HIGH ABSORPTION BUT VERY LOW BIOAVAILABILITY OF ORAL RESVERATROL IN HUMANS

By T. Walle, Faye Hsieh, M. DeLegge, J. Oatis, U. Walle. Drug Metabolism And Disposition, 2004

1,829 citations recorded by the source corpus.

Subfields: Geriatrics and Gerontology, Pathology and Forensic Medicine, Pharmacology

View Paper: https://www.semanticscholar.org/paper/4e08fde1e692fea18fca522a90c9c3334ea23522

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In Geriatrics and Gerontology

1. T. Walle
2. Joseph A. Baur

In Pathology and Forensic Medicine

1. T. Walle
2. Jianbo Xiao

In Pharmacology

1. T. Walle
2. I. Kapetanovic

Citations in the corpus

• Phase I Dose Escalation Pharmacokinetic Study in Healthy Volunteers of Resveratrol, a Potential Cancer Chemopreventive Agent (2007, background): “This interpretation is congruent with results obtained in rats after oral resveratrol (35) and in human volunteers who received a low oral dose (25 mg) of (14)C-labeled resveratrol (28).”
• Resveratrol: a review of preclinical studies for human cancer prevention. (2007, background): “In humans, following its absorption, it is readily metabolized in the liver by phase-2 drug-metabolizing enzymes to water-soluble trans-resveratrol-3-O-glucuronide and trans-resveratrol-3-O-sulfate, accounting for its predominant urine excretion (Walle et al., 2004).”
• Dietary (Poly)phenolics in Human Health: Structures, Bioavailability, and Evidence of Protective Effects Against Chronic Diseases (2013, positive): “It is of note that feeding studies with [2-(14)C]resveratrol have provided evidence that metabolites of the stilbene do undergo enterohepatic recycling in humans (480).”
• The therapeutic potential of resveratrol: a review of clinical trials (2017, background): “This poor bioavailability can be attributed to the rapid conjugation of transresveratrol to glucuronic acid and sulfates, producing glucuronides and sulfate conjugates which accumulate in plasma and urine.(25) Many trials are in progress to determine the appropriate oral dosage given the rapid metab”
• Repeat Dose Study of the Cancer Chemopreventive Agent Resveratrol in Healthy Volunteers: Safety, Pharmacokinetics and Effect on the Insulin-like Growth Factor Axis (2010, positive): “Reports on trials of resveratrol in humans after single (8,9) or multiple daily doses of up to 600 mg per day administered over two or three days (10,11) suggest that it is safe under the tested conditions.”
• Bioavailability of resveratrol (2011, methodology): “LC/radioactivity tracings with fraction collection of a 0–12-h urine extract after a 25-mg oral dose of (14)C-resveratrol.(4) M1–M5 are glucuronides and sulfate conjugates.”
• Bioactivity of dietary polyphenols: The role of metabolites (2020, background): “In urine, metabolites accounted for 22–44% of the ingested dose, with 11–31% sulfate conjugates and 9–16% glucuronides (Walle et al. 2004; Tome-Carneiro et al. 2013).”
• Pharmacokinetics, oral bioavailability, and metabolic profile of resveratrol and its dimethylether analog, pterostilbene, in rats (2010, background): “It has been proposed that these conjugates could serve as storage pools for the parent drugs, as has been demonstrated for estrone sulfate [40,41].”
• Anti-Inflammatory Action and Mechanisms of Resveratrol (2021, background): “Rapid absorption, poor bioavailability, and low aqueous solubility are some of the crucial limitations and challenges of the in vivo use of resveratrol [12,13].”
• Antioxidant Phytochemicals for the Prevention and Treatment of Chronic Diseases (2015, background): “around 400–500 ng/mL, indicating a very low oral bioavailability of free resveratrol [140,142,143].”
• Potential Adverse Effects of Resveratrol: A Literature Review (2020, background): “For instance, it was found that 70% of a 25-mg oral dose of RE was absorbed in the intestines, but only trace amounts of RE were found in blood plasma [66].”