Hypolipidemic action of the SERM acolbifene is associated with decreased liver MTP and increased SR-BI and LDL receptors

Journal of Lipid Research

Volumn 46, Issue 6, 2005, Pages 1285-1294

  Lemieux, Christian ^a   Gélinas, Yves ^a   Lalonde, Josée ^a   Labrie, Fernand ^b   Cianflone, Katherine ^c   Deshaies, Yves ^a  

^a LAVAL UNIVERSITY   (Canada)

^b UNIVERSITÉ LAVAL   (Canada)

^c ROYAL VICTORIA HOSPITAL   (Canada)

Author keywords

Cholesterol; Hypocholesterolemic drug; Liver lipoprotein receptors; Low density lipoprotein receptor; Microsomal triglyceride transfer protein; Scavenger receptor class B type I; Selective estrogen receptor modulator; Triglycerides

Indexed keywords

ACOLBIFENE; ANTILIPEMIC AGENT; HIGH DENSITY LIPOPROTEIN; HIGH DENSITY LIPOPROTEIN CHOLESTEROL; HYDROXYMETHYLGLUTARYL COENZYME A REDUCTASE; LOW DENSITY LIPOPROTEIN RECEPTOR; MESSENGER RNA; MICROSOMAL TRIGLYCERIDE TRANSFER PROTEIN; SCAVENGER RECEPTOR BI; SELECTIVE ESTROGEN RECEPTOR MODULATOR; STEROL REGULATORY ELEMENT BINDING PROTEIN 1A; STEROL REGULATORY ELEMENT BINDING PROTEIN 1C; STEROL REGULATORY ELEMENT BINDING PROTEIN 2; TRIACYLGLYCEROL; UNCLASSIFIED DRUG; VERY LOW DENSITY LIPOPROTEIN; VERY LOW DENSITY LIPOPROTEIN CHOLESTEROL; CARRIER PROTEIN; CCAAT ENHANCER BINDING PROTEIN; CD36 ANTIGEN; CHOLESTEROL; DNA BINDING PROTEIN; IMMUNOGLOBULIN RECEPTOR; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR ALPHA; PIPERIDINE DERIVATIVE; RITETRONIUM; SCARB1 PROTEIN, RAT; SCAVENGER RECEPTOR; SCAVENGER RECEPTOR B; SREBF1 PROTEIN, RAT; STEROL REGULATORY ELEMENT BINDING PROTEIN 1; TRANSCRIPTION FACTOR;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; CONTROLLED STUDY; CORRELATION ANALYSIS; DIET RESTRICTION; FEMALE; GLUCOSE BLOOD LEVEL; HYPOCHOLESTEROLEMIA; LIVER CIRCULATION; NONHUMAN; NUTRITIONAL STATUS; PRIORITY JOURNAL; RAT; TIME SERIES ANALYSIS; TRIACYLGLYCEROL BLOOD LEVEL; ANIMAL; BLOOD; FOOD DEPRIVATION; KINETICS; LIPID METABOLISM; LIVER; METABOLISM; SPRAGUE DAWLEY RAT; TIME; WESTERN BLOTTING;

ANIMALS; ANTIGENS, CD36; BLOTTING, WESTERN; CARRIER PROTEINS; CCAAT-ENHANCER-BINDING PROTEINS; CHOLESTEROL; DNA-BINDING PROTEINS; FEMALE; FOOD DEPRIVATION; HYDROXYMETHYLGLUTARYL COA REDUCTASES; KINETICS; LIPID METABOLISM; LIVER; PIPERIDINES; PPAR ALPHA; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, IMMUNOLOGIC; RECEPTORS, LDL; RECEPTORS, SCAVENGER; RNA, MESSENGER; SCAVENGER RECEPTORS, CLASS B; SELECTIVE ESTROGEN RECEPTOR MODULATORS; STEROL REGULATORY ELEMENT BINDING PROTEIN 1; TIME FACTORS; TRANSCRIPTION FACTORS; TRIGLYCERIDES;

EID: 24744442832     PISSN: 00222275     EISSN: 15397262     Source Type: Journal    
DOI: 10.1194/jlr.M400448-JLR200     Document Type: Article

References (65)

