ヒト腸上皮細胞株Ｃａｃｏ‐２のａｃｙｌ‐ＣｏＡ：ｃｈｏｌｅｓｔｅｒｏｌ　ａｃｙｌｔｒａｎｓｆｅｒａｓｅ（ＡＣＡＴ）活性とコレステロールエステル分泌に対するＡＣＡＴ阻害薬，Ｆ‐１３９４の作用

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タイトル別名
  • Effect of F-1394, a potent and selective inhibitor of acyl-CoA:cholesterol acyltransferase(ACAT), on esterification of cholesterol and basolateral secretion of cholesteryl ester in Caco-2 cells.
  • ヒト チョウ ジョウヒ サイボウカブ Caco-2 ノ acyl-CoA ch

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The present study was conducted to investigate the inhibitory effect of F-1394, a potent and selective inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT), on incorporation of 14C-oleic acid into cholesteryl ester in cultured Caco-2 cells, a human intestinal cell line, and compare its effect to those of other ACAT inhibitors and hypolipidemic agents. The cholesterol esterification in Caco-2 cells was strongly inhibited by F-1394 in a concentration-dependent manner with the estimated IC50 value of 71 nM. In contrast, the estimated IC50 values of the other ACAT inhibitors such as YM-17E, CI-976, CL-277, 082 and DL-melinamide are 121 nM, 702 nM, 21.5 μM and 20.9 μM, respectively. Simvastatin, a 3-hydroxy-3-methylglutaryl-CoA reductase inhibitor, also inhibited the ACAT activity in Caco-2 cells with an IC50 value of 22.5 μM, whereas pravastatin Na, probucol and clofibrate did not affect the activity. Furthermore, F-1394 at a concentration of 100 nM inhibited the basolateral secretion of cholesteryl ester by 90 % from differentiated Caco-2 cells that were cultured on a membrane filter. These results demonstrate that F-1394 strongly inhibits human intestinal ACAT activity and basolateral secretion of cholesterol from Caco-2 cells. Therefore, F-1394 may have a therapeutic potential for dietary hyperlipidemic subjects.

収録刊行物

  • 日本薬理学雑誌

    日本薬理学雑誌 110 (6), 357-365, 1997

    公益社団法人 日本薬理学会

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