Plant sterols have been investigated as one of the safe potential alternati
ve methods in lowering plasma cholesterol levels. Several human studies hav
e shown that plant sterols/stanols significantly reduce plasma total and LD
L cholesterol. In this article, pharmacological characteristics of plant st
erols/stanols have been summarized and discussed. In particular, experiment
al data that demonstrate the effects of dietary phytosterols on lipid metab
olism and development of atherosclerotic lesions have been critically revie
wed. Despite their similar chemical structures, phytosterols and cholestero
l differ markedly from each other in regard to their pharmacological charac
teristics including intestinal absorption and metabolic fate. Compared to c
holesterol, plant sterols have poor intestinal absorption. The most and bes
t studied effects of plant sterols are their inhibition of intestinal chole
sterol absorption. Other biological activities of phytosterols such as effe
cts on lecithin:cholesterol acyltransferase activity, bile acid synthesis,
oxidation and uptake of lipoproteins, hepatic and lipoprotein lipase activi
ties and coagulation system have been linked to their anti-atherogenic prop
erties, Moreover, evidence for beneficial effects of plant sterols on disor
ders such as cutaneous xanthomatosis, colon cancer and prostate hyperplasia
has been discussed. Finally, the potential adverse effects of plant sterol
s as well as pathophysiology of hereditary sitosterolemia are also reviewed
. In conclusion, more pharmacokinetic data are needed to better understand
metabolic fate of plant sterols/stanols and their fatty acid esters as well
as their interactions with other nutraceutical/pharmaceutical agents. (C)
2000 Elsevier Science Inc. All rights reserved.