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https://www.readbyqxmd.com/read/28218710/substitution-at-the-c-3-position-of-catechins-has-an-influence-on-the-binding-affinities-against-serum-albumin
#1
Masaki Ikeda, Manabu Ueda-Wakagi, Kaori Hayashibara, Rei Kitano, Masaya Kawase, Kunihiro Kaihatsu, Nobuo Kato, Yoshitomo Suhara, Naomi Osakabe, Hitoshi Ashida
It is known that catechins interact with the tryptophan (Trp) residue at the drug-binding site of serum albumin. In this study, we used catechin derivatives to investigate which position of the catechin structure strongly influences the binding affinity against bovine serum albumin (BSA) and human serum albumin (HSA). A docking simulation showed that (-)-epigallocatechin gallate (EGCg) interacted with both Trp residues of BSA (one at drug-binding site I and the other on the molecular surface), mainly by π-π stacking...
February 18, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28212930/molecular-recognition-between-pancreatic-lipase-and-natural-and-synthetic-inhibitors
#2
Martiniano Bello, Lucia Basilio-Antonio, Jonathan Fragoso-Vázquez, Anaguiven Avalos-Soriano, José Correa-Basurto
Pancreatic lipase (PL) is a primary lipase critical for triacylglyceride digestion in humans and is considered as a promising target for the treatment of obesity. Although the current synthetic drugs available for treating obesity have been demonstrated to be effective in inhibiting PL, their prolonged usage results in severe side effects. Based on this argument, in this study, we evaluated the structural and energetic features linked to molecular recognition between two well-known PL inhibitors, orlistat (ORL, synthetic inhibitor) and (-)-epigallocatechin gallate (EGCG, natural inhibitor) and PL through molecular dynamics simulations and free energy calculations of ORL and EGCG at the PL binding site when it is isolated (PL) from the heterodimer complex, forming the heterodimer complex with colipase (PLCL) and lacking structural calcium...
February 16, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28211475/biofilm-formation-of-the-black-yeast-like-fungus-exophiala-dermatitidis-and-its-susceptibility-to-antiinfective-agents
#3
Lisa Kirchhoff, Maike Olsowski, Katrin Zilmans, Silke Dittmer, Gerhard Haase, Ludwig Sedlacek, Eike Steinmann, Jan Buer, Peter-Michael Rath, Joerg Steinmann
Various fungi have the ability to colonize surfaces and to form biofilms. Fungal biofilm-associated infections are frequently refractory to targeted treatment because of resistance to antifungal drugs. One fungus that frequently colonises the respiratory tract of cystic fibrosis (CF) patients is the opportunistic black yeast-like fungus Exophiala dermatitidis. We investigated the biofilm-forming ability of E. dermatitidis and its susceptibility to various antiinfective agents and natural compounds. We tested 58 E...
February 17, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28203607/epigallocatechin-gallate-a-useful-therapy-for-cognitive-disability-in-down-syndrome
#4
Fiorenza Stagni, Andrea Giacomini, Marco Emili, Sandra Guidi, Elisabetta Ciani, Renata Bartesaghi
Neurodevelopmental alterations and cognitive disability are constant features of Down syndrome (DS), a genetic condition due to triplication of chromosome 21. DYRK1A is one of the triplicated genes that is thought to be strongly involved in brain alterations. Treatment of Dyrk1A transgenic mice with epigallocatechin gallate (EGCG), an inhibitor of DYRK1A, improves cognitive performance, suggesting that EGCG may represent a suitable treatment of DS. Evidence in the Ts65Dn mouse model of DS shows that EGCG restores hippocampal development, although this effect is ephemeral...
2017: Neurogenesis (Austin, Tex.)
https://www.readbyqxmd.com/read/28198717/mitochondrial-dna-induced-inflammatory-responses-and-lung-injury-in-thermal-injury-rat-model-protective-effect-of-epigallocatechin-gallate
#5
Ruiqi Liu, Fei Xu, Si Si, Xueshan Zhao, Siwei Bi, Ying Cen
Lungs are easily damaged by the inflammatory responses induced after extensive burns. The aim here was to investigate the protective role of epigallocatechin gallate (EGCG) in mitochondrial DNA (mtDNA)-mediated inflammatory responses and acute respiratory distress syndrome (ARDS) in a rat model of thermal injury. Male Sprague-Dawley rats were randomly assigned to five groups. In the first experiment, a full-thickness thermal injury or control procedure, covering 30% of the TBSA, was inflicted on three groups designated as the thermal injury, EGCG, and sham control groups...
