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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Background
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Absorption and isomerization of caffeoylquinic acids from different foods using ileostomist volunteers
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“In another study [13], the administration of green coffee extract in capsules containing 121.”
Background
Associations of tea and coffee consumption with prostate cancer risk
Geybels, M. S., Neuhouser, M. L., & Stanford, J. L. (2013) · Cancer Causes & Control · doi:10.1007/s10552-013-0170-8 · Cited by 28
“While the biological properties of tea are mostly attributed to its polyphenol content [1, 2], coffee is a complex mixture of many potentially chemopreventive agents such as caffeine, cafestol, kahweol, polyphenols, chlorogenic acid, and caffeic acid [3–6].”
Background
Vitamins, Phytonutrients, and Minerals in Potato
Navarre, D. A., Shakya, R., & Hellmann, H. A. (2016) · Elsevier eBooks · doi:10.1016/b978-0-12-800002-1.00006-6 · Cited by 29
Antifungal Inhibitory Activities of Caffeic and Quinic Acid Derivatives
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Berry-Enriched Diet in Salt-Sensitive Hypertensive Rats: Metabolic Fate of (Poly)Phenols and the Role of Gut Microbiota
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“Simpler phenolic acids, like the ones found in our study, such as gallic acid can undergo phase I and II metabolism, which will generate compounds such as pyrogallol [68], hippuric acid [63], syringic acid [74], gallic acid sulphate, and 4-O-methylgallic acid sulphate [69], also present in urine and faeces of the rats…”
Background
Effects of Viburnum opulus fruit extracts on adipogenesis of 3T3-L1 cells and lipase activity
Podsędek, A., Zakłos‐Szyda, M., Kajszczak, D., & Sosnowska, D. (2020) · Journal of Functional Foods · doi:10.1016/j.jff.2020.104111 · Cited by 28
Interactions of Hydroxycinnamic Acids with Proteins and Their Technological and Nutritional Implications
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“The main volatile products of degradation of caffeic and chlorogenic acids are 4-vinylguaiacol, guaiacol, vanillin, 4-ethylcatechol, and catechol, which can occur, among others, in popcorn, tortillas, and coffee.(47) Moreover, bitter oligomers of 4vinylcatechol and sour N-phenylpropenyl derivatives of L-amino acids ar…”
Background
Inhibition of vascular endothelial growth factor-induced angiogenesis by chlorogenic acid via targeting the vascular endothelial growth factor receptor 2-mediated signaling pathway
Lin, S., Hu, J., Zhou, X., & Cheung, P. C. K. (2017) · Journal of Functional Foods · doi:10.1016/j.jff.2017.03.009 · Cited by 27
Coffee Extracts Suppress Tryptophan Breakdown in Mitogen-Stimulated Peripheral Blood Mononuclear Cells
Gostner, J. M., Schroecksnadel, S., Jenny, M., Klein, A., Ueberall, F., Schennach, H., & Fuchs, D. (2015) · Journal of the American College of Nutrition · doi:10.1080/07315724.2014.907756 · Cited by 27
“Determination of gallic acid was used as biomarker for tea- and coffee-derived polyphenol exposure [11], because gallic acid is one of the major urinary phenolic compounds excreted after green coffee consumption [12].”
BackgroundMethodInfluential
A review on the potential use of natural products in overweight and obesity
Li, X., Zhang, Y., Wang, S., Shi, C., Wang, S., Wang, X., & Lü, X. (2022) · Phytotherapy Research · doi:10.1002/ptr.7426 · Cited by 28
Bioaccessibility of coffee bean hydroxycinnamic acids during in vitro digestion influenced by the degree of roasting and activity of intestinal probiotic bacteria, and their activity in Caco-2 and HT29 cells
Grzelczyk, J., Szwajgier, D., Baranowska‐Wójcik, E., Budryn, G., Zakłos‐Szyda, M., & Sosnowska, B. (2022) · Food Chemistry · doi:10.1016/j.foodchem.2022.133328 · Cited by 27
Phenolic content, antioxidant and enzyme inhibitory capacity of two Trametes species
Zengin, G., Karanfil, A., Uren, M. C., Kocak, M. S., Sarıkürkçü, C., Güngör, H., Picot, C. M. N., & Mahomoodally, M. F. (2016) · RSC Advances · doi:10.1039/c6ra09991b · Cited by 27
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Structural and Biochemical Analyses Reveal that Chlorogenic Acid Inhibits the Shikimate Pathway
Neetu, N., Katiki, M., Dev, A., Gaur, S., Tomar, S., & Kumar, P. (2020) · Journal of Bacteriology · doi:10.1128/jb.00248-20 · Cited by 26
“of unique reflections 123,349 (6,118) 52,924 (4,762) Multiplicity 3.”
