Assessment of the neuroprotective effects of (-)-epigallocatechin-3-gallate on spinal cord ischemia-reperfusion injury in rats.

Objective: Paraplegia or paraparesis due to spinal cord ischemia is one of the complications following thoracoabdominal aortic surgery. Recent studies revealed the neuroprotective effects of (-)-epigallocatechin-3-gallate (EGCG) on a variety of neurological disorders. The purpose of this study was to determine the neuroprotective effects of EGCG following spinal cord ischemia-reperfusion injury (IRI).Design: The present study was conducted on four groups of rats each as follows: Sham-operated group (laparotomy alone); Control group (with IRI); EGCGI group (50-mg/kg, i.p., before IRI), and EGCGII group (50-mg/kg, i.p., after IRI). Neurological function evaluated with motor deficit index (MDI) test. Spinal cord samples were taken 48 h after IRI and studied for determination of malodialdehyde (MDA) level, histopathology, and immunohistochemistry of caspase-3, TNF-α, and iNOS.Setting: Mazandaran University of Medical Sciences, Sari, Iran.Results: The level of MDA was significantly decreased in EGCG-treated rats. Attenuated caspase-3, TNF-α, and iNOS expression could be significantly detected in the EGCG-treated rats. Also, EGCG reduced the extent of degeneration of the spinal cord neurons, in addition to a significant reduction of MDI.Conclusion: The results suggest that pre- and post-treatment with EGCG may be effective in protecting spinal cord from IRI.

Maltoheptaoside hydrolysis with chromatographic detection and starch hydrolysis with reducing sugar analysis: Comparison of assays allows assessment of the roles of direct α-amylase inhibition and starch complexation.

The aim was to determine inhibition of human α-amylase activity by (poly)phenols using maltoheptaoside as substrate with direct chromatographic product quantification, compared to hydrolysis of amylose and amylopectin estimated using 3,5-dinitrosalicylic acid. Acarbose exhibited similar IC50 values (50% inhibition) with maltoheptaoside, amylopectin or amylose as substrates (2.37 ± 0.11, 3.71 ± 0.12 and 2.08 ± 0.01 µM respectively). Epigallocatechin gallate, quercetagetin and punicalagin were weaker inhibitors of hydrolysis of maltoheptaoside (<50% inhibition) than amylose (IC50: epigallocatechin gallate = 20.41 ± 0.25 µM, quercetagetin = 30.15 ± 2.05 µM) or amylopectin. Interference using 3,5-dinitrosalicylic acid was in the order punicalagin > epigallocatechin gallate > quercetagetin, with minimal interference using maltoheptaoside as substrate. The main inhibition mechanism of epigallocatechin gallate and punicalagin was through complexation with starch, especially amylose, whereas only quercetagetin additionally binds to the α-amylase active site. Interference is minimised using maltoheptaoside as substrate with product detection by chromatography, potentially allowing assessment of direct enzyme inhibition by almost any compound.

White tea - A cost effective alternative to EGCG in fight against benzo(a)pyrene (BaP) induced lung toxicity in SD rats.

Tea is a natural resource of catechins and exhibits antioxidative and anticancer activities. This study was designed to elucidate the comparative efficacy of white tea and pure EGCG in containing benzo (a) pyrene (BaP)-induced pulmonary stress. Rats were treated with white tea extract (WT) (1%) and pure EGCG at a dose of 80µg/ml in drinking water on alternate days for 12 weeks (4 weeks prior, during and after BaP treatment). BaP(50 mg/kg b. wt) was administered to rats orally in olive oil twice a week for four weeks. The indices such as stress biomarkers (LPO, PCC & ROS), antioxidant enzymes (SOD, CAT, GSH, GST, GR, GPx) activities and lung histoarchitecture were assessed. BaP administration enhanced the levels of inflammatory markers (NO and citrulline) and reduced activities of antioxidant enzymes. We observed similar antioxidant efficacy by both WT and EGCG as seen by their ameliorative action in restoring BaP induced oxidative and inflammatory stress as well as lung histoarchitecture. Our findings suggest that WT is equally beneficial as EGCG in maintaining the integrity of alveoli and is a potential candidate to be used as a cost effective and protective agent in conditions of BaP-induced lung damage.

