QUICK SEARCH:   [advanced] Author: Keyword(s): Year:  Vol:  Page:

This Article Full Text Full Text (PDF) Purchase Article View Shopping Cart Alert me when this article is cited Alert me if a correction is posted Services Similar articles in this journal Similar articles in PubMed Alert me to new issues of the journal Download to citation manager Citing Articles Citing Articles via HighWire Citing Articles via Google Scholar Google Scholar Articles by Kay, C. D. Articles by Holub, B. J. Search for Related Content PubMed PubMed Citation Articles by Kay, C. D. Articles by Holub, B. J.

---

Human Nutrition and Metabolism

Anthocyanins Exist in the Circulation Primarily as Metabolites in Adult Men¹

Colin D. Kay^*,,2, Giuseppe (Joe) Mazza and Bruce J. Holub^*

^* Department of Human Biology and Nutritional Sciences, University of Guelph, ON, Canada and Agriculture and Agri-Food Canada, Pacific Agri-Food Research Centre, Summerland, BC, Canada

²To whom correspondence should be addressed. E-mail: cdk14{at}psu.edu.

Anthocyanins are reported to have many "health promoting" properties; however, despite numerous reports of their bioactivities, their absorption and metabolism in humans are poorly understood. The objective of this research was to detail the pharmacokinetic parameters of anthocyanins after the administration of a 721-mg oral dose of cyanidin 3-glycosides from chokeberry extract to human subjects. Solid-phase extraction, preparative-HPLC, preparative-TLC, HPLC-diode array detection, HPLC-MS, and NMR were utilized to isolate, identity, and quantify anthocyanins in 0- to 7-h (0, 1, 2, 3, 4, 5, 6, 7 h) serum and 0- to 24-h urine samples (total individual urine voids over 24 h). The cumulative concentration of total anthocyanins (parent and metabolites) detected in the serum (0–7 h) was 376.65 ± 16.20 (nmol · h)/L (area under the concentration time curve), reaching a maximum concentration (C_max = 96.08 ± 6.04 nmol/L) within 2.8 h. The parent anthocyanins represented only 32.0% [120.63 ± 2.85 (nmol · h)/L] of the total anthocyanins detected with 68.0% [256.02 ± 5.23 (nmol · h) identified as conjugated metabolites. Additionally, the total urinary excretion of anthocyanins over 24 h was 1071.54 ± 375.46 µg, reaching a maximal rate of excretion (R_max = 202.74 ± 85.06 µg/h) at 3.72 ± 0.83 h. Parallel to the serum data, only 32.5% (347.85 ± 60.61 µg) of the anthocyanins excreted in the urine (total 24 h) were the parent compounds with 67.5% (723.69 ± 92.59 µg) occurring as conjugated metabolites. The metabolites were identified as glucuronidated and methylated derivatives of the parent cyanidin 3-glycosides. The above results indicate that cyanidin 3-glycosides are rapidly absorbed and metabolized extensively following a moderate-to-high oral dose in humans.

KEY WORDS: • anthocyanins • cyanidin 3-glycosides • pharmacokinetics • metabolites

This article has been cited by other articles:

				P. Vitaglione, G. Donnarumma, A. Napolitano, F. Galvano, A. Gallo, L. Scalfi, and V. Fogliano Protocatechuic Acid Is the Major Human Metabolite of Cyanidin-Glucosides J. Nutr., September 1, 2007; 137(9): 2043 - 2048. [Abstract] [Full Text] [PDF]

				P. E. Milbury, B. Graf, J. M. Curran-Celentano, and J. B. Blumberg Bilberry (Vaccinium myrtillus) Anthocyanins Modulate Heme Oxygenase-1 and Glutathione S-Transferase-pi Expression in ARPE-19 Cells Invest. Ophthalmol. Vis. Sci., May 1, 2007; 48(5): 2343 - 2349. [Abstract] [Full Text] [PDF]

				J. W. Erdman Jr., D. Balentine, L. Arab, G. Beecher, J. T. Dwyer, J. Folts, J. Harnly, P. Hollman, C. L. Keen, G. Mazza, et al. Flavonoids and Heart Health: Proceedings of the ILSI North America Flavonoids Workshop, May 31-June 1, 2005, Washington, DC J. Nutr., March 1, 2007; 137(3): 718S - 737S. [Abstract] [Full Text] [PDF]