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Chlorogenic Acids from Green Coffee Extract are Highly Bioavailable in Humans
Open accessAbstract
Chlorogenic acids (CGA) are cinnamic acid derivatives with biological effects mostly related to their antioxidant and antiinflammatory activities. Caffeoylquinic acids (CQA) and dicaffeoylquinic acids (diCQA) are the main CGA found in nature. Because green coffee is a major source of CGA, it has been used for production of nutraceuticals. However, data on the bioavailability of CGA from green coffee in humans are inexistent. The present study evaluated the pharmacokinetic profile and apparent bioavailability of CGA in plasma and urine of 10 healthy adults for 8 h after the consumption of a decaffeinated green coffee extract containing 170 mg of CGA. Three CQA, 3 diCQA, and caffeic, ferulic, isoferulic, and p-coumaric acids were identified in plasma by HPLC-Diode Array Detector-MS after treatment. Over 30% (33.1 +/- 23.1%) of the ingested cinnamic acid moieties were recovered in plasma, including metabolites, with peak levels from 0.5 to 8 h after treatment. CGA and metabolites identified in urine after treatment were 4-CQA, 5-CQA, and sinapic, p-hydroxybenzoic, gallic, vanillic, dihydrocaffeic, caffeic, ferulic, isoferulic, and p-coumaric acids, totaling 5.5 +/- 10.6% urinary recovery of the ingested cinnamic and quinic acid moiteties. This study shows that the major CGA compounds present in green coffee are highly absorbed and metabolized in humans.
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“Coffee is also a source of CGA (Table 1), a hydroxycinnamic acid with health-promoting properties such as antioxidant, antibacterial, and anti-inflammatory activities, among others [212].”
From Effects of Coffee and Its Components on the Gastrointestinal Tract and the Brain–Gut Axis (2020) · cites this paper as [212]
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Antiulcerogenic activity of chlorogenic acid in different models of gastric ulcer
Shimoyama, A. T., Santin, J. R., Machado, I. D., Silva, A. M. D. O. E., de Melo, I. L. P., Mancini-Filho, J., & Farsky, S. H. P. (2012) · Naunyn-Schmiedeberg s Archives of Pharmacology · doi:10.1007/s00210-012-0807-2 · Cited by 104
“Although CGA is ingested by the oral route and absorbed by gastric and intestinal cells (Farah et al. 2008; Stalmach et al. 2010) and acts as a cytoprotective agent in several disease models (Krakauer 2002; Dos Santos et al.”
BackgroundComparison of antioxidant activity between green and roasted coffee beans using molecular methods
Priftis, A., Stagos, D., Konstantinopoulos, K., Tsitsimpikou, C., Spandidos, D. A., Tsatsakis, A. M., Tzatzarakis, M. N., & Kouretas, D. (2015) · Molecular Medicine Reports · doi:10.3892/mmr.2015.4377 · Cited by 102
“Several studies have been performed to investigate the quantity, as well as the antioxidant and other disease-related properties, of CGA (19,21-24).”
Selenium increases chlorogenic acid, chlorophyll and carotenoids of Lycium chinense leaves
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“The enriched bread exhibited a significantly higher antioxidant activity (compared to the control) probably due to a significantly increased content of caffeine and phenolics acid – antioxidants with well–documented antioxidant capacity (Dziki et al., 2015; Farah et al., 2008; Li Kwok Cheong et al., 2014).”
BackgroundZhang, Y.-J., Huang, X., Wang, Y., Xie, Y., Qiu, X.-J., Ren, P., Gao, L., Zhou, H., Zhang, H.-Y., & Qiao, M.-Q. (2011) · Brain Research Bulletin · doi:10.1016/j.brainresbull.2011.07.002 · Cited by 99
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“Studies on bioavailability of CQA and diCQA from green coffee extract have shown that these compounds are absorbed and metabolized in humans [47]; they quantified CQA, diCQAs, and phenolics in plasma for up to 8 h after ingestion of 451 mmol total chlorogenic acid.”
BackgroundPrecision medicine for suicidality: from universality to subtypes and personalization
Niculescu, A. B., Le-Niculescu, H., Levey, D. F., Phalen, P. L., Dainton‐Howard, H., Roseberry, K., Niculescu, E. M., Niezer, J., Williams, A., Graham, D. L., et al. (2017) · Molecular Psychiatry · doi:10.1038/mp.2017.128 · Cited by 95
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“Some researchers have reported high amounts of intact 3-, 4-, and 5-CQA [129,147], while others have reported their absence [130,148].”
BackgroundHouttuynia cordata Targets the Beginning Stage of Herpes Simplex Virus Infection
Hung, P.-Y., Ho, B., Lee, S.-Y., Chang, S., Kao, C., Lee, S., & Lee, C. (2015) · PLoS ONE · doi:10.1371/journal.pone.0115475 · Cited by 90
“The phenolic parts including chlorogenic acid have antipyretic and antibiotic activity [32, 33].”
