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Mechanisms of action of plant sterols on inhibition of cholesterol absorption

Comparison of sitosterol and sitostanol

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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 umol/min (32 ± 11%) for group I (sitosterol) and 0.68 ± 0.33 umol/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 umol/min (16%). Following the same dose of sitostanol, cholesterol absorption diminished significantly to 0.15 ± 0.11 umol/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.

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References

  1. Grundy SM, Metzger AL (1972) A physiological method for estimation of hepatic secretion of biliary lipids. Gastroenterology 62: 1200–1217

    PubMed  CAS  Google Scholar 

  2. Grundy SM, Mok HYI (1977) Determination of cholesterol absorption in man by intestinal perfusion. J Lipid Res 18: 263–271

    PubMed  CAS  Google Scholar 

  3. 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

    PubMed  CAS  Google Scholar 

  4. 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

    PubMed  CAS  Google Scholar 

  5. Peterson DW, Nichols CW, Peek NF, Chaikoff IL (1956) Depression of cholesterol in human subjects consuming butter containing soy sterols. Fed Proc 15: 569

    Google Scholar 

  6. 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

    Google Scholar 

  7. 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

    Article  PubMed  CAS  Google Scholar 

  8. Lederle RM (1983) Langzeitbehandlung der Hypercholesterinämie bei terminaler Niereninsuffizienz. Med Klin 78: 136–137

    Google Scholar 

  9. 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

    Google Scholar 

  10. 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

    PubMed  CAS  Google Scholar 

  11. Oster P, Schlierf G, Heuck C, Greten H, Grundert-Remy U, Haase W, Klose G, et al. (1976) Sitosterol in tpye II hyperlipoproteinemia. In: Greten H (ed) Lipoprotein metabolism. Springer, New York Berlin Heidelberg, pp 125–130

    Google Scholar 

  12. Salen G, Ahrens EH Jr, Grundy SM (1970) Metabolism of betasitosterol in man. J Clin Invest 49: 952–967

    Article  PubMed  CAS  Google Scholar 

  13. Hassan AS, Rampone AJ (1979) Intestinal absorption and lymphatic transport of cholesterol and beta-sitostanol in the rat. J Lipid Res 20: 646–653

    PubMed  CAS  Google Scholar 

  14. 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

    PubMed  CAS  Google Scholar 

  15. Heinemann T, Leiss O, von Bergmann K (1986) Effects of low-dose sitostanol on serum cholesterol in patients with hypercholesterolemia. Atherosclerosis 61: 219–223

    Article  PubMed  CAS  Google Scholar 

  16. Ikeda I, Sugano M (1978) Comparison of absorption and metabolism of beta-sitosterol and beta-sitostanol in rats. Atherosclerosis 30: 227–237

    Article  PubMed  CAS  Google Scholar 

  17. Chandler RF, Hooper SN, Ismail HA (1979) Antihypercholesterolemic studies with sterols: beta-sitosterol and stigmasterol. J Pharm Sci 68: 245–247

    Article  PubMed  CAS  Google Scholar 

  18. 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

    PubMed  CAS  Google Scholar 

  19. 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

    PubMed  CAS  Google Scholar 

  20. Ivy AC, Lin TM, Karvinen F (1955) Absorption of dihydrocholesterol and soya sterols by the rat’s intestine. Am J Physol 183: 79–85

    CAS  Google Scholar 

  21. Armstrong MJ, Carey MC (1987) Thermodynamic and molecular determinants of sterol solubilities in bile salt micelles. J Lipid Res 28: 1144–1155

    PubMed  CAS  Google Scholar 

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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 (Suppl 1), S59–S63 (1991). https://doi.org/10.1007/BF03216292

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  • DOI: https://doi.org/10.1007/BF03216292

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