Resveratrol Bioavailability And Toxicity In Humans.
Charles-Henry Cottart, V. Nivet-Antoine, C. Laguillier-Morizot, J. Beaudeux
Published 2010 · Chemistry, Medicine
Download PDFAnalyze on Scholarcy
Numerous data are now available on the beneficial properties of the polyphenolic compound resveratrol including its anti-inflammatory and antitumor effects. However, few studies have been performed with resveratrol in humans, and the results of these studies appear fragmentary and sometimes contradictory due to variations in conditions of administration, protocols and methods of assessment. This review article presents the results of recent studies investigating the pharmacokinetics, bioavailability, and toxicity of resveratrol in humans. Resveratrol is well absorbed, rapidly metabolized, mainly into sulfo and glucuronides conjugates which are eliminated in urine. Resveratrol seems to be well tolerated and no marked toxicity was reported. These data are important in the context of human efficacy studies, and they provide further support for the use of resveratrol as a pharmacological drug in human medicine.
This paper references
Intestinal Breast Cancer Resistance Protein (BCRP)/Bcrp1 and Multidrug Resistance Protein 3 (MRP3)/Mrp3 Are Involved in the Pharmacokinetics of Resveratrol
K. van de Wetering (2009)
Structure-activity relationship of trans-resveratrol and its analogues.
Z. Ovesná (2005)
Resveratrol-loaded calcium-pectinate beads: effects of formulation parameters on drug release and bead characteristics.
S. Das (2010)
Effect of food on the pharmacokinetic profile of trans-resveratrol.
M. Vaz-da-Silva (2008)
Small molecule activators of sirtuins extend Saccharomyces cerevisiae lifespan
K. Howitz (2003)
Bioactivity and metabolism of trans-resveratrol orally administered to Wistar rats.
Elisabeth Wenzel (2005)
Postterm delivery: a challenge for epidemiologic research.
K. Shea (1998)
Uptake of diet resveratrol into the human low-density lipoprotein. Identification and quantification of resveratrol metabolites by liquid chromatography coupled with tandem mass spectrometry.
M. Urpi-Sardà (2005)
Safety studies conducted on high-purity trans-resveratrol in experimental animals.
Lonnie D Williams (2009)
Resveratrol glucuronides as the metabolites of resveratrol in humans: characterization, synthesis, and anti-HIV activity.
L. Wang (2004)
Determination of piceid and resveratrol in Spanish wines deriving from Monastrell (Vitis vinifera L.) grape variety.
Juan F Moreno-Labanda (2004)
Ultrasensitive assay for three polyphenols (catechin, quercetin and resveratrol) and their conjugates in biological fluids utilizing gas chromatography with mass selective detection.
G. Soleas (2001)
Bioavailability, metabolism and physiological impact of 4-oxo-flavonoids
C. Manach (1996)
Alcohol and Mortality in Middle‐Aged Men from Eastern France
S. Renaud (1998)
Synthesis and biological properties of new stilbene deri
P. de Medina
Resveratrol metabolites in urine as a biomarker of wine intake in free-living subjects: The PREDIMED Study.
R. Zamora-Ros (2009)
Distribution of [3H]trans-resveratrol in rat tissues following oral administration.
Manal Abd El-Mohsen (2006)
An LC-MS method for analyzing total resveratrol in grape juice, cranberry juice, and in wine.
Y. Wang (2002)
Urinary and plasma levels of resveratrol and quercetin in humans, mice, and rats after ingestion of pure compounds and grape juice.
X. Meng (2004)
Pharmacokinetic and safety profile of trans-resveratrol in a rising multiple-dose study in healthy volunteers.
L. Almeida (2009)
Plasma metabolites of quercetin and their antioxidant properties.
C. Morand (1998)
Molecular mechanisms of the chemopreventive effects of resveratrol and its analogs in colorectal cancer: key role of polyamines?
F. Wolter (2004)
Resveratrol oligomers from Vitis amurensis attenuate beta-amyloid-induced oxidative stress in PC12 cells.
M. H. Jang (2007)
Quantification of trans-resveratrol and its metabolites in rat plasma and tissues by HPLC.
M. Juan (2010)
HPLC-tandem mass spectrometric method to characterize resveratrol metabolism in humans.
M. Urpi-Sardà (2007)
Diagnostic performance of urinary resveratrol metabolites as a biomarker of moderate wine consumption.