1. Rossouw, J. E., G. L. Anderson, R. L. Prentice, A. Z. LaCroix, C. Kooperberg, M. L. Stefanick, R. D. Jackson, S. A. Beresford, B. V. Howard, K. C. Johnson, et al. 2002. Risks and benefits of estrogen plus progestin in healthy postmenopausal women: principal results from the Women's Health Initiative randomized controlled trial. J. Am. Med. Assoc. 288: 321-333.
2. Kuller, L. H. 2003. Hormone replacement therapy and risk of cardiovascular disease: implications of the results of the Women's Health Initiative. Arterioscler. Thromb. Vasc. Biol. 23: 11-16.
3. Alving, B. NIH asks participants in Women's Health Initiative Estrogen-Alone Study to stop study pills, begin follow-up phase. NIH News. March 2, 2004. www.nhlbi.nih.gov/new/press/04-03-02.htm.
4. Labrie, F., C. Labrie, A. Bélanger, J. Simard, S. Gauthier, V. Luu-The, Y. Mérand, V. Giguère, B. Candas, S. Luo, et al. 1999. EM-652 (SCH 57068), a third generation SERM acting as pure antiestrogen in the mammary gland and endometrium. J. Steroid Biochem. Mol. Biol. 69: 51-84.
5. Labrie, F., C. Labrie, A. Belanger, J. Simard, V. Giguere, A. Tremblay, and G. Tremblay. 2001. EM-652 (SCH57068), a pure SERM having complete antiestrogenic activity in the mammary gland and endometrium. J. Steroid Biochem. Mol. Biol. 79: 213-225.
6. Tremblay, A., G. B. Tremblay, C. Labrie, F. Labrie, and V. Giguère. 1998. EM-800, a novel antiestrogen, acts as a pure antagonist of the transcriptional functions of estrogen receptors alpha and beta. Endocrinology. 139: 111-118.
7. Luo, S., A. Sourla, C. Labrie, A. Bélanger, and F. Labrie. 1997. Combined effects of dehydroepiandrosterone and EM-800 on bone mass, serum lipids, and the development of dimethylbenz(A)anthracene-induced mammary carcinoma in the rat. Endocrinology. 138: 4435-4444.
8. Luo, S., C. Labrie, A. Bélanger, B. Candas, and F. Labrie. 1998. Prevention of development of dimethylbenz(a)anthracene (DMBA)-induced mammary tumors in the rat by the new nonsteroidal antiestrogen EM-800 (SCH57050). Breast Cancer Res. Treat. 49: 1-11.
9. Lemieux, C., F. Picard, F. Labrie, D. Richard, and Y. Deshaies. 2003. The estrogen antagonist EM-652 and dehydroepiandrosterone prevent diet- and ovariectomy-induced obesity. Obes. Res. 11: 477-490.
10. Picard, F., Y. Deshaies, J. Lalonde, P. Samson, C. Labrie, A. Bélanger, F. Labrie, and D. Richard. 2000. Effects of the estrogen antagonist EM-652.HCl on energy balance and lipid metabolism in ovariectomized rats. Int. J. Obes. Relat. Metab. Disord. 24: 830-840.
11. Gray, J. M., S. Schrock, and M. Bishop. 1993. Estrogens and antiestrogens: actions and interactions with fluphenazine on food intake and body weight in rats. Am. J. Physiol. Regul. Integr. Comp. Physiol. 264: R1214-R1218.
12. Sato, M., M. K. Rippy, and H. U. Bryant. 1996. Raloxifene, tamoxifen, nafoxidine, or estrogen effects on reproductive and nonreproductive tissues in ovariectomized rats. FASEB J. 10: 905-912.
13. Wade, G. N., J. D. Blaustein, J. M. Gray, and J. M. Meredith. 1993. ICI-182,780: a pure antiestrogen that affects behaviors and energy balance in rats without acting in the brain. Am. J. Physiol. Regul. Integr. Comp. Physiol. 265: R1392-R1398.
14. Wade, G. N., and H. W. Heller. 1993. Tamoxifen mimics the effects of estradiol on food intake, body weight, and body composition in rats. Am. J. Physiol. Regul. Integr. Comp. Physiol. 264: R1219-R1223.
