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Bioavailability and bioefficacy of polyphenols in humans. I. Review of 97 bioavailability studies
Open accessAbstract
Polyphenols are abundant micronutrients in our diet, and evidence for their role in the prevention of degenerative diseases is emerging. Bioavailability differs greatly from one polyphenol to another, so that the most abundant polyphenols in our diet are not necessarily those leading to the highest concentrations of active metabolites in target tissues. Mean values for the maximal plasma concentration, the time to reach the maximal plasma concentration, the area under the plasma concentration-time curve, the elimination half-life, and the relative urinary excretion were calculated for 18 major polyphenols. We used data from 97 studies that investigated the kinetics and extent of polyphenol absorption among adults, after ingestion of a single dose of polyphenol provided as pure compound, plant extract, or whole food/beverage. The metabolites present in blood, resulting from digestive and hepatic activity, usually differ from the native compounds. The nature of the known metabolites is described when data are available. The plasma concentrations of total metabolites ranged from 0 to 4 mumol/L with an intake of 50 mg aglycone equivalents, and the relative urinary excretion ranged from 0.3% to 43% of the ingested dose, depending on the polyphenol. Gallic acid and isoflavones are the most well-absorbed polyphenols, followed by catechins, flavanones, and quercetin glucosides, but with different kinetics. The least well-absorbed polyphenols are the proanthocyanidins, the galloylated tea catechins, and the anthocyanins. Data are still too limited for assessment of hydroxycinnamic acids and other polyphenols. These data may be useful for the design and interpretation of intervention studies investigating the health effects of polyphenols.
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“Some of the biomarkers listed in Table 1 have half-lives that do not exceed 24 h [polyphenols, alkylresorcinols, and amino acids (34,35)].”
From The food metabolome: a window over dietary exposure (2014) · cites this paper as [34]
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Flavanols and Anthocyanins in Cardiovascular Health: A Review of Current Evidence
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“Galloylated catechins are rapidly eliminated, probably not by degalloylation, which has been shown to be a minor process in humans, but rather by preferential excretion of these compounds in bile [27,28].”
BackgroundResultInfluentialPolyphenolic phytochemicals – just antioxidants or much more?
Stevenson, D. E., & Hurst, R. D. (2007) · Cellular and Molecular Life Sciences · doi:10.1007/s00018-007-7237-1 · Cited by 551
Quercetin Reduces Blood Pressure in Hypertensive Subjects1,
Edwards, R. L., Lyon, T., Litwin, S. E., Rabovsky, A. B., Symons, J. D., & Jalili, T. (2007) · Journal of Nutrition · doi:10.1093/jn/137.11.2405 · Cited by 551
Bioavailability of dietary flavonoids and phenolic compounds
Crozier, A., Rio, D. D., & Clifford, M. N. (2010) · Molecular Aspects of Medicine · doi:10.1016/j.mam.2010.09.007 · Cited by 568
Mechanisms of Neuroprotection by Quercetin: Counteracting Oxidative Stress and More
Costa, L. G., Garrick, J. M., Roqué, P. J., & Pellacani, C. (2016) · Oxidative Medicine and Cellular Longevity · doi:10.1155/2016/2986796 · Cited by 550
“The half-life of quercetin ranges between 11 and 28 h, suggesting the possibility of significantly increasing plasma concentration upon supplementation [8, 10].”
BackgroundBERMUDEZSOTO, M., Tomás-Barberán, F. A., & García‐Conesa, M. (2006) · Food Chemistry · doi:10.1016/j.foodchem.2006.06.025 · Cited by 564
Metabolic fate of polyphenols in the human superorganism
van Duynhoven, J., Vaughan, E. E., Jacobs, D. M., A. Kemperman, R., van Velzen, E. J. J., Gross, G., Roger, L. C., Possemiers, S., Smilde, A. K., Doré, J., et al. (2011) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1000098107 · Cited by 540
“Effects on food (89) and endogenous (90) metabolomes have typically been assessed by targeting a limited number of predefined (hypothesis-driven) metabolites.”
BackgroundAnthocyanins: from plant to health
de Pascual‐Teresa, S., & Sánchez-Ballesta, M. T. (2007) · Phytochemistry Reviews · doi:10.1007/s11101-007-9074-0 · Cited by 548
“As recently reviewed by Manach et al. (2005), existing literature in the field of anthocyanin bioavailability shows that this group of pigments is less well absorbed than other flavonoids.”