Chlorogenic acid protects human chondrocyte C28/I2 cells from oxidative stress-induced cell death through activation of autophagy
Zada, S., Pham, T. M., Hwang, J. S., Ahmed, M., Lai, T. H., Elashkar, O., Kim, J. H., Kim, D. H., & Kim, D. R. (2021) · Life Sciences · doi:10.1016/j.lfs.2021.119968 · Cited by 25
Coffee and tea consumption in relation to prostate cancer prognosis
Geybels, M. S., Neuhouser, M. L., Wright, J. L., Stott‐Miller, M., & Stanford, J. L. (2013) · Cancer Causes & Control · doi:10.1007/s10552-013-0270-5 · Cited by 26
“Coffee is also a major source of chlorogenic acid; several biologic activities have been associated with the consumption of these phenolic compounds, including anti-inflammatory and antioxidant effects and modulation of glucose metabolism [3, 30].”
Bioavailability and Bioactivities of Polyphenols Eco Extracts from Coffee Grounds after In Vitro Digestion
Vamanu, E., Gatea, F., & Pelinescu, D. R. (2020) · Foods · doi:10.3390/foods9091281 · Cited by 30
“The bioavailability of chlorogenic acid was different depending on the substrate, demonstrating that the presence of other components influenced the whole process and bioactivity [12].”
Background
Daily Intake of Chlorogenic Acids from Consumption of Maté (Ilex paraguariensis A.St.-Hil.) Traditional Beverages
Gebara, K. S., Gasparotto, A., Santiago, P. G., Cardoso, C. A. L., de Souza, L. M., Morand, C., Costa, T. A., & Cardozo, E. L. (2017) · Journal of Agricultural and Food Chemistry · doi:10.1021/acs.jafc.7b04093 · Cited by 25
Comparative chemical profiling and antimicrobial activity of two interchangeably used ‘Imphepho’ species (Helichrysum odoratissimum and Helichrysum petiolare)
Serabele, K., Chen, W., Tankeu, S., Combrinck, S., Veale, C. G. L., van Vuuren, S. F., Chaudhary, S. K., & Viljoen, A. M. (2020) · South African Journal of Botany · doi:10.1016/j.sajb.2020.09.023 · Cited by 25
A Systematic Review and Comprehensive Evaluation of Human Intervention Studies to Unravel the Bioavailability of Hydroxycinnamic Acids
Pede, G. D., Mena, P. R., Bresciani, L., Achour, M., Lamuela-Raventós, R. M., Estruch, R., Landberg, R., Kulling, S. E., Wishart, D. S., Rodriguez‐Mateos, A., et al. (2023) · Antioxidants and Redox Signaling · doi:10.1089/ars.2023.0254 · Cited by 24
Effects of chlorogenic acid, caffeine and coffee on components of the purinergic system of streptozotocin-induced diabetic rats
Stefanello, N., Schmatz, R., Pereira, L. B., Cardoso, A. M., Passamonti, S., Spanevello, R. M., Thomé, G. R., de Oliveira, G. M. T., Kist, L. W., Bogo, M. R., et al. (2016) · The Journal of Nutritional Biochemistry · doi:10.1016/j.jnutbio.2016.08.015 · Cited by 24
“tract and can be found in high levels in the plasma of subjects that ingested chlorogenic acid from green coffee[63], but whether chlorogenic acid could be found in the brain in high concentrations is still unknown.”
Background
Evaluation of anti-proliferative and cytotoxic effects of chlorogenic acid on breast cancer cell lines by real-time, label-free and high-throughput screening
Bender, O., & Atalay, A. (2018) · MARMARA PHARMACEUTCAL JOURNAL · doi:10.12991/mpj.2018.54 · Cited by 24
“Chlorogenic acid (CGA) is a polyphenolic compound and it is the major constituent of many natural products, such as the coffee beans [10-11].”
