Bile acid receptors in non-alcoholic fatty liver disease

Biochemical Pharmacology

Volumn 86, Issue 11, 2013, Pages 1517-1524

  Li, Yuanyuan ^a   Jadhav, Kavita ^a   Zhang, Yanqiao ^a  

^a Northeastern Ohio Medical University   (United States)

Author keywords

Cholesterol; FXR; Inflammation; TGR5; Triglyceride

Indexed keywords

3 [2 [2 CHLORO 4 [3 (2,6 DICHLOROPHENYL) 5 ISOPROPYL 4 ISOXAZOLYLMETHOXY]PHENYL]VINYL]BENZOIC ACID; ALANINE AMINOTRANSFERASE; BILE ACID; CHENODEOXYCHOLIC ACID; CHOLESTEROL; CHOLIC ACID; DEOXYCHOLIC ACID; FARNESOID X RECEPTOR; FATTY ACID SYNTHASE; G PROTEIN COUPLED RECEPTOR; GAMMA GLUTAMYLTRANSFERASE; GAMMA INTERFERON; GELATINASE A; GLUCAGON LIKE PEPTIDE 1; GLUCOSE; HIGH DENSITY LIPOPROTEIN CHOLESTEROL; INTERLEUKIN 1BETA; KERATINOCYTE DERIVED CHEMOKINE; LIPOPROTEIN; LITHOCHOLIC ACID; LOW DENSITY LIPOPROTEIN RECEPTOR; MONOCYTE CHEMOTACTIC PROTEIN 1; OBETICHOLIC ACID; SCAVENGER RECEPTOR BI; TGR5 PROTEIN; TISSUE INHIBITOR OF METALLOPROTEINASE 1; TRIACYLGLYCEROL; TUMOR NECROSIS FACTOR ALPHA; TUROFEXORATE ISOPROPYL; UNCLASSIFIED DRUG; UNINDEXED DRUG;

ALANINE AMINOTRANSFERASE BLOOD LEVEL; ATHEROSCLEROSIS; BILE ACID METABOLISM; BILE COMPOSITION; BROWN ADIPOSE TISSUE; CALCIUM MOBILIZATION; CHEMICAL STRUCTURE; CHOLESTEROL BLOOD LEVEL; CHOLESTEROL LIVER LEVEL; CHOLESTEROL METABOLISM; CHOLESTEROL STONE; CHRONIC INFLAMMATION; COLITIS; CYTOKINE RELEASE; DNA BINDING; ENERGY EXPENDITURE; ENZYME METABOLISM; FAT INTAKE; FATTY ACID BLOOD LEVEL; FATTY ACID SYNTHESIS; FATTY LIVER; GALLSTONE FORMATION; GENE TARGETING; GLUCONEOGENESIS; GLUCOSE BLOOD LEVEL; GLUCOSE HOMEOSTASIS; GLUCOSE INFUSION; HUMAN; IN VIVO STUDY; INFLAMMATION; INFLAMMATORY INFILTRATE; INSULIN RELEASE; INSULIN RESISTANCE; INSULIN SENSITIVITY; INTRAHEPATIC BILE DUCT; KUPFFER CELL; LIPID DIET; LIPID LIVER LEVEL; LIPID PEROXIDATION; LIPOGENESIS; LIPOPROTEIN BLOOD LEVEL; LIPOPROTEIN METABOLISM; LIVER FIBROSIS; LIVER FUNCTION; LUNG ALVEOLUS MACROPHAGE; MEMBRANE DEPOLARIZATION; NON INSULIN DEPENDENT DIABETES MELLITUS; NONALCOHOLIC FATTY LIVER; NONHUMAN; OBSERVATIONAL STUDY; OXIDATIVE PHOSPHORYLATION; PANCREAS ISLET BETA CELL; PHASE 2 CLINICAL TRIAL (TOPIC); PRIORITY JOURNAL; PROTEIN SUBUNIT; REVIEW; TRANSGENIC MOUSE; WEIGHT GAIN; WILD TYPE;

EID: 84887477319     PISSN: 00062952     EISSN: 18732968     Source Type: Journal    
DOI: 10.1016/j.bcp.2013.08.015     Document Type: Note

References (74)

