3D organotypic HepaRG cultures as in vitro model for acute and repeated dose toxicity studies

Aninat, 2006, Expression of cytochromes P450, conjugating enzymes and nuclear receptors in human hepatoma HepaRG cells, Drug Metab. Dispos., 34, 75, 10.1124/dmd.105.006759 Antherieu, 2012, Oxidative stress plays a major role in chlorpromazine-induced cholestasis in human HepaRG cells, Hepatology Argikar, 2009, Effect of aging on glucuronidation of valproic acid in human liver microsomes and the role of UDP-glucuronosyltransferase UGT1A4, UGT1A8, and UGT1A10, Drug Metab. Dispos., 37, 229, 10.1124/dmd.108.022426 Baillie, 1992, Metabolism of valproate to hepatotoxic intermediates, Pharm. Weekblad Sci., 14, 122, 10.1007/BF01962701 Bedard, 2006, Aflatoxin B1-induced DNA damage and its repair, Cancer Lett., 241, 174, 10.1016/j.canlet.2005.11.018 Biagini, 2006, Investigation of the hepatotoxicity profile of chemical entities using liverbeads and WIF-B9 in vitro models, Toxicol. In Vitro, 20, 1051, 10.1016/j.tiv.2006.01.013 Broeders, 2013, In vitro biokinetics of chlorpromazine and the influence of different dose metrics on effect concentrations for cytotoxicity in Balb/c 3T3, Caco-2 and HepaRG cell cultures, Toxicol. In Vitro, 27, 1057, 10.1016/j.tiv.2013.01.010 Chaumontet, 1998, The polarized hepatic human/rat hybrid WIF 12-1 and WIF-B cells communicate efficiently in vitro via connexin 32-constituted gap junctions, Hepatology, 28, 164, 10.1002/hep.510280122 Corcuera, 2012, An approach to the toxicity and toxicokinetics of aflatoxin B1 and ochratoxin A after simultaneous oral administration to fasted F344 rats, Food Chem. Toxicol., 10.1016/j.fct.2012.06.048 Darnell, 2011, Cytochrome P450-dependent metabolism in HepaRG cells cultured in a dynamic three-dimensional bioreactor, Drug Metab. Dispos., 39, 1131, 10.1124/dmd.110.037721 Darnell, 2012, In vitro evaluation of major in vivo drug metabolic pathways using primary human hepatocytes and HepaRG cells in suspension and in a dynamic three-dimensional bioreactor system, J. Pharm. Exp. Ther., 10.1124/jpet.112.195834 Drewitz, 2011, Towards automated production and drug sensitivity testing using scaffold-free spherical tumor microtissues, Biotechnol. J., 6, 1488, 10.1002/biot.201100290 Eadie, 1988, Valproate-associated hepatotoxicity and its biochemical mechanisms, Med. Toxicol. Adverse Drug Exp., 3, 85, 10.1007/BF03259935 Fey, 2012, Determination of drug toxicity using 3D spheroids constructed from an immortal human hepatocyte cell line, Toxicol. Sci., 127, 403, 10.1093/toxsci/kfs122 Gerlach, 2003, Use of primary human liver cells originating from discarded grafts in a bioreactor for liver support therapy and the prospects of culturing adult liver stem cells in bioreactors: a morphologic study, Transplantation, 76, 781, 10.1097/01.TP.0000083319.36931.32 Godoy, 2009, Extracellular matrix modulates sensitivity of hepatocytes to fibroblastoid dedifferentiation and transforming growth factor beta-induced apoptosis, Hepatology, 49, 2031, 10.1002/hep.22880 Golli-Bennour, 2012, Cytotoxicity effects of amiodarone on cultured cells, Exp. Toxicol. Pathol., 64, 425, 10.1016/j.etp.2010.10.008 Gomez-Lechon, 2003, Human hepatocytes as a tool for studying toxicity and drug metabolism, Curr. Drug Metab., 4, 292, 10.2174/1389200033489424 Gripon, 2002, Infection of a human hepatoma cell line by hepatitis B virus, Proc. Natl. Acad. Sci. USA, 99, 15655, 10.1073/pnas.232137699 Guengerich, 2011, Mechanisms of drug toxicity and relevance to pharmaceutical development, Drug Metab. Pharm., 26, 3, 10.2133/dmpk.DMPK-10-RV-062 Guillouzo, 1998, Liver cell models in in vitro toxicology, Environ. Health