Beyond blood lipids: phytosterols, statins and omega-3 polyunsaturated fatty acid therapy for hyperlipidemia

Micallef, Michelle; Garg, Manohar L.

doi:10.1016/j.jnutbio.2009.06.009

Cited by 69 publications

(44 citation statements)

References 142 publications

(140 reference statements)

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“…According to the literature, this combination is safe for patients and produces no side effects (Eussen et al, 2010). Even when patients are intolerant to statins, nutraceuticals can have a fundamental role in treating dyslipidaemia (Micallef & Garg, 2009;Sikka et al, 2011;Stock, 2012). Panahi et al (2011) demonstrated that Heracleum persicum supplementation of atorvastatin at 10 mg allowed comparable reduction in lipid plasma levels to atorvastatin at 20 mg. H. persicum can be added to traditional lipid lowering therapy to reduce the dosage and, consequentially, the side effects related to statin administration (Panahi et al, 2011).…”

Section: Nutraceuticals Versus Lipid Lowering Drugs In Dyslipidaemia mentioning

confidence: 99%

Nutraceuticals and dyslipidaemia: Beyond the common therapeutics

Scicchitano

Cameli

Maiello³

et al. 2014

Journal of Functional Foods

322

236

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Section: Nutraceuticals Versus Lipid Lowering Drugs In Dyslipidaemia mentioning

confidence: 99%

Nutraceuticals and dyslipidaemia: Beyond the common therapeutics

Scicchitano

Cameli

Maiello³

et al. 2014

Journal of Functional Foods

322

236

View full text Add to dashboard Cite

“…Current strategies to control cholesterol levels in blood are based on: (i) restriction of cholesterol intake from the food (diet) (Micallef and Garg , 2009 ), (ii) reduction of cholesterol and bile acids absorption from the gut (ion-exchange resins (Ginsberg , 1995 ), microsomal triglyceride transport protein (MTP) inhibitors (Cuchel et al , 2007 ), Niemman-Pick C1 Like 1 protein inhibitors, (iii) inhibition of de novo cholesterol synthesis (statins, squalene synthase, 2,3-oxidosqualene cyclase, squalene monooxygenase inhibitors) (Endo et al , 1976 ;Grundy , 1988 ), (iv) inhibition of LDL particles formation (proprotein convertase subtilisin/kexin type 9 (PCSK9) antisense oligonucleotides) (Rizzo , 2010 ), (v) increasing the number of LDL receptors (enhancers of LDL receptors synthesis and inhibitors of its degradation) (Boguslawski, 1993 ;Lagace et al , 2006 ;Graham et al , 2007 ;Shan et al , 2008 ), and (vi) raising high-density lipoprotein levels (cholesteryl ester transfer protein (CETP) inhibitors) (Barter et al , 2007 ). All of these are sophisticated but none of them fully cover patients ' demands (Katsnelson, 2010 ).…”

Section: Current Strategies For Lowering Cholesterol Level In Bloodmentioning

confidence: 99%

“…Daily cholesterol consumption is approximately 500 mg and it is even two times higher than average in developing countries (Callejo Gimenez et al , 2003 ). Cardiovascular prevention must therefore target sedentary lifestyle, excess weight, and favor low-calorie, low-fat diet and natural compounds with potential cardiovascular benefi ts, such as phytosterols, omega-3 fatty acids (Butt et al , 2009 ;Micallef and Garg , 2009 ;Smart et al , 2011 ). Therapeutic education holds a growing and complementary role in the public health system (Baudet et al , 2011 ).…”

