We measured levels of plant sterols, cholesterol precursors, and oxysterols by gas chromatography-mass spectrometry in 47 hypercholesterolemics and 32 controls. Twenty-four hypercholesterolemics received 10?mg ezetimibe/day for 4 weeks.
Plant sterols were 30-42 % higher in hypercholesterolemics than in controls and positively correlated with low-density lipoprotein-cholesterol (LDL-C). Ezetimibe decreased plant sterols by 21-53 % , but did not change bile acid synthesis markers. 7¦Â-hydroxycholesterol, a marker for non-enzymatic oxidation of cholesterol, was 66 % higher in hypercholesterolemics than controls. Ezetimibe decreased 7¦Â-hydroxycholesterol levels by 15 % regardless of LDL-C reduction.
Ezetimibe decreases serum oxidized cholesterol generated by non-enzymatic reactions without impairing bile acid synthesis. Ezetimibe may maintain cholesterol excretion into bile and alleviate the diet-derived oxidative burden.