Holistic Health Articles and Research Related to Herbal Medicines, Foods and Phytochemicals

Friday, 8 November 2013

Phytochemicals in Foods - 15 Health Benefits of Catechins

Catechins is phytochemicals of Flavan-3-ols, in the group of Flavonoids (polyphenols), found abundantly in white tea, green tea, black tea, grapes, wine, apple juice, cocoa, lentils, etc.

Health Benefits
1. Body-weight regulation
Green tea has been proposed as a tool for obesity management as strategies for weight loss and weight maintenance, as researchers found that a green tea-caffeine mixture improves weight maintenance, through thermogenesis, fat oxidation, and sparing fat free mass. The sympathetic nervous system is involved in the regulation of lipolysis, and the sympathetic innervation of white adipose tissue may play an important role in the regulation of total body fat in general, according to "Green tea catechins, caffeine and body-weight regulation" by Westerterp-Plantenga MS.(1)

2. Cholesterol
In a systematic review and meta-analysis of randomized controlled trials evaluating the relationship between GTCs and serum lipid levels, including total, low-density lipoprotein (LDL), high-density lipoprotein (HDL) cholesterol, and triglycerides, found that the consumption of GTCs is associated with a statistically significant reduction in total and LDL cholesterol levels; however, there was no significant effect on HDL cholesterol or triglyceride levels, according to " Green tea catechins decrease total and low-density lipoprotein cholesterol: a systematic review and meta-analysis" by Kim A, Chiu A, Barone MK, Avino D, Wang F, Coleman CI, Phung OJ.(2)

3. Anti liver cancer
In the examination ofthe effect of catechins on the antitumor efficacy of doxorubicin (DOX) in a murine model, found that tea catechins at non-toxic doses can augment DOX-induced cell killing and sensitize chemoresistant HCC cells to DOX. The chemosensitizing effect of catechins may occur directly or indirectly by reversal of multidrug resistance, involving the suppression of MDR1 expression, or by enhancement of intracellular DOX accumulation, involving inhibition of P-gp function, according to "Green tea catechins augment the antitumor activity of doxorubicin in an in vivo mouse model for chemoresistant liver cancer" by

Liang G, Tang A, Lin X, Li L, Zhang S, Huang Z, Tang H, Li QQ.

4. Antioxidant activity
In the research on polyphenolic compounds (included catechins) in the berries of edible honeysuckle and their biological effects, including recommended utilization, are reviewed found that These berries seem to be prospective sources of health-supporting phytochemicals that exhibit beneficial anti-adherence and chemo-protective activities, thus they may provide protection against a number of chronic conditions, e.g., cancer, diabetes mellitus, tumour growth or cardiovascular and neurodegenerative diseases, according to "Phenolic profile of edible honeysuckle berries (genus lonicera) and their biological effects" by Jurikova T, Rop O, Mlcek J, Sochor J, Balla S, Szekeres L, Hegedusova A, Hubalek J, Adam V, Kizek R.(4)

5. Severe dyslipidemia
In the observation of three-month old ATX mice were treated, or not, for 3 months with the polyphenol (+)-catechin (CAT, 30 mg/kg/day) and compared to wild-type (WT) controls,
found that cctive remodeling of the cerebrovascular wall in ATX mice was further suggested by the increase (P<0.05) in pro-metalloproteinase-9 activity, which was normalized by CAT. We conclude that by preserving the endothelial function, a chronic treatment with CAT prevents the deleterious effect of severe dyslipidemia on cerebral artery wall structure and biomechanical properties, contributing to preserving resting cerebral blood flow, according to "Catechin prevents severe dyslipidemia-associated changes in wall biomechanics of cerebral arteries in LDLr-/-:hApoB+/+ mice and improves cerebral blood flow" by Bolduc V, Baraghis E, Duquette N, Thorin-Trescases N, Lambert J, Lesage F, Thorin E.(5)

6. Anti-inflammatory effect
In the preparation of the gel of Chinese medicine catechu, and to observe the release mechanism in vitro and anti-inflammatory activity in rats, found that the optimum condition of extraction from catechu was as follows, the concentration of ethanol, ratio of raw material to solvent, ultrasonic time, and extraction temperature were 50% , 1: 12, 35 min and 60 degrees C, respectively. The formulation of catechu gel was carbomer-9 400.5 g, glycerol 5.0 g, the extracts of catechu 50.0 mL, and triethanomine 0.5 mL The gel was semitransparent and stable. The drugs released quickly. The catechu gel reduced the paw edema considerably in dose-dependent manner compared to carrageenan-induced rat, according to "[Preparation and pharmacodynamics studies on anti-inflammatory effect of catechu gel].[Article in Chinese]" by Zheng X, Zheng C.(6)

7. Neuropathic pain
In the investigation of Epigallocatechin-3-gallate (EGCG), the major catechin in green tea and its effect on intrathecal EGCG in neuropathic pain induced by spinal nerve ligation, found that This antinociceptive effect was reversed by intrathecal pretreatment with l-arginine, a precursor of NO. Intrathecal EGCG also blocked the increase in nNOS expression in the spinal cord of spinal nerve-ligated rats, but iNOS expression was not significantly suppressed. These findings suggest that intrathecal EGCG could produce an antiallodynic effect against spinal nerve ligation-induced neuropathic pain, mediated by blockade of nNOS protein expression and inhibition of the pronociceptive effects of NO, according to "Role of neuronal nitric oxide synthase in the antiallodynic effects of intrathecal EGCG in a neuropathic pain rat model" by Choi JI, Kim WM, Lee HG, Kim YO, Yoon MH.(7)

8. Cholesterol and glucose levels
In the examination of the effect of the main green tea catechin, epigallocatechin gallate (EGCG), taken in a green tea extract, Polyphenon E (PPE) and their effect on circulating hormone levels, an established breast cancer risk factor, found that Glucose and insulin levels decreased nonsignificantly in the PPE groups but increased in the placebo group; statistically significant differences in changes in glucose (P=0.008) and insulin (P=0.01) were found. In summary, green tea (400 and 800 mg EGCG as PPE; ~5-10 cups) supplementation for 2 months had suggestive beneficial effects on LDL cholesterol concentrations and glucose-related markers, according to "Effect of 2-month controlled green tea intervention on lipoprotein cholesterol, glucose, and hormonal levels in healthy postmenopausal women" by
Wu AH, Spicer D, Stanczyk FZ, Tseng C, Yang CS, Pike MC.(8)

9. Neuroprotective effects
In the evaluation the neuroprotective effects of theanine and catechins contained in green tea , found that the mechanism of the neuroprotective effect of theanine is related not only to the glutamate receptor but also to other mechanisms such as the glutamate transporter, although further studies are needed. One of the onset mechanisms for arteriosclerosis, a major factor in ischemic cerebrovascular disease, is probably the oxidative alteration of low-density lipoprotein (LDL) by active oxygen species. The oxidative alterations of LDL were shown to be prevented by tea catechins. Scavenging of *O(2)(-) was also exhibited by tea catechins. The neuroprotective effects of theanine and catechins contained in green tea are a focus of considerable attention, and further studies are warranted, according to "Neuroprotective effects of the green tea components theanine and catechins" by Kakuda T.(9)

10. Anti-obesity effects
In the elucidation of the anti-obesity effects of three major components of green tea, catechins, caffeine and theanine, female ICR mice, found that The body weight increase and weight of IPAT were significantly reduced by the diets containing green tea, caffeine, theanine, caffeine + catechins, caffeine + theanine and caffeine + catechins + theanine. Noticeably, the IPAT weight decreased by 76.8% in the caffeine + catechins compared to the control group. Serum concentrations of triglycerides (TG) and non-esterified fatty acids (NEFA) were decreased by green tea, catechins and theanine. Moreover, caffeine + catechins, caffeine + theanine and caffeine + catechins + theanine also decreased NEFA in the serum. The TG level in the liver was significantly reduced by catechins and catechins + theanine in comparison with the control, according to "Anti-obesity effects of three major components of green tea, catechins, caffeine and theanine, in mice" by Zheng G, Sayama K, Okubo T, Juneja LR, Oguni I.(10)

11. Nonalcoholic fatty liver disease
In the investigation of green tea's effect on nonalcoholic fatty liver disease (NAFLD), a constellation of progressive liver disorders, found that green tea is rich in polyphenolic catechins that have hypolipidemic, thermogenic, antioxidant, and anti-inflammatory activities that may mitigate the occurrence and progression of NAFLD. This review presents the experimental evidence demonstrating the hepatoprotective properties of green tea and its catechins and the proposed mechanisms by which these targeted dietary agents protect against NAFLD, according to"Therapeutic potential of green tea in nonalcoholic fatty liver disease" by Masterjohn C, Bruno RS.(11)

12. Age-related Neurodegeneration
In the identification of green tea (GT) and the effect of large amounts of brain-accessible polyphenols, found that the beneficial action of catechins in learning and memory with a particular focus on the hippocampal formation. We conclude that GT polyphenols can have a promising role in the reversal of age-related loss of neuronal plasticity and recovery after neuronal lesions associated with aging, according to "Protective Effects of Chronic Green Tea Consumption on Age-related Neurodegeneration" by Andrade JP, Assunção M.(12)

