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Nutraceuticals based on plant extracts rich in polyphenols, as well as dietary fibres, are new means to fight overweight/obesity and associated diseases. However, to understand the potential effects of polyphenols on health it is critical to study their bioavailability and metabolic fate. Consumption of a green coffee phenolic extract (GCPE) in combination with oat beta-glucan (BG) could affect the pharmacokinetic profile of the main polyphenols present in coffee (hydroxycinnamates). Moreover, the regular intake of the combination could also induce changes. Nine overweight men and women consumed a novel nutraceutical product containing 300 mg of green coffee hydroxycinnamic acids and 2.5 g of BG twice a day for 8 weeks. A pharmacokinetic study was carried out in blood and urine samples taken before (baseline) and at week 8 after the nutraceutical intervention, collecting samples at different times in a 0–24 h interval. Faecal samples were also obtained at 0 and 24 h after the intake of the nutraceutical at baseline and week 8. Phenolic metabolites were analysed by LC-MS-QToF. Results showed that polyphenols were differentially absorbed and extensively metabolized throughout the gastrointestinal tract. An apparent reduction in the excretion of small intestinal metabolites was accompanied by a tendency to increase colonic metabolites after sustained intake (p = 0.052). In conclusion, continued consumption of the GCPE/BG nutraceutical appears to enhance the absorption of hydroxycinnamates by increasing the colonic bioavailability of their derived metabolites compared to baseline, although the regular intake of the nutraceutical did not modify the metabolite profile in any of the biological samples., This research was funded by project AGL2015-69986-R from the Ministerio de Economía y Competitividad and grant PIE202070E184 funded by CSIC. MAS and JGC had predoctoral grants funded by Comunidad de Madrid (PEJD-2018-PRE/SAL-9104), respectively.

Obesity and its associated comorbidities are a major public health concern worldwide. Reduced energy intake and increased physical activity interventions have limited success in the long term. Nutraceuticals might be an alternative means to help lose weight and reduce obesity-associated cardiometabolic risk factors without changes in the habitual diet. The objective of the present study was to comparatively evaluate the efficiency of nutraceuticals based on the combination of a decaffeinated green coffee bean extract (GCBE) and two types of oat beta-glucans (BG) with different physiochemical properties on obesity related biomarkers in overweight/obese subjects. A randomized, dose–response, parallel, blind study was carried out in four groups of subjects (n = 15 each) who consumed for 6 weeks, twice a day, a nutraceutical containing 3 g d−1 or 5 g d−1 doses of 35% or 70% BG and a fixed amount of GCBE providing 600 mg d−1 of phenols. 35% BG showed a 10 and 100 times higher molecular weight and viscosity, respectively, compared to 70% BG. Food intake, anthropometry and different cardiometabolic markers were assessed at the beginning and end of the intervention. According to the general model of variance with repeated measure analysis, the intervention caused positive changes in the levels of total cholesterol, LDL cholesterol, VLDL cholesterol, triglycerides, alanine aminotransferase, aspartate aminotransferase, haemoglobin A1c, insulin, systolic blood pressure (SBP), total body fat percentage (TBF%), visceral fat percentage, and waist and hip circumferences without differences among the treatments, except for SBP and TBF%. Looking into the rates of change [(end value − beginning value)/beginning value] of these parameters, 5 g – 70% BG was the treatment that lowered TBF% the most. In conclusion, 5 g – 70% BG may be more effective in helping to lose weight and additionally, it produced the least bloating according to participants’ subjective perception., This research was funded by project AGL2015-69986-R from the Ministerio de Economía y Competitividad. JGC had a predoctoral grant funded by Comunidad de Madrid (PEJD-2018-PRE/SAL-9104).

Purpose This study aimed to assess the effect of dietary consumption of olive pomace oil (OPO) on blood lipids (primary outcome) and other cardiovascular disease (CVD) risk factors (blood pressure, inflammation and endothelial function as secondary outcomes). Methods A randomized, controlled, blind, crossover intervention was carried out in healthy and at-risk (hypercholesterolemic) subjects. Participants consumed daily 45 g of OPO or high-oleic acid sunflower oil (HOSO) as control oil during 4 weeks. Results OPO significantly reduced low-density lipoprotein cholesterol (LDL-C; P = 0.003) and apolipoprotein B (Apo B; P = 0.022) serum concentrations, and LDL/HDL ratio (P = 0.027) in healthy and at-risk volunteers. These effects were not observed with HOSO. Blood pressure, peripheral artery tonometry (PAT), endothelial function and inflammation biomarkers were not affected. Conclusions Regular consumption of OPO in the diet could have hypolipidemic actions in subjects at cardiovascular risk as well as in healthy consumers, contributing to CVD prevention. Clinical trial registry NCT04997122, August 8, 2021, retrospectively registered.

Olive-pomace oil is rich in oleic acid, and thus it can be an interesting dietary fat alternative as it can allow reaching the recommendation of consuming 20% of total diet energy in the form of monounsaturated fatty acids. In addition, olive-pomace oil also contains a wide range of minor components that may contribute to its healthy properties. The major components identified with healthy properties are triterpenic dialcohols and acids, squalene, tocopherols, sterols, fatty alcohols and phenolic compounds. The refining process, that the crude pomace-oil must undergo for commercial purposes, significantly reduces the content of phenolic compounds, while the other minor components remain at concentrations which can induce positive health effects, especially on cardiovascular health, outstanding pentacyclic triterpenes and aliphatic fatty alcohols in olive-pomace oil. Numerous in vitro and preclinical studies support that mainly the pure compounds, or extracts isolated from plant sources, play an important role in preventing cardiovascular disease and risk factors. Likewise, tocopherols, squalene and phytosterols, in addition to the minor fraction of phenolic compounds, have shown high biological activity with particular association to the cardiovascular function. In the light of the foregoing, and taking into consideration the absence of clinical studies with olive-pomace oil, it would be of great interest to develop randomized, crossover, controlled, double-blind studies to extend the knowledge and understanding on the health effects of olive-pomace olive., The authors thank ORIVA (Interprofesional del Aceite de orujo de Oliva) for finanacial support (Projects-References 20175429 and 20185194).

