Ezetimibe prevents cholesterol gallstone formation in mice

Liver International

Volumn 28, Issue 7, 2008, Pages 935-947

  Zúñiga, Silvia ^a   Molina, Héctor ^a   Azocar, Lorena ^a   Amigo, Ludwig ^a   Nervi, Flavio ^a   Pimentel, Fernando ^a   Jarufe, Nicolás ^a   Arrese, Marco ^a   Lammert, Frank ^b   Miquel, Juan F ^a  

^a PONTIFICIA UNIVERSIDAD CATÓLICA DE CHILE   (Chile)

^b SAARLAND UNIVERSITY   (Germany)

Author keywords

Biliary lipids; Cholesterol gallstones; Ezetimibe; Gall bladder

Indexed keywords

ABC TRANSPORTER; ABC TRANSPORTER G5; ABC TRANSPORTER G8; BILE SALT; EZETIMIBE; GLUTATHIONE; LIPID TRANSFER PROTEIN; NIEMAN PICK C1 LIKE 1 PROTEIN; PHOSPHOLIPID; SCAVENGER RECEPTOR BI;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; BILE FLOW; CHOLESTEROL BLOOD LEVEL; CHOLESTEROL LIVER LEVEL; CHOLESTEROL STONE; CLINICAL ARTICLE; CONTROLLED STUDY; DUODENUM; ENTEROHEPATIC CIRCULATION; HUMAN; HUMAN TISSUE; HYPERCHOLESTEROLEMIA; INTESTINE ABSORPTION; LIPID ABSORPTION; LIPID BILE LEVEL; LIVER WEIGHT; MALE; MOUSE; NONHUMAN; PROTEIN EXPRESSION;

ANIMALS; ANTICHOLESTEREMIC AGENTS; ANTIGENS, CD36; AZETIDINES; CHOLESTEROL; CHOLESTEROL, DIETARY; DISEASE MODELS, ANIMAL; DUODENUM; FEMALE; GALLSTONES; GENE EXPRESSION; HUMANS; INTESTINAL ABSORPTION; LIVER; MALE; MEMBRANE PROTEINS; MEMBRANE TRANSPORT PROTEINS; MICE; MICE, INBRED C57BL;

EID: 47949108449     PISSN: 14783223     EISSN: 14783231     Source Type: Journal    
DOI: 10.1111/j.1478-3231.2008.01808.x     Document Type: Article

References (50)

