Importance of acyl-coenzyme A:cholesterol acyltransferase 1/2 dual inhibition for anti-atherosclerotic potency of pactimibe

European Journal of Pharmacology

Volumn 540, Issue 1-3, 2006, Pages 121-130

  Kitayama, Ken ^a   Tanimoto, Tatsuo ^a   Koga, Teiichiro ^b   Terasaka, Naoki ^a   Fujioka, Tomoyuki ^a   Inaba, Toshimori ^a  

^a DAIICHI SANKYO CO   (Japan)

^b Sankyo Pharma Research Institute   (United States)

Author keywords

ACAT (Acyl coenzyme A:cholesterol acyltransferase); Atherosclerosis; Hypercholesterolemia; Pactimibe

Indexed keywords

ACYL COENZYME A; AVASIMIBE; CHOLESTEROL ACYLTRANSFERASE INHIBITOR; CHOLESTEROL ESTER; LOW DENSITY LIPOPROTEIN; PACTIMIBE; PROBUCOL;

ANALYTIC METHOD; ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; ATHEROGENIC DIET; ATHEROSCLEROSIS; CONTROLLED STUDY; DRUG POTENCY; HAMSTER; HUMAN; HUMAN CELL; HYPERCHOLESTEROLEMIA; HYPERLIPIDEMIA; IC 50; INHIBITION KINETICS; MACROPHAGE; MALE; NONHUMAN; OXIDATION; PRIORITY JOURNAL; RAT;

ACYL COENZYME A; ANIMALS; ANTILIPEMIC AGENTS; ARTERIOSCLEROSIS; CATALYSIS; CELL LINE; CELL-FREE SYSTEM; CHOLESTEROL ESTERS; CRICETINAE; DIET, ATHEROGENIC; DOSE-RESPONSE RELATIONSHIP, DRUG; HUMANS; HYPERCHOLESTEROLEMIA; HYPOLIPIDEMIC AGENTS; INDOLEACETIC ACIDS; LIPIDS; LIPOPROTEINS, LDL; MACROPHAGES; MONOCYTES; OXIDATION-REDUCTION; PHOSPHATIDYLCHOLINE-STEROL O-ACYLTRANSFERASE; RABBITS; RATS; RATS, SPRAGUE-DAWLEY; STEROL O-ACYLTRANSFERASE;

EID: 33744971569     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ejphar.2006.04.022     Document Type: Article

References (60)

