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Lin Han, Chun Fang, Ruixue Zhu, Qiang Peng, Ding Li, Min Wang
As the aglycone of phloridzin, phloretin belongs to dihydrochalcone with antioxidant, anti-inflammatory and antimicrobial activities. In this study, multispectroscopic techniques and molecular docking analysis were used to investigate the inhibitory activity and mechanisms of phloretin on α-glucosidase. The results showed that phloretin reversibly inhibited α-glucosidase in a mixed-type manner and the value of IC50 was 31.26μg·L(-1). The intrinsic fluorescence of α-glucosidase was quenched by the interactions with phloretin through a static quenching mechanism and spontaneously formed phloretin-α-glucosidase complex by the driving forces of van der Waals force and hydrogen bond...
November 25, 2016: International Journal of Biological Macromolecules
Jinfei Wang, Yumin Huang, Kaixiang Li, Yingying Chen, Diana Vanegas, Eric Scott McLamore, Yingbai Shen
The purpose of this study was to investigate the effects of leaf extract from Lithocarpus polystachyus Rehd. on type II diabetes mellitus (T2DM) and the active ingredients of this effect. In addition, this study determined, for the first time, the underlying molecular and pharmacological mechanisms of the extracts on hyperglycemia using long-term double high diet-fed and streptozotocin (STZ) induced type II diabetic mice. In the present study, leaf extract, phloridzin and trilobatin were assessed in vivo (gavage) and in vitro (non-invasive micro-test technique, NMT) in experimental T2DM mice...
2016: PloS One
Ji-Hoon Song, Hae-Rim Lee, Soon-Mi Shim
The objectives of the current study were to determine S-methyl-L-methionine (SMM) from various Brassicaceae family vegetables by using validated analytical method and to characterize the intestinal transport mechanism of SMM by the Caco-2 cells. The SMM is well known to provide therapeutic activity in peptic ulcers. The amount of SMM from various Brassicaceae family vegetables ranged from 89.08 ± 1.68 μg/g to 535.98 ± 4.85 μg/g of dry weight by using validated ultra-performance liquid chromatography-electrospray ionization-mass spectrometry method...
November 24, 2016: Journal of Food Science
Zhiwei Xu, Wendong Wang, Xiaofeng Nian, Guiqin Song, Xiaoyun Zhang, Hongyuan Xiao, Xiaobo Zhu
Luminal glucose is an important stimulus for glucagon-like peptide 1 (GLP-1) secretion from intestinal endocrine cells. However, the effects of luminal glucose concentration on GLP-1 secretion remain unknown. In this study, we investigated the effect of luminal glucose concentrations (3.5, 5, 10, 15, and 20 mmol/L) on GLP-1 secretion from isolated perfused rat ileum. Results showed that the perfusate glucose concentration dose-dependently stimulated GLP-1 secretion from isolated perfused rat ileum, which was eliminated by the sweet taste receptor inhibitor gurmarin (30 μg/mL), but not inhibited by phloridzin (1 mmol/L), a Na(+)-coupled glucose transporters inhibitor...
November 15, 2016: Endocrine Journal
Tingjing Zhang, Jianqiang Liang, Panxue Wang, Ying Xu, Yutang Wang, Xinyuan Wei, Mingtao Fan
Phloretin-2'-O-glycosyltransferase (P2'GT) catalyzes the last glycosylation step in the biosynthesis of phloridzin that contributes to the flavor, color and health benefits of apples and processed apple products. In this work, a novel P2'GT of Malus x domestica (MdP2'GT) with a specific activity of 46.82 μkat/Kg protein toward phloretin and uridine diphosphate glucose (UDPG) at an optimal temperature of 30 °C and pH 8.0 was purified from the engineered Pichia pastoris broth to homogeneity by anion exchange chromatography, His-Trap affinity chromatography and gel filtration...
October 12, 2016: Scientific Reports
Giancarlo Verardo, Andrea Gorassini, Donata Ricci, Daniele Fraternale
INTRODUCTION: Very rarely fruit pulp has been used in in vitro culture to produce secondary metabolites useful in promoting health. OBJECTIVES: The aims of this work were the study of the best conditions to obtain the callus cultures from the pulp of two varieties of apples, Golden Delicious (GD) and "Mela Rosa Marchigiana" (MRM), and the quali-quantitative analysis of secondary metabolites produced by the two in vitro callus cultures. METHODOLOGY: Callus was induced on both Murashige and Skoog and Gamborg B5 media containing various combinations of supplements...
September 30, 2016: Phytochemical Analysis: PCA
Shefalee K Bhavsar, Yogesh Singh, Piyush Sharma, Vishal Khairnar, Zohreh Hosseinzadeh, Shaqiu Zhang, Monica Palmada, Ivan Sabolic, Hermann Koepsell, Karl S Lang, Philipp A Lang, Florian Lang
BACKGROUND: Similar to tumor cells, activated T-lymphocytes generate ATP mainly by glycolytic degradation of glucose. Lymphocyte glucose uptake involves non-concentrative glucose carriers of the GLUT family. In contrast to GLUT isoforms, Na+-coupled glucose-carrier SGLT1 accumulates glucose against glucose gradients and is effective at low extracellular glucose concentrations. The present study explored expression and regulation of SGLT1 in activated murine splenic cytotoxic T cells (CTLs) and human Jurkat T cells...