13. Anti-influenza virus activity
In the study of Polyphenolic compounds present in green tea, particularly catechins, and its effect on strong anti-influenza activity, found that therapeutic administration of green tea by-products via feed or water supplement resulted in a dose-dependent significant antiviral effect in chickens, with a dose of 10 g/kg of feed being the most effective (P < 0.001), according to "Anti-influenza virus activity of green tea by-products in vitro and efficacy against influenza virus infection in chickens" by Lee HJ, Lee YN, Youn HN, Lee DH, Kwak JH, Seong BL, Lee JB, Park SY, Choi IS, Song CS.(13)

14. Prostate Cancer
In the review of Prostate cancer, the most commonly diagnosed cancer and second most common cause of cancer deaths in American men indicated that epidemiological studies suggest that tea consumption has protective effects against a variety of human cancers, including that of the prostate. Laboratory and clinical studies have demonstrated that green tea components, specifically the green tea catechin (GTC) epigallocatechin gallate, can induce apoptosis, suppress progression, and inhibit invasion and metastasis of prostate cancer, according to "New Insights Into the Mechanisms of Green Tea Catechins in the Chemoprevention of Prostate Cancer" by Connors SK, Chornokur G, Kumar NB.(14)

15. Breast cancer
In the developing a chronically induced breast cell carcinogenesis model to the exposure of non-cancerous, human breast epithelial MCF10A cells to bioachievable picomolar concentrations of environmental carcinogens, such as 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone (NNK) and benzo[a]pyrene (B[a]P), to progressively induce cellular acquisition of cancer-associated properties, as measurable end points, found that green tea catechins (GTCs) , at non-cytotoxic levels, were able to suppress chronically induced cellular carcinogenesis by blocking carcinogen-induced ROS elevation, ERK activation, cell proliferation and DNA damage in each exposure cycle. Our model may help accelerate the identification of preventive agents to intervene in carcinogenesis induced by long-term exposure to environmental carcinogens, thereby safely and effectively reducing the health risk of sporadic breast cancer, according to "Green tea catechin intervention of reactive oxygen species-mediated ERK pathway activation and chronically induced breast cell carcinogenesis" by Rathore K, Choudhary S, Odoi A, Wang HC.(15)

16. Etc.

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Phytochemicals in Foods - 13 Health Benefits of Gallocatechin

Gallocatechin, containing catechin is phytochemicals of Flavan-3-ols, in the group of Flavonoids (polyphenols), found abundantly in green tea, almonds, black diamond plums, black tea, cocoa beans, Fuji apples, golden delicious apple, etc.

Health Benefits
1. Bone metabolism
In the investigation of three tea catechins, epigallocatechin (EGC), gallocatechin (GC), and gallocatechin gallate (GCG) for their effects on bone metabolism, found that EGC significantly inhibited osteoclast formations from RAW 264.7 cells upon receptor activation of nuclear factor-kappaB ligand induction on the fourth day of treatment, at a concentration of 10 microM. EGC also dose-dependently inhibited the mRNA expression of tatrate-resistant acid phosphatase. GC and GCG could decrease osteoclastogenesis at 20 microM. The present study illustrated that the tea catechins, EGC in particular, had positive effects on bone metabolism through a double process of promoting osteoblastic activity and inhibiting osteoclast differentiations, according to "Effects of tea catechins, epigallocatechin, gallocatechin, and gallocatechin gallate, on bone metabolism" by Ko CH, Lau KM, Choy WY, Leung PC.(1)

2. Antimetastatic effects
In the evaluation of the antimetastatic effects of P urinaria L extracts (PUE), containingpolyphenols including gallic acid, methyl gallate, epicatechin, epigallocatechin-3-gallate, gallocatechin-3-gallate, rutin, epicatechin-3-gallate, and naringin, found that PUE inhibits the transcription of MMP-2 mRNA. PUE also exerted an inhibitory effect on the DNA-binding activity and the nuclear translocation of NF-κB and AP-1. Furthermore, the inhibitory effects of PUE on the metastasis and growth of LLC cells in vivo were proven. These results indicate that PUE could be applied to be a potential antimetastatic agent, according to "Antimetastatic Potentials of Phyllanthusurinaria L on A549 and Lewis Lung Carcinoma Cells via Repression of Matrix-Degrading Proteases" by Tseng HH, Chen PN, Kuo WH, Wang JW, Chu SC, Hsieh YS.(2)

3. Anti skin cancer
In the determination of the effect of green tea catechins on the invasive potential of human melanoma cells and the molecular mechanisms underlying these effects using A375 (BRAF-mutated) and Hs294t (Non-BRAF-mutated) melanoma cell lines as an in vitro model, found that Inhibition of melanoma cell migration by EGCG was associated with transition of mesenchymal stage to epithelial stage, which resulted in an increase in the levels of epithelial biomarkers (E-cadherin, cytokeratin and desmoglein 2) and a reduction in the levels of mesenchymal biomarkers (vimentin, fibronectin and N-cadherin) in A375 melanoma cells. Together, these results indicate that EGCG, a major green tea catechin, has the ability to inhibit melanoma cell invasion/migration, an essential step of metastasis, by targeting the endogenous expression of COX-2, PGE(2) receptors and epithelial-to-mesenchymal transition, according to "Green tea catechins reduce invasive potential of human melanoma cells by targeting COX-2, PGE2 receptors and epithelial-to-mesenchymal transition" by Singh T, Katiyar SK(3)

4. Antidiabetic activity
In the observation of Terminalia sericea stem bark extract and theirs effect against alpha-glucosidase and alpha-amylase enzymes, found that four known compounds namely beta-sitosterol (1), beta-sitosterol-3-acetate (2), lupeol (3), and stigma-4-ene-3-one (4), in addition to two inseparable sets of mixtures of isomers [epicatechin-catechin (M1), and gallocatechin-epigallocatechin (M2). 1 and 3 showed the best inhibitory activity on alpha-glucosidase (IC50:54.5 and 66.5 microM). Bio-evaluation of the inhibitory activity of the purified compounds on alpha-amylase showed that 3 and 1 exhibited IC50 values of 140.7 and 216.02 microM, respectively against alpha-amylase, according to "Antidiabetic activity of Terminalia sericea constituents" by Nkobole N, Houghton PJ, Hussein A, Lall N.(4)

5. Anti-uveal melanoma activity
In the study of the MeOH extract of Acacia nilotica pods, resulted in the isolation of the new compound gallocatechin 5-O-gallate in addition to methyl gallate, gallic acid, catechin, catechin 5-O-gallate, 1-O-galloyl-β-D-glucose, 1,6-di-O-galloyl-β-D-glucose and digallic acid, found that in addition to uveal melanoma, the antiproliferative activities of the isolated compounds and the related compound epigallocatechin 3-O-gallate (EGCG) were evaluated against cutaneous melanoma, ovarian cancer, glioblastoma and normal retinal pigmented cells, according to "In vitro anti-uveal melanoma activity of phenolic compounds from the Egyptian medicinal plant Acacia nilotica" by Salem MM, Davidorf FH, Abdel-Rahman MH.(5)

6. Degenerative diseases
In the inestigation of whether green tea and its components can regulate the osteogenic and adipogenic differentiation in pluripotent rat mesenchymal stem cells (MSCs). The rat MSCs were isolated from the bone marrow of tibiae and femora, found that among six tested tea polyphenols, epigallocatechin (EGC) was shown to be the most effective in promoting osteogenic differentiation. At 20 μM, EGC increased ALP levels and Ca deposition significantly by 2.3- and 1.7-fold, respectively, when compared with the control group. EGC also increased the mRNA expression of bone formation markers runt-related transcription factor 2, ALP, osteonectin, and osteopontin, according to "Pro-bone and antifat effects of green tea and its polyphenol, epigallocatechin, in rat mesenchymal stem cells in vitro" by Ko CH, Siu WS, Wong HL, Shum WT, Fung KP, San Lau CB, Leung PC.(6)

7. Antioxidants
In the identification of Glucose-6-phosphate dehydrogenase (G6PD) and its important roles in the maintenance of cellular redox balance, found that Pretreatment with green tea polyphenol epigallocatechin-3-gallate (EGCG) effectively blocked peroxynitrite-induced glutathione depletion, p53 accumulation, and apoptosis in both normal and G6PD-deficient cells. EGCG, administered to cells alone or as pretreatment, caused activation of Akt. The protective effect was abolished by phosphatidylinositol 3-kinase (PI3K) inhibitors, wortmannin, and LY294002, according to "Green tea polyphenol epigallocatechin-3-gallate protects cells against peroxynitrite-induced cytotoxicity: modulatory effect of cellular G6PD status" by Ho HY, Wei TT, Cheng ML, Chiu DT.(7)

8. Anti HIV
In the investigation of Epigallocatechin gallate (EGCG), the most abundant catechin in green tea and its effect on HIV-1, found that EGCG appears to act mainly as an allosteric reverse transcriptase inhibitor with mechanisms different from those of currently approved NNRTIs that directly interact with the NNRTI binding pocket. Thus, EGCG is a good candidate for use as an additional or supportive anti-HIV agent derived from natural plants, according to "Epigallocatechin gallate inhibits the HIV reverse transcription step" by Li S, Hattori T, Kodama EN.(8)

