Effects of NTE-122, an Acyl-CoA:Cholesterol Acyltransferase Inhibitor, on Cholesterol Esterification and Lipid Secretion From CaCo-2 Cells, and Cholesterol Absorption in Rats

The Japanese Journal of Pharmacology

Masahiro Yamasaki¹  Masaru Chiba¹  Yukimasa Azuma¹  Hiroshi Mikami¹  Katsutoshi Ohno¹  Jiro Seto¹  Toshihiro Yamada¹  Yoichi Nobuhara¹ 

[1]Central Research Institute, Nissin Food Products Co., Ltd.

关键词: NTE-122;    Acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor;    Cholesterol absorption;   

DOI  :  10.1254/jjp.80.81

学科分类：药理学

来源: Nihon Yakuri Gakkai Henshuubu / Japanese Pharmacological Society

【 摘 要 】

References(14)Cited-By(2)The effect of NTE-122 (trans-1, 4-bis[[1-cyclohexyl-3-(4-dimethylamino phenyl)ureido]methyl]cyclohexane), an acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor, on cholesterol absorption was investigated. NTE-122 inhibited whole-cell ACAT activity in CaCo-2 cells, a human intestinal cell line, with an IC50 value of 4.7 nM. In CaCo-2 cells cultured on a membrane filter, NTE-122 pronouncedly inhibited the basolateral secretion of newly synthesized cholesteryl esters, and significantly reduced the basolateral secretion of newly synthesized triglycerides without influencing the cellular triglyceride synthesis. Furthermore, NTE-122 (1 mg/kg, p.o.) inhibited [14C]cholesterol absorption in rats. These results suggest that NTE-122 is capable of exhibiting anti-hyperlipidemic effects by reducing the absorption of dietary cholesterol.

【 授权许可】

Unknown