2016: Cellular Physiology and Biochemistry
Chun-Ling Zhang, Jie-Chao Liu, Wen-Bo Yang, Da-Lei Chen, Zhong-Gao Jiao
Phloridzin is a nutraceutical. Its use in food, medicine and cosmetics is limited because of its low aqueous solubility and stability limits, but it can be improved by complexing with cyclodextrins. In this study, we investigated the inclusion mechanism between phloridzin and hydroxylpropyl-β-cyclodextrin (HP-β-CD) using isothermal titration calorimetry (ITC), ultraviolet-visible spectrometry (UV), infrared spectrometry (IR), proton nuclear magnetic resonance spectroscopy ((1)H NMR) and molecular docking simulations...
January 15, 2017: Food Chemistry
Wasundara Fernando, Melanie R Power Coombs, David W Hoskin, H P Vasantha Rupasinghe
Docosahexaenoic acid-acylated phloridzin (PZ-DHA), a novel polyphenol fatty acid ester derivative, was synthesized through a regioselective acylation reaction with the aim of increasing the bioactivity of phloridzin (PZ) and docosahexaenoic acid (DHA). In this study, PZ-DHA's cytotoxic activity was explored using in vitro and in vivo models of mammary carcinoma. PZ-DHA was selectively cytotoxic for mammary carcinoma (MDA-MB-231, MDA-MB-468, 4T1, MCF-7 and T-47D) cells compared to non-malignant human mammary epithelial cells (HMEC and MCF-10A) and fibroblasts by MTS assay and Annexin-V-FLUOS/propidium iodide staining...
October 2016: Carcinogenesis
Barberis Antonio, Garbetta Antonella, Cardinali Angela, Bazzu Gianfranco, D 'Antuono Isabella, Rocchitta Gaia, Fadda Angela, Linsalata Vito, D 'Hallewin Guy, Serra Pier Andrea, Minervini Fiorenza
An integrated device for real-time monitoring of glucose and phenols absorption, that consists of a sensors/biosensors system (SB) and a Caco-2TC7 human intestinal cell culture, is described in this study. The SB is composed of a glucose oxidase-based biosensor, a sentinel platinum sensor, a laccase/tyrosinase-based biosensor and a sentinel carbon sensor, all located in the basolateral compartment (BC) of a cell culture plate. Caco-2TC7 cells, differentiated on culture inserts, separated the apical compartment that simulates the intestinal lumen, from the BC which represented the bloodstream...
August 3, 2016: Biosensors & Bioelectronics
Tingjing Zhang, Xinyuan Wei, Zhuang Miao, Hamada Hassan, Yunbo Song, Mingtao Fan
BACKGROUND: Synthetic antioxidants and antimicrobials are losing ground to their natural counterparts and therefore, the food industry has motivated to seek other natural alternatives. Apple pomace, a by-product in the processing of apples, is rich in polyphenols, and plant polyphenols have been used as food additives owing to their strong antioxidant and antimicrobial properties. The goal of this study was to screen the individual polyphenols with antioxidant and antimicrobial activities from the extracts (methanol, ethanol, acetone, ethyl acetate, and chloroform) of Golden Delicious pomace...
2016: Chemistry Central Journal
Ana María Mendoza-Wilson, Sergio Ivan Castro-Arredondo, Angélica Espinosa-Plascencia, María Del Refugio Robles-Burgueño, René Renato Balandrán-Quintana, María Del Carmen Bermúdez-Almada
The apple is a food rich in diverse classes of polyphenols (PP), among which the proanthocyanidins (PCs), which are primarily concentrated in the skin, are one of the most abundant. These compounds are of considerable interest for their possible positive health effects because of their antioxidant properties. However, depending on the classes of PP present (chemical composition) and their relative concentrations in the apple skin, their antioxidant effects vary and some of their components can even generate prooxidant effects...
February 2016: Heliyon
Tine Rysman, Mariana Utrera, David Morcuende, Geert Van Royen, Stephanie Van Weyenberg, Stefaan De Smet, Mario Estévez
The effect of apple phenolics on the oxidative damage caused to myofibrillar proteins by an in vitro metal-catalyzed oxidation system was investigated. Three pure phenolic compounds (chlorogenic acid, (-)-epicatechin and phloridzin) and an apple peel extract were added to myofibrillar proteins in three concentrations (50, 100 and 200μM), and a blank treatment was included as a control. All suspensions were subjected to Fe(3+)/H2O2 oxidation at 37°C during 10days, and protein oxidation was evaluated as carbonylation (α-amino adipic and γ-glutamic semialdehydes) and Schiff base cross-links...
