In vitro assay of six UDP-glucuronosyltransferase isoforms in human liver microsomes, using cocktails of probe substrates and liquid chromatography-tandem mass spectrometry

Drug Metabolism and Disposition

Volumn 42, Issue 11, 2014, Pages 1803-1810

  Seo, Kyung Ah ^a   Kim, Hyo Ji ^a   Jeong, Eun Sook ^a   Abdalla, Nagi ^a   Choi, Chang Soo ^b   Kim, Dong Hyun ^a   Shin, Jae Gook ^a  

^a Inje University College of Medicine   (South Korea)

^b Inje University College of Medicine   (South Korea)

Author keywords

[No Author keywords available]

Indexed keywords

4 HYDROXYINDOLE; CHENODEOXYCHOLIC ACID; ESTRADIOL; GLUCURONOSYLTRANSFERASE; GLUCURONOSYLTRANSFERASE 1A1; GLUCURONOSYLTRANSFERASE 1A9; GLUCURONOSYLTRANSFERASE 2B7; INDOLE; ISOENZYME; NALOXONE; PROPOFOL; TRIFLUOPERAZINE; UNCLASSIFIED DRUG; ENZYME INHIBITOR;

ANALYTIC METHOD; ARTICLE; CONTROLLED STUDY; ENZYME ACTIVITY; ENZYME ASSAY; ENZYME INHIBITION; ENZYME SUBSTRATE; GLUCURONIDATION; IN VITRO STUDY; LIQUID CHROMATOGRAPHY; LIVER MICROSOME; PROCESS OPTIMIZATION; SENSITIVITY AND SPECIFICITY; TANDEM MASS SPECTROMETRY; ANTAGONISTS AND INHIBITORS; ENZYME SPECIFICITY; ENZYMOLOGY; HUMAN; METABOLISM; PROCEDURES; VALIDATION STUDY;

CHROMATOGRAPHY, LIQUID; ENZYME INHIBITORS; GLUCURONOSYLTRANSFERASE; HUMANS; IN VITRO TECHNIQUES; ISOENZYMES; MICROSOMES, LIVER; SUBSTRATE SPECIFICITY; TANDEM MASS SPECTROMETRY;

EID: 84907912715     PISSN: 00909556     EISSN: 1521009X     Source Type: Journal    
DOI: 10.1124/dmd.114.058818     Document Type: Article

References (30)

