Dietary guidelines for optimal health call for reducing the intake of cholesterol. One strategy for doing so involves the plant sterols, including sitosterol, stigmasterol, stigmastanol, and campesterol, shown in the figure. Despite their structural similarity to cholesterol, minor isomeric differences and/or the presence of methyl and ethyl groups in the side chains of these substances result in their poor absorption by intestinal mucosal cells. Interestingly, although plant sterols are not effectively absorbed by the body, they nonetheless are highly effective in blocking the absorption of cholesterol itself by intestinal cells.
The practical development of plant sterol drugs as cholesterol-lowering agents will depend both on structural features of the sterols themselves and on the form of the administered agent. For example, the unsaturated sterol sitosterol is poorly absorbed in the human intestine, whereas sitostanol, the saturated analog, is almost totally unabsorbable. In addition, there is evidence that plant sterols administered in a soluble, micellar form (see page 261 for a description of micelles) are more effective in blocking cholesterol absorption than plant sterols administered in a solid, crystalline form.
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