Section: Current Strategies For Lowering Cholesterol Level In Bloodmentioning

confidence: 99%

Squalene monooxygenase – a target for hypercholesterolemic therapy

Belter¹,

Skupińska²,

Giel-Pietraszuk

et al. 2011

BCHM

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Squalene monooxygenase catalyzes the epoxidation of C-C double bond of squalene to yield 2,3-oxidosqualene, the key step of sterol biosynthesis pathways in eukaryotes. Sterols are essential compounds of these organisms and squalene epoxidation is an important regulatory point in their synthesis. Squalene monooxygenase downregulation in vertebrates and fungi decreases synthesis of cholesterol and ergosterol, respectively, which makes squalene monooxygenase a potent and attractive target of hypercholesterolemia and antifungal therapies. Currently some fungal squalene monooxygenase inhibitors (terbinafi ne, naftifi ne, butenafi ne) are in clinical use, whereas mammalian enzymes ' inhibitors are still under investigation. Research on new squalene monooxygenase inhibitors is important due to the prevalence of hypercholesterolemia and the lack of both suffi cient and safe remedies. In this paper we (i) review data on activity and the structure of squalene monooxygenase, (ii) present its inhibitors, (iii) compare current strategies of lowering cholesterol level in blood with some of the most promising strategies, (iv) underline advantages of squalene monooxygenase as a target for hypercholesterolemia therapy, and (v) discuss safety concerns about hypercholesterolemia therapy based on inhibition of cellular cholesterol biosynthesis and potential usage of squalene monooxygenase inhibitors in clinical practice. After many years of use of statins there is some clinical evidence for their adverse effects and only partial effectiveness. Currently they are drugs of choice but are used with many restrictions, especially in case of children, elderly patients and women of childbearing potential. Certainly, for the next few years, statins will continue to be a suitable tool for cost-effective cardiovascular prevention; however research on new hypolipidemic drugs is highly desirable. We suggest that squalene monooxygenase inhibitors could become the hypocholesterolemic agents of the future.

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“…The presence of subclinical inflammation along with hyperlipidemia has been well documented in the development of metabolic disorders (Kuipers et al 2011;Raymond et al 2006). Hyperlipidemia is commonly characterized by elevated circulating triacylglycerols and lowdensity lipoprotein (LDL)-cholesterol and reduced highdensity lipoprotein (HDL)-cholesterol (Micallef and Garg 2009). The adipose tissue is recognized for its participation in various physiological and pathophysiological activities (Antuna-Puente et al 2008).…”

Section: Introductionmentioning

confidence: 99%

Novel quercetin-3-O-glucoside eicosapentaenoic acid ester ameliorates inflammation and hyperlipidemia

et al. 2015

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Quercetin, a major flavonol, present abundantly in apples and onions, is widely studied for ameliorating metabolic syndrome abnormalities. However, quercetin is mainly present in plant food in the form of quercetin glycosides and has been reported for poor gastrointestinal absorption. The present study was designed with the purpose of imparting a lipophilic property to quercetin-3-O-glucoside (QG) by its acylation with eicosapentaenoic acid (EPA) and to study the influence of eicosapentaenoic acid ester of quercetin-3-O-glucoside (QE) on hyperlipidemia and inflammation in vivo and in vitro. QE was more effective in reducing the production of tumor necrosis factor-alpha (TNF-α), prostaglandin 2 (PGE2), cyclo-oxygenase (COX)-2 levels and nuclear expression of nuclear factor-kappa B (NF-кB) compared to the parent compounds (QG and EPA) and commercial drugs, after lipopolysaccharides (LPS) induced inflammation in THP-1 derived macrophages. Serum high-density lipoprotein (HDL)-cholesterol was significantly higher and hepatic total cholesterol concentration was lower in the rats fed high-fat diet supplemented with QE, compared to the high-fat diet with inflammation (HFL). The serum concentrations of C-reactive protein (CRP), interleukin (IL)-6, and interferon-gamma (IFN-γ) were significantly lower in QE treatment group than HFL group. EPA conjugated flavonol, QE, had significant anti-inflammatory and hypolipidemic properties and may be effective for the treatment of obesity-related disorders.

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Beyond blood lipids: phytosterols, statins and omega-3 polyunsaturated fatty acid therapy for hyperlipidemia

Cited by 69 publications

References 142 publications

Nutraceuticals and dyslipidaemia: Beyond the common therapeutics

Nutraceuticals and dyslipidaemia: Beyond the common therapeutics

Squalene monooxygenase – a target for hypercholesterolemic therapy

Novel quercetin-3-O-glucoside eicosapentaenoic acid ester ameliorates inflammation and hyperlipidemia

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