Resveratrol

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Ketan R Patel - One of the best experts on this subject based on the ideXlab platform.

  • repeat dose study of the cancer chemopreventive agent Resveratrol in healthy volunteers safety pharmacokinetics and effect on the insulin like growth factor axis
    Cancer Research, 2010
    Co-Authors: Victoria A Brown, Ketan R Patel, Maria Viskaduraki, Tristan D Booth, Marjorie Perloff, James A Crowell, Anna M Schinas, Grygoriy Vasilinin, Gianfranca Piccirilli, Karen Brown
    Abstract:

    Resveratrol, a naturally occurring polyphenol, has cancer chemopreventive properties in preclinical models. It has been shown to downregulate the levels of insulin-like growth factor-1 (IGF-I) in rodents. The purpose of the study was to assess its safety, pharmacokinetics, and effects on circulating levels of IGF-I and IGF-binding protein-3 (IGFBP-3) after repeated dosing. Forty healthy volunteers ingested Resveratrol at 0.5, 1.0, 2.5, or 5.0 g daily for 29 days. Levels of Resveratrol and its metabolites were measured by high performance liquid chromatography-UV in plasma obtained before and up to 24 hours after a dose between days 21 and 28. IGF-I and IGFBP-3 were measured by ELISA in plasma taken predosing and on day 29. Resveratrol was safe, but the 2.5 and 5 g doses caused mild to moderate gastrointestinal symptoms. Resveratrol-3-O-sulfate, Resveratrol-4′-O-glucuronide, and Resveratrol-3-O-glucuronide were major plasma metabolites. Maximal plasma levels and areas under the concentration versus time curve for the metabolites dramatically exceeded those for Resveratrol, in the case of areas under the concentration versus time curve, by up to 20.3-fold. Compared with predosing values, the ingestion of Resveratrol caused a decrease in circulating IGF-I and IGFBP-3 (P

  • clinical pharmacology of Resveratrol and its metabolites in colorectal cancer patients
    Cancer Research, 2010
    Co-Authors: Ketan R Patel, Victoria A Brown, Donald J L Jones, Robert G Britton, David Hemingway, A S Miller, Kevin West, Tristan D Booth, Marjorie Perloff, James A Crowell
    Abstract:

    Resveratrol is a phytochemical with chemopreventive activity in preclinical rodent models of colorectal carcinogenesis. Antiproliferation is one of the many chemopreventive modes of action it has been shown to engage in. Concentrations of Resveratrol, which can be achieved in human tissues after p.o. administration, have not yet been defined. The purpose of this study was to measure concentrations of Resveratrol and its metabolites in the colorectal tissue of humans who ingested Resveratrol. Twenty patients with histologically confirmed colorectal cancer consumed eight daily doses of Resveratrol at 0.5 or 1.0 g before surgical resection. Resveratrol was found to be well tolerated. Normal and malignant biopsy tissue samples were obtained before dosing. Parent compound plus its metabolites Resveratrol-3-O-glucuronide, Resveratrol-4'-O-glucuronide, Resveratrol-3-O-sulfate, Resveratrol-4'-O-sulfate, Resveratrol sulfate glucuronide, and Resveratrol disulfate were identified by high-performance liquid chromatography (HPLC) with UV or mass spectrometric detection in colorectal resection tissue. Quantitation was achieved by HPLC/UV. Cell proliferation, as reflected by Ki-67 staining, was compared in preintervention and postintervention tissue samples. Resveratrol and Resveratrol-3-O-glucuronide were recovered from tissues at maximal mean concentrations of 674 and 86.0 nmol/g, respectively. Levels of Resveratrol and its metabolites were consistently higher in tissues originating in the right side of the colon compared with the left. Consumption of Resveratrol reduced tumor cell proliferation by 5% (P = 0.05). The results suggest that daily p.o. doses of Resveratrol at 0.5 or 1.0 g produce levels in the human gastrointestinal tract of an order of magnitude sufficient to elicit anticarcinogenic effects. Resveratrol merits further clinical evaluation as a potential colorectal cancer chemopreventive agent.