Perspect., 106, 511, 10.1289/ehp.98106511 Guillouzo, 2007, The human hepatoma HepaRG cells: a highly differentiated model for studies of liver metabolism and toxicity of xenobiotics, Chem. Biol. Interact., 168, 66, 10.1016/j.cbi.2006.12.003 Gunness, 2013, 3D organotypic cultures of human HepaRG cells: a tool for in vitro toxicity studies, Toxicol. Sci., 10.1093/toxsci/kft021 Haouzi, 2005, Three-dimensional polarization sensitizes hepatocytes to Fas/CD95 apoptotic signalling, J. Cell Sci., 118, 2763, 10.1242/jcs.02403 Hobbs, 1998, Regulation of transport pathways in tumor vessels: role of tumor type and microenvironment, Proc. Natl. Acad. Sci. USA, 95, 4607, 10.1073/pnas.95.8.4607 Hoekstra, 2011, The HepaRG cell line is suitable for bioartificial liver application, Int. J. Biochem. Cell Biol., 43, 1483, 10.1016/j.biocel.2011.06.011 Horning, 2008, 3-D tumor model for in vitro evaluation of anticancer drugs, Mol. Pharm., 5, 849, 10.1021/mp800047v Kanebratt, 2008, Evaluation of HepaRG cells as an in vitro model for human drug metabolism studies, Drug Metab. Dispos., 36, 1444, 10.1124/dmd.107.020016 Kashima, 2005, Pharmacokinetic characteristics of amiodarone in long-term oral therapy in Japanese population, Biol. Pharm. Bull., 28, 1934, 10.1248/bpb.28.1934 Kelm, 2004, Microscale tissue engineering using gravity-enforced cell assembly, Trends Biotechnol., 22, 195, 10.1016/j.tibtech.2004.02.002 Kelm, 2003, Method for generation of homogeneous multicellular tumor spheroids applicable to a wide variety of cell types, Biotechnol. Bioeng., 83, 173, 10.1002/bit.10655 Klein, 2012, Isotope labeling experiments in metabolomics and fluxomics, Wiley Interdiscip. Rev. Syst. Biol. Med., 4, 261, 10.1002/wsbm.1167 Kono, 1996, Modulation of the expression of liver-specific functions in novel human hepatocyte lines cultured in a collagen gel sandwich configuration, Biochem. Biophys. Res. Commun., 220, 628, 10.1006/bbrc.1996.0454 Kramer, 2012, Quantifying processes determining the free concentration of phenanthrene in Basal cytotoxicity assays, Chem. Res. Toxicol., 25, 436, 10.1021/tx200479k Larrey, 1997, Genetic predisposition to drug-induced hepatotoxicity, J. Hepatol., 26, 12, 10.1016/S0168-8278(97)80492-8 Latini, 1984, Clinical pharmacokinetics of amiodarone, Clin. Pharmacokinet., 9, 136, 10.2165/00003088-198409020-00002 Le Vee, 2006, Functional expression of sinusoidal and canalicular hepatic drug transporters in the differentiated human hepatoma HepaRG cell line, Eur. J. Pharm. Sci., 28, 109, 10.1016/j.ejps.2006.01.004 Leite, 2012, 3D HepaRG model as an attractive tool for toxicity testing, Toxicol. Sci., 10.1093/toxsci/kfs232 Li, 2012, Chem. Biol. Interact., 199, 1, 10.1016/j.cbi.2012.05.003 Limonciel, 2011, Lactate is an ideal non-invasive marker for evaluating temporal alterations in cell stress and toxicity in repeat dose testing regimes, Toxicol. In Vitro, 25, 1855, 10.1016/j.tiv.2011.05.018 Lubberstedt, 2011, HepaRG human hepatic cell line utility as a surrogate for primary human hepatocytes in drug metabolism assessment in vitro, J. Pharmacol. Toxicol. Methods, 63, 59, 10.1016/j.vascn.2010.04.013 Mandenius, 2011, Toward preclinical predictive drug testing for metabolism and hepatotoxicity by using in vitro models derived from human embryonic stem cells and human cell lines – a report on the Vitrocellomics EU-project, Altern. Lab. Anim., 39, 147, 10.1177/026119291103900210 Mandenius, 2011, Cardiotoxicity testing using pluripotent stem cell-derived human cardiomyocytes and state-of-the-art bioanalytics: a review, J. Appl. Toxicol., 31, 191, 10.1002/jat.1663 McGill, 2011, HepaRG cells: a human