BackgroundNutrients and phytochemicals: from bioavailability to bioefficacy beyond antioxidants
Holst, B., & Williamson, G. (2008) · Current Opinion in Biotechnology · doi:10.1016/j.copbio.2008.03.003 · Cited by 536
“Thus, the estimated absorption of polyphenols when based on urinary data from healthy volunteers and from ileostomist studies (ileostomy involves bringing the ileum to the abdominal surface by surgical intervention; ileostomy patients are often enrolled into studies on small intestinal absorption and metabolism) is be…”
BackgroundFerreira, J., Luthria, D. L., Sasaki, T., & Heyerick, A. (2010) · Molecules · doi:10.3390/molecules15053135 · Cited by 532
“Thus, we recommend the reading of two excellent reviews on bioavailability and bioefficacy of polyphenols in humans [152,153].”
MethodThe food metabolome: a window over dietary exposure
Scalbert, A., Brennan, L., Manach, C., Andres-Lacueva, C., Dragsted, L. O., Draper, J., Rappaport, S. M., van der Hooft, J. J., & Wishart, D. S. (2014) · The American Journal of Clinical Nutrition · doi:10.3945/ajcn.113.076133 · Cited by 519
Kulling, S. E., & Rawel, H. M. (2008) · Planta Medica · doi:10.1055/s-0028-1088306 · Cited by 517
“The data regarding the absorption and metabolism of the phenolic constituents (reviewed in [57], [58]) manifest their contribution to the health potential benefits of Aronia berries.”
BackgroundTena, N., Martı́n, J., & Asuero, A. G. (2020) · Antioxidants · doi:10.3390/antiox9050451 · Cited by 547
“The pattern followed by anthocyanins after oral dispensation is unique and different from other flavonoids [77].”
The role of metabolism (and the microbiome) in defining the clinical efficacy of dietary flavonoids
Cassidy, A., & Minihane, A. M. (2016) · American Journal of Clinical Nutrition · doi:10.3945/ajcn.116.136051 · Cited by 522
“Although currently completely unknown, because of the key role of LPH and b-glucosidases (see Absorption) in the initial hydrolysis of flavonoid glycosides, it is likely that variants in these loci may be important determinants of the bioavailability of the majority of flavonoid subclasses from the small intestine.”
BackgroundInfluentialTherapeutic potential of quercetin as a cardiovascular agent
Patel, R. V., Mistry, B. M., Shinde, S. K., Syed, R., Singh, V., & Shin, H. (2018) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2018.06.053 · Cited by 506
Chemical Composition of Mango (Mangifera indica L.) Fruit: Nutritional and Phytochemical Compounds
Celis, M. E. M., Yahia, E. M., Bedoya, R. A., Landázuri, P., Loango, N., Osma, J. A., Restrepo, B., & Ospina, J. C. G. (2019) · Frontiers in Plant Science · doi:10.3389/fpls.2019.01073 · Cited by 563
The pharmacokinetics of anthocyanins and their metabolites in humans
de Ferrars, R. M., Czank, C., Zhang, Q., Botting, N. P., Kroon, P. A., Cassidy, A., & Kay, C. D. (2014) · British Journal of Pharmacology · doi:10.1111/bph.12676 · Cited by 500
Habitual intake of flavonoid subclasses and incident hypertension in adults
Cassidy, A., O’Reilly, É. J., Kay, C. D., Sampson, L., FRANZ, M. M., Forman, J., Curhan, G. C., & Rimm, E. B. (2010) · American Journal of Clinical Nutrition · doi:10.3945/ajcn.110.006783 · Cited by 512
“The differences in the chemical structures of these subclasses alter both their biological efficacy and bioavailability (6, 7).”
BackgroundProtocatechuic Acid Is the Major Human Metabolite of Cyanidin-Glucosides3
Vitaglione, P., Donnarumma, G., Napolitano, A., Galvano, F., Gallo, A., Scalfi, L., & Fogliano, V. (2007) · Journal of Nutrition · doi:10.1093/jn/137.9.2043 · Cited by 504
Lako, J., Trenerry, V. C., Wahlqvist, M. L., Wattanapenpaiboon, N., Sotheeswaran, S., & Premier, R. R. (2006) · Food Chemistry · doi:10.1016/j.foodchem.2006.01.031 · Cited by 503
Zhao, L., Zhang, Q., Ma, W., Tian, F., Shen, H., & Zhou, M. (2017) · Food & Function · doi:10.1039/c7fo01383c · Cited by 501
Flavonols and Flavones as Potential anti‐Inflammatory, Antioxidant, and Antibacterial Compounds
Chagas, M. D. S. S., Behrens, M. D., Moragas-Tellis, C. J., Penedo, G. X. M., Silva, A. R., & Gonçalves-de-Albuquerque, C. F. (2022) · Oxidative Medicine and Cellular Longevity · doi:10.1155/2022/9966750 · Cited by 550
Flavonoid metabolism: the interaction of metabolites and gut microbiota
Murota, K., Nakamura, Y., & Uehara, M. (2018) · Bioscience Biotechnology and Biochemistry · doi:10.1080/09168451.2018.1444467 · Cited by 487
“The basic structure of flavonoids, meaning the structure of the aglycon form, and which type of sugar moiety is attached strongly affect their bioavailability [9].”
