Feedback regulation of bile acid synthesis in primary human hepatocytes: Evidence that CDCA is the strongest inhibitor

Hepatology

Volumn 38, Issue 4, 2003, Pages 930-938

  Ellis, Ewa ^a   Axelson, Magnus ^a   Abrahamsson, Arma ^a   Eggertsen, Gösta ^a   Thörne, Anders ^a   Nowak, Grzegorz ^a   Ericzon, Bo Göran ^a   Björkhem, Ingemar ^a   Einarsson, Curt ^a  

^a KAROLINSKA UNIVERSITY HOSPITAL   (Sweden)

Author keywords

[No Author keywords available]

Indexed keywords

BILE ACID; CHENODEOXYCHOLIC ACID; CHOLESTEROL 7ALPHA MONOOXYGENASE; CHOLIC ACID; CYTOCHROME P450; CYTOCHROME P450 27A1; CYTOCHROME P450 8B1; GLYCINE; GLYCODEOXYCHOLIC ACID; GLYCOURSODEOXYCHOLIC ACID; MESSENGER RNA; OXYGENASE; STEROL 12ALPHA HYDROXYLASE; STEROL 27 HYDROXYLASE; UNCLASSIFIED DRUG;

ARTICLE; BILE ACID SYNTHESIS; CELL FUNCTION; CELL SECRETION; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG EFFECT; DRUG MECHANISM; FEEDBACK SYSTEM; HUMAN; HUMAN CELL; IN VITRO STUDY; LIVER CELL; LIVER CELL CULTURE; NORMAL HUMAN; POLYMERASE CHAIN REACTION; PRIORITY JOURNAL;

EID: 0141532288     PISSN: 02709139     EISSN: None     Source Type: Journal    
DOI: 10.1053/jhep.2003.50394     Document Type: Article

References (45)