1. Alkharfy KM and Frye RF (2002) Sensitive liquid chromatographic method using fluorescence detection for the determination of estradiol 3- and 17-glucuronides in rat and human liver microsomal incubations: formation kinetics. J Chromatogr B Analyt Technol Biomed Life Sci 774:33-38.
2. Bae SK, Jeong YJ, Lee C, and Liu KH (2011) Identification of human UGT isoforms responsible for glucuronidation of efavirenz and its three hydroxy metabolites. Xenobiotica 41:437-444.
3. Barbier O, Turgeon D, Girard C, Green MD, Tephly TR, Hum DW, and Bélanger A (2000) 39-azido-39-deoxythimidine (AZT) is glucuronidated by human UDP-glucuronosyltransferase 2B7 (UGT2B7). Drug Metab Dispos 28:497-502.
4. Court MH (2005) Isoform-selective probe substrates for in vitro studies of human UDPglucuronosyltransferases. Methods Enzymol 400:104-116.
5. Di Marco A, D'Antoni M, Attaccalite S, Carotenuto P, and Laufer R (2005) Determination of drug glucuronidation and UDP-glucuronosyltransferase selectivity using a 96-well radiometric assay. Drug Metab Dispos 33:812-819.
6. Dixit V, Hariparsad N, Desai P, and Unadkat JD (2007) In vitro LC-MS cocktail assays to simultaneously determine human cytochrome P450 activities. Biopharm Drug Dispos 28: 257-262.
7. Donato MT, Montero S, Castell JV, Gómez-Lechón MJ, and Lahoz A (2010) Validated assay for studying activity profiles of human liver UGTs after drug exposure: inhibition and induction studies. Anal Bioanal Chem 396:2251-2263.
8. Edavana VK, Dhakal IB, Williams S, Penney R, Boysen G, Yao-Borengasser A, and Kadlubar S (2013) Potential role of UGT1A4 promoter SNPs in anastrozole pharmacogenomics. Drug Metab Dispos 41:870-877.
9. Fallon JK, Neubert H, Goosen TC, and Smith PC (2013a) Targeted precise quantification of 12 human recombinant uridine-diphosphate glucuronosyl transferase 1A and 2B isoforms using nano-ultra-high-performance liquid chromatography/tandem mass spectrometry with selected reaction monitoring. Drug Metab Dispos 41:2076-2080.
10. Fallon JK, Neubert H, Hyland R, Goosen TC, and Smith PC (2013b) Targeted quantitative proteomics for the analysis of 14 UGT1As and -2Bs in human liver using NanoUPLC-MS/MS with selected reaction monitoring. J Proteome Res 12:4402-4413.
11. Gagez AL, Rouguieg-Malki K, Sauvage FL, Marquet P, and Picard N (2012) Simultaneous evaluation of six human glucuronidation activities in liver microsomes using liquid chromatography-tandem mass spectrometry. Anal Biochem 427:52-59.
12. Hanioka N, Ozawa S, Jinno H, Ando M, Saito Y, and Sawada J (2001) Human liver UDPglucuronosyltransferase isoforms involved in the glucuronidation of 7-ethyl-10-hydroxycamptothecin. Xenobiotica 31:687-699.
13. Itäaho K, Mackenzie PI, Ikushiro S, Miners JO, and Finel M (2008) The configuration of the 17-hydroxy group variably influences the glucuronidation of beta-estradiol and epiestradiol by human UDP-glucuronosyltransferases. Drug Metab Dispos 36:2307-2315.
14. Ito M, Yamamoto K, Sato H, Fujiyama Y, and Bamba T (2001) Inhibitory effect of troglitazone on glucuronidation catalyzed by human uridine diphosphate-glucuronosyltransferase 1A6. Eur J Clin Pharmacol 56:893-895.
15. Lépine J, Bernard O, Plante M, Têtu B, Pelletier G, Labrie F, Bélanger A, and Guillemette C (2004) Specificity and regioselectivity of the conjugation of estradiol, estrone, and their catecholestrogen and methoxyestrogen metabolites by human uridine diphospho-glucuronosyltransferases expressed in endometrium. J Clin Endocrinol Metab 89:5222-5232.
16. Manevski N, Kurkela M, Höglund C, Mauriala T, Court MH, Yli-Kauhaluoma J, and Finel M (2010) Glucuronidation of psilocin and 4-hydroxyindole by the human UDP-glucuronosyltransferases. Drug Metab Dispos 38:386-395.
17. Mano Y, Usui T, and Kamimura H (2006) In vitro inhibitory effects of non-steroidal antiinflammatory drugs on 4-methylumbelliferone glucuronidation in recombinant human UDPglucuronosyltransferase 1A9 - potent inhibition by niflumic acid. Biopharm Drug Dispos 27: 1-6.
18. Mano Y, Usui T, and Kamimura H (2007) Comparison of inhibition potentials of drugs against zidovudine glucuronidation in rat hepatocytes and liver microsomes. Drug Metab Dispos 35: 602-606.
19. Matern S, Matern H, Farthmann EH, and Gerok W (1984) Hepatic and extrahepatic glucuronidation of bile acids in man. Characterization of bile acid uridine 59-diphosphateglucuronosyltransferase in hepatic, renal, and intestinal microsomes. J Clin Invest 74:402-410.
20. Miners JO, Bowalgaha K, Elliot DJ, Baranczewski P, and Knights KM (2011) Characterization of niflumic acid as a selective inhibitor of human liver microsomal UDP-glucuronosyltransferase 1A9: application to the reaction phenotyping of acetaminophen glucuronidation. Drug Metab Dispos 39:644-652.
21. Miners JO, Mackenzie PI, and Knights KM (2010) The prediction of drug-glucuronidation parameters in humans: UDP-glucuronosyltransferase enzyme-selective substrate and inhibitor probes for reaction phenotyping and in vitro-in vivo extrapolation of drug clearance and drugdrug interaction potential. Drug Metab Rev 42:196-208.
22. Pelkonen O, Turpeinen M, Uusitalo J, Rautio A, and Raunio H (2005) Prediction of drug metabolism and interactions on the basis of in vitro investigations. Basic Clin Pharmacol Toxicol 96:167-175.
23. Pillai VC, Strom SC, Caritis SN, and Venkataramanan R (2013) A sensitive and specific CYP cocktail assay for the simultaneous assessment of human cytochrome P450 activities in primary cultures of human hepatocytes using LC-MS/MS. J Pharm Biomed Anal 74:126-132.
24. Soars MG, Ring BJ, and Wrighton SA (2003) The effect of incubation conditions on the enzyme kinetics of udp-glucuronosyltransferases. Drug Metab Dispos 31:762-767.
25. Tachibana M, Tanaka M, Masubuchi Y, and Horie T (2005) Acyl glucuronidation of fluoroquinolone antibiotics by the UDP-glucuronosyltransferase 1A subfamily in human liver microsomes. Drug Metab Dispos 33:803-811.
26. Trottier J, Verreault M, Grepper S, Monté D, Bélanger J, Kaeding J, Caron P, Inaba TT, and Barbier O (2006) Human UDP-glucuronosyltransferase (UGT)1A3 enzyme conjugates chenodeoxycholic acid in the liver. Hepatology 44:1158-1170.
27. Uchaipichat V, Mackenzie PI, Elliot DJ, and 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 Dispos 34:449-456.
28. Verreault M, Senekeo-Effenberger K, Trottier J, Bonzo JA, Bélanger J, Kaeding J, Staels B, Caron P, Tukey RH, and Barbier O (2006) The liver X-receptor alpha controls hepatic expression of the human bile acid-glucuronidating UGT1A3 enzyme in human cells and transgenic mice. Hepatology 44:368-378.
29. Williams JA, Hyland R, Jones BC, Smith DA, Hurst S, Goosen TC, Peterkin V, Koup JR, and Ball SE (2004) Drug-drug interactions for UDP-glucuronosyltransferase substrates: a pharmacokinetic explanation for typically observed low exposure (AUCi/AUC) ratios. Drug Metab Dispos 32:1201-1208.
30. Williams JA, Ring BJ, Cantrell VE, Campanale K, Jones DR, Hall SD, and Wrighton SA (2002) Differential modulation of UDP-glucuronosyltransferase 1A1 (UGT1A1)-catalyzed estradiol-3- glucuronidation by the addition of UGT1A1 substrates and other compounds to human liver microsomes. Drug Metab Dispos 30:1266-1273.