9. Antioxidant and anti-inflammatory activities
In the evaluation of the radioprotective efficacy of green tea polyphenols and the component ingredients against irradiated-induced damage in mice and elucidate the underlying mechanisms, found that Moreover GTP and its bioactive components (catechin, epigallocatechin and epigallocatechin-3-gallate) assisted in decreasing the leukocytopenia seen after whole mice irradiation and significantly reduced the elevated serum inflammatory cytokines (TNF-α, IL-1β, and IL-6). Green tea polyphenols have a potential to be developed as radioprotective agents against irradiated-induced toxicity. Furthermore the antioxidant and anti-inflammatory activities of GTP can be attributed to the interaction of the different components through multiple and synergistic mechanisms, according to "Bioactive components from the tea polyphenols influence on endogenous antioxidant defense system and modulate inflammatory cytokines after total-body irradiation in mice" by Hu Y, Guo DH, Liu P, Cao JJ, Wang YP, Yin J, Zhu Y, Rahman K.(9)

10. Anti-inflammatory and antimicrobial effects
In the evaluation of the anti-inflammatory and antimicrobial effect of nanocatechin on CBP and plasma concentration of catechins in an animal model, found that the use of ciprofloxacin, catechin, and nanocatechin showed statistically significant decrease in bacterial growth and improvement in prostatic inflammation compared with the control group. The nanocatechin group showed statistically significant decrease in bacterial growth and improvement in prostatic inflammation compared with the catechin group. Plasma concentrations of epicatechin, gallocatechin gallate, and epigallocatechin gallate were significantly higher in the nanocatechin group than those in the catechin group. These results suggest that nanocatechin has better antimicrobial and anti-inflammatory effects on rat CBP than catechin due to higher absorption into the body, according to "Anti-inflammatory and antimicrobial effects of nanocatechin in a chronic bacterial prostatitis rat model" by Yoon BI, Ha US, Sohn DW, Lee SJ, Kim HW, Han CH, Lee CB, Cho YH.(10)

11. Ultraviolet B irradiation protection
In the investigation of the protective effect of epigallocatechin gallate (EGCG) on the immune function of dendritic cells (DCs) after ultraviolet B irradiation (UVB), found that the inhibition rate of DCs was improved to some extent after treatment with 200 microg/mL of EGCG. UVB showed no significant influence on the secretion of IL-10 and IL-12 from DCs, while EGCG was able to down-regulate the secretion level of IL-12 and up-regulate that of IL-10, according to "Protective effect of epigallocatechin gallate on the immune function of dendritic cells after ultraviolet B irradiation" by Jin SL, Zhou BR, Luo D.(11)

12. Antiviral effect
In the identification of tea polyphenols were evaluated for their ability to inhibit enterovirus 71 (EV71) replication in Vero cell culture, found that The viral inhibitory effect correlated well with the antioxidant capacity of polyphenol. Mechanistically, EV71 infection led to increased oxidative stress, as shown by increased dichlorofluorescein and MitoSOX Red fluorescence. Upon EGCG treatment, reactive oxygen species (ROS) generation was significantly reduced. Consistent with this, EV71 replication was enhanced in glucose-6-phosphate dehydrogenase deficient cells, and such enhancement was largely reversed by EGCG, according to "Antiviral effect of epigallocatechin gallate on enterovirus 71" by Ho HY, Cheng ML, Weng SF, Leu YL, Chiu DT.(12)

13. Neuroprotective effect
In the research of beta-Amyloid (Abeta) peptide, a major component of senile plaques has been regarded to play a crucial role in the development and neuropathogenesis of Alzheimer's disease (AD), found that EGCG may have preventive and/or therapeutic potential in AD patients by augmenting cellular antioxidant defense capacity and attenuating Abeta-mediated oxidative and/or nitrosative cell death, according to" Neuroprotective effect of epigallocatechin-3-gallate against beta-amyloid-induced oxidative and nitrosative cell death via augmentation of antioxidant defense capacity" by Kim CY, Lee C, Park GH, Jang JH.(13)

14. Etc.
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Sources
(1) http://pubs.acs.org/doi/abs/10.1021/jf901545u
(2) http://www.ncbi.nlm.nih.gov/pubmed/22144737
(3) http://www.ncbi.nlm.nih.gov/pubmed/22022384
(4) http://www.ncbi.nlm.nih.gov/pubmed/22224265
(5) http://www.ncbi.nlm.nih.gov/pubmed/21903153
(6) http://www.ncbi.nlm.nih.gov/pubmed/21877759
(7) http://www.ncbi.nlm.nih.gov/pubmed/16506813
(8) http://www.ncbi.nlm.nih.gov/pubmed/21730371
(9) http://www.ncbi.nlm.nih.gov/pubmed/21498061
(10) http://www.ncbi.nlm.nih.gov/pubmed/20694569
(11) http://www.ncbi.nlm.nih.gov/pubmed/19735514
(12) http://www.ncbi.nlm.nih.gov/pubmed/21903153
(13) http://www.ncbi.nlm.nih.gov/pubmed/19557365

Phytochemicals in Foods- 13 Health Benefits of Epicatechin

Epicatechin, containing catechins, is phytochemicals of Flavan-3-ols, in the group of Flavonoids (polyphenols), found abundantly in kola nut, tea and grapes, etc.

Health benefits
1. Testosterone
In the study of the effects of catechins on testosterone secretion in rat testicular Leydig cells (LCs) both in vivo and in vitro, found that Catechins increased plasma testosterone in vivo in male rats. In vitro, low-dose concentration of catechins increased gonadotropin releasing hormone (GnRH)-stimulated luteinizing hormone (LH) release by anterior pituitary gland and hCG-stimulated testosterone release by LCs of male rats, according to "Effects of catechin, epicatechin and epigallocatechin gallate on testosterone production in rat leydig cells" by Yu PL, Pu HF, Chen SY, Wang SW, Wang PS(1)

2. Insulin Resistance
In the study of increased plasma levels of free fatty acids (FFAs) are associated with profound insulin resistance in skeletal muscle and may also play a critical role in the insulin resistance of obesity and type 2 diabetes mellitus, found that epigallocatechin gallate (EGCG) and curcumin treatment reduce insulin receptor substrate-1 (IRS-1) Ser307 phosphorylation, and curcumin is more potent to increase Akt phosphorylation in TPA induction. Moreover, we found that after 5 h of palmitate incubation, epicatechin gallate (ECG) can suppress IRS-1 Ser307 phosphorylation and significantly promote Akt, ERK1/2, p38 MAPK, and AMP-activated protein kinase activation. With a longer incubation with palmitate, IRS-1 exhibited a dramatic depletion, and treatment with EGCG, ECG, and curcumin could reverse IRS-1 expression, Akt phosphorylation, and MAPK signaling cascade activation and improve glucose uptake in C2C12 skeletal muscle cells, according to "Suppression of Free Fatty Acid-Induced Insulin Resistance by Phytopolyphenols in C2C12 Mouse Skeletal Muscle Cells" by Deng YT, Chang TW, Lee MS, Lin JK.(2)

3. Genoprotective effects
In the determination of what effects could trigger the effects of epicatechin gallate (ECG) in C6 cells, found that ECG as a dose-dependent genoprotective compound in C6 astroglial cells. This indicates that small doses of polyphenols included in our diet could have beneficial effects on neural cells, contributing to prevention of oxidative stress-associated brain pathologies. In addition, our data highlight the importance of strictly modulating doses and/or consumption of antioxidant-fortified foods or additional supplements containing such beneficial molecules, according to "Genoprotective effects of the green tea-derived polyphenol/epicatechin gallate in C6 astroglial cells' by Abib RT, Quincozes-Santos A, Zanotto C, Zeidán-Chuliá F, Lunardi PS, Gonçalves CA, Gottfried C.(3)

4. Colon cancer
In the identification of the anticarcinogenic effects of the flavanols epicatechin (EC), epicatechin-gallate (ECG) and procyanidin B2 (PB2) on Caco-2 and SW480 colon cancer cells, found that the different cytotoxicity of flavanols is caused by their different activity and the degree of differentiation of the colon cancer cell line. Thus, ECG induced apoptosis in SW480 cells and contributed to the cytotoxic effect, whereas ECG enhanced the antioxidant potential in Caco-2 cells. PB2 activated cell proliferation and survival/proliferation pathways in SW480 cells, accoridng to "Dietary flavanols exert different effects on antioxidant defenses and apoptosis/proliferation in Caco-2 and SW480 colon cancer cells" by
Ramos S, Rodríguez-Ramiro I, Martín MA, Goya L, Bravo L.(4)

5. Anti cancer
In the demonstration of the ability of monomeric and dimeric flavanols in scavenging reactive nitrogen species derived from nitrous acid, found that epicatechin was transferred across the jejunum of the small intestine yielding metabolites, its nitroso form was not absorbed. Dimer B2 but not epicatechin monomer inhibited the proliferation of, and triggered apoptosis in, Caco-2 cells. The latter was accompanied by caspase-3 activation and reductions in Akt phosphorylation, suggesting activation of apoptosis via inhibition of prosurvival signaling, according to "The reaction of flavanols with nitrous acid protects against N-nitrosamine formation and leads to the formation of nitroso derivatives which inhibit cancer cell growth" by Lee SY, Munerol B, Pollard S, Youdim KA, Pannala AS, Kuhnle GG, Debnam ES, Rice-Evans C, Spencer JP.(5)