1. Anderson R.A., Joyce C., Davis M., Reagan J.W., Clark M., Shelness G.S., and Rudel L.L. Identification of a form of acyl-CoA:cholesterol acyltransferase specific to liver and intestine in nonhuman primates. J. Biol. Chem. 273 (1998) 26747-26754
2. Bar-Tana J., and Shapiro B. Long-chain fatty acyl-CoA synthetase from rat liver microsomes. EC 6.2.1.3 fatty acyl-CoA ligase (ATP). Methods Enzymol. 35 (1975) 117-122
3. Bradford M.M. A rapid and sensitive method for the quantitation of microgram quantities of protein utilizing the principle of protein-dye binding. Anal. Biochem. 72 (1976) 248-254
4. Brown M.S., Goldstein J.L., Krieger M., Ho Y.K., and Anderson R.G. Reversible accumulation of cholesteryl esters in macrophages incubated with acetylated lipoproteins. J. Cell Biol. 82 (1979) 597-613
5. Buhman K.F., Accad M., and Farese R.V. Mammalian acyl-CoA:cholesterol acyltransferases. Biochim. Biophys. Acta 1529 (2000) 142-154
6. Buhman K.K., Chen H.C., and Farese Jr. R.V. The enzymes of neutral lipid synthesis. J. Biol. Chem. 276 (2001) 40369-40372
7. Burnett J.R., Wilcox L.J., Telford D.E., Kleinstiver S.J., Barrett P.H., Newton R.S., and Huff M.W. Inhibition of ACAT by avasimibe decreases both VLDL and LDL apolipoprotein B production in miniature pigs. J. Lipid Res. 40 (1999) 1317-1327
8. Carew T.E., Schwenke D.C., and Steinberg D. Antiatherogenic effect of probucol unrelated to its hypocholesterolemic effect: evidence that antioxidants in vivo can selectively inhibit low density lipoprotein degradation in macrophage-rich fatty streaks and slow the progression of atherosclerosis in the Watanabe heritable hyperlipidemic rabbit. Proc. Natl. Acad. Sci. U. S. A. 84 (1987) 7725-7729
9. Cases S., Novak S., Zheng Y.W., Myers H.M., Lear S.R., Sande E., Welch C.B., Lusis A.J., Spencer T.A., Krause B.R., Erickson S.K., and Farese Jr. R.V. ACAT-2, a second mammalian acyl-CoA:cholesterol acyltransferase. Its cloning, expression, and characterization. J. Biol. Chem. 273 (1998) 26755-26764
10. Chang C.C., Huh H.Y., Cadigan K.M., and Chang T.Y. Molecular cloning and functional expression of human acyl-coenzyme A:cholesterol acyltransferase cDNA in mutant Chinese hamster ovary cells. J. Biol. Chem. 268 (1993) 20747-20755
11. Chang T.Y., Chang C.C., Lin S., Yu C., Li B.L., and Miyazaki A. Roles of acyl-coenzyme A:cholesterol acyltransferase-1 and -2. Curr. Opin. Lipidol. 12 (2001) 289-296
12. Cho K.H., An S., Lee W.S., Paik Y.K., Kim Y.K., and Jeong T.S. Mass-production of human ACAT-1 and ACAT-2 to screen isoform-specific inhibitor: a different substrate specificity and inhibitory regulation. Biochem. Biophys. Res. Commun. 309 (2003) 864-872
13. Davies M.J. Stability and instability: two faces of coronary atherosclerosis. The Paul Dudley White Lecture 1995. Circulation 94 (1996) 2013-2020
14. Doolittle G.M., and Chang T.Y. Solubilization, partial purification, and reconstitution in phosphatidylcholine-cholesterol liposomes of acyl-CoA:cholesterol acyltransferase. Biochemistry 21 (1982) 674-679
15. Edelson P.J., and Cohn Z.A. Effects of concanavalin A on mouse peritoneal macrophages. I. Stimulation of endocytic activity and inhibition of phago-lysosome formation. J. Exp. Med. 140 (1974) 1364-1386
16. Faggiotto A., and Ross R. Studies of hypercholesterolemia in the nonhuman primate. II. Fatty streak conversion to fibrous plaque. Arteriosclerosis 4 (1984) 341-356
17. Faggiotto A., Ross R., and Harker L. Studies of hypercholesterolemia in the nonhuman primate. I. Changes that lead to fatty streak formation. Arteriosclerosis 4 (1984) 323-340
18. Falk E., Shah P.K., and Fuster V. Coronary plaque disruption. Circulation 92 (1995) 657-671
19. Fazio S., Major A.S., Swift L.L., Gleaves L.A., Accad M., Linton M.F., and Farese Jr. R.V. Increased atherosclerosis in LDL receptor-null mice lacking ACAT1 in macrophages. J. Clin. Invest. 107 (2001) 163-171
20. Folch J., Lees M., and Sloane Stanley G.H. A simple method for the isolation and purification of total lipids from animal tissues. J. Biol. Chem. 226 (1957) 497-509
21. Fujioka T., Tsujita Y., and Shimotsu H. Induction of fatty acid synthesis by pravastatin sodium in rat liver and primary hepatocytes. Eur. J. Pharmacol. 328 (1997) 235-239
