Effects of disodium ascorbyl phytostanol phosphates (FM-VP4) on cholesterol accumulation within rat intestinal cells

Yau, Edwin; Boulanger, Kathy D.; Ramswamy, Manisha; Pritchard, P H

doi:10.1208/ps050106

Cited by 8 publications

(6 citation statements)

References 9 publications

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“…In an in vitro study, DAPP decreased cholesterol accumulation in Caco-2 cells, suggesting that DAPP may modify some extracellular mechanisms of cholesterol influx and efflux (41). Most recently, Wasan et al (42) observed that DAPP reduced the accumulation of cholesterol in cultured rat small intestinal crypt cells and speculated that DAPP might inhibit the interaction of cholesterol or cholesterol micelles with the receptors of enterocytes or act as an antagonist of cholesterol influx channels. Transporters of the ATPbinding cassette (ABC) family appear to play important roles in regulating cholesterol absorption and excretion (43,44).…”

Section: Discussionmentioning

confidence: 99%

Effects of a water‐soluble phytostanol ester on plasma cholesterol levels and red blood cell fragility in hamsters

Ebine¹,

Xiao-ming²,

Demonty³

et al. 2005

Lipids

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The aim of this study was to assess the efficacy of a novel water‐soluble phytostanol anolog, disodium ascorbyl phytostanyl phosphate (DAPP), on plasma lipid levels and red blood cell fragility in hamsters fed atherogenic diets. For 4 wk, 50 male Golden Syrian hamsters were fed a semipurified diet without added cholesterol (noncholesterol, group 1), or a semipurified diet with 0.25% cholesterol (cholesterol‐control, group 2). Groups 3–5 were fed the cholesterol‐control diet with an addition of 1% phytostanols (diet 3), 0.71% DAPP (DAPP 0.7%, diet 4), or 1.43% DAPP (DAPP 1.4%, diet 5). Diets 4 and 5 provided 0.5 and 1% phytostanols, respectively. Supplementation of 0.71 and 1.43% DAPP decreased plasma total cholesterol concentrations by 34 (P<0.001) and 46% (P<0.001), respectively, in comparison with the cholesterol‐control group, whereas free stanols reduced (P=0.007) plasma cholesterol concentrations by 14%. Similarly, non‐HDL‐cholesterol concentrations were reduced by 39 (P<0.001) and 54% (P<0.001) in hamsters supplemented with DAPP 0.7% and DAPP 1.4%, respectively, relative to the cholesterol‐control group. The hypocholesterolemic effect of DAPP 1.4% was threefold stronger than that of free stanols. In hamsters supplemented with DAPP 1.4%, plasma TG concentrations were 45% lower (P=0.018) than in cholesterol‐control‐fed hamsters, whereas no such beneficial effect was observed in the free stanol group. Erythrocyte fragility was unaffected by DAPP or free phytostanols. Results of the current study demonstrate that DAPP lowers cholesterol more efficiently than free stanols, without an adverse effect on erythrocyte fragility in hamsters.

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Section: Discussionmentioning

confidence: 99%

Effects of a water‐soluble phytostanol ester on plasma cholesterol levels and red blood cell fragility in hamsters

Ebine¹,

Xiao-ming²,

Demonty³

et al. 2005

Lipids

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“…Further work by Bhadra and Subbiah showed a significant reduction in cellular cholesterol content with a corresponding increase in sitosterol concentration in human skin fibroblasts and HepG2 cells incubated with liposomes containing sitosterol 26. Recent findings by our laboratory reported that the incubation of Caco‐2 and IEC‐6 cells with FM‐VP4 decreased uptake of cholesterol from the incubation medium 27,28…”

Section: Discussionmentioning

confidence: 75%

“…Phytostanol Phosphoryl Ascorbate (FM‐VP4; Fig. 1) is a water‐soluble phytostanol mixture composed of sitostanol and campestanol ascorbate that has been shown to decrease cholesterol gastrointestinal absorption1–4 and cellular accumulation 27,28. Recent studies from our laboratory have observed that when rats were coadministered FM‐VP4 with radiolabeled and cold cholesterol incorporated into a lipid emulsion (Intralipid ® ), the area under [ 3 H]cholesterol concentration vs. time curve and maximum plasma concentration of [ 3 H]cholesterol were decreased in a dose‐dependent manner 1,2.…”

Section: Introductionmentioning

confidence: 99%

Influence of Phytostanol Phosphoryl Ascorbate (FM-VP4) on Insulin Resistance, Hyperglycemia, Plasma Lipid Levels, and Gastrointestinal Absorption of Exogenous Cholesterol in Zucker (fa/fa) Fatty and Lean Rats

Zamfir

Pritchard

Pederson

2003

Journal of Pharmaceutical Sciences

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“…This mechanism has been illustrated by an in vitro cholesterol uptake study using cells derived from the duodenal and jejunal segments of rat small intestine (184). In that study, rat intestinal epithelial crypt cells (IEC-6) were incubated with [ (184).…”

Section: Mechanism Of Action Of Disodium Ascorbyl Phytostanyl Phosphatementioning

confidence: 99%

Lipid-lowering Activity of Natural and Semi-Synthetic Sterols and Stanols

2015

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-Consumption of plant sterols/ stanols has long been demonstrated to reduce plasma cholesterol levels. The objective of this review is to demonstrate the lipid-lowering activity and antiatherogenic effects of natural and semi-synthetic plant sterols/ stanols based on evidence from cell-culture studies, animal studies and clinical trials. Additionally, this review highlights certain molecular mechanisms by which plant sterols/ stanols lower plasma cholesterol levels with a special emphasis on factors that affect the cholesterol-lowering activity of plant sterols/stanols. The crystalline nature and the poor oil solubility of these natural products could be important factors that limit their cholesterol-lowering efficiency. Several attempts have been made to improve the cholesterol-lowering activity by enhancing the bioavailability of crystalline sterols and stanols. Approaches involved reduction of the crystal size and/or esterification with fatty acids from vegetable or fish oils. However, the most promising approach in this context is the chemical modification of plant sterols /stanols into water soluble disodium ascorbyl phytostanyl phosphates analogue by esterification with ascorbic acid. This novel semi-synthetic stanol derivative has improved efficacy over natural plant sterols/ stanols and can provide additional benefits by combining the cholesterol-lowering properties of plant stanols with the antioxidant potential of ascorbic acid.

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Effects of disodium ascorbyl phytostanol phosphates (FM-VP4) on cholesterol accumulation within rat intestinal cells

Cited by 8 publications

References 9 publications

Effects of a water‐soluble phytostanol ester on plasma cholesterol levels and red blood cell fragility in hamsters

Effects of a water‐soluble phytostanol ester on plasma cholesterol levels and red blood cell fragility in hamsters

Influence of Phytostanol Phosphoryl Ascorbate (FM-VP4) on Insulin Resistance, Hyperglycemia, Plasma Lipid Levels, and Gastrointestinal Absorption of Exogenous Cholesterol in Zucker (fa/fa) Fatty and Lean Rats

Lipid-lowering Activity of Natural and Semi-Synthetic Sterols and Stanols

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