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 ◽  
...  

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.

2008 ◽  
Vol 78 (3) ◽  
pp. 242-249 ◽  
Author(s):  
Jun Xu ◽  
Jue Wang ◽  
Fei Deng ◽  
Zhihong Hu ◽  
Hualin Wang

2011 ◽  
Vol 127 (2) ◽  
pp. AB210-AB210
Author(s):  
S.J. Wu ◽  
J.I. Silverberg ◽  
H.G. Durkin ◽  
R. Joks ◽  
T.A. Smith-Norowitz

2020 ◽  
Vol 11 (4) ◽  
pp. 3105-3111
Author(s):  
So-Hee Yoo ◽  
Yeong-Eun Lee ◽  
Jin-Oh Chung ◽  
Chan-Su Rha ◽  
Yong-Deog Hong ◽  
...  

Results from the current study suggested that whole green tea components rich in flavonols and polysaccharides could be potential hypoglycemic excipient ingredients into green tea catechins by enhancing catechin absorption.


2010 ◽  
Vol 105 (8) ◽  
pp. 1138-1144 ◽  
Author(s):  
Rosalind J. Miller ◽  
Kim G. Jackson ◽  
Tony Dadd ◽  
Andrew E. Mayes ◽  
A. Louise Brown ◽  
...  

The beneficial effects of green tea catechins, such as the proposed improvement in endothelial function, may be influenced by phase II metabolism during and after absorption. The methylation enzyme, catechol-O-methyltransferase (COMT), has a missense mutation rs4680 (G to A), proposed to result in a 40 % reduction in enzyme activity. In the present pilot study, twenty subjects (ten of each homozygous COMT genotype) were recruited. Green tea extract capsules (836 mg green tea catechins) were given in a fasted state, and a high-carbohydrate breakfast was given after 60 min. Blood samples and vascular function measurements were taken at regular intervals. The change in digital volume pulse stiffness index (SI) from baseline was shown to be different between genotype groups at 120 and 240 min, with a lower SI in the GG individuals (P ≤ 0·044). The change in blood pressure from baseline also differed between genotype groups, with a greater increase in systolic (P = 0·023) and diastolic (P = 0·034) blood pressure at 120 min in the GG group. The AA group was shown to have a greater increase in insulin concentrations at 120 min (P = 0·019) and 180 min (P = 0·008) compared with baseline, despite similar glucose profiles. No genotypic differences were found in vascular reactivity measured using laser Doppler iontophoresis, total nitrite, lipids, plasma total antioxidant capacity or inflammatory markers after ingestion of the green tea extract. In conclusion, SI and insulin response to the glucose load differed between the COMT genotype groups, and this may be suggestive of a green tea extract and genotype interaction.


2017 ◽  
Vol 9 (5) ◽  
pp. 91
Author(s):  
Delly Ramadon ◽  
Seshiana Sebti Pramesti ◽  
Effionora Anwar

Objective: The aim of this study was to increase penetration of epigallocatechin gallate (EGCG) from the extract using transethosomal gel.Methods: Transethosomes (TE) formulae were made using thin layer hydration method with different concentration of green tea extract which was equivalent to 1% (F1), 1.5% (F2), and 2% (F3) of EGCG. F1 was the chosen formula to be incorporated into a gel as a transethosomal gel (TEG). A gel containing green tea extract was also made as a control called as non-transethosomal gel (NTEG). A stability test and in vitro penetration study of gels using Franz diffusion cell were performed.Results: F1 was the chosen formula because it had a spherical shape, a particle size of 112.14±2.19 nm, PDI of 0.166±0.03, a zeta potential of-52.05±1.34 mV, and %EE of 58.06±0.08%. Stability test results showed that TEG more stable than NTEG. The amount of EGCG penetrated from TEG and NTEG were 1391.16±34.89 µg/cm2 and 485.29±14.49 µg/cm2, respectively (p<0.05). The lag time for TEG was around 0.99±0.2 h, while NTEG was 8.69±0.2 h (p<0.05).Conclusion: It can be concluded that transethosomes can improve gel stability and increase the amount of EGCG penetrated through the skin.  


2019 ◽  
Vol 20 (15) ◽  
pp. 3630 ◽  
Author(s):  
Monira Pervin ◽  
Keiko Unno ◽  
Akiko Takagaki ◽  
Mamoru Isemura ◽  
Yoriyuki Nakamura

Over the last three decades, green tea has been studied for its beneficial effects, including anti-cancer, anti-obesity, anti-diabetes, anti-inflammatory, and neuroprotective effects. At present, a number of studies that have employed animal, human and cell cultures support the potential neuroprotective effects of green tea catechins against neurological disorders. However, the concentration of (−)-epigallocatechin gallate (EGCG) in systemic circulation is very low and EGCG disappears within several hours. EGCG undergoes microbial degradation in the small intestine and later in the large intestine, resulting in the formation of various microbial ring-fission metabolites which are detectable in the plasma and urine as free and conjugated forms. Recently, in vitro experiments suggested that EGCG and its metabolites could reach the brain parenchyma through the blood–brain barrier and induce neuritogenesis. These results suggest that metabolites of EGCG may play an important role, alongside the beneficial activities of EGCG, in reducing neurodegenerative diseases. In this review, we discuss the function of EGCG and its microbial ring-fission metabolites in the brain in suppressing brain dysfunction. Other possible actions of EGCG metabolites will also be discussed.


2019 ◽  
Vol 16 (04) ◽  
pp. 715-723
Author(s):  
Mohd Suhail ◽  
Asma parveen ◽  
Amjad Husain ◽  
Mohd Rehan

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.


2020 ◽  
Vol 6 (2) ◽  
Author(s):  
Lisni Noraida Waruwu ◽  
Maria Bintang ◽  
Bambang Pontjo Priosoeryanto

Green tea (Camellia sinensis) is one of traditional plants that have the potential as an anticancer. The sample used in this research commercial green tea extract. The purpose of this study was to test the antiproliferation activity of green tea extract on breast cancer cell MCM-B2 in vitro. Green tea extract fractionated using three solvents, ie water, ethanol 70%, and n-hexane. Extract and fraction of green tea water have value Lethality Concentration 50 (LC50) more than 1000 ppm. The fraction of ethanol 70% and n-hexane had an LC50 value of 883.48 ppm and 600.56 ppm, respectively. The results of the phytochemical screening of green tea extract are flavonoids, tannins, and saponins, while the phytochemical screening results of n-hexane fraction are flavonoids and tannins. Antiproliferation activity was tested on breast cancer cells MCM-B2 and normal cells Vero by trypan blue staining method. The highest MCM-B2 cell inhibitory activity was achieved at a concentration of 13000 ppm green tea extract and 1000 ppm of n-hexane fraction, 59% and 59%, respectively. The extract and n-hexane fraction of green tea are not toxic to normal Vero cells characterized by not inhibiting normal cell proliferation. Keywords: antiproliferative, cancer cell MCM-B2, commercial green tea, cytotoxicity


2011 ◽  
Vol 62 (2) ◽  
pp. 139-146 ◽  
Author(s):  
Ksenija Durgo ◽  
Sandra Kostić ◽  
Katarina Gradiški ◽  
Draženka Komes ◽  
Maja Osmak ◽  
...  

Genotoxic Effects of Green Tea Extract on Human Laryngeal Carcinoma Cells In VitroGreen tea (Camellia sinensis) contains several bioactive compounds which protect the cell and prevent tumour development. Phytochemicals in green tea extract (mostly flavonoids) scavenge free radicals, but also induce pro-oxidative reactions in the cell. In this study, we evaluated 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) and its cross-resistant cell line CK2. The aim was to see if the extract and its two flavonoids could increase the sensitivity of the cisplatin-resistant cell line CK2 in comparison to the parental cell line. The results show that EGCG and green tea extract increased the DNA damage in the CK2 cell line during short exposure. 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.


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