6. Antioxidants
In the evaluation of evaluate the antioxidant response of colon-derived Caco2 cells to dietary flavanols, found that Flavanols ( epicatechin (EC), epicatechin-3-gallate (ECG), epigallocatechin-3-gallate (EGCG) and procyanidin B2 (PB2)) protect Caco2 cells against an induced oxidative stress and subsequent cellular death by reducing ROS production and preventing caspase-3 activation. In particular, PB2 increases the activity of antioxidant/detoxification enzymes and thus protects Caco2 cells by directly counteracting free radicals and also by activating the antioxidant defence system, according to "Comparative effects of dietary flavanols on antioxidant defences and their response to oxidant-induced stress on Caco2 cells" by Rodríguez-Ramiro I, Martín MA, Ramos S, Bravo L, Goya L.(6)

7. Hepatitis C virus
In the investigation of the polyphenol, epigallocatechin-3-gallate (EGCG) and and its derivatives, epigallocatechin (EGC), epicatechin gallate (ECG), and epicatechin (EC), as an inhibitor of HCV entry, found that treatment with EGCG directly during inoculation strongly inhibited HCV infectivity. Expression levels of all known HCV (co-)receptors were unaltered by EGCG. Finally, we showed that EGCG inhibits viral attachment to the cell, thus disrupting the initial step of HCV cell entry and concluded that the green tea molecule, EGCG, potently inhibits HCV entry and could be part of an antiviral strategy aimed at the prevention of HCV reinfection after liver transplantation, according to "The green tea polyphenol, epigallocatechin-3-gallate, inhibits hepatitis C virus entry" by Ciesek S, von Hahn T, Colpitts CC, Schang LM, Friesland M, Steinmann J, Manns MP, Ott M, Wedemeyer H, Meuleman P, Pietschmann T, Steinmann E.(7)

8. Genotoxic effects
In the evaluation of the potential cytotoxic and prooxidative effects of green tea extract and its two main flavonoid constituents epigallocatechin gallate (EGCG) and epicatechin gallate (ECG) on human laryngeal carcinoma cell line (HEp2), found that the cytotoxicity of EGCG and ECG increased with the time of incubation. Green tea extract induced lipid peroxidation in the CK2 cell line. The pro-oxidant effect of green tea was determined at concentrations higher than those found in traditionally prepared green tea infusions, according to "Genotoxic effects of green tea extract on human laryngeal carcinoma cells in vitro" by Durgo K, Kostić S, Gradiški K, Komes D, Osmak M, Franekić J.(8)

9. Anti inflammatory properties
In the comparison of anti-tumoral properties of EGCG on human pancreatic ductal adenocarcinoma (PDAC) cells PancTu-I, Panc1, Panc89 and BxPC3 and the effects of two minor components of green tea catechins, catechin gallate (CG) and epicatechin gallate (ECG), found that all three catechins inhibited proliferation of PDAC cells in a dose- and time-dependent manner. Interestingly, CG and ECG exerted much stronger anti-proliferative effects than EGCG. Western blot analyses performed with PancTu-I cells revealed catechin-mediated modulation of cell cycle regulatory proteins (cyclins, cyclin-dependent kinases [CDK], CDK inhibitors). Again, these effects were clearly more pronounced in CG or ECG than in EGCG-treated cells, according to "Epicatechin gallate and catechin gallate are superior to epigallocatechin gallate in growth suppression and anti-inflammatory activities in pancreatic tumor cells" by Kürbitz C, Heise D, Redmer T, Goumas F, Arlt A, Lemke J, Rimbach G, Kalthoff H, Trauzold A.(9)

10. Breast cancer
In the identification of an inverse association between the risk of breast cancer and the intake of green tea has also been reported in Asian Americans, found that Nude mice inoculated with human breast cancer MDA-MB-231 cells and treated with GTP and EGCG were effective in delaying the tumor incidence as well as reducing the tumor burden when compared to the water fed and similarly handled control. GTP and EGCG treatment were also found to induce apoptosis and inhibit the proliferation when the tumor tissue sections were examined by immunohistochemistry, according to "Green tea polyphenols and its constituent epigallocatechin gallate inhibits proliferation of human breast cancer cells in vitro and in vivo" by Thangapazham RL, Singh AK, Sharma A, Warren J, Gaddipati JP, Maheshwari RK.(10)

11. Blastocysts
In the analyzing the cytotoxic effects of epicatechin gallate (ECG), a polyphenol extract from green tea, on the blastocyst stage of mouse embryos, subsequent embryonic attachment, and in vitro and in vivo outgrowth implantation after embryo transfer, found that Blastocysts treated with 50 microM ECG exhibited a significant increase in apoptosis and a corresponding decrease in total cell number. Importantly, the implantation success rate of blastocysts pretreated with 50 microM ECG was lower than that of controls, and in vitro treatment with 50 microM ECG was associated with increased resorption of post-implantation embryos and decreased fetal weight, according to "Epicatechin gallate decreases the viability and subsequent embryonic development of mouse blastocysts" by Tu HC, Chen CP, Chan WH.(11)

12. Prostate cancer
In the examination of the HGF/c-Met pathway, an important regulator of signaling pathways responsible for invasion and metastasis of most human cancers, found that EGCG could act both by preventing activation of c-Met by HGF and by attenuating the activity of pathways already induced by HGF. HGF did not activate the MAPK and PI3-K pathways in cells treated with methyl-beta-cyclodextrin (mCD) to remove cholesterol. Furthermore, subcellular fractionation approaches demonstrated that only phosphorylated c-Met accumulated in Triton X-100 membrane insoluble fractions, supporting a role for lipid rafts in regulating c-Met signaling. Finally, EGCG treatment inhibited DiIC16 incorporation into membrane lipid ordered domains, and cholesterol partially inhibited the EGCG effects on signaling, according to "The polyphenol epigallocatechin-3-gallate affects lipid rafts to block activation of the c-Met receptor in prostate cancer cells" by Duhon D, Bigelow RL, Coleman DT, Steffan JJ, Yu C, Langston W, Kevil CG, Cardelli JA.(12)

13. Periodontal disease
in the investigation of IL-6 is well recognized to be a potent bone resorptive agent and thus in the development of periodontal disease, found that EGCG, ECG, and TFDG prevented TNFSF14-mediated IL-6 production in HGFs. EGCG, ECG, and TFDG prevented TNFSF14-induced extracellular signal-regulated kinase (ERK), c-Jun N-terminal kinase (JNK), and nuclear factor-kappaB activation in HGFs. Inhibitors of ERK, JNK, and nuclear factor-kappaB decreased TNFSF14-induced IL-6 production. In addition, EGCG, ECG, and TFDG attenuated TNFSF14 receptor expression on HGFs, according to "Tea polyphenols inhibit IL-6 production in tumor necrosis factor superfamily 14-stimulated human gingival fibroblasts" by Hosokawa Y, Hosokawa I, Ozaki K, Nakanishi T, Nakae H, Matsuo T.(13)

14. Glucose tolerance
In the investigation of the benefit of green tea extract (GTE) consumption in effecting prolonged postprandial hyperglycemia, a detrimental factor for type 2 diabetes and obesity, found that the gallated catechin when it is in the circulation elevates blood glucose level by blocking normal glucose uptake into the tissues, resulting in secondary hyperinsulinemia, whereas it decreases glucose entry into the circulation when they are inside the intestinal lumen. These findings encourage the development of non-absorbable derivatives of gallated catechins for preventative treatment of type 2 diabetes and obesity, which would specifically induce only the positive luminal effect, according to "Ambivalent role of gallated catechins in glucose tolerance in humans: a novel insight into non-absorbable gallated catechin-derived inhibitors of glucose absorption" by Park JH, Jin JY, Baek WK, Park SH, Sung HY, Kim YK, Lee J, Song DK.(13)

14. Etc.
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Sources
(1) http://www.ncbi.nlm.nih.gov/pubmed/20432242
(2) http://www.ncbi.nlm.nih.gov/pubmed/22191431
(3) http://www.ncbi.nlm.nih.gov/pubmed/20828315
(4) http://www.ncbi.nlm.nih.gov/pubmed/21945981
(5) http://www.ncbi.nlm.nih.gov/pubmed/16413414
(6) http://www.ncbi.nlm.nih.gov/pubmed/21046126
(7) http://www.ncbi.nlm.nih.gov/pubmed/21837753
(8) http://www.ncbi.nlm.nih.gov/pubmed/21705301
(9) http://www.ncbi.nlm.nih.gov/pubmed/21241417
(10) http://www.ncbi.nlm.nih.gov/pubmed/16519995
(11) http://www.ncbi.nlm.nih.gov/pubmed/20708524
(12) http://www.ncbi.nlm.nih.gov/pubmed/20623641
(13) http://www.ncbi.nlm.nih.gov/pubmed/20461739
(14) http://www.ncbi.nlm.nih.gov/pubmed/20065503

Phytochemicals in Foods - 11 Health Benefits of Epigallocatechin

Epigallocatechin, including catechins, is phytochemicals of Flavan-3-ols, in the group of Flavonoids (polyphenols) with with the gallate residue being in an isomeric cis position, found abundantly in green tea, St John wort, black Tea, carob flour, Fuji apples, etc.

Health Benefits
1. Anti-Breast Cancer Activities
In the testing the hypothesis that administration of epigallocatechin-3-gallate (EGCG), a polyphenol present in abundance in widely consumed tea, and its inhibition of cell proliferation, invasion, and angiogenesis in breast cancer, found that treatment with combination of radiotherapy and EGCG feeding for 2-8 weeks to in vitro cultures of highly-metastatic human MDA-MB-231 breast cancer cells resulted in the following significant changes: (1) suppression of cell proliferation and invasion; (2) arrest of cell cycles at the G0/G1 phase; (3) reduction of activation of MMP9/MMP2, expressions of Bcl-2/Bax, c-Met receptor, NF-κB, and the phosphorylation of Akt. MDA-MB-231 cells exposed to 5-10 µM EGCG also showed significant augmentation of the apoptosis inducing effects of γ-radiation, concomitant with reduced NF-κB protein level and AKT phosphorylation, according to "Anti-Cancer Activities of Tea Epigallocatechin-3-Gallate in Breast Cancer Patients under Radiotherapy" by Zhang G, Wang Y, Zhang Y, Wan X, Li J, Liu K, Wang F, Liu Q, Yang C, Yu P, Huang Y, Wang S, Jiang P, Qu Z, Luan J, Duan H, Zhang L, Hou A, Jin S, Hsieh TC (1)

2. Anti cancers
In the review and outline the wide range of mechanisms by which epigallocatechin gallate (ECGC) and other green and black tea polyphenols' inhibition of cancer cell found that EGCG reduced dihydrofolate reductase activity, which would affect nucleic acid and protein synthesis. It also acted as an aryl hydrocarbon receptor an-tagonist by directly binding the receptor's molecular chaperone, heat shock protein 90. In conclusion, green and black tea polyphenols act at numerous points regulating cancer cell growth, survival, and metastasis, including effects at the DNA, RNA, and protein levels, according to "Mechanisms of cancer prevention by green and black tea polyphenols" by Beltz LA, Bayer DK, Moss AL, Simet IM.(2)

3. Anti-atherosclerotic effects
In the localization and target sites of tea catechins underlying their biological activity including anti-atherosclerotic activity, found that ECg could suppress the gene expression of a scavenger receptor CD36, a key molecule for foam cell formation, in macrophage cells. These results, for the first time, showed the target site of a tea component ECg in the aorta and might provide a mechanism for the anti-atherosclerotic actions of the catechins, according to "(-)-Epicatechin gallate accumulates in foamy macrophages in human atherosclerotic aorta: implication in the anti-atherosclerotic actions of tea catechins" by Kawai Y, Tanaka H, Murota K, Naito M, Terao J.(3)

4. Inflammatory effects
In the determination of the up-regulated expressions of IL-8 or PGE(2) in Streptococci or PAMP-stimulated HDPF were inhibited by catechins, (-)-epicatechin gallate (ECG) and (-)-epigallocatechin gallate (EGCG). In TLR2 ligand-stimulated HDPF, found that catechins might be useful therapeutically as an anti-inflammatory modulator of dental pulpal inflammation, according to "Tea catechins reduce inflammatory reactions via mitogen-activated protein kinase pathways in toll-like receptor 2 ligand-stimulated dental pulp cells" by Hirao K, Yumoto H, Nakanishi T, Mukai K, Takahashi K, Takegawa D, Matsuo T.(4)

5. Cardiovascular diseases
In the identification of green tea catechins and its lowering the risk of cardiovascular diseases, found that green tea catechins, particularly (-)-epigallocatechin gallate, interfere with the emulsification, digestion, and micellar solubilization of lipids, critical steps involved in the intestinal absorption of dietary fat, cholesterol, and other lipids. Based on the observations, it is likely that green tea or its catechins lower the absorption and tissue accumulation of other lipophilic organic compounds, according to "Green tea as inhibitor of the intestinal absorption of lipids: potential mechanism for its lipid-lowering effect" by Koo SI, Noh SK.(5)

6. Antiviral activities
In the observation of Catechin derivatives including (-)-epicatechin gallate (ECG), (-)-epigallocatechin gallate (EGCG), (-)-epigallocatechin (EGC) and green tea extract (GTE) and theirs inhibition of the activities of cloned human immunodeficiency virus type 1 reverse transcriptase (HIV-1 RT), duck hepatitis B virus replication complexes reverse transcriptase (DHBV RCs RT), herpes simplex virus 1 DNA polymerase (HSV-1 DNAP) and cow thymus DNA polymerase alpha (CT DNAP alpha, found that GCG exerts a mixed inhibition with respect to external template inducer poly (rA).oligo (dT) 12-18 and a noncompetitive inhibition with respect to substrate dTTP for HIV-1 RT. Bovine serum albumin significantly reduced the inhibitory effects of catechin analogues and GTE on HIV-1 RT. In tissue culture GTE inhibited the cytopathic effect of coxsackie B3 virus, but did not inhibit the cytopathic effects of HSV-1, HSV-2, influenza A or influenza B viruses, according to "[The inhibitory effects of catechin derivatives on the activities of human immunodeficiency virus reverse transcriptase and DNA polymerases].[Article in Chinese]" by Tao P.(6)

7. Metabolic syndrome
In the investigation of Tea catechins, including the gallate esters of catechins, (-)-epicatechin gallate (ECG) and (-)-epigallocatechin gallate (EGCG). in reducing serum cholesterol concentrations and suppressing postprandial hypertriacylglycerolemia in experimental animals and humans, found that tea catechins and heat-treated tea catechins with the galloyl moiety improve lipid metabolism and contribute to the prevention of the metabolic syndrome, according to "Multifunctional effects of green tea catechins on prevention of the metabolic syndrome" by Ikeda I.(7)

8. Cognitive effects
in the examination of examined whether long-term administration of green tea catechins [Polyphenon E (PE): 63% of epigallocatechin-3-gallate, 11% of epicatechin, 6% of (-)-epigallocatechin and 6% of (-)-epicatechin-gallate] prevents cognitive impairment in an animal model of AD, rats infused with Abeta1-40 into the cerebral ventricle, found that rats with preadministered PE had higher ferric-reducing antioxidation power of plasma as compared with the Vehicle group. Our results suggest that long-term administration of green tea catechins provides effective prophylactic benefits against Abeta-induced cognitive impairment by increasing antioxidative defenses, according to "Green tea catechins prevent cognitive deficits caused by Abeta1-40 in rats" by Haque AM, Hashimoto M, Katakura M, Hara Y, Shido O.(8)

9. Cholesterol
In the examination of the influence of green tea extract, epicatechin (EC), epicatechin galate (ECG) as well as epigallocatechin galate (EGCG) on oxidative modifications of LDL of human blood serum, found that Catechins and green tea abilities to protect lipophilic antioxidant--alpha-tocopherol against oxidation have been also examined. The results reveal that peroxidation of LDL is markedly prevented by green tea extract and in a slightly weaker way by catechins (EGCG in particular), which is manifested by a decrease in concentration of conjugated dienes, lipid hydroperoxides, MDA, dityrosine and by an increase in tryptophan content, according to "The comparison of effect of catechins and green tea extract on oxidative modification of LDL in vitro" by Ostrowska J, Skrzydlewska E.(9)

10. Anti diabetes
In the observation of the effect of tea catechins (epigallocatechin gallate (EGCG), epigallocatechin (EGC), epicatechin gallate (ECG) and epicatechin (EC)) on markers of oxidative stress (malondialdehyde (MDA), reduced glutathione (GSH) and membrane -SH group) in erythrocytes from type 2 diabetics, found that tea catechins protect erythrocytes from t-BHP-induced oxidative stress, the effect being more pronounced in diabetic erythrocytes. The relative effectiveness of individual catechins are in the order of EGCG>ECG>EGC>EC. 7. We hypothesise that a higher intake of catechin-rich food by diabetic patients may provide some protection against the development of long-term complications of diabetes, according to "Protective role of tea catechins against oxidation-induced damage of type 2 diabetic erythrocytes" by Rizvi SI, Zaid MA, Anis R, Mishra N.(10)

11. Antioxidants
In the evaluation of the effects of the main polyphenolic components extracted from green tea leaves, i.e. (-)-epicatechin (EC), (-)-epigallocatechin (EGC), (-)-epicatechin gallate (ECG), (-)-epigallocatechin gallate (EGCG) and gallic acid (GA), against free radical initiated peroxidation of human low density lipoprotein (LDL), found that The antioxidative action of the green tea polyphenols includes trapping the initiating and/or propagating peroxyl radicals with the activity sequence EC>EGCG>ECG>EGC>GA for the AAPH initiated peroxidation, and reducing the alpha-tocopheroxyl radical to regenerate alpha-tocopherol with the activity sequence of ECG>EC>EGCG>EGC>GA and ECG>EGCG>GA>EC>EGC for the AAPH-initiated and BP-photosensitized peroxidations respectively, according to "Antioxidative effects of green tea polyphenols on free radical initiated and photosensitized peroxidation of human low density lipoprotein" by Liu Z, Ma LP, Zhou B, Yang L, Liu ZL.(11)

12. Etc.
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Sources
(1) http://www.ncbi.nlm.nih.gov/pubmed/22280355
(2) http://www.ncbi.nlm.nih.gov/pubmed/17017850
(3) http://www.ncbi.nlm.nih.gov/pubmed/18657514
(4) http://www.ncbi.nlm.nih.gov/pubmed/20176036
(5) http://www.ncbi.nlm.nih.gov/pubmed/17296491
(6) http://www.ncbi.nlm.nih.gov/pubmed/1284389
(7) http://www.ncbi.nlm.nih.gov/pubmed?term=epicatechin%20gallate%20and%20fat%20oxidation
(8) http://www.ncbi.nlm.nih.gov/pubmed?term=epicatechin%20gallate%20and%20coginive%20effects
(9) http://www.ncbi.nlm.nih.gov/pubmed/17357329
(10) http://www.ncbi.nlm.nih.gov/pubmed/15730438
(11) http://www.ncbi.nlm.nih.gov/pubmed/10878235

Phytochemicals in foods - 12 Health Benefits of Epigallocatechin gallate (EGCG)

Epigallocatechin gallate (EGCG), including catechins, is phytochemicals of Flavan-3-ols, in the group of Flavonoids (polyphenols) found abundantly catechin in green tea.

Health Benefits
1. Anti-human immunodeficiency virus type-1 (HIV-1)
In the investigation of the investigated possible anti-human immunodeficiency virus type-1 (HIV-1) activity of EGCg and its mechanisms of action in the viral life cycle. EGCg, found that EGCg had a destructive effect on the viral particles, and post-adsorption entry and RT in acutely infected monocytoid cells were significantly inhibited at concentrations of EGCg greater than 1 μM, and protease kinetics were suppressed at a concentration higher than 10 μM in the cell-free study. Viral production by THP-1 cells chronically-infected with HIV-1 was also inhibited in a dose-dependent manner and the inhibitory effect was enhanced by liposome modification of EGCg, according to "Inhibitory effects of (−)-epigallocatechin gallate on the life cycle of human immunodeficiency virus type 1 (HIV-1)" by Koushi Yamaguchi, Mitsuo Honda,Hajime Ikigai,Yukihiko Hara, Tadakatsu Shimamura(1)

2. Breast cancer
In the investigation of the effect of Epigallocatechin-3-gallate (EGCG) against the initiation, progression, and invasion of carcinogenesis of MMP-9 in the human breast cancer cell line, found that EGCG treatment reduced the activity, protein, and mRNA expression ofMMP-9 and enhanced the expression of the tissue inhibitor of MMP 1 (TIMP-1). EGCG downregulated the activation of focal adhesion kinase (FAK) and extracellular regulated kinase (ERK), reduced the adhesion of MDA-MB-231 cells to fibronectin and vitronectin, and reduced the mRNA expression of the integrin receptors alpha5beta1 and alphavbeta3 and concluded that EGCG as a potential inhibitor of the expression and activity of MMP-9 by a process involving FAK/ERK and transcription factorsin MDA-MB-231, according to "Epigallocatechin-3-gallate (EGCG) downregulates gelatinase-B (MMP-9) by involvement of FAK/ERK/NFkappaB and AP-1 in the human breast cancer cell line MDA-MB-231" by Sen T, Dutta A, Chatterjee A.(2)

3. Anti inflammatory effects
In the investigation of investigate the effect of EGCG on the expression of fibrogenic factors and whether EGCG attenuates the severity of oxidative stress and inflammatory response in chronic liver injury, found that Treatment with EGCG significantly reduced liver injury, oxidative stress and the inflammatory response. EGCG also significantly reduced the formation of collagen in the liver, the expression of alpha-SMA and all of the assayed pro-fibrogenic markers except TIMP-2 and MMP-9. EGCG significantly attenuated the severity of CCl(4)-induced liver injury and the progression of liver fibrosis. The protective effect of EGCG may in part be a consequence of the reduction in oxidative stress and the pro-inflammatory response, according to "Epigallocatechin-3-gallate (EGCG) reduces liver inflammation, oxidative stress and fibrosis in carbon tetrachloride (CCl4)-induced liver injury in mice" by Tipoe GL, Leung TM, Liong EC, Lau TY, Fung ML, Nanji AA.(3)

4. Cardiovascular disease
In the examination of the cellular and molecular mechanisms of cardiovascular protection of green tea polyphenols, particularly epigallocatechin gallate (EGCG), found that The protective effect of EGCG is due to its ability to decrease lipid peroxidation, oxidative stress and the production of nitric oxide (NO) radicals by inhibiting the expression of iNOS. EGCG also ameliorates the overproduction of pro-inflammatory cytokines and mediators, reduces the activity of NF-kappaB and AP-1 and the subsequent formation of peroxynitrite with NO and reactive oxygen species. Thus, EGCG effectively mitigates cellular damage by lowering the inflammatory reaction and reducing the lipid peroxidation and NO generated radicals leading to the oxidative stress. Green tea is proposed to be a dietary supplement in the prevention of cardiovascular diseases in which oxidative stress and proinflammation are the principal causes, according to "Green tea polyphenols as an anti-oxidant and anti-inflammatory agent for cardiovascular protection' by Tipoe GL, Leung TM, Hung MW, Fung ML.(4)

5. Sjogren’s syndrome (SS)
In the evuation of the Protection of glandular acinar cells from autoimmune-induced damage to Sjogren’s syndrome (SS) patients, found that EGCG is able to protect the NOD mouse submandibular glands from autoimmune-induced inflammation, and reduces serum autoantibody levels. Abnormal proliferation, rather than apoptosis, appears to be a characteristic of the NOD mouse gland that is normalized by EGCG, according to "

Effects of oral consumption of the green tea polyphenol EGCG in a murine model for human Sjogren’s syndrome, an autoimmune disease" by Kevin Gillespie, DMD, Isamu Kodani, MD, PhD, Douglas P. Dickinson, PhD, Kalu U.E. Ogbureke, MD, PhD, Amy M. Camba, BS, Mengjie Wu, DMD, PhD, Stephen Looney, PhD, Tin-Chun Chu, Haiyan Qin, MS, Frederick Bisch, DMD, Mohamed Sharawy, PhD, George S. Schuster, DDS, PhD, and Stephen D. De Hsu, PhD (5)

6. Endometriosis
In the investigation of the effects of EGCG on angiogenesis signal transduction were further characterized in a human endothelial cell line, found that EGCG, but not vitamin E, inhibited microvessels in endometriotic implants. EGCG selectively suppressed vascular endothelial growth factor C (VEGFC) and tyrosine kinase receptor VEGF receptor 2 (VEGFR2) expression. EGCG down-regulated VEGFC/VEGFR2 signaling through c-JUN, interferon-γ, matrix metalloproteinase 9, and chemokine (C-X-C motif) ligand 3 pathways for endothelial proliferation, inflammatory response, and mobility. EGCG also suppressed VEGFC expression and reduced VEGFR2 and ERK activation in endothelial cells. VEGFC supplementation attenuated the inhibitory effects by EGCG, according to "Green tea epigallocatechin-3-gallate inhibits angiogenesis and suppresses vascular endothelial growth factor C/vascular endothelial growth factor receptor 2 expression and signaling in experimental endometriosis in vivo" by Hui Xu, M.D., Ph.D., Christian M. Becker, M.D., Wai Ting Lui, M.Phil., Ching Yan Chu, M.Phil., Tina N. Davis, Andrew L. Kung, M.D., Ph.D., Amy E. Birsner, Ph.D., Robert J. D’Amato, M.D., Ph.D., Gene Chi Wai Man, M.Phil., Chi Chiu Wang, M.D., Ph.D.(6)

7. Chronic neuropathic pain
In the analyzing the effect of epigallocatechin gallate (EGCG) on spinal inflammation and immune response in neuropathic pain, found that the TLR4 signaling pathway plays an important role in the occurrence and development of neuropathic pain, and the therapy targeting TLR4 might be a novel strategy in the treatment of neuropathic pain, according to "Effects of intrathecal epigallocatechin gallate, an inhibitor of Toll-like receptor 4, on chronic neuropathic pain in rats" by Kuang X, Huang Y, Gu HF, Zu XY, Zou WY, Song ZB, Guo QL.(7)

8. Acute neurocognitive effects
In the investigationwhether the flavonoid epigallocatechin gallate (EGCG) modulates brain activity and self-reported mood in a double-blind, placebo controlled crossover study,
found that EGCG administration was associated with a significant overall increase in alpha, beta and theta activity, also reflected in overall EEG activity, more dominant in midline frontal and central regions, specifically in the frontal gyrus and medial frontal gyrus. In comparison to placebo the EGCG treatment also increased self-rated calmness and stress, according to "Acute neurocognitive effects of epigallocatechin gallate (EGCG)" by Scholey A, Downey LA, Ciorciari J, Pipingas A, Nolidin K, Finn M, Wines M, Catchlove S, Terrens A, Barlow E, Gordon L, Stough C.(8)

9. Antiviral activity
In examination of the synthesis and antiviral activities of various quercetin derivatives with substitution of C3, C3', and C5 hydroxyl functions with various phenolic ester, alkoxy, and aminoalkoxy moieties, found that newly synthesized compounds, quercetin-3-gallate which is structurally related toEGCG showed comparable antiviral activity against influenza virus (porcine H1N1 strain) to that of EGCG with improved in vitro therapeutic index, according to "Synthesis and antiviral activity of substituted quercetins" by Thapa M, Kim Y, Desper J, Chang KO, Hua DH.(9)

10. Pro-apoptotic and anti-inflammatory properties
In the comparison of mouse mammary carcinoma (BA) cells and transplanted BA tumors growing in C3H mice, treated with PH-mediated PDT and select groups of treated cells and mice also received EGCG and then cytotoxicity, tumor response, and expression of survival molecules were evaluated in all experimental groups, found that the polyphenol EGCG improves PDT efficacy by increasing tumor apoptosis and decreasing expression of pro-survival and angiogenic molecules within the tumor microenvironment, according to "Pro-apoptotic and anti-inflammatory properties of the green tea constituent epigallocatechin gallate increase photodynamic therapy responsiveness" by Ferrario A, Luna M, Rucker N, Wong S, Gomer CJ.(10)

