Component Of Green Tea Research Articles

EGCG induces β-defensin 3 against influenza A virus H1N1 by the MAPK signaling pathway.

Epigallocatechin gallate (EGCG) is the main component of green tea, which has been proven to inhibit a variety of viruses, including influenza A virus. However, the mechanism of EGCG against influenza virus remains to be further explored. The mechanism of EGCG against influenza virus was studied. The results showed that EGCG significantly increased the levels of HBD3 mRNA and protein, while the levels of phosphorylation of (p)-p38 MAPK, ERK and JNK after EGCG treatment were significantly up-regulated. p38 MAPK, ERK and JNK inhibitors significantly inhibited the expression of HBD3 induced by EGCG. On the other hand, EGCG significantly inhibited the expression of HA and NP proteins in influenza A virus H1N1, but attenuated the anti-influenza A virus effect of EGCG after silencing HBD3. Thus, the anti-influenza virus effect of EGCG is related to the induction of HBD3 expression. In addition, the expression of EGCG-induced HBD3 is related to the p38 MAPK, ERK and JNK signaling pathways. The research data show that EGCG can induce HBD3 expression through p38 MAPK, ERK and JNK signaling pathway to inhibit the replication of influenza A virus H1N1, providing a new and effective candidate drug for influenza virus.

The green tea polyphenol epigallocatechin-3-gallate attenuates age-associated muscle loss via regulation of miR-486-5p and myostatin

(−)-Epigallocatechin-3-gallate (EGCG), the most abundant catechin component in green tea, has been reported to attenuate age-associated insulin resistance, lipogenesis and loss of muscle mass through restoring Akt activity in skeletal muscle in our previous and present studies. Accumulated data has suggested that polyphenols regulate signaling pathways involved in aging process such as inflammation and oxidative stress via modulation of miRNA expression. Here we found that miRNA-486-5p was significantly decreased in both aged senescence accelerated mouse-prone 8 (SAMP8) mice and late passage C2C12 cells. Thus, we further investigated the regulatory effect of EGCG on miRNA-486-5p expression in age-regulated muscle loss. SAMP8 mice were fed with chow diet containing without or with 0.32% EGCG from aged 32 weeks for 8 weeks. Early passage (<12 passages) and late passage (>30 passages) of C2C12 cells were treated without or with EGCG at concentrations of 50 μM for 24h. Our data showed that EGCG supplementation increased miRNA-486-5p expression in both aged SAMP8 mice and late passage C2C12 cells. EGCG stimulated AKT phosphorylation and inhibited FoxO1a-mediated MuRF1 and Atrogin-1 transcription via up-regulating the expression of miR-486 in skeletal muscle of 40-wk-old SAMP8 mice as well as late passage C2C12 cells. In addition, myostatin expression was increased in late passage C2C12 cells and anti-myostatin treatment upregulated the expression of miR-486-5p. Our results identify a unique mechanism of a dietary constituent of green tea and suggest that use of EGCG or compounds derived from it attenuates age-associated muscle loss via myostatin/miRNAs/ubiquitin-proteasome signaling.

Activation of Myosin Phosphatase by Epigallocatechin-Gallate Sensitizes THP-1 Leukemic Cells to Daunorubicin.

The Myosin Phosphatase (MP) holoenzyme is composed of a Protein Phosphatase type 1 (PP1) catalytic subunit and a regulatory subunit termed Myosin Phosphatase Target subunit 1 (MYPT1). Besides dephosphorylation of myosin, MP has been implicated in the control of cell proliferation via dephosphorylation and activation of the tumor suppressor gene products, retinoblastoma protein (pRb) and merlin. Inhibition of MP was shown to attenuate the drug-induced cell death of leukemic cells by chemotherapeutic agents, while activation of MP might have a sensitizing effect. Recently, Epigallocatechin-Gallate (EGCG), a major component of green tea, was shown to activate MP by inducing the dephosphorylation of MYPT1 at phospho-Thr696 (MYPT1pT696), which might confer enhanced chemosensitivity to cancer cells. THP-1 leukemic cells were treated with EGCG and Daunorubicin (DNR) and cell viability was analyzed. Phosphorylation of tumor suppressor proteins was detected by Western blotting. EGCG or DNR (at sub-lethal doses) alone had moderate effects on cell viability, while the combined treatment caused a significant decrease in the number of viable cells by enhancing apoptosis and decreasing proliferation. EGCG plus DNR decreased the phosphorylation level of MYPT1pT696, which was accompanied by prominent dephosphorylation of pRb. In addition, significant dephosphorylation of merlin was observed when EGCG and DNR were applied together. Our results suggest that EGCG-induced activation of MP might have a regulatory function in mediating the chemosensitivity of leukemic cells via dephosphorylation of tumor suppressor proteins.