The present work aimed at understanding gut microbiota bioconversion of phenolic compounds (PC) and organic acids in predigested Hibiscus sabdariffa (Hb) calyces and the mixture of Hb and Agave (Agave tequilana Weber) fructans (AF). With this purpose, dried Hb and Hb/AF were predigested with enzymatic treatment, and then fermented in a dynamic in vitro model of the human colon (TIM-2). After HPLC-ESI-QToF-MS analysis of samples taken at 0, 24, 48 and 72 h of fermentation, it was observed that hydroxycinnamic acids, flavanols, flavonols, and anthocyanins were mainly transformed into derivatives of hydroxyphenylpropionic, hydroxyphenylacetic and hydroxybenzoic acids. Moreover, organic acids, such as hydroxycitric and hibiscus acids, were formed along with unidentified lactones and reduced compounds. Interestingly, no differences were observed between microbial-derived metabolites formed after the fermentation of Hb and Hb/AF. In conclusion, colonic fermentation of polyphenol-rich Hb yields a wide range of microbial phenolic metabolites with potential effects on health., RMB and SGSA acknowledge to Science and Technology for Development Program (CYTED) through the Ibero-American Network of Underutilized Autonomous Foods (ALSUB-CYTED, 118RT0543). SGSA acknowledges CONACYT-Mexico for the sabbatical grant 260935. The Spanish Ministry of Science, Innovation and Universities (Project AGL2015-69986-R) is also acknowledged. This research has been made possible with the support of the Dutch Province of Limburg.

Resumen del póster presentado a la 1st International E-Conference on Antioxidants in Health and Disease, celebrada del 1 al 15 de diciembre de 2020., Mango byproducts are a relevant source of phenolic compounds that have already been shown to display a multitud e of health beneficial properties. The biological activity of a compound is determined by its absorption and metabolism. Considering the low bioavailability of polyphenols at small intestinal level, it is important to study the biotransformation of mango peel polyphenols bythe gut microbiota to determine the chemical structure of the potential bioactive microbial·derived metabolites. Thus, gut microbiota bioconversion of polyphenols in predigested mango 'Ataulfo' peel was studied using a validated, dynamic in vitro human colon model (TIM·2) with faecal microbial inoculum. Driel peels were predigested with enzymatic treatment, followed by TIM·2 fermentation (72h). Samples were taken at O, 24, 48 and 72h and a nelyzed by HPLC·QToF. Derivatives of hydroxyphenylpropionic, hydroxyphenylacetic and hydroxybenzoic acids, as well as pyrogallol were the main polyphenols identified. These metabolites might derive from the biotrasnsformation of flavonoids (flavanols and flavonols), gel lates and gallotannins in mango peel. Despite the high content of ellagic acid, low amounts were detected in TIM·2 samples due to trasnsformation mainly into urolithins A and C. Xanthone and benzophenone derivatives, specific to mango, remained after the colonic biotransformation, contrary to flavonoids, which completely disappeared. In conclusion, microbiel derived metabolites, especially xanthone and benzophenone derivatives, are partially stable after colonic fermentation, and thus have the potential to contribute to mango peel bioactivity.

Rosmarinus officinalis L. is a widespread aromatic plant commonly consumed as a tea in traditional cuisine and in folk medicine to treat various illnesses due to its therapeutic properties. To the best of our knowledge, there are no reports on the bioavailability and metabolism of R. officinalis tea polyphenols in humans. This study was aimed at assessing the bioavailability and nutrikinetics of R. officinalis phenolic compounds in healthy humans for the first time. Forty-eight compounds were identified in plasma and urine. Few un-metabolized compounds were detected since rosemary polyphenols were extensively metabolized into phase II conjugates, with rapid appearance and clearance in plasma, pointing to small intestinal absorption. Phase II derivatives of caffeic acid showed kinetics compatible with both intestinal and colonic hydrolysis of rosmarinic acid yielding free caffeic and 3,4-dihydroxyphenyl-lactic acids, which were absorbed and metabolized into phase II derivatives. These metabolites, along with reduced forms of caffeic acid and their phase II metabolites, and those of hydroxyphenylpropionic, hydroxylphenylacetic, benzoic and hippuric acids, highlight the importance of colonic absorption. Total urinary excretion of the phenols added up to 235 µmol, corresponding to 22.3% of the ingested amount (1055 µM). In conclusion, rosemary tea polyphenols are partially bioavailable and extensively metabolized, mainly by the colonic microbiota., We acknowledge financial support received from the Tunisian Ministry of Higher Education and Scientific Research, and from the Spanish Ministry of Economy, Industry and Competitivity (project AGL2015-69986-R).

Husk tomato (Physalis ixocarpa Brot. ex. Horm) is mainly used in the preparation of many Mexican sauces due to its unique and slightly acidic flavor, both in raw and cooked forms. These sauces also usually contain Serrano hot pepper (Capsicum annuum L), onion (Allium cepa L.), garlic (Allium sativum L.), coriander (Coriandrum sativum L.) and salt. Mexican sauces are a pre-Hispanic staple food, yet there is scarce knowledge on the phenolic compounds (PC) that reach the colon bound to the indigestible fraction (IF) after intestinal digestion. Thus, the aim of the present work was to evaluate the indigestible fraction of two types of Mexican sauces made with cooked and raw husk tomato: cooked green sauce (CGS) and raw green sauce (RGS). IF of CGS and RGS were fermented in the in vitro model of the human colon (TIM-2) to investigate the PC bioconversion by the gut microbiota after 24, 48 and 72 h. PC of the original sauces and their predigested fractions, as well as the formed metabolites were identified and monitored by HPLC-ESI-QToF-MS. Cooking husk tomato significantly increased the total indigestible fraction (TIF), mainly due to its insoluble indigestible fraction (IIF), and diminished PC. Flavonoids (flavonols and flavones) were the most abundant phenolic group in digested sauces followed by capsaicinoids (a characteristic group derived from hot pepper), hydroxycinnamic acids, and hydroxybenzoic acids. The metabolites 3-(ρ-hydroxyphenyl) propionic acid, 3-(3-hydroxyphenyl) propionic acid and 4-hydroxyphenylacetic acid were the most abundant colonic metabolites identified, which are thought to be derived from the biotransformation of flavonoids and hydroxycinnamates. These results are the first obtained on in vitro colonic fermentation of Mexican sauces and should be considered in future studies on the health effects related to consuming this staple food., The Spanish Ministry of Science, Innovation and Universities (Project AGL2015-69986-R) is also acknowledged. Alicia Paulina Cárdenas Castro thanks CONACYT-Mexico for the financial support, grant registration number: 662703 and Koen Venema acknowledges the support of the Dutch Province of Limburg.

