We therefore aimed to … An analysis of variance (ANOVA) model appropriate for a 2-period, 2-arm crossover design with terms for treatment, sequence, patient within sequence, and period was used to calculate differences between placebo and ezetimibe treatment using SAS statistic package (SAS Institute Inc). Membrane proteins mediating the intestinal absorption of cholesterol, plant sterols, vitamin E, and vitamin K 1. This site needs JavaScript to work properly. ; Writing—original draft, Y.Y. This inhibition was associated with a compensatory increase in cholesterol synthesis. Thus, the present study was undertaken to measure the effect of ezetimibe on the intestinal cholesterol absorption in humans. 2013;2013:549627. doi: 10.1155/2013/549627. There was a correlation between intestinal ABCA1 mRNA and SREBP-1c mRNA contents, but not between SREBP-1c mRNA content and cholesterol absorption. Find support for a specific problem on the support section of our website. In the intestinal lumen, phytosterols displace cholesterol from mixed micelles and reduce cholesterol absorption . Very low-density lipoprotein and low-density lipoprotein (VLDL/LDL) are increased in Western diet (WD)-fed mice in an NPC1L1-dependent manner, so we comprehensively analyzed the NPC1L1-dependent VLDL/LDL components. ezetimibe (zetia) works to lower ldl by inhibiting the absorption of cholesterol in the intestines. J. Lipid Res. Importantly, variations in cholesterol absorption did not correlate significantly with changes in total cholesterol and did not correlate with variations in LDL cholesterol reductions after ezetimibe treatment, likely due to the influence of other factors, including compensatory changes in cholesterol synthesis.In conclusion, 2 weeks of treatment with ezetimibe at 10 mg/d produced a 54% inhibition of cholesterol absorption in mildly to moderately hypercholesterolemic subjects. Managing cholesterol at the site of absorption is an increasingly popular strategy in the treatment of nism of their intestinal absorption remains poorly understood. Recent studies demonstrated that NPC1L1 regulates the intestinal absorption of several fat-soluble nutrients, in addition to cholesterol. Our dedicated information section provides allows you to learn more about MDPI. eCollection 2020.Cholesterol. Regarding the NPC1L1-mediated uptake of cholesterol, it has been reported that N-terminal domain of NPC1L1 binds cholesterol and promotes the formation of cholesterol-enriched microdomain in the plasma membrane to facilitate cholesterol transport [In conclusion, our results indicate that NPC1L1, a cholesterol importer, is involved in the uptake of dietary SM and controls diet-induced VLDL/LDL-apoM-S1P levels in the blood (Conceptualization, Y.Y., T.T. from the Ministry of Education, Culture, Sports, Science and Technology of Japan, and partly supported by a Lotte Research Promotion Grant from the Lotte Foundation (to T.T.) To examine this possibility, we analyzed the intestinal absorption of SM using radioisotope ([Consistent with in vivo observations, in vitro uptake assays using NPC1L1-overexpressing human colorectal epithelial Caco-2 cells (Taken together, our in vivo and in vitro results demonstrate that NPC1L1 functions as an SM importer in the intestine and regulates VLDL/LDL-apoM-S1P levels in the blood (In this study, we first demonstrated that NPC1L1 regulates S1P distribution to VLDL/LDL particles in mice fed a WD. Recent studies demonstrated that NPC1L1 regulates the intestinal absorption of several fat-soluble nutrients, in addition to cholesterol. and AMED (grant number JP20gm5910028 to Y.Y. At each concentration of dietary cholesterol, there was a similar significant inverse correlation between intestinal ABCA1 mRNA content and the amount of cholesterol absorbed. Hepatic cholesterol and bile acid metabolism and intestinal cholesterol absorption in scavenger receptor class B type I-deficient mice. Consumption of a high-cholesterol diet also increased intestinal ABCA1 expression. Results showed that ezetimibe inhibited cholesterol absorption by 54% relative to placebo. Low-density lipoprotein (LDL) cholesterol was calculated by the method of Friedewald et al.All data were analyzed in an intention-to-treat approach.