Home
Resources
Publications
[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]

[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]

J Kusunoki, K Aragane, T Kitamine, T Yamaura, H Ohnishi

Nihon Yakurigaku Zasshi. 1997 Dec;110(6):357-65.

PMID: 9503394

Abstract:

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 microM and 20.9 microM, 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 microM, 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.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP191219804	YM 976		191219-80-4	Price

As a specialist in analytical chemical Products, Alfa Chemistry offers consumers a wealth of raw materials and a full range of technologies and services.

QUICK LINKS

HEADQUARTERS

Tel:

Fax:

Email: