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  1 / 1003 MEDLINE  
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PMID:28482241
Autor:Yahyaa M; Ali S; Davidovich-Rikanati R; Ibdah M; Shachtier A; Eyal Y; Lewinsohn E; Ibdah M
Endereço:Newe Yaar Research Center, Agriculture Research Organization, P.O.Box 1021, Ramat Yishay, 30095, Israel.
Título:Characterization of three chalcone synthase-like genes from apple (Malus x domestica Borkh.).
Fonte:Phytochemistry; 140:125-133, 2017 Aug.
ISSN:1873-3700
País de publicação:England
Idioma:eng
Resumo:Apple (Malus x domestica Brokh.) is a widely cultivated deciduous tree species of significant economic importance. Apple leaves accumulate high levels of flavonoids and dihydrochalcones, and their formation is dependent on enzymes of the chalcone synthase family. Three CHS genes were cloned from apple leaves and expressed in Escherichia coli. The encoded recombinant enzymes were purified and functionally characterized. In-vitro activity assays indicated that MdCHS1, MdCHS2 and MdCHS3 code for proteins exhibiting polyketide synthase activity that accepted either p-dihydrocoumaroyl-CoA, p-coumaroyl-CoA, or cinnamoyl-CoA as starter CoA substrates in the presence of malonyl-CoA, leading to production of phloretin, naringenin chalcone, and pinocembrin chalcone. MdCHS3 coded a chalcone-dihydrochalcone synthase enzyme with narrower substrate specificity than the previous ones. The apparent Km values of MdCHS3 for p-dihydrocoumaryl-CoA and p-coumaryl-CoA were both 5.0 µM. Expression analyses of MdCHS genes varied according to tissue type. MdCHS1, MdCHS2 and MdCHS3 expression levels were associated with the levels of phloretin accumulate in the respective tissues.
Tipo de publicação: JOURNAL ARTICLE
Nome de substância:0 (Chalcones); 0 (pinocembrin chalcone); 73692-50-9 (naringenin chalcone); EC 2.3.- (Acyltransferases); EC 2.3.1.74 (flavanone synthetase); S5J5OE47MK (Phloretin)


  2 / 1003 MEDLINE  
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PMID:28445002
Autor:Kunimasa K; Nagano T; Shimono Y; Dokuni R; Kiriu T; Tokunaga S; Tamura D; Yamamoto M; Tachihara M; Kobayashi K; Satouchi M; Nishimura Y
Endereço:Division of Respiratory Medicine, Kobe University Graduate School of Medicine, Kobe, Japan.
Título:Glucose metabolism-targeted therapy and withaferin A are effective for epidermal growth factor receptor tyrosine kinase inhibitor-induced drug-tolerant persisters.
Fonte:Cancer Sci; 108(7):1368-1377, 2017 Jul.
ISSN:1349-7006
País de publicação:England
Idioma:eng
Resumo:In pathway-targeted cancer drug therapies, the relatively rapid emergence of drug-tolerant persisters (DTPs) substantially limits the overall therapeutic benefit. However, little is known about the roles of DTPs in drug resistance. In this study, we investigated the features of epidermal growth factor receptor-tyrosine kinase inhibitor-induced DTPs and explored a new treatment strategy to overcome the emergence of these DTPs. We used two EGFR-mutated lung adenocarcinoma cell lines, PC9 and II-18. They were treated with 2 µM gefitinib for 6, 12, or 24 days or 6 months. We analyzed the mRNA expression of the stem cell-related markers by quantitative RT-PCR and the expression of the cellular senescence-associated proteins. Then we sorted DTPs according to the expression pattern of CD133 and analyzed the features of sorted cells. Finally, we tried to ablate DTPs by glucose metabolism targeting therapies and a stem-like cell targeting drug, withaferin A. Drug-tolerant persisters were composed of at least two types of cells, one with the properties of cancer stem-like cells (CSCs) and the other with the properties of therapy-induced senescent (TIS) cells. The CD133 cell population had CSC properties and the CD133 cell population had TIS properties. The CD133 cell population containing TIS cells showed a senescence-associated secretory phenotype that supported the emergence of the CD133 cell population containing CSCs. Glucose metabolism inhibitors effectively eliminated the CD133 cell population. Withaferin A effectively eliminated the CD133 cell population. The combination of phloretin and withaferin A effectively suppressed gefitinib-resistant tumor growth.
Tipo de publicação: JOURNAL ARTICLE
Nome de substância:0 (Protein Kinase Inhibitors); 0 (Quinazolines); 0 (Withanolides); EC 2.7.10.1 (EGFR protein, human); EC 2.7.10.1 (Receptor, Epidermal Growth Factor); IY9XDZ35W2 (Glucose); L6DO3QW4K5 (withaferin A); S5J5OE47MK (Phloretin); S65743JHBS (gefitinib)


