Plasma Cholesterol Reducing Effect of FR129169, a Novel Acyl-CoA:Cholesterol Acyltransferase Inhibitor, in the Rat

Japanese Journal of Pharmacology - Tập 70 - Trang 35-41 - 1996
Yuri Sakuma1, Hiroyuki Hagihara1, Kazuhiko Ohne1, Akira Nagayoshi1, Seitaro Mutoh1, Yoshikuni Ito1, Yoshitada Notsu1, Masakuni Okuhara1
1Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., 5-2-3, Tokodai, Tsukuba, Ibaraki, 300-26 Japan

Tài liệu tham khảo

Fielding, 1978, Metabolism of cholesterol enriched chylomicrons, J Lipid Res, 19, 705, 10.1016/S0022-2275(20)41270-2 Erickson, 1980, Rat liver acyl-coenzyme A:holesterol acyl transferase, J Lipid Res, 21, 930, 10.1016/S0022-2275(20)34791-X Gillies, 1986, Regulation of Acyl-CoA:cholesterol acytransferase activity in normals atherosclerotic rabbit aortas, Exp Mol Pathol, 44, 329, 10.1016/0014-4800(86)90046-8 Tabas, 1987, Protein synthesis inhibition in mouse peritoneal macrophages results in increased acyl-coenzyme A:cholesterol acyltransferase activity and cholesterol ester accumulation in the presence of native low density lipoprotein, J Biol Chem, 262, 12175, 10.1016/S0021-9258(18)45333-1 Suckling, 1985, Role of acyl-CoA:cholesterol acytransferase in cellular cholesterol metabolism, J Lipid Res, 26, 647, 10.1016/S0022-2275(20)34322-4 Krause, 1993, Divergent pharmacologic activities of PD132301–2 and CL277092, urea inhibitor of acyl-CoA:cholesterol acyltransferase, J Pharmacol Exp Ther, 262, 734 Trivedi, 1993, Inhibitors of acyl-CoA:cholesterol acyltransferase. 4. A novel series of urea ACAT inhibitor as potential hypocholesterolemic agents, J Med Chem, 29, 3300, 10.1021/jm00074a011 Bocan, 1991, Comparison of CI976, on ACAT inhibitor, and selected lipid lowering agents antiatherosclepotic activity in iliac-fomeral and thoracic aortic lesions. A chemical, morphological, and morphometric evaluation, Arterioscler Thromb, 11, 1830, 10.1161/01.ATV.11.6.1830 Tanaka, 1994, Effect of the acyl-CoA:cholesterol acyltransferase inhibitor, E5324, on experimental atherosclerosis in rabbits, Atherosclerosis, 107, 187, 10.1016/0021-9150(94)90020-5 Heider, 1986, Agents which inhibit cholesterol esterification in intestine and their potential value in the treatment of hypercholesterolemia, 423 Krause, 1993, In vivo evidence that the lipid-regulating activity of the ACAT inhibitor CI-976 in rats is due to inhibition of both intestinal and liver ACAT, J Lipid Res, 34, 279, 10.1016/S0022-2275(20)40755-2 Heigerud, 1981, AcylCoA:choIesterol acyltransferase in human small intestine, its activity and some properties of the enzymatic reaction, J Lipid Res, 22, 271, 10.1016/S0022-2275(20)35370-0 Gallo, 1987, Normal cholesterol absorption in rats deficient in intestinal acylcoenzyme A:cholesterol acyltransferase activity, J Lipid Res, 28, 381, 10.1016/S0022-2275(20)38691-0 Bell, 1992, U-73482: A novel ACAT inhibitor that elevates HDL-cholesterol, lower plasma triglyceride and facilitates hepatic cholesterol mobilization in the rat, Atherosclerosis, 92, 115, 10.1016/0021-9150(92)90270-Q Kam, 1989, Inhibition of acylcoenzyme A:cholesterol acyltransferase activity in CaCo-2 cells results in intracellular triglyseride accumulation, J Lipid Res, 30, 371, 10.1016/S0022-2275(20)38365-6 Bennett, 1984, Reduced cholesterol transmucosal transport in rats with inhibited mucosal acyl CoA:cholesterol acyltransferase and normal pancreatic function, J Lipid Res, 25, 148, 10.1016/S0022-2275(20)37835-4 Tanaka, 1993, Regulation of apolipoprotein B production and secretion in response to the change of intracellular cholesterol ester contents in rabbit hepatocytes, J Biol Chem, 268, 12713, 10.1016/S0021-9258(18)31446-7 Dashti, 1992, The effect of low density lipoproteins, cholesterol, and 25-hydroxycholesterol on apolipoprotein B gene expression in HepG2 cells, J Biol Chem, 267, 7160, 10.1016/S0021-9258(19)50552-X Jiao, 1991, Abnormalities of plasma lipoproteins in a new genetically obese rat with non-insulin-dependent diabetes mellitus (Wistar fatty rats), Int J Obesity, 15, 487 Jiao, 1988, Increased activity of intestinal acyl-CoA:cholesterol acyltransferase in rats with streptozosin-induced diabetes and restoration by insulin supplementation, Diabetes, 37, 342, 10.2337/diab.37.3.342 Yang, 1994, Comparison of the effect of hyperinsulinemia acyl-CoA:cholesterol acyltransferase activity in the liver and intestine of the rat, Atherosclerosis, 107, 25, 10.1016/0021-9150(94)90138-4 Maecher, 1993, Importance of exogenous cholesterol in diabetic rats: effect of treatment with insulin or with an acyl-CoA:cholesterol acytransferase inhibitor, Ann Nutr Metab, 37, 199, 10.1159/000177769 Kojima, 1994, Clinical study of exogenous sterol absorption and post-heparin plasma diamine oxidase (DAO) activity, J Jpn Atheroscler Soc, 22, 85, 10.5551/jat1973.22.1_85 Garg, 1992, Lipid-Lowering therapy and macrovascular disease in diabetes mellitus, Diabetes, 41, 111, 10.2337/diab.41.2.S111