NTE-122, an acyl-coa:cholesterol acyltransferase inhibitor, prevents the progression of atherogenesis in cholesterol-fed rabbits.
The cholesterol-lowering and anti-atherosclerotic effects of NTE-122 (trans-1,4-bis[[1-cyclohexyl-3-(4-dimethylaminophenyl)ureido]methyl]cyclohexane), an acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor, were evaluated in 1% cholesterol diet-fed rabbits. NTE-122 (1, 3 and 10 mg/kg per day) lowered the total cholesterol levels in both plasma and liver dose-dependently (by 99% and 94% at 10 mg/kg per day, respectively). In the aortic wall of the rabbits given NTE-122, the atherosclerotic lesion area in both aortic arch and thoracic aorta were dose-dependently reduced (by 100% at 10 mg/kg per day), and the total cholesterol content in aortic arch was also lowered significantly at more than 3 mg/kg per day. These results suggest that NTE-122 is capable of exhibiting anti-atherosclerotic effects.
Azuma
Y
Y
Central Research Institute, Nissin Food Products Co., Ltd., Kusatsu, Shiga, Japan. y-azuma@mb1.nissinfoods.co.jp
Date
K
K
Ohno
K
K
Matsushiro
S
S
Nobuhara
Y
Y
Yamada
T
T
D000101:Acetyl-CoA C-Acetyltransferase / Q000037:antagonists & inhibitors*; D000814:Aniline Compounds / Q000494:pharmacology*; D000818:Animals; D000924:Anticholesteremic Agents / Q000494:pharmacology*; D001013:Aorta, Thoracic / Q000473:pathology; D001161:Arteriosclerosis / Q000473:pathology / Q000517:prevention & control*; D001835:Body Weight / Q000187:drug effects; D002784:Cholesterol / Q000097:blood; D002791:Cholesterol, Dietary; D003510:Cyclohexanes / Q000494:pharmacology*; D004032:Diet; D018450:Disease Progression; D004435:Eating; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D008297:Male; D011817:Rabbits
D000814:Aniline Compounds; D000924:Anticholesteremic Agents; D002791:Cholesterol, Dietary; D003510:Cyclohexanes; D004791:Enzyme Inhibitors; C111531:NTE 122; D002784:Cholesterol; D000101:Acetyl-CoA C-Acetyltransferase