High absorption but very low bioavailability of oral resveratrol in humans

Drug Metabolism and Disposition

Volumn 32, Issue 12, 2004, Pages 1377-1382

  Walle, Thomas ^a   Hsieh, Faye ^c   DeLegge, Mark H ^b   Oatis Jr , John E ^a   Walle, U Kristina ^a  

^a MEDICAL UNIVERSITY OF SOUTH CAROLINA   (United States)

^b MEDICAL UNIVERSITY OF SOUTH CAROLINA   (United States)

^c AMGEN INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CYTOCHROME P450 1A1; GLUCURONIC ACID; POLYPHENOL; RESVERATROL; SULFATE;

ADULT; APOPTOSIS; ARTICLE; CARDIOVASCULAR DISEASE; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG METABOLISM; EPITHELIUM CELL; FEMALE; HUMAN; HUMAN EXPERIMENT; HYDROGENATION; INGESTION; INTESTINE FLORA; LIQUID CHROMATOGRAPHY; MALE; MASS SPECTROMETRY; NORMAL HUMAN; PLASMA HALF LIFE; PRIORITY JOURNAL;

ADMINISTRATION, ORAL; ADULT; ANTINEOPLASTIC AGENTS, PHYTOGENIC; BIOLOGICAL AVAILABILITY; BIOTRANSFORMATION; CHROMATOGRAPHY, HIGH PRESSURE LIQUID; FECES; FEMALE; HALF-LIFE; HUMANS; INJECTIONS, INTRAVENOUS; INTESTINAL ABSORPTION; MALE; MASS SPECTROMETRY; STILBENES; SULFATES;

EID: 9444296057     PISSN: 00909556     EISSN: None     Source Type: Journal    
DOI: 10.1124/dmd.104.000885     Document Type: Article

References (22)

1. Banerjee S, Bueso-Ramos C, and Aggarwal BB (2002) Suppression of 7,12-dimethylbenz(a)anthracene-induced mammary carcinogenesis in rats by resveratrol: role of nuclear factor-κB, cyclooxygenase 2, and matrix metalloprotease 9. Cancer Res 62:4945-4954.
2. Bhat KP and Pezzuto JM (2002) Cancer preventive activity of resveratrol. Ann NY Acad Sci 957:210-229.
3. Falany CN, Krasnykh V, and Falany JL (1995) Bacterial expression and characterization of a cDNA for human liver estrogen sulfotransferase. J Steroid Biochem Mol Biol 52:529-539.
4. Galijatovic A, Otake Y, Walle UK, and Walle T (1999) Extensive metabolism of the flavonoid chrysin by human Caco-2 and Hep G2 cells. Xenobiotica 29:1241-1256.
5. Ganguly TC, Krasnykh V, and Falany CN (1995) Bacterial expression and kinetic characterization of the human monoamine-sulfating form of phenol sulfotransferase. Drug Metab Dispos 23:945-950.
6. Gescher AJ and Steward WP (2003) Relationship between mechanisms, bioavailability, and preclinical chemopreventive efficacy of resveratrol: a conundrum. Cancer Epidemiol Biomark Prev 12:953-957.
7. Goldberg DM, Yan J, and Soleas GJ (2003) Absorption of three wine-related polyphenols in three different matrices by healthy subjects. Clin Biochem 36:79-87.
8. Jang M, Cai L, Udeani GO, Slowing KV, Thomas CF, Beecher CWW, Fong HHS, Farnsworth NR, Kinghorn AD, Mehta RG, et al. (1997) Cancer chemopreventive activity of resveratrol, a natural product derived from grapes. Science (Wash DC) 275:218-220.
9. Kageura T, Matsuda H, Morikawa T, Toguchida I, Harima S, Oda M, and Yoshikawa M (2001) Inhibitors from rhubarb on lipopolysaccharide-induced nitric oxide production in macrophages: structural requirements of stilbenes for the activity. Bioorg Med Chem 9:1887-1893.
10. Kaldas MI, Walle UK, and Walle T (2003) Resveratrol transport and metabolism by human intestinal Caco-2 cells. J Pham Pharmacol 55:307-312.
11. Li ZG, Hong T, Shimada Y, Komoto I, Kawabe A, Ding Y, Kaganoi J, Hashimoto Y, and Imamura M (2002) Suppression of N-nitrosomethylbetizylamine (NMBA)-induced esophageal tumorigenesis in F344 rats by resveratrol. Carcinogenesis 23:1531-1536.
12. Meng X, Maliakal P, Lu H, Lee M-J, and Yang CS (2004) Urinary and plasma levels of resveratrol and quercetin in humans, mice and rats after ingestion of pure compounds and grape juice. J Agric Food Chem 52:935-942.
13. Parkinson A (2001). Chapter 6. Biotransformation of xenobiotics, in Casarett and Doull's Toxicology: The Basic Science of Poisons (Klaassen CD ed), pp 133-224, McGraw-Hill, New York.
14. Pervaiz S (2003) Resveratrol: from grapevines to mammalian biology. FASEB J 17:1975-1985.
15. Santner SJ, Feil PD, and Santen RJ (1984) In situ estrogen production via estrone sulphatase pathway in breast tumours: relative importance versus aromatase pathway. J Clin Endocrinol Metab 59:29-33.
16. Scarlatti F, Sala G, Somenzi G, Signorelli P, Sacchi N, and Ghidoni R (2003) Resveratrol induces growth inhibition and apoptosis in metastatic breast cancer cells via de novo ceramide signaling. FASEB J 17:2339-2341.
17. Stivala LA, Savio M, Carafoli F, Perucca P, Bianchi L, Maga G, Forti L, Pagnoni UM, Albini A, Prosperi E, and Vannini V (2001) Specific structural determinants are responsible for the antioxidant activity and the cell cycle effects of resveratrol. J Biol Chem 276:22586-22594.
18. Tessitore L, Davit A, Sarotto I, and Caderni G (2000) Resveratrol depresses the growth of colorectal aberrant crypt foci by affecting box and p21CIP expression. Carcinogenesis 21:1619-1622.
19. Varin L, Barren D, and Ibrahim RK (1987) Enzymatic assay for flavonoid sulfotransferase. Anal Biochem 161:176-180.
20. Walle T (2004) Absorption and metabolism of flavonoids. Free Radic Biol Med 36:829-837.
21. Walle UK, Galijatovic A, and Walle T (1999) Transport of the flavonoid chrysin and its conjugated metabolites by the human intestinal cell line Caco-2. Biochem Pharmacol 58:431-438.
22. Yu C, Shin YG, Chow A, Li Y, Kosmeder JW, Lee YS, Hirschelman WH, Pezzuto JM, Mehta RG, and van Breemen RB (2002) Human, rat and mouse metabolism of resveratrol. Pham Res 19:1907-1914.