scholarly journals Exploring Inhibitory Mechanisms of Green Tea Catechins as Inhibitors of a Cancer Therapeutic Target, Nuclear Factor-κB (NF-κB)

2019 ◽  
Vol 16 (04) ◽  
pp. 715-723
Author(s):  
Mohd Suhail ◽  
Asma parveen ◽  
Amjad Husain ◽  
Mohd Rehan
Keyword(s):  
Transcription Factor ◽  
Green Tea ◽  
Therapeutic Target ◽  
Epigallocatechin Gallate ◽  
Nuclear Factor Κb ◽  
Nuclear Factor ◽  
Epicatechin Gallate ◽  
Tea Catechins ◽  
Green Tea Catechins ◽  
Cancer Types

Nuclear factor kappa B (NF-κB), a transcription factor is a well-established cancer therapeutic target. NF-κB’s linkage with cancer is known through the constitutive activation of NF-κB in several cancer types. The most important role of NF-κB as a transcription factor is its ability to promote cell survival through the induction of transcription of target pro-survival genes and thus inhibition of programmed cell death (PCD) by resulting proteins in both malignant and normal cells. Current findings have unveiled that green tea catechins exert anticancer effect by inhibiting the activity of various receptors including NF-κB. The current study is designed to gain the structural insights for inhibitory mechanism of catechin derivatives against NF-κB. The major green tea catechins include (-)-epicatechin (EC), (-)-epigallocatechin (EGC), (-)-epicatechin gallate (ECG), and (-)-epigallocatechin gallate (EGCG) and are included in the current study. The study explored the binding pose, interacting residues, molecular interactions, and predicted binding energy and dissociation constant for the catechin derivatives. Our results showed that the catechin derivatives bound well in the DNA binding site with adequate binding strength scores. The study suggested that the four catechin derivatives may act as potential inhibitors of NF-κB and thus, may inhibit the progression of various cancer types.

scholarly journals Molecular Rescue of Dyrk1A Overexpression Alterations in Mice with Fontup® Dietary Supplement: Role of Green Tea Catechins

2020 ◽  
Vol 21 (4) ◽  
pp. 1404 ◽  
Author(s):  
Yuchen Gu ◽  
Gautier Moroy ◽  
Jean-Louis Paul ◽  
Anne-Sophie Rebillat ◽  
Mara Dierssen ◽  
...  
Keyword(s):  
Green Tea ◽  
Epigallocatechin Gallate ◽  
Nutritional Supplement ◽  
Green Tea Extract ◽  
Epicatechin Gallate ◽  
Tea Catechins ◽  
Green Tea Catechins ◽  
Tea Extract ◽  
Vitro Effect

Epigallocatechin gallate (EGCG) is an inhibitor of DYRK1A, a serine/threonine kinase considered to be a major contributor of cognitive dysfunctions in Down syndrome (DS). Two clinical trials in adult patients with DS have shown the safety and efficacy to improve cognitive phenotypes using commercial green tea extract containing EGCG (45% content). In the present study, we performed a preclinical study using FontUp®, a new nutritional supplement with a chocolate taste specifically formulated for the nutritional needs of patients with DS and enriched with a standardized amount of EGCG in young mice overexpressing Dyrk1A (TgBACDyrk1A). This preparation is differential with previous one used, because its green tea extract has been purified to up 94% EGCG of total catechins. We analyzed the in vitro effect of green tea catechins not only for EGCG, but for others residually contained in FontUp®, on DYRK1A kinase activity. Like EGCG, epicatechin gallate was a noncompetitive inhibitor against ATP, molecular docking computations confirming these results. Oral FontUp® normalized brain and plasma biomarkers deregulated in TgBACDyrk1A, without negative effect on liver and cardiac functions. We compared the bioavailability of EGCG in plasma and brain of mice and have demonstrated that EGCG had well crossed the blood-brain barrier.

scholarly journals Green tea (−)-epigallocatechin gallate inhibits the growth of human villous trophoblasts via the ERK, p38, AMP-activated protein kinase, and protein kinase B pathways

2016 ◽  
Vol 311 (2) ◽  
pp. C308-C321 ◽  
Author(s):  
Li-Jane Shih ◽  
Tz-Fang Chen ◽  
Cheng-Kuo Lin ◽  
Hang-Shen Liu ◽  
Yung-Hsi Kao
Keyword(s):  
Protein Kinase ◽  
P38 Mapk ◽  
Green Tea ◽  
Protein Kinase B ◽  
Epigallocatechin Gallate ◽  
Cell Number ◽  
Brdu Incorporation ◽  
Tea Catechins ◽  
Green Tea Catechins ◽  
Amp Activated Protein Kinase