BackgroundLu, Z., Nie, G., Belton, P., Tang, H., & Zhao, B. (2005) · Neurochemistry International · doi:10.1016/j.neuint.2005.10.010 · Cited by 485
“The mammalian metabolism of gallic acid has been thoroughly studied (Haslam and Cai, 1994; Zong et al., 1999; Manach et al., 2005).”
BackgroundPolyphenols and their benefits: A review
Rasouli, H., Farzaei, M. H., & Khodarahmi, R. (2017) · International Journal of Food Properties · doi:10.1080/10942912.2017.1354017 · Cited by 490
Anthocyanins in Cardiovascular Disease
Wallace, T. C. (2011) · Advances in Nutrition · doi:10.3945/an.110.000042 · Cited by 490
Antioxidant Therapy: Current Status and Future Prospects
Firuzi, O., Miri, R., Tavakkoli, M., & Saso, L. (2011) · Current Medicinal Chemistry · doi:10.2174/092986711803414368 · Cited by 476
Metabolism of Anthocyanins by Human Gut Microflora and Their Influence on Gut Bacterial Growth
Hidalgo, M., Oruña-Concha, M. J., Kolida, S., Walton, G., Καλλιθράκα, Σ., Spencer, J. P. E., Gibson, G. R., & de Pascual‐Teresa, S. (2012) · Journal of Agricultural and Food Chemistry · doi:10.1021/jf3002153 · Cited by 464
El-Seedi, H., Elsaid, A. M. A., Khalifa, S., Göransson, U., Bohlin, L., Borg-Karlson, A., & Verpoorte, R. (2012) · Journal of Agricultural and Food Chemistry · doi:10.1021/jf301807g · Cited by 450
Metadata
- Authors
- Manach, C., Williamson, G., Morand, C., Scalbert, A., & Rémésy, C.
- Affiliations
- Institut National de Recherche pour l'Agriculture, l'Alimentation et l'Environnement (FR)
- Institut National de la Recherche Agronomique (FR)
- Corresponding author
- Manach, Claudine
- Venue
- The American Journal of Clinical Nutrition
- Publisher
- Elsevier BV
- Published
- 2005-01
- Volume
- 81
- Issue
- 1
- Pages
- 230S-242S
- ISSN
- 0002-9165 (ISSN-L)
- OpenAlex
- W2119331100
- Cited by
- 4,219
- References
- 162
- Citations by year
- 2026: 201 · 2025: 170 · 2024: 170 · 2023: 170 · 2022: 189 · 2021: 215 · 2020: 241 · 2019: 216 · 2018: 224 · 2017: 242 · 2016: 235 · 2015: 211 · 2014: 246 · 2013: 257 · 2012: 266
- FWCI
- 78.00
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Licence
- Locations
- American Journal of Clinical Nutrition (publishedVersion)
- PubMed (publishedVersion)
- HAL (submittedVersion)
- Topics
- Health Sciences › Medicine › Biochemistry (medical) › Phytochemicals and Antioxidant Activities
- Health Sciences › Medicine › Public Health, Environmental and Occupational Health › Nutritional Studies and Diet
- Health Sciences › Nursing › Nutrition and Dietetics › Pomegranate: compositions and health benefits
- Keywords
- polyphenols, bioavailability, bioefficacy, plasma concentration, urinary excretion, polyphenol metabolism, absorption kinetics, gallic acid, isoflavones, catechins, flavanones, quercetin glucosides, proanthocyanidins, anthocyanins, hydroxycinnamic acids, degenerative disease prevention
- MeSH terms
- Adult, Anthocyanins, Biological Availability, Female, Flavonoids, Food Analysis, Half-Life, Humans, Intestinal Absorption, Isoflavones, Male, Phenols, Area Under Curve, Polyphenols
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