Background
Polyphenols
Cvejić, J., Krstonošić, M. A., Bursać, M., & Miljić, U. D. (2017) · Elsevier eBooks · doi:10.1016/b978-0-12-805257-0.00007-7 · Cited by 25
Comparison of phytochemical profiles, antioxidant and cellular antioxidant activities of seven cultivars ofAloe
Lai, Q., Wang, H., Guo, X., Abbasi, A. M., Wang, T., Li, T., Fu, X., Li, J., & Liu, R. H. (2016) · International Journal of Food Science & Technology · doi:10.1111/ijfs.13093 · Cited by 24
Bioavailability and Metabolism of Chlorogenic Acids from Coffee
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Self-citation
Growth of Leonurus sibiricus L. roots with over-expression of AtPAP1 transcriptional factor in closed bioreactor, production of bioactive phenolic compounds and evaluation of their biological activity
Sitarek, P., Kowalczyk, T., Picot, L., Michalska-Hejduk, D., Bijak, M., Białas, A. J., Wielanek, M., Śliwiński, T., & Skała, E. (2018) · Industrial Crops and Products · doi:10.1016/j.indcrop.2018.06.059 · Cited by 24
“These bioactive compounds are reported to be potent antioxidant, anti-inflammatory, anticancer compounds and can be used in nutraceuticals intended for weight loss (Farah et al., 2008).”
Background
Green coffee ameliorates components of diet-induced metabolic syndrome in rats
Bhandarkar, N. S., Mouatt, P., Brown, L., & Panchal, S. K. (2019) · Journal of Functional Foods · doi:10.1016/j.jff.2019.04.003 · Cited by 24
Phytochemical Profiling, Antioxidant and Cognitive-Enhancing Effect of Helichrysum italicum ssp. italicum (Roth) G. Don (Asteraceae)
Gevrenova, R., Kostadinova, I., Stefanova, A., Balabanova, V., Zengin, G., Zheleva‐Dimitrova, D., & Momekov, G. (2023) · Plants · doi:10.3390/plants12152755 · Cited by 23
Viburnum opulus L. fruit phenolic compounds protect against FFA-induced steatosis of HepG2 cells via AMPK pathway
Pietrzyk, N., Zakłos‐Szyda, M., Koziołkiewicz, M., & Podsędek, A. (2021) · Journal of Functional Foods · doi:10.1016/j.jff.2021.104437 · Cited by 23
In VitroAntioxidant Activities of Polyphenols Purified from Four Plant Species Used in Rice Beer Preparation in Assam India
Das, A. J., Das, G., Miyaji, T., & Deka, S. C. (2015) · International Journal of Food Properties · doi:10.1080/10942912.2015.1038835 · Cited by 23
“Chlorogenic acid has been associated with reduction in risk of cardiovascular disease, type 2 diabetes, Alzheimer’s disease, antibacterial and anti-inflammatory activities.([38]) Quinic acid was present and it possesses DNA repair, immune, and antiinflammatory enhancing properties and versatile chiral starting materia…”
Background
Current trends in small molecule discovery targeting key cellular signaling events towards the combined management of diabetes and obesity
Sangeetha, K. N., Sujatha, S., Muthusamy, V. S., Anand, S., Shilpa, K., kumari, P. J., Sarathkumar, B., Gopal, T., & Lakshmi, B. S. (2017) · Bioinformation · doi:10.6026/97320630013394 · Cited by 23
Helianthus annuus Seed Extract Affects Weight and Body Composition of Healthy Obese Adults during 12 Weeks of Consumption: A Randomized, Double-Blind, Placebo-Controlled Pilot Study
Leverrier, A., Daguet, D., Calame, W., Dhoye, P., & Kodimule, S. P. (2019) · Nutrients · doi:10.3390/nu11051080 · Cited by 24
“They are produced by many plants, and green coffee is one of the major sources found in nature (5–12 g/100 g) [10].”
Background
Aortic Relaxant Activity of Crataegus gracilior Phipps and Identification of Some of Its Chemical Constituents
Hernández-Pérez, A., Bah, M., Ibarra‐Alvarado, C., Rivero-Cruz, J. F., Rojas‐Molina, A., Rojas-Molina, J., & Cabrera-Luna, J. A. (2014) · Molecules · doi:10.3390/molecules191220962 · Cited by 22
“The mechanisms by which some flavonoids and triterpenes already found in Crataegus exert their effects on cardiovascular system have been elucidated [15–17].”
