Absorption of three wine-related polyphenols in three different matrices by healthy subjects

Goldberg, David M.; Yan, Joseph; Soleas, George J.

doi:10.1016/s0009-9120(02)00397-1

Cited by 615 publications

(446 citation statements)

References 57 publications

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“…This notion is borne out by studies in mice, rats and dogs, which suggest consistently that resveratrol is well absorbed but avidly glucuronidated and sulphated both in the liver and in intestinal epithelial cells (Asensi et al, 2002;Juan et al, 2002;Marier et al, 2002). One study in humans also hints at a poor bioavailability of resveratrol (Goldberg et al, 2003). In the wake of the discovery of the interesting pharmacological properties of resveratrol, the trihydroxystilbene scaffold has become the subject of imaginative synthetic manipulations by medicinal chemists with the aim of generating novel congeners of pharmacological interest and to characterise structural features, which impart activity to the molecule.…”

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confidence: 99%

Pharmacokinetics in mice and growth-inhibitory properties of the putative cancer chemopreventive agent resveratrol and the synthetic analogue trans 3,4,5,4′-tetramethoxystilbene

et al. 2004

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Resveratrol (trans-3,5,4 0 -trihydroxystilbene) is a naturally occurring polyphenol with cancer chemopreventive properties in preclinical models of carcinogenesis, including those of colorectal cancer. Recently, a variety of analogues of resveratrol have been synthesised and investigated in in vitro assays. One analogue, 3,4,5,4 0 -tetramethoxystilbene (DMU 212), showed preferential growth-inhibitory and proapoptotic properties in transformed cells, when compared with their untransformed counterparts. As part of a chemoprevention drug development programme, the pharmacokinetic properties of DMU 212 were compared with those of resveratrol in the plasma, liver, kidney, lung, heart, brain and small intestinal and colonic mucosa of mice. DMU 212 or resveratrol (240 mg kg À1 ) were administered intragastrically, and drug concentrations were measured by HPLC. Metabolites were characterised by cochromatography with authentic reference compounds and were identified by mass spectrometry. The ratios of area of plasma or tissue concentration vs time curves of resveratrol over DMU 212 (AUC res /AUC DMU212 ) for the plasma, liver, small intestinal and colonic mucosa were 3.5, 5, 0.1 and 0.15, respectively. Thus, resveratrol afforded significantly higher levels than DMU 212 in the plasma and liver, while DMU 212 exhibited superior availability compared to resveratrol in the small intestine and colon. Resveratrol was metabolised to its sulphate or glucuronate conjugates, while DMU 212 underwent metabolic hydroxylation or single and double O-demethylation. DMU 212 and resveratrol inhibited the growth of human-derived colon cancer cells HCA-7 and HT-29 in vitro with IC 50 values of between 6 and 26 mM. In the light of the superior levels achieved in the gastrointestinal tract after the administration of DMU 212, when compared to resveratrol, the results provide a good rationale to evaluate DMU 212 as a colorectal cancer chemopreventive agent.

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confidence: 99%

Pharmacokinetics in mice and growth-inhibitory properties of the putative cancer chemopreventive agent resveratrol and the synthetic analogue trans 3,4,5,4′-tetramethoxystilbene

et al. 2004

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“…However, high micromolar concentrations of resveratrol and quercetin were required to modulate TF expression and other cellular activities (see Introduction). This plus poor absorption of these compounds in vivo [40][41][42] raise valid doubts about the importance of the individual polyphenolic constituents of red wine in providing the cardioprotective effect. However, earlier studies suggested that synergism could exist between wine phenolics in inhibiting platelet function [47] and in promoting antioxidation [48].…”

Section: Discussionmentioning

confidence: 99%

“…However, a 10 to 100 µM concentration of resveratrol or quercetin was required to suppress TF induction. In vivo pharmacokinetics data suggest that accumulation of such concentrations of resveratrol and quercetin is unlikely after moderate consumption of red wine [40][41][42].…”