1. C. Postic, and J. Girard Contribution of de novo fatty acid synthesis to hepatic steatosis and insulin resistance: lessons from genetically engineered mice J Clin Investig 118 2008 829 838
2. J.C. Cohen, J.D. Horton, and H.H. Hobbs Human fatty liver disease: old questions and new insights Science 332 2011 1519 1523
3. H. Fujii, and N. Kawada Inflammation and fibrogenesis in steatohepatitis J Gastroenterol 47 2012 215 225
4. C.P. Day, and O.F. James Steatohepatitis: a tale of two hits Gastroenterology 114 1998 842 845
5. J.C. Cohen, J.D. Horton, and H.H. Hobbs Human fatty liver disease: old questions and new insights Science 332 2011 1519 1523
6. N. Anderson, and J. Borlak Molecular mechanisms and therapeutic targets in steatosis and steatohepatitis Pharmacol Rev 60 2008 311 357
7. C. Thomas, R. Pellicciari, M. Pruzanski, J. Auwerx, and K. Schoonjans Targeting bile-acid signalling for metabolic diseases Nat Rev Drug Discov 7 2008 678 693
8. Y. Zhang, and P.A. Edwards FXR signaling in metabolic disease FEBS Lett 582 2008 10 18
9. P. Lefebvre, B. Cariou, F. Lien, F. Kuipers, and B. Staels Role of bile acids and bile acid receptors in metabolic regulation Physiol Rev 89 2009 147 191
10. F.Y. Lee, H. Lee, M.L. Hubbert, P.A. Edwards, and Y.F.X.R. Zhang FXR, a multipurpose nuclear receptor Trends Biochem Sci 31 2006 572 580
11. T.W. Pols, L.G. Noriega, M. Nomura, J. Auwerx, and K. Schoonjans The bile acid membrane receptor TGR5 as an emerging target in metabolism and inflammation J Hepatol 54 2011 1263 1272
12. R. Pellicciari, A. Gioiello, A. Macchiarulo, C. Thomas, E. Rosatelli, and B. Natalini Discovery of 6alpha-ethyl-23(S)-methylcholic acid (S-EMCA, INT-777) as a potent and selective agonist for the TGR5 receptor, a novel target for diabesity J Med Chem 52 2009 7958 7961
13. M. Rakhshandehroo, B. Knoch, M. Muller, and S. Kersten Peroxisome proliferator-activated receptor alpha target genes PPAR Res 2010 PMID: 20936127
14. T. Furihata, M. Hosokawa, F. Nakata, T. Satoh, and K. Chiba Purification, molecular cloning, and functional expression of inducible liver acylcarnitine hydrolase in C57BL/6 mouse, belonging to the carboxylesterase multigene family Arch Biochem Biophys 416 2003 101 109
15. W. Insull Jr. Clinical utility of bile acid sequestrants in the treatment of dyslipidemia: a scientific review South Med J 99 2006 257 273
16. M. Nakahara, H. Fujii, P.R. Maloney, M. Shimizu, and R. Sato Bile acids enhance low density lipoprotein receptor gene expression via a MAPK cascade-mediated stabilization of mRNA J Biol Chem 277 2002 37229 37234
17. C. Langhi, C. Le May, S. Kourimate, S. Caron, B. Staels, and M. Krempf Activation of the farnesoid X receptor represses PCSK9 expression in human hepatocytes FEBS Lett 582 2008 949 955
18. G. Lambert, M.J. Amar, G. Guo, H.B. Brewer Jr., F.J. Gonzalez, and C.J. Sinal The farnesoid X- receptor is an essential regulator of cholesterol homeostasis J Biol Chem 278 2003 2563 2570
19. Y. Zhang, F.Y. Lee, G. Barrera, H. Lee, C. Vales, and F.J. Gonzalez Activation of the nuclear receptor FXR improves hyperglycemia and hyperlipidemia in diabetic mice Proc Natl Acad Sci USA 103 2006 1006 1011
20. Y. Zhang, L. Yin, J. Anderson, H. Ma, F.J. Gonzalez, and T.M. Willson Identification of novel pathways that control farnesoid X receptor-mediated hypocholesterolemia J Biol Chem 285 2010 3035 3043
21. -/- mice J Lipid Res 50 2009 1090 1100
22. B. Flatt, R. Martin, T.L. Wang, P. Mahaney, B. Murphy, and X.H. Gu Discovery of XL335 (WAY-362450), a highly potent, selective, and orally active agonist of the farnesoid X receptor (FXR) J Med Chem 52 2009 904 907