Yerba mate is highly consumed in South America and has become a popular beverage worldwide because of its healthy properties: antioxidant, vaso-dilating, lipid-reducing, anti-glycation, anti-inflammatory and weight-reducing effects, among others. These effects have been attributed to its high content in polyphenols, mainly chlorogenic acidS, but also quercetin, kaempferol and rutin. Other components in mate are methylxhantines, saponins, vitamins, minerals and alkaloids.The objective of this work was to evaluate the effects of regularly consuming a moderate, realistic amount of yerba mate (3 beverages/day) on cardiovascular health and anthropometric parameters, in healthy and cardiovascular risk subjects.A randomized, crossover, controlled study was performed in normocholesterolemic (NC, n = 25) and hypercholesterolemic (HC, n = 27), non-smoker, non-vegetarian, men and women, with BMI 18–25 kg/m2. After a run-in stage, the effects of consuming three servings/day of mate during 8 weeks (mate stage) were compared with an isotonic drink during the same time (control stage). Along the study, polyphenol rich foods were restricted. At the beginning and the end of each intervention, blood pressure was measured, urine and blood samples were collected. Triglycerides (TG), total cholesterol (TC), high-density lipoprotein (HDL), low-density lipoprotein (LDL) and very-low-density lipoprotein (VLDL) cholesterol concentrations were measured. Dietary records and physical activity questionnaires were completed in each stage. Results were statistically studied using a mix model with repeated measures and Bonferroni test (SPSS 23.0).The regular consumption of yerba mate decreased blood lipid concentrations [TC (p < 0.001), LDL (p = 0.001), TG (p = 0.027)] and blood pressure [systolic (p < 0.001), diastolic (< 0.001)] in both groups, with greater effects in HC than NC. Thus, it may be concluded that moderate consumption of yerba mate reduces cardiovascular risk, particularly in hypercholesterolemic subjects.Funded by the Spanish State Research Agency, projects AGL2010-18269 and AGL2015-69986-R

[Background]: In many cocoa intervention studies, health outcomes are related to cocoa components without taking into account the bioavailability of the main bioactive components: phenolic compounds and methylxanthines., [Methods]: The present work associates the results of bioavailability and randomised controlled crossover studies in humans carried out with similar cocoa products, so that the main phenol and methylxanthine metabolites observed in plasma and urine are associated to the health effects observed in the chronic studies. We outstand that doses of cocoa and consumption rate used are realistic. In the bioavailability study, a conventional (CC) and a methylxanthine-polyphenol rich (MPC) cocoa product were used, whereas in the chronic study a dietary fibre-rich (DFC) and a polyphenol-rich (PC) product were studied in healthy and cardiovascular risk subjects., [Results and Discussion]: The main phenolic metabolites formed after CC and MPC intake, 5-(4′-hydroxyphenyl)-γ-valerolactone-3′-sulfate, 3′-methyl-epicatechin-5-sulfate, 4-hydroxy-5-(4′-hydroxyphenyl)valeric acid-sulfate, 5-phenyl-γ-valerolactone--sulfate and 5-(4′-hydroxyphenyl)-γ-valerolactone-3′-glucuronide, may contribute to the changes in cholesterol (and indirectly HDL-cholesterol) observed after the regular intake of both DFC and PC, in healthy and cardiovascular risk subjects, whereas 7-methylxanthine (the main cocoa methylxanthine metabolite) and theobromine, together with its content in insoluble dietary fibre, may be responsible for the decrease of IL-1β and hypoglycemic effects observed with DFC. With both phenolic and methylxanthine metabolites a strong dose–response effect was observed., [Conclusion]: After the regular consumption of both DFC and PC, positive changes were observed in volunteer’s lipid profile, which may be related to the long-lasting presence of colonic phenolic metabolites in blood. In contrast, the anti-inflammatory and hypoglycemic effects were only observed with DFC, and these may be related to methylxanthine metabolites, and it is likely that insoluble dietary fibre may have also played a role., Nutrexpa, S.L. funded the study and the Spanish Ministry of Economy and Competitivity (MINECO-FEDER), projects AGL2010-18269 and AGL2015-69986-R provided financial support. Sara Martínez López was a predoctoral fellow of the JAE Program (JAEPre097) co-funded by CSIC and the European Social Fund. Miren Gómez-Juaristi was a predoctoral FPI fellow BES2008-007138 of the Spanish Ministry of Science and Innovation.

Obesity and its associated comorbidities (type 2 diabetes mellitus, cardiovascular disease, etc.) are a major public health concern worldwide, with prevalence of obesity affecting in Europe up to 17% of the adult population (OCED/EU 2016). Strategies to lose weight mostly relay in lifestyle changes such as restriction in food intake and increased exercise. However, these are not always easily accepted by overweight/obese subjects and their long-term efficiency is limited. Nutraceuticals and functional foods might be an alternative means to help lose weight and reduce associated cardiometabolic risk factors in affected subjects. There are different nutraceuticals/functional foods containing dietary fibre (DF) or polyphenol-rich plant extracts, but to our knowledge there is no nutraceutical combining both bioactive compounds.The objective of the present study was to assess the efficiency on different risk makers of a dietary supplement combining a soluble DF (oat beta-glucan -BG-) and a green coffee bean extract (GCBE) rich in polyphenols (PP) in overweight/obese subject.A randomized, parallel, blind, dose-response study was performed in 60 overweight/obese subjects divided into four groups (n = 15) who consumed during 6 weeks two servings per day of one of four nutraceutical formulations containing low (3 g/d) or high (5 g/d) doses of BG of different purity (35 & 70%) and a fixed amount of GCBE providing 600 mg/d PP. Food intake, anthropometry and different cardiometabolic markers were assessed at the beginning and end of the intervention.Results showed reduced levels of total cholesterol (p = 0.0001), LDL-cholesterol (p = 0.01), VLDL-cholesterol (p = 0.014) and triglycerides (p = 0.023). There were differences among both types of BG, with the 35% BG being more effective reducing lipid plasma levels than the 70% BG. Percentage of body fat significantly decreased after the intervention, the 70% BG being more efficient than the 35% BG. However, there was no effect on body weight and body mass index, which were not significantly modifiedIt can be concluded that DF and PP might have a synergistic effect reducing cardiometabolic risk factors in overweight/obese subjects.Funded by Spanish State Research Agency, project AGL2015-69986-R

Studying bioavailability of polyphenols is essential to understand the health effects of these compounds. Human epithelial cells are commonly used in intestinal absorption and transport experiments but the changes polyphenols undergo during incubation, due to their chemical instability under the cell culture conditions, are scarcely known and might lead to inaccurate conclusions. Based on abundance of flavanols and hydroxycinnamic acids in the diet, epicatechin, epicatechin-3-gallate and procyanidin B2 as flavanols along with 5-caffeoylquinic and 3,5-dicaffeoylquinic acids as hydroxycinnamic acids were selected to comparatively evaluate their absorption and metabolism using an in vitro Caco-2 cell model. Special emphasis was paid to the structure-stability relationship of these phenolic compounds in Dulbecco’s Modified Eagle’s Medium (DMEM) under the cell culture conditions. The tested compounds were scarcely absorbed and minimally metabolized by the intestinal epithelium cells. The cell transport study showed prevalent efflux for flavanols opposite to absorption for hydroxycinnamates. Intestinal metabolism revealed that hydroxycinnamates were preferentially hydrolyzed and subsequently methylated, whereas hydrolysis of flavanols could not be confirmed, being mostly conjugated to sulfate, methyl- and methyl-sulfate derivatives. It is noteworthy that methyl derivatives of procyanidin-B2 were detected inside Caco-2 cells, confirming its absorption. In addition, culture medium influenced phenol isomerization to a higher extent than cells. In conclusion, hydroxycinnamates were better absorbed than flavanols although their bioavailability was limited in this intestinal cell model., The authors acknowledge financial support from the Spanish Ministry of Economy, Industry and Competitivity (Project AGL2015-69986-R) and the Analytical Techniques Service (USTA) at the Institute of Food Science, Technology and Nutrition (ICTAN-CSIC) for support in the LC-MS-QTOF analysis. M. G.-J. was a predoctoral FPI fellow BES2008-007138 of the Spanish Ministry of Science and Innovation.

Yerba mate (Ilex paraguariensis) infusions have been shown to reduce plasma glucose in animals and serum lipids in humans. However, the effects of regularly consuming yerba mate on glucose metabolism in humans has been less studied. The objective of the study was to evaluate the effects of regularly consuming yerba mate on diabetes related biomarkers in healthy and moderately hypercholesterolemic people.A randomized, crossover, controlled study was carried out in normocholesterolemic (NC, n = 25) and hypercholesterolemic (HC, n = 27), non-smoker and non-vegetarian, men and women, with BMI 18–25 kg/m2. After a run-in stage, the effects of consuming three servings/day of yerba mate in boiled water during 8 weeks (mate stage) were compared with an isotonic drink during the same time (control stage). Along the study, polyphenol rich foods were restricted. At the beginning and the end of each intervention, urine and blood samples were collected. Dietary records and physical activity questionnaires were completed in each stage. Glucose was analyzed using a colorimetric kit (Sprinreact), and insulin, glucagon, C-peptide, glucose-dependent insulinotropic polypeptide (GIP), glucagon-like peptide-1 (GLP-1), plasminogen activator inhibitor-1 (PAI-1), resistin and visfatin were analyzed using Bio-Rad Multiplex Diabetes kits on Bio-Plex MAGPIX system. Results were statistically studied using a mix model with repeated measures and a Bonferroni test within each group (SPSS 23.0).Nutrient intake and physical activitiy did not show changes along the study. In contrast, fasting levels of glucose, insulin, glucagon, and GLP-1 significantly decreased after the mate stage, showing glucagon a significant yerba mate*group interaction. Attending to these results, it may be concluded that sustained consumption of yerba mate may prevent type 2 diabetes. These outcomes indicate that the effects of yerba mate in pre-diabetes and T2DM subjects are worth further studying.Funded by the Spanish State Research Agency, projects AGL2010-18269 and AGL2015-69986-R

[Background]: Rosmarinus officinalis is an aromatic plant used in folk medicine as a result of the therapeutic properties associated with its phenolic composition, being rich in rosmarinic acid (RA) and caffeic acid (CA). To better understand the bioactivity of these compounds, their absorption and metabolism were assessed in human Caco-2 and HepG2 cells, as small intestine and liver models, respectively, using RA and CA standards, as well as a rosemary infusion and ferulic acid (FA). [Results]: Test compounds were partially up-taken and metabolized by Caco-2 and HepG2 cells, although a higher metabolization rate was observed after hepatic incubation compared to intestinal incubation. CA was the compound best absorbed followed by RA and FA, showing metabolites percentages of 30.4%, 11.8% and 4.4% in Caco-2 and 34.3%, 10.3% and 3.2% in HepG2 cells, respectively. RA in the rosemary infusion showed improved bioavailability compared to pure RA. Methyl derivatives were the main metabolites detected for CA and RA after intestinal and hepatic metabolism, followed by methyl-glucuronidates and glucuronidates. RA was also minimally hydrolyzed into CA, whereas FA only was glucuronidated. Rosemary polyphenols followed the same biotransformation pathways as the standards. In addition, phase II derivatives of luteolin were observed. [Conclusion]: Rosemary polyphenols are partially metabolized in both the intestine and liver., We acknowledge financial support received from the Tunisian Ministry of Higher Education and Scientific Research, and from the Spanish Ministry of Economy, Industry and Competitivity (Project AGL2015-69986-R).