R. Zamora-Ros (2006)
Phase I Dose Escalation Pharmacokinetic Study in Healthy Volunteers of Resveratrol, a Potential Cancer Chemopreventive Agent
D. Boocock (2007)
HIGH ABSORPTION BUT VERY LOW BIOAVAILABILITY OF ORAL RESVERATROL IN HUMANS
T. Walle (2004)
J. Biol. Chem
Resveratrol-loaded polymeric micelles protect cells from Abeta-induced oxidative stress.
Xiaowei Lu (2009)
Synthesis and biological properties of new stilbene derivatives of resveratrol as new selective aryl hydrocarbon modulators.
P. de Médina (2005)
Quantification of free and protein-bound trans-resveratrol metabolites and identification of trans-resveratrol-C/O-conjugated diglucuronides - two novel resveratrol metabolites in human plasma.
Alexander Burkon (2008)
Concentration of the Phytoalexin Resveratrol in Wine
E. Siemann (1992)
Synthesis and biological evaluation of resveratrol and analogues as apoptosis-inducing agents.
M. Roberti (2003)
Resveratrol improves health and survival of mice on a high-calorie diet
J. Baur (2006)
The daily oral administration of high doses of trans-resveratrol to rats for 28 days is not harmful.
M. Juan (2002)
Metabolism and bioavailability of trans-resveratrol.
Elisabeth Wenzel (2005)
Resveratrol-associated renal toxicity.
J. Crowell (2004)
Analysis of resveratrol in wine by capillary electrophoresis.
X. Gu (2000)
Absorption of three wine-related polyphenols in three different matrices by healthy subjects.
D. Goldberg (2003)
The cancer preventative agent resveratrol is converted to the anticancer agent piceatannol by the cytochrome P450 enzyme CYP1B1
G. Potter (2002)
Bioavailability of trans-resveratrol from red wine in humans.
P. Vitaglione (2005)
Cancer Prevention and Treatment with Resveratrol: From Rodent Studies to Clinical Trials
Anupam Bishayee (2009)
Distribution of [ 3 H ] trans-resveratrol in rat tissues following oral administration
M. A. El-Mohsen (2006)
Simple spectrophotometric assessment of the trans-/cis-resveratrol ratio in aqueous solutions.
L. Camont (2009)
Measurement of trans-resveratrol, (+)-catechin, and quercetin in rat and human blood and urine by gas chromatography with mass selective detection.
G. Soleas (2001)
Cancer chemopreventive and therapeutic potential of resveratrol: mechanistic perspectives.
J. Kundu (2008)
Synthesis and biological properties of new stilbene deri- Mol. Nutr
P. de Medina (2010)
Identification and bioactivities of resveratrol oligomers and flavonoids from Carex folliculata seeds.
L. Li (2009)
Metabolism and Disposition of Resveratrol in Rats: Extent of Absorption, Glucuronidation, and Enterohepatic Recirculation Evidenced by a Linked-Rat Model
J. Marier (2002)
Piceid, the major resveratrol derivative in grape juices.
A. Romero-Pérez (1999)
Deglucuronidation of a flavonoid, luteolin monoglucuronide, during inflammation.
K. Shimoi (2001)
Direct HPLC Analysis of cis- and trans-Resveratrol and Piceid Isomers in Spanish Red Vitis vinifera Wines
R. M. Lamuela-Raventós (1995)
Quantitation of trans-resveratrol and detection of its metabolites in human plasma and urine by high performance liquid chromatography.
D. Boocock (2007)
Molecular mechanisms of the chemopreventive effects of resveratrol and its analogs in carcinogenesis.
S. Ulrich (2005)
Determination of stilbenes (trans-astringin, cis- and trans-piceid, and cis- and trans-resveratrol) in Portuguese wines.
M. T. Ribeiro de Lima (1999)
Distribution of [14C]-trans-resveratrol, a cancer chemopreventive polyphenol, in mouse tissues after oral administration.
X. Vitrac (2003)
Quercetin glucuronide prevents VSMC hypertrophy by angiotensin II via the inhibition of JNK and AP-1 signaling pathway.
M. Yoshizumi (2002)
Resveratrol Promotes Clearance of Alzheimer's Disease Amyloid-β Peptides*
P. Marambaud (2005)
Alcohol, ischemic heart disease, and the french paradox
J. Constant (1997)
This paper is referenced by
Diabetic complications in pregnancy: is resveratrol a solution?