15. Ke, H. Z., V. M. Paralkar, W. A. Grasser, D. T. Crawford, H. Qi, H. A. Simmons, C. M. Pirie, K. L. Chidsey-Frink, T. A. Owen, S. L. Smock, et al. 1998. Effects of CP-336,156, a new, nonsteroidal estrogen agonist/ antagonist, on bone, serum cholesterol, uterus and body composition in rat models. Endocrinology. 139: 2068-2076.
16. Cleary, M. P. 1991. The antiobesity effect of dehydroepiandrosterone in rats. Proc. Soc. Exp. Biol. Med. 196: 8-16.
17. Berdanier, C. D., J. A. Parente, and M. K. McIntosh. 1993. Is dehydroepiandrosterone an antiobesity agent? FASEB J. 7: 414-419.
18. Lea-Currie, Y. R., S. M. Wu, and M. K. McIntosh. 1997. Effects of acute administration of dehydroepiandrosterone-sulfate on adipose tissue mass and cellularity in male rats. Int. J. Obes. Relat. Metab. Disord. 21: 147-154.
19. Mauriège, P., D. Langin, V. Montminy, C. Martel, J-P. Després, A. Bélanger, F. Labrie, and Y. Deshaies. 2000. Effect of a long-term percutaneous adrenal steroid treatment on rat adipose tissue metabolism. Int. J. Obes. Relat. Metab. Dis. 24 (Suppl. 1): 1-3.
20. Knopp, R. H., X. D. Zhu, and B. Bonet. 1994. Effects of estrogens on lipoprotein metabolism and cardiovascular disease in women. Atherosclerosis. 110 (Suppl.): 83-91.
21. Parini, P., B. Angelin, A. Stavreus-Evers, B. Freyschuss, H. Eriksson, and M. Rudling. 2000. Biphasic effects of the natural estrogen 17β-estradiol on hepatic cholesterol metabolism in intact female rats. Arterioscler. Thromb. Vasc. Biol. 20: 1817-1823.
22. Parini, P., B. Angelin, and M. Rudling. 1997. Importance of estrogen receptors in hepatic LDL receptor regulation. Arterioscler. Thromb. Vasc. Biol. 17: 1800-1805.
23. Acton, S., A. Rigotti, K. T. Landschulz, S. Xu, H. H. Hobbs, and M. Krieger. 1996. Identification of scavenger receptor SR-BI as a high density lipoprotein receptor. Science. 271: 518-520.
24. Krieger, M. 1999. Charting the fate of the "good cholesterol": identification and characterization of the high-density lipoprotein receptor SR-BI. Annu. Rev. Biochem. 68: 523-558.
25. Trigatti, B. L., M. Krieger, and A. Rigotti. 2003. Influence of the HDL receptor SR-BI on lipoprotein metabolism and atherosclerosis. Arterioscler. Thromb. Vasc. Biol. 23: 1732-1738.
26. Rigotti, A., H. E. Miettinen, and M. Krieger. 2003. The role of the high-density lipoprotein receptor SR-BI in the lipid metabolism of endocrine and other tissues. Endocr. Rev. 24: 357-387.
27. Silver, D. L., and A. R. Tall. 2001. The cellular biology of scavenger receptor class B type I. Curr. Opin. Lipidol. 12: 497-504.
28. Trigatti, B., A. Rigotti, and M. Krieger. 2000. The role of the highdensity lipoprotein receptor SR-BI in cholesterol metabolism. Curr. Opin. Lipidol. 11: 123-131.
29. Landschulz, K. T., R. K. Pathak, A. Rigotti, M. Krieger, and H. H. Hobbs. 1996. Regulation of scavenger receptor, class B, type I, a high density lipoprotein receptor, in liver and steroidogenic tissues of the rat. J. Clin. Invest. 98: 984-995.
30. Stangl, H., G. A. Graf, L. Yu, G. Cao, and K. Wyne. 2002. Effect of estrogen on scavenger receptor BI expression in the rat. J. Endocrinol. 175: 663-672.
31. Deshaies, Y., A. Géloën, A. Paulin, and L. J. Bukowiecki. 1991. Restoration of lipoprotein lipase activity in insulin-deficient rats by insulin infusion is tissue-specific. Can. J. Physiol. Pharmacol. 69: 746-751.
32. Matthews, D. R., J. P. Hosker, A. S. Rudenski, B. A. Naylor, D. F. Treacher, and R. C. Turner. 1985. Homeostasis model assessment: insulin resistance and beta-cell function from fasting plasma glucose and insulin concentrations in man. Diabetologia. 28: 412-419.
