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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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“Some polyphenols are quite well absorbed and a significant proportion is excreted in the urine; examples include gallic acid, the isoflavones genistein and daidzein, and the (citrus) flavanones hesperetin and naringenin (Manach et al., 2005).”
InfluentialNeuroprotective effects of digested polyphenols from wild blackberry species
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“The available data suggests that among flavonoids, isoflavones have the highest bioavailability, with absorption between 33 and 100%, followed by flavonols (12–41%), and flavanones (11–16%) [122].”
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Effect of flavonoids on rat splenocytes, a structure–activity relationship study
López-Posadas, R., Ballester, I., Abadía‐Molina, A. C., Suárez, M. D., Zarzuelo, A., Martínez‐Augustin, O., & de Medina, F. S. (2008) · Biochemical Pharmacology · doi:10.1016/j.bcp.2008.06.001 · Cited by 84
Heinz, S. A., Henson, D. A., Nieman, D. C., Austin, M. D., & Jin, F. (2010) · British Journal Of Nutrition · doi:10.1017/s000711451000156x · Cited by 84
“Quercetin is found in fruits and vegetables in a water-soluble form in which the quercetin molecule is conjugated to a sugar((2)).”
BackgroundInfluentialAnticoagulant effect of polyphenols-rich extracts from black chokeberry and grape seeds
Bijak, M., Bobrowski, M., Borowiecka, M., Podsędek, A., Golański, J., & Nowak, P. (2011) · Fitoterapia · doi:10.1016/j.fitote.2011.04.017 · Cited by 84
Ras, R. T., Zock, P. L., Zebregs, Y. E. M. P., Johnston, N. R., Webb, D. J., & Draijer, R. (2013) · British Journal Of Nutrition · doi:10.1017/s000711451300161x · Cited by 84
“phenolic compounds, which should theoretically increase bioavailability((26)).”
BackgroundZamora‐Ros, R., Rabassa, M., Cherubini, A., Urpí-Sardà, M., Bandinelli, S., Ferrucci, L., & Andrés‐Lacueva, C. (2013) · Journal of Nutrition · doi:10.3945/jn.113.177121 · Cited by 85
“The health effects of polyphenols depend on their quantity consumed and bioavailability, which varies greatly from one molecule to another (15) and among individuals (16).”
BackgroundHo, G. T. T., Kase, E. T., Wangensteen, H., & Barsett, H. (2017) · Journal of Agricultural and Food Chemistry · doi:10.1021/acs.jafc.6b05582 · Cited by 84
Role of fruit juice in achieving the 5-a-day recommendation for fruit and vegetable intake
Benton, D., & Young, H. A. (2019) · Nutrition Reviews · doi:10.1093/nutrit/nuz031 · Cited by 90
“nins have been found to vary 1–4 hours; flavonols, 1– 13 hours; flavanones, 1–3 hours; flavanols, 1–3 hours; and isoflavones, 4–8 hours.(84) Generalizations are difficult given the thousands of phenolic compounds that exist; there is, however, an impression that to maintain a high plasma concentration of polyphenols t…”
BackgroundRay, S. K., & Mukherjee, S. (2021) · Frontiers in Nutrition · doi:10.3389/fnut.2021.634944 · Cited by 98
“A minor amount of dietary polyphenols (5–10% of total intake) can be easily absorbed using deconjugation reactions such as deglycosylation in the small intestine (26).”