  • Repeat Dose Study of the Cancer Chemopreventive Agent Resveratrol in Healthy Volunteers : Safety , Pharmacokinetics , and Effect on the Insulin-like Growth Factor Axis
    Cancer Research, 2010
    Co-Authors: Victoria A Brown, Ketan R Patel, Maria Viskaduraki
    Abstract:

    Resveratrol, a naturally occurring polyphenol, has cancer chemopreventive properties in preclinical models. It has been shown to downregulate levels of insulin-like growth factor-1 (IGF-1) in rodents. The purpose of the study was to assess its safety, pharmacokinetics and effects on circulating levels of IGF-1 and insulin-like growth factor binding protein-3 (IGFBP-3) after repeated dosing. Forty healthy volunteers ingested Resveratrol at 0.5, 1.0, 2.5 or 5.0g daily for 29 days. Levels of Resveratrol and its metabolites were measured by HPLC-UV in plasma obtained before and up to 24h after a dose between days 21 and 28. IGF-1 and IGFBP-3 were measured by enzyme-linked immunosorbent assay in plasma taken pre-dosing and on day 29. Resveratrol was safe, but the 2.5 and 5g doses caused mild to moderate gastrointestinal symptoms. Resveratrol-3- O-sulfate, Resveratrol-4′-O-glucuronide and Resveratrol-3-O-glucuronide were major plasma metabolites. Maximal plasma levels and areas under the concentration versus time curve (AUC) for the metabolites dramatically exceeded those for Resveratrol, in the case of the AUC by up to 20.3-fold. Ingestion of Resveratrol caused a decrease in circulating IGF-1 and IGFBP-3 (P

  • phase i dose escalation pharmacokinetic study in healthy volunteers of Resveratrol a potential cancer chemopreventive agent
    Cancer Epidemiology Biomarkers & Prevention, 2007
    Co-Authors: David J Boocock, Ketan R Patel, Tristan D Booth, Marjorie Perloff, James A Crowell, Guy Faust, Anna M Schinas, Victoria Brown, Murray P Ducharme, Andreas J Gescher
    Abstract:

    The red grape constituent Resveratrol possesses cancer chemopreventive properties in rodents. The hypothesis was tested that, in healthy humans, p.o. administration of Resveratrol is safe and results in measurable plasma levels of Resveratrol. A phase I study of oral Resveratrol (single doses of 0.5, 1, 2.5, or 5 g) was conducted in 10 healthy volunteers per dose level. Resveratrol and its metabolites were identified in plasma and urine by high-performance liquid chromatography-tandem mass spectrometry and quantitated by high-performance liquid chromatography-UV. Consumption of Resveratrol did not cause serious adverse events. Resveratrol and six metabolites were recovered from plasma and urine. Peak plasma levels of Resveratrol at the highest dose were 539 ± 384 ng/mL (2.4 μmol/L, mean ± SD; n = 10), which occurred 1.5 h post-dose. Peak levels of two monoglucuronides and Resveratrol-3-sulfate were 3- to 8-fold higher. The area under the plasma concentration curve (AUC) values for Resveratrol-3-sulfate and Resveratrol monoglucuronides were up to 23 times greater than those of Resveratrol. Urinary excretion of Resveratrol and its metabolites was rapid, with 77% of all urinary agent-derived species excreted within 4 h after the lowest dose. Cancer chemopreventive effects of Resveratrol in cells in vitro require levels of at least 5 μmol/L. The results presented here intimate that consumption of high-dose Resveratrol might be insufficient to elicit systemic levels commensurate with cancer chemopreventive efficacy. However, the high systemic levels of Resveratrol conjugate metabolites suggest that their cancer chemopreventive properties warrant investigation. (Cancer Epidemiol Biomarkers Prev 2007;16(6):1246–52)

Victoria A Brown - One of the best experts on this subject based on the ideXlab platform.

  • repeat dose study of the cancer chemopreventive agent Resveratrol in healthy volunteers safety pharmacokinetics and effect on the insulin like growth factor axis
    Cancer Research, 2010
    Co-Authors: Victoria A Brown, Ketan R Patel, Maria Viskaduraki, Tristan D Booth, Marjorie Perloff, James A Crowell, Anna M Schinas, Grygoriy Vasilinin, Gianfranca Piccirilli, Karen Brown
    Abstract:

