Most animal and human studies show that phytosterols reduce serum/or plasma total cholesterol and low density lipoprotein (LDL) cholesterol levels. Phytosterols are structurally very similar to cholesterol except that they always contain some substitutions at the C24 position on the sterol side chain. Plasma phytosterol levels in mammalian tissue are normally very low due primarily to poor absorption from the intestine and faster excretion from liver compared to cholesterol. Phytosterols are able to be metabolized in the liver into C21 bile acids via liver other than normal C24 bile acids in mammals. It is generally assumed that cholesterol reduction results directly from inhibition of cholesterol absorption through displacement of cholesterol from micelles. Structure-specific effects of individual phytosterol constituents have recently been shown where saturated phytosterols are more efficient compared to unsaturated compounds in reducing cholesterol levels. In addition, phytosterols produce a wide spectrum of therapeutic effects in animals including anti-tumour properties. Phytosterols have been shown experimentally to inhibit colon cancer development. With regard to toxicity, no obvious side effects of phytosterol have been observed in studies to date, except in individual with phytosterolemia, an inherited lipid disorder. Further characterization of the influence of various phytosterol subcomponents on lipoprotein profiles in humans is required to maximize the usefulness of this non-pharmacological approach to reduction of atherosclerosis in the population.