Uptake of ursodeoxycholate and its conjugates by human hepatocytes: Role of Na+-taurocholate cotransporting polypeptide (NTCP), organic anion transporting polypeptide (OATP) 1B1 (OATP-C), and OATP1B3 (OATP8)

Molecular Pharmaceutics

Volumn 3, Issue 1, 2006, Pages 70-77

  Maeda, Kazuya ^a   Kambara, Miyuki ^a   Tian, Ying ^a   Hofmann, Alan F ^b   Sugiyama, Yuichi ^a  

^a UNIVERSITY OF TOKYO   (Japan)

^b UNIVERSITY OF CALIFORNIA SAN DIEGO   (United States)

Author keywords

Hepatic uptake; Human hepatocytes; Na + taurocholate cotransporting polypeptide (NTCP); OATP; Organic anion transporting polypeptide; Ursodeoxycholate

Indexed keywords

CARRIER PROTEIN; GLYCINE; GLYCOURSODEOXYCHOLIC ACID; ORGANIC ANION TRANSPORTER 1; ORGANIC ANION TRANSPORTER 1B1; ORGANIC ANION TRANSPORTER 1B3; SODIUM ION; SODIUM TAUROCHOLATE COTRANSPORTING POLYPEPTIDE; TAURINE; TAUROURSODEOXYCHOLIC ACID; UNCLASSIFIED DRUG; URSODEOXYCHOLIC ACID;

ARTICLE; CELL STRAIN HEK293; CONCENTRATION RESPONSE; DRUG CLEARANCE; DRUG CONJUGATION; DRUG UPTAKE; ENTEROHEPATIC CIRCULATION; HUMAN; HUMAN CELL; LIVER CELL; PRIORITY JOURNAL;

CELL LINE; HEPATOCYTES; HUMANS; ORGANIC ANION TRANSPORT POLYPEPTIDE C; ORGANIC ANION TRANSPORTERS, SODIUM-DEPENDENT; ORGANIC ANION TRANSPORTERS, SODIUM-INDEPENDENT; STRUCTURE-ACTIVITY RELATIONSHIP; SYMPORTERS; TAUROCHENODEOXYCHOLIC ACID; TAUROCHOLIC ACID; URSODEOXYCHOLIC ACID;

EID: 33644695809     PISSN: 15438384     EISSN: 15438392     Source Type: Journal    
DOI: 10.1021/mp050063u     Document Type: Article

References (31)

