Bioactivity of dietary polyphenols: The role of metabolites

Luca, Simon Vlad; Macovei, Irina; Bujor, Alexandra; Miron, Anca; Skalicka-Woźniak, Krystyna; Aprotosoaie, Ana Clara; Trifan, Anca

doi:10.1080/10408398.2018.1546669

Cited by 494 publications

(367 citation statements)

References 265 publications

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“…RSV has important effects on adipose tissue due to its ability to inhibit differentiation of preadipocytes and stimulation of lipolysis. Thus, RSV inhibits proliferation and adipogenic differentiation of human preadipocytes by a SIRT1-dependent mechanism and in the 3T3 cells downregulate the expression of PPARγ, CCAAT-enhancer-binding proteins α (C/EBPα), SREBP-1c, FAS and lipoprotein lipase (LPL), which are important regulators of the lipolysis [113]. RSV has protective effects in terms of CVD risk due to its capacity to improve PON1 activity.…”

Section: Stilbenesmentioning

confidence: 99%

“…Ingested quercetin is rapidly eliminated as metabolites through feces and urine. The bioavailability of quercetin orally administered to humans was estimated at~45% with 3.3-5.7% of the dose found in the urine and 0.2-4.6% in the feces [113,157].…”

Section: Flavonolsmentioning

confidence: 99%

“…A small part of the intake of isoflavone aglycones (10%) is absorbed from the small intestine and metabolized in the liver. Most of the ingested isoflavone (90%) undergoes different transformations under gut microbiota action in the colon [113].…”

Section: Isoflavonesmentioning

confidence: 99%

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Phenolic Compounds Exerting Lipid-Regulatory, Anti-Inflammatory and Epigenetic Effects as Complementary Treatments in Cardiovascular Diseases

et al. 2020

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Atherosclerosis is the main process behind cardiovascular diseases (CVD), maladies which continue to be responsible for up to 70% of death worldwide. Despite the ongoing development of new and potent drugs, their incomplete efficacy, partial intolerance and numerous side effects make the search for new alternatives worthwhile. The focus of the scientific world turned to the potential of natural active compounds to prevent and treat CVD. Essential for effective prevention or treatment based on phytochemicals is to know their mechanisms of action according to their bioavailability and dosage. The present review is focused on the latest data about phenolic compounds and aims to collect and correlate the reliable existing knowledge concerning their molecular mechanisms of action to counteract important risk factors that contribute to the initiation and development of atherosclerosis: dyslipidemia, and oxidative and inflammatory-stress. The selection of phenolic compounds was made to prove their multiple benefic effects and endorse them as CVD remedies, complementary to allopathic drugs. The review also highlights some aspects that still need clear scientific explanations and draws up some new molecular approaches to validate phenolic compounds for CVD complementary therapy in the near future.In the last decade the scientific researchers turned their attention to phytochemicals, as effective, safe and low-cost natural bioactive compounds for CVD treatment.Dyslipidemia consists of increased blood concentrations of total cholesterol (TC), low density lipoproteins-cholesterol (LDL-C) and/or triglycerides (TG), and decreased high density lipoproteins-cholesterol (HDL-C) [6]. The lipid metabolism is complex and the candidate mechanisms that could generate dyslipidemia include: (i) excessive dietary lipid absorption in the small intestine; (ii) packing of exogenous lipids with cholesterol and fatty acids produced de novo in the liver and their secretion as very low density lipoproteins (VLDL); (iii) hydrolysis of TG from VLDL by lipases and their conversion into LDL, which are taken up by the peripheral tissues through LDL receptor (LDL-R) and scavenger receptors; (iv) diminished production of HDL by the liver and small intestine, thereby decreasing reverse cholesterol transport (RCT) from the peripheral tissues to the liver; (v) lowered excess cholesterol excretion from the liver into gallbladder or to the intestinal lumen through the ATP-binding cassette G5 and G8 transporters (ABCG5/G8) that facilitate trans-intestinal cholesterol efflux (TICE). Dyslipidemia is associated with the accumulation of LDL in the sub-endothelium of the artery wall. At this site, LDL undergoes oxidative modifications (oxLDL) that trigger inflammatory responses, and is taken up by the monocyte-derived macrophages infiltrated in the sub-endothelium which thus become lipid-loaded foam cells, the hallmark of atheroma development [7]. Until now, the most effective lipid-lowering treatment for hyperlipidemic patients was the statin therapy. But recen...