Beverages prepared from antioxidant-rich plants are sources of polyphenols, the bioactivity of which depends on bioaccessibility in the gastrointestinal tract. This work evaluated the polyphenol content and antioxidant capacity of widely consumed beverages such as chamomile tea, yerba mate, a coffee blend (65% roasted: 35% green), and coffee-like substitutes such as chicory, malt and a soluble cereal mixture. Additionally, the bioaccessibility of the two beverages with the highest antioxidant capacity was evaluated using an in vitro digestion model.; Results: Total phenolic content ranged from 11.15 mg 200 mL-1 in chamomile tea, up to 154.53 mg 200 mL-1 in mate or 215.05 mg 200 mL-1 in the blend. These results correlated with the antioxidant capacity analysed by ferric reducing antioxidant power, oxygen radical scavenging capacity and 2,2'-azinobis-3-ethylbenzothiazoline-6-sulphonic acid methods. Yerba mate and the coffee blend showed an average polyphenol recovery after in vitro gastrointestinal digestion of 57% and 78%, respectively. Although both beverages showed similar phenolic composition, polyphenols in coffee were more stable than in yerba mate. Alkaline pH in the intestinal digestion stage was responsible for the observed reduction in polyphenol stability.; Conclusion: Regular consumption of the studied beverages provides considerable amounts of antioxidants which are relatively stable after simulated digestion, and thus have the potential to prevent oxidative stress-related disorders. © 2017 Society of Chemical Industry.; © 2017 Society of Chemical Industry.

Cocoa has beneficial health effects partly due to its high flavanol content. This study was aimed at assessing the absorption and metabolism of polyphenols in two soluble cocoa products: a conventional (CC) and a flavanol-rich product (CC-PP). A crossover, randomized, blind study was performed in 13 healthy men and women. On two different days, after an overnight fast, volunteers consumed one serving of CC (15 g) or CC-PP (25 g) in 200 mL of semi-skimmed milk containing 19.80 mg and 68.25 mg of flavanols, respectively. Blood and urine samples were taken, before and after CC and CC-PP consumption, and analyzed by high-performance liquid chromatography coupled to electrospray ionisation and quadrupole time-of-flight mass spectrometry (HPLC-ESI-QToF-MS). Up to 10 and 30 metabolites were identified in plasma and urine, respectively. Phase II derivatives of epicatechin were identified with kinetics compatible with small intestine absorption, although the most abundant groups of metabolites were phase II derivatives of phenyl-&gamma, valerolactone and phenylvaleric acid, formed at colonic level. 5-(4&prime, Hydroxyphenyl)-&gamma, valerolactone-sulfate could be a sensitive biomarker of cocoa flavanol intake. CC and CC-PP flavanols showed a dose-dependent absorption with a recovery of 35%. In conclusion, cocoa flavanols are moderately bioavailable and extensively metabolized, mainly by the colonic microbiota.

Coffee is the most widely consumed hot beverage worldwide. Intake of coffee may have an important impact on public health, and determining whether such impact is detrimental or positive has encouraged intensive research over the last decades. This chapter will review evidences from epidemiological and intervention studies on the effect of coffee on cardiovascular diseases (CVDs), discussing the role and mechanisms of action of the most relevant phytochemicals in coffee to shed light on the still controversial effects of coffee on cardiovascular health.Findings from case–control studies suggest a negative effect of coffee. In contrast, prospective studies systematically reveal that long-term consumption of moderate amounts of coffee is associated with a lower risk of coronary heart disease, heart failure, and stroke, but not with incident hypertension. Different outcomes on the effects of coffee on risk factors such as blood pressure, endothelial function, serum lipids, plasma homocysteine levels, or markers of oxidative stress and inflammation have been found depending on aspects like the type and methods of preparation (filtered vs. unfiltered), doses, content of chlorogenic acids and caffeine, acute vs. long-term effects, etc. Overall, evidences do not support a negative health impact of coffee, suggesting a preventive effect of moderate intakes against CVDs.

The main phenol in mate and coffee, 5-caffeoylquinic-acid (5-CQA), and its relevant microbial metabolites, dihydrocaffeic (DHCA) and dihydroferulic (DHFA) acids, have shown oxidative-stress protective effects in HepG2 cells. To evaluate possible endothelial-protective effects of the extracts and compounds, endothelial EA.hy926 cells were pre-treated with yerba mate (YME) and green coffee bean (GCBE) phenolic extracts, 5-CQA, DHCA and DHFA and afterwards stressed with tumour-necrosis-factor-alpha (TNF-α). Then oxidative-stress markers and endothelial-nitric-oxide-synthase levels were studied. TNF-α (10 ng/mL, 24 h) depleted reduced glutathione (GSH) and eNOS levels, increased reactive oxygen species (ROS) production, glutathione peroxidase (GPx) and reductase (GR) activities, and protein oxidation (carbonyl groups, CG) in EA.hy926 cells. Pre-treatment with YME, GCBE, 5-CQA, DHCA at certain physiological concentrations, lowered ROS production, recovered depleted GSH, reduced GR and GPx activities, and CG levels, and enhanced eNOS concentration.. YME, GCBE and 5-CQA show antioxidant effects in endothelial cells playing DHCA an important role in such protection; moreover, the extracts, 5-CQA, DHCA and DHFA increased eNOS levels., This work was supported by projects AGL2010-18269 and AGL2015-69986-R funded by the Spanish Ministry of Economy and Competitivity, and project PIE-201670E061 funded by Consejo Superior de Investigaciones Cientificas (CSIC). Shenli Wang thanks the Chinese Government for her PhD Scholarship.

