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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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“Alternatively, the absorption of native quercetin is poor, and may not reach the liver in a concentration that will inhibit SULT in vivo [66].”
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“Nevertheless, the bioavailability of ACNs is low as compared with other BB polyphenols (Manach et al., 2005; McGhie & Walton, 2007) but these low levels of ACNs can be bioavailable and well retained in tissues (Kalt et al., 2008).”
BackgroundNatural antioxidants as stabilizers for polymers
Kirschweng, B., Tátraaljai, D., Földes, E., & Pukánszky, B. (2017) · Polymer Degradation and Stability · doi:10.1016/j.polymdegradstab.2017.07.012 · Cited by 239
“A limiting factor of medical applications is the poor bioavailability of flavonoids [84,85].”
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Nielsen, I. L. F., & Williamson, G. (2007) · Nutrition and Cancer · doi:10.1080/01635580701267677 · Cited by 229
“The bioavailability of isoflavones compared with other flavonoids has been reviewed (6).”
BackgroundPhytochemicals in Cancer Prevention and Therapy: Truth or Dare?
Russo, M., Spagnuolo, C., Tedesco, I., & Russo, G. L. (2010) · Toxins · doi:10.3390/toxins2040517 · Cited by 225
“The very low concentrations of free aglycones found in vivo are due to the scarce bioavailability and biotransformation of these molecules discussed in excellent reviews [7,8].”
BackgroundAntioxidant Properties of Hydroxycinnamic Acids: A Review of Structure- Activity Relationships
Razzaghi‐Asl, N., Garrido, J., Khazraei, H., Borges, F., & Firuzi, O. (2013) · Current Medicinal Chemistry · doi:10.2174/09298673113209990141 · Cited by 231
“They have been categorized as structural and functional constituents of plant cell walls and also as bioactive ingredi- ents of the diet [40, 41].”
BackgroundIron-binding properties of plant phenolics and cranberry's bio-effects
Guo, M., Perez, C., Wei, Y., Rapoza, E., Su, G. M., Bou‐Abdallah, F., & Chasteen, N. D. (2007) · Dalton Transactions · doi:10.1039/b705136k · Cited by 227
Hormesis and synergy: pathways and mechanisms of quercetin in cancer prevention and management
Vargas, A. J., & Burd, R. (2010) · Nutrition Reviews · doi:10.1111/j.1753-4887.2010.00301.x · Cited by 229
Protective effects of flavonoids against microbes and toxins: The cases of hesperidin and hesperetin
Iranshahi, M., Rezaee, R., Parhiz, H., Roohbakhsh, A., & Soltani, F. (2015) · Life Sciences · doi:10.1016/j.lfs.2015.07.014 · Cited by 222
“The antibacterial activity and bioavailability of flavonoids are affected by various parameters, such as molecular conformation, hydrophobicity, solubility, presence or absence of sugar moiety and the type of sugar in the chemical backbone (Manach et al., 2005).”
BackgroundA review of the health care potential of bioactive compounds
Hooper, L., & Cassidy, A. (2006) · Journal of the Science of Food and Agriculture · doi:10.1002/jsfa.2599 · Cited by 221
Jennings, A., Welch, A. A., Spector, T. D., MacGregor, A. J., & Cassidy, A. (2013) · Journal of Nutrition · doi:10.3945/jn.113.184358 · Cited by 220
“, procyanidins]; isoflavones; and anthocyanins and other polymeric flavonoids) can alter both bioavailability and bioactivity (14,15), which highlights the importance of investigating each subclass individually.”
BackgroundA Review of the Health Benefits of Cherries
Kelley, D. S., Adkins, Y. C., & Laugero, K. D. (2018) · Nutrients · doi:10.3390/nu10030368 · Cited by 223
“Both anthocyanins and hydoxycinnamates are believed to be rapidly absorbed in humans reaching maximum plasma concentrations in less than 2 h and are quickly eliminated [31,32].”
BackgroundDendrimers in combination with natural products and analogues as anti-cancer agents
Mignani, S. M., Rodrigues, J., Tomás, H., Zabłocka, M., Shi, X., Caminade, A., & Majoral, J. (2017) · Chemical Society Reviews · doi:10.1039/c7cs00550d · Cited by 222
Eker, M. E., Aaby, K., Budić-Leto, I., Brnčić, S. R., El, S. N., Karakaya, S., Şimşek, Ş., Manach, C., Wiczkowski, W., & de Pascual‐Teresa, S. (2019) · Foods · doi:10.3390/foods9010002 · Cited by 230
“After consumption, a very low proportion (<2%) of the original anthocyanins are retrieved in the circulation (plasma/urine) [39].”
BackgroundAbsorption, metabolism and excretion of Choladi green tea flavan‐3‐ols by humans
Stalmach, A., Troufflard, S., Serafini, M., & Crozier, A. (2008) · Molecular Nutrition & Food Research · doi:10.1002/mnfr.200800169 · Cited by 218
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Apigenin and luteolin modulate microglial activation via inhibition of STAT1-induced CD40 expression
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Dietary Intake of Natural Antioxidants: Vitamins and Polyphenols
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Curcumin, Gut Microbiota, and Neuroprotection
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“A number of the measured polyphenolic compounds have a rapid metabolism and elimination [54].”
BackgroundAbsorption, metabolism, and excretion of green tea flavan‐3‐ols in humans with an ileostomy
Stalmach, A., Mullen, W., Steiling, H., Williamson, G., Lean, M. E. J., & Crozier, A. (2009) · Molecular Nutrition & Food Research · doi:10.1002/mnfr.200900194 · Cited by 216
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miRNA as molecular target of polyphenols underlying their biological effects
Milenković, D., Jude, B., & Morand, C. (2013) · Free Radical Biology and Medicine · doi:10.1016/j.freeradbiomed.2013.05.046 · Cited by 223
Polyphenols in Fruits and Vegetables and Its Effect on Human Health
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Gorelik, S., Ligumsky, M., Kohen, R., & Kanner, J. (2007) · The FASEB Journal · doi:10.1096/fj.07-9041com · Cited by 213
“It is well accepted that diets rich in polyphenols have health benefits (4, 6–9), but the absorption of polyphenols in humans is limited and the mechanisms of action of these molecules in the human body are not fully understood (1, 8).”
BackgroundMemariani, Z., Abbas, S. Q., Hassan, S. S. U., Ahmadi, A., & Chabra, A. (2020) · Pharmacological Research · doi:10.1016/j.phrs.2020.105264 · Cited by 219
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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