  3 / 1003 MEDLINE  
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PMID:28365326
Autor:Lopes LAA; Dos Santos Rodrigues JB; Magnani M; de Souza EL; de Siqueira-Júnior JP
Endereço:Laboratório de Genética de Microrganismos, Departamento de Biologia Molecular, Universidade Federal da Paraíba, João Pessoa, Paraíba, Brazil.
Título:Inhibitory effects of flavonoids on biofilm formation by Staphylococcus aureus that overexpresses efflux protein genes.
Fonte:Microb Pathog; 107:193-197, 2017 Jun.
ISSN:1096-1208
País de publicação:England
Idioma:eng
Resumo:This study evaluated the efficacy of glycone (myricitrin, hesperidin and phloridzin) and aglycone flavonoids (myricetin, hesperetin and phloretin) in inhibiting biofilm formation by Staphylococcus aureus RN4220 and S. aureus SA1199B that overexpress the msrA and norA efflux protein genes, respectively. The minimum inhibitory concentration (MIC) and minimum biofilm inhibitory concentration (MBIC - defined as the lowest concentration that resulted in ≥50% inhibition of biofilm formation) of flavonoids were determined using microdilution in broth procedures. The flavonoids showed MIC >1024 µg/mL against S. aureus RN4220 and S. aureus SA1199B; however, these compounds at lower concentrations (1-256 µg/mL) showed inhibitory effects on biofilm formation by these strains. Aglycone flavonoids showed lower MBIC values than their respective glycone forms. The lowest MBIC values (1 and 4 µg/mL) were observed against S. aureus RN4220. Myricetin, hesperetin and phloretin exhibited biofilm formation inhibition >70% for S. aureus RN4220, and lower biofilm formation inhibition against S. aureus SA1199B. These results indicate that sub-MICs of the tested flavonoids inhibit biofilm formation by S. aureus strains that overexpress efflux protein genes. These effects are more strongly established by aglycone flavonoids.
Tipo de publicação: JOURNAL ARTICLE
Nome de substância:0 (Anti-Bacterial Agents); 0 (Bacterial Proteins); 0 (Flavonoids); 0 (Membrane Transport Proteins); 0 (Multidrug Resistance-Associated Proteins); 133135-40-7 (NorA protein, Staphylococcus); 5Z0ZO61WPJ (myricitrin); 76XC01FTOJ (myricetin); CU9S17279X (Phlorhizin); E750O06Y6O (Hesperidin); Q9Q3D557F1 (hesperetin); S5J5OE47MK (Phloretin)


  4 / 1003 MEDLINE  
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PMID:28223777
Autor:Shen X; Zhou N; Mi L; Hu Z; Wang L; Liu X; Zhang S
Endereço:Department of Medicinal Chemistry, School of Pharmacy.
Título:Phloretin exerts hypoglycemic effect in streptozotocin-induced diabetic rats and improves insulin resistance in vitro.
Fonte:Drug Des Devel Ther; 11:313-324, 2017.
ISSN:1177-8881
País de publicação:New Zealand
Idioma:eng
Resumo:The present study investigated the possible antiobesity and hypoglycemic effects of phloretin (Ph). In an attempt to discover the hypoglycemic effect and potential mechanism of Ph, we used the streptozotocin-induced diabetic rats and (L6) myotubes. Daily oral treatment with Ph for 4 weeks significantly ( <0.05) reduced postprandial blood glucose and improved islet injury and lipid metabolism. Glucose consumption and glucose tolerance were improved by Ph via GOD-POD method. Western blot results revealed that the expression of Akt, PI3K, IRS-1, and GLUT4 were upregulated in skeletal muscle of type 2 diabetes (T2D) rats and in L6 myotubes by Ph. The immunofluorescence studies confirmed that Ph improved the translocation of GLUT4 in L6 myotubes. Ph exerted hypoglycemic effects in vivo and in vitro, hence it may play an important role in the management of diabetes.
Tipo de publicação: JOURNAL ARTICLE
Nome de substância:0 (Blood Glucose); 0 (Hypoglycemic Agents); 5W494URQ81 (Streptozocin); IY9XDZ35W2 (Glucose); S5J5OE47MK (Phloretin)