Green tea catechins, especially (−)-epigallocatechin gallate (EGCG), have been reported to circulate in the placenta of animals and blood of humans after consumption. Whether EGCG regulates activity of human villous trophoblasts (HVT) is unknown. This study investigated the pathways involved in EGCG modulation of trophoblast mitogenesis. EGCG inhibited trophoblast proliferation in a dose-dependent and time-dependent manner, as indicated by the number of cells and incorporation of bromodeoxyuridine (BrdU). EGCG was more effective than other green tea catechins in inhibiting cell growth. EGCG also increased the phosphorylation of the MAPK pathway proteins, ERK1/2, and p38, but not JNK. Furthermore, EGCG had no effects on the total amounts of ERK1/2, p38 MAPK, and JNK proteins. This suggests that EGCG selectively affects particular MAPK subfamilies. Pretreatment with specific inhibitors of ERK1/2, p38 MAPK, and AMP-activated protein kinase (AMPK) antagonized EGCG-induced decreases in both cell number and BrdU incorporation. These inhibitors also blocked EGCG-induced increases in the levels of phospho-ERK1/2, phospho-p38, and phospho-AMPK proteins, respectively. Moreover, EGCG was similar to the phosphatidylinositol 3-kinase inhibitors wortmannin and LY-294002 to decrease protein kinase B (AKT) phosphorylation, cell number, and BrdU incorporation. These data imply that EGCG inhibits the growth of HVT through the ERK, p38, AMPK, and AKT pathways.

scholarly journals Beneficial Properties of Green Tea Catechins

2020 ◽  
Vol 21 (5) ◽  
pp. 1744 ◽  
Author(s):  
Claudia Musial ◽  
Alicja Kuban-Jankowska ◽  
Magdalena Gorska-Ponikowska
Keyword(s):  
Green Tea ◽  
Antioxidant Properties ◽  
Biologically Active ◽  
Hydroxyl Groups ◽  
Molecular Signaling ◽  
Epicatechin Gallate ◽  
Tea Catechins ◽  
Green Tea Catechins ◽  
Antioxidant Agents ◽  
Anti Inflammatory

Green tea (Camellia sinesis) is widely known for its anticancer and anti-inflammatory properties. Among the biologically active compounds contained in Camellia sinesis, the main antioxidant agents are catechins. Recent scientific research indicates that the number of hydroxyl groups and the presence of characteristic structural groups have a major impact on the antioxidant activity of catechins. The best source of these compounds is unfermented green tea. Depending on the type and origin of green tea leaves, their antioxidant properties may be uneven. Catechins exhibit the strong property of neutralizing reactive oxygen and nitrogen species. The group of green tea catechin derivatives includes: epicatechin, epigallocatechin, epicatechin gallate and epigallocatechin gallate. The last of these presents the most potent anti-inflammatory and anticancer potential. Notably, green tea catechins are widely described to be efficient in the prevention of lung cancer, breast cancer, esophageal cancer, stomach cancer, liver cancer and prostate cancer. The current review aims to summarize the potential anticancer effects and molecular signaling pathways of major green tea catechins. It needs to be clearly emphasized that green tea as well as green tea catechols cannot replace the standard chemotherapy. Nonetheless, their beneficial effects may support the standard anticancer approach.

scholarly journals Green Tea Catechins Induce Inhibition of PTP1B Phosphatase in Breast Cancer Cells with Potent Anti-Cancer Properties: In Vitro Assay, Molecular Docking, and Dynamics Studies

Antioxidants ◽  
2020 ◽  
Vol 9 (12) ◽  
pp. 1208
Author(s):  
Alicja Kuban-Jankowska ◽  
Tomasz Kostrzewa ◽  
Claudia Musial ◽  
Giampaolo Barone ◽  
Giosuè Lo-Bosco ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Enzymatic Activity ◽  
Cancer Cells ◽  
Green Tea ◽  
Breast Cancer Cells ◽  
Computational Analysis ◽  
Epigallocatechin Gallate ◽  
Tea Catechins ◽  
Green Tea Catechins ◽  
Mcf 7

The catechins derived from green tea possess antioxidant activity and may have a potentially anticancer effect. PTP1B is tyrosine phosphatase that is oxidative stress regulated and is involved with prooncogenic pathways leading to the formation of a.o. breast cancer. Here, we present the effect of selected green tea catechins on enzymatic activity of PTP1B phosphatase and viability of MCF-7 breast cancer cells. We showed also the computational analysis of the most effective catechin binding with a PTP1B molecule. We observed that epigallocatechin, epigallocatechin gallate, epicatechin, and epicatechin gallate may decrease enzymatic activity of PTP1B phosphatase and viability of MCF-7 cells. Conclusions: From the tested compounds, epigallocatechin and epigallocatechin gallate were the most effective inhibitors of the MCF-7 cell viability. Moreover, epigallocatechin was also the strongest inhibitor of PTP1B activity. Computational analysis allows us also to conclude that epigallocatechin is able to interact and bind to PTP1B. Our results suggest also the most predicted binding site to epigallocatechin binding to PTP1B.

