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https://www.readbyqxmd.com/read/28334643/dual-tail-approach-to-discovery-of-novel-carbonic-anhydrase-ix-inhibitors-by-simultaneously-matching-the-hydrophobic-and-hydrophilic-halves-of-the-active-site
#1
Zhuang Hou, Bin Lin, Yu Bao, Hai-Ning Yan, Miao Zhang, Xiao-Wei Chang, Xin-Xin Zhang, Zi-Jie Wang, Gao-Fei Wei, Mao-Sheng Cheng, Yang Liu, Chun Guo
Dual-tail approach was employed to design novel Carbonic Anhydrase (CA) IX inhibitors by simultaneously matching the hydrophobic and hydrophilic halves of the active site, which also contains a zinc ion as part of the catalytic center. The classic sulfanilamide moiety was used as the zinc binding group. An amino glucosamine fragment was chosen as the hydrophilic part and a cinnamamide fragment as the hydrophobic part in order to draw favorable interactions with the corresponding halves of the active site. In comparison with sulfanilamide which is largely devoid of the hydrophilic and hydrophobic interactions with the two halves of the active site, the compounds so designed and synthesized in this study showed 1000-fold improvement in binding affinity...
March 16, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28333077/an-overview-of-the-protective-effects-of-chitosan-and-acetylated-chitosan-oligosaccharides-against-neuronal-disorders
#2
REVIEW
Cui Hao, Wei Wang, Shuyao Wang, Lijuan Zhang, Yunliang Guo
Chitin is the second most abundant biopolymer on Earth and is mainly comprised of a marine invertebrate, consisting of repeating β-1,4 linked N-acetylated glucosamine units, whereas its N-deacetylated product, chitosan, has broad medical applications. Interestingly, chitosan oligosaccharides have therapeutic effects on different types of neuronal disorders, including, but not limited to, Alzheimer's disease, Parkinson's disease, and nerve crush injury. A common link among neuronal disorders is observed at a sub-cellular level, such as atypical protein assemblies and induced neuronal death...
March 23, 2017: Marine Drugs
https://www.readbyqxmd.com/read/28332780/differentiation-of-patented-crystalline-glucosamine-sulfate-from-other-glucosamine-preparations-will-optimize-osteoarthritis-treatment
#3
REVIEW
Sukit Saengnipanthkul, Saranatra Waikakul, Sattaya Rojanasthien, Kitti Totemchokchyakarn, Attarit Srinkapaibulaya, Tai Cheh Chin, Nguyen Mai Hong, Olivier Bruyère, Cyrus Cooper, Jean-Yves Reginster, Myat Lwin
Symptomatic slow-acting drugs for osteoarthritis (SYSADOAs) are recommended for the medium- to long-term management of knee osteoarthritis (OA) due to their abilities to control pain, improve function and delay joint structural changes. Among SYSADOAs, evidence is greatest for the patented crystalline glucosamine sulfate (pCGS) formulation (Mylan). Glucosamine is widely available as glucosamine sulfate (GS) and glucosamine hydrochloride (GH) preparations that vary substantially in molecular form, pharmaceutical formulation and dose regimen...
March 23, 2017: International Journal of Rheumatic Diseases
https://www.readbyqxmd.com/read/28331832/glucosamine-and-chondroitin-use-in-canines-for-osteoarthritis-a-review
#4
REVIEW
Angel Bhathal, Meredith Spryszak, Christopher Louizos, Grace Frankel
Osteoarthritis is a slowly progressive and debilitating disease that affects canines of all breeds. Pain and decreased mobility resulting from osteoarthritis often have a negative impact on the affected canine's quality of life, level of comfort, daily functioning, activity, behaviour, and client-pet companionship. Despite limited and conflicting evidence, the natural products glucosamine hydrochloride (HCl) and chondroitin sulfate are commonly recommended by veterinarians for treating osteoarthritis in dogs...
2017: Open veterinary journal
https://www.readbyqxmd.com/read/28330083/enzymatic-production-of-glucosamine-and-chitooligosaccharides-using-newly-isolated-exo-%C3%AE-d-glucosaminidase-having-transglycosylation-activity
#5
Sujata Sinha, Subhash Chand, Pushplata Tripathi
Exochitosanase secreting fungus (A. fumigatus IIT-004) was isolated from fish waste using 1 % (w/v) chitosan as sole carbon source after multistage screening. Chitosan-dependent exochitosanase enzyme production (6 IU ml(-1)) in log phase of growth (chitosan utilization rate 0.11 g g(-1) cell h(-1)) was observed for Aspergillus fumigatus in chitosan minimal salt medium and there was no enzyme production in glucose medium. Enzyme production was found to be extracellular and subjected to purification by a number of steps like acetone fractionation as well as column chromatography...
June 2016: 3 Biotech
https://www.readbyqxmd.com/read/28325311/improved-fluorescent-labeling-of-chitin-oligomers-chitinolytic-properties-of-acidic-mammalian-chitinase-under-somatic-tissue-ph-conditions
#6
Satoshi Wakita, Masahiro Kimura, Naoki Kato, Akinori Kashimura, Shunsuke Kobayashi, Naoto Kanayama, Misa Ohno, Shotaro Honda, Masayoshi Sakaguchi, Yasusato Sugahara, Peter O Bauer, Fumitaka Oyama
Acidic mammalian chitinase (AMCase) has been implicated in various pathophysiological conditions including asthma, allergic inflammation and food processing. AMCase is most active at pH 2.0, and its activity gradually decreases to up to pH 8. Here we analyzed chitin degradation by AMCase in weak acidic to neutral conditions by fluorophore-assisted carbohydrate electrophoresis established originally for oligosaccharides analysis. We found that specific fragments with slower-than-expected mobility as defined by chitin oligosaccharide markers were generated at pH 5...
May 15, 2017: Carbohydrate Polymers
https://www.readbyqxmd.com/read/28322163/geriatric-oriented-high-dose-nutraceutical-odts-formulation-and-physicomechanical-characterization
#7
Ahmed M Agiba, Sameh Abdel-Hamid, Maha Nasr, Ahmed S Geneidi
CONTEXT: Oral disintegrating tablets (ODTs) represent a better option than conventional tablets for geriatric population, owing to their fast onset of action and their better patient compliance. OBJECTIVE: Two principal therapeutic high-dose nutraceuticals; chondroitin sulphate and glucosamine were formulated into an oral disintegration tablet (ODT) intended for sublingual administration, and optimized to improve compliance and achieve rapid onset of action in osteoarthritis treatment...
March 20, 2017: Current Drug Delivery
https://www.readbyqxmd.com/read/28319083/structures-of-human-o-glcnacase-and-its-complexes-reveal-a-new-substrate-recognition-mode
#8
Baobin Li, Hao Li, Lei Lu, Jiaoyang Jiang
Human O-GlcNAcase (hOGA) is the unique enzyme responsible for the hydrolysis of the O-linked β-N-acetyl glucosamine (O-GlcNAc) modification, an essential protein glycosylation event that modulates the function of numerous cellular proteins in response to nutrients and stress. Here we report crystal structures of a truncated hOGA, which comprises the catalytic and stalk domains, in apo form, in complex with an inhibitor, and in complex with a glycopeptide substrate. We found that hOGA forms an unusual arm-in-arm homodimer in which the catalytic domain of one monomer is covered by the stalk domain of the sister monomer to create a substrate-binding cleft...
March 20, 2017: Nature Structural & Molecular Biology
https://www.readbyqxmd.com/read/28306711/is-glucosamine-effective-for-osteoarthritis
#