February 6, 2017: Journal of Burn Care & Research: Official Publication of the American Burn Association
https://www.readbyqxmd.com/read/28191529/the-green-tea-polyphenol-epigallocatechin-3-gallate-and-its-beneficial-roles-in-chronic-kidney-disease
#6
REVIEW
Hui Bao, Ai Peng
Chronic kidney disease (CKD), a condition that affects around 10% of the population, has become a significant public health concern. Current therapeutic strategies to slow down the progression of CKD remain limited. Thus, it is urgent to develop new strategies to manage the patients with CKD. Work within the past decade has improved our understanding of the mechanisms contributing to CKD. In particular, oxidative stress as well as inflammation appears to play a pivotal role in CKD progression. ()-Epigallocatechin-3-gallate (EGCG), the major catechin of green tea extract, is known as a powerful antioxidant and reactive oxygen species scavenger...
September 1, 2016: Journal of Translational Internal Medicine
https://www.readbyqxmd.com/read/28186133/green-tea-polyphenol-tailors-cell-adhesivity-of-rgd-displaying-surfaces-multicomponent-models-monitored-optically
#7
Beatrix Peter, Eniko Farkas, Eniko Forgacs, Andras Saftics, Boglarka Kovacs, Sandor Kurunczi, Inna Szekacs, Antal Csampai, Szilvia Bosze, Robert Horvath
The interaction of the anti-adhesive coating, poly(L-lysine)-graft-poly(ethylene glycol) (PLL-g-PEG) and its Arg-Gly-Asp (RGD) functionalized form, PLL-g-PEG-RGD, with the green tea polyphenol, epigallocatechin-gallate (EGCg) was in situ monitored. After, the kinetics of cellular adhesion on the EGCg exposed coatings were recorded in real-time. The employed plate-based waveguide biosensor is applicable to monitor small molecule binding and sensitive to sub-nanometer scale changes in cell membrane position and cell mass distribution; while detecting the signals of thousands of adhering cells...
February 10, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28181408/epigallocatechin-gallate-induces-an-up-regulation-of-ldl-receptor-accompanied-by-a-reduction-of-pcsk9-via-the-annexin-a2-independent-pathway-in-hepg2-cells
#8
Kohei Kitamura, Yudai Okada, Kenji Okada, Yuya Kawaguchi, Satoshi Nagaoka
SCOPE: In animal studies, epigallocatechin gallate (EGCG), the dominant catechin in green tea, has been shown to improve cholesterol metabolism. However, the molecular mechanisms of EGCG underlying these functions have not been fully understood. In this study, we aimed to clarify the molecular mechanisms of the effect of EGCG on cholesterol metabolism mainly in HepG2 cells. METHODS AND RESULTS: We found that EGCG induced a reduction of the extracellular proprotein convertase subtilisin/kexin 9 (PCSK9) level accompanied by an up-regulation of the LDL receptor (LDLR) in HepG2 cells...
February 9, 2017: Molecular Nutrition & Food Research
https://www.readbyqxmd.com/read/28177724/dose-dependent-decrease-in-mortality-with-no-cognitive-or-muscle-function-improvements-due-to-dietary-egcg-supplementation-in-aged-mice
#9
Brandt D Pence, Tushar K Bhattacharya, Pul Park, Jennifer L Rytych, Jacob M Allen, Yi Sun, Robert H McCusker, Keith W Kelley, Rodney W Johnson, Justin S Rhodes, Jeffrey A Woods
We have previously shown that a diet containing epigallocatechin gallate (EGCG) and beta-alanine is not effective in improving either cognitive or muscle function in aged (18 month) mice (Gibbons et al. Behav Brain Res 2014, Pence et al. Appl Physiol Nutr Metab 2016). However, this diet reduced oxidative stress in the brain, and previous studies using longer-term interventions and other doses have documented beneficial effects in cognitive and muscle function, especially with EGCG. Here we hypothesized that a different dose of EGCG or longer feeding period would be more efficacious in improving cognition...
January 5, 2017: Applied Physiology, Nutrition, and Metabolism, Physiologie Appliquée, Nutrition et Métabolisme
https://www.readbyqxmd.com/read/28172997/influence-of-prenatal-egcg-treatment-and-dyrk1a-dosage-reduction-on-craniofacial-features-associated-with-down-syndrome
#10
Samantha D McElyea, John M Starbuck, Danika M Tumbleson-Brink, Emily Harrington, Joshua D Blazek, Ahmed Ghoneima, Katherine Kula, Randall J Roper
No abstract text is available yet for this article.