The effect of L-theanine and S-ketamine on d-serine cellular uptake

Decreased extracellular level of d-Serine (D-Ser), a co-agonist of the N-methyl-d-aspartate (NMDA) receptors was connected to receptor hypofunction in the brain and the related deficit of cognitive functions. Extracellular D-Ser concentration is modulated by ASCT neutral amino acid transporters. L-Theanine (L-Tea), a neutral amino acid component of green tea was reported to improve cognitive functions.We thus intended to investigate the possible inhibitory effect of L-Tea on the D-Ser uptake of SH-SY5Y neuroblastoma cells, which was previously found as a good model of D-Ser transport into astrocytes.Cells were incubated with D-Ser and various concentrations of L-Tea or the reference compound S-ketamine (S-Ket). The effect on the uptake was assessed by measuring the intracellular D-Ser concentration using a capillary electrophoresis – laser induced fluorescence detection method.L-Tea competitively inhibited D-Ser uptake into SH-SY5Y cells with an IC50 value of 9.68 mM. Having previously described as an inhibitor of ASCT-2 transporter, S-Ket was intended to be used as a positive control. However, no acute inhibition of D-Ser transport by S-Ket was observed. Its long-term effect on the transport was also examined. No significant difference in D-Ser uptake in control and S-Ket-treated cells was found after 72 h treatment, although the intracellular D-Ser content of the 50 μM S-Ket pre-treated cells was significantly higher.L-Tea was found to be a weak competitive inhibitor of the ASCT transporters, while S-Ket did not directly affect D-Ser uptake or modify the uptake kinetics after a long-term incubation period.

Epigallocatechin-3-Gallate (EGCG)-Inducible SMILE Inhibits STAT3-Mediated Hepcidin Gene Expression.

Hepatic peptide hormone hepcidin, a key regulator of iron metabolism, is induced by inflammatory cytokine interleukin-6 (IL-6) in the pathogenesis of anemia of inflammation or microbial infections. Small heterodimer partner-interacting leucine zipper protein (SMILE)/CREBZF is a transcriptional corepressor of nuclear receptors that control hepatic glucose and lipid metabolism. Here, we examined the role of SMILE in regulating iron metabolism by inflammatory signals. Overexpression of SMILE significantly decreased activation of the Janus kinase 2-signal transducer and activator of transcription 3 (STAT3)-mediated hepcidin production and secretion that is triggered by the IL-6 signal in human and mouse hepatocytes. Moreover, SMILE co-localized and physically interacted with STAT3 in the nucleus in the presence of IL-6, which significantly suppressed binding of STAT3 to the hepcidin gene promoter. Interestingly, epigallocatechin-3-gallate (EGCG), a major component of green tea, induced SMILE expression through forkhead box protein O1 (FoxO1), as demonstrated in FoxO1 knockout primary hepatocytes. In addition, EGCG inhibited IL-6-induced hepcidin expression, which was reversed by SMILE knockdown. Finally, EGCG significantly suppressed lipopolysaccharide-induced hepcidin secretion and hypoferremia through induction of SMILE expression in mice. These results reveal a previously unrecognized role of EGCG-inducible SMILE in the IL-6-dependent transcriptional regulation of iron metabolism.

Quality assessment of instant green tea using portable NIR spectrometer.