BackgroundAlmatroudi, A., Allemailem, K. S., Alwanian, W. M., Alharbi, B. F., Alrumaihi, F., Khan, A. A., Almatroodi, S. A., & Rahmani, A. H. (2023) · International Journal of Molecular Sciences · doi:10.3390/ijms24108630 · Cited by 90
Gallic Acid Intake Induces Alterations to Systems Metabolism in Rats
Shi, X., Xiao, C., Wang, Y., & Tang, H. (2012) · Journal of Proteome Research · doi:10.1021/pr301041k · Cited by 82
Adsorptive recovery of phenolic compounds from apple juice
Kammerer, D. R., Saleh, Z. S., Carle, R., & Stanley, R. A. (2006) · European Food Research and Technology · doi:10.1007/s00217-006-0346-5 · Cited by 83
New C-Deoxyhexosyl Flavones and Antioxidant Properties of Passiflora edulis Leaf Extract
Ferreres, F., Sousa, C., Valentão, P., Andrade, P. B., Seabra, R. M., & Gil‐Izquierdo, Á. (2007) · Journal of Agricultural and Food Chemistry · doi:10.1021/jf072119y · Cited by 83
Protective effects of genistein in homocysteine-induced endothelial cell inflammatory injury
Han, S., Wu, H. B. K., Li, W., & Gao, P. (2015) · Molecular and Cellular Biochemistry · doi:10.1007/s11010-015-2335-0 · Cited by 84
“Moreover, GEN antagonizes estrogen- and androgen-mediated signaling pathways in the processes of carcinogenesis [35, 36].”
BackgroundProcyanidins protect Caco-2 cells from bile acid- and oxidant-induced damage
Erlejman, A. G., Fraga, C. G., & Oteiza, P. I. (2006) · Free Radical Biology and Medicine · doi:10.1016/j.freeradbiomed.2006.07.002 · Cited by 84
Fisetin, morin and myricetin attenuate CD36 expression and oxLDL uptake in U937-derived macrophages
Lian, T.-W., Wang, L., Lo, Y., Huang, I., & Wu, M. (2008) · Biochimica et Biophysica Acta (BBA) - Molecular and Cell Biology of Lipids · doi:10.1016/j.bbalip.2008.06.009 · Cited by 82
Morrison, M. C., van der Heijden, R. A., Heeringa, P., Kaijzel, E. L., Verschuren, L., Blomhoff, R., Kooistra, T., & Kleemann, R. (2014) · Atherosclerosis · doi:10.1016/j.atherosclerosis.2013.12.027 · Cited by 87
The molecular basis of nutritional intervention in multiple sclerosis: A narrative review
Riccio, P. (2011) · Complementary Therapies in Medicine · doi:10.1016/j.ctim.2011.06.006 · Cited by 86
Effect of grape and other berries on cardiovascular health
Wightman, J. D., & Heuberger, R. (2014) · Journal of the Science of Food and Agriculture · doi:10.1002/jsfa.6890 · Cited by 84
Barbosa, P. O., Pala, D., Silva, C. T., de Souza, M. O., do Amaral, J. F., Vieira, R. A. L., Folly, G. A. D. F., Volp, A. C. P., & de Freitas, R. N. (2015) · Nutrition · doi:10.1016/j.nut.2015.12.030 · Cited by 83
“Since anthocyanins are the least bioavailable polyphenols [60], studies of the antioxidant effect of açai in humans are necessary before to include them in the antioxidant food list.”
BackgroundParohan, M., Anjom-Shoae, J., Nasiri, M., Khodadost, M., Khatibi, S. R., & Sadeghi, O. (2019) · European Journal of Nutrition · doi:10.1007/s00394-019-01922-9 · Cited by 81
Cao, X., Liu, M., Tuo, J., Shen, D., & Chan, C. (2010) · Experimental Eye Research · doi:10.1016/j.exer.2010.03.016 · Cited by 83
“When compared with humans, for whom the daily intake of flavonols has been estimated at only 20e35 mg/day (Manach et al., 2005), of which quercetin represents 70% of the total (Hertog et al.”
Quercetin Attenuates TNF-Induced Inflammation in Hepatic Cells by Inhibiting the NF-κB Pathway
Granado‐Serrano, A. B., Martín, M. Á., Bravo, L., Goya, L., & Ramos, S. (2012) · Nutrition and Cancer · doi:10.1080/01635581.2012.661513 · Cited by 82
“5 μM after 28 days of supplementation with >1 g/day of quercetin (41).”
