Fig. 6.

Ezetimibe inhibits the internalization of NPC1L1 and cholesterol in mouse intestine. Male C57BL/6 mice (12 weeks old; n = 6 per group) were pretreated with ezetimibe or vehicle before being gavaged with cholesterol. Thirty minutes later, intestinal samples were excised and subjected to immunohistochemistry and filipin staining. A: Ezetimibe blocked cholesterol-induced endocytosis of NPC1L1. Paraffin-embedded sections were applied to immunohistochemistry staining with anti-NPC1L1 and anti-Villin or anti-Rab11 antibodies. B: Ezetimibe blocked dietary cholesterol from entering enterocytes. Frozen sections of mouse intestine were stained with filipin to indicate free cholesterol. C: Cholesterol and phospholipids were measured enzymatically. The relative amount of cholesterol was normalized to that of phospholipids. D: Male C57BL/6 mice were orally gavaged with vehicle (control) or ezetimibe once daily for 3 days. Then [¹⁴C]cholesterol and [³H]sitostanol in 150 μl corn oil were orally gavaged. Cholesterol absorption was determined by the fecal ratio method. Values are mean ± SD. P values were calculated by ANOVA. **0.001 < P < 0.01.