Caffeine and catechin are two main components of instant green tea, and are essential components of tea quality. This paper mainly focuses on the feasibility of rapidly determining instant green tea components by using a portable near infrared (NIR) spectrometer. The two main components (caffeine and catechin) were studied. In addition, the instrument performance levels of portable and benchtop NIR spectrometers were studied and compared. Quantitative models developed using portable and benchtop spectrometers for measuring caffeine, total catechins, and four individual catechins were established and compared. After preprocessing using standard normal variate (SNV), the Rp values of the caffeine, total catechins, (-)-epigallocatechin, (-)-epigallocatechin 3-gallate, (-)-epicatechin, and (-)-epicatechin gallate in the partial least squares models for a portable NIR spectrometer were 0.974, 0.962, 0.669, 0.945, 0.942 and 0.905, respectively. For a benchtop NIR spectrometer, Rp values were 0.993, 0.958, 0.883, 0.955, 0.966 and 0.936, respectively. Passing-Bablok regression method results indicated no significant differences between the two instruments. A genetic algorithm (GA) and the successive projections algorithm (SPA) were used to screen the wavelength of the NIR spectrum and establish the model. The GA obtained more robust modeling results. This study concludes that the developed portable spectroscopy system combined with appropriate variable selection methods can be effectively used for rapid determination of caffeine, total catechins, and four individual catechins in instant green tea.

Simultaneous quantification of active constituents and antioxidant capability of green tea using NIR spectroscopy coupled with swarm intelligence algorithm

A simple, rapid and low-cost analytical method was employed for simultaneous determination of bioactive constituents and antioxidant capability of green tea. The strategy was based on swarm intelligence algorithms with partial least squares (PLS) such as simulated annealing PLS (SA-PLS), ant colony optimization PLS (ACO-PLS), genetic algorithm PLS (GA-PLS), and synergy interval PLS (Si-PLS) coupled with Near-infrared (NIR) spectroscopy. These algorithms were independently applied to select informative spectral variables and improve the prediction of green tea components. Results showed that NIR combined with SA-PLS and Si-PLS had a strong correlation coefficient with the wet-chemical methods for predicting epigallocatechin gallate (Rp2 = 0.97); epigallocatechin (Rp2 = 0.97); epicatechin gallate (Rp2 = 0.96); epicatechin (Rp2 = 0.91); catechin (Rp2 = 0.98); caffeine (Rp2 = 0.96); theanine (Rp2 = 0.93); and antioxidant capability (Rp2 = 0.80) in green tea. Our results revealed the potential utilization of NIR spectroscopy coupled with SA-PLS and Si-PLS algorithms as an effective and robust technique to simultaneously predict active constituents and antioxidant capability of green tea.

SG-SP1 suppresses mast cell-mediated allergic inflammation via inhibition of FcɛRI signaling

Abstract As the number of allergic disease cases increases, studies to identify new treatments take on new urgency. In previous study, gallic acid (GA), a part of EGCG, a major component of green tea, has shown anti-allergic inflammatory effect. However, GA has low metabolic stability and structure-activity relationship. Therefore, we designed SG-SP1 based on GA. We aimed to assess the effects of SG-SP1 on mast cell-mediated allergic inflammation using various animal and in vitro models. For in vitro experiments, IgE-mediated various mast cells (RBL-2H3 and primary cultured peritoneal and bone marrow-derived mast cells) were used to determine the role of SG-SP1 (0.1–1 nM). Immunoglobulin (Ig) E-induced passive cutaneous anaphylaxis and Ovalbumin-induced systemic anaphylaxis are standard animal models for immediate-type hypersensitivity. For in vitro, SG-SP1 reduced degranulation of mast cells by down-regulating intracellular calcium levels in a concentration-dependent manner. In addition, SG-SP1 decreased expression and secretion of inflammatory cytokines in activated mast cells. This suppressive effect was associated to inhibition of the phosphorylation of Lyn, Syk and Akt, and the nuclear translocation of nuclear factor-κB. Due to the strong inhibitory effect of SG-SP1 on Lyn, the known upstream signaling of FcɛRI-dependent pathway, we confirmed the direct binding of SG-SP1 to FcɛRI, a high affinity IgE receptor by surface plasmon resonance experiment. We determined that SG-SP1 directly interacts with FcɛRI and propose SG-SP1 as a therapeutic candidate for mast cell-mediated allergic inflammatory disorders via inhibition of FcɛRI signaling.

L-Theanine attenuates neointimal hyperplasia via suppression of vascular smooth muscle cell phenotypic modulation

Neointimal hyperplasia is a prominent pathological phenomenon in the process of stent restenosis. Abnormal proliferation and migration of vascular smooth muscle cells (VSMCs) play major pathological processes involved in the development of restenosis. l-Theanine, one of the major amino acid components in green tea, has been reported to improve vascular function. Here we display the effects of l-theanine on neointima formation and the underlying mechanism. In the rat carotid-artery balloon-injury model, l-theanine greatly inhibited neointima formation and prevented VSMCs from a contractile phenotype switching to a synthetic phenotype. In vitro study showed that l-theanine significantly inhibited PDGF-BB-induced VSMC proliferation and migration, which was comparable with the effect of l-theanine on AngII-induced VSMC proliferation and migration. Western blot analysis demonstrated that l-theanine suppressed PDGF-BB and AngII-induced reduction of SMA and SM22α and increment of OPN, suggesting that l-theanine inhibited the transformation of VSMCs from contractile to the synthetic phenotype. Further experiments showed that l-theanine exhibits potential preventive effects on neointimal hyperplasia and related vascular remodeling via inhibition of phosphorylation of Elk-1 and activation of MAPK1. The present study provides the new experimental evidence that l-theanine has potential clinical application as an anti-restenosis agent for the prevention of restenosis.

Nutritional Supplements and Periodontal Disease Prevention—Current Understanding

This review updates the current knowledge on nutrient supplements, which are reported as effective in maintaining the health of periodontal tissues or preventing diseases, as a complementary therapy to existing periodontal treatments. The latest meta-analysis reported that green tea component might be used as a complementary method to existing periodontal treatments. New multifunctional food-derived components such as rice- and soybean-derived proteins and amino acids have also been reported recently. Several previous reports describe that nutritional supplements may help bacterial control and host immune regulation based on cellular or animal experiments, but evidence regarding most nutritional supplements is still insufficient to apply for prevention or treatment of periodontal disease. Complementary use of green tea extract, including catechin, potentially controlling the symptoms of periodontal disease combined with existing therapies could be beneficial, although randomized clinical trials and larger cohort studies are required properly.

Possibility that the Onset of Autism Spectrum Disorder is Induced by Failure of the Glutamine-Glutamate Cycle.

Autism spectrum disorder (ASD) is a neurodevelopmental disease, and the number of patients has increased rapidly in recent years. The causes of ASD involve both genetic and environmental factors, but the details of causation have not yet been fully elucidated. Many reports have investigated genetic factors related to synapse formation, and alcohol and tobacco have been reported as environmental factors. This review focuses on endoplasmic reticulum stress and amino acid cycle abnormalities (particularly glutamine and glutamate) induced by many environmental factors. In the ASD model, since endoplasmic reticulum stress is high in the brain from before birth, it is clear that endoplasmic reticulum stress is involved in the development of ASD. On the other hand, one report states that excessive excitation of neurons is caused by the onset of ASD. The glutamine- glutamate cycle is performed between neurons and glial cells and controls the concentration of glutamate and GABA in the brain. These neurotransmitters are also known to control synapse formation and are important in constructing neural circuits. Theanine is a derivative of glutamine and a natural component of green tea. Theanine inhibits glutamine uptake in the glutamine-glutamate cycle via slc38a1 without affecting glutamate; therefore, we believe that theanine may prevent the onset of ASD by changing the balance of glutamine and glutamate in the brain.

(-)-Epigallocatechin-3-gallate induces interferon-λ2 expression to anti-influenza A virus in human bronchial epithelial cells (BEAS-2B) through p38 MAPK signaling pathway.

Background(-)-Epigallocatechin-3-gallate (EGCG), a major component of green tea, has been found to inhibit the influenza virus. However, the mechanism of EGCG anti-influenza virus effect needs to be further explored.MethodsBEAS-2B cells were treated with different concentrations of EGCG or were treated with EGCG for different times. CCK8 assay was used to detect the cell viability, and quantitative real time polymerase chain reaction (qRT-PCR) and enzyme-linked immunosorbent assay were employed to measure the interferon (IFN)-λ2 mRNA and protein expression levels. The phospho-p38 mitogen-activated protein kinase (P-p38 MAPK), phospho-extracellular signal-regulated kinase (P-ERK), and phospho-c-Jun N-terminal kinase (P-JNK) expression were tested by western blot. Then, p38 MAPK, ERK, and JNK inhibitor were used to study the effect of p38 MAPK, ERK, and JNK signaling pathways on IFN-λ2 expression. The BEAS-2B cells were treated with EGCG, EGCG and IFN λ2 neutralizing antibody or control antibody for 12 h, and were infected with influenza A virus (IAV) (H1N1) for 1 h. After 12 h, nucleoprotein (NP) mRNA and protein expression levels of H1N1 were assessed by qRT-PCR and western blot.ResultsThe IFN-λ2 mRNA and protein expression levels in BEAS-2B cells were up-regulated after EGCG (treatment in time- and dose-dependent manners the concentration range from 0 to 50 µg/mL had no cytotoxicity). Meanwhile, the P-p38 MAPK, P-ERK, and P-JNK expression levels were up-regulated. IFN-λ2 mRNA and protein expression was inhibited after p38 MAPK inhibitor pre-treatment, but not by ERK and JNK inhibitors. Furthermore, the expression of H1N1 NP gene and protein decreased after EGCG pre-treatment, while IFN-λ2 neutralizing antibody attenuated the effect of EGCG inhibiting the expression of H1N1 NP gene and protein.ConclusionsEGCG inhibited IAV H1N1 by inducing the expression of IFN-λ2 in BEAS-2B cells through the p38 MAPK signaling pathway.

Epigallocatechin-3-Gallate Toxicity in Children: A Potential and Current Toxicological Event in the Differential Diagnosis With Virus-Triggered Fulminant Hepatic Failure.

The use of nutraceuticals is considerably increasing worldwide with a demand for organic and clean foods in the last two decades, which is probably incomparable with other periods of our civilization. The consistent application of nutraceuticals and so-called “superfood” may have remarkable effects on the prevention of several chronic diseases, including cancer. Moreover, the increased rate of overweight and obesity in Western countries does not spare childhood and youth, and the number of parents using natural remedies for preventing pediatric illness is vastly increasing worldwide. However, the overwhelming effects on diseases often overshadow the side effects of such nutrition, particularly in societies without millennial experience with botanicals and natural elements. Thus, the final result may be disastrous for some individuals. The liver is the most important and conspicuous target organ of numerous molecular compounds, and the cell damage is particularly striking on the infantile and pediatric liver due to the immaturity of the hepatocytes. Here, we target some generic data on fulminant hepatic failure, the benefits, and toxicity of epigallocatechin-3-gallate, which is one of the major components of green tea, and the histopathology of the “green-tea”-associated liver disease.

SG-SP1 Suppresses Mast Cell-Mediated Allergic Inflammation via Inhibition of FcεRI Signaling

