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Coffea spp.
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Evidence of Activity
Pharmacokinetics (ADME)
Investigated the interaction of coffee diterpenes cafestol, kahweol, and 16-O-methylcafestol palmitates
with serum albumins to help explain their interactions with biologically active xenobiotics. Berti 2020
Demonstrated a new MEKC method for determining caffeine and its three main downstream metabolites, paraxanthine, theobromine, and theophylline, in human plasma. The plasma concentrations of the four analytes are significantly lower in patients with early PD than in control subjects. Han 2020
A 3 arm crossover randomized trial of 21 volunteers assessing the absorption, pharmacokinetics, and urinary exretion of coffee pyridines and their metabolites after daily regular exposure to coffee or cocoa-based products containing coffee. Bresciani 2020
Erratum for: Molecular networking based LC/MS reveals novel biotransformation products of green coffee by ex vivo cultures of the human gut microbiome. [No abstract] Farag 2020
Developed, applied and validated a LC-MS/MS-based method for the simultaneous measurement of methylxanthines and methylurates in a pharmacokinetic study of 12 subjects orally administered caffeine and methylurates (methylliberine and theacrine) from Coffea liberica. Wang 2020
Results from an 18-week study of coffee drinkers show that 2'R-ochratoxin A has more than a 7-fold higher biological half-life in human blood compared to ochratoxin A. Sueck 2019
In an in vitro model of digestion-fermentation, the bioactivity of green and roasted coffees were uniquely altered, with significant changes to antioxidant capacity, polyphenol profile, production of short chain fatty acids, as well as change in human gut microbiota community structure. Pérez-Burillo 2019
Identified 6 potential markers of coffee consumption in the human urine volatilome. Mack 2019
A cross-sectional analysis of 1664 participants assessed associations between 387 metabolite levels with total, caffeinated, or decaffeinated coffee consumption. Papandreou 2019
Based on intra-class correlations obtained from Exposure Reconstruction Approach study samples, it may be possible to estimate urine caffeine, theophylline, and paraxanthine concentrations over a 24-h period by use of a single spot urine sample, with more samples needed for longer timeframes. Rybak 2019
A human intervention study which investigated the excretion of alkylpyrazine metabolites in urine after the ingestion of brewed coffee containing alkylpyrazines is consistent with earlier rodent studies. Kremer 2019
Profiled metabolites of 16 green and roasted Indonesian coffees from different species and geographical origins. Putri 2019
Metabolic profiling performed on serum samples from 451 European participants identified coffee metabolites associated with self-reported habitual coffee intake. Correlation strength for each metabolite varied by the participant's nationality. Rothwell 2019
Development of a UHPLC-QTOF mass spectrometry-based method for the quantification of uptake and determination of intracellular bacterial concentrations of dietary phenolics from coffee and tea. Data indicated a time-dependent differential uptake of nutritional compounds. Hakeem Said 2018
A 4-day human intervention study on the excretion of major niacin metabolites in the urine of volunteers after ingestion of 500 mL regular coffee concluded that regular coffee consumption is a source of niacin in the human diet. Kremer 2018
Analyzed individual metabolite changes in responses to changes in coffee intake in 47 habitual coffee consumers. A total of 115 metabolites were significantly associated with coffee intake. Cornelis 2018
Oral intake of coffee by bilateral cataract patients scheduled for cataract surgery significantly increased caffeine concentrations in the lens capsule and lens epithelial cells in a dose-dependent manner. Kronschläger 2018
A double-blind crossover study in 16 healthy males showed that chlorogenic acid compounds from a green coffee extract are bioavailable; 3-CGA may be the best absorbed. Caffeine sourced from a green coffee extract versus a synthetic caffeine were statistically similar for pharmacokinetic parameters. Morton 2018
(Poly)phenolic compounds in the green tea and green coffee bean extracts were absorbed and excreted after simultaneous consumption, with green tea resulting in more inter-individual variability in urinary excretion of phenolic metabolites. Mena 2018
Review discussed data concerning the genetic variability affecting caffeine levels and effects at the pharmacokinetic and pharmacodynamic levels that both critically drive the level of caffeine consumption. Nehlig 2018
Review of results from dietary intervention studies and observational studies indicated that a variety of compounds derived from phenolic acids, alkaloids, and terpenes were shown to be associated with coffee intake and trigonelline and cyclo(isoleucylprolyl) showed a particularly high specificity. Rothwell 2018
Proposed two parallel degradation pathways, an oxidative route and a reductive route, of quinic acid in gut metabolism. Quinic acid is abundant in its free form in foods, like coffee. It is released in the colon when chlorogenic acid is hydrolyzed by microbial esterases. Naranjo Pinta 2018
Determination of the bioavailability of hydroxycinnamates in an instant green/roasted coffee blend in 12 healthy, fasting adults via analysis of blood, urine, and colonic metabolites. Gómez-Juaristi 2018
Consumption of a cup of coffee altered urinary excretion of some proteins in a sample of 30 healthy individuals. Peerapen 2017
Results from a controlled, open-label, randomized, cross-over indicated that the pharmokinetics of caffeine administered using chewing gum versus instant coffee are comparable and existing scientific literature on caffeine can be leveraged to support the safety of caffeinated chewing gum. Sadek 2017
Identification of urinary polyphenol metabolite patterns by a novel algorithm to explain polyphenol-rich food intake. High performance was observed for explaining recent intake of coffee. These metabolite patterns performed better or equally well compared to single polyphenol biomarkers. Noh 2017
Correction to 2-Furoylglycine as a Candidate Biomarker of Coffee Consumption. [No abstract] Heinzmann 2016
Isochlorogenic acid A, commonly found in coffee and other plant-based food and herbal products, indicated that it weakly inhibits CYP2C9 activity in human liver microsomes in vitro and inhibits UGT1A6 activity in mice. Moreover, ICQA showed no mechanism-based inhibition on CYP2C9 or UGT1A6. Wang 2016
Identification of genetic factors contributing to variation in caffeine metabolism and their role in dietary caffeine consumption behavior among individuals of European ancestry. Variants associated with slow caffeine and paraxanthine metabolism were associated with lower coffee consumption. Cornelis 2016
Results of a genome-wide association study in 2 Italian populations highlight a novel gene, PDSS2, which was shown to negatively regulate the expression of the caffeine metabolism genes and can thus be linked to coffee consumption. Pirastu 2016
Identification of novel biomarkers of reported habitual food intake, including coffee, using targeted and nontargeted metabolomic blood profiling in a large twin cohort. Pallister 2016
In vitro simulated digestion caused a reduction in the phenolic contents and antioxidant activities of beverages, including coffee, indicating that measurements of antioxidant activities of beverages submitted solely to aqueous extraction may be overestimated. Koehnlein 2016
Assessed the potential intestinal absorption of phenolic compounds and organic acids from commercial instant coffee samples using an in vitro model. López-Froilán 2016
A case report of a 32-yr-old lactating mother who smoked tobacco and consumed caffeinated drinks. Analysis of her breast milk after smoking 1 cigarette and drinking 1 cup of espresso revealed that it took 3 hr for nicotine, 72 hr for cotinine, and 24 hr for caffeine to be cleared from the milk. Calvaresi 2016
Results of a study of 24 healthy subjects aged 18-30 suggested that caffeine absorption and exposure from coffee and energy drink is similar irrespective of beverage temperature or rate of consumption. White 2016
A randomized, double-blind, crossover study of 12 healthy volunteers found that the roasting process did not influence the extent of conjugation of chlorogenic and phenolic acids from instant coffees, despite different absorption rates between roasting degrees. Sanchez-Bridge 2016
Cafestol and 16-O-methylcafestol, diterpenes present in coffee, reacted with three different albumins such that the diterpenes did not displace reference binding drugs of site 2, but rather they enhanced the affinity of the site for the drugs. Guercia 2016
Evaluation of changes in polyphenol profile and antioxidant capacity of five soluble coffees throughout a simulated gastro-intestinal digestion, including absorption through a dialysis machine. Podio 2015
Identification of 2-furoylglycine (2-FG) as a novel putative biomarker for coffee consumption. Quantification of 2-FG in the urine of coffee drinkers, and investigation of its origin, metabolism, and excretion kinetics. Heinzmann 2015
Chlorogenic acids from spent coffee grounds were found to be bioaccessible to a relatively low degree in in vitro models of human digestion and intestinal absorption. Monente 2015
Data from a nested case-control study indicates serum metabolites can distinguish coffee drinkers from nondrinkers; some caffeine-related metabolites were inversely associated with colorectal cancer and should be studied further to clarify the role of coffee in the cause of colorectal cancer. Guertin 2015
A rapid absorption, metabolization and excretion of caffeine and its derived methylxanthines and methyluric acids were observed in 12 subjects after consumption of a green/roasted coffee product. Martínez-López 2014
Differentiation of metabolites from consumption of caffeinated vs decaffeinated coffee using a GC-TOF-MS-based metabolomics approach. Data may inform why consumption of caffeinated coffee, but not decaffeinated coffee or caffeine, appears to have benefits against dementia and Alzheimer's disease. Chang 2014
Characterization and quantification of α-Dicarbonyl (α-DC) compounds in roasted coffee, barley coffee, and soy sauce. In vitro simulated digestion reduced coffee's free α-DC content. Papetti 2014
Identification of metabolites that are biomarkers of usual dietary intake in serum from 502 participants in the Prostate, Lung, Colorectal, and Ovarian Cancer Screening Trial. Coffee was strongly associated with trigonelline-N-methylnicotinate and quinate. Guertin 2014
PNon-targeted profiling of the urinary metabolome of cohort study subjects, including both high coffee consumers and low consumers, identified new biomarkers of coffee consumption. Rothwell 2014
Development of a high-performance liquid chromatography-tandem mass spectrometric (LC-MS/MS) method for determining urine caffeine and 14 caffeine metabolites suitable for estimating caffeine exposure and metabolic phenotyping in population studies. Rybak 2014
Use of a validated liquid chromatography-electrospray ionization-tandem mass spectrometry (LC-ESI-MS/MS) method to analyze and quantify the metabolites of chlorogenic and phenolic acids in human plasma after oral ingestion of soluble coffee. Marmet 2014
Coffee phenolics appear in a positive dose-response manner in human adult plasma when drank at nutritionally relevant doses. Renouf 2014
Caffeic acid, present in coffee, fruits, and vegetables, inhibited organic anion transporters OAT1 and OAT3, which are responsible for renal tubular secretion of anionic drugs, in the rat kidney. Uwai 2013
Identification of putative bioactive coffee-metabolites in urine from coffee drinkers compared to non-coffee drinkers that may contribute to preventing type 2 diabetes and Alzheimer's disease. Lang 2013
Investigation of the effect of the simultaneous consumption of coffee and milk on the urinary excretion of chlorogenic acids (CGA) and metabolites shows the simultaneous consumption of milk and coffee may impair the bioavailability of coffee CGA in humans. Duarte 2011
In a randomised cross-over design with 9 healthy subjects dihydroferulic acid and dihydrocaffeic acid were the major metabolites that appeared after coffee consumption with a long time needed to reach maximum plasma concentration, suggesting metabolism and absorption in the colon. Renouf 2010
History of Record
ORIGINAL RESEARCH BY: J. Mohanasundaram, MD, PhD
April 2013
May 2019
LATEST UPDATES BY: Oren Rabinowitz, MSc
December 2020