November 15, 2016: Human Molecular Genetics
https://www.readbyqxmd.com/read/28166993/resveratrol-and-epigallocatechin-3-gallate-addition-to-thawed-boar-sperm-improves-in%C3%A2-vitro-fertilization
#11
B Gadani, D Bucci, M Spinaci, C Tamanini, G Galeati
Thawing is one of the most delicate process after semen cryopreservation as spermatozoa pass from a dormant metabolic stage to a sudden awakening in cellular metabolism. The rapid oxygen utilization leads to an overproduction of reactive oxygen species that can damage sperm cells, thus causing a significant decrease of fertilizing potential of frozen-thawed spermatozoa. Resveratrol (Res) is a natural grape-derived phytoalexin and Epigallocatechin-3-gallate (EGCG) is the major polyphenol in green tea (Camellia sinensis); both molecules are known to possess high levels of antioxidant activity...
March 1, 2017: Theriogenology
https://www.readbyqxmd.com/read/28166649/evaluation-of-plasma-antioxidant-activity-in-rats-given-excess-egcg-with-reference-to-endogenous-antioxidants-concentrations-and-assay-methods
#12
Kaori Yokotani, Keizo Umegaki
The contribution of (-)-epigallocatechin gallate (EGCg) intake to in vivo antioxidant activity is unclear, even with respect to plasma. In this study, we examined how administration of EGCg contributes to plasma antioxidant activity, relative to its concentration, endogenous antioxidants, and assay methods, namely oxygen radical absorbance capacity (ORAC) and ferric reducing/antioxidant power (FRAP). Administration of EGCg (500 mg/kg) to rats increased plasma EGCg (4 µmol/L as free form) and ascorbic acid (1...
February 6, 2017: Free Radical Research
https://www.readbyqxmd.com/read/28163906/an-elisa-dyrk1a-non-radioactive-assay-suitable-for-the-characterization-of-inhibitors
#13
Yong Liu, Tatyana Adayev, Yu-Wen Hwang
The DYRK1A (dual specificity tyrosine phosphorylation-regulated kinase 1A) gene encodes a proline-directed Ser/Thr kinase. Elevated expression and/or altered distribution of the kinase have been implicated in the neurological impairments associated with Down syndrome (DS) and Alzheimer's disease (AD). Consequently, DYRK1A inhibition has been of significant interest as a potential strategy for therapeutic intervention of DS and AD. Many classes of novel inhibitors have been described in the past decade. Although non-radioactive methods for analyzing DYRK1A inhibition have been developed, methods employing radioactive tracers are still commonly used for quantitative characterization of DYRK1A inhibitors...
2017: F1000Research
https://www.readbyqxmd.com/read/28163121/-epigallocatechin-gallate-synergistically-potentiates-prostaglandin-e2-stimulated-osteoprotegerin-synthesis-in-osteoblasts
#14
Gen Kuroyanagi, Haruhiko Tokuda, Naohiro Yamamoto, Shingo Kainuma, Kazuhiko Fujita, Reou Ohguchi, Tetsu Kawabata, Go Sakai, Rie Matsushima-Nishiwaki, Atsushi Harada, Osamu Kozawa, Takanobu Otsuka
(-)-Epigallocatechin gallate (EGCG), the most abundant flavonoid in green tea, and chlorogenic acid, the main polyphenol found in coffee, attract significant attention owing to health benefits. We have previously demonstrated that prostaglandin E2 (PGE2) stimulates osteoprotegerin synthesis through the activation of p38 mitogen-activated protein (MAP) kinase and stress-activated protein kinase/c-Jun N-terminal kinase (SAPK/JNK) in osteoblast-like MC3T3-E1 cells. In the present study, we investigated the effects of EGCG or chlorogenic acid on the PGE2-stimulated osteoprotegerin synthesis in MC3T3-E1 cells...
February 2, 2017: Prostaglandins & Other Lipid Mediators
https://www.readbyqxmd.com/read/28160861/antibacterial-activity-of-epigallocatechin-3-gallate-egcg-and-its-synergism-with-%C3%AE-lactam-antibiotics-sensitizing-carbapenem-associated-multidrug-resistant-clinical-isolates-of-acinetobacter-baumannii
#15
Spencer Lee, Ghaida Saleh Al Razqan, Dong H Kwon
BACKGROUND: Infections caused by Acinetobacter baumannii were responsive to conventional antibiotic therapy. However, recently, carbapenem-associated multidrug resistant isolates have been reported worldwide and present a major therapeutic challenge. Epigallocatechin-3-Gallate (EGCG) extracted from green tea exhibits antibacterial activity. PURPOSE: We evaluated the antibacterial activity of EGCG and possible synergism with antibiotics in carbapenem-associated multidrug resistant A...
January 15, 2017: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
https://www.readbyqxmd.com/read/28158944/urea-driven-epigallocatechin-gallate-egcg-permeation-into-the-ferritin-cage-an-innovative-method-for-fabrication-of-protein-polyphenol-co-assemblies
#16
Rui Yang, Yuqian Liu, Demei Meng, Zhiyu Chen, Christopher L Blanchard, Zhongkai Zhou
The 8 nm diameter cavity endows the ferritin cage with a natural space to encapsulate food components. In this work, urea was explored as a novel medium to facilitate the formation of ferritin-polyphenol co-assemblies. Results indicated that urea (20 mM) could expand the 4-fold channel size of apo-red bean ferritin (apoRBF) with an increased initial iron release rate υ0 (0.22 ± 0.02 μM min(-1)) and decreased α-helix content (5.6%). Moreover, urea (20 mM) could facilitate the permeation of EGCG into the apoRBF without destroying the ferritin structure and thus form ferritin-EGCG co-assemblies (FECs) with an encapsulation ratio and loading capacity of 17...
February 13, 2017: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/28155509/skin-delivery-of-epigallocatechin-3-gallate-egcg-and-hyaluronic-acid-loaded-nano-transfersomes-for-antioxidant-and-anti-aging-effects-in-uv-radiation-induced-skin-damage
#17
Kiran S Avadhani, Jyothsna Manikkath, Mradul Tiwari, Misra Chandrasekhar, Ashok Godavarthi, Shimoga M Vidya, Raghu C Hariharapura, Guruprasad Kalthur, Nayanabhirama Udupa, Srinivas Mutalik
The present work attempts to develop and statistically optimize transfersomes containing EGCG and hyaluronic acid to synergize the UV radiation-protective ability of both compounds, along with imparting antioxidant and anti-aging effects. Transfersomes were prepared by thin film hydration technique, using soy phosphatidylcholine and sodium cholate, combined with high-pressure homogenization. They were characterized with respect to size, polydispersity index, zeta potential, morphology, entrapment efficiency, Fourier Transform Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), X-ray Diffraction (XRD), in vitro antioxidant activity and ex vivo skin permeation studies...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28145499/targeted-nanoparticles-encapsulating-epigallocatechin-3-gallate-for-prostate-cancer-prevention-and-therapy
#18
Vanna Sanna, Chandra K Singh, Rahime Jashari, Vaqar M Adhami, Jean Christopher Chamcheu, Islam Rady, Mario Sechi, Hasan Mukhtar, Imtiaz A Siddiqui
Earlier we introduced the concept of 'nanochemoprevention' i.e. the use of nanotechnology to improve the outcome of cancer chemoprevention. Here, we extended our work and developed polymeric EGCG-encapsulated nanoparticles (NPs) targeted with small molecular entities, able to bind to prostate specific membrane antigen (PSMA), a transmembrane protein that is overexpressed in prostate cancer (PCa), and evaluated their efficacy in preclinical studies. First, we performed a molecular recognition of DCL- and AG-PEGylation on ligand binding on PSMA active site...
February 1, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28141493/functional-amyloids-in-streptococcus-mutans-their-use-as-targets-of-biofilm-inhibition-and-initial-characterization-of-smu_63c
#19
Richard N Besingi, Iwona B Wenderska, Dilani B Senadheera, Dennis G Cvitkovitch, Joanna R Long, Zezhang T Wen, L Jeannine Brady
Amyloids have been identified as functional components of the extracellular matrix of bacterial biofilms. Streptococcus mutans is an established etiologic agent of dental caries and biofilm dweller. In addition to the previously identified amyloidogenic adhesin P1 (aka AgI/II, PAc), we show that the naturally occurring Antigen A derivative of S. mutans wall-associated protein A (WapA), and the secreted protein SMU_63c, can also form amyloid fibrils. P1, WapA and SMU_63c were found to significantly influence biofilm development and architecture, and all three proteins were shown by immunogold electron microscopy to reside within fibrillar extracellular matrix of the biofilms...
January 28, 2017: Microbiology
https://www.readbyqxmd.com/read/28137482/epigallocatechin-3-gallate-egcg-activates-ampk-through-the-inhibition-of-glutamate-dehydrogenase-in-muscle-and-pancreatic-%C3%A3-cells-a-potential-beneficial-effect-in-the-pre-diabetic-state
#20
Shirin Pournourmohammadi, Mariagrazia Grimaldi, Malin H Stridh, Vanessa Lavallard, Helle S Waagepetersen, Claes B Wollheim, Pierre Maechler
Glucose homeostasis is determined by insulin secretion from the ß-cells in pancreatic islets and by glucose uptake in skeletal muscle and other insulin target tissues. While glutamate dehydrogenase (GDH) senses mitochondrial energy supply and regulates insulin secretion, its role in the muscle has not been elucidated. Here we investigated the possible interplay between GDH and the cytosolic energy sensing enzyme 5'-AMP kinase (AMPK), in both isolated islets and myotubes from mice and humans. The green tea polyphenol epigallocatechin-3-gallate (EGCG) was used to inhibit GDH...
January 27, 2017: International Journal of Biochemistry & Cell Biology
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