Efficacy of sinecatechins 10% as proactive sequential therapy of external genital warts after laser CO2 ablative therapy: The PACT study (post-ablation immunomodulator treatment of condylomata with sinecatechins): a randomized, masked outcome assessment, multicenter trial.

External genital warts (EGW) are the most common viral sexually transmitted infection. Ablative treatments like cryotherapy, curettage, and CO2 laser therapies offer rapid onset of effect, fast clearance, and reduction of virus load. However, these procedures are associated with high recurrence rates (RRs) ranging from 20% to 77% in the short and medium terms and do not provide sustained clearance. After laser therapy removal of EGW, an RR up to 77% has been reported. Topical sinecatechins (TS) 10% is a patient-applied regimen for the treatment of EGW with a low RR (<6.5%) at three months after completion of the therapy in the pivotal trials conducted so far. Sinecatechins can be considered a suitable proactive sequential therapy (PST) after ablative strategies to obtain a low RR. So far, no prospective data are available regarding the efficacy of sinecatechins 10% as PST. We evaluated the efficacy and tolerability of TS 10% ointment applied twice daily in subjects with "difficult to treat" EGW after CO2 laser ablative treatment in a prospective controlled trial. A total of 87 subjects (76 men and 11 women; mean age 42 years) were enrolled in this three-month masked outcome assessment parallel group trial with imbalanced randomization allocation (2:1). One week after a successful CO2 laser treatment, 60 subjects were randomized to TS 10% treatment and 27 subjects to no treatment (control group: ConTRol (CTR); no sequential therapy). All patients had a history of an average of 4.5 previous ablative treatments in the last 12 months due to recurrent EGW. Mean (standard deviation) baseline number of treated lesions was 6.5 (2.7). One subject in the TS arm dropped out due to burning sensation after the application of the product. Therefore, 86 subjects completed the study. After three months, in the TS group, three subjects presented new EGW lesions (RR: 5%) on treated sites. In the CTR group, eight subjects presented new EGW lesions (RR: 29%) on treated sites (p = 0.0024; odds ratio: 0.16; 95% confidence interval: 0.04-0.68). In the TS group, 34 subjects (56%) reported mild to moderate erythema or burning sensation at the application site. In this prospective multicenter trial, the use of TS 10% as PST after ablative treatment with CO2 laser was associated with a lower recurrence rate of new EGW lesions in the short term in comparison with the control group. Comparative larger trials are warranted to evaluate the role of this approach as PST (Trial Registration Number: ISRCTN44037479).

Epigallocatechin-3 Gallate Inhibits STAT-1/JAK2/IRF-1/HLA-DR/HLA-B and Reduces CD8 MKG2D Lymphocytes of Alopecia Areata Patients.

BACKGROUND: Alopecia areata (AA) is associated with Interferon- γ (IFN-γ) mediated T-lymphocyte dysfunction and increased circulating Interleukine-17 (IL-17) levels. Epigallocatechin-3-gallate (EGCG) specifically inhibits IFN-γ pathways and unlike Janus Kinase 1 and 2 (JAK1/JAK2) inhibitors (tofacitinib, ruxolitinib), EGCG is safer, more cost-effective, and is a topically active agent. Our objective is to test the mode of action of EGCG in vitro and ex vivo using HaCat, Jurkat cell lines, and peripheral blood mononuclear cells (PBMCs) of AA patients and healthy controls (HCs), respectively. METHODS: distribution of T helper cells (Th1, Th17), and cytotoxic cells (CD8) in PBMCs isolated from 30 AA patients and 30 HCs was investigated by flowcytomterty. In vitro treatment of HaCat and Jurkat cells with 40 µm EGCG for 48 h was performed to measure the level of phosphorylation of signal transducer and activator of transcription protein STAT1, and replicated in ex vivo model using PBMCs of AA patients. RESULTS: Interestingly, 40 µm EGCG is capable of completely inhibiting phosphorylation of STAT1 after 48 h in HaCat and Jurkat cells and ex vivo in PBMCs of AA patients. Based on QPCR data, the action of EGCG on p-STAT1 seems to be mediated via downregulation of the expression of JAK2 but not JAK1 leading to the inhibition of human leukocyte antigens (HLA-DR and HLA-B) expression probably via IRF-1. On the other hand, AA patients have significantly increased levels of Th1, Th17, and CD8 cells and the production of IFN-γ and IL-17 by PBMCs in AA patients was significantly higher compared to HC; p = 0.008 and p = 0.006, respectively. Total numbers of CD8+ cells were not significantly different between treated and untreated samples. However, CD8+ cells with positive Natural killer group 2 member D (NKG2D) transmembrane receptor (CD8+ NKG2D+ subset) was significantly reduced when PBMCs were treated with 20 µm EGCG for 48 h. CONCLUSION: These results suggest that EGCG has a synergistic action that inhibits expression of HLA-DR and HLA-B molecules via the IFN-γ pathway to maintain immune privilege in HF; also it reduces CD8+ NKG2D+ subset.