ANTIOXIDANT CHEMISTRY OF GREEN TEA CATECHINS: OXIDATION PRODUCTS OF (-)-EPIGALLOCATECHIN GALLATE AND (-)-EPIGALLOCATECHIN WITH PEROXIDASE

2007 ◽  
Vol 7 (4) ◽  
pp. 275-282 ◽  
Author(s):  
NANQUN ZHU ◽  
SHENGMIN SANG ◽  
TZOU-CHI HUANG ◽  
NAISHENG BAI ◽  
CHUNG S. YANG ◽  
...  
Keyword(s):  
Green Tea ◽  
Epigallocatechin Gallate ◽  
Oxidation Products ◽  
Tea Catechins ◽  
Green Tea Catechins

scholarly journals Efficacy of Topical Treatment with (−)-Epigallocatechin Gallate, A Green Tea Catechin, in Mice with Cutaneous Leishmaniasis

Molecules ◽  
2020 ◽  
Vol 25 (7) ◽  
pp. 1741
Author(s):  
Andrea M. Sosa ◽  
Agustín Moya Álvarez ◽  
Estefanía Bracamonte ◽  
Masataka Korenaga ◽  
Jorge D. Marco ◽  
...  
Keyword(s):  
Cutaneous Leishmaniasis ◽  
Green Tea ◽  
Topical Treatment ◽  
Epigallocatechin Gallate ◽  
Parasite Burden ◽  
Antileishmanial Activity ◽  
Control Group ◽  
Tea Catechins ◽  
Reference Drug ◽  
Green Tea Catechins

The treatment of leishmaniasis includes pentavalent antimony drugs but, because of the side effects, toxicity and cases of treatment failure or resistance, the search of new antileishmanial compounds are necessary. The aims of this study were to evaluate and compare the in vitro antileishmanial activity of four green tea catechins, and to assess the efficacy of topical (−)-epigallocatechin gallate in a cutaneous leishmaniasis model. The antileishmanial activity of green tea catechins was evaluated against intracellular amastigotes, and cytotoxicity was performed with human monocytic cell line. BALB/c mice were infected in the ear dermis with Leishmania (Leishmania) amazonensis and treated with topical 15% (−)-epigallocatechin gallate, intraperitoneal Glucantime, and control group. The efficacy of treatments was evaluated by quantifying the parasite burden and by measuring the lesions size. (−)-Epigallocatechin gallate and (−)-epigallocatechin were the most active compounds with IC50 values <59.6 µg/mL and with a selectivity index >1. Topical treatment with (−)-epigallocatechin gallate decreased significantly both lesion size and parasite burden (80.4% inhibition) compared to control group (p < 0.05), and moreover (−)-epigallocatechin gallate showed a similar efficacy to Glucantime (85.1% inhibition), the reference drug for leishmaniasis treatment.

scholarly journals Health effects of green tea catechins in overweight and obese men: a randomised controlled cross-over trial

2011 ◽  
Vol 106 (12) ◽  
pp. 1880-1889 ◽  
Author(s):  
A. L. Brown ◽  
J. Lane ◽  
C. Holyoak ◽  
B. Nicol ◽  
A. E. Mayes ◽  
...  
Keyword(s):  
Blood Pressure ◽  
Body Weight ◽  
Health Effects ◽  
Green Tea ◽  
Metabolic Flux ◽  
Epigallocatechin Gallate ◽  
Metabolic Function ◽  
Tea Catechins ◽  
Green Tea Catechins ◽  
Modifying Effect

Regular consumption of green tea may be cardioprotective. In the present study we investigated the health effects of dietary supplementation with green tea catechins and the potential modifying effect of the catechol-O-methyltransferase (COMT) Val/Met genotype. Subjects (sedentary males, aged 40–69 years, with BMI ≥  28 and ≤  38 kg/m2) were randomly assigned to consume decaffeinated green tea extract (DGT; 530 mg containing about 400 mg total catechins/capsule, twice daily) and placebo in a complete cross-over design. Ambulatory blood pressure and biomarkers of metabolic function (cholesterol, TAG, glucose and insulin) were measured at weeks 0 and 6. Although a marked increase in the concentration of plasma epigallocatechin gallate (EGCG), urinary epigallocatechin (EGC) and urinary 4′-O-methyl EGC was found after DGT treatment, no effect on blood pressure or biomarkers of metabolic function was observed. However, a period × treatment interaction (P < 0·05) was detected for body-weight change. Despite a similar increase in estimated energy intake during intervention period 1, body weight decreased by 0·64 (sd 2·2) kg and increased by 0·53 (sd 1·9) kg in the DGT and placebo groups, respectively (P = 0·025), suggesting a protective effect of green tea catechins on weight gain. Additionally, the COMT Val/Met genotype influenced urinary accumulation of EGC and 4′-O-methyl EGC (P < 0·01). Mean concentrations were lower in individuals homozygous for the high-activity G-allele, possibly reflecting increased metabolic flux and a more rapid conversion to downstream metabolic species, compared with individuals carrying at least one copy of the low-activity A-allele. Additional studies are needed to confirm these findings and further explore the modifying effect of genotype.

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