1. Russell DW, Setchell KD. Bile acid biosynthesis. Biochemistry 1992;31: 4737-4749.
2. Hylemon P, Pandak M, Vlahcevic Z. Regulation of hepatic cholesterol homeostasis. In: Arias IM, Boyer JL, Chisari FV, Fausti N, Schachter D, Shafritz DA, eds. The Liver: Biology & Pathobiology. 4th ed. Philadelphia: Lippincott Williams & Wilkins, 2001.
3. Heuman DM, Hylemon PB, Vlahcevic ZR. Regulation of bile acid synthesis. III. Correlation between biliary bile salt hydrophobicity index and the activities of enzymes regulating cholesterol and bile acid synthesis in the rat. J Lipid Res 1989;30:1161-1171.
4. Princen HM, Post SM, Twisk J. Regulation of bile acid biosynthesis. Curr Pharmaceutical Design 1997;3:59-84.
5. Einarsson K, Hellstrom K, Kallner M. Feedback regulation of bile acid formation in man. Metabolism 1973;22:1477-1483.
6. LaRusso NF, Hoffman NE, Hofmann AF, Northfield TC, Thistle JL. Effect of primary bile acid ingestion on bile acid metabolism and bilialy lipid secretion in gallstone patients. Gastroenterology 1975;69:1301-1314.
7. Nilsell K, Angelin B, Leijd B, Einarsson K. Comparative effects of ursodeoxycholic acid and chenodeoxycholic acid on bile acid kinetics and biliary lipid secretion in humans. Evidence for different modes of action on bile acid synthesis. Gastroenterology 1983;85:1248-1256.
8. Einarsson K, Hellstrom K, Kallner M. Influence of deoxycholic acid feeding on the elimination of cholesterol in normolipaemic subjects. Clin Sci Mol Med 1974;47:425-433.
9. Pomare EW, Low-Beer TS. The selective inhibition of chenodeoxycholate synthesis by cholate metabolites in man. Clin Sci Mol Med 1975;48:315-321.
10. LaRusso NF, Szczepanik PA, Hofmann AF. Effect of deoxycholic acid ingestion on bile acid metabolism and biliary lipid secretion in normal subjects. Gastroenterology 1977;72:132-140.
11. Coyne MJ, Bonorris GG, Goldstein LI, Schoenfield LJ. Effect of chenode-oxycholic acid and phenobarbital on the rate-limiting enzymes of hepatic cholesterol and bile acid synthesis in patients with gallstones. J Lab Clin Med 1976;87:281-291.
12. Reihner E, Bjorkhem I, Angelin B, Ewerth S, Einarsson K. Bile acid synthesis in humans: regulation of hepatic microsomal cholesterol 7 alpha-hydroxylase activity. Gastroenterology 1989;97:1498-1505.
13. Rudling M, Angelin B, Stahle L, Reihner E, Sahlin S, Olivecrona H, Bjorkhem I, et al. Regulation of hepatic low-density lipoprotein receptor, 3-hydroxy-3-methylglutaryl coenzyme A reductase, and cholesterol 7alpha-hydroxylase mRNAs in human liver. J Clin Endocrinol Metab 2002; 87:4307-4313.
14. Hillebrant C, Nyberg B, Angelin B, Axelson M, Bjorkhem I, Rudling M, Einarsson C. Deoxycholic acid treatment in patients with cholesterol gallstones: failure to detect a suppression of cholesterol 7alpha-hydroxylase activity. J Intern Med 1999;246:399-407.
15. Einarsson C, Hillebrant CG, Axelson M. Effects of treatment with deoxycholic acid and chenodeoxycholic acid on the hepatic synthesis of cholesterol and bile acids in healthy subjects. HEPATOLOGY 2001;33:1189-1193.
16. Bertolotti M, Abate N, Loria P, Dilengite M, Carubbi F, Pinetti A, Digrisolo A, et al. Regulation of bile acid synthesis in humans: effect of treatment with bile acids, cholestyramine or simvastatin on cholesterol 7 alpha-hydroxylation rates in vivo. HEPATOLOGY 1991;14:830-837.
17. Ahlberg J, Angelin B, Bjorkhem I, Einarsson K, Gustafsson JA, Rafter J. Effects of treatment with chenodeoxycholic acid on liver microsomal metabolism of steroids in man. J Lab Clin Med 1980;95:188-194.
18. Bjorkhem I, Araya Z, Rudling M, Angelin B, Einarsson C, Wikvall K. Differences in the regulation of the classical and the alternative pathway for bile acid synthesis in human liver. No coordinate regulation of CYP7A1 and CYP27A1. J Biol Chem 2002;277:26804-26807.
19. Li AP, Roque MA, Beck DJ, Kaminski DL. Isolation and culturing of hepatocytes from human livers. J Tissue Cult Methods 1992; 14:139-146.
20. Ellis E, Goodwin B, Abrahamsson A, Liddle C, Mode A, Rudling M, Bjorkhem I, et al. Bile acid synthesis in primary cultures of rat and human hepatocytes. HEPATOLOGY 1998;27:615-620.
21. Axelson M, Ellis E, Mork B, Garmark K, Abrahamsson A, Bjorkhem I, Ericzon BG, et al. Bile acid synthesis in cultured human hepatocytes: support for an alternative biosynthetic pathway to cholic acid. HEPATOLOGY 2000;31:1305-1312.
22. Einarsson C, Ellis E, Abrahamsson A, Ericzon BG, Bjorkhem I, Axelson M. Bile acid formation in primary human hepatocytes. World J Gastroenterol 2000;6:522-525.