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Section: Stilbenesmentioning

confidence: 99%

Section: Flavonolsmentioning

confidence: 99%

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Phenolic Compounds Exerting Lipid-Regulatory, Anti-Inflammatory and Epigenetic Effects as Complementary Treatments in Cardiovascular Diseases

et al. 2020

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“…Polyphenols are a highly versatile group of natural substances, divided into several subclasses, and by virtue of their abundance in a vast spectrum of edible plant materials, they have been a subject of intense research [7]. Some of the major properties of polyphenols associated with their pharmacological potency and biological effects are their antioxidant, anti-inflammatory, cardioprotective and chemopreventive activities [8,9].…”

Section: Introductionmentioning

confidence: 99%

Polyphenol Extraction from Humulus lupulus (Hop) Using a Neoteric Glycerol/L-Alanine Deep Eutectic Solvent: Optimisation, Kinetics and the Effect of Ultrasound-Assisted Pretreatment

et al. 2019

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The investigation presented herein had as its scope the development of an integrated process for the efficient extraction of polyphenols from hop. For this purpose, a novel, natural deep eutectic solvent (DES) was synthesised, composed of glycerol and L-alanine, and the process was optimised by deploying a response surface methodology based on a Box-Behnken design. The variables considered were the DES/water proportion, the liquid-to-solid ratio and the stirring speed. Under the optimised conditions, the yield in total polyphenols achieved was 118.97 ± 8.27 mg gallic acid equivalents per g of dry mass. Ultrasonication, incorporated into the process as a pretreatment step, was shown to significantly change the kinetic pattern of polyphenol extraction and contributed to attaining higher yields only at 80 • C, whereas at lower temperatures a supressing effect was observed. Furthermore, increasing temperature was negatively correlated with the second-order extraction rates, evidencing a slow-down of the extraction rate at elevated temperatures.

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“…This is the case of quercetin‐3‐ O ‐rutinoside (rutin), a glycosylated flavonoid with broad therapeutic interest due to its antidiabetic effect, among other demonstrated pharmacological activity . Its low bioavailability is a result of its low aqueous solubility and intestinal metabolism, when rutin turns into quercetin (its aglycone) and other by‐products …”

Section: Introductionmentioning

confidence: 99%

Matrix effects of the hydroethanolic extract and the butanol fraction of calyces from Physalis peruviana L. on the biopharmaceutics classification of rutin

Moré

Feltrin

Brambila

et al. 2020

Journal of Pharmacy and Pharmacology

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Objectives The Biopharmaceutics Classification System (BCS) categorizes active pharmaceutical ingredients according to their solubility and permeability properties, which are susceptible to matrix or formulation effects. The aim of this research was to evaluate the matrix effects of a hydroethanolic extract of calyces from Physalis peruviana L. (HEE) and its butanol fraction (BF), on the biopharmaceutics classification of their major compound, quercetin‐3‐O‐rutinoside (rutin, RU). Methods Rutin was quantified by HPLC‐UV, and Caco‐2 cell monolayer transport studies were performed to obtain the apparent permeability values (Papp). Aqueous solubility was determined at pH 6.8 and 7.4. Key findings The Papp values followed this order: BF > HEE > RU (1.77 ± 0.02 > 1.53 ± 0.07 > 0.90 ± 0.03 × 10−5 cm/s). The lowest solubility values followed this order: HEE > RU > BF (2.988 ± 0.07 > 0.205 ± 0.002 > 0.189 ± 0.005 mg/ml). Conclusions According to these results, rutin could be classified as BCS classes III (high solubility/low permeability) and IV (low solubility/low permeability), depending on the plant matrix. Further work needs to be done in order to establish how apply the BCS for research and development of new botanical drugs or for bioequivalence purposes.

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Bioactivity of dietary polyphenols: The role of metabolites

Cited by 494 publications

References 265 publications

Phenolic Compounds Exerting Lipid-Regulatory, Anti-Inflammatory and Epigenetic Effects as Complementary Treatments in Cardiovascular Diseases

Phenolic Compounds Exerting Lipid-Regulatory, Anti-Inflammatory and Epigenetic Effects as Complementary Treatments in Cardiovascular Diseases

Polyphenol Extraction from Humulus lupulus (Hop) Using a Neoteric Glycerol/L-Alanine Deep Eutectic Solvent: Optimisation, Kinetics and the Effect of Ultrasound-Assisted Pretreatment

Matrix effects of the hydroethanolic extract and the butanol fraction of calyces from Physalis peruviana L. on the biopharmaceutics classification of rutin

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