BackgroundGround green coffee beans as a functional food supplement – Preliminary study
Dziki, D., Gawlik‐Dziki, U., Pecio, Ł., Różyło, R., Świeca, M., Krzykowski, A., & Rudy, S. (2015) · LWT · doi:10.1016/j.lwt.2015.03.076 · Cited by 90
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Interaction of chlorogenic acids and quinides from coffee with human serum albumin
Sinisi, V., Forzato, C., Cefarin, N., Navarini, L., & Berti, F. (2014) · Food Chemistry · doi:10.1016/j.foodchem.2014.07.080 · Cited by 89
Hydroxycinnamic acids on gut microbiota and health
Leonard, W., Zhang, P., Ying, D., & Fang, Z. (2020) · Comprehensive Reviews in Food Science and Food Safety · doi:10.1111/1541-4337.12663 · Cited by 94
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“5 h to 96 h, because this concentration was described as the physiological concentration (13,14).”
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Mullen, W., Nemzer, B. V., Stalmach, A., Ali, S., & Combet, E. (2013) · Journal of Agricultural and Food Chemistry · doi:10.1021/jf4003126 · Cited by 93
Biotransformation of polyphenols in a dynamic multistage gastrointestinal model
Ekbatan, S. S., Sleno, L., Sabally, K., Khairallah, J., Azadi, B., Rodes, L., Prakash, S., Donnelly, D. J., & Kubow, S. J. (2016) · Food Chemistry · doi:10.1016/j.foodchem.2016.02.140 · Cited by 86
The effect of artichoke on lipid profile: A review of possible mechanisms of action
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Chlorogenic acid–phospholipid complex improve protection against UVA induced oxidative stress
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“A study [37] evaluating the pharmacokinetic profile and bioavailability of CHL in plasma and urine of 10 healthy participants showed a great deal of inter-individual variation in CHL absorption, metabolism and kinetics with uptake values ranged from 7.”
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“The methanolic and aqueous extracts of the leaves have the same compounds; such compounds have been previously described for mate leaves (Filip et al., 2000; Heck et al., 2008; Marques & Farah, 2009). However, besides the phenolic acids mentioned above, syringic, ferulic, and p-coumaric acids were also detected in mat…”
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Henry-Vitrac, C., Ibarra, A., Roller, M., Mérillon, J., & Vitrac, X. (2010) · Journal of Agricultural and Food Chemistry · doi:10.1021/jf9044827 · Cited by 81
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Impact of coffee components on inflammatory markers: A review
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Burgos‐Morón, E., Calderón‐Montaño, J. M., Orta, M. L., Pastor, N., Pérez‐Guerrero, C., Austin, C. A., Mateos, S., & López‐Lázaro, M. (2012) · Journal of Agricultural and Food Chemistry · doi:10.1021/jf300999e · Cited by 78
Metadata
- Authors
- Farah, A., Monteiro, M., Donangelo, C. M., & Lafay, S.
- Affiliations
- Universidade Federal do Rio de Janeiro (BR)
- Naturex (France) (FR)
- Corresponding author
- Farah, Adriana
- Venue
- The Journal of Nutrition
- Publisher
- Elsevier BV
- Published
- 2008-12
- Volume
- 138
- Issue
- 12
- Pages
- 2309-2315
- ISSN
- 0022-3166 (ISSN-L)
- OpenAlex
- W2127688626
- Cited by
- 578
- References
- 50
- Citations by year
- 2026: 18 · 2025: 16 · 2024: 20 · 2023: 33 · 2022: 29 · 2021: 40 · 2020: 43 · 2019: 42 · 2018: 49 · 2017: 52 · 2016: 48 · 2015: 39 · 2014: 35 · 2013: 28 · 2012: 32
- FWCI
- 12.42
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Licence
- Locations
- Journal of Nutrition (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Health Sciences › Medicine › Pharmacology (medical) › Coffee research and impacts
- Health Sciences › Medicine › Biochemistry (medical) › Phytochemicals and Antioxidant Activities
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Genomics, phytochemicals, and oxidative stress
- Keywords
- chlorogenic acid, green coffee bean extract, bioavailability, pharmacokinetics, caffeoylquinic acids, dicaffeoylquinic acids, cinnamic acid derivatives, urinary excretion, plasma absorption, metabolites, nutraceuticals, decaffeinated coffee
- MeSH terms
- Adult, Biological Availability, Caffeic Acids, Caffeine, Chlorogenic Acid, Cinnamates, Coffee, Coumaric Acids, Female, Humans, Male, Middle Aged, Propionates, Quinic Acid, Young Adult
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