1. Paigen B, Carey MC. Gallstones. In: King RA, Rotter JI, Motulsky AG, eds. Genetic Basis of Common Diseases. New York: Oxford University Press, 2002; 298-335.
2. Carey MC. Pathogenesis of gallstones. Am J Surg 1993; 165: 410-9.
3. Lammert F, Sauerbruch T. Mechanisms of disease: The genetic epidemiology of gallbladder stones. Nat Clin Pract Gastroenterol Hepatol 2005; 2: 423-33.
4. Kern F Jr. Effects of dietary cholesterol on cholesterol and bile acid homeostasis in patients with cholesterol gallstones. J Clin Invest 1994; 93: 1186-94.
5. Amigo L, Quinones V, Mardones P, et al. Impaired biliary cholesterol secretion and decreased gallstone formation in apolipoprotein E-deficient mice fed a high-cholesterol diet. Gastroenterology 2000; 118: 772-9.
6. Buhman KK, Accad M, Novak S, et al. Resistance to diet-induced hypercholesterolemia and gallstone formation in ACAT2-deficient mice. Nat Med 2000; 6: 1341-7.
7. Wang HH, Wang DQ. Reduced susceptibility to cholesterol gallstone formation in mice that do not produce apolipoprotein B48 in the intestine. Hepatology 2005; 42: 894-904.
8. Meng CQ. Ezetimibe, Schering-Plough. Curr Opin Invest Drugs 2002; 3: 427-32.
9. Nutescu EA, Shapiro NL. Ezetimibe: A selective cholesterol absorption inhibitor. Pharmacotherapy 2003; 23: 1463-74.
10. Garcia-Calvo M, Lisnock J, Bull HG, et al. The target of ezetimibe is Niemann-Pick C1-like 1 (NPC1L1). Proc Natl Acad Sci USA 2005; 102: 8132-7.
11. Davis HR Jr, Zhu LJ, Hoos LM, et al. Niemann-Pick C1 like 1 (NPC1L1) is the intestinal phytosterol and cholesterol transporter and a key modulator of whole-body cholesterol homeostasis. J Biol Chem 2004; 279: 33586-92.
12. Altmann SW, Davis HR Jr, Zhu LJ, et al. Niemann-Pick C1 like 1 protein is critical for intestinal cholesterol absorption. Science 2004; 303: 1201-4.
13. Miquel JF, Moreno M, Amigo L, et al. Expression and regulation of scavenger receptor class B type I (SR-BI) in gall bladder epithelium. Gut 2003; 52: 1017-24.
14. Davis HR Jr, Compton DS, Hoos L, Tetzloff G. Ezetimibe, a potent cholesterol absorption inhibitor, inhibits the development of atherosclerosis in ApoE knockout mice. Arterioscler Thromb Vasc Biol 2001; 21: 2032-8.
15. Schwarz M, Russell DW, Dietschy JM, Turley SD. Marked reduction in bile acid synthesis in cholesterol 7alpha-hydroxylase-deficient mice does not lead to diminished tissue cholesterol turnover or to hypercholesterolemia. J Lipid Res 1998; 39: 1833-43.
16. Miettinen TA, Ahrens EH Jr, Grundy SM. Quantitative isolation and gas-liquid chromatographic analysis of total dietary and fecal neutral steroids. J Lipid Res 1965; 6: 411-24.
17. Turley SD, Daggy BP, Dietschy JM. Effect of feeding psyllium and cholestyramine in combination on low density lipoprotein metabolism and fecal bile acid excretion in hamsters with dietary-induced hypercholesterolemia. J Cardiovasc Pharmacol 1996; 27: 71-9.
18. Salisbury BG, Davis HR, Burrier RE, et al. Hypocholesterolemic activity of a novel inhibitor of cholesterol absorption, SCH 48461. Atherosclerosis 1995; 115: 45-63.
19. Moreno M, Molina H, Amigo L, et al. Hepatic overexpression of caveolins increases bile salt secretion in mice. Hepatology 2003; 38: 1477-88.
20. Moschetta A, Bookout AL, Mangelsdorf DJ. Prevention of cholesterol gallstone disease by FXR agonists in a mouse model. Nat Med 2004; 10: 1352-8.
21. Rigotti A, Trigatti BL, Penman M, Rayburn H, Herz J, Krieger M. A targeted mutation in the murine gene encoding the high density lipoprotein (HDL) receptor scavenger receptor class B type I reveals its key role in HDL metabolism. Proc Natl Acad Sci USA 1997; 94: 12610-5.
22. Nervi F, Marinovic I, Rigotti A, Ulloa N. Regulation of biliary cholesterol secretion. Functional relationship between the canalicular and sinusoidal cholesterol secretory pathways in the rat. J Clin Invest 1988; 82: 1818-25.
23. Holan KR, Holzbach RT, Hermann RE, Cooperman AM, Claffey WJ. Nucleation time: A key factor in the pathogenesis of cholesterol gallstone disease. Gastroenterology 1979; 77 (Part 1): 611-7.
24. Erranz B, Miquel JF, Argraves WS, Barth JL, Pimentel F, Marzolo MP. Megalin and cubilin expression in gallbladder epithelium and regulation by bile acids. J Lipid Res 2004; 45: 2185-98.
25. Pizarro M, Balasubramaniyan N, Solis N, et al. Bile secretory function in the obese Zucker rat: Evidence of cholestasis and altered canalicular transport function. Gut 2004; 53: 1837-43.
26. Ananthanarayanan M, Ng OC, Boyer JL, Suchy FJ. Characterization of cloned rat liver Na(+)-bile acid cotransporter using peptide and fusion protein antibodies. Am J Physiol 1994; 267 (Part 1): G637-43.