November 15, 2016: Food Chemistry
Cristina Otero-Rodiño, Cristina Velasco, Rosa Álvarez-Otero, Marcos A López-Patiño, Jesús M Míguez, José L Soengas
We previously obtained evidence in rainbow trout peripheral tissues such as liver and Brockmann bodies (BB) for the presence and response to changes in circulating levels of glucose (induced by intraperitoneal hypoglycaemic and hyperglycaemic treatments) of glucosensing mechanisms others than that mediated by glucokinase (GK). There were based on mitochondrial production of reactive oxygen species (ROS) leading to increased expression of uncoupling protein 2 (UCP2), and sweet taste receptor in liver and BB, and on liver X receptor (LXR) and sodium/glucose co-transporter 1 (SGLT-1) in BB...
October 2016: Comparative Biochemistry and Physiology. Part B, Biochemistry & Molecular Biology
Ying Xu, Mingtao Fan, Junjian Ran, Tingjing Zhang, Huiye Sun, Mei Dong, Zhe Zhang, Haiyan Zheng
Polyphenols are the predominant ingredients in apple seeds. However, few data are available on the phenolic profile or antioxidant activity in apple seeds in previous researches. In this study, low-molecular-weight phenolic compounds and antioxidant activity in seeds, peels, and flesh of seven apple cultivars grown in northwest China were measured and analyzed using HPLC and FRAP, DPPH, ABTS assays, respectively. HPLC analysis revealed phloridzin as the dominant phenolic compound in the seeds with its contents being 240...
May 2016: Saudi Journal of Biological Sciences
P L Reshma, Neethu S Sainu, Anil K Mathew, K G Raghu
AIMS: The present study investigates the protective effect of partially characterized Tribulus terrestris L. fruit methanol extract against mitochondrial dysfunction in cell based (H9c2) myocardial ischemia model. MAIN METHODS: To induce ischemia, the cells were maintained in an ischemic buffer (composition in mM -137 NaCl, 12 KCl, 0.5 MgCl2, 0.9 CaCl2, 20 HEPES, 20 2-deoxy-d-glucose, pH-6.2) at 37°C with 0.1% O2, 5% CO2, and 95% N2 in a hypoxia incubator for 1h...
May 1, 2016: Life Sciences
Cristina Otero-Rodiño, Cristina Velasco, Rosa Álvarez-Otero, Marcos A López-Patiño, Jesús M Míguez, José L Soengas
We previously obtained evidence in rainbow trout for the presence and response to changes in circulating levels of glucose (induced by intraperitoneal hypoglycaemic and hyperglycaemic treatments) of glucosensing mechanisms based on liver X receptor (LXR), mitochondrial production of reactive oxygen species (ROS) leading to increased expression of uncoupling protein 2 (UCP2), and sweet taste receptor in the hypothalamus, and on sodium/glucose co-transporter 1 (SGLT-1) in hindbrain. However, these effects of glucose might be indirect...
June 1, 2016: Journal of Experimental Biology
Marcos Roberto de Oliveira
Phloretin (C15 H14 O5 ), a dihydrochalcone flavonoid, is mainly found in fruit, leaves, and roots of apple tree. Phloretin exerts antioxidant, anti-inflammatory, and anti-tumor activities in mammalian cells through mechanisms that have been partially elucidated throughout the years. Phloretin bioavailability is well known in humans, but still remains to be better studied in experimental animals, such as mouse and rat. The focus of the present review is to gather information regarding the mechanisms involved in the phloretin-elicited effects in different in vitro and in vivo experimental models...
January 2016: BioFactors
Salah Abdel-Rahman, Nadia Shaban, Amany Haggag, Doaa Awad, Ahmad Bassiouny, Iman Talaat
The effect of Eruca sativa seed extract (SE) on nuclear factor kappa B (NF-κB), cyclooxygenase-2 (COX-2) and B-cell lymphoma-2 (Bcl-2) gene expression levels was investigated in rat mammary gland carcinogenesis induced by 7,12 dimethylbenz(α)anthracene (DMBA). DMBA increased NF-κB, COX-2 and Bcl-2 gene expression levels and lipid peroxidation (LP), while, decreased glutathione-S-transferase (GST) and superoxide dismutase (SOD) activities and total antioxidant concentration (TAC) compared to the control group...
2015: Asian Pacific Journal of Cancer Prevention: APJCP
Dominik Szwajgier
INTRODUCTION: Alzheimer's disease is a progressively developing neurodegenerative disorder of the central nervous system. The only present treatment of this disease is the use of acetyl- and butyrylcholinesterase inhibitors. Previously, the neuroprotection of phenolic acids and flavonoids in the brain has been indicated. MATERIALS AND METHOD: This study measured anticholinesterase activities of 9 phenolic acids and 6 flavonoids, singly or in combination. The synergy/antagonism/zero interaction between compounds was evaluated taking into consideration the statistical significance...
2015: Annals of Agricultural and Environmental Medicine: AAEM
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