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Journal of Lipid Research, Vol 29, 1573-1582, Copyright © 1988 by Lipid Research, Inc.
I Ikeda, K Tanaka, M Sugano, GV Vahouny and LL Gallo
The extent and site(s) of inhibition of cholesterol absorption by plant
sterols, sitosterol and fucosterol, were studied in rats. The intragastric
administration of a single emulsified lipid meal containing 25 mg
[3H]cholesterol and 25 mg of either sitosterol or fucosterol inhibited the
lymphatic absorption of cholesterol by 57% and 41%, respectively, in 24 hr.
Less than 2% of each plant sterol was absorbed in the 24-hr period. In
contrast, neither plant sterol (50 microM) inhibited cholesterol absorption
when co-administered with equimolar amounts of cholesterol in
phospholipid-bile salt micelles nor was either absorbed from the micellar
solution. A series of in vitro studies was conducted to identify the
site(s) of plant sterol inhibition of cholesterol absorption and to account
for the difference in inhibitory effectiveness of sitosterol and
fucosterol. A comparison of the micellar solubility of each sterol alone
and in equimolar binary mixtures (to 2.0 mM) revealed that the solubility
of individual sterols decreased in the following order: cholesterol,
fucosterol, sitosterol, and that in binary mixtures cholesterol solubility
was decreased by sitosterol and, to a lesser extent, by fucosterol relative
to its solubility alone. A comparison between micellar-solubilized
cholesterol and either sitosterol or fucosterol for binding to isolated
brush border membranes, intestinal mucin, or for esterification by either
cholesterol esterase or acyl coenzyme A:cholesterol acyltransferase
revealed moderate to no competition. The data suggest that plant sterols
displace cholesterol from bile salt (taurocholate) micelles and that
sitosterol is more effective than fucosterol in this capacity.
ARTICLES
Inhibition of cholesterol absorption in rats by plant sterols
Department of Biochemistry, George Washington University, School of Medicine, Washington, DC 20037.
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