23. M.C. Bateson, D. Maclean, J.R. Evans, and I.A. Bouchier Chenodeoxycholic acid therapy for hypertriglyceridaemia in men Br J Clin Pharmacol 5 1978 249 254
24. J.R. Crouse 3rd Hypertriglyceridemia: a contraindication to the use of bile acid binding resins Am J Med 83 1987 243 248
25. M. Watanabe, S.M. Houten, L. Wang, A. Moschetta, D.J. Mangelsdorf, and R.A. Heyman Bile acids lower triglyceride levels via a pathway involving FXR, SHP, and SREBP-1c J Clin Investig 113 2004 1408 1418
26. S. Cipriani, A. Mencarelli, G. Palladino, and S. Fiorucci FXR activation reverses insulin resistance and lipid abnormalities and protects against liver steatosis in Zucker (fa/fa) obese rats J Lipid Res 51 4 2010 771 784
27. S. Zhang, J. Wang, Q. Liu, and D.C. Harnish Farnesoid X receptor agonist WAY-362450 attenuates liver inflammation and fibrosis in murine model of non-alcoholic steatohepatitis J Hepatol 51 2009 380 388
28. C.J. Sinal, M. Tohkin, M. Miyata, J.M. Ward, G. Lambert, and F.J. Gonzalez Targeted disruption of the nuclear receptor FXR/BAR impairs bile acid and lipid homeostasis Cell 102 2000 731 744
29. K. Boulias, N. Katrakili, K. Bamberg, P. Underhill, A. Greenfield, and I. Talianidis Regulation of hepatic metabolic pathways by the orphan nuclear receptor SHP EMBO J 24 2005 2624 2633
30. L. Wang, J. Liu, P. Saha, J. Huang, L. Chan, and B. Spiegelman The orphan nuclear receptor SHP regulates PGC-1alpha expression and energy production in brown adipocytes Cell Metab 2 2005 227 238
31. J. Huang, J. Iqbal, P.K. Saha, J. Liu, L. Chan, and M.M. Hussain Molecular characterization of the role of orphan receptor small heterodimer partner in development of fatty liver Hepatology 46 2007 147 157
32. K.E. Matsukuma, M.K. Bennett, J. Huang, L. Wang, G. Gil, and T.F. Osborne Coordinated control of bile acids and lipogenesis through FXR-dependent regulation of fatty acid synthase J Lipid Res 47 2006 2754 2761
33. E. Ip, G.C. Farrell, G. Robertson, P. Hall, R. Kirsch, and I. Leclercq Central role of PPARalpha-dependent hepatic lipid turnover in dietary steatohepatitis in mice Hepatology 38 2003 123 132
34. X. Ge, L. Yin, H. Ma, T. Li, J.Y. Chiang, and Y. Zhang Aldo-keto reductase 1B7 is a target gene of FXR and regulates lipid and glucose homeostasis J Lipid Res 52 2011 1561 1568
35. H.R. Kast, C.M. Nguyen, C.J. Sinal, S.A. Jones, B.A. Laffitte, and K. Reue Farnesoid X-activated receptor induces apolipoprotein C-II transcription: a molecular mechanism linking plasma triglyceride levels to bile acids Mol Endocrinol 15 2001 1720 1728
36. J. Prawitt, M. Abdelkarim, J.H. Stroeve, I. Popescu, H. Duez, and V.R. Velagapudi Farnesoid × receptor deficiency improves glucose homeostasis in mouse models of obesity Diabetes 60 2011 1861 1871
37. T. Claudel, Y. Inoue, O. Barbier, D. Duran-Sandoval, V. Kosykh, and J. Fruchart Farnesoid X receptor agonists suppress hepatic apolipoprotein CIII expression Gastroenterology 125 2003 544 555
38. A. Sirvent, T. Claudel, G. Martin, J. Brozek, V. Kosykh, and R. Darteil The farnesoid X receptor induces very low density lipoprotein receptor gene expression FEBS Lett 566 2004 173 177
39. A.M. Anisfeld, H.R. Kast-Woelbern, M.E. Meyer, S.A. Jones, Y. Zhang, and K.J. Williams Syndecan-1 expression is regulated in an isoform-specific manner by the farnesoid-X receptor J Biol Chem 278 2003 20420 20428
40. I. Pineda Torra, T. Claudel, C. Duval, V. Kosykh, J.C. Fruchart, and B. Staels Bile acids induce the expression of the human peroxisome proliferator-activated receptor alpha gene via activation of the farnesoid X receptor Mol Endocrinol 17 2003 259 272