    Resveratrol, a naturally occurring polyphenol, has cancer chemopreventive properties in preclinical models. It has been shown to downregulate the levels of insulin-like growth factor-1 (IGF-I) in rodents. The purpose of the study was to assess its safety, pharmacokinetics, and effects on circulating levels of IGF-I and IGF-binding protein-3 (IGFBP-3) after repeated dosing. Forty healthy volunteers ingested Resveratrol at 0.5, 1.0, 2.5, or 5.0 g daily for 29 days. Levels of Resveratrol and its metabolites were measured by high performance liquid chromatography-UV in plasma obtained before and up to 24 hours after a dose between days 21 and 28. IGF-I and IGFBP-3 were measured by ELISA in plasma taken predosing and on day 29. Resveratrol was safe, but the 2.5 and 5 g doses caused mild to moderate gastrointestinal symptoms. Resveratrol-3-O-sulfate, Resveratrol-4′-O-glucuronide, and Resveratrol-3-O-glucuronide were major plasma metabolites. Maximal plasma levels and areas under the concentration versus time curve for the metabolites dramatically exceeded those for Resveratrol, in the case of areas under the concentration versus time curve, by up to 20.3-fold. Compared with predosing values, the ingestion of Resveratrol caused a decrease in circulating IGF-I and IGFBP-3 (P

  • clinical pharmacology of Resveratrol and its metabolites in colorectal cancer patients
    Cancer Research, 2010
    Co-Authors: Ketan R Patel, Victoria A Brown, Donald J L Jones, Robert G Britton, David Hemingway, A S Miller, Kevin West, Tristan D Booth, Marjorie Perloff, James A Crowell
    Abstract:

    Resveratrol is a phytochemical with chemopreventive activity in preclinical rodent models of colorectal carcinogenesis. Antiproliferation is one of the many chemopreventive modes of action it has been shown to engage in. Concentrations of Resveratrol, which can be achieved in human tissues after p.o. administration, have not yet been defined. The purpose of this study was to measure concentrations of Resveratrol and its metabolites in the colorectal tissue of humans who ingested Resveratrol. Twenty patients with histologically confirmed colorectal cancer consumed eight daily doses of Resveratrol at 0.5 or 1.0 g before surgical resection. Resveratrol was found to be well tolerated. Normal and malignant biopsy tissue samples were obtained before dosing. Parent compound plus its metabolites Resveratrol-3-O-glucuronide, Resveratrol-4'-O-glucuronide, Resveratrol-3-O-sulfate, Resveratrol-4'-O-sulfate, Resveratrol sulfate glucuronide, and Resveratrol disulfate were identified by high-performance liquid chromatography (HPLC) with UV or mass spectrometric detection in colorectal resection tissue. Quantitation was achieved by HPLC/UV. Cell proliferation, as reflected by Ki-67 staining, was compared in preintervention and postintervention tissue samples. Resveratrol and Resveratrol-3-O-glucuronide were recovered from tissues at maximal mean concentrations of 674 and 86.0 nmol/g, respectively. Levels of Resveratrol and its metabolites were consistently higher in tissues originating in the right side of the colon compared with the left. Consumption of Resveratrol reduced tumor cell proliferation by 5% (P = 0.05). The results suggest that daily p.o. doses of Resveratrol at 0.5 or 1.0 g produce levels in the human gastrointestinal tract of an order of magnitude sufficient to elicit anticarcinogenic effects. Resveratrol merits further clinical evaluation as a potential colorectal cancer chemopreventive agent.

  • Repeat Dose Study of the Cancer Chemopreventive Agent Resveratrol in Healthy Volunteers : Safety , Pharmacokinetics , and Effect on the Insulin-like Growth Factor Axis
    Cancer Research, 2010
    Co-Authors: Victoria A Brown, Ketan R Patel, Maria Viskaduraki
    Abstract:

    Resveratrol, a naturally occurring polyphenol, has cancer chemopreventive properties in preclinical models. It has been shown to downregulate levels of insulin-like growth factor-1 (IGF-1) in rodents. The purpose of the study was to assess its safety, pharmacokinetics and effects on circulating levels of IGF-1 and insulin-like growth factor binding protein-3 (IGFBP-3) after repeated dosing. Forty healthy volunteers ingested Resveratrol at 0.5, 1.0, 2.5 or 5.0g daily for 29 days. Levels of Resveratrol and its metabolites were measured by HPLC-UV in plasma obtained before and up to 24h after a dose between days 21 and 28. IGF-1 and IGFBP-3 were measured by enzyme-linked immunosorbent assay in plasma taken pre-dosing and on day 29. Resveratrol was safe, but the 2.5 and 5g doses caused mild to moderate gastrointestinal symptoms. Resveratrol-3- O-sulfate, Resveratrol-4′-O-glucuronide and Resveratrol-3-O-glucuronide were major plasma metabolites. Maximal plasma levels and areas under the concentration versus time curve (AUC) for the metabolites dramatically exceeded those for Resveratrol, in the case of the AUC by up to 20.3-fold. Ingestion of Resveratrol caused a decrease in circulating IGF-1 and IGFBP-3 (P

Maria Viskaduraki - One of the best experts on this subject based on the ideXlab platform.