33. Otway, S., and D. S. Robinson. 1967. The use of a non-ionic detergent (Triton WR 1339) to determine rates of triglyceride entry into the circulation of the rat under different physiological conditions. J. Physiol. 190: 321-332.
34. Cohen, J. C. 1989. Chylomicron triglyceride clearance: comparison of three assessment methods. Am. J. Clin. Nutr. 49: 306-313.
35. Folch, J., M. Lees, and G. H. Sloane Stanley. 1957. A simple method for the isolation and purification of total lipides from animal tissues. J. Biol. Chem. 226: 497-509.
36. Lowry, O. H., N. J. Rosebrough, A. L. Farr, and R. J. Randall. 1951. Protein measurement with the Folin phenol reagent. J. Biol. Chem. 193: 265-275.
37. Shimomura, I., Y. Bashmakov, S. Ikemoto, J. D. Horton, M. S. Brown, and J. L. Goldstein. 1999. Insulin selectively increases SREBP-1c mRNA in the livers of rats with streptozotocin-induced diabetes. Proc. Natl. Acad. Sci. USA. 96: 13656-13661.
38. Erickson, S. K., and P. E. Fielding. 1986. Parameters of cholesterol metabolism in the human hepatoma cell line, Hep-G2. J. Lipid Res. 27: 875-883.
39. Huff, M. W., D. E. Telford, P. H. Barrett, J. T. Billheimer, and P. J. Gillies. 1994. Inhibition of hepatic ACAT decreases apoB secretion in miniature pigs fed a cholesterol-free diet. Arterioscler. Thromb. 14: 1498-1508.
40. Tofovic, S. P., R. K. Dubey, and E. K. Jackson. 2001. 2-Hydroxyestradiol attenuates the development of obesity, the metabolic syndrome, and vascular and renal dysfunction in obese ZSF1 rats. J. Pharmacol. Exp. Ther. 299: 973-977.
41. Després, J-P. 1998. The insulin resistance-dyslipidemic syndrome of visceral obesity: effect on patients' risk. Obes. Res. 6 (Suppl. 1): 8-17.
42. Kelley, M. J., and J. A. Story. 1985. Effect of type of diet and feeding status on modulation of hepatic HMG-CoA reductase in rats. Lipids. 20: 53-55.
43. Helgerud, P., R. Haugen, and K. R. Norum. 1982. The effect of feeding and fasting on the activity of acyl-CoA:cholesterol acyltransferase in rat small intestine. Eur. J. Clin. Invest. 12: 493-500.
44. Erickson, S. K., M. A. Shrewsbury, C. Brooks, and D. J. Meyer. 1980. Rat liver acyl-coenzyme A:cholesterol acyltransferase: its regulation in vivo and some of its properties in vitro. J. Lipid Res. 21: 930-941.
45. Shimano, H., N. Yahagi, M. Amemiya-Kudo, A. H. Hasty, J. Osuga, Y. Tamura, F. Shionoiri, Y. Iizuka, K. Ohashi, K. Harada, et al. 1999. Sterol regulatory element-binding protein-1 as a key transcription factor for nutritional induction of lipogenic enzyme genes. J. Biol. Chem. 274: 35832-35839.
46. Horton, J. D., Y. Bashmakov, I. Shimomura, and H. Shimano. 1998. Regulation of sterol regulatory element binding proteins in livers of fasted and refed mice. Proc. Natl. Acad. Sci. USA. 95: 5987-5992.
47. Krauss, R. M., and R. T. Burkman. 1992. The metabolic impact of oral contraceptives. Am. J. Obstet. Gynecol. 167: 1177-1184.
48. Wetterau, J. R., R. E. Gregg, T. W. Harrity, C. Arbeeny, M. Cap, F. Connolly, C. H. Chu, R. J. George, D. A. Gordon, H. Jamil, et al. 1998. An MTP inhibitor that normalizes atherogenic lipoprotein levels in WHHL rabbits. Science. 282: 751-754.
49. Lewis, G. F., A. Carpentier, K. Adeli, and A. Giacca. 2002. Disordered fat storage and mobilization in the pathogenesis of insulin resistance and type 2 diabetes. Endocr. Rev. 23: 201-229.
