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Both dietary oleic acid and plant sterols are known to reduce the risk of cardiovascular disease. We have produced phytosteryl oleates through enzymatic reactions. Cardiovascular benefits of phytosteryl oleates were investigated in apolipoprotein E knockout (apo E-KO) mice over 7 weeks at an oral dose of 2% (w/w). The mice treated with phytosteryl oleates had significantly lower very-low-density lipoprotein-cholesterol (VLDL-C) and higher high-density lipoprotein-cholesterol (HDL-C) concentrations as compared to the control group. The treated group also had significantly higher levels of cholesterol, campesterol and sitosterol in faecal materials as compared to the control group. These changes were accompanied by significant reductions in the volume of atherosclerotic lesions in the aortic roots. Furthermore, histological and biochemical analysis of hepatic tissues showed comparable data between the 2 groups of mice. This plus comparable body weight gain suggest a higher degree of safety and tolerability for phytosteryl oleates over 7 weeks of experimentation in this animal model. The data so obtained suggest a strong anti-atherogenic activity for phytosteryl oleates in apo E-KO mice. Additional studies are needed to confirm such effects over a longer period of time in this and other relevant animal models.

Both dietary oleic acid and plant sterols are known to reduce the risk of cardiovascular disease. We have produced phytosteryl oleates through enzymatic reactions. Cardiovascular benefits of phytosteryl oleates were investigated in apolipoprotein E knockout (apo E-KO) mice over 7 weeks at an oral dose of 2% (w/w). The mice treated with phytosteryl oleates had significantly lower very-low-density lipoprotein-cholesterol (VLDL-C) and higher high-density lipoprotein-cholesterol (HDL-C) concentrations as compared to the control group. The treated group also had significantly higher levels of cholesterol, campesterol and sitosterol in faecal materials as compared to the control group. These changes were accompanied by significant reductions in the volume of atherosclerotic lesions in the aortic roots. Furthermore, histological and biochemical analysis of hepatic tissues showed comparable data between the 2 groups of mice. This plus comparable body weight gain suggest a higher degree of safety and tolerability for phytosteryl oleates over 7 weeks of experimentation in this animal model. The data so obtained suggest a strong anti-atherogenic activity for phytosteryl oleates in apo E-KO mice. Additional studies are needed to confirm such effects over a longer period of time in this and other relevant animal models. [ABSTRACT FROM AUTHOR]

Abstract: Phytosterols have attracted much attention in recent years due to their health benefits, such as cholesterol lowering, anti-inflammatory, anti-atherogenicity, and anti-cancer potential. Docosahexaenoic acid (DHA) has been demonstrated to possess cardioprotective and immune-enhancing effects. Esterification of phytosterols with DHA may render improved physiochemical properties such as solubility, miscibility, oxidative stability and hence bioactivity and bioavailability. Thus, phytosteryl docosahexaneates (PS-DHA) may offer both the benefits of phytosterols and DHA, possibly in a synergistic manner. Here, we describe a method for enzymatic synthesis of phytosteryl docosahexaneates and evaluation of metabolic and cardiovascular benefits in apo-E deficient (apo E-KO) mice. The structures of phytosteryl docosahexaneates were confirmed by infrared (IR) and high performance liquid chromatography–mass spectrometry (HPLC–MS) using both normal and reverse phase chromatography. Apo E-KO mice were fed with an atherogenic diet containing 2% (w/w) PS-DHA for 7weeks. Plasma lipid levels and the extent and complexity of atherosclerotic lesions were examined and compared with those in the control group. The PS-DHA-treated mice had significantly lower plasma cholesterol levels and three times smaller atherosclerotic lesions in the aortic roots. This pilot study suggests cardiovascular benefits for PS-DHA. Further experimental and clinical studies are needed to confirm such benefits of PS-DHA. [Copyright &y& Elsevier]