Section: Introductionmentioning

confidence: 99%

Suppression of human monocyte tissue factor induction by red wine phenolics and synthetic derivatives of resveratrol

Kaur

Roberti

Raul

et al. 2007

Thrombosis Research

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Prevention of cardiovascular disease through nutritional supplements is growing in popularity throughout the world. Multiple epidemiologic studies found that moderate consumption of alcohol, particularly red wine, lowers mortality rates from coronary heart diseases (CHD). Chronic inflammation and atherosclerosis associated with CHD culminate in aberrant intravascular expression of tissue factor (TF), which triggers blood coagulation leading to thrombosis, a major cause for heart attack. We showed earlier that two red wine phenolics, resveratrol and quercetin, suppressed TF induction in endothelial cells. In the present study, we investigated efficacy of seven resveratrol derivatives, which were shown to be effective in regulating cancer cell growth in vitro at much lower concentrations than the parent compound resveratrol, in inhibiting TF induction in peripheral blood mononuclear cells (PBMCs). We also tested possible synergistic effects of resveratrol and quercetin with the other major red wine phenolics in suppression of lipopolysaccharide-induced TF expression in human PBMCs. We found that several resveratrol derivatives were 2-to 10-fold more efficient than resveratrol in inhibiting TF induction. Our study found no evidence for synergism among red wine polyphenolics. These data suggest that structural alterations of resveratrol can be effective in producing potent antithrombotic agents that will have therapeutic potential in the improvement of cardiovascular health and prevention of CHD. Among major red wine phenolics, quercetin appears to be the predominant suppressor of TF induction.

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“…Two isomeric forms ( cis and Trans ) of RSV exist in nature; however, only the trans form of RSV participates in the majority of biological activities because of its stability (Wu & Liu, 2013) (Figure 2). Despite 70% absorption of resveratrol in the body (Walle, 2011), studies performed on rats showed that its bioavailability is relatively low due to its rapid metabolism in the intestine and liver (Goldberg, Yan, & Soleas, 2003). RSV bioavailability exhibits a variability from one person to another that depends on age and gender (Nunes et al., 2009).…”

Section: Introductionmentioning

confidence: 99%

Resveratrol: A miraculous natural compound for diseases treatment

Koushki

Amiri-Dashatan

Ahmadi

et al. 2018

Food Science & Nutrition

210

109

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Resveratrol (3, 5, 4′‐trihydroxystilbene) is a nonflavonoid polyphenol that naturally occurs as phytoalexin. It is produced by plant sources such as grapes, apples, blueberries, plums, and peanut. This compound has critical roles in human health and is well known for its diverse biological activities such as antioxidant and anti‐inflammatory properties. Nowadays, due to rising incidence of different diseases such as cancer and diabetes, efforts to find novel and effective disease‐protective agents have led to the identification of plant‐derived compounds such as resveratrol. Furthermore, several in vitro and in vivo studies have revealed the effectiveness of resveratrol in various diseases such as diabetes mellitus, cardiovascular disease, metabolic syndrome, obesity, inflammatory, neurodegenerative, and age‐related diseases. This review presents an overview of currently available studies on preventive properties and essential molecular mechanisms involved in various diseases.

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Absorption of three wine-related polyphenols in three different matrices by healthy subjects

Cited by 615 publications

References 57 publications

Pharmacokinetics in mice and growth-inhibitory properties of the putative cancer chemopreventive agent resveratrol and the synthetic analogue trans 3,4,5,4′-tetramethoxystilbene

Pharmacokinetics in mice and growth-inhibitory properties of the putative cancer chemopreventive agent resveratrol and the synthetic analogue trans 3,4,5,4′-tetramethoxystilbene

Suppression of human monocyte tissue factor induction by red wine phenolics and synthetic derivatives of resveratrol

Resveratrol: A miraculous natural compound for diseases treatment

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