Cited by 578Coffee research and impactsPhytochemicals and Antioxidant ActivitiesGenomics, phytochemicals, and oxidative stress

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Chlorogenic Acids from Green Coffee Extract are Highly Bioavailable in Humans

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Farah, Adriana, Monteiro, Mariana, Donangelo, Carmen M., Lafay, Sophie·2008·The Journal of Nutrition

DOI 10.3945/jn.108.095554

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Abstract

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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No effect of the farming system (organic/conventional) on the bioavailability of apple (Malus domestica Bork., cultivar Golden Delicious) polyphenols in healthy men: a comparative study
Stracke, B. A., Rüfer, C. E., Bub, A., Seifert, S., Weibel, F., Kunz, C., & Watzl, B. (2009) · European Journal of Nutrition · doi:10.1007/s00394-009-0088-9 · Cited by 50
“After intake of green coffee extract, tmax of coumaric acid in plasma of the volunteers was 2.5 ± 1.8 h [ 30 ].”
MethodInfluential
Green coffee bean extract and 5-O-caffeoylquinic acid regulate fat metabolism in Caenorhabditis elegans
Farias‐Pereira, R., Oshiro, J., Kim, K., & Park, Y. (2018) · Journal of Functional Foods · doi:10.1016/j.jff.2018.07.049 · Cited by 50
First identification of dimethoxycinnamic acids in human plasma after coffee intake by liquid chromatography–mass spectrometry
Nagy, K., Redeuil, K. M., Williamson, G., Rezzi, S., Dionisi, F., Longet, K., Destaillats, F., & Renouf, M. (2010) · Journal of Chromatography A · doi:10.1016/j.chroma.2010.11.076 · Cited by 49
Chromatographic Methods for Coffee Analysis: A Review
Yashin, A. Y., Yashin, Y. I., Xia, X., & Nemzer, B. V. (2017) · Journal of Food Research · doi:10.5539/jfr.v6n4p60 · Cited by 49
The bioaccessible phenolic profile and antioxidant potential of Hypericum perfoliatum L. after simulated human digestion
Celep, E., İnan, Y., Akyüz, S., & Yeşilada, E. (2017) · Industrial Crops and Products · doi:10.1016/j.indcrop.2017.09.032 · Cited by 49
Priming agents of plant defence stimulate the accumulation of mono- and di-acylated quinic acids in cultured tobacco cells
Mhlongo, M. I., Piater, L. A., Steenkamp, P. A., Madala, N. E., & Dubery, I. A. (2014) · Physiological and Molecular Plant Pathology · doi:10.1016/j.pmpp.2014.09.002 · Cited by 49
“This bioactivity is not only limited to plant defence but includes biomedical properties [21,22].”
Pharmacokinetics and Pharmacodynamics of Key Components of a Standardized Centella asiatica Product in Cognitively Impaired Older Adults: A Phase 1, Double-Blind, Randomized Clinical Trial
Wright, K. M., Bollen, M., David, J., Speers, A. B., Brandes, M. S., Gray, N. E., Magaña, A. A., McClure, C., Stevens, J. F., Maier, C. S., et al. (2022) · Antioxidants · doi:10.3390/antiox11020215 · Cited by 51
“In humans administered coffee, intact mono- and di-CQAs were reported to be found in high levels in plasma [82,83].”
Background
Quantification of phenolic acids and their methylates, glucuronides, sulfates and lactones metabolites in human plasma by LC–MS/MS after oral ingestion of soluble coffee
Marmet, C., Actis‐Goretta, L., Renouf, M., & Giuffrida, F. (2013) · Journal of Pharmaceutical and Biomedical Analysis · doi:10.1016/j.jpba.2013.10.009 · Cited by 48
Effects of Chlorogenic Acid and Bovine Serum Albumin on the Oxidative Stability of Low Density Lipoproteins in Vitro
Gordon, M. H., & Wishart, K. (2010) · Journal of Agricultural and Food Chemistry · doi:10.1021/jf100106e · Cited by 48
Coffee phytochemicals and post-harvest handling—A complex and delicate balance
Munyendo, L., Njoroge, D., Owaga, E., & Mugendi, B. (2021) · Journal of Food Composition and Analysis · doi:10.1016/j.jfca.2021.103995 · Cited by 57
Proanthocyanidin: Chemistry and Biology: From Phenolic Compounds to Proanthocyanidins
Zuiter, A. S. (2014) · Elsevier eBooks · doi:10.1016/b978-0-12-409547-2.11046-7 · Cited by 52
Ameliorative effect of Eucommia ulmoides Oliv. leaves extract (ELE) on insulin resistance and abnormal perivascular innervation in fructose-drinking rats
Jin, X. K., Amitani, K., Zamami, Y., Takatori, S., Hobara, N., Kawamura, N., Hirata, T., Wada, A., Kitamura, Y., & Kawasaki, H. (2010) · Journal of Ethnopharmacology · doi:10.1016/j.jep.2010.02.019 · Cited by 48
Determination of antibacterial activity of green coffee bean extract on periodontogenic bacteria like Porphyromonas gingivalis, Prevotella intermedia, Fusobacterium nucleatum and Aggregatibacter actinomycetemcomitans: An in vitrostudy
Bharath, N., Sowmya, N., & Mehta, D. S. (2015) · Contemporary Clinical Dentistry · doi:10.4103/0976-237x.156036 · Cited by 47
“In addition, green coffee beans have been found to have antibacterial effects against pathogenic microorganisms.[7] Green coffee bean extract is a natural supplement whose primary ingredients [Table 3] help people be well and healthy.”
BackgroundInfluential
Comparative metabolism study on chlorogenic acid, cryptochlorogenic acid and neochlorogenic acid using UHPLC-Q-TOF MS coupled with network pharmacology
LI, J., WANG, S.-P., WANG, Y.-Q., SHI, L., ZHANG, Z.-K., DONG, F., LI, H.-R., ZHANG, J.-Y., & MAN, Y.-Q. (2021) · Chinese Journal of Natural Medicines · doi:10.1016/s1875-5364(21)60023-7 · Cited by 47
Neuromodulation and neuroprotective effects of chlorogenic acids in excitatory synapses of mouse hippocampal slices
Fernandes, M. Y. S. D., Dobrachinski, F., Silva, H. B. L., Lopes, J. P., Gonçalves, F. Q., Soares, F. A. A., Porciúncula, L. O., de Andrade, G. M., Cunha, R. A., & Tomé, Â. R. (2021) · Scientific Reports · doi:10.1038/s41598-021-89964-0 · Cited by 48
Guayusa ( Ilex guayusa L.) new tea: phenolic and carotenoid composition and antioxidant capacity
García‐Ruiz, A., Baenas, N., Benítez-González, A. M., Stinco, C. M., Meléndez‐Martínez, A. J., Moreno, D. A., & Ruales, J. (2017) · Journal of the Science of Food and Agriculture · doi:10.1002/jsfa.8255 · Cited by 46
“A cc ep te d A rti cl e type 2 diabetes and Alzheimer's disease.(27) Chlorogenic acids are major constituents of plants, such as coffee beans(27), yerba mate(23) and other Ilex spp.”
Background
Increased ROS Scavenging and Antioxidant Efficiency of Chlorogenic Acid Compound Delivered via a Chitosan Nanoparticulate System for Efficient In Vitro Visualization and Accumulation in Human Renal Adenocarcinoma Cells
Rajan, R. K., Hussein, M. Z., Fakurazi, S., Yusoff, K., & Masarudin, M. J. (2019) · International Journal of Molecular Sciences · doi:10.3390/ijms20194667 · Cited by 45
“Hence to confront these limitations, administration of a high dosage was used [1] but in which led to observable events of severe side effects such as DNA damage [32], cardiovascular complications [33], inflammatory and oxidative stress injuries [34], disruption in natural oxidant and antioxidant balance mechanisms [3…”
BackgroundResultInfluential
Effects of dietary supplementation with chlorogenic acid on growth performance, antioxidant capacity, and hepatic inflammation in broiler chickens subjected to diquat-induced oxidative stress
Zha, P., Wei, L., Liu, W., Chen, Y., & Zhou, Y. (2023) · Poultry Science · doi:10.1016/j.psj.2023.102479 · Cited by 45
“Although its absorption rate varies greatly among different animal species, CGA can be absorbed in the stomach and small intestine and then rapidly enter into liver via portal vein system in mammals, and therefore, liver plays an important role in the transport and metabolism of absorbed CGA in animal body (Olthof et…”
Background
Assessment of potential bioavailability of major phenolic compounds in Lavandula stoechas L. ssp. stoechas
Celep, E., Akyüz, S., İnan, Y., & Yeşilada, E. (2018) · Industrial Crops and Products · doi:10.1016/j.indcrop.2018.03.041 · Cited by 45
Pharmacokinetics and brain penetration study of chlorogenic acid in rats
Kumar, G., Paliwal, P., Mukherjee, S., Patnaik, N., Krishnamurthy, S., & Patnaik, R. (2018) · Xenobiotica · doi:10.1080/00498254.2018.1445882 · Cited by 45
“5–12% CGA but only 1% caffeine (Farah et al., 2008; George et al., 2008).”
In vitro study of genotoxic and cytotoxic activities of methanol extracts of Artemisia vulgaris L. and Artemisia alba Turra
Jakovljević, M. R., Grujičić, D., Vukajlović, J. T., Marković, A., Milutinović, M. G., Stanković, M. S., Vuković, N. L., Vukić, M., & Milošević-Djordjević, O. (2020) · South African Journal of Botany · doi:10.1016/j.sajb.2020.04.016 · Cited by 45
A Systematic Review of the European Rapid Alert System for Food and Feed: Tendencies in Illegal Food Supplements for Weight Loss
Koncz, D., Tóth, B., Roza, O., & Csupor, D. (2021) · Frontiers in Pharmacology · doi:10.3389/fphar.2020.611361 · Cited by 46
“are good sources of chlorogenic acids (13) that are not present in roasted coffee because of their thermolability (Farah et al., 2008).”
Background
Influence of green extraction techniques on green coffee: Nutraceutical compositions, antioxidant potential and in vitro bio-accessibility of phenolics
Pimpley, V. A., & Murthy, P. S. (2021) · Food Bioscience · doi:10.1016/j.fbio.2021.101284 · Cited by 45
Chlorogenic Acid and Coffee Prevent Hypoxia-Induced Retinal Degeneration
Jang, H., Ahn, H. R., Jo, H., Kim, K., Lee, E. H., Lee, K. W., Jung, S. H., & Lee, C. Y. (2013) · Journal of Agricultural and Food Chemistry · doi:10.1021/jf404285v · Cited by 45
Potential Oral Health Care Agent from Coffee against Virulence Factor of Periodontitis
Tsou, S., Hu, S., Yang, J., Yan, M., & Lin, Y. (2019) · Nutrients · doi:10.3390/nu11092235 · Cited by 45
“A major source of chlorogenic acid can be found in green coffee extract, which is highly bioavailable to humans [41].”
Background
Phenolic Acids as Antidepressant Agents
Cordeiro, M. L. D. S., Aquino-Martins, V. G. D. Q., da Silva, A. P., Rocha, H. A. O., Soares-Rachetti, V. D. P., & Scortecci, K. C. (2022) · Nutrients · doi:10.3390/nu14204309 · Cited by 50
“It is mostly consumed in coffee because of the high concentrations [75,76].”
Background
Effects of chlorogenic acid on neutrophil locomotion functions in response to inflammatory stimulus
Hebeda, C. B., Bolonheis, S. M., Nakasato, A., Belinati, K. D., Souza, P. D. C., Gouvea, D. R., Lopes, N. P., & Farsky, S. H. P. (2011) · Journal of Ethnopharmacology · doi:10.1016/j.jep.2011.02.033 · Cited by 43
“CGA is daily consumed inhigh concentrations, because it is component of a huge diversity of food and beverages present in human diet (Farah et al., 2008; Kempf et al., 2010; Olthof et al., 2001) and it is an important component of medicinal plants broadly used as anti-inflammatory agents (Keles et al.”
Background
Pilot-Scale Culture of Hypericum Perforatum L. Adventitious Roots in Airlift Bioreactors for the Production of Bioactive Compounds
Cui, X.-H., Murthy, H. N., & Paek, K. (2014) · Applied Biochemistry and Biotechnology · doi:10.1007/s12010-014-1123-8 · Cited by 43
Chemo-protective activity and characterization of phenolic extracts from Corema album
León‐González, A. J., Mateos, R., Ramos, S., Martín, M. Á., Sarriá, B., Martı́n-Cordero, C., López‐Lázaro, M., Bravo, L., & Goya, L. (2012) · Food Research International · doi:10.1016/j.foodres.2012.09.016 · Cited by 43
Determination of Total Chlorogenic Acids in Commercial Green Coffee Extracts
Vinson, J. A., Chen, X., & Garver, D. D. (2019) · Journal of Medicinal Food · doi:10.1089/jmf.2018.0039 · Cited by 43
Molecular mechanism of action of chlorogenic acid on erythrocyte and lipid membranes
Bonarska‐Kujawa, D., Cyboran-Mikołajczyk, S., & Kleszczyńska, H. (2015) · Molecular Membrane Biology · doi:10.3109/09687688.2015.1031833 · Cited by 42
“8 mmol/l (Farah et al., 2008), which falls well within the used range (2.”
BackgroundInfluential
Molecular conformational analysis, vibrational spectra, NBO analysis and first hyperpolarizability of (2E)-3-phenylprop-2-enoic anhydride based on density functional theory calculations
Mary, Y. S., Raju, K., Panicker, C. Y., Al‐Saadi, A. A., Thiemann, T., & Alsenoy, C. V. (2014) · Spectrochimica Acta Part A Molecular and Biomolecular Spectroscopy · doi:10.1016/j.saa.2014.02.194 · Cited by 42
Excretion of Avenanthramides, Phenolic Acids and their Major Metabolites Following Intake of Oat Bran
Schär, M. Y., Corona, G., Soycan, G., Dine, C., Kristek, A., Alsharif, S. N., Behrends, V., Lovegrove, A., Shewry, P. R., & Spencer, J. P. E. (2017) · Molecular Nutrition & Food Research · doi:10.1002/mnfr.201700499 · Cited by 42
“small intestine, a larger proportion is absorbed following release by fermentation by the colonic microbiota with previous studies suggesting that it originated partly from the metabolism of avenanthramides and hydroxycinnamic acids [25, 32, 34, 35].”
Background
The increase in human plasma antioxidant capacity after acute coffee intake is not associated with endogenous non-enzymatic antioxidant components
Moura‐Nunes, N., Perrone, D., Farah, A., & Donangelo, C. M. (2009) · International Journal of Food Sciences and Nutrition · doi:10.1080/09637480903158893 · Cited by 42
“We chose 90 min based on previous results both on the plasma antioxidant capacity response and the pharmacokinetics of coffee antioxidant compounds after coffee intake (Natella et al. 2002; Nardini et al. 2002; Monteiro et al. 2007; Farah et al. 2008).”
MethodSelf-citation
Chlorogenic Acid Targeting of the AKT PH Domain Activates AKT/GSK3β/FOXO1 Signaling and Improves Glucose Metabolism
Gao, J., He, X., Ma, Y., Zhao, X., Hou, X., Hao, E., Deng, J., & Bai, G. (2018) · Nutrients · doi:10.3390/nu10101366 · Cited by 42
“Furthermore, CGA is highly absorbed and metabolized in humans, and it retains bioactivity across the intestinal barrier [9,10].”