50. Borradaile, N. M., L. E. de Dreu, L. J. Wilcox, J. Y. Edwards, and M. W. Huff. 2002. Soya phytoestrogens, genistein and daidzein, decrease apolipoprotein B secretion from HepG2 cells through multiple mechanisms. Biochem. J. 366: 531-539.
51. Simoncini, T., G. Varone, L. Fornari, P. Mannella, M. Luisi, F. Labrie, and A. R. Genazzani. 2002. Genomic and nongenomic mechanisms of nitric oxide synthesis induction in human endothelial cells by a fourth-generation selective estrogen receptor modulator. Endocrinology. 143: 2052-2061.
52. Tatchum-Talom, R., C. Martel, F. Labrie, and A. Marette. 2003. Acute vascular effects of the selective estrogen receptor modulator EM-652 (SCH 57068) in the rat mesenteric vascular bed. Cardiovasc. Res. 57: 535-543.
53. Neuschwander-Tetri, B. A., and S. H. Caldwell. 2003. Nonalcoholic steatohepatitis: summary of an AASLD Single Topic Conference. Hepatology. 37: 1202-1219.
54. Kovanen, P. T., M. S. Brown, and J. L. Goldstein. 1979. Increased binding of low density lipoprotein to liver membranes from rats treated with 17 alpha-ethinyl estradiol. J. Biol. Chem. 254: 11367-11373.
55. Windler, E. E., P. T. Kovanen, Y. S. Chao, M. S. Brown, R. J. Havel, and J. L. Goldstein. 1980. The estradiol-stimulated lipoprotein receptor of rat liver. A binding site that membrane mediates the uptake of rat lipoproteins containing apoproteins B and E. J. Biol. Chem. 255: 10464-10471.
56. Bertolotti, M., and D. K. Spady. 1996. Effect of hypocholesterolemic doses of 17 alpha-ethinyl estradiol on cholesterol balance in liver and extrahepatic tissues. J. Lipid Res. 37: 1812-1822.
57. Fluiter, K., D. R. van der Westhuijzen, and T. J. van Berkel. 1998. In vivo regulation of scavenger receptor BI and the selective uptake of high density lipoprotein cholesteryl esters in rat liver parenchymal and Kupffer cells. J. Biol. Chem. 273: 8434-8438.
58. Goldstein, J. L., and M. S. Brown. 1990. Regulation of the mevalonate pathway. Nature. 343: 425-430.
59. Lopez, D., and M. P. McLean. 1999. Sterol regulatory elementbinding protein-1a binds to cis elements in the promoter of the rat high density lipoprotein receptor SR-BI gene. Endocrinology. 140: 5669-5681.
60. Ness, G. C., Z. Zhao, and D. Lopez. 1996. Inhibitors of cholesterol biosynthesis increase hepatic low-density lipoprotein receptor protein degradation. Arch. Biochem. Biophys. 325: 242-248.
61. Roach, P. D., S. Balasubramaniam, F. Hirata, M. Abbey, A. Szanto, L. A. Simons, and P. J. Nestel. 1993. The low-density lipoprotein receptor and cholesterol synthesis are affected differently by dietary cholesterol in the rat. Biochim. Biophys. Acta. 1170: 165-172.
62. Srivastava, R. A., D. Baumann, and G. Schonfeld. 1993. In vivo regulation of low-density lipoprotein receptors by estrogen differs at the post-transcriptional level in rat and mouse. Eur. J. Biochem. 216: 527-538.
63. Sérougne, C., C. Feurgard, T. Hajri, G. Champarnaud, J. Férézou, D. Mathé, and C. Lutton. 1999. Catabolism of HDL1 cholesteryl ester in the rat. Effect of ethinyl estradiol treatment. C. R. Acad. Sci. III. 322: 591-596.
64. Pittman, R. C., and D. Steinberg. 1984. Sites and mechanisms of uptake and degradation of high density and low density lipoproteins. J. Lipid Res. 25: 1577-1585.
65. Zak, Z., L. Lagrost, T. Gautier, D. Masson, V. Deckert, L. Duverneuil, J. P. De Barros, N. Le Guern, L. Dumont, M. Schneider, et al. 2002. Expression of simian CETP in normolipidemic Fisher rats has a profound effect on large sized apoE-containing HDL. J. Lipid Res. 43: 2164-2171.