1. Hofmann, A. F. The continuing importance of bile acids in liver and intestinal disease. Arch. Intern. Med. 1999, 159, 2647-2658.
2. Paumgartner, G.; Beuers, U. Ursodeoxycholic acid in cholestatic liver disease: mechanisms of action and therapeutic use revisited. Hepatology 2002, 36, 525-531.
3. Invernizzi, P.; Setchell, K. D.; Crosignani, A.; Battezzati, P. M.; Larghi, A.; O'Connell, N. C.; Podda, M. Differences in the metabolism and disposition of ursodeoxycholic acid and of its taurine-conjugated species in patients with primary biliary cirrhosis. Hepatology 1999, 29, 320-327.
4. Lindor, K. D.; Lacerda, M. A.; Jorgensen, R. A.; DeSotel, C. K.; Batta, A. K.; Salen, G.; Dickson, E. R.; Rossi, S. S.; Hofmann, A. F. Relationship between biliary and serum bile acids and response to ursodeoxycholic acid in patients with primary biliary cirrhosis. Am. J. Gastroenterol. 1998, 93, 1498-1504.
5. Van Dyke, R. W.; Stephens, J. E.; Scharschmidt, B. F. Bile acid transport in cultured rat hepatocytes. Am. J. Physiol. 1982, 243, G484-492.
6. Anwer, M. S.; Hegner, D. Effect of Na on bile acid uptake by isolated rat hepatocytes. Evidence for a heterogeneous system. Hoppe-Seyler's Z. Physiol. Chem. 1978, 359, 181-192.
7. Hagenbuch, B.; Meier, P. J. Molecular cloning, chromosomal localization, and functional characterization of a human liver Na+/ bile acid cotransporter. J. Clin. Invest. 1994, 93, 1326-1331.
8. Hagenbuch, B.; Meier, P. J. The superfamily of organic anion transporting polypeptides. Biochim. Biophys. Acta 2003, 1609, 1-18.
9. Meier, P. J.; Eckhardt, U.; Schroeder, A.; Hagenbuch, B.; Stieger, B. Substrate specificity of sinusoidal bile acid and organic anion uptake systems in rat and human liver. Hepatology 1997, 26, 1667-1677.
10. Kullak-Ublick, G. A.; Hagenbuch, B.; Stieger, B.; Schteingart, C. D.; Hofmann, A. F.; Wolkoff, A. W.; Meier, P. J. Molecular and functional characterization of an organic anion transporting polypeptide cloned from human liver. Gastroenterology 1995, 109, 1274-1282.
11. Alcorn, J.; Lu, X.; Moscow, J. A.; McNamara, P. J. Transporter gene expression in lactating and nonlactating human mammary epithelial cells using real-time reverse transcription-polymerase chain reaction. J. Pharmacol. Exp. Ther. 2002, 303, 487-496.
12. Eckhardt, U.; Schroeder, A.; Stieger, B.; Hochli, M.; Landmann, L.; Tynes, R.; Meier, P. J.; Hagenbuch, B. Polyspecific substrate uptake by the hepatic organic anion transporter Oatp1 in stably transfected CHO cells. Am. J. Physiol. 1999, 276, G1037-1042.
13. Reichel, C.; Gao, B.; Van Montfoort, J.; Cattori, V.; Rahner, C.; Hagenbuch, B.; Stieger, B.; Kamisako, T.; Meier, P. J. Localization and function of the organic anion-transporting polypeptide Oatp2 in rat liver. Gastroenterology 1999, 117, 688-695.
14. Walters, H. C.; Craddock, A. L.; Fusegawa, H.; Willingham, M. C; Dawson, P. A. Expression, transport properties, and chromosomal location of organic anion transporter subtype 3. Am. J. Physiol. 2000, 279, G1188-1200.
15. Poupon, R.; Chretien, Y.; Parquet, M.; Ballet, F.; Rey, C.; Infante, R. Hepatic transport of bile acids in the isolated perfused rat liver. Structure-kinetic relationship. Biochem. Pharmacol. 1988, 37, 209-212.
16. Sorscher, S.; Lillienau, J.; Meinkoth, J. L.; Steinbach, J. H.; Schteingart, C. D.; Feramisco, J.; Hofmann, A. F. Conjugated bile acid uptake by Xenopus laevis oocytes induced by microinjection with ileal Poly A+ mRNA. Biochem. Biophys. Res. Commun. 1992, 186, 1455-1462.
17. Hirano, M.; Maeda, K.; Shitara, Y.; Sugiyama, Y. Contribution of OATP2 (OATP1B1) and OATP8 (OATP1B3) to the Hepatic Uptake of Pitavastatin in Humans. J. Pharmacol. Exp. Ther. 2004, 311, 139-146.
18. Shitara, Y.; Li, A. P.; Kato, Y.; Lu, C.; Ito, K.; Itoh, T.; Sugiyama, Y. Function of uptake transporters for taurocholate and estradiol-17beta-D- glucuronide in cryopreserved human hepatocytes. Drug Metab. Pharmacokinet. 2003, 18, 33-41.
19. Yamaoka, K.; Tanigawara, Y.; Nakagawa, T.; Uno, T. A pharmacokinetic analysis program (multi) for microcomputer. J Pharmacobio-Dyn. 1981, 4, 879-885.
20. Schroeder, A.; Eckhardt, U.; Stieger, B.; Tynes, R.; Schteingart, C. D.; Hofmann, A. F.; Meier, P. J.; Hagenbuch, B. Substrate specificity of the rat liver Na(+)-bile salt cotransporter in Xenopus laevis oocytes and in CHO cells. Am. J. Physiol. 1998, 274, G370-375.
21. Kim, R. B.; Leake, B.; Cvetkovic, M.; Roden, M. M.; Nadeau, J.; Walubo, A.; Wilkinson, G. R. Modulation by drugs of human hepatic sodium-dependent bile acid transporter (sodium taurocholate cotransporting polypeptide) activity. J. Pharmacol. Exp. Ther. 1999, 291, 1204-1209.
22. Hsiang, B.; Zhu, Y.; Wang, Z.; Wu, Y.; Sasseville, V.; Yang, W. P.; Kirchgessner, T. G. A novel human hepatic organic anion transporting polypeptide (OATP2). Identification of a liver-specific human organic anion transporting polypeptide and identification of rat and human hydroxymethylglutaryl-CoA reductase inhibitor transporters. J. Biol. Chem. 1999, 274, 37161-37168.
23. Cui, Y.; Konig, J.; Leier, I.; Buchholz, U.; Keppler, D. Hepatic uptake of bilirubin and its conjugates by the human organic anion transporter SLC21A6. J. Biol. Chem. 2001, 276, 9626-9630.
24. Hata, S.; Wang, P.; Eftychiou, N.; Ananthanarayanan, M.; Batta, A.; Salen, G.; Pang, K. S.; Wolkoff, A. W. Substrate specificities of rat oatp1 and ntcp: implications for hepatic organic anion uptake. Am. J. Physiol. 2003, 255, G829-839.
25. Crosignani, A.; Setchell, K. D.; Invemizzi, P.; Larghi, A.; Rodrigues, C. M.; Podda, M. Clinical pharmacokinetics of therapeutic bile acids. Clin. Pharmacokinet. 1996, 30, 333-358.
26. Takikawa, H.; Takemura, T.; Yamanaka, M. The mechanism of tauroursodeoxycholate uptake by isolated rat hepatocytes. Int. Hepatol. Commun. 1995, 3, 20-25.
27. von Dippe, P.; Amoui, M.; Stellwagen, R. H.; Levy, D. The functional expression of sodium-dependent bile acid transport in Madin-Darby canine kidney cells transfected with the cDNA for microsomal epoxide hydrolase. J. Biol. Chem. 1996, 271, 18176-18180.
28. Bouscarel, B.; Nussbaum, R.; Dubner, H.; Fromm, H. The role of sodium in the uptake of ursodeoxycholic acid in isolated hamster hepatocytes. Hepatology 1995, 21, 145-154.
29. Briz, O.; Serrano, M. A.; Rebollo, N.; Hagenbuch, B.; Meier, P. J.; Koepsell, H.; Marin, J. J. Carriers involved in targeting the cytostatic bile acid-cisplatin derivatives cis-diammine-chlorocholylglycinate-platinum(II) and cis-diammine-bisursodeoxycholate-platinum(II) toward liver cells. Mol. Pharmacol. 2002, 61, 853-860.
30. Ewerth, S.; Angelin, B.; Einarsson, K.; Nilsell, K.; Bjorkhem, I. Serum concentrations of ursodeoxycholic acid in portal venous and systemic venous blood of fasting humans as determined by isotope dilution-mass spectrometry. Gastroenterology 1985, 88, 126-133.
31. Marzolini, C.; Tirona, R. G.; Kim, R. B. Pharmacogenomics of OATP and OAT families. Pharmacogenomics 2004, 5, 273-282.