The role of the enterohepatic circulation of bile salts and nuclear hormone receptors in the regulation of cholesterol homeostasis: Bile salts as ligands for nuclear hormone receptors

Canadian Journal of Gastroenterology

Volumn 17, Issue 4, 2003, Pages 265-271

  Redinger, Richard N ^a  

^a University of Louisville School of Medicine   (United States)

Author keywords

Bile acid; Cholesterol homeostasis; Nuclear hormone receptors

Indexed keywords

3 [2 [2 CHLORO 4 [3 (2,6 DICHLOROPHENYL) 5 ISOPROPYL 4 ISOXAZOLYLMETHOXY]PHENYL]VINYL]BENZOIC ACID; 3 [3 [[2 CHLORO 3 (TRIFLUOROMETHYL)BENZYL](2 DIPHENYLETHYL)AMINO]PROPOXY]PHENYLACETIC ACID; BILE ACID; BILE SALT; BINDING PROTEIN; CARRIER PROTEIN; CHOLESTEROL; COLESTYRAMINE; FARNESOID X RECEPTOR; GUGGELSTERONE; GW 9047; HORMONE RECEPTOR; HORMONE RECEPTOR AFFECTING AGENT; LG 268; LIGAND; LIVER X RECEPTOR; OXYSTEROL; PODOCARPIC ACID DERIVATIVE; PREGNAN X RECEPTOR; PREGNANEDIONE; RETINOID X RECEPTOR; T 1317; TAUROCHOLIC ACID; TRANSCRIPTION FACTOR; UNCLASSIFIED DRUG; URSODEOXYCHOLIC ACID; VITAMIN D RECEPTOR;

BILE ACID BLOOD LEVEL; BILE ACID METABOLISM; BILE ACID SYNTHESIS; CHOLESTASIS; CHOLESTEROL BLOOD LEVEL; CHOLESTEROL METABOLISM; CHOLESTEROL TRANSPORT; DETOXIFICATION; DNA RESPONSIVE ELEMENT; DRUG MECHANISM; DRUG TARGETING; ENTEROHEPATIC CIRCULATION; HOMEOSTASIS; HUMAN; HYDROXYLATION; HYPERCHOLESTEROLEMIA; INTESTINE ABSORPTION; LIPOLYSIS; LIVER; LIVER INJURY; NEGATIVE FEEDBACK; POSITIVE FEEDBACK; PRIORITY JOURNAL; PROTEIN FUNCTION; REVIEW; SIGNAL TRANSDUCTION; TOXICITY;

EID: 0037502452     PISSN: 08357900     EISSN: None     Source Type: Journal    
DOI: 10.1155/2003/190784     Document Type: Review

References (65)