  5 / 1003 MEDLINE  
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PMID:28154809
Autor:Wang J; Liu B; Teng Z; Zhou X; Wang X; Zhang B; Lu G; Niu X; Yang Y; Deng X
Endereço:Key Laboratory of Zoonosis, Ministry of Education, College of Veterinary Medicine, Jilin University Changchun, China.
Título:Phloretin Attenuates Virulence Both and by Simultaneously Targeting Listeriolysin O and Sortase A.
Fonte:Front Cell Infect Microbiol; 7:9, 2017.
ISSN:2235-2988
País de publicação:Switzerland
Idioma:eng
Resumo:The critical roles of sortase A (SrtA) and listeriolysin O (LLO) in pathogenicity render these two virulence factors as ideal targets for the development of anti-virulence agents against infection. Additionally, the structures of SrtA and LLO are highly conserved among the members of sortase enzyme family and cholesterol dependent toxin family. Here, phloretin, a natural polyphenolic compound derived from apples and pears that has little anti- activity, was identified to simultaneously inhibit LLO expression and neutralize SrtA catalytic activity. Phloretin neutralized SrtA activity by causing a conformational change in the protein's active pocket, which prevented engagement with its substrate. Treatment with phloretin simultaneously reduced invasion into host cells and blocked the escape of vacuole-entrapped into cytoplasm. Further, -infected mice that received phloretin showed lower mortality, decreased bacterial burden and reduced pathological injury. Our results demonstrate that phloretin is a promising anti-infective therapeutic for infections caused by due to its simultaneous targeting of SrtA and LLO, which may result in fewer side effects than those caused by other antibiotics.
Tipo de publicação: JOURNAL ARTICLE
Nome de substância:0 (Anti-Bacterial Agents); 0 (Bacterial Proteins); 0 (Bacterial Toxins); 0 (Enzyme Inhibitors); 0 (Heat-Shock Proteins); 0 (Hemolysin Proteins); 72270-41-8 (hlyA protein, Listeria monocytogenes); EC 2.3.2.- (Aminoacyltransferases); EC 2.3.2.- (sortase A); EC 3.4.22.- (Cysteine Endopeptidases); S5J5OE47MK (Phloretin)


  6 / 1003 MEDLINE  
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PMID:28117761
Autor:Jeon D; Jeong MC; Jnawali HN; Kwak C; Ryoo S; Jung ID; Kim Y
Endereço:Department of Bioscience and Biotechnology, Konkuk University, Seoul 05029, Korea. dasom921012@konkuk.ac.kr.
Título:Phloretin Exerts Anti-Tuberculosis Activity and Suppresses Lung Inflammation.
Fonte:Molecules; 22(1), 2017 Jan 22.
ISSN:1420-3049
País de publicação:Switzerland
Idioma:eng
Resumo:An increase in the prevalence of the drug-resistant necessitates developing new types of anti-tuberculosis drugs. Here, we found that phloretin, a naturally-occurring flavonoid, has anti-mycobacterial effects on H37Rv, multi-drug-, and extensively drug-resistant clinical isolates, with minimum inhibitory concentrations of 182 and 364 µM, respectively. Since cause lung inflammation that contributes to tuberculosis pathogenesis, anti-inflammatory effects of phloretin in interferon-γ-stimulated MRC-5 human lung fibroblasts and lipopolysaccharide (LPS)-stimulated dendritic cells were investigated. The release of interleukin (IL)-1ß, IL-12, and tumor necrosis factor (TNF)-α was inhibited by phloretin. The mRNA levels of IL-1ß, IL-6, IL-12, TNF-α, and matrix metalloproteinase-1, as well as p38 mitogen-activated protein kinase and extracellular signal-regulated kinase phosphorylation, were suppressed. A mouse in vivo study of LPS-stimulated lung inflammation showed that phloretin effectively suppressed the levels of TNF-α, IL-1ß, and IL-6 in lung tissue with low cytotoxicity. Phloretin was found to bind ß-ketoacyl acyl carrier protein synthase III (mtKASIII) with high affinity (7.221 × 107 M ); a binding model showed hydrogen bonding of A-ring 2'-hydroxy and B-ring 4-hydroxy groups of phloretin with Asn261 and Cys122 of mtKASIII, implying that mtKASIII can be a potential target protein. Therefore, phloretin can be a useful dietary natural product with anti-tuberculosis benefits.
Tipo de publicação: JOURNAL ARTICLE
Nome de substância:0 (Anti-Inflammatory Agents); 0 (Antitubercular Agents); 0 (Cytokines); 0 (Lipopolysaccharides); EC 2.3.1.180 (3-ketoacyl-acyl carrier protein synthase III); EC 2.3.1.41 (3-Oxoacyl-(Acyl-Carrier-Protein) Synthase); EC 2.7.11.24 (Extracellular Signal-Regulated MAP Kinases); EC 2.7.11.24 (p38 Mitogen-Activated Protein Kinases); S5J5OE47MK (Phloretin)