  • repeat dose study of the cancer chemopreventive agent Resveratrol in healthy volunteers safety pharmacokinetics and effect on the insulin like growth factor axis
    Cancer Research, 2010
    Co-Authors: Victoria A Brown, Ketan R Patel, Maria Viskaduraki, Tristan D Booth, Marjorie Perloff, James A Crowell, Anna M Schinas, Grygoriy Vasilinin, Gianfranca Piccirilli, Karen Brown
    Abstract:

    Resveratrol, a naturally occurring polyphenol, has cancer chemopreventive properties in preclinical models. It has been shown to downregulate the levels of insulin-like growth factor-1 (IGF-I) in rodents. The purpose of the study was to assess its safety, pharmacokinetics, and effects on circulating levels of IGF-I and IGF-binding protein-3 (IGFBP-3) after repeated dosing. Forty healthy volunteers ingested Resveratrol at 0.5, 1.0, 2.5, or 5.0 g daily for 29 days. Levels of Resveratrol and its metabolites were measured by high performance liquid chromatography-UV in plasma obtained before and up to 24 hours after a dose between days 21 and 28. IGF-I and IGFBP-3 were measured by ELISA in plasma taken predosing and on day 29. Resveratrol was safe, but the 2.5 and 5 g doses caused mild to moderate gastrointestinal symptoms. Resveratrol-3-O-sulfate, Resveratrol-4′-O-glucuronide, and Resveratrol-3-O-glucuronide were major plasma metabolites. Maximal plasma levels and areas under the concentration versus time curve for the metabolites dramatically exceeded those for Resveratrol, in the case of areas under the concentration versus time curve, by up to 20.3-fold. Compared with predosing values, the ingestion of Resveratrol caused a decrease in circulating IGF-I and IGFBP-3 (P

  • Repeat Dose Study of the Cancer Chemopreventive Agent Resveratrol in Healthy Volunteers : Safety , Pharmacokinetics , and Effect on the Insulin-like Growth Factor Axis
    Cancer Research, 2010
    Co-Authors: Victoria A Brown, Ketan R Patel, Maria Viskaduraki
    Abstract:

    Resveratrol, a naturally occurring polyphenol, has cancer chemopreventive properties in preclinical models. It has been shown to downregulate levels of insulin-like growth factor-1 (IGF-1) in rodents. The purpose of the study was to assess its safety, pharmacokinetics and effects on circulating levels of IGF-1 and insulin-like growth factor binding protein-3 (IGFBP-3) after repeated dosing. Forty healthy volunteers ingested Resveratrol at 0.5, 1.0, 2.5 or 5.0g daily for 29 days. Levels of Resveratrol and its metabolites were measured by HPLC-UV in plasma obtained before and up to 24h after a dose between days 21 and 28. IGF-1 and IGFBP-3 were measured by enzyme-linked immunosorbent assay in plasma taken pre-dosing and on day 29. Resveratrol was safe, but the 2.5 and 5g doses caused mild to moderate gastrointestinal symptoms. Resveratrol-3- O-sulfate, Resveratrol-4′-O-glucuronide and Resveratrol-3-O-glucuronide were major plasma metabolites. Maximal plasma levels and areas under the concentration versus time curve (AUC) for the metabolites dramatically exceeded those for Resveratrol, in the case of the AUC by up to 20.3-fold. Ingestion of Resveratrol caused a decrease in circulating IGF-1 and IGFBP-3 (P

Karen Brown - One of the best experts on this subject based on the ideXlab platform.

  • what is new for an old molecule systematic review and recommendations on the use of Resveratrol
    PLOS ONE, 2011
    Co-Authors: Ole Vang, Karen Brown, Nihal Ahmad, Clifton A Baile, Joseph A Baur, Anna Csiszar, Dominique Delmas, Carmem Gottfried, Partha Mukhopadhyay, Namasivayam Nalini
    Abstract:

    Background: Resveratrol is a natural compound suggested to have beneficial health effects. However, people are consuming Resveratrol for this reason without having the adequate scientific evidence for its effects in humans. Therefore, scientific valid recommendations concerning the human intake of Resveratrol based on available published scientific data are necessary. Such recommendations were formulated after the Resveratrol 2010 conference, held in September 2010 in Helsingor, Denmark. Methodology: Literature search in databases as PubMed and ISI Web of Science in combination with manual search was used to answer the following five questions: 1 Can Resveratrol be recommended in the prevention or treatment of human diseases?; 2 Are there observed ‘‘side effects’’ caused by the intake of Resveratrol in humans?; 3 What is the relevant dose of Resveratrol?; 4 What valid data are available regarding an effect in various species of experimental animals?; 5 Which relevant (overall) mechanisms of action of Resveratrol have been documented? Conclusions/Significance: The overall conclusion is that the published evidence is not sufficiently strong to justify a recommendation for the administration of Resveratrol to humans, beyond the dose which can be obtained from dietary sources. On the other hand, animal data are promising in prevention of various cancer types, coronary heart diseases and diabetes which strongly indicate the need for human clinical trials. Finally, we suggest directions for future research in Resveratrol regarding its mechanism of action and its safety and toxicology in human subjects.

  • repeat dose study of the cancer chemopreventive agent Resveratrol in healthy volunteers safety pharmacokinetics and effect on the insulin like growth factor axis
    Cancer Research, 2010
    Co-Authors: Victoria A Brown, Ketan R Patel, Maria Viskaduraki, Tristan D Booth, Marjorie Perloff, James A Crowell, Anna M Schinas, Grygoriy Vasilinin, Gianfranca Piccirilli, Karen Brown
    Abstract:

    Resveratrol, a naturally occurring polyphenol, has cancer chemopreventive properties in preclinical models. It has been shown to downregulate the levels of insulin-like growth factor-1 (IGF-I) in rodents. The purpose of the study was to assess its safety, pharmacokinetics, and effects on circulating levels of IGF-I and IGF-binding protein-3 (IGFBP-3) after repeated dosing. Forty healthy volunteers ingested Resveratrol at 0.5, 1.0, 2.5, or 5.0 g daily for 29 days. Levels of Resveratrol and its metabolites were measured by high performance liquid chromatography-UV in plasma obtained before and up to 24 hours after a dose between days 21 and 28. IGF-I and IGFBP-3 were measured by ELISA in plasma taken predosing and on day 29. Resveratrol was safe, but the 2.5 and 5 g doses caused mild to moderate gastrointestinal symptoms. Resveratrol-3-O-sulfate, Resveratrol-4′-O-glucuronide, and Resveratrol-3-O-glucuronide were major plasma metabolites. Maximal plasma levels and areas under the concentration versus time curve for the metabolites dramatically exceeded those for Resveratrol, in the case of areas under the concentration versus time curve, by up to 20.3-fold. Compared with predosing values, the ingestion of Resveratrol caused a decrease in circulating IGF-I and IGFBP-3 (P

James A Crowell - One of the best experts on this subject based on the ideXlab platform.

  • repeat dose study of the cancer chemopreventive agent Resveratrol in healthy volunteers safety pharmacokinetics and effect on the insulin like growth factor axis
    Cancer Research, 2010
    Co-Authors: Victoria A Brown, Ketan R Patel, Maria Viskaduraki, Tristan D Booth, Marjorie Perloff, James A Crowell, Anna M Schinas, Grygoriy Vasilinin, Gianfranca Piccirilli, Karen Brown
    Abstract:

    Resveratrol, a naturally occurring polyphenol, has cancer chemopreventive properties in preclinical models. It has been shown to downregulate the levels of insulin-like growth factor-1 (IGF-I) in rodents. The purpose of the study was to assess its safety, pharmacokinetics, and effects on circulating levels of IGF-I and IGF-binding protein-3 (IGFBP-3) after repeated dosing. Forty healthy volunteers ingested Resveratrol at 0.5, 1.0, 2.5, or 5.0 g daily for 29 days. Levels of Resveratrol and its metabolites were measured by high performance liquid chromatography-UV in plasma obtained before and up to 24 hours after a dose between days 21 and 28. IGF-I and IGFBP-3 were measured by ELISA in plasma taken predosing and on day 29. Resveratrol was safe, but the 2.5 and 5 g doses caused mild to moderate gastrointestinal symptoms. Resveratrol-3-O-sulfate, Resveratrol-4′-O-glucuronide, and Resveratrol-3-O-glucuronide were major plasma metabolites. Maximal plasma levels and areas under the concentration versus time curve for the metabolites dramatically exceeded those for Resveratrol, in the case of areas under the concentration versus time curve, by up to 20.3-fold. Compared with predosing values, the ingestion of Resveratrol caused a decrease in circulating IGF-I and IGFBP-3 (P