1. Hofmann AF. Enterohepatic circulation of bile acids. In: Shultz SG, Forte JG, Rainer BB, eds. Handbook of Physiology (Volume 3). New York: Oxford University Press, 1989.
2. Hofmann AF, Small DM. Detergent properties of bile salts: Correlation with physiological function. Annu Rev Med 1967;18:333-76.
3. Hofmann AF. Intestinal absorption of bile acids and biliary constituents: The intestinal components of the enterohepatic circulation and the integrated system. In: Johnson LR, ed. Physiology of the Gastrointestinal Tract. New York: Raven Press Limited, 1994.
4. Repa JJ, Mangelsdorf DJ. Nuclear receptor regulation of cholesterol and bile acid metabolism. Curr Opin Biotechnol 1999;10:557-63.
5. Chiang JY. Bile acid regulation of gene expression: Roles of nuclear hormone receptors. Endocr Rev 2002;23:443-63.
6. Gupta S, Pandak WM, Hylemon PB. LXR alpha is the dominant regulator of CYP7A1 transcription. Biochem Biophys Res Commun 2002;293:338-43.
7. Lu TT, Repa JJ, Mangelsdorf DJ. Orphan nuclear receptors as eLiXiRs and FiXeRs of sterol metabolism. J Biol Chem 2001;276:37735-8.
8. Fitzgerald ML, Moore KJ, Freeman MW. Nuclear hormone receptors and cholesterol trafficking: The orphans find a new home. J Mol Med 2002;80:271-81.
9. Debril MB, Renaud JP, Fajas L, Auwerx J. The pleiotropic functions of peroxisome proliferator-activated receptor. J Mol Med 2001;79:30-47.
10. Houseknecht KL, Cole BM, Steele PJ. Peroxisome proliferator-activated receptor gamma (PPARgamma) and its ligands: A review. Domest Anim Endocrinol 2002;22:1-23.
11. Aranda A, Pascual A. Nuclear hormone receptors and gene expression. Physiol Rev 2001;81:1269-1304.
12. Repa JJ, Mangelsdorf DJ. The role of orphan nuclear receptors in the regulation of cholesterol homeostasis. Annu Rev Cell Dev Biol 2000;16:459-81.
13. Schoonjans K, Brendel C, Mangelsdorf D, Auwerx J. Sterols and gene expression: Control of affluence. Biochim Biophys Acta 2000;1529:114-25.
14. Russell DW, Setchell KD. Bile acid biosynthesis. Biochemistry 1992;31:4737-49.
15. Lecureur V, Courtois A, Payen L, Verhnet L, Guillouzo A, Fardel O. Expression and regulation of hepatic drug and bile acid transporters. Toxicology 2000;153:203-19.
16. Small DM, Dowling RH, Redinger RN. The enterohepatic circulation of bile salts. Arch Intern Med 1972;130:552-73.
17. Thaysen EH, Pedersen L. Idiopathic bile acid catharsis. Gut 1976;17:965-70.
18. Redinger RN, Hawkins JW, Grace DM. The economy of the enterohepatic circulation of bile acids in the baboon. 1. Studies of controlled enterohepatic circulation of bile acids. J Lipid Res 1984;25:428-36.
19. Redinger RN. The economy of the enterohepatic circulation of bile acids in the baboon. 2. Regulation of bile acid synthesis by enterohepatic circulation of bile acids. J Lipid Res 1984;25:437-47.
20. Shefer S, Hauser, Bekersky I, Mosbach EH. Biochemical site of regulation of bile acid biosynthesis in the rat. J Lipid Res 1970;11:404-11.
21. Tu H, Okamoto AY, Shan B. FXR, a bile acid receptor and biological sensor. Trends Cardiovasc Med 2000;10:30-5.
22. Brown MS, Goldstein JL. A proteolytic pathway that controls the cholesterol content of membranes, cells, and blood. Proc Natl Acad Sci USA 1999;96:11041-8.
23. Wang X, Sato R, Brown MS, Hua X, Goldstein JL. SREBP-1, a membrane-bound transcription factor released by sterol-regulated proteolysis. Cell 1994;77:53-62.
24. Escriva H, Delaunay F, Laudet V. Ligand binding and nuclear receptor evolution. Bioessays 2000;22:717-27.