11. Neuroprotective effects
In the evaluation of whether the green tea extract, epigallocatechin gallate (EGCG), could prevent an ovariectomy-induced overactive bladder, found that ovary hormone deficiency induced overactive bladder dysfunction via intramural nerve damage and muscarinic receptor overexpression. EGCG prevented ovariectomy-induced bladder dysfunction through neuroprotective effects in a dose-dependent fashion, according to "Neuroprotection of green tea catechins on surgical menopause-induced overactive bladder in a rat model" by Juan YS, Chuang SM, Long CY, Chen CH, Levin RM, Liu KM, Huang CH.(11)

12. Alzheimer's Disease
In the evaluation of the effect in Alzheimer's Disease, after internalization of Aβ(42) into human neuroblastoma (SH-EP) cells, with moderately intense 670-nm laser light (1000 Wm(-2)) and/or treated with epigallocatechin gallate (EGCG), found that irradiation with moderate levels of 670-nm light and EGCG supplementation complementarily reduces Aβ aggregates in SH-EP cells. Transcranial penetration of moderate levels of red to near-infrared (NIR) light has already been amply exploited in the treatment of patients with acute stroke; the blood-brain barrier (BBB) penetration of EGCG has been demonstrated in animals. We hope that our approach will inspire a practical therapy for AD, according to "670 nm Laser Light and EGCG Complementarily Reduce Amyloid-β Aggregates in Human Neuroblastoma Cells: Basis for Treatment of Alzheimer's Disease?" by Sommer AP, Bieschke J, Friedrich RP, Zhu D, Wanker EE, Fecht HJ, Mereles D, Hunstein W.(12)

13. Etc.

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Phytochemicals in foods - 13 Health Benefits of Theaflavin

Theaflavin with reddish in color, is a phytochemical of Flavan-3-ols, in the group of Flavonoids (polyphenols), formed in tea leaves during fermentation.

Health Benefits
1. Skin cancer
In the investigation of the tumor-inhibiting property of black tea polyphenol, theaflavin, found that The treatment of theaflavin downregulated the gelatinolytic activity, mRNA and protein expression of MMP-2. It reduced the mRNA and protein expression of membrane type-1 MMP (MT1-MMP) and induced mRNA and protein expression of tissue inhibitor of MMP-2 (TIMP-2), suggesting theaflavin's inhibitory effect on MMP-2 activation. Theaflavin reduced the binding of A375 cell to ECM ligands demonstrating that theaflavin treatment hinders cell-ECM adhesion, cell motility, and integrin-mediated MMP-2 activation, according to "Black tea polyphenol (theaflavin) downregulates MMP-2 in human melanoma cell line A375 by involving multiple regulatory molecules" by Sil H, Sen T, Moulik S, Chatterjee A.(1)

2. Anti cancers
In the review of anti-tumor p53 functions by dietary plant polyphenols particularly black tea and its active component theaflavins, by dietary plant polyphenols particularly black tea and its active component theaflavins has gained immense recognition from the point of view of both efficacy and safety, indicated that the review discusses about the possible role of theaflavin-p53 cross talk in targeting CSCs. Such attempts to target the complexities of p53 functions during neogenesis will be of immense help in developing a "new" strategy for successful cancer prevention and therapy by theaflavins, according to "Operation 'p53 Hunt' to combat cancer: Theaflavins in action" by Mohanty S, Adhikary A, Chakrabarty S, Sa G, Das T.(2)

3. Anti-oxidant, anti-inflammatory, and anti-apoptotic activities
In the investigation of the role of theaflavin, a polyphenol substance extracted from black tea, in attenuating acute I/R injury in a fatty liver model, found that theaflavin significantly diminished the ROS production of steatotic hepatocytes and TNF-α production by LPS-stimulated RAW264.7 cells and concluded that theaflavin has protective effects against I/R injury in fatty livers by anti-oxidant, anti-inflammatory, and anti-apoptotic mechanisms, according to "Theaflavin attenuates ischemia-reperfusion injury in a mouse fatty liver model" by

Luo XY, Takahara T, Hou J, Kawai K, Sugiyama T, Tsukada K, Takemoto M, Takeuchi M, Zhong L, Li XK.(3)

4. HIV-1 infection
In the investigation of the mechanism by which TFmix inhibits HIV-1 infection was investigated using time-of-addition, found that TFmix is an economic natural product preparation containing high content of theaflavins with potent anti-HIV-1 activity by targeting the viral entry step through the disruption of gp41 6-HB core structure. It has a potential to be developed as a safe and affordable topical microbicide for preventing sexual transmission of HIV, according to "A natural theaflavins preparation inhibits HIV-1 infection by targeting the entry step: Potential applications for preventing HIV-1 infection" by Yang J, Li L, Tan S, Jin H, Qiu J, Mao Q, Li R, Xia C, Jiang ZH, Jiang S, Liu S.(4)

5. Cholesterol
In the investigation of 240 men and women 18 years or older on a low-fat diet with mild to moderate hypercholesterolemia were randomly assigned to receive a daily capsule containing theaflavin-enriched green tea extract (375 mg) or placebo for 12 weeks, found that after 12 weeks, the mean ± SEM changes from baseline in total cholesterol, LDL-C, HDL-C, and triglyceride levels were -11.3% ± 0.9% (P = .01), -16.4% ± 1.1% (P = .01), 2.3% ± 2.1% (P = .27), and 2.6% ± 3.5% (P = .47), respectively, in the tea extract group. The mean levels of total cholesterol, LDL-C, HDL-C, and triglycerides did not change significantly in the placebo group. No significant adverse events were observed, according to "Cholesterol-Lowering Effect of a Theaflavin-Enriched Green Tea Extract" by David J. Maron, MD; Guo Ping Lu, MD; Nai Sheng Cai, MD; Zong Gui Wu, MD; Yue Hua Li, MD; Hui Chen, MD; Jian Qiu Zhu, MD; Xue Juan Jin, MS; Bert C. Wouters, MA; Jian Zhao, PhD.(5)

6. Parkinson's disease
In the assessment of the effect of theaflavin against MPTP/p induced neurodegenaration in C57BL/6 mice, found that theaflavin attenuates MPTP/p induced apoptosis and neurodegeneration as evidenced by increased expression of nigral tyrosine hydroxylase (TH), dopamine transporter (DAT) and reduced apoptotic markers such as caspase-3, 8, 9 accompanied by normalized behavioral characterization. This may be due to anti oxidative and anti apoptotic activity, according to "Theaflavin, a black tea polyphenol, protects nigral dopaminergic neurons against chronic MPTP/probenecid induced Parkinson's disease" by Anandhan A, Tamilselvam K, Radhiga T, Rao S, Essa MM, Manivasagam T.(6)

7. Antioxidant effects
In the investigation of four main TF derivatives (theaflavin (TF(1)), theaflavin-3-gallate (TF(2)A), theaflavin-3'-gallate (TF(2)B), and theaflavin-3,3'-digallate (TF(3))) in scavenging reactive oxygen species (ROS) in vitro, their properties of inhibiting superoxide, singlet oxygen, hydrogen peroxide, and the hydroxyl radical, and their effects on hydroxyl radical-induced DNA oxidative damage, found that compared with (-)-epigallocatechin gallate (EGCG), TF derivatives were good antioxidants for scavenging ROS and preventing the hydroxyl radical-induced DNA damage in vitro. TF(3) was the most positive in scavenging hydrogen peroxide and hydroxyl radical, and TF(1) suppressed superoxide. Positive antioxidant capacities of TF(2)B on singlet oxygen, hydrogen peroxide, hydroxyl radical, and the hydroxyl radical-induced DNA damage in vitro were found, according to "Evaluation of the antioxidant effects of four main theaflavin derivatives through chemiluminescence and DNA damage analyses" by Wu YY, Li W, Xu Y, Jin EH, Tu YY.(7)

8. Antibacterial effects
in the evaluation of the antibacterial effects of various concentrations of theaflavin as well as combinations of theaflavin and epicatechin, using the disk diffusion assay, found that strong antibacterial activity of theaflavin against eight clinical isolates of S. maltophilia and A. baumannii. Significant synergy (P≤0.05) was also observed between theaflavin and epicatechin against all isolates, according to "Antibacterial effects of theaflavin and synergy with epicatechin against clinical isolates of Acinetobacter baumannii and Stenotrophomonas maltophilia" by Betts JW, Kelly SM, Haswell SJ.(8)

9. Gastric ulcer healing
In the investigation of black tea (BT) and its constituent theaflavins (TFs) during their healing action against indomethacin-induced stomach ulceration in mice, found that Treatment with BT (40 mg/kg) and TF (1 mg/kg) for 3 days reversed these parameters and provided excellent (78-81%) ulcer healing. However, alterations of NOS expressions and levels of selectins and CAMs were only partially responsible for the excellent healing capacity (∼80%) of omeprazole (3 mg/kg × 3 days), according to "Black tea and theaflavins suppress various inflammatory modulators and i-NOS mediated nitric oxide synthesis during gastric ulcer healing" by Adhikary B, Yadav SK, Chand S, Bandyopadhyay SK, Chattopadhyay S.(9)

10. Cardio-protective activities
In the analyzing the protective effect of theaflavin (TF1) and its underlying mechanism,
found that (1) compared with the control group, TF1 (10, 20, 40 μmol/l) displayed a better recovery of cardiac function after ischemia/reperfusion in a concentration-dependent manner. At 60 min of reperfusion, LVDP, ± LVdP/dt (max) and CF in the TF1 group were much higher than those in the control group, whereas left ventricular end-diastolic pressure (LVEDP) in the TF1 group was lower than that in the control group (P < 0.01). (2) Pretreatment with glibenclamide (10 μmol/l), a K(ATP) antagonist, completely abolished the cardioprotective effects of TF1 (20 μmol/l). Also, most of the effects of TF1 (20 μmol/l) on cardiac function after 60 min of reperfusion were reversed by 5-HD (100 μmol/l), a selective mitochondria K(ATP) antagonist. (3) Atractyloside (20 μmol/l), a mitochondrial permeability transition pore (mPTP) opener, administered at the beginning of 15 min of reperfusion completely abolished the cardioprotection of TF1 (20 μmol/l), according to "ATP-dependent potassium channels and mitochondrial permeability transition pores play roles in the cardioprotection of theaflavin in young rat" by Ma H, Huang X, Li Q, Guan Y, Yuan F, Zhang Y.(10)

11. Cervical cancer
In the study of antiproliferative activity of theaflavins in cervical carcinoma HeLa cells and their effects on cellular microtubules and purified goat brain tubulin, found that in vitro, polymerization of purified tubulin into microtubules was also inhibited by theaflavins with an IC(50) value of 78 ± 2.43 μg/mL (P < 0.01). Thus, disruption of cellular microtubule network of HeLa cells through microtubule depolymerization may be one of the possible mechanisms of antiproliferative activity of theaflavins, according to " Theaflavins depolymerize microtubule network through tubulin binding and cause apoptosis of cervical carcinoma HeLa cells" by Chakrabarty S, Das A, Bhattacharya A, Chakrabarti G.(11)

12. Allergic effects
In the determination of the preventive effects of black tea theaflavins, theaflavin-3-gallate (3-TF) and theaflavin-3,3'-digallate (TFDG), on oxazolone-induced type IV allergy in male ICR mice, found that the anti-allergic mechanisms of action of theaflavins involve inhibition of the fluctuations of cytokines and maintenance of antioxidant status in allergic mice, according to "Preventive effects of black tea theaflavins against mouse type IV allergy" by Yoshino K, Yamazaki K, Sano M.(12)

13. Alzheimer's disease and obesity
In the investigation of the effect of Theaflavin and the symptoms of Alzheimer's disease and reduce the body weight of obese individuals, found that Clearly TH(2) inhibits PAI-1 and might play a role in slowing down the progression of Alzheimer's disease or obesity by a PAI-1-dependent pathway. While the clinical value of TH(2) has not been proven, long-term prospective studies assessing its efficacy are warranted due to the benign nature of the substance, according to "Theaflavin digallate inactivates plasminogen activator inhibitor: could tea help in Alzheimer's disease and obesity?" by Skrzypczak-Jankun E, Jankun J.(13)

14. Etc.

Phytochemicals in Foods- 8 Health Benefits of Theaflavin-3-gallate

Theaflavin-3-gallate, a theaflavin derivative, is phytochemicals of Flavan-3-ols, in the group of Flavonoids (polyphenols) found abundantly in black tea.

Health benefits
1. Antioxidant capacities
In the comparison of TF derivatives (theaflavin (TF(1)), theaflavin-3-gallate (TF(2)A), theaflavin-3'-gallate (TF(2)B), and theaflavin-3,3'-digallate (TF(3))) in scavenging reactive oxygen species (ROS) in vitro, indicated that positive antioxidant capacities of TF(2)B on singlet oxygen, hydrogen peroxide, hydroxyl radical, and the hydroxyl radical-induced DNA damage in vitro were found, according to "Evaluation of the antioxidant effects of four main theaflavin derivatives through chemiluminescence and DNA damage analyses" by Wu YY, Li W, Xu Y, Jin EH, Tu YY.(1)

2. Cholesterol
In the study of Theaflavins, which are formed in the production of black tea, have been suggested being responsible for the blood-cholesterol-lowering (BCL), found that Ultracentrifugation and HPLC analysis revealed that the pellets contained mainly theaflavin-3-gallate, while the remaining theaflavins were found to be present in the supernatant. Using purified theaflavin subtypes confirmed that mainly theaflavin-3-gallate is responsible for multilamellar vesicle formation. These results show that theaflavins can play a role in decreased intestinal cholesterol absorption via inhibition of micelle formation, according to "Theaflavins from black tea, especially theaflavin-3-gallate, reduce the incorporation of cholesterol into mixed micelles" by Vermeer MA, Mulder TP, Molhuizen HO.(2)

3. Antimicrobial activities
In the evaluation of the antimicrobial activities of seven green tea catechins and four black tea theaflavins, found that (-)-gallocatechin-3-gallate, (-)-epigallocatechin-3-gallate, (-)-catechin-3-gallate, (-)-epicatechin-3-gallate, theaflavin-3, 3'-digallate, theaflavin-3'-gallate, and theaflavin-3-gallate showed antimicrobial activities at nanomolar levels; (ii) most compounds were more active than were medicinal antibiotics, such as tetracycline or vancomycin, at comparable concentrations; (iii) the bactericidal activities of the teas could be accounted for by the levels of catechins and theaflavins as determined by high-pressure liquid chromatography; (iv) freshly prepared tea infusions were more active than day-old teas; and (v) tea catechins without gallate side chains, gallic acid and the alkaloids caffeine and theobromine also present in teas, and herbal (chamomile and peppermint) teas that contain no flavonoids are all inactive, according to "Antimicrobial activities of tea catechins and theaflavins and tea extracts against Bacillus cereus" by Friedman M, Henika PR, Levin CE, Mandrell RE, Kozukue N.(3)

4. Edema, 5. anti inflammation
found that a single topical application of equimolar of black tea constituents (TF, theaflavin-3-gallate, theaflavin-3'-gallate, and theaflavin-3,3'-digallate) strongly inhibited TPA-induced edema of mouse ears. Application of TFs mixture to mouse ears 20 min prior to each TPA application once a day for 4 days inhibited TPA-induced persistent inflammation, as well as TPA-induced increase in IL-1beta and IL-6 protein levels. TFs also inhibited arachidonic acid (AA) metabolism via both cyclooxygenase (COX) and lipoxygenase pathways, according to "Inhibitory effects of black tea theaflavin derivatives on 12-O-tetradecanoylphorbol-13-acetate-induced inflammation and arachidonic acid metabolism in mouse ears" by Huang MT, Liu Y, Ramji D, Lo CY, Ghai G, Dushenkov S, Ho CT.(4)

6. Allergic effect
In the investigation of the preventive effects of black tea theaflavins, theaflavin-3-gallate (3-TF) and theaflavin-3,3'-digallate (TFDG), on oxazolone-induced type IV allergy in male ICR mice.
found that oral administration of 3-TF(theaflavin-3-gallate) and TFDG at a dose of 50 mg kg(-1) body weight prevented the increases in levels of some proinflammatory cytokines, interleukin-12 (IL-12), interferon-gamma (IFN-gamma), and tumour necrosis factor-alpha (TNF-alpha), according to "Preventive effects of black tea theaflavins against mouse type IV allergy" by Yoshino K, Yamazaki K, Sano M.(5)

7. Anti cancers
In the investigation of the inhibition effects of tea theaflavins complex (TFs), theaflavin-3-3'-digallate (TFDG), theaflavin-3'-gallate (TF2B), and an unidentified compound (UC) on the growth of human liver cancer BEL-7402 cells, gastric cancer MKN-28 cells and acute promyelocytic leukemia LH-60 cells, found that the inhibition effects of theaflavin-3'-gallate (TF2B), TFDG, and UC on BEL-7402 and MKN-28 were stronger than TFs. The relationship coefficients between monomer concentration and its inhibition rate against MKN-28 and BEL-7402 were 0.87 and 0.98 for TF2B, 0.96 and 0.98 for UC, respectively. The IC50 values of TFs, TF2B, and TFDG were 0.18, 0.11, and 0.16 mM on BEL-7402 cells, and 1.11, 0.22, and 0.25 mM on MKN-28 cells respectively, according to "The theaflavin monomers inhibit the cancer cells growth in vitro" by Tu YY, Tang AB, Watanabe N.(6)

8. Leukemia
in the investigation of the inhibitory effects of five tea polyphenols, namely theaflavin (TF1), theaflavin-3-gallate (TF2), theaflavin-3,3'-digallate (TF3), (-)-epigallocatechin-3-gallate (EGCG), and gallic acid, and propyl gallate (PG) on xanthine oxidase (XO) found that Tea polyphenols and PG all have potent inhibitory effects (>50%) on PMA-stimulated superoxide production at 20 approximately 50 microM in HL-60 cells. Gallic acid (GA) showed no inhibition under the same conditions. At 10 microM, only EGCG, TF3, and PG showed significant inhibition with potency of PG > EGCG > TF3, according to "Inhibition of xanthine oxidase and suppression of intracellular reactive oxygen species in HL-60 cells by theaflavin-3,3'-digallate, (-)-epigallocatechin-3-gallate, and propyl gallate" by Lin JK, Chen PC, Ho CT, Lin-Shiau SY.(7)

9. Etc.

Pharmacy In Vegetables
Use the science behind the health benefits of vegetables
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