27. Gerloff T, Stieger B, Hagenbuch B, et al. The sister of P-glycoprotein represents the canalicular bile salt export pump of mammalian liver. J Biol Chem 1998; 273: 10046-50.
28. Yu L, Hammer RE, Li-Hawkins J, et al. Disruption of Abcg5 and Abcg8 in mice reveals their crucial role in biliary cholesterol secretion. Proc Natl Acad Sci USA 2002; 99: 16237-42.
29. Guo Q, Penman M, Trigatti BL, Krieger M. A single point mutation in epsilon-COP results in temperature-sensitive, lethal defects in membrane transport in a Chinese hamster ovary cell mutant. J Biol Chem 1996; 271: 11191-6.
30. Chomczynski P, Sacchi N. Single-step method of RNA isolation by acid guanidinium thiocyanate-phenol-chloroform extraction. Anal Biochem 1987; 162: 156-9.
31. Mardones P, Quinones V, Amigo L, et al. Hepatic cholesterol and bile acid metabolism and intestinal cholesterol absorption in scavenger receptor class B type I-deficient mice. J Lipid Res 2001; 42: 170-80.
32. Pfaffl MW, Horgan GW, Dempfle L. Relative expression software tool (REST) for group-wise comparison and statistical analysis of relative expression results in real-time PCR. Nucleic Acids Res 2002; 30: E36.
33. Repa JJ, Dietschy JM, Turley SD. Inhibition of cholesterol absorption by SCH 58053 in the mouse is not mediated via changes in the expression of mRNA for ABCA1, ABCG5, or ABCG8 in the enterocyte. J Lipid Res 2002; 43: 1864-74.
34. Van Erpecum KJ, Wang DQ, Moschetta A, et al. Gallbladder histopathology during murine gallstone formation: Relation to motility and concentrating function. J Lipid Res 2006; 47: 32-41.
35. Wang DQ, Tazuma S. Effect of beta-muricholic acid on the prevention and dissolution of cholesterol gallstones in C57L/J mice. J Lipid Res 2002; 43: 1960-8.
36. Figge A, Lammert F, Paigen B, et al. Hepatic overexpression of murine Abcb11 increases hepatobiliary lipid secretion and reduces hepatic steatosis. J Biol Chem 2004; 279: 2790-9.
37. Accatino L, Pizarro M, Solis N, Arrese M, Koenig CS. Bile secretory function after warm hepatic ischemia-reperfusion injury in the rat. Liver Transpl 2003; 9: 1199-210.
38. Fickert P, Zollner G, Fuchsbichler A, et al. Effects of ursodeoxycholic and cholic acid feeding on hepatocellular transporter expression in mouse liver. Gastroenterology 2001; 121: 170-83.
39. Yu L, York J, Von Bergmann K, Lutjohann D, Cohen JC, Hobbs HH. Stimulation of cholesterol excretion by the liver X receptor agonist requires ATP-binding cassette transporters G5 and G8. J Biol Chem 2003; 278: 15565-70.
40. Temel RE, Tang W, Ma Y, et al. Hepatic Niemann-Pick C1-like 1 regulates biliary cholesterol concentration and is a target of ezetimibe. J Clin Invest 2007; 117: 1968-78.
41. Van Heek M, France CF, Compton DS, et al. In vivo metabolism-based discovery of a potent cholesterol absorption inhibitor, SCH58235, in the rat and rhesus monkey through the identification of the active metabolites of SCH48461. J Pharmacol Exp Ther 1997; 283: 157-63.
42. Van Heek M, Farley C, Compton DS, Hoos L, Davis HR. Ezetimibe selectively inhibits intestinal cholesterol absorption in rodents in the presence and absence of exocrine pancreatic function. Br J Pharmacol 2001; 134: 409-17.
43. Sudhop T, Lutjohann D, Kodal A, et al. Inhibition of intestinal cholesterol absorption by ezetimibe in humans. Circulation 2002; 106: 1943-8.
44. Lyons MA, Wittenburg H. Cholesterol gallstone susceptibility loci: A mouse map, candidate gene evaluation, and guide to human LITH genes. Gastroenterology 2006;131: 1943-70.
45. Wang DQ, Zhang L, Wang HH. High cholesterol absorption efficiency and rapid biliary secretion of chylomicron remnant cholesterol enhance cholelithogenesis in gallstone-susceptible mice. Biochim Biophys Acta 2005; 1733: 90-9.
46. Yamanashi Y, Takada T, Suzuki H. Niemann-Pick C1-like 1 overexpression facilitates ezetimibe-sensitive cholesterol and beta-sitosterol uptake in CaCo-2 cells. J Pharmacol Exp Ther 2007; 320: 559-64.
47. Wang DQ, Schmitz F, Kopin AS, Carey MC. Targeted disruption of the murine cholecystokinin-1 receptor promotes intestinal cholesterol absorption and susceptibility to cholesterol cholelithiasis. J Clin Invest 2004; 114: 521-8.
48. Ito S, Fujimori T, Furuya A, Satoh J, Nabeshima Y. Impaired negative feedback suppression of bile acid synthesis in mice lacking betaKlotho. J Clin Invest 2005; 115: 2202-8.
49. Corradini SG, Elisei W, Giovannelli L, et al. Impaired human gallbladder lipid absorption in cholesterol gallstone disease and its effect on cholesterol solubility in bile. Gastroenterology 2000; 118: 912-20.
50. Mathur A, Walker JJ, Al-Azzawi HH, et al. Ezetimibe ameliorates cholecystosteatosis. Surgery 2007; 142: 228-33.