Effects of Dietary Cholesterol and Phytosterol Overload on Wistar Rat Plasma Lipids

Laraki, Loubaba; Pelletier, Xavier; Debry, G

doi:10.1159/000177649

Cited by 23 publications

(20 citation statements)

References 8 publications

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“…Both AO and PO are rich in ST, which is widely reported to reduce serum cholesterol levels in animals and humans (Laraki et al, 1991;Howard and Kritchevsky, 1997). The hypocholesterolemic effect of ST may be explained by two mechanisms including the inhibition of (a) cholesterol absorption and (b) hepatic cholesterol esterase.…”

Section: Impact Of Ao and Op Supplementation On The Plasma Lipid Profilementioning

confidence: 99%

Apricot and pumpkin oils reduce plasma cholesterol and triacylglycerol concentrations in rats fed a high-fat diet

Ramadan¹,

Zayed²,

Abozid³

et al. 2011

Grasas y Aceites

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Section: Impact Of Ao and Op Supplementation On The Plasma Lipid Profilementioning

confidence: 99%

Apricot and pumpkin oils reduce plasma cholesterol and triacylglycerol concentrations in rats fed a high-fat diet

Ramadan¹,

Zayed²,

Abozid³

et al. 2011

Grasas y Aceites

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“…[10][11][12][13] The potent ability of DANA87 to reduce plasma cholesterol levels could also be explained by inhibition or displacement of cholesterol by the b-sitosterol part of DANA87 from cholesterol-containing micelles, formed with bile acids in the small intestine, which are required for cholesterol absorption.…”

Section: Resultsmentioning

confidence: 99%

“…It has been known that they inhibit the absorption of dietary and endogenously produced cholesterol from the small intestine, reducing blood cholesterol concentrations both in animal models and in humans. [10][11][12][13] b-Sitosterol and b-sitostanol fatty acid esters were recently commercialized as food additives to reduce serum cholesterol levels. A novel hydrophilic phytostanol analogue, FM-VP4, was also developed to reduce serum cholesterol levels.…”

mentioning

confidence: 99%

Effect of a New .BETA.-Sitosterol Analogue on Plasma Lipid Concentrations in Rats

Song

Hong

Lim

et al. 2004

CHEMICAL & PHARMACEUTICAL BULLETIN

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A major risk factor for the development of coronary heart disease (CHD) or atherosclerosis is elevated levels of serum cholesterol. Recent clinical trials and studies have confirmed that lowering of low-density lipoprotein (LDL) cholesterol is related to a reduction in CHD risk.2,3) The reduction of serum cholesterol levels has mainly been accomplished by inhibiting cholesterol biosynthesis or by blocking the absorption of dietary cholesterol. Statins, such as pravastatin, that effectively inhibit cholesterol biosynthesis are HMG-CoA reductase (3-hydroxy-3-methylglutaryl-coenzyme A reductase) inhibitors and are widely prescribed in the treatment of hypercholesterolemia. 4,5) Several squalene synthesis inhibitors have been also reported.6,7) SCH-48461 (a trans-azetidinone) 8) and 4Љ,6Љ-bis((2-fluorophenyl)carbamoyl) b-O-cellobioside (a steriodal glycoside) 9) have recently been reported to be cholesterol absorption inhibitors.Phytosterols, or plant sterols, are an interesting class of compound due to their application and biological activities. The phytosterols found most frequently in nature are b-sitosterol, campesterol, and stigmasterol. It has been known that they inhibit the absorption of dietary and endogenously produced cholesterol from the small intestine, reducing blood cholesterol concentrations both in animal models and in humans.10-13) b-Sitosterol and b-sitostanol fatty acid esters were recently commercialized as food additives to reduce serum cholesterol levels. A novel hydrophilic phytostanol analogue, FM-VP4, was also developed to reduce serum cholesterol levels. 14)However, even with the current therapeutic agents, it is not easy to achieve proper plasma cholesterol levels without side effect. Therefore the discovery of more effective, well-tolerated agents that reduce high cholesterol levels is needed. We here report the synthesis and interesting pharmacologic properties of novel succinamic acid ester derivatives that are bsitosterol analogues, compounds 1 and 2, that have the ability to lower plasma cholesterol levels and that can be more effective cholesterol-lowering alternatives to b-sitosterol and bsitostanol fatty acid esters. ChemistryThe synthesis of b-sitosterol analogues 1 and 2 are summarized Chart 1. The b-sitosterol-3-hemisuccinate ester 1 was prepared by the reaction of b-sitosterol and succinic anhydride in toluene with a catalytic amount of DMAP.15) The chlorination of the resulting acid compound 1 with SOCl 2 and then direct amination with appropriate amines afforded N-substituted succinamic acid b-sitosteryl ester derivatives 2. Compounds 2 were also synthesized in 76-92% yields by the reaction of 1 with methyl chloroformate, followed by amination of the activated intermediate. Interestingly, compound 2a (DANA87) was also easily obtained in one step by the direct addition of b-sitosterol to dicyclohexylcarbodiimide (DCC) in 80% yield. It was considered that compound DANA87 was prepared by slow thermal degradation of the N-Substituted succinamic acid b b-sitosteryl ester derivat...

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“…This initial observation was soon confirmed in humans by Pollak (28) who reported a significant reduction in plasma total cholesterol levels of about 28% in 26 healthy subjects fed plant sterols at a dose ranging from 5.7-10 g/day for 2 weeks. Thereafter, a series of experiments have been conducted on a number of animals including rabbits (28), mice (29), rats (30,31) and hamsters (32). Results from these studies have shown that plant sterols and stanols significantly reduce total plasma cholesterol, LDL-cholesterol (LDL-C) and liver cholesterol concentrations.…”

Section: Cholesterol-lowering Effect Of Phytosterolsmentioning

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 Dietary Cholesterol and Phytosterol Overload on Wistar Rat Plasma Lipids

Cited by 23 publications

References 8 publications

Apricot and pumpkin oils reduce plasma cholesterol and triacylglycerol concentrations in rats fed a high-fat diet

Apricot and pumpkin oils reduce plasma cholesterol and triacylglycerol concentrations in rats fed a high-fat diet

Effect of a New .BETA.-Sitosterol Analogue on Plasma Lipid Concentrations in Rats

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

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