41. R.S. Savkur, K.S. Bramlett, L.F. Michael, and T.P. Burris Regulation of pyruvate dehydrogenase kinase expression by the farnesoid X receptor Biochem Biophys Res Commun 329 2005 391 396
42. T. Inagaki, P. Dutchak, G. Zhao, X. Ding, L. Gautron, and V. Parameswara Endocrine regulation of the fasting response by PPARalpha-mediated induction of fibroblast growth factor 21 Cell Metab 5 2007 415 425
43. H.A. Cyphert, X. Ge, A.B. Kohan, L.M. Salati, Y. Zhang, and F.B. Hillgartner Activation of the farnesoid X receptor induces hepatic expression and secretion of fibroblast growth factor 21 J Biol Chem 287 2012 25123 25138
44. T. Furihata, M. Hosokawa, T. Satoh, and K. Chiba Synergistic role of specificity proteins and upstream stimulatory factor 1 in transactivation of the mouse carboxylesterase 2/microsomal acylcarnitine hydrolase gene promoter Biochem J 384 2004 101 110
45. B. Konig, A. Koch, J. Spielmann, C. Hilgenfeld, F. Hirche, and G.I. Stangl Activation of PPARalpha and PPARgamma reduces triacylglycerol synthesis in rat hepatoma cells by reduction of nuclear SREBP-1 Eur J Pharmacol 605 2009 23 30
46. Y. Zhang, T. Lei, J.F. Huang, S.B. Wang, L.L. Zhou, and Z.Q. Yang The link between fibroblast growth factor 21 and sterol regulatory element binding protein 1c during lipogenesis in hepatocytes Mol Cell Endocrinol 342 2011 41 47
47. I. Kim, K. Morimura, Y. Shah, Q. Yang, J.M. Ward, and F.J. Gonzalez Spontaneous hepatocarcinogenesis in farnesoid X receptor-null mice Carcinogenesis 28 2007 940 946
48. Y. Zhang, X. Ge, L.A. Heemstra, W.D. Chen, J. Xu, and J.L. Smith Loss of FXR protects against diet-induced obesity and accelerates liver carcinogenesis in ob/ob mice Mol Endocrinol 26 2012 272 280
49. Y.D. Wang, W.D. Chen, M.H. Wang, D.N. Yu, B.M. Forman, and W.D. Huang Farnesoid X receptor antagonizes nuclear factor kappa B in hepatic inflammatory response Hepatology 48 2008 1632 1643
50. B. Kong, J.P. Luyendyk, O. Tawfik, and G.L. Guo Farnesoid X receptor deficiency induces nonalcoholic steatohepatitis in low-density lipoprotein receptor-knockout mice fed a high-fat diet J Pharmacol Exp Ther 328 2009 116 122
51. Z.X. Yang, W. Shen, and H. Sun Effects of nuclear receptor FXR on the regulation of liver lipid metabolism in patients with non-alcoholic fatty liver disease Hepatol Int 4 2010 741 748
52. L.P. Bechmann, P. Kocabayoglu, J.P. Sowa, S. Sydor, J. Best, and M. Schlattjan Free fatty acids repress small heterodimer partner (SHP) activation and adiponectin counteracts bile acid-induced liver injury in superobese patients with nonalcoholic steatohepatitis Hepatology 57 2013 1394 1406
53. T. Inagaki, M. Choi, A. Moschetta, L. Peng, C.L. Cummins, and J.G. McDonald Fibroblast growth factor 15 functions as an enterohepatic signal to regulate bile acid homeostasis Cell Metab 2 2005 217 225
54. S. Cipriani, A. Mencarelli, G. Palladino, and S. Fiorucci FXR activation reverses insulin resistance and lipid abnormalities and protects against liver steatosis in Zucker (fa/fa) obese rats J Lipid Res 51 2010 771 784
55. L. Adorini, M. Pruzanski, and D. Shapiro Farnesoid X receptor targeting to treat nonalcoholic steatohepatitis Drug Discov Today 17 2012 988 997
56. S. Mudaliar, R.R. Henry, A.J. Sanyal, L. Morrow, H.U. Marschall, and M. Kipnes Efficacy and safety of the farnesoid X receptor agonist obeticholic acid in patients with type 2 diabetes and nonalcoholic fatty liver disease Gastroenterology 145 3 2013 574 582