22. Hainer J.W., Terry J.G., Connell J.M., Zyruk H., Jenkins R.M., Shand D.L., Gillies P.J., Livak K.J., Hunt T.L., and Crouse III J.R. Effect of the acyl-CoA:cholesterol acyltransferase inhibitor DuP 128 on cholesterol absorption and serum cholesterol in humans. Clin. Pharmacol. Ther. 56 (1994) 65-74
23. Harris W.S., Dujovne C.A., von Bergmann K., Neal J., Akester J., Windsor S.L., Greene D., and Look Z. Effects of the ACAT inhibitor CL 277,082 on cholesterol metabolism in humans. Clin. Pharmacol. Ther. 48 (1990) 189-194
24. Hatch F.T. Practical methods for plasma lipoprotein analysis. Adv. Lipid Res. 6 (1968) 1-68
25. Havel R.J., Eder H.A., and Bragdon J.H. The distribution and chemical composition of ultracentrifugally separated lipoproteins in human serum. J. Clin. Invest. 34 (1955) 1345-1353
26. Insull Jr. W., Koren M., Davignon J., Sprecher D., Schrott H., Keilson L.M., Brown A.S., Dujovne C.A., Davidson M.H., McLain R., and Heinonen T. Efficacy and short-term safety of a new ACAT inhibitor, avasimibe, on lipids, lipoproteins, and apolipoproteins, in patients with combined hyperlipidemia. Atherosclerosis 157 (2001) 137-144
27. Ishi M., Tomono Y., Sanma H., Yamoto C., Sekino H., Nomura M., and Nakaya N. Pharmacokinetics of novel ACAT inhibitor E5324, in healthy volunteers. Atherosclerosis 109 (1994) 283 (253-Abs)
28. Ishii I., Oka M., Katto N., Shirai K., Saito Y., and Hirose S. Beta-VLDL-induced cholesterol ester deposition in macrophages may be regulated by neutral cholesterol esterase activity. Arterioscler. Thromb. 12 (1992) 1139-1145
29. Kashiwa M., Masuyama Y., Miyauchi H., Uchida T., Naganuma S., Kakuta H., Terada M., Kiriyama T., Matsuda K., Ito N., Iizumi Y., and Takenaka T. Pharmacological properties of YM17E, an acyl-CoA:cholesterol acyltransferase inhibitor, and diarrheal effect in beagle dogs. Jpn. J. Pharmacol. 73 (1997) 41-50
30. Kleinveld H.A., Hak-Lemmers H.L., Stalenhoef A.F., and Demacker P.N. Improved measurement of low-density-lipoprotein susceptibility to copper-induced oxidation: application of a short procedure for isolating low-density lipoprotein. Clin. Chem. 38 (1992) 2066-2072
31. Kowala M.C., Mazzucco C.E., Hartl K.S., Seiler S.M., Warr G.A., Abid S., and Grove R.I. Prostacyclin agonists reduce early atherosclerosis in hyperlipidemic hamsters. Octimibate and BMY 42393 suppress monocyte chemotaxis, macrophage cholesteryl ester accumulation, scavenger receptor activity, and tumor necrosis factor production. Arterioscler. Thromb. 13 (1993) 435-444
32. Kris-Etherton P.M., and Dietschy J. Design criteria for studies examining individual fatty acid effects on cardiovascular disease risk factors: human and animal studies. Am. J. Clin. Nutr. 65 (1997) 1590S-1596S
33. Kuroda M., and Endo A. Inhibition of in vitro cholesterol synthesis by fatty acids. Biochim. Biophys. Acta 486 (1976) 70-81
34. Lee H.T., Sliskovic D.R., Picard J.A., Roth B.D., Wierenga W., Hicks J.L., Bousley R.F., Hamelehle K.L., Homan R., Speyer C., Stanfield R.L., and Krause B.R. Inhibitors of acyl-CoA: cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. CI-1011: an acyl sulfamate with unique cholesterol-lowering activity in animals fed noncholesterol-supplemented diets. J. Med. Chem. 39 (1996) 5031-5034
35. Libby P. Molecular bases of the acute coronary syndromes. Circulation 91 (1995) 2844-2850
36. Matsuo M., Hashimoto M., Suzuki J., Iwanami K., Tomoi M., and Shimomura K. Difference between normal and WHHL rabbits in susceptibility to the adrenal toxicity of an acyl-CoA:cholesterol acyltransferase inhibitor, FR145237. Toxicol. Appl. Pharmacol. 140 (1996) 387-392
37. Nakaya N., Nakamichi N., Sekino H., Nomura M., Ishii M., Tomono Y., and Yamato C. Effect of a novel ACAT inhibitor, E5324, on serum lipids and lipoproteins in healthy volunteers. Atherosclerosis 109 (1994) 284 (253-Abs)
38. Nilsson-Ehle P., and Schotz M.C. A stable, radioactive substrate emulsion for assay of lipoprotein lipase. J. Lipid Res. 17 (1976) 536-541
39. Oelkers P., Behari A., Cromley D., Billheimer J.T., and Sturley S.L. Characterization of two human genes encoding acyl coenzyme A:cholesterol acyltransferase-related enzymes. J. Biol. Chem. 273 (1998) 26765-26771
40. Prasad K., and Kalra J. Oxygen free radicals and hypercholesterolemic atherosclerosis: effect of vitamin E. Am. Heart J. 125 (1993) 958-973
