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Xenobiotica
the fate of foreign compounds in biological systems
Volume 39, 2009 - Issue 5
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Research Article

Assessment of cryopreserved human hepatocytes as a model system to investigate sulfation and glucuronidation and to evaluate inhibitors of drug conjugation

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Pages 374-381 | Received 09 Dec 2008, Accepted 20 Jan 2009, Published online: 03 Apr 2009

References

  • Adjei AA, Gaedigk A, Simon SD, Weinshilboum RM, Leeder JS. (2008). Interindividual variability in acetaminophen sulfation by human fetal liver: Implications for pharmacogenetic investigations of drug-induced birth defects. Birth Defect Res A: Clin Mol Teratol. 82:155–65.
  • Brown HS, Griffin M, Houston JB. (2007). Evaluation of cryopreserved human hepatocytes as an alternative in vitro system to microsomes for the prediction of metabolic clearance. Drug Metab Disposit 35:293–301.
  • Clements JA, Critchley JAJH, Prescott LF. (1984). The role of sulfate conjugation in the metabolism and disposition of oral and intravenous paracetamol in man. Br J Clin Pharmacol 18:481–5.
  • Coughtrie MWH, Gilissen RAHJ, Shek B, Strange RC, Fryer AA, Jones PW, Bamber DE. (1999). Phenol sulphotransferase SULT1A1 polymorphism: molecular diagnosis and allele frequencies in Caucasian and African populations. Biochem J 337:45–9.
  • Court M, Duan SX, Von Moltke LL, Greenblatt DJ, Patten CJ, Miners JO, Mackenzie PI. (2001). Interindividual variability in acetaminophen glucuronidation by human liver microsomes: Identification of relevant acetaminophen UDP-glucuronosyltransferase isoforms. J Pharmacol Exp Ther 299:998–1006.
  • Critchley JAJH, Critchley LAH, Anderson PJ, Tomlinson B. (2005). Differences in the single-oral-dose pharmacokinetics and urinary excretion of paracetamol and its conjugates between Hong Kong Chinese and Caucasian subjects. J Clin Pharm Ther 30:179–84.
  • Critchley JAJH, Nimmo GR, Gregson CA, Woolhouse NM, Prescott LF. (1986). Inter-subject and ethnic differences in paracetamol metabolism. Br J Clin Pharmacol 22:649–57.
  • Fayz S, Cherry WF, Dawson JR, Mulder GJ, Pang KS. (1984). Inhibition of acetaminophen sulfation by 2,6-dichloro-4-nitrophenol in the perfused rat liver preparation. Lack of a compensatory increase of glucuronidation. Drug Metab Disposit 12:323–9.
  • Fujiwara R, Nakajima M, Yamanaka H, Katoh M, Yokoi T. (2008). Product inhibition of UDP-glucuronosyltransferase (UGT) enzymes by UDP obfuscates the inhibitory effects of UGT substrates. Drug Metab Disposit 36:361–7.
  • Hirata-Koizumi M, Saito M, Miyake S, Hasegawa R. (2007). Adverse events caused by drug interactions involving glucuronoconjugates of zidovudine, valproic acid and lamotrigine, and analysis of how such potential events are discussed in package inserts of Japan, UK and USA. J Clin Pharm Ther 32:177–85.
  • Itoh H, Nagano T, Takeyama M. (2001). Cisapride raises the bioavailability of paracetamol by inhibiting its glucuronidation in man. J Pharm Pharmacol 53:1041–5.
  • Itoh H, Nagano T, Takeyama M. (2002). Effect of nizatidine on paracetamol and its metabolites in human plasma. J Pharm Pharmacol 54:869–73.
  • Kamali F. (1993). The effect of probenecid on paracetamol metabolism and pharmacokinetics. Eur J Clin Pharmacol 45:551–3.
  • Katoh M, Matsui T, Yokoi T. (2007). Glucuronidation of antiallergic drug, tranilast: Identification of human UDP-glucuronosyltransferase isoforms and effect of its phase I metabolite. Drug Metab Disposit 35:583–9.
  • Kerdpin O, Elliot DJ, Mackenzie PI, Miners JO. (2006). Sulfinpyrazone C-glucuronidation is catalyzed selectively by human UDP-glucuronosyltransferase 1A9. Drug Metab Disposit 34:1950–3.