Background
Simultaneous determination of chlorogenic acids in green coffee bean extracts with effective relative response factors
Shan, Y., Jin, X., Cheng, Y., & Yan, W. (2016) · International Journal of Food Properties · doi:10.1080/10942912.2016.1230746 · Cited by 22
“CHA are cinnamic acid derivatives with biological effects mostly related to their antioxidant([17]) and anti-inflammatory activities.([18])”
Background
Efficiency of Lactiplantibacillus plantarum JT-PN39 and Paenibacillus motobuensis JT-A29 for Fermented Coffee Applications and Fermented Coffee Characteristics
Ngamnok, T., Nimlamool, W., Amador‐Noguez, D., Palaga, T., & Meerak, J. (2023) · Foods · doi:10.3390/foods12152894 · Cited by 21
Synthesis of p-coumaroylquinic acids and analysis of their interconversion
Ortiz, A. L. G., Berti, F., Navarini, L., Monteiro, Â. F. A., Resmini, M., & Forzato, C. (2017) · Tetrahedron Asymmetry · doi:10.1016/j.tetasy.2017.01.015 · Cited by 21
A perspective on phenolic compounds, their potential health benefits, and international regulations: The revised Brazilian normative on food supplements
de Camargo, A. C., & Lima, R. D. S. (2019) · Journal of Food Bioactives · doi:10.31665/jfb.2019.7193 · Cited by 21
“Coffee is the primary source of chlorogenic acid in nature, with green coffee beans presenting around 5-12 g CGA/100 g on a dry weight basis (DW) while a cup of 200 mL of standard brewed coffee has 0.07- 0.35 g (Farah et al., 2008).”
BackgroundInfluential
Antioxidant efficacy and in silico toxicity prediction of free and spray-dried extracts of green Arabica and Robusta coffee fruits and their application in edible oil
Faria, W. C. S., de Oliveira, M. G., da Conceição, E. C., da Silva, V. B., Veggi, N., Converti, A., de Barros, W. M., da Silva, M. F., & Bragagnolo, N. (2020) · Food Hydrocolloids · doi:10.1016/j.foodhyd.2020.106004 · Cited by 23
Chemical composition and anti-radical properties of coffee cherry cultivated in Mediterranean climate
Stefano, V. A. D., Buzzanca, C., Ruvutuso, F., Scuderi, D., Palazzolo, E., Gugliuzza, G., Tinebra, I., & Farina, V. (2023) · Food Bioscience · doi:10.1016/j.fbio.2023.103349 · Cited by 21
EFFECT OF GREEN AND ROASTED COFFEE ANTIOXIDANTS ON QUALITY AND SHELF LIFE OF COOKIES AND CHOCOLATES
Budryn, G., & Nebesny, E. (2012) · Journal of Food Processing and Preservation · doi:10.1111/j.1745-4549.2012.00710.x · Cited by 21
Influence of 2-Weeks Ingestion of High Chlorogenic Acid Coffee on Mood State, Performance, and Postexercise Inflammation and Oxidative Stress: A Randomized, Placebo-Controlled Trial
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“CQAs are poorly and incompletely absorbed in the upper gastrointestinal tract, with most entering the large intestine unmetabolized (Farah et al., 2008; Monteiro et al., 2007; Renouf et al., 2014; Stalmach et al., 2010).”
Background
Development and Validation of Methods for the Extraction of Phenolic Acids from Plasma, Urine, and Liver and Analysis by UPLC-MS
de Oliveira, D. M., Pinto, C. B., Sampaio, G. R., Yonekura, L., Catharino, R. R., & Bastos, D. H. M. (2013) · Journal of Agricultural and Food Chemistry · doi:10.1021/jf401534d · Cited by 21
A Natural Polyphenol, Chlorogenic Acid, Attenuates Obesity-Related Metabolic Disorders in Male Rats via miR-146a-IRAK1-TRAF6 and NRF2-Mediated Antioxidant Pathways
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“These findings are consistent with prior reports showing that CGA reduces adiposity and improves metabolic health in obese animal models [17].”
Optimization of the extraction process of coffee pulp as a source of antioxidant
Kusumocahyo, S. P., Wijaya, S., Dewi, A., Rahmawati, D., & Widiputri, D. I. (2020) · IOP Conference Series Earth and Environmental Science · doi:10.1088/1755-1315/443/1/012052 · Cited by 20
“Since coffee bean has been known to have an antioxidant property [2,3], the study on the bioactive compounds in the coffee byproduct is important with the aim to give an economical added value of this byproduct [4–6].”
Background
Synergistic Effect of Acarbose–Chlorogenic Acid on α-Glucosidase Inhibition: Kinetics and Interaction Studies Reveal Mixed-Type Inhibition and Denaturant Effect of Chlorogenic Acid
Abioye, R. O., Nwamba, O. C., Okagu, O. D., & Udenigwe, C. C. (2023) · ACS Food Science & Technology · doi:10.1021/acsfoodscitech.3c00146 · Cited by 20
Improved on-line high performance liquid chromatography method for detection of antioxidants in Eucommia ulmoides Oliver flower
Zhang, Q., Zhu, M.-Q., Zhang, J., & Su, Y. (2014) · Journal of Bioscience and Bioengineering · doi:10.1016/j.jbiosc.2013.12.009 · Cited by 20

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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