Effects of (-)-Epigallocatechin Gallate (EGCG) on Energy Expenditure and Microglia-Mediated Hypothalamic Inflammation in Mice Fed a High-Fat Diet.

Obesity is an escalating global epidemic caused by an imbalance between energy intake and expenditure. (-)-Epigallocatechin-3-gallate (EGCG), the major polyphenol in green tea, has been reported to be conducive to preventing obesity and alleviating obesity-related chronic diseases. However, the role of EGCG in energy metabolism disorders and central nervous system dysfunction induced by a high-fat diet (HFD) remains to be elucidated. The aim of this study was to evaluate the effects of EGCG on brown adipose tissue (BAT) thermogenesis and neuroinflammation in HFD-induced obese C57BL/6J mice. Mice were randomly divided into four groups with different diets: normal chow diet (NCD), normal chow diet supplemented with 1% EGCG (NCD + EGCG), high-fat diet (HFD), and high-fat diet supplemented with 1% EGCG (HFD + EGCG). Investigations based on a four-week experiment were carried out including the BAT activity, energy consumption, mRNA expression of major inflammatory cytokines in the hypothalamus, nuclear factor-kappa B (NF-κB) and signal transducer and activator of transcription 3 (STAT3) phosphorylation, and immunofluorescence staining of microglial marker Iba1 in hypothalamic arcuate nucleus (ARC). Experimental results demonstrated that dietary supplementation of EGCG significantly inhibited HFD-induced obesity by enhancing BAT thermogenesis, and attenuated the hypothalamic inflammation and microglia overactivation by regulating the NF-κB and STAT3 signaling pathways.

Safety assessment of green tea based beverages and dried green tea extracts as nutritional supplements.

The safety of green tea infusions and green tea extract (GTE)-based products is reviewed regarding catechins. Epigallocatechin 3-gallate (EGCG), the major catechin present in green tea, is suspected of being responsible for liver toxicity reported in humans consuming food supplements. Intake of EGCG with green tea infusions and GTE-based beverages is up to about 450mg EGCG/person/day in Europe and higher in Asia. Consumption of green tea is not associated with liver damage in humans, and green tea infusion and GTE-based beverages are considered safe in the range of historical uses. In animal studies, EGCG's potency for liver effects is highly dependent on conditions of administration. Use of NOAELs from bolus administration to derive a tolerable upper intake level applying the margin of safety concept results in acceptable EGCG-doses lower than those from one cup of green tea. NOAELs from toxicity studies applying EGCG with diet/split of the daily dose are a better point of departure for risk characterization. In clinical intervention studies, liver effects were not observed after intakes below 600mg EGCG/person/day. Thus, a tolerable upper intake level of 300mg EGCG/person/day is proposed for food supplements; this gives a twofold safety margin to clinical studies that did not report liver effects and a margin of safety of 100 to the NOAELs in animal studies with dietary administration of green tea catechins.

A minireview of effects of green tea on energy expenditure.

