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
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概要
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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.
- 社団法人 日本薬理学会の論文
- 1999-05-01
著者
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田中 東
日清食品ホールディングス株式会社食品安全研究所
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東 幸雅
日清食品(株)食品安全研究所
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Yamasaki Masahiro
Central Research Institute Nissin Food Products Co. Ltd.
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Yamasaki M
Kumamoto Univ. Kumamoto Jpn
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Tanaka Azuma
Food Safety Research Institute Nissin Food Products Co. Ltd.
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Azuma Yukimasa
Food Safety Research Institute Nissin Food Products Co. Ltd.
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Azuma Yukimasa
Central Research Institute Nissin Food Products Co. Ltd.
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SETO Jiro
Central Research Institute, Nissin Food Products Co., Ltd.,
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OHNO Katsutoshi
Central Research Institute, Nissin Food Products Co., Ltd.,
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MIKAMI Hiroshi
Central Research Institute, Nissin Food Products Co., Ltd.,
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YAMADA Toshihiro
Central Research Institute, Nissin Food Products Co., Ltd.,
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CHIBA Masaru
Central Research Institute, Nissin Food Products Co., Ltd.,
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NOBUHARA Yoichi
Central Research Institute, Nissin Food Products Co., Ltd.,
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Seto Jiro
Central Research Institute Nissin Food Products Co. Ltd.
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Nobuhara Yoichi
Central Research Institute Nissin Food Products Co. Ltd.
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Nobuhara Yoichi
Central Research Institute Nissin Food Products Co. Ltd
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Yamada Toshihiro
The Food Safety Research Institute Nissin Foods Holdings Co. Ltd.
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Nobuhara Youichi
Central Research Institute Nissin Food Products Co. Ltd.
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Chiba Masaru
Central Research Institute Nissin Food Products Co. Ltd.
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Mikami Hiroshi
Central Research Institute Nissin Food Products Co. Ltd.
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Yamada Toshihiro
Food Safety Research Institute Nissin Foods Holdings Co. Ltd.
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