Background: As the number of allergic disease increases, studies to identify new treatments take on new urgency. Epigallocatechin gallate (EGCG), a major component of green tea, has been shown to possess a wide range of pharmacological properties, including anti-inflammation and anti-viral infection. In previous study, gallic acid (GA), a part of EGCG, has shown anti-allergic inflammatory effect. To improve on preliminary evidence that GA has allergy mitigating effect, we designed SG-SP1 based on GA, and aimed to assess the effects of SG-SP1 on mast cell-mediated allergic inflammation using various animal and in vitro models.Methods: For in vitro experiments, various types of IgE-stimulated mast cells (RBL-2H3: mast cell-like basophilic leukemia cells, and primary cultured peritoneal and bone marrow-derived mast cells) were used to determine the role of SG-SP1 (0.1–1 nM). Immunoglobulin (Ig) E-induced passive cutaneous anaphylaxis and ovalbumin-induced systemic anaphylaxis, standard animal models for immediate-type hypersensitivity were also used.Results: For in vitro, SG-SP1 reduced degranulation of mast cells by down-regulating intracellular calcium levels in a concentration-dependent manner. SG-SP1 decreased expression and secretion of inflammatory cytokines in activated mast cells. This suppressive effect was associated with inhibition of the phosphorylation of Lyn, Syk and Akt, and the nuclear translocation of nuclear factor-κB. Due to the strong inhibitory effect of SG-SP1 on Lyn, the known upstream signaling to FcεRI-dependent pathway, we confirmed the direct binding of SG-SP1 to FcεRI, a high affinity IgE receptor by surface plasmon resonance experiment. Oral administration of SG-SP1 hindered allergic symptoms of both anaphylaxis models evidenced by reduction of hypothermia, serum IgE, ear thickness, and tissue pigmentation. This inhibition was mediated by the reductions in serum histamine and interleukin-4.Conclusions: We determined that SG-SP1 directly interacts with FcεRI and propose SG-SP1 as a therapeutic candidate for mast cell-mediated allergic inflammatory disorders via inhibition of FcεRI signaling.

Epigallocatechin-3-O-gallate modulates the diversity of gut microbiota in ovariectomized rats.

Epigallocatechin‐3‐O‐gallate (EGCG) exists as one of the major active components of green tea and has been studied extensively; however, the relationship between EGCG and the changes in the gut microflora of ovariectomized (OVX) rats as a model of menopause women have not yet been studied. Female Wistar rats were fed on a maintenance material diet and underwent either ovariectomy or SHAM surgery. The ovariectomized rats were divided into OVX group with the treatment of placebo or EGCG group which was treated with EGCG by oral gavage. After 8 weeks of treatment, anxiety‐like behaviors were assessed using elevated plus maze test (EMP) and open field test (OFT). The serum estradiol concentration was assayed through ELISA. High‐throughput V3–V4 16S rDNA sequencing was conducted to assess the microbial diversity in fecal samples collected from all rats. EGCG, at a concentration of 10 mg/kg, caused behavioral changes in rats similar to anxiety. In EPM, OVX rats spent less time in open arms than SHAM group rats and EGCG group rats (F = 16.043, p < .01). In OFT, the total travelled distance and the number of entries for EGCG group were higher compared with OVX group (F = 30.939, H = 13.107, respectively; p < .01). In addition, the distribution and composition of intestinal microflora in rats changed after ovariectomy. EGCG modulated the diversity of gut microbiota in OVX group at the phylum and the genus levels. Our results suggested that the composition of gut microbiota and anxiety in OVX rats were simultaneously affected by EGCG, and therefore, the two conditions might be strongly related, yet the deeper mechanistic links need further exploration.

The Potential Role of Tea in Periodontal Therapy: An Updated Review.

Periodontal diseases are highly prevalent and can affect high percentage of the worlds' population. Oxidative stress and inflammation play an important role in the pathogenesis of periodontal diseases. Nowadays, more attention has been focused on the herbal remedies in the field of drug discovery. Green tea is an important source of polyphenol antioxidants. It has long been used as a beverage worldwide. The most interesting polyphenol components of green tea leaves that are related with health benefits are the catechins. Taken together, this review suggested that green tea, with its wide spectrum of activities, could be a healthy alternative for controlling the damaging reactions seen in periodontal diseases.

The Influence of Epigallocatechin Gallate on the Nuclear Factor Associated T Cell-1 and Sclerostin Expression in Wistar Rats (Rattus novergicus) during the Orthodontic Tooth Movement

Orthodontic tooth movement is obtained through alveolar bone remodeling and periodontal tissue in response to the mechanical forces. Epigallocatechin Gallate (EGCG) is the most abundant bioactive component in green tea which is promising therapy for bone remodeling. The aim of the study was to elucidate the effect of EGCG to the expression of Nuclear Factor of Associated T Cells-1 (NFATC1) and sclerostin (SOST) in orthodontic tooth movement animal model. The samples consisted of 28-healthy male wistar rats (Rattus Novergicus) which were randomly selected then divided into 4 groups (n=7): negative control group (K-) without Orthodontic Tooth Movement (OTM) and EGCG; positive control group (K+) with OTM and without EGCG, group (T1) with OTM and EGCG from day 7 to day 14, group (T2) with OTM (14 days) and EGCG for 14 days. The OTM were installed from the labial surfaces of both maxillary central incisor with light force of 10g/mm2 close coil spring connected to the first left maxillary molar. NFATC1 and SOST expression in the alveolar bone was examined by means of Imunohistochemistry. Analysis of Variance (ANOVA) then continued with Tukey HSD (p<0.05) was done. The highest number of NFATc1 and SOST expression was found in the K+ group compression area. There were significant different of NFATc1 and SOST expression in compression and tensile area between groups (p<0.05). Daily oral administration of EGCG for 14 days can reduce the SOST and NFATc1 expression during OTM in compression area and tensile area during OTM.

Acute cognitive, mood and cardiovascular effects of green and black tea

AbstractTea is often described as having “refreshing” properties. Indeed, components of both green and black tea have been shown to acutely improve aspects of cognition and mood and to affect cardiovascular function. There is, however, surprising little research directly comparing these effects between different types of tea. This study therefore examined acute cognitive, mood, and cardiovascular effects of green tea and black tea.A double blind, randomised, placebo-controlled,balanced, three-way cross-over study was conducted. Fourteen healthy young adults (M = 23.8, SD = 3 years) consumed placebo (water), green tea and black tea in balanced order at least 24 h apart.The drinks were prepared according to standardised procedures and consumed under double-blind conditions (in opaque containers with lemon cordial added for taste-masking). Mood and cognition were measured at baseline then 90 min post-treatment, cardiovascular function was assessed post-dose only. Mood was evaluated using a series of visual analogue scales, cognitive performance was assessed using a suite of standardised tests from the Computerised Mental Performance Assessment System (COMPASS), gauging performance on aspects of attention, memory and executive function.Peripheral and central systolic and diastolic pressure,augmentation pressure, augmentation index,and blood flow velocity were measured via Sphygmocor pulse wave analysis and Doppler ultrasound, respectively. There were a number of significant effects associated with the active treatments. Compared with placebo, black tea and green tea was associated with significantly improved digit vigilance accuracy (p &lt; .01), while green tea was associated with higher alertness (p &lt; .05).Regarding cardiovascular outcomes, black tea and green tea significantly increased central diastolic pressure, and peripheral diastolic pressure in comparison to placebo (P &lt; .01). Black tea also significantly increased central systolic pressure compared to green tea and placebo (p &lt; .05). Analysis of treatment guessing suggested that the masking procedure was highly effective. In conclusion, the present study shows that green tea improves alertness. Since black tea contains higher levels of caffeine, this effect is likely underpinned by non-caffeine mechanisms or caffeine/non-caffeine compound interactions.Improved vigilance is consistent with caffeine effects which may be modulated by cardiovascular effects. Interestingly the cardiovascular effects are opposite to those reported for chronic tea interventions. These results suggest that acute cognitive and cardiovascular components of tea merit further investigation both in the presence and absence of caffeine.

Addition of flavonols and polysaccharides as excipient ingredients into epicatechin rich green tea extract inhibited free radical formation and glucose uptake.

It was revealed that excipient ingredients such as flavonols (FVN) or polysaccharides (GTP) which could be derived from green tea enhanced catechin absorption. We hypothesized that the addition of FVN or GTP as excipient ingredients into epicatechin rich green tea extracts (GTE) may improve the health benefits that accompany its consumption. When FVN8.7 (8.7% of GTE, w/w) was added to the GTE (20 mg) as an excipient ingredient, the bioaccessibility and intestinal absorption of total epicatechins was 1.2 and 1.5 times higher than that of only GTE, respectively. This was due to the free radical scavenging capacity of flavonols, showing 114.23 ± 3.07 μmol TE per g for GTE 100 + FVN8.7 and 113.64 ± 1.61 μmol TE per g for GTE 100 + FVN2, respectively. This was significantly higher than the GTE or GTE 100 + OW2 (onion peel and whangchil extracts, 2% of GTE, w/w) which have the same amount of total flavonols. Regarding potential hypoglycemic effects, co-digestion of GTE (20 mg) + green tea polysaccharides (2 mg) + FVN (5 mg) with wheat starch significantly reduced glucose intestinal absorption by 41.85 ± 1.75% compared to only the wheat starch. The results from the current study suggest that whole green tea components rich in flavonols and polysaccharides could be potential hypoglycemic excipient ingredients for green tea catechins.

In Silico Molecular Dynamics Docking of Drugs to the Inhibitory Active Site of SARS-CoV-2 Protease and Their Predicted Toxicology and ADME

A in silico molecular dynamics (MD) docking investigation was conducted to identify drugs (ligands) which could potentially be of interest for repurposing. We sought ligands which formed the strongest binding potential energy with the x-ray crystallography-based active site of the SARS-CoV-2 protease C3Lpro. A total of 11,013 ligands were obtained from DrugBank. Because of the larger size of the active site of 3CLpro, we chose ligands whose molecular weight (MW) was greater than 400 (daltons) and less than 700, which resulted in 5,920 ligands. After correction of bonds and hydrogens, there were 4,634 ligands available for docking. Docking results indicate that the top 10 investigational and experimental drugs with binding energy (BE)≤-9 kcal/mol were Lorecivivint, Tivantinib, Omipalisib, DrugBank B08450, SRT-2104, R-428, DrugBank B01897, Bictegravir, Ridinilazole, and Itacitinib, while the top 10 approved drugs with BE≤-8.2 were Olaparib, Etoposide, Ouabain, Indinavir, Idelalisib, Trametinib, Lumacaftor, Ergotamine, Canagliflozin, and Edoxaban. There were two antiviral drugs among the top 30 hits, which were Bictegravir (investigational) and Indinavir (approved). The top 10 antivirals with BE≤-8.2 were Bictegravir, Tegobuvir, Filibuvir, Saquinavir, Fostemsavir, Indinavir, Temsavir, Pimodivir, Amenamevir, and Doravirine. Interestingly, the antiviral Remdesavir ranked low among the top 30 antivirals, since its BE was a low value of -7.5 kcal/mol. In silico toxicology and ADME (absorption, distribution, metabolism, excretion) prediction indicates that only 20% (6/30) of the top ligands were “drug-like,” and none were “lead-like,” since the lower bound of MW was 400. Another interesting finding was that the investigational natural supplement Diosmin (DrugBank ID B08995), used without prescription for varicose veins, ranked 22 overall (out of 3,896 with BE≤-6) with a strong BE=-8.8, and formed 8 hydrogen bonds with the active site for the putative best pose. Its energy-minimized 3D structure deeply penetrated and fully covered the width of the active site’s pocket. Diosmin had a lower BE than 97% of the top 30 antiviral drugs and formed more hydrogen bonds with the active site than 93% of the top 30 antivirals. Diosmin could therefore potentially serve as a strong inhibitor of the 3CLpro protease of SARS-CoV-2 and could be investigated in human clinical trials. Since a prescription is not required for its use, it could also be explored as a self-medicating natural alternative to prescribed synthetic drugs. Lastly, the green tea component epigallocatechin gallate (DrugBank ID B12116) also had a low BE=-8.3, and formed 2 hydrogen bonds with the active site, which was a BE that was better than 70% of the top 30 antivirals.