In recent years, individuals have begun to tend more frequently to some natural and herbal products to be used alone or as a combination with diet and exercise for ensuring the weight loss. Green tea is the leading one of these products. In some studies, it is reported that the green tea causes an increase in thermogenesis and substrate with fat oxidation by affecting on the sympathetic nervous system. It is reported that green tea has two main components that are associated with energy expenditure. One of them is caffeine and the other is catechin content. Each of these two components has an impact on energy mechanism separately. In this minireview article, mechanisms of action and effects of caffeine and catechin, which are found in green tea composition, on energy expenditure are assessed.

Physiological effects of epigallocatechin-3-gallate (EGCG) on energy expenditure for prospective fat oxidation in humans: A systematic review and meta-analysis.

Green tea catechins (GTCs) are known to improve fat oxidation (FOX) during fasted, rested and exercise conditions wherein epigallocatechin-3-gallate (EGCG) is thought to be the most pharmacologically active and has been studied extensively. From the available data of randomized controlled trials (RCTs) on EGCG, we carried out a systematic review and meta-analysis to elucidate whether EGCG consumption indeed increase energy expenditure (EE) and promote FOX. A systematic review of the literature was conducted using electronic databases (PubMed, Embase, Cochrane Library, CINAHL, JICST, JSTPLUS, and JMEDPLUS and others) and eight RCTs were included. RCTs were reviewed using Preferred Reporting Items for Systematic Reviews and Meta-Analyses guidelines and methodological quality was assessed. After data extraction, results were aggregated using fixed- and random-effect approaches and expressed to quantify the relationship between the dose of EGCG for respiratory quotient (RQ), EE and rate of FOX to compare the EGCG and placebo treatments. The meta-analysis results of verities of studies in terms of dose and length of duration revealed that EGCG supplementation provided significant mean difference (MD) when compared with placebo for RQ [MD: -0.02; 95% confidence intervals (95% CI), -0.04 to 0.00; I2=67%; P=.01] and EE [MD: 158.05 kJ/day; 95% CI, 4.72 to 311.38; I2=0%; P=.04] in fixed-effect approach. Changes in FOX did not reach the level of statistical significance. Meta-analyses of EGCG influence on the body mass index, waist circumference and total body fat mass (TBFM) were also examined and their impact on the promotion of FOX is reported. Effect of EGCG doses was also systematically reviewed. Finding showed that EGCG intake moderately accelerates EE and reduces RQ. The analyses revealed that the EGCG resulted in difference in RQ and EE but the effect on the other measures of energy metabolism was relatively mild. Possibly, EGCG alone has the potential to increase metabolic rate at 300 mg dose. Collectively, the outcome supports the findings that EGCG has an effect on metabolic parameters. However, the large prospective trials are needed to confirm the findings.

Correlation of In Vivo and In Vitro Assay Results for Assessment of Free Radical Scavenging Activity of Green Tea Nutraceuticals.

Green tea (GT)-derived catechins; epigallocatechin gallate (EGCG) in particular are commonly used nutraceuticals for their free-radical scavenging activity (FRSA). The influence of photodegradation on the protective power of GT nutracenticals against oxidative stress was thoroughly explored. Photodegradation of GT extracts was carried out and monitored using orthogonal stability-indicating testing protocol; in vitro and in vivo assays. Total polyphenol content (TPC) and FRSA were determined spectrophotometrically while EGCG was selectively monitored using SPE-HPLC. In vivo assessment of photodegraded samples was investigated via measuring a number of biomarkers for hepatic oxidative stress and apoptosis (caspase-3, inducible nitric oxide synthase, nitric oxide, mitogen-activated protein kinase, glutathione, thiobarbituric acid reactive substances, nuclear factor kappa beta, and nuclear factor erythroid 2-related factor) as well as liver damage (alanine transaminase and aspartate transaminase) in serum of rats previously subjected to oxidative stress. Results showed complete degradation of EGCG in photodegraded green tea samples with no correlation with either TPC or FRSA. On the other hand, in vivo assay results revealed not only loss of activity but formation of harmful pro-oxidants. Photostability was found crucial for the protective effect of GT extract against lead acetate insult. Results confirmed that careful design of quality control protocols requires correlation of chemical assays to bioassays to verify efficacy, stability, and most importantly safety of nutraceuticals.