Study on the Postprandial Glucose Responses to a Chlorogenic Acid-Rich Extract of Decaffeinated Green Coffee Beans in Rats and Healthy Human Subjects
Iwai, K., Narita, Y., Fukunaga, T., Nakagiri, O., Kamiya, T., Ikeguchi, M., & KIKUCHI, Y. (2012) · Food Science and Technology Research · doi:10.3136/fstr.18.849 · Cited by 41
“%) of ingested cinnamic acid moieties, including metabolites, were recovered in plasma with peak levels being observed 0.5 to 8 h after the consumption of 2 capsules of green coffee extract (Svetol; 400 mg) (Farah et al., 2008).”
MethodInfluential
The Janus face of chlorogenic acid on vascular reactivity: A study on rat isolated vessels
Tom, E. N. L., Girard, C., & Demougeot, C. (2016) · Phytomedicine · doi:10.1016/j.phymed.2016.06.012 · Cited by 40
Antioxidant Generation during Coffee Roasting: A Comparison and Interpretation from Three Complementary Assays
Opitz, S., Smrke, S., Goodman, B., Keller, M., Schenker, S., & Yeretzian, C. (2014) · Foods · doi:10.3390/foods3040586 · Cited by 39
“In unroasted coffee beans, the chlorogenic acids (CGAs) are a major source of the total antioxidant capacity [14,15] with a high level of bioavailability [16], although as esters of primarily caffeic and quinic acids, they belong to a different sub-family of phenols from those in teas.”
Background
Synthetic Cinnamides and Cinnamates: Antimicrobial Activity, Mechanism of Action, and In Silico Study
de Morais, M. C., Lima, E. D. O., Pérez‐Castillo, Y., & de Sousa, D. P. (2023) · Molecules · doi:10.3390/molecules28041918 · Cited by 43
Development and Validation of an in vitro Experimental GastroIntestinal Dialysis Model with Colon Phase to Study the Availability and Colonic Metabolisation of Polyphenolic Compounds
Breynaert, A., Bosscher, D., Kahnt, A., Claeys, M., Cos, P., Pieters, L. A. C., & Hermans, N. (2015) · Planta Medica · doi:10.1055/s-0035-1546154 · Cited by 39
The Impact of the Roast Levels of Coffee Extracts on their Potential Anticancer Activities
Mojica, B. E., Fong, L. E., Biju, D., Muharram, A., Davis, I. M., Vela, K. O., Rios, D., Osorio‐Camacena, E., Kaur, B., Rojas, S. M., et al. (2018) · Journal of Food Science · doi:10.1111/1750-3841.14102 · Cited by 41
Microencapsulation of antioxidant phenolic compounds from green coffee
Desai, N. M., Haware, D. J., Basavaraj, K., & Murthy, P. S. (2019) · Preparative Biochemistry & Biotechnology · doi:10.1080/10826068.2019.1575858 · Cited by 39
“1mg GAE g 1 and corroborates the reported values by others.([15]) The decaffeination was successfully achieved using a GRAS ethyl lactate and caffeine accounted to 0.”
Method

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
ORCID: Farah, Adriana
Monteiro, Mariana
Donangelo, Carmen M.
Venue: The Journal of Nutrition
Publisher: Elsevier BV
Published: 2008-12
Volume: 138
Issue: 12
Pages: 2309-2315
ISSN: 0022-3166 (ISSN-L)
DOI: 10.3945/jn.108.095554
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: www.elsevier.com/tdm/userlicense/1.0/ (tdm)
www.elsevier.com/open-access/userlicense/1.0/ (vor, 5181 d)
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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Chlorogenic Acids from Green Coffee Extract are Highly Bioavailable in Humans

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