BackgroundRowlands, D. J., Chapple, S. J., Siow, R. C. M., & Mann, G. E. (2011) · Hypertension · doi:10.1161/hypertensionaha.110.162198 · Cited by 82
Fujita, A., Sarkar, D., Wu, S., Kennelly, E. J., Shetty, K., & Genovese, M. I. (2015) · Food Research International · doi:10.1016/j.foodres.2015.07.009 · Cited by 83
Oral delivery system enhanced the bioavailability of stilbenes: Resveratrol and pterostilbene
Peng, R., Lin, G., Ting, Y., & Hu, J. (2018) · BioFactors · doi:10.1002/biof.1405 · Cited by 85
“However, studies had also shown the plasma concentration of such compounds rarely reached 1lM at normal dietary level [28,39].”
BackgroundChemopreventive Potential of Flavonoids in Oral Squamous Cell Carcinoma in Human Studies
Iriti, M., & Varoni, E. M. (2013) · Nutrients · doi:10.3390/nu5072564 · Cited by 82
Anthocyanin Metabolites Are Abundant and Persistent in Human Urine
Kalt, W., Liu, Y., McDonald, J. E., Vinqvist, M. R., & Fillmore, S. A. E. (2014) · Journal of Agricultural and Food Chemistry · doi:10.1021/jf500107j · Cited by 81
Postharvest fruit quality and antioxidants of nectarine fruit as influenced by chlorogenic acid
Xi, Y., Fan, X., Zhao, H., Li, X., Cao, J., & Jiang, W. (2016) · LWT · doi:10.1016/j.lwt.2016.10.004 · Cited by 81
Kardum, N., Takić, M. M., Šavikin, K., Zec, M. M., Zdunić, G. M., Spasić, S., & Konić‐Ristić, A. (2014) · Journal of Functional Foods · doi:10.1016/j.jff.2014.04.019 · Cited by 82
Murota, K., & Terao, J. (2005) · FEBS Letters · doi:10.1016/j.febslet.2005.08.060 · Cited by 81
“Not only the function but also the bioavailability of flavonoids have been widely investigated in cell culture [6,7], animal models [8,9] and in human volunteers [10–12].”
BackgroundThe pro‐apoptotic effect of quercetin in cancer cell lines requires ERβ‐dependent signals
Bulzomi, P., Galluzzo, P., Bolli, A., Leone, S., Acconcia, F., & Marino, M. (2011) · Journal of Cellular Physiology · doi:10.1002/jcp.22917 · Cited by 81
“Thus, the E2 protective effect on colon cancer should be mediated by specific signal transduction pathways activated by ERb (Acconcia et al., 2005; Galluzzo et al., 2007).”
BackgroundIdentification and quantification of flavonol glycosides in cultivated blueberry cultivars
Vrhovšek, U., Masuero, D., Palmieri, L., & Mattivi, F. (2011) · Journal of Food Composition and Analysis · doi:10.1016/j.jfca.2011.04.015 · Cited by 81
Schwanke, R. C., Marcon, R., Meotti, F. C., Bento, A. F., Dutra, R. C., Pizzolatti, M. G., & Calixto, J. Β. (2013) · Molecular Nutrition & Food Research · doi:10.1002/mnfr.201300134 · Cited by 81
Modulation of Aromatase by Phytoestrogens
Lephart, E. D. (2015) · Enzyme Research · doi:10.1155/2015/594656 · Cited by 86
“Additionally, phytoestrogens denote a wide variety of compounds, which are divided into several classes, that is, hydroxybenzoic acids, hydroxycinnamic acids, anthocyanins, proanthocyanidins, flavonols, flavones, flavanols, flavanones, isoflavones, stilbenes, and lignans [25].”
BackgroundInfluential
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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