25. Bocher V, Pineda-Torra I, Fruchart JC, Staels B. PPARs: Transcription factors controlling lipid and lipoprotein metabolism. Ann NY Acad Sci 2002;967:7-18.
26. Robinson-Rechavi M, Carpentier AS, Duffraisse M, Laudet V. How many nuclear hormone receptors are there in the human genome? Trends Genet 2001;17:554-6.
27. Duarte J, Perriere G, Laudet V, Robinson-Rechavi M. NUREBASE: database of nuclear hormone receptors. Nucleic Acids Res 2002;30:364-8.
28. Giquere V. Orphan nuclear receptors: Gene to function. Endocr Rev 1999;20:689-725.
29. Urizar NL, Liverman AB, Dodds DT, et al. A natural product that lowers cholesterol as an antagonist ligand for FXR. Science 2002;296:1703-6.
30. Willson TM, Jones SA, Moore JT, Kliewer SA. Chemical genomics: Functional analysis of orphan nuclear receptors in the regulation of bile acid metabolism. Med Res Rev 2001;21:513-22.
31. Schultz JR, Tu H, Luk A, et al. Role of LXRs in control of lipogenesis. Genes Dev 2000;14:2831-8.
32. Sparrow CP, Baffic J, Lam MH, et al. A potent synthetic LXR agonist is more effective than cholesterol loading at inducing ABCA1 mRNA and stimulating cholesterol efflux. J Biol Chem 2002;277:10021-7.
33. Joseph SB, McKilligin E, Pei L, et al. Synthetic LXR ligand inhibits the development of atherosclerosis in mice. Proc Natl Acad Sci USA 2002;99:7604-9.
34. Repa JJ, Berge KE, Pomajzl C, Richardson JA, Hobbs H, Mangelsdorf DJ. Regulation of ATP-binding cassette sterol transporters ABCG5 and ABCG8 by the liver X receptors alpha and beta. J Biol Chem 2002;277:18793-800.
35. Repa JJ, Turley SD, Lobaccaro JA, et al. Regulation of absorption and ABC-1 mediated efflux of cholesterol by RXR heterodimers. Science 2000;289:1524-9.
36. Waxman DJ. P450 gene induction by structurally diverse xenochemicals: Central role of nuclear receptors CAR, PXR, and PPAR. Arch Biochem Biophys 1999;369:11-23.
37. Russell DW Oxysterol biosynthetic enzymes. Biochim Biophys Acta 2000;1529:126-35.
38. Lu TT, Makishima M, Repa JJ, et al. Molecular basis for feedback regulation of bile acid synthesis by nuclear receptors. Mol Cell 2000;6:507-15.
39. Willy PJ, Umesono K, Ong ES, Evans RM, Heyman RA, Mangelsdorf DJ. LXR, a nuclear receptor that defines a distinct retinoid response pathway. Genes Dev 1995;9:1033-45.
40. Plat J, Mensink RP. Increased intestinal ABCA1 expression contributes to the decrease in cholesterol absorption after plant stanol consumption. FASEB J 2002; 16:1248-53.
41. Yu L, Li-Hawkins J, Hammer RE, et al. Overexpression of ABCG5 and ABCG8 promotes biliary cholesterol secretion and reduces fractional absorption of dietary cholesterol. J Clin Invest 2002;110:671-80.
42. Berge KE, Tian H, Graf GA, et al. Accumulation of dietary cholesterol in sitosterolemia caused by mutations in adjacent ABC transporters. Science 2000;290:1771-5.
43. Kast HR, Nguyen CM, Sinal CJ, et al. Farnesoid X-activated receptor induces apolipoprotein C-II transcription: A molecular mechanism linking plasma triglyceride levels to bile acids. Mol Endocrinol 2001;15:1720-8.
44. Urizar NL, Dowhan DH, Moore DD. The farnesoid X-activated receptor mediates bile acid activation of phospholipid transfer protein gene expression. J Biol Chem 2000;275:39313-7.
45. Laffitte BA, Kast HR, Nguyen CM, Zavacki AM, Moore DD, Edwards PA. Identification of the DNA binding specificity and potential target genes for the farnesoid X-activated receptor. J Biol Chem 2000;275:10638-47.
46. Cao G, Beyer TP, Yang XF, et al. Phospholipid transfer protein is regulated by liver x receptors in vivo. J Biol Chem 2002;277:39561-5.
47. Luo Y, Liang CF, Tall AR. The orphan nuclear receptor LRH-1 potentiates the sterol-mediated induction of the human CETP gene by liver X receptor. J Biol Chem 2001;276:24767-73.
48. Laffitte BA, Repa JJ, Joseph SB, et al. LXRs control lipid-inducible expression of the apolipoprotein E gene in macrophages and adipocytes. Proc Natl Acad Sci USA 2001;98:507-12.
49. Makishima M, Okamoto AY, Repa JJ, et al. Identification of a nuclear receptor for bile acids. Science 1999;284:1362-5.
50. Parks DJ, Blanchard SG, Bledsoe RK, et al. Bile acids: Natural ligands for an orphan nuclear receptor. Science 1999;284:1365-8.
51. Goodwin B, Jones SA, Price RR, et al. A regulatory cascade of the nuclear receptors FXR, SHP-1, and LRH-1 represses bile acid biosynthesis. Mol Cell 2000;6:517-26.
52. Gupta S, Stravitz RT, Dent P, Hylemon PB. Down-regulation of cholesterol 7alpha-hydroxylase (CYP7A1) gene expression by bile acids in primary rat hepatocytes; is mediated by the c-Jun N-terminal kinase pathway. J Biol Chem 2001;276:15816-22.
53. Grober J, Zaghini I, Fujii H, et al. Identification of a bile acid-responsive element in the human ileal bile acid-binding protein gene. Involvement of the farnesol F receptor/9-cis-retinoic acid receptor heterodimer. J Biol Chem 1999;274:29749-54.
54. Hwang ST, Urizar NL, Moore DD, Henning SJ. Bile acids regulate the ontogenic expression of ileal bile acid binding protein in the rat via the farnesoid X receptor. Gastroenterology 2002;122:1483-92.
55. Sinal CJ, Tohkin M, Miyata M, Ward JM, Lambert G, Gonzalez FJ. Targeted disruption of the nuclear receptor FXR/BAR impairs bile acid and lipid homeostasis. Cell 2000;102:731-44.
56. Denson LA, Sturm E, Echevarria W, et al. The orphan nuclear receptor, shp, mediates bile acid-induced inhibition of the rat bile acid transporter, ntcp. Gastroenterology 2001;121:140-7.
57. Ananthanarayanan M, Balasubramanian N, Makishima M, Mangelsdorf DJ, Suchy FJ. Human bile salt export pump promoter is transactivated by the famesoid X receptor/bile acid receptor. J Biol Chem 2001;276:28857-65.
58. Xie W, Radominska-Pandya A, Shi Y, et al. An essential role for nuclear receptors SXR/PXR in detoxification bile acids. Proc Natl Acad Sci USA 2001;98:3375-80.
59. Staudinger JL, Goodwin B, Jones SA, et al. The nuclear receptor PXR is a lithocholic acid sensor that protects against liver toxicity. Proc Natl Acad Sci USA 2001;98:3369-74.
60. Schuetz EG, Strom S, Yasuda K, et al. Disrupted bile acid homeostasis reveals an unexpected interaction among nuclear hormone receptors, transporters, and cytochrome P450. J Biol Chem 2001;276:39411-8.
61. Carey MC. The enterohepatic circulation. In: Arias I, Popper H, et al, eds. The Liver: Biology, and Pathobiology. New York: Raven Press Limited, 1982.
62. Makishima M, Lu TT, Xie W, et al. Vitamin D receptor as an intestinal bile acid sensor. Science 2002;296:1313-6.
63. Drobnik W, Lindenthal B, Lieser B, et al. ATP-binding cassette transporter A1 (ABC-A1) affects total body sterol metabolism. Gastroenterology 2001;120:1203-11.
64. Balistreri WF. Inborn errors of bile acid biosynthesis and transport: Novel forms of metabolic liver disease. Gastroenterol Clin North Am 1999;28:145-72.
65. Kadakol A, Ghosh SS, Sappa BS, Sharma G, Chowdhury JR, Chowdhury NR. Genetic lesions of bilirubin uridine-diphosphoglucuronate Glucuronosyltransferase (UGT1A1) causing Crigler-Najjar and Gilbert syndromes: Correlation of genotype to phenotype. Human Mutation 2000;16:297-306.