  • Khetani SR, Bhatia SN. (2008). Microscale culture of human liver cells for drug development. Nat Biotechnol 26:120–6.
  • Kiang TK, Ensom MH, Chang TK. (2005). UDP-glucuronosyltransferases and clinical drug–drug interactions. Pharmacol Ther 106:97–132.
  • Kostrubsky SE, Strom SC, Ellis E, Nelson SD, Mutlib AE. (2007). Transport, metabolism, and hepatotoxicity of flutamide, drug–drug interaction with acetaminophen involving phase I and phase II metabolites. Chem Res Toxicol 20:1503–12.
  • Li AP. (2007). Human hepatocytes: Isolation, cryopreservation and applications in drug development. Chemico-Biol Interact 168:16–29.
  • Liu L, Klaassen CD. (1996). Different mechanisms of saturation of acetaminophen sulfate conjugation in mice and rats. Toxicol Appl Pharmacol 139:128–34.
  • Marchetti F, De SC, Vietri M, Pietrabissa A, Spisni R, Mosca F, Pacifici GM. (2001). Differential inhibition of human liver and duodenum sulphotransferase activities by quercetin, a flavonoid present in vegetables, fruit and wine. Xenobiotica 31:841–7.
  • Miners JO, Lillywhite KJ, Yoovathaworn K, Pongmarutai M, Birkett DJ. (1990). Characterization of paracetamol UDP-glucuronosyltransferase activity in human liver microsomes. Biochem Pharmacol 40:595–600.
  • Mutlib AE, Goosen TC, Bauman JN, Williams JA, Kulkarni S, Kostrubsky S. (2006). Kinetics of acetaminophen glucuronidation by UDP-glucuronosyltransferases 1A1, 1A6, 1A9 and 2B15. Potential implications in acetaminophen-induced hepatotoxicity. Chem Res Toxicol 19:701–9.
  • Nagar S, Walther S, Blanchard RL. (2006). Sulfotransferase (SULT) 1A1 polymorphic variants *1, *2, and *3 are associated with altered enzymatic activity, cellular phenotype, and protein degradation. Mol Pharmacol 69:2084–92.
  • Obach RS, Baxter JG, Liston TE, Silber BM, Jones BC, MacIntyre F, Rance DJ, Wastall P. (1997). The prediction of human pharmacokinetic parameters from preclinical and in vitro metabolism data. J Pharmacol Exp Ther 283:46–58.
  • Oddy EA, Manchee GR, Coughtrie MWH. (1997). Assessment of rat liver slices as a suitable model system for studying the simultaneous sulphation and glucuronidation of phenolic xenobiotics. Xenobiotica 27:369–77.
  • Patel M, Tang BK, Kalow W. (1992). Variability of acetaminophen metabolism in Caucasians and Orientals. Pharmacogenetics 2:38–45.
  • Reiter C, Weinshilboum R. (1982). Platelet phenol sulfotransferase activity: correlation with sulfate conjugation of acetaminophen. Clin Pharmacol Ther 32:612–21.
  • Richard K, Hume R, Kaptein E, Stanley EL, Visser TJ, Coughtrie MWH. (2001). Sulfation of thyroid hormone and dopamine during human development – ontogeny of phenol sulfotransferases and arylsulfatase in liver, lung and brain. J Clin Endocrinol Metab 86:2734–42.
  • Rogers SM, Back DJ, Stevenson PJ, Grimmer SFM, Orme L-E. (1987). Paracetamol interaction with oral contraceptive steroids: increased plasma concentrations of ethinyloestradiol. Br J Clin Pharmacol 23:721–5.
  • Schrag ML, Cui D, Rushmore TH, Shou M, Ma B, Rodrigues AD. (2004). Sulfotransferase 1E1 is a low Km isoform mediating the 3-O-sulfation of ethinyl estradiol. Drug Metab Disposit 32:1299–303.
  • Singh SS. (2006). Preclinical pharmacokinetics: an approach towards safer and efficacious drugs. Curr Drug Metab 7:165–82.
  • Soars MG, McGinnity DF, Grime K, Riley RJ. (2007). The pivotal role of hepatocytes in drug discovery. Chemico-Biol Interact 168:2–15.
  • Uchaipichat V, Mackenzie PI, Elliot DJ, Miners JO. (2006). Selectivity of substrate (trifluoperazine) and inhibitor (amitriptyline, androsterone, canrenoic acid, hecogenin, phenylbutazone, quinidine, quinine, and sulfinpyrazone) ‘probes’ for human UDP-glucuronosyltransferases. Drug Metab Disposit 34:449–56.

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