  7 / 1003 MEDLINE  
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PMID:27997810
Autor:Cho SJ; Moon JS; Lee CM; Choi AM; Stout-Delgado HW
Endereço:1 Joan and Sanford I. Weill Department of Medicine, Weill Cornell Medical College and New York-Presbyterian Hospital, New York, New York.
Título:Glucose Transporter 1-Dependent Glycolysis Is Increased during Aging-Related Lung Fibrosis, and Phloretin Inhibits Lung Fibrosis.
Fonte:Am J Respir Cell Mol Biol; 56(4):521-531, 2017 Apr.
ISSN:1535-4989
País de publicação:United States
Idioma:eng
Resumo:Aging is associated with metabolic diseases such as type 2 diabetes mellitus, cardiovascular disease, cancer, and neurodegeneration. Aging contributes to common processes including metabolic dysfunction, DNA damage, and reactive oxygen species generation. Although glycolysis has been linked to cell growth and proliferation, the mechanisms by which the activation of glycolysis by aging regulates fibrogenesis in the lung remain unclear. The objective of this study was to determine if glucose transporter 1 (GLUT1)-induced glycolysis regulates age-dependent fibrogenesis of the lung. Mouse and human lung tissues were analyzed for GLUT1 and glycolytic markers using immunoblotting. Glycolytic function was measured using a Seahorse apparatus. To study the effect of GLUT1, genetic inhibition of GLUT1 was performed by short hairpin RNA transduction, and phloretin was used for pharmacologic inhibition of GLUT1. GLUT1-dependent glycolysis is activated in aged lung. Genetic and pharmacologic inhibition of GLUT1 suppressed the protein expression of α-smooth muscle actin, a key cytoskeletal component of activated fibroblasts, in mouse primary lung fibroblast cells. Moreover, we demonstrated that the activation of AMP-activated protein kinase, which is regulated by GLUT1-dependent glycolysis, represents a critical metabolic pathway for fibroblast activation. Furthermore, we demonstrated that phloretin, a potent inhibitor of GLUT1, significantly inhibited bleomycin-induced lung fibrosis in vivo. These results suggest that GLUT1-dependent glycolysis regulates fibrogenesis in aged lung and that inhibition of GLUT1 provides a potential target of therapy of age-related lung fibrosis.
Tipo de publicação: JOURNAL ARTICLE
Nome de substância:0 (Glucose Transporter Type 1); 11056-06-7 (Bleomycin); EC 2.7.11.31 (AMP-Activated Protein Kinases); S5J5OE47MK (Phloretin)


  8 / 1003 MEDLINE  
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PMID:27894824
Autor:Han L; Fang C; Zhu R; Peng Q; Li D; Wang M
Endereço:College of Food Science and Engineering, Northwest A&F University, Yangling 712100, PR China; College of Life Science and Engineering, Chongqing Three Gorges University, Chongqing 404100, PR China.
Título:Inhibitory effect of phloretin on α-glucosidase: Kinetics, interaction mechanism and molecular docking.
Fonte:Int J Biol Macromol; 95:520-527, 2017 Feb.
ISSN:1879-0003
País de publicação:Netherlands
Idioma:eng
Resumo: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 IC was 31.26µgL . 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. Atomic force microscope (AFM) studies and FT-IR measurements suggested that the interactions could change the micro-environments and conformation of the enzymes and the molecular docking analysis displayed the exact binding site of phloretin on α-glucosidase. These results indicated that phloretin is a strong α-glucosidase inhibitor, thus could be contribute to the improvement of diabetes mellitus.
Tipo de publicação: JOURNAL ARTICLE
Nome de substância:0 (Glycoside Hydrolase Inhibitors); EC 3.2.1.20 (alpha-Glucosidases); S5J5OE47MK (Phloretin)