Red grape pomace (RGP) is a major winery by-product with interesting applications due to its high phenolic content and antioxidant capacity. Effects of in vitro gastrointestinal digestion and storage on the phenolic content and antioxidant capacity of RGP were studied. RGP polyphenols were stable under stomach-mimicking conditions and more sensitive to small intestine conditions, reducing anthocyanins and flavonols. After 3- and 6-month storage, at either 4 or 25 °C, there were no changes in the total phenolic and condensed tannin content, or antioxidant capacity (evaluated by ABTS, FRAP, ORAC assays); however, after 9 months these parameters decreased. Contrarily, chromatic b* values were higher, thus the samples had more intense red color, which may be related to the increased condensed tannin content. Storage time or temperature induced no changes in microbiological load. RGP preserves high antioxidant capacity after storage and in vitro digestion and thus presents potential as a functional ingredient or nutraceutical., This research has been funded by Projects AGL2010-18269, CSD2010-00063 and INCOMES. S. W. would like to thank the Chinese Government for her PhD Scholarship and M. A-B. would like to thank the CSIC and European Social Funds for financing her JAEdoc contract in the period 2011–2014.

Yerba mate is a beverage rich in bioactive compounds popular in South America. Polyphenols and methylxanthines were qualitatively and quantitatively analyzed in four commercial brands of yerba mate, as well as the antioxidant capacity of the beverages. Using LC/MS analysis, 58 polyphenols were observed of which 4-sinapoylquinic acid, di- and tri-methoxycinnamoylquinic acids, two isomers of trimethoxycinnamoylshikimic acid and four isomers of caffeoyl-2,7-anhydro-3-deoxy-2-octulopyranosonic acid were identified for the first time in mate. Additionally, 46 polyphenols and 2 methylxanthines were quantified by HPLC-DAD. Hydroxycinnamic acid derivatives and flavonols comprised 90% and 10% of mate phenols, respectively, 3-caffeoylquinic (26.8–28.8%), 5-caffeoylquinic (21.1–22.4%), 4-caffeoylquinic (12.6–14.2%) and 3,5-dicaffeoylquinic acids (9.5–11.3%) along with rutin (7.1–7.8%) were the most abundant polyphenols, whereas caffeine was the main methylxanthine (90%). Ilex paraguariensis is an important source of polyphenols with moderate methylxanthines content; therefore its high antioxidant capacity was mainly associated to its polyphenolic composition., This work was funded by the Spanish Ministry of Economy and Competitivity (MINECO-FEDER), projects AGL2010-18269 and AGL2015-69986-R. G.B. is a FPI fellow (BES-2011-047476) funded by the Spanish Ministry of Science and Innovation and performed most experiments.

Roasting greatly reduces the phenolic content in green coffee beans. Considering the beneficial effects of coffee polyphenols, blends containing green coffee beans are being consumed as a healthier alternative to roasted coffee. This study was aimed at assessing the absorption and metabolism of hydroxycinnamates in an instant green/roasted (35/65) coffee blend in healthy humans. Twelve fasting men and women consumed a cup of coffee containing 269.5 mg (760.6 μmol) of chlorogenic acids. Blood and urine samples were taken before and after coffee consumption at different times and analyzed by LC-MS-QToF. Up to 25 and 42 metabolites were identified in plasma and urine, respectively, mainly in the form of sulfate and methyl derivatives, and to a lower extent as glucuronides. Un-metabolized hydroxycinnamate esters (caffeoyl-, feruloyl-, and coumaroylquinic acids), hydroxycinnamic acids (caffeic, ferulic and coumaric acids) and their phase II metabolites, in addition to phase II derivatives of lactones, represented a minor group of metabolites (16.3% of the metabolites excreted in urine) with kinetics compatible with small intestine absorption. Dihydrohydroxycinnamic acids and their phase II derivatives, in addition to feruloylglycine, showed delayed kinetics due to their colonic origin and represented the most abundant group of metabolites (75.7% of total urinary metabolites). Dihydrohydroxycinnamate esters (dihydroferuloyl-, dihydrocaffeoyl- and dihydrocoumaroylquinic acids) have been identified for the first time in both plasma and urine, with microbial origin (excreted 8-12 h after coffee intake) amounting to 8% of total urinary metabolites. In conclusion, coffee polyphenols are partially bioavailable and extensively metabolized, mainly by the colonic microbiota.

[Purpose]: Coffee is rich in bioactive compounds with health beneficial properties, with green coffee presenting higher phenol content than roasted. We evaluated the effects of regularly consuming realistic amounts of a green/roasted coffee blend on cardiovascular health-related biomarkers., [Methods]: A randomized, cross-over, controlled study was carried out in 25 normocholesterolemic [total cholesterol (TC), [Results]: Attending to the general lineal model of variance for repeated measures, after the green/roasted coffee intervention significant reductions in TC, LDL-C, VLDL-C and triglycerides levels (p = 0.006, 0.001, 0.003 and 0.017, respectively), and a significant group effect were observed (0.001, [Conclusion]: Regular consumption of moderate amounts of a soluble green/roasted (35:65) coffee blend may contribute to improve cardiovascular health in moderately hypercholesterolemic people, as reducing serum lipids, blood pressure and body weight effects, as well as increasing plasma antioxidant capacity, have been observed. Moreover, positive influences on blood pressure, body weight, and plasma antioxidant capacity were obtained in the healthy group. Therefore, incorporation of green coffee beans into the coffee brew can be recommended as part of a dietary strategy to protect from cardiovascular disease., This study was funded by Projects AGL2010-18269 and AGL2015-69986-R from the Spanish Ministry of Economy and Competitivity. S. M.-L. thanks the Spanish National Research Council for her pre-doctoral fellowship under the JAE-Pre programme co-funded by CSIC and the European Social Fund.