41. Reindel J.F., Dominick M.A., Bocan T.M., Gough A.W., and McGuire E.J. Toxicologic effects of a novel acyl-CoA:cholesterol acyltransferase inhibitor in cynomolgus monkeys. Toxicol. Pathol. 22 (1994) 510-518
42. Risser T.R., Reaven G.M., and Reaven E.P. Intestinal contribution to secretion of very low density lipoproteins into plasma. Am. J. Physiol. 234 (1978) E277-E281
43. Ross A.C. Retinol esterification by rat liver microsomes. Evidence for a fatty acyl coenzyme A: retinol acyltransferase. J. Biol. Chem. 257 (1982) 2453-2459
44. Ross A.C., and Rowe J.F. Cholesterol esterification by mammary gland microsomes from the lactating rat. Proc. Soc. Exp. Biol. Med. 176 (1984) 42-47
45. Rudel L.L., Lee R.G., and Cockman T.L. Acyl coenzyme A: cholesterol acyltransferase types 1 and 2: structure and function in atherosclerosis. Curr. Opin. Lipidol. 12 (2001) 121-127
46. Sliskovic D.R., and White A.D. Therapeutic potential of ACAT inhibitors as lipid lowering and anti-atherosclerotic agents. Trends Pharmacol. Sci. 12 (1991) 194-199
47. Steinberg D., Parthasarathy S., Carew T.E., Khoo J.C., and Witztum J.L. Beyond cholesterol. Modifications of low-density lipoprotein that increase its atherogenicity. N. Engl. J. Med. 320 (1989) 915-924
48. Stokke K.T., and Norum K.R. Determination of lecithin: cholesterol acyltransfer in human blood plasma. Scand. J. Clin. Lab. Invest. 27 (1971) 21-27
49. Su Y.R., Dove D.E., Major A.S., Hasty A.H., Boone B., Linton M.F., and Fazio S. Reduced ABCA1-mediated cholesterol efflux and accelerated atherosclerosis in apolipoprotein E-deficient mice lacking macrophage-derived ACAT1. Circulation 111 (2005) 2373-2381
50. Suckling K.E., Benson G.M., Bond B., Gee A., Glen A., Haynes C., and Jackson B. Cholesterol lowering and bile acid excretion in the hamster with cholestyramine treatment. Atherosclerosis 89 (1991) 183-190
51. Sugimoto K., Tsujita M., Wu C.A., Suzuki K., and Yokoyama S. An inhibitor of acylCoA:cholesterol acyltransferase increases expression of ATP-binding cassette transporter A1 and thereby enhances the ApoA-I-mediated release of cholesterol from macrophages. Biochim. Biophys. Acta 1636 (2004) 69-76
52. Tabas I. Consequences of cellular cholesterol accumulation: basic concepts and physiological implications. J. Clin. Invest. 110 (2002) 905-911
53. Tabas I. Consequences and therapeutic implications of macrophage apoptosis in atherosclerosis: the importance of lesion stage and phagocytic efficiency. Arterioscler. Thromb. Vasc. Biol. 25 (2005) 2255-2264
54. Tardif J.C., Gregoire J., Schwartz L., Title L., Laramee L., Reeves F., Lesperance J., Bourassa M.G., L'Allier P.L., Glass M., Lambert J., and Guertin M.C. Effects of AGI-1067 and probucol after percutaneous coronary interventions. Circulation 107 (2003) 552-558
55. Tardif J.C., Gregoire J., L'Allier P.L., Anderson T.J., Bertrand O., Reeves F., Title L.M., Alfonso F., Schampaert E., Hassan A., McLain R., Pressler M.L., Ibrahim R., Lesperance J., Blue J., Heinonen T., and Rodes-Cabau J. Effects of the acyl coenzyme A:cholesterol acyltransferase inhibitor avasimibe on human atherosclerotic lesions. Circulation 110 (2004) 3372-3377
56. Urbich C., Heeschen C., Aicher A., Dernbach E., Zeiher A.M., and Dimmeler S. Relevance of monocytic features for neovascularization capacity of circulating endothelial progenitor cells. Circulation 108 (2003) 2511-2516
57. Vernetti L.A., MacDonald J.R., Wolfgang G.H., Dominick M.A., and Pegg D.G. ATP depletion is associated with cytotoxicity of a novel lipid regulator in guinea pig adrenocortical cells. Toxicol. Appl. Pharmacol. 118 (1993) 30-38
58. Wrenn Jr. S.M., Parks J.S., Immermann F.W., and Rudel L.L. ACAT inhibitors CL 283,546 and CL 283,796 reduce LDL cholesterol without affecting cholesterol absorption in African green monkeys. J. Lipid Res. 36 (1995) 1199-1210
59. Yamauchi Y., Chang C.C., Hayashi M., Abe-Dohmae S., Reid P.C., Chang T.Y., and Yokoyama S. Intracellular cholesterol mobilization involved in the ABCA1/apolipoprotein-mediated assembly of high density lipoprotein in fibroblasts. J. Lipid Res. 45 (2004) 1943-1951
60. Zilversmit D.B., and Hughes L.B. Validation of a dual-isotope plasma ratio method for measurement of cholesterol absorption in rats. J. Lipid Res. 15 (1974) 465-473