  9 / 1003 MEDLINE  
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PMID:27520503
Autor:Barberis A; Garbetta A; Cardinali A; Bazzu G; D'Antuono I; Rocchitta G; Fadda A; Linsalata V; D'Hallewin G; Serra PA; Minervini F
Endereço:Institute of Sciences of Food Production (ISPA), National Research Council (CNR), Traversa La Crucca, 3 Regione Baldinca, 07100 Li Punti, Sassari, Italy.
Título:Real-time monitoring of glucose and phenols intestinal absorption through an integrated Caco-2TC7cells/biosensors telemetric device: Hypoglycemic effect of fruit phytochemicals.
Fonte:Biosens Bioelectron; 88:159-166, 2017 02 15.
ISSN:1873-4235
País de publicação:England
Idioma:eng
Resumo: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. The system recorded currents relative to glucose (1mM) absorption, obtaining bioavailability values (5.1%) comparable to HPLC analysis (4.8%). Phloridzin and phloretin, specific phenolic inhibitors of SGLT1 and GLUT2 glucose transporters, reduced the glucose transport of almost 10 times. They were minimally absorbed in the BC with a bioavailability of 0.13% and 0.49% respectively. The hypoglycemic potential of blueberry and pomegranate juices was also studied. In particular, the amount of glucose absorbed through the Caco-2TC7 monolayer was 8‰ for pomegranate and 1.7‰ for blueberry, demonstrating the potential hypoglycemic effect of the juices. Polyphenols absorption was also monitored by the SB and an increase was recorded during the first 50min in presence of both blueberry and pomegranate juices, then a constant decrease occurred. The proposed device has been developed as innovative tool for the dynamic monitoring of natural compounds effects on glucose absorption, in order to manage postprandial hyperglycemia.
Tipo de publicação: JOURNAL ARTICLE
Nome de substância:0 (Hypoglycemic Agents); 0 (Phenols); CU9S17279X (Phlorhizin); IY9XDZ35W2 (Glucose); S5J5OE47MK (Phloretin)


  10 / 1003 MEDLINE  
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PMID:26971858
Autor:Barreca D; Laganà G; Toscano G; Calandra P; Kiselev MA; Lombardo D; Bellocco E
Endereço:Dipartimento di Scienze chimiche, biologiche, farmaceutiche ed ambientali, Università di Messina. Viale F. Stagno d'Alcontres 31, 98166 Messina, Italy.
Título:The interaction and binding of flavonoids to human serum albumin modify its conformation, stability and resistance against aggregation and oxidative injuries.
Fonte:Biochim Biophys Acta; 1861(1 Pt B):3531-3539, 2017 01.
ISSN:0006-3002
País de publicação:Netherlands
Idioma:eng
Resumo:BACKGROUND: Interactions of ligands with proteins imply changes in the properties of the macromolecules that may deeply modify their biological activities and conformations and allow them to acquire new and, sometimes, unexpected abilities. The flavonoid phloretin has several pharmacological properties that are starting to be elucidated, one of which is the well-known inhibition of glucose transport. METHODS: The interactions of phloretin to human serum albumin have been investigated by fluorescence, UV-visible, FTIR spectroscopy, native electrophoresis, protein ligand docking studies, fluorescence and scanning electron microscopy. RESULTS: Spectroscopic investigations suggest that the flavonoid binds to human serum albumin inducing a decrease in α-helix structures as shown by deconvolution of FTIR Amide I' band. Fluorescence and displacement studies highlight modifications of environment around Trp214 with the primary binding site located in the Sudlow's site I. In the hydrophobic cavity of subdomain IIA, molecular modeling studies suggest that phloretin is in non-planar conformation and hydrogen-bonded with Ser202 and Ser454. These changes make HSA able to withstand protein degradation due to HCLO and fibrillation. GENERAL SIGNIFICANCE: Our work aims to open new perspectives as far as the binding of flavonoids to HSA are concern and shows as the properties of both compounds can be remarkable modified after the complex formation, resulting, for instance, in a protein structure much more resistant to oxidation and fibrillation. This article is part of a Special Issue entitled "Science for Life" Guest Editor: Dr. Austen Angell, Dr. Salvatore Magazù and Dr. Federica Migliardo.
Tipo de publicação: JOURNAL ARTICLE
Nome de substância:0 (Flavonoids); 0 (Protein Aggregates); 0 (Serum Albumin); S5J5OE47MK (Phloretin)



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