Assessment of the activity of directly acting antivirals and other products against different genotypes of hepatitis C virus prevalent in resource-poor countries.

Certain food additives and drugs used for other indications have been shown to inhibit in vitro replication of HCV and have been proposed as cheap options for the treatment of HCV infections in resource-poor countries. We here report that the in vitro anti-HCV (genotypes 1a, 1b, 2a and 4b) activity of nitazoxanide, silymarin, silibinin and the green tea extract EGCG is very weak when compared to directly acting antivirals. HCV-infected patients in resource-poor countries should receive the best possible treatment (if possible via expanded access programs); it is therefore advisable not to plan clinical studies with drugs/compounds with weak anti-HCV activity.

Antioxidant supplementation can reduce the survival costs of excess amino acid intake in honeybees.

Over-consuming amino acids is associated with reduced survival in many species, including honeybees. The mechanisms responsible for this are unclear but one possibility is that excessive intake of amino acids increases oxidative damage. If this is the case, antioxidant supplementation may help reduce the survival costs of high amino acid intake. We tested this hypothesis in African honeybees (Apis mellifera scutellata) using the major antioxidant in green tea, epigallocatechin-3-gallate (EGCG). We first determined the dose-range of EGCG that improved survival of caged honeybees fed sucrose solution. We then provided bees with eight diets that differed in their ratio of essential amino acids (EAA) to carbohydrate (C) (0:1, 1:250, 1:100, 1:75, 1:50, 1:25, 1:10, 1:5 EAA:C) and also in their EGCG dose (0.0 or 0.4 mM). We found that bees fed sucrose only solution survived better than bees fed EAA diets. Despite this, bees preferred a diet that contained intermediate ratios of EAA:C (ca. 1:25), which may represent the high demands for nitrogen of developing nurse bees. EGCG supplementation improved honeybee survival but only at an intermediate dose (0.3-0.5 mM) and in bees fed low EAA diets (1:250, 1:100 EAA:C). That EGCG counteracted the lifespan reducing effects of eating low EAA diets suggests that oxidative damage may be involved in the association between EAAs and lifespan in honeybees. However, that EGCG had no effect on survival in bees fed high EAA diets suggests that there are other physiological costs of over-consuming EAAs in honeybees.

Assessment of extraction parameters on antioxidant capacity, polyphenol content, epigallocatechin gallate (EGCG), epicatechin gallate (ECG) and iriflophenone 3-C-ß-glucoside of agarwood (Aquilaria crassna) young leaves.

The effects of ethanol concentration (0%-100%, v/v), solid-to-solvent ratio (1:10-1:60, w/v) and extraction time (30-180 min) on the extraction of polyphenols from agarwood (Aquilaria crassna) were examined. Total phenolic content (TPC), total flavonoid content (TFC) and total flavanol (TF) assays and HPLC-DAD were used for the determination and quantification of polyphenols, flavanol gallates (epigallocatechin gallate--EGCG and epicatechin gallate--ECG) and a benzophenone (iriflophenone 3-C-ß-glucoside) from the crude polyphenol extract (CPE) of A. crassna. 2,2'-Diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity was used to evaluate the antioxidant capacity of the CPE. Experimental results concluded that ethanol concentration and solid-to-solvent ratio had significant effects (p<0.05) on the yields of polyphenol and antioxidant capacity. Extraction time had an insignificant influence on the recovery of EGCG, ECG and iriflophenone 3-C-ß-glucoside, as well as radical scavenging capacity from the CPE. The extraction parameters that exhibited maximum yields were 40% (v/v) ethanol, 1:60 (w/v) for 30 min where the TPC, TFC, TF, DPPH, EGCG, ECG and iriflophenone 3-C-ß-glucoside levels achieved were 183.5 mg GAE/g DW, 249.0 mg QE/g DW, 4.9 mg CE/g DW, 93.7%, 29.1 mg EGCG/g DW, 44.3 mg ECG/g DW and 39.9 mg iriflophenone 3-C-ß-glucoside/g DW respectively. The IC50 of the CPE was 24.6 mg/L.

[Assessment of inner filter effect corrections in fluorimetry of the interaction between polyphenols and proteins].

Using persimmon tannin fraction (PT40), epicatechin-3-gallate-(4beta-->8, 2beta-->O-->7)-epicatechin-3-gallate (A-type ECG dimer) and epigallocatechin-3-gallate (EGCG) as representatives of polyphenols and Chinese cobra snake venom phospholipase A2 (PLA2) as a model protein, different mathematical equations were compared to correct the inner filter effects produced by the fluorescence quenching of those polyphenols to PLA2 based on the gradient, linearity and intercept of Stern-Volmer regression equation. The results revealed that correction by the equation developed by Gauthier et al made a significant reduction in gradients. Besides, the linearity was clearly improved and the intercepts were closer to 1 after correction in all cases. The binding constant of PT40 and PLA2 declined by 60% and the inferred interaction forces were more convinced after correction by the above equation. Therefore, the equation developed by Gauthier et al was the most appropriate equation for correcting the inner filter effects when studying the interaction of polyphenols and protein using fluorescence quenching method.

6-methoxyflavanones as bitter taste receptor blockers for hTAS2R39.

Many (dietary) bitter compounds, e.g. flavonoids, activate bitter receptor hTAS2R39 in cell-based assays. Several flavonoids, amongst which some flavanones, are known not to activate this receptor. As certain flavanones are known to mask bitter taste sensorially, flavanones might act as bitter receptor antagonists. Fourteen flavanones were investigated for their potential to reduce activation of hTAS2R39 by epicatechin gallate (ECG), one of the main bitter compounds occurring in green tea. Three flavanones showed inhibitory behavior towards the activation of hTAS2R39 by ECG: 4'-fluoro-6-methoxyflavanone, 6,3'-dimethoxyflavanone, and 6-methoxyflavanone (in order of decreasing potency). The 6-methoxyflavanones also inhibited activation of hTAS2R14 (another bitter receptor activated by ECG), though to a lesser extent. Dose-response curves of ECG at various concentrations of the full antagonist 4'-fluoro-6-methoxyflavanone and wash-out experiments indicated reversible insurmountable antagonism. The same effect was observed for the structurally different agonist denatonium benzoate.

Reduction of microbiological risk in minced meat by a combination of natural antimicrobials.

BACKGROUND: Responsibility for food safety must be taken through the entire food-production chain, to avoid consumer cross-contamination. The antimicrobial activities of an Alpinia katsumadai seed extract and epigallocatechin gallate (EGCG), and their combination, were evaluated against individual food-borne pathogenic strains of Listeria monocytogenes, Escherichia coli and Campylobacter jejuni, individually and as a cocktail, in chicken-meat juice and sterile minced meat as food models, and in minced meat with the naturally present microflora, as an actual food sample. RESULTS: The antimicrobial combination of the A. katsumadai extract and EGCG was the most efficient for C. jejuni growth inhibition, followed by inhibition of L. monocytogenes, which was reduced more efficiently in the bacterial cocktail than as an individual strain. The antimicrobial combination added to minced meat at refrigeration temperatures used in the food chain (8 °C) revealed inhibition of these pathogens and inhibition of the naturally present bacteria after 5 days. CONCLUSIONS: The antibacterial efficiencies of the tested combinations are influenced by storage temperature. Food safety can be improved by using the appropriate combination of natural antimicrobials to reduce the microbiological risk of minced meat.

Short-term supplementation with a specific combination of dietary polyphenols increases energy expenditure and alters substrate metabolism in overweight subjects.

