Summary
The effects of two different plant sterols on intestinal cholesterol absorption were compared in normal volunteers by an intestinal perfusion study during a control period followed by high dose infusion of sitosterol or sitostanol (3.6 μmol/min), to which subjects were allocated in a randomized manner. Cholesterol absorption during the control period was similar in the two groups, averaging 0.88 ± 0.48 μmol/min (32 ± 11%) for group I (sitosterol) and 0.68 ± 0.33 μmol/min (29 ± 9%) for group II (sitostanol). The infusion of a high dose of sitosterol resulted in a significant reduction of cholesterol absorption to 0.47 μmol/min (16%). Following the same dose of sitostanol, cholesterol absorption diminished significantly to 0.15 ± 0.11 μmol/min (5.1 ± 2.9%). Overall cholesterol absorption declined during sitosterol infusion by almost 50%, whereas sitostanol infusion caused a reduction of cholesterol absorption by almost 85%. These findings of a more effective inhibition of cholesterol absorption by sitostanol might confirm the observation recorded by others that an increase in hydrophobicity of a plant sterol results in a higher affinity but lower capacity to mixed micells. This may cause an effective displacement of cholesterol from micellar binding and therefore diminished cholesterol absorption.
Article PDF
Similar content being viewed by others
Avoid common mistakes on your manuscript.
References
Grundy SM, Metzger AL (1972) A physiological method for estimation of hepatic secretion of biliary lipids. Gastroenterology 62: 1200–1217
Grundy SM, Mok HYI (1977) Determination of cholesterol absorption in man by intestinal perfusion. J Lipid Res 18: 263–271
Mok HYI, von Bergmann K, Grundy SM (1979) Effects of continuous and intermittent feeding on biliary lipid outputs in man: application for measurements of intestinal absorption of cholesterol and bile acids. J Lipid Res 20: 389–398
Samuel P, McNamara DJ, Ahrens EH, Crouse JR, Parker T (1982) Further validation of the plasma isotope ratio method for measurement of cholesterol absorption. J Lipid Res 23: 480–489
Peterson DW, Nichols CW, Peek NF, Chaikoff IL (1956) Depression of cholesterol in human subjects consuming butter containing soy sterols. Fed Proc 15: 569
Grundy SM, Mok HYI (1976) Effects of low dose phytosterols on cholesterol absorption in man. In: Greten H (ed) Lipoprotein metabolism. Springer, New York Berlin Heidelberg, pp 112–118
Lees AM, Mok HYI, Lees RS, McCluskey MA, Grundy SM (1977) Plant sterols as cholesterol — lowering agents: clinical trials in patients with hypercholesterolemia and studies of sterol balance. Atherosclerosis 28: 325–338
Lederle RM (1983) Langzeitbehandlung der Hypercholesterinämie bei terminaler Niereninsuffizienz. Med Klin 78: 136–137
Lees RS, Lees AM (1976) Effects of sitosterol therapy on plasma lipid and lipoprotein concentrations. In: Greten H (ed) Lipoprotein metabolism. Springer, New York Berlin Heidelberg, pp 119–124
Farquhar JW, Smith RE, Dempsey ME (1956) The effect of beta sitosterol on the serum lipids of young men with arteriosclerotic heart disease. Circulation 14: 77–82
Oster P, Schlierf G, Heuck C, Greten H, Grundert-Remy U, Haase W, Klose G, et al. (1976) Sitosterol in type II hyperlipoproteinemia. In: Greten H (ed) Lipoprotein metabolism. Springer, New York Berlin Heidelberg, pp 125–130
Salen G, Ahrens EH Jr, Grundy SM (1970) Metabolism of betasitosterol in man. J Clin Invest 49: 952–967
Hassan AS, Rampone AJ (1979) Intestinal absorption and lymphatic transport of cholesterol and beta-sitostanol in the rat. J Lipid Res 20: 646–653
Sugano M, Morioka H, Ikeda I (1977) A comparison of hypocholesterolemic activity of beta-sitosterol and beta-sitostanol in rats. J Nutr 107: 2011–2019
Heinemann T, Leiss O, von Bergmann K (1986) Effects of low-dose sitostanol on serum cholesterol in patients with hypercholesterolemia. Atherosclerosis 61: 219–223
Ikeda I, Sugano M (1978) Comparison of absorption and metabolism of beta-sitosterol and beta-sitostanol in rats. Atherosclerosis 30: 227–237
Chandler RE, Hooper SN, Ismail HA (1979) Antihypercholesterolemic studies with sterols: beta-sitosterol and stigmasterol. J Pharm Sci 68: 245–247
Leiss O, von Bergmann K, Streicher U, Strotkoetter H (1984) Effect of three different dihydroxy bile acids on intestinal cholesterol absorption in normal volunteers. Gastroenterology 87: 144–149
Mattson FH, Grundy SM, Crouse JR (1982) Optimizing the effect of plant sterols on cholesterol absorption in man. Am J Clin Nutr 35: 697–700
Ivy AC, Lin TM, Karvinen F (1955) Absorption of dihydrocholesterol and soya sterols by the rat's intestine. Am J Physol 183: 79–85
Armstrong MJ, Carey MC (1987) Thermodynamic and molecular determinants of sterol solubilities in bile salt micelles. J Lipid Res 28: 1144–1155
Author information
Authors and Affiliations
Rights and permissions
About this article
Cite this article
Heinemann, T., Kullak-Ublick, G.A., Pietruck, B. et al. Mechanisms of action of plant sterols on inhibition of cholesterol absorption. Eur J Clin Pharmacol 40, S59–S63 (1991). https://doi.org/10.1007/BF01409411
Issue Date:
DOI: https://doi.org/10.1007/BF01409411