Coffee is widely consumed worldwide; therefore, the methylxanthines contained in coffee, mainly caffeine (CF), are among the most abundant bioactive compounds in our diet. In the present work, the bioavailability and metabolism of methylxanthines in a commercial soluble green/roasted coffee blend was studied. After a 3-day restriction of methylxanthine-containing foods, fasting healthy subjects (12 men and women) consumed the coffee product containing 70.69mg CF and 0.119mg theobromine (TB). Plasma samples were taken before (t=0h) and after coffee consumption at different time points (0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 9, 10 and 12h). Urine was collected at baseline (-2-0h) and at different intervals (0-2, 2-5, 5-8, 8-12 and 12-24h). Samples were analyzed by HPLC-DAD and LC-MS-QToF, and pharmacokinetic parameters were calculated. CF was the main methylxanthine found in plasma (Cmax=10.50μM, Tmax=1.2h). In addition, seven methylxanthines and methyluric acids were detected between 0.5 and 12h after coffee intake, paraxanthine (PX) being the major metabolite (Cmax=3.36μM), followed by 1-methyluric acid (1-MU; Cmax=1.44μM) and 1-methylxanthine (1-MX; Cmax=1.27μM), identified in plasma samples for the first time. In 24h urine, eleven methylxanthines and methyluric acids were detected, 1-MU being the major metabolite (Cmax=150.52μM, Tmax=12h) amounting to 67.7% of the total urinary metabolites. In conclusion, a rapid absorption, metabolization and excretion of caffeine and its derived methylxanthines and methyluric acids have been observed after consumption of a green/roasted coffee product. © 2014 Elsevier Ltd., This work was funded by the Spanish Ministry of Science and Innovation (AGL2010-18269 and Consolider-IngenioCSD2007-00063). S.M.-L. is a predoctoral fellow of the JAE Program (JAEPre-097) funded by CSIC and the European Social Fund. G. B. is a FPI (BES-2011-047476) fellow funded by the Spanish Ministry of Science and Innovation

Beverages prepared from antioxidant-rich plants are sources of polyphenols, the bioactivity of which depends on bioaccessibility in the gastrointestinal tract. This work evaluated the polyphenol content and antioxidant capacity of widely consumed beverages such as chamomile tea, yerba mate, a coffee blend (65% roasted: 35% green), and coffee-like substitutes such as chicory, malt and a soluble cereal mixture. Additionally, the bioaccessibility of the two beverages with the highest antioxidant capacity was evaluated using an in vitro digestion model.Total phenolic content ranged from 11.15 mg 200 mLRegular consumption of the studied beverages provides considerable amounts of antioxidants which are relatively stable after simulated digestion, and thus have the potential to prevent oxidative stress-related disorders. © 2017 Society of Chemical Industry.

Bioavailability of yerba mate phenolic compounds was assessed in healthy humans. More than 34 metabolites were identified in biological fluids, mainly sulfated conjugates of caffeic and ferulic/isoferulic acids, in addition to non-metabolized caffeoyl-, feruloyl- and p-coumaroilquinic acids, with rapid appearance and clearance in plasma indicative of small intestinal absorption. These compounds amounted to 13.1% of the urinary metabolites. Delayed absorption of dihydrocaffeic, dihydroferulic and dihydrocoumaric acids and their phase II metabolites, in addition to feruloylglycine, pointed to their microbial origin and colonic absorption, accounting for 81.0% of excreted metabolites. Phase II flavonol metabolites (0.2%) derived mainly from rutin after colonic transformation and absorption were also detected. Additionally, dihydroferuloyl-, dihydrocaffeoyl- and dihydrocoumaroylquinic acids (5.7%) were identified, showing the most delayed kinetics. Total phenolic excretion (147.6 μmol) corresponded to 13.2% of ingested phenols. In conclusion, yerba mate polyphenols are partially bioavailable and extensively metabolized, mainly by the colonic microbiota., We also are grateful to the Spanish Ministry of Economy and Competitivity (MINECO-FEDER) for financial support (projects AGL2010-18269 and AGL2015-69986-R). S.M.-L. was a predoctoral fellow of the JAE Program (JAEPre097) co-funded by CSIC and the European Social Fund. M. G.-J. was a predoctoral FPI fellow (BES2008-007138) of the Spanish Ministry of Science and Innovation.

This work aimed at studying the effects of green coffee bean (GCBE) and yerba mate (YME) extracts, their main phenolic components (5-caffeoylquinic acid, 5-CQA; 3,5-dicaffeoylquinic acid, 3,5-DCQA) and metabolites (ferulic acid, FA; caffeic acid, CA; dihydrocaffeic acid, DHCA; and dihydroferulic acid, DHFA) along with caffeine (CAF) on the viability and proliferation of different human cell lines. Extracts (10–1000 μg/mL) and standards (10–1000 μM) were assayed in colon (Caco-2), lung (A549), oesophageal (OE-33), urinary bladder (T24) human carcinoma cells, and a non-cancer cell line (CCD-18Co). YME significantly reduced viability of cancer cells at all assayed concentrations, the higher doses also reducing cell proliferation. GCBE effects on cell viability were more effective at 100 and 1000 μg/mL, showing modest effects on cell proliferation. The highest doses of 5-CQA and 3,5-DCQA reduced cell viability and proliferation in all cell lines, whereas FA, DHCA and DHFA had lower and variable effects. Caffeine had no effect. Dietary-attainable concentrations (0.1, 1 and 10 μg/mL) of YME were tested for cytotoxicity and reactive oxygen species generation, showing no cytotoxic effect. Low concentrations of all tested compounds were non-cytotoxic to CCD-18Co cells. [Conclusion]: YME and to a lower degree GCBE, their phenolic components and metabolites may decrease cancer cell viability and proliferation., This work was funded by the Spanish Ministry of Economy and Competitivity (MINECO-FEDER), projects AGL2010-18269 and AGL2015-69986-R and by CSIC, project PIE-201670E061. M. A-B. thanks CSIC and European Social Funds for financing her JAEdoc contract in the period 2011–2014. S. W. thanks the China Scholarship Council for her PhD grant.