  • clinical pharmacology of Resveratrol and its metabolites in colorectal cancer patients
    Cancer Research, 2010
    Co-Authors: Ketan R Patel, Victoria A Brown, Donald J L Jones, Robert G Britton, David Hemingway, A S Miller, Kevin West, Tristan D Booth, Marjorie Perloff, James A Crowell
    Abstract:

    Resveratrol is a phytochemical with chemopreventive activity in preclinical rodent models of colorectal carcinogenesis. Antiproliferation is one of the many chemopreventive modes of action it has been shown to engage in. Concentrations of Resveratrol, which can be achieved in human tissues after p.o. administration, have not yet been defined. The purpose of this study was to measure concentrations of Resveratrol and its metabolites in the colorectal tissue of humans who ingested Resveratrol. Twenty patients with histologically confirmed colorectal cancer consumed eight daily doses of Resveratrol at 0.5 or 1.0 g before surgical resection. Resveratrol was found to be well tolerated. Normal and malignant biopsy tissue samples were obtained before dosing. Parent compound plus its metabolites Resveratrol-3-O-glucuronide, Resveratrol-4'-O-glucuronide, Resveratrol-3-O-sulfate, Resveratrol-4'-O-sulfate, Resveratrol sulfate glucuronide, and Resveratrol disulfate were identified by high-performance liquid chromatography (HPLC) with UV or mass spectrometric detection in colorectal resection tissue. Quantitation was achieved by HPLC/UV. Cell proliferation, as reflected by Ki-67 staining, was compared in preintervention and postintervention tissue samples. Resveratrol and Resveratrol-3-O-glucuronide were recovered from tissues at maximal mean concentrations of 674 and 86.0 nmol/g, respectively. Levels of Resveratrol and its metabolites were consistently higher in tissues originating in the right side of the colon compared with the left. Consumption of Resveratrol reduced tumor cell proliferation by 5% (P = 0.05). The results suggest that daily p.o. doses of Resveratrol at 0.5 or 1.0 g produce levels in the human gastrointestinal tract of an order of magnitude sufficient to elicit anticarcinogenic effects. Resveratrol merits further clinical evaluation as a potential colorectal cancer chemopreventive agent.

  • phase i dose escalation pharmacokinetic study in healthy volunteers of Resveratrol a potential cancer chemopreventive agent
    Cancer Epidemiology Biomarkers & Prevention, 2007
    Co-Authors: David J Boocock, Ketan R Patel, Tristan D Booth, Marjorie Perloff, James A Crowell, Guy Faust, Anna M Schinas, Victoria Brown, Murray P Ducharme, Andreas J Gescher
    Abstract:

    The red grape constituent Resveratrol possesses cancer chemopreventive properties in rodents. The hypothesis was tested that, in healthy humans, p.o. administration of Resveratrol is safe and results in measurable plasma levels of Resveratrol. A phase I study of oral Resveratrol (single doses of 0.5, 1, 2.5, or 5 g) was conducted in 10 healthy volunteers per dose level. Resveratrol and its metabolites were identified in plasma and urine by high-performance liquid chromatography-tandem mass spectrometry and quantitated by high-performance liquid chromatography-UV. Consumption of Resveratrol did not cause serious adverse events. Resveratrol and six metabolites were recovered from plasma and urine. Peak plasma levels of Resveratrol at the highest dose were 539 ± 384 ng/mL (2.4 μmol/L, mean ± SD; n = 10), which occurred 1.5 h post-dose. Peak levels of two monoglucuronides and Resveratrol-3-sulfate were 3- to 8-fold higher. The area under the plasma concentration curve (AUC) values for Resveratrol-3-sulfate and Resveratrol monoglucuronides were up to 23 times greater than those of Resveratrol. Urinary excretion of Resveratrol and its metabolites was rapid, with 77% of all urinary agent-derived species excreted within 4 h after the lowest dose. Cancer chemopreventive effects of Resveratrol in cells in vitro require levels of at least 5 μmol/L. The results presented here intimate that consumption of high-dose Resveratrol might be insufficient to elicit systemic levels commensurate with cancer chemopreventive efficacy. However, the high systemic levels of Resveratrol conjugate metabolites suggest that their cancer chemopreventive properties warrant investigation. (Cancer Epidemiol Biomarkers Prev 2007;16(6):1246–52)