Chandra K Singh (2013)
Resveratrol enhances ionizing radiation-induced premature senescence in lung cancer cells
Hongmei Luo (2013)
Resveratrol, Potential Therapeutic Interest in Joint Disorders: A Critical Narrative Review
Christelle Nguyen (2017)
Determination of resveratrol and its sulfate and glucuronide metabolites in plasma by LC-MS/MS and their pharmacokinetics in dogs.
M. Muzzio (2012)
Resveratrol and Its Human Metabolites—Effects on Metabolic Health and Obesity
M. Springer (2019)
Resveratrol-loaded liposomes for topical treatment of the vaginal inflammation and infections.
May Wenche Jøraholmen (2015)
Modified resveratrol Longevinex improves endothelial function in adults with metabolic syndrome receiving standard treatment.
K. Fujitaka (2011)
Resveratrol ameliorates diabetes-related metabolic changes via activation of AMP-activated protein kinase and its downstream targets in db/db mice.
G. Do (2012)
Cytoprotective effect of resveratrol diastereomers in CHO-K1 cells exposed to beauvericin.
B. Mallebrera (2015)
The grape antioxidant resveratrol for skin disorders: promise, prospects, and challenges.
M. Ndiaye (2011)
Therapeutic targeting of replicative immortality
P. Yaswen (2015)
Resveratrol mediates anti-atherogenic effects on cholesterol flux in human macrophages and endothelium via PPARγ and adenosine.
I. Voloshyna (2013)
Health benefits of resveratrol: Evidence from clinical studies.
Akhand Pratap Singh (2019)
CArG-driven GADD 45 α activated by resveratrol inhibits lung cancer cells
Qiwen Shi (2015)
RESVERATROL: RECOMMENDING ITS WIDE INCREASE – A PREMATURE DECISION OR NOT? A REVIEW
Marieta Georgieva (2015)
Improved extraction of resveratrol and antioxidants from grape peel using heat and enzymatic treatments.
J. Averilla (2019)
Resveratrol and Alzheimer’s Disease: Mechanistic Insights
T. Ahmed (2016)
Modulation of bacterial ghosts – induced nitric oxide production in macrophages by bacterial ghost‐delivered resveratrol
V. Koller (2013)
Effects of resveratrol and cigarette smoking onbone healing: histomorphometric evaluation.
Özge Kolkesen Şahin (2016)
Resveratrol: Effects on Lipids and Cardiovascular Risk
Evan Paul Cherniack (2013)
Effect of Resveratrol Treatment on the Pharmacokinetics of Diclofenac in Healthy Human Volunteers.
Satish Kumar Bedada (2016)
Preclinical pharmacokinetics comparison between resveratrol 2-hydroxypropyl-β-cyclodextrin complex and resveratrol suspension after oral administration
Zhiqian Yang (2016)
Effets des polyphénols de vin rouge sur la prolifération cellulaire et sur le métabolisme du resvératrol
Frédéric Mazué (2011)
Role of resveratrol in the management of insulin resistance and related conditions: Mechanism of action
Ebrahim Abbasi Oshaghi (2017)
A novel red grape cells complex: health effects and bioavailability of natural resveratrol
M. Azachi (2014)
Nanostructured Chitosan-Based Biomaterials for Sustained and Colon-Specific Resveratrol Release
N. Iglesias (2019)
Plant polyphenols in prevention of heart disease.
E. Ginter (2012)
Resveratrol Modulates Cytokine-Induced JAK/STAT Activation More Efficiently than 5-Aminosalicylic Acid: An In Vitro Approach
Diana Serra (2014)
Leukocyte Production of Inflammatory Mediators Is Inhibited by the Antioxidants Phloretin, Silymarin, Hesperetin, and Resveratrol
J. B. Fordham (2014)
Deneysel sigara modelinde resveratrolün total oksidan/antioksidan kapasite üzerine etkilerinin araştırılması
Özge Sahin (2015)
Novel Apoptotic Regulators in Carcinogenesis
G. Chen (2012)
Resveratrol analogue 3,4,4′-trihydroxy-trans-stilbene induces apoptosis and autophagy in human non-small-cell lung cancer cells in vitro
L. Zhang (2015)See more