Saponins are secondary plant metabolites constituted by a triterpenoid aglycone with one or more sugar chains. There is increasing interest in saponins due to their potential health effects. Yerba mate is an important source of saponins in many South American diets. The aim of this study was to develop a one-step procedure to isolate saponins from yerba mate, followed by their characterization by liquid chromatography/tandem high-resolution mass spectrometry (LC-ESI–MS) and quantification by high performance liquid chromatography-diode array (HPLC-DAD). Methanol extraction proved to be a highly effective method to extract yerba mate saponins. LC/MSn analysis allowed identifying three free triterpenes and 16 saponins of which five were identified for the first time. HPLC-DAD results revealed that ursolic acid was the main free aglycone (1.557–1.807 mg/g vs. 0.229–0.294 mg/g oleanolic acid and 0.024–0.036 mg/g hydroxylated aglycone). Saponin contents varied from 4.4 to 5.5 mg/g in four commercial brands, being matesaponin D or J3a the most abundant., This work was funded by the Spanish Ministry of Economy and Competitivity (MINECO-FEDER), projects AGL2010-18269 and AGL2015-69986-R. G.B. was a FPI fellow (BES-2011-047476) funded by the Spanish Ministry of Science and Innovation and performed most experiments. S.M.-L. was a predoctoral fellow of the JAE Program (JAEPre097) co-funded by CSIC and the European Social Fund.

Coffee is one of the most consumed beverages in the world, due to its unique aroma and stimulant properties. Although its health effects are controversial, moderate intake seems to be beneficial. The present work deals with the characterization and quantification of polyphenols and methylxanthines in four Arabica green coffee beans from different geographical origins. The antioxidant activity was also evaluated. Forty-three polyphenols (cinnamic acid, cinnamoyl-amide, 5 cinammoyl-glycosides, and 36 cinnamate esters) were identified using LC-MS

Yerba mate is a beverage rich in bioactive compounds popular in South America. Polyphenols and methylxanthines were qualitatively and quantitatively analyzed in four commercial brands of yerba mate, as well as the antioxidant capacity of the beverages. Using LC/MS

Cocoa products present great health potential due to their high content of polyphenols, mainly of flavanols. However, the antioxidant, anti-inflammatory and other health effects of regularly consuming cocoa products seem to depend on the intake and health status of the consumer, etc. and need to be further clarified. A randomised, controlled, cross-over, free-living study was carried out in healthy (n 24) and moderately hypercholesterolaemic (>2000mg/l, n 20) subjects to assess the influence of regularly consuming (4 weeks) two servings (15g each) of a cocoa product rich in fibre (containing 33·9% of total dietary fibre (TDF) and 13·9mg/g of soluble polyphenols) in milk v. consuming only milk (control) on (1) serum lipid and lipoprotein profile, (2) serum malondialdehyde levels, carbonyl groups, ferric reducing/antioxidant power, oxygen radical absorbance capacity and free radical-scavenging capacity, (3) IL-1β, IL-6, TNF-α, IL-10, IL-8, monocyte chemoattractant protein-1, and vascular and intracellular cell adhesion molecule levels, and (4) systolic and diastolic blood pressure and heart rate. Throughout the study, the diet and physical activity of the volunteers, as well as any possible changes in weight or other anthropometric parameters, were also evaluated. The intake of TDF increased (P, Project Consolider-Ingenio (CSD 2007-00063) from the Spanish Ministry of Science and Innovation.

A series of alkyl nitrohydroxytyrosyl ether derivatives has been synthesized from free hydroxytyrosol (HT), the natural olive oil phenol, in order to increase the assortment of compounds with potential neuroprotective activity in Parkinson's disease. In this work, the antioxidant activity of these novel compounds has been evaluated using Ferric Reducing Antioxidant Power (FRAP), 2,2′-azinobis(3-ethylbenzothiazoline-6-sulfonic1 acid) diammonium salt (ABTS), and Oxygen Radical Scavenging Capacity (ORAC) assays compared to tothat that of of nitrohydroxytyrosol (NOHT)2 HT) and and free free HT. HT. New New compounds showed variable antioxidant activity depending on the alkyl side chain length; compounds with short chains (2-4 carbon atoms) maintained or even improved the antioxidant activity compared to NOHT2 and/or HT, whereas those with longer side chains (6-8 carbon atoms) showed lower activity than NOHT2 but higher than HT., This work was supported by Grant P09-AGR-5098 from Junta de Andalucía (Spain). E.G.

[Purpose]: Preventive health effects of coffee could have a widespread impact on public health. Green coffee has more phenols than roasted and thus is healthier, although with less acceptable organoleptic properties. Therefore, the effects of regularly consuming a green/roasted coffee blend (35/65) on the main components of metabolic syndrome (MetS) in humans were evaluated. [Methods]: A crossover, randomized, controlled study was performed in 25 normocholesterolaemic and 27 hypercholesterolaemic men and women, aged 18-45y with BMI 18-25kg/m2. Three servings/day of the blend, providing 510.6mg hydroxycinnamic acids and 121.2mg caffeine/day, were consumed versus a control drink, during 8 weeks each. Polyphenol and methylxanthine-rich foods were restricted along the study. At the beginning (baseline) and end of the control and coffee interventions, blood samples were collected and glucose, HDL-Cholesterol, triglycerides, insulin, leptin, plasminogen activator inhibitor-1 (PAI-1), resistin and visfatin were analysed; waist circumference, %body fat, blood pressure were measured and dietary records and physical activity questionnaires completed. [Results]: Systolic and diastolic blood pressure decreased (p=0.001 and p, Project AGL2010-18269 from the Spanish Ministry of Economy and Competitivity is acknowledged. S.M.-L. thanks the Spanish National Research Council for her predoctoral fellowship under the JAE-Pre programme funded by the European Social Fund.