23. Everson GT, Polokoff MA. HepG2. A human hepatoblastoma cell line exhibiting defects in bile acid synthesis and conjugation. J Biol Chem 1986;261:2197-2201.
24. Axelson M, Mork B, Everson GT. Bile acid synthesis in cultured human hepatoblastoma cells. J Biol Chem 1991;266:17770-17777.
25. Cooper AD, Craig WY, Taniguchi T, Everson GT. Characteristics and regulation of bile salt synthesis and secretion by human hepatoma HepG2 cells. HEPATOLOGY 1994;20:1522-1531.
26. Davis RA, Highsmith WE, McNeal MM, Schexnayder JA, Kuan JC. Bile acid synthesis by cultured hepatocytes. Inhibition by mevinolin, but not by bile acids. J Biol Chem 1983;258:4079-4082.
27. Kubaska WM, Gurley EC, Hylemon PB, Guzelian PS, Vlahcevic ZR. Absence of negative feedback control of bile acid biosynthesis in cultured rat hepatocytes. J Biol Chem 1985;260:13459-13463.
28. Whiting MJ, Wishart RA, Gowing MR, McManus ME, Mackinnon AM. Bile acid synthesis and secretion by rabbit hepatocytes in primary monolayer culture: comparison with rat hepatocytes. Biochim Biophys Acta 1989;1001:176-184.
29. Kwekkeboom J, van Voorthuizen EM, Princen HM, Kempen HJ. Feedback inhibition of bile acid synthesis in cultured pig hepatocytes. Biochem Biophys Res Commun 1988; 155:850-856.
30. Kwekkeboom J, Princen HM, van Voorthuizen EM, Kempen HJ. Bile acids exert negative feedback control on bile acid synthesis in cultured pig hepatocytes by suppression of cholesterol 7 alpha-hydroxylase activity. HEPATOLOGY 1990;12:1209-1215.
31. Twisk J, Lehmann EM, Princen HM. Differential feedback regulation of cholesterol 7 alpha-hydroxylase mRNA and transcriptional activity by rat bile acids in primary monolayer cultures of rat hepatocytes. Biochem J 1993;290:685-691.
32. Stravitz RT, Hylemon PB, Heuman DM, Hagey LR, Schteingart CD, Ton-Nu HT, Hofmann AF, et al. Transcriptional regulation of cholesterol 7 alpha-hydroxylase mRNA by conjugated bile acids in primary cultures of rat hepatocytes. J Biol Chem 1993;268:13987-13993.
33. Taniguchi T, Chen J, Cooper AD. Regulation of cholesterol 7 alpha-hydroxylase gene expression in Hep-G2 cells. Effect of serum, bile salts, and coordinate and noncoordinate regulation with other sterol-responsive genes. J Biol Chem 1994;269:10071-10078.
34. Pandak WM, Stravitz RT, Lucas V, Heuman DM, Chiang JY. Hep G2 cells: a model for studies on regulation of human cholesterol 7alpha-hydroxylase at the molecular level. Am J Physiol 1996;270:G401-410.
35. Chen W, Owsley E, Yang Y, Stroup D, Chiang JY. Nuclear receptor-mediated repression of human cholesterol 7alpha-hydroxylase gene transcription by bile acids. J Lipid Res 2001;42:1402-1412.
36. Makishima M, Okamoto AY, Repa JJ, Tu H, Learned RM, Luk A, Hull MV, et al. Identification of a nuclear receptor for bile acids. Science 1999; 284:1362-1365.
37. Cui J, Heard TS, Yu J, Lo JL, Huang L, Li Y, Schaeffer JM, et al. The amino acid residues asparagine 354 and isoleucine 372 of human farnesoid X receptor confer the receptor with high sensitivity to chenodeoxycholate. J Biol Chem 2002;277:25963-25969.
38. Chiang JY. Bile acid regulation of gene expression: roles of nuclear hor-mone receptors. Endocrinol Rev 2002;23:443-463.
39. Lu TT, Makishima M, Repa JJ, Schoonjans K, Kerr TA, Auwerx J, Man-gelsdorf DJ. Molecular basis for feedback regulation of bile acid synthesis by nuclear receptors. Mol Cell 2000;6:507-515.
40. Goodwin B, Jones SA, Price RR, Watson MA, McKee DD, Moore LB, Galardi C, et al. A regulatory cascade of the nuclear receptors FXR, SHP-1, and LRH-1 represses bile acid biosynthesis. Mol Cell 2000;6:517-526.
41. Vlahcevic ZR, Eggertsen G, Bjorkhem I, Hylemon PB, Redford K, Pandak WM. Regulation of sterol 12alpha-hydroxylase and cholic acid biosynthe-sis in the rat. Gastroenterology 2000;118:599-607.
42. Yang Y, Zhang M, Eggertsen G, Chiang JY. On the mechanism of bile acid inhibition of rat sterol 12alpha-hydroxylase gene (CYP8B1) transcription: roles of alpha-fetoprotein transcription factor and hepatocyte nuclear fac-tor 4alpha. Biochim Biophys Acta 2002;1583:63-73.
43. del Castillo-Olivares A, Gil G. Suppression of sterol 12alpha-hydroxylase transcription by the short heterodimer partner: insights into the repression mechanism. Nucleic Acids Res 2001;29:4035-4042.
44. Zhang M, Chiang JY. Transcriptional regulation of the human sterol 12al-pha-hydroxylase gene (CYP8B1): roles of hepatocyte nuclear factor 4alpha in mediating bile acid repression. J Biol Chem 2001;276:41690-41699.
45. Andreou ER, Prokipcak RD. Analysis of human CYP7A1 mRNA decay in HepG2 cells by reverse transcription-polymerase chain reaction. Arch Bio-chem Biophys 1998;357:137-146.