metabolic activation, induction of detoxifying enzymes and antioxidant activity [1]. Moreover a broad antiinfective potential of XN is described [2]. Despite many advances in understanding the pharmacology of XN, one largely unresolved issue is the low bioavailability of XN in the human organism. Also little is known about actual concentrations and pharmacokinetic of the compound and its metabolites in liver and intestinal cells.

We studied the cellular uptake of xanthohumol (XN) in various cell lines, namely hepato cellular carcinoma cells (Huh-7), hepatic stellate cells (HSZ-B) and colorectal adenocarcinoma cells (Caco-2), as well as in primary hepatocytes. Uptake and intracellular distribution of fluorescent XN was analysed using advanced fluorescence imaging techniques. XN concentrations, determined via reversed-phase high-performance liquid chromatography (HPLC), and cell volumes, obtained using 3D-Imaging, were combined for the estimation of inner cell concentrations.

We observed a very rapid accumulation of XN, reaching a maximum already after 30–60min. Furthermore we found that HSZ-B and Caco-2 cells showed a much higher XN uptake than Huh-7 cells. In addition different XN metabolites were identified. Our data provide deeper insights into XN biology on the cell level and will contribute to a better understanding of its pharmacology.

Acknowledgements: We thank Dr. Thomas Weiss, Center for Liver Cell Research, Department of Surgery, University of Regensburg, Germany, for providing primary hepatocytes.

References: [1] Zanoli, P. et al. (2008)J. Ethnopharmacol. 116:383–396.

[2] Gerhäuser, C. (2005) Mol. Nutr. Food Res. 49:827–831.