BACKGROUND AND OBJECTIVES: Impaired regulation of lipid oxidation (metabolic inflexibility) is associated with obesity and type 2 diabetes mellitus. Recent evidence has indicated that dietary polyphenols may modulate mitochondrial function, substrate metabolism and energy expenditure in humans. The present study investigated the effects of short-term supplementation of two combinations of polyphenols on energy expenditure (EE) and substrate metabolism in overweight subjects. SUBJECTS AND METHODS: Eighteen healthy overweight volunteers (9 women, 9 men; age 35±2.5 years; body mass index 28.9±0.4 kg m(-2)) participated in a randomized, double-blind cross-over trial. Combinations of epigallocatechin-gallate (E, 282 mg day(-1))+resveratrol (R, 200 mg day(-1)) and E+R+80 mg day(-1) soy isoflavones (S) or placebo capsules (PLA) were supplemented twice daily for a period of 3 days. On day 3, circulating metabolite concentrations, EE and substrate oxidation (using indirect calorimetry) were measured during fasting and postprandial conditions for 6 h (high-fat-mixed meal (2.6 MJ, 61.2 E% fat)). RESULTS: Short-term supplementation of E+R increased resting EE (E+R vs PLA: 5.45±0.24 vs 5.23±0.25 kJ min(-1), P=0.039), whereas both E+R (699±18 kJ 120 min(-1) vs 676±20 kJ 120 min(-1), P=0.028) and E+R+S (704±18 kJ 120 min(-1) vs 676±20 kJ 120 min(-1), P=0.014) increased 2-4 h-postprandial EE compared with PLA. Metabolic flexibility, calculated as the postprandial increase to the highest respiratory quotient achieved, tended to be improved by E+R compared with PLA and E+R+S only in men (E+R vs PLA: 0.11±0.02 vs 0.06±0.02, P=0.059; E+R+S: 0.03±0.02, P=0.009). E+R+S significantly increased fasting plasma free fatty acid (P=0.064) and glycerol (P=0.021) concentrations compared with PLA. CONCLUSIONS: We demonstrated for the first time that combined E+R supplementation for 3 days significantly increased fasting and postprandial EE, which was accompanied by improved metabolic flexibility in men but not in women. Addition of soy isoflavones partially reversed these effects possibly due to their higher lipolytic potential. The present findings may imply that long-term supplementation of these dosages of epigallocatechin-gallate combined with resveratrol may improve metabolic health and body weight regulation.

Acute effect on satiety, resting energy expenditure, respiratory quotient, glucagon-like peptide-1, free fatty acids, and glycerol following consumption of a combination of bioactive food ingredients in overweight subjects.

OBJECTIVE: A combination of bioactive food ingredients (capsaicinoids, epigallocatechin gallate, piperin, and l-carnitine, CBFI) may promote satiety and thermogenesis. The study was conducted in order to assess whether there is any effect on satiety, resting energy expenditure (REE), respiratory quotient, glucagon-like peptide-1 (GLP-1), free fatty acids (FFA) and glycerol release, following a standardized mixed meal with or without single consumption of a CBFI. DESIGN: An 8-week randomized double-blind placebo-controlled trial. SETTING: Dietetic and Metabolic Unit, Azienda di Servizi alla Persona, University of Pavia and "Villa delle Querce" Clinical Rehabilitation Institute, Rome, Italy. PARTICIPANTS: Thirty-seven overweight adults (body mass index [BMI]: 25-35). INTERVENTION: Nineteen overweight subjects were included in the supplemented group (14 women, 5 men; age 46.4 ± 6.4; BMI: 30.5 ± 3.3) and 18 in the placebo group (13 women, 5 men; age 40.8 ± 11.5; BMI: 30.1 ± 2.6). Satiety was assessed using 100-mm visual analogue scales (VAS) and the area under the curve was calculated. RESULTS: All measured parameters increased significantly in comparison with baseline in response to meal, both with CBFI and with placebo. However, throughout the study day, the supplemented group experienced a significantly greater increase than the placebo group in their sensation of satiety following acute administration of the supplement. CONCLUSION: CBFI may therefore be of great value in the treatment of overweight patients by increasing satiety and stimulating thermogenesis.

Activation of the hTAS2R14 human bitter-taste receptor by (-)-epigallocatechin gallate and (-)-epicatechin gallate.

Tea catechins have strong bitterness and influence the taste of tea. Among the 25 human bitter-taste receptors (TAS2Rs), we found that hTAS2R14 responded to catechins, in addition to hTAS2R39, a known catechin receptor. Although hTAS2R14 responded to (-)-epicatechin gallate and (-)-epigallocatechin gallate, it did not respond to (-)-epicatechin and (-)-epigallocatechin.