model to study mechanisms of acetaminophen hepatotoxicity, Hepatology, 53, 974, 10.1002/hep.24132 McLean, 1995, Cellular interactions and metabolism of aflatoxin: an update, Pharmacol. Ther., 65, 163, 10.1016/0163-7258(94)00054-7 Mueller, 2011, Organotypic cultures of HepG2 cells for in vitro toxicity studies, J. Bioeng. Biomed. Sci. S, 2, 002 Mueller, 2011, In-depth physiological characterization of primary human hepatocytes in a 3D hollow-fiber bioreactor, J. Tissue Eng. Regen. Med., 5, e207, 10.1002/term.418 Mueller, 2012, Real-time in situ viability assessment in a 3D bioreactor with liver cells using resazurin assay, Cytotechnology Narayanan, 2002, Differential gene expression analysis during porcine hepatocyte spheroid formation, Mamm. Genome, 13, 515, 10.1007/s00335-002-2179-2 Nibourg, 2012, Perfusion flow rate substantially contributes to the performance of the HepaRG-AMC-bioartificial liver, Biotechnol. Bioeng., 10.1002/bit.24586 Nibourg, 2012, Liver progenitor cell line HepaRG Differentiated in a bioartificial liver effectively supplies liver support to rats with acute liver failure, PLoS One, 7, e38778, 10.1371/journal.pone.0038778 Niklas, 2009, Effects of drugs in subtoxic concentrations on the metabolic fluxes in human hepatoma cell line Hep G2, Toxicol. Appl. Pharmacol., 240, 327, 10.1016/j.taap.2009.07.005 Ohyama, 2000, A significant role of human cytochrome P450 2C8 in amiodarone N-deethylation: an approach to predict the contribution with relative activity factor, Drug Metab. Dispos., 28, 1303 Padda, 2012, Drug-induced cholestasis, Hepatology, 53, 1377, 10.1002/hep.24229 Park, 1995, The role of cytochrome P450 enzymes in hepatic and extrahepatic human drug toxicity, Pharmacol. Ther., 68, 385, 10.1016/0163-7258(95)02013-6 Powell-Jackson, 1984, Hepatotoxicity to sodium valproate: a review, Gut, 25, 673, 10.1136/gut.25.6.673 Samanez, 2012, The human hepatocyte cell lines IHH and HepaRG: models to study glucose, lipid and lipoprotein metabolism, Arch. Physiol. Biochem., 118, 102, 10.3109/13813455.2012.683442 Sauer, 2003, Clinical extracorporeal hybrid liver support-phase I study with primary porcine liver cells, Xenotransplantation, 10, 460, 10.1034/j.1399-3089.2003.00062.x Schuster, 2005, Why drugs fail – a study on side effects in new chemical entities, Curr. Pharm. Des., 11, 3545, 10.2174/138161205774414510 Spaniol, 2001, Toxicity of amiodarone and amiodarone analogues on isolated rat liver mitochondria, J. Hepatol., 35, 628, 10.1016/S0168-8278(01)00189-1 van de Kerkhove, 2003, Bridging a patient with acute liver failure to liver transplantation by the AMC-bioartificial liver, Cell Transplant., 12, 563, 10.3727/000000003108747163 Waldhauser, 2006, Hepatocellular toxicity and pharmacological effect of amiodarone and amiodarone derivatives, J. Pharmacol. Exp. Ther., 319, 1413, 10.1124/jpet.106.108993 Waldhauser, 2008, Interaction with the hERG channel and cytotoxicity of amiodarone and amiodarone analogues, Brit. J. Pharmacol., 155, 585, 10.1038/bjp.2008.287 Wen, 2009, Metabolic activation of the phenothiazine antipsychotics chlorpromazine and thioridazine to electrophilic iminoquinone species in human liver microsomes and recombinant P450s, Chem. Biol. Interact., 181, 220, 10.1016/j.cbi.2009.05.014 Winter, 2007, Open-label steady-state pharmacokinetic drug interaction study on co-administered quetiapine fumarate and divalproex sodium in patients with schizophrenia, schizoaffective disorder, or bipolar disorder, Hum. Psychopharmacol., 22, 469, 10.1002/hup.869 Yuan, 1995, Vascular permeability in a human tumor xenograft: molecular size dependence and cutoff size, Cancer Res., 55, 3752