57. K. Yamagata, H. Daitoku, Y. Shimamoto, H. Matsuzaki, K. Hirota, and J. Ishida Bile acids regulate gluconeogenic gene expression via small heterodimer partner-mediated repression of hepatocyte nuclear factor 4 and Foxo1 J Biol Chem 279 2004 23158 23165
58. K. Ma, P.K. Saha, L. Chan, and D.D. Moore Farnesoid X receptor is essential for normal glucose homeostasis J Clin Investig 116 2006 1102 1109
59. M. Watanabe, Y. Horai, S.M. Houten, K. Morimoto, T. Sugizaki, and E. Arita Lowering bile acid pool size with a synthetic farnesoid X receptor (FXR) agonist induces obesity and diabetes through reduced energy expenditure J Biol Chem 286 2011 26913 26920
60. G. Rizzo, D. Passeri, F. De Franco, G. Ciaccioli, L. Donadio, and G. Rizzo Functional characterization of the semisynthetic bile acid derivative INT-767, a dual farnesoid X receptor and TGR5 agonist Mol Pharmacol 78 2010 617 630
61. M. Watanabe, S.M. Houten, C. Mataki, M.A. Christoffolete, B.W. Kim, and H. Sato Bile acids induce energy expenditure by promoting intracellular thyroid hormone activation Nature 439 2006 484 489
62. C. Thomas, A. Gioiello, L. Noriega, A. Strehle, J. Oury, and G. Rizzo TGR5-mediated bile acid sensing controls glucose homeostasis Cell Metab 10 2009 167 177
63. T.W. Pols, M. Nomura, T. Harach, G. Lo Sasso, M.H. Oosterveer, and C. Thomas TGR5 activation inhibits atherosclerosis by reducing macrophage inflammation and lipid loading Cell Metab 14 2011 747 757
64. S. Katsuma, A. Hirasawa, and G. Tsujimoto Bile acids promote glucagon-like peptide-1 secretion through TGR5 in a murine enteroendocrine cell line STC-1 Biochem Biophys Res Commun 329 2005 386 390
65. B.G. Talayero, and F.M. Sacks The role of triglycerides in atherosclerosis Curr Cardiol Rep 13 2011 544 552
66. V. Keitel, M. Donner, S. Winandy, R. Kubitz, and D. Haussinger Expression and function of the bile acid receptor TGR5 in Kupffer cells Biochem Biophys Res Commun 372 2008 78 84
67. Y. Kawamata, R. Fujii, M. Hosoya, M. Harada, H. Yoshida, and M. Miwa A G protein-coupled receptor responsive to bile acids J Biol Chem 278 2003 9435 9440
68. T. Yoshimura, C. Kurita, T. Nagao, E. Usami, T. Nakao, and S. Watanabe Inhibition of tumor necrosis factor-alpha and interleukin-1-beta production by beta-adrenoceptor agonists from lipopolysaccharide-stimulated human peripheral blood mononuclear cells Pharmacology 54 1997 144 152
69. Y.D. Wang, W.D. Chen, D. Yu, B.M. Forman, and W. Huang The G-protein-coupled bile acid receptor, Gpbar1 (TGR5), negatively regulates hepatic inflammatory response through antagonizing nuclear factor kappa light-chain enhancer of activated B cells (NF-kappaB) in mice Hepatology 54 2011 1421 1432
70. S. Cipriani, A. Mencarelli, M.G. Chini, E. Distrutti, B. Renga, and G. Bifulco The bile acid receptor GPBAR-1 (TGR5) modulates integrity of intestinal barrier and immune response to experimental colitis PLoS ONE 6 2011 e25637
71. V.Z. Rocha, and P. Libby Obesity, inflammation, and atherosclerosis Nat Rev Cardiol 6 2009 399 409
72. V. Keitel, R. Reinehr, P. Gatsios, C. Rupprecht, B. Gorg, and O. Selbach The G-protein coupled bile salt receptor TGR5 is expressed in liver sinusoidal endothelial cells Hepatology 45 2007 695 704
73. G. Baffy Kupffer cells in non-alcoholic fatty liver disease: the emerging view J Hepatol 51 2009 212 223
74. R.H. McMahan, X.X. Wang, L.L. Cheng, T. Krisko, M. Smith, and K. El Kasmi Bile acid receptor activation modulates hepatic monocyte activity and improves nonalcoholic fatty liver disease J Biol Chem 288 2013 11761 11770