Fig. 1.
Inhibition of cholesterol uptake and esterification by ezetimibe. Caco-2 cells were preincubated for 30 min with (○) or without (●) 50 μM of ezetimibe and then incubated with solution containing micelles with 5 μM of [3H]cholesterol. Cells were then washed, and total radioactivity associated with the cells was measured as indicated in materials and methods (A). In other set of experiments (B), total lipids were extracted from the cells and then separated by thin-layer chromatography. Bands corresponding to free cholesterol and cholesteryl ester were scraped, and the associated radioactivity was counted. Ezetimibe-sensitive cholesterol esterification was then calculated as described in materials and methods. Data are presented (in B and A) as means ± SE from 4–6 values obtained from at least 3 separate occasions. Error bars are not shown when they are smaller than the symbol. *P < 0.05 or less compared with cells without ezetimibe in A and B.