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Opportunities and challenges in using human hepatocytes in cytochromes P450 induction assays

Pages 169-174 | Received 23 Sep 2015, Accepted 25 Nov 2015, Published online: 08 Jan 2016

References

  • Papers of special note have been highlighted as either “of interest” (●) or “of considerable interest” (●●) to readers.
  • Tian D, Hu Z. CYP3A4-mediated pharmacokinetic interactions in cancer therapy. Curr Drug Metab. 2014;15:808–817.
  • Sevrioukova IF, Poulos TL. Current approaches for investigating and predicting cytochrome P450 3A4-ligand interactions. Adv Exp Med Biol. 2015;851:83–105.
  • Sinz MW. Evaluation of pregnane X receptor (PXR)-mediated CYP3A4 drug-drug interactions in drug development. Drug Metab Rev. 2013;45:3–14.
  • Matoulkova P, Pavek P, Maly J, et al. Cytochrome P450 enzyme regulation by glucocorticoids and consequences in terms of drug interaction. Expert Opin Drug Metab Toxicol. 2014;10:425–435.
  • Pavek P, Dvorak Z. Xenobiotic-induced transcriptional regulation of xenobiotic metabolizing enzymes of the cytochrome P450 superfamily in human extrahepatic tissues. Curr Drug Metab. 2008;9:129–143.
  • Moreau A, Vilarem MJ, Maurel P, et al. Xenoreceptors CAR and PXR activation and consequences on lipid metabolism, glucose homeostasis, and inflammatory response. Mol Pharm. 2008;5:35–41.
  • Pascussi JM, Gerbal-Chaloin S, Duret C, et al. The tangle of nuclear receptors that controls xenobiotic metabolism and transport: crosstalk and consequences. Annu Rev Pharmacol Toxicol. 2008;48:1–32.

• Shows mutual relationships between xenobiotics and endobiotics cell signaling

  • Hewitt NJ, Lechon MJ, Houston JB, et al. Primary hepatocytes: current understanding of the regulation of metabolic enzymes and transporter proteins, and pharmaceutical practice for the use of hepatocytes in metabolism, enzyme induction, transporter, clearance, and hepatotoxicity studies. Drug Metab Rev. 2007;39:159–234.
  • Lloyd TD, Orr S, Dennison AR. A survey of consumer attitudes to the supply and use of human hepatocytes in the United Kingdom. Altern Lab Anim. 2003;31:483–488.
  • Yajima K, Uno Y, Murayama N, et al. Evaluation of 23 lots of commercially available cryopreserved hepatocytes for induction assays of human cytochromes P450. Drug Metab Dispos. 2014;42:867–871.
  • Kamiguchi N, Aoyama E, Okuda T, et al. A 96-well plate assay for CYP4503A induction using cryopreserved human hepatocytes. Drug Metab Dispos. 2010;38:1912–1916.
  • Duret C, Moreno D, Anangi B, et al. Cold-preservation of human adult hepatocytes for liver cell therapy. Cell Transplant. 2015.
  • Ferrini JB, Pichard L, Domergue J, et al. Long-term primary cultures of adult human hepatocytes. Chem Biol Interact. 1997;107:31–45.

• Describes experimental conditions allowing HHs culture in long time

  • Kono Y, Yang S, Roberts EA. Extended primary culture of human hepatocytes in a collagen gel sandwich system. In Vitro Cell Dev Biol Anim. 1997;33:467–472.
  • Badolo L, Jensen B, Sall C, et al. Evaluation of 309 molecules as inducers of CYP3A4, CYP2B6, CYP1A2, OATP1B1, OCT1, MDR1, MRP2, MRP3 and BCRP in cryopreserved human hepatocytes in sandwich culture. Xenobiotica. 2015;45:177–187.
  • Xia L, Hong X, Sakban RB, et al. Cytochrome P450 induction response in tethered spheroids as a three-dimensional human hepatocyte in vitro model. J Appl Toxicol. 2015.
  • Gross-Steinmeyer K, Stapleton PL, Tracy JH, et al. Influence of Matrigel-overlay on constitutive and inducible expression of nine genes encoding drug-metabolizing enzymes in primary human hepatocytes. Xenobiotica. 2005;35:419–438.
  • Vinci B, Duret C, Klieber S, et al. Modular bioreactor for primary human hepatocyte culture: medium flow stimulates expression and activity of detoxification genes. Biotechnol J. 2011;6:554–564.
  • Ramboer E, De Craene B, De Kock J, et al. Strategies for immortalization of primary hepatocytes. J Hepatol. 2014;61:925–943.
  • Hariparsad N, Carr BA, Evers R, et al. Comparison of immortalized Fa2N-4 cells and human hepatocytes as in vitro models for cytochrome P450 induction. Drug Metab Dispos. 2008;36:1046–1055.
  • Walldorf J, Aurich H, Cai H, et al. Expanding hepatocytes in vitro before cell transplantation: donor age-dependent proliferative capacity of cultured human hepatocytes. Scand J Gastroenterol. 2004;39:584–593.
  • Yoon JH, Gwak GY, Woo GH, et al. Augmentation of butyrate-induced differentiation of human hepatocyte by cyclin E over-expression. Int J Artif Organs. 2005;28:44–50.
  • Deurholt T, Ten Bloemendaal L, Chhatta AA, et al. In vitro functionality of human fetal liver cells and clonal derivatives under proliferative conditions. Cell Transplant. 2006;15:811–822.
  • Duret C, Gerbal-Chaloin S, Ramos J, et al. Isolation, characterization, and differentiation to hepatocyte-like cells of nonparenchymal epithelial cells from adult human liver. Stem Cells. 2007;25:1779–1790.
  • Gerbal-Chaloin S, Duret C, Raulet E, et al. Isolation and culture of adult human liver progenitor cells: in vitro differentiation to hepatocyte-like cells. Hepatocytes Methods Protoc. 2010;640:247–260.
  • Song ZH, Cai J, Liu YX, et al. Efficient generation of hepatocyte-like cells from human induced pluripotent stem cells. Cell Research. 2009;19:1233–1242.
  • Si-Tayeb K, Noto FK, Nagaoka M, et al. Highly efficient generation of human hepatocyte-like cells from induced pluripotent stem cells. Hepatology. 2010;51:297, 1094.
  • Ulvestad M, Nordell P, Asplund A, et al. Drug metabolizing enzyme and transporter protein profiles of hepatocytes derived from human embryonic and induced pluripotent stem cells. Biochem Pharmacol. 2013;86:691–702.
  • Medine CN, Lucendo-Villarin B, Storck C, et al. Developing high-fidelity hepatotoxicity models from pluripotent stem cells. Stem Cells Transl Med. 2013;2:505–509.
  • Holmgren G, Sjogren AK, Barragan I, et al. Long-term chronic toxicity testing using human pluripotent stem cell-derived hepatocytes. Drug Metab Dispos. 2014;42:1401–1406.
  • Szkolnicka D, Farnworth SL, Lucendo-Villarin B, et al. Accurate prediction of drug-induced liver injury using stem cell-derived populations. Stem Cells Transl Med. 2014;3:141–148.
  • Kondo Y, Iwao T, Nakamura K, et al. An efficient method for differentiation of human induced pluripotent stem cells into hepatocyte-like cells retaining drug metabolizing activity. Drug Metab Pharmacokinet. 2014;29:237–243.
  • Takayama K, Morisaki Y, Kuno S, et al. Prediction of interindividual differences in hepatic functions and drug sensitivity by using human iPS-derived hepatocytes. Proc Natl Acad Sci USA. 2014;111:16772–16777.
  • Villarin BL, Cameron K, Szkolnicka D, et al. Polymer supported directed differentiation reveals a unique gene signature predicting stable hepatocyte performance. Adv Healthc Mater. 2015;4:1820–1825.
  • Parent R, Marion MJ, Furio L, et al. Origin and characterization of a human bipotent liver progenitor cell line. Gastroenterology. 2004;126:1147–1156.

•• The first report on HepaRG cells

  • Aninat C, Piton A, Glaise D, et al. Expression of cytochromes P450, conjugating enzymes and nuclear receptors in human hepatoma HepaRG cells. Drug Metab Dispos. 2006;34:75–83.
  • Kanebratt KP, Andersson TB. HepaRG cells as an in vitro model for evaluation of cytochrome p450 induction in humans. Drug Metab Dispos. 2008;36:137–145.
  • McGinnity DF, Zhang G, Kenny JR, et al. Evaluation of multiple in vitro systems for assessment of CYP3A4 induction in drug discovery: human hepatocytes, pregnane X receptor reporter gene, and Fa2N-4 and HepaRG cells. Drug Metab Dispos. 2009;37:1259–1268.
  • Yamasaki C, Kataoka M, Kato Y, et al. In vitro evaluation of cytochrome P450 and glucuronidation activities in hepatocytes isolated from liver-humanized mice. Drug Metab Pharmacokinet. 2010;25:539–550.
  • Kakuni M, Yamasaki C, Tachibana A, et al. Chimeric mice with humanized livers: a unique tool for in vivo and in vitro enzyme induction studies. Int J Mol Sci. 2014;15:58–74.
  • Ishida Y, Yamasaki C, Yanagi A, et al. Novel robust in vitro hepatitis B virus infection model using fresh human hepatocytes isolated from humanized mice. Am J Pathol. 2015;185:1275–1285.
  • Rogue A, Lambert C, Spire C, et al. Interindividual variability in gene expression profiles in human hepatocytes and comparison with HepaRG cells. Drug Metab Dispos. 2012;40:151–158.
  • Gomez-Lechon MJ, Castell JV, Donato MT. Hepatocytes--the choice to investigate drug metabolism and toxicity in man: in vitro variability as a reflection of in vivo. Chem Biol Interact. 2007;168:30–50.
  • Goyak KM, Johnson MC, Strom SC, et al. Expression profiling of interindividual variability following xenobiotic exposures in primary human hepatocyte cultures. Toxicol Appl Pharmacol. 2008;231:216–224.
  • Wilkening S, Stahl F, Bader A. Comparison of primary human hepatocytes and hepatoma cell line HEPG2 with regard to their biotransformation properties. Drug Metab Dispos. 2003;31:1035–1042.
  • Gerets HHJ, Tilmant K, Gerin B, et al. Characterization of primary human hepatocytes, HepG2 cells, and HepaRG cells at the mRNA level and CYP activity in response to inducers and their predictivity for the detection of human hepatotoxins. Cell Biol Toxicol. 2012;28:69–87.
  • Daujat M, Pichard L, Fabre I, et al. Induction protocols for cytochromes P450iiia invivo and in primary cultures of animal and human hepatocytes. Methods Enzymol. 1991;206:345–353.
  • Richert L, Abadie C, Bonet A, et al. Inter-laboratory evaluation of the response of primary human hepatocyte cultures to model CYP inducers – a european centre for validation of alternative methods (ECVAM) – funded pre-validation study. Toxicol Vitro. 2010;24:335–345.
  • Rodriguez-Antona C, Donato MT, Pareja E, et al. Cytochrome P-450 mRNA expression in human liver and its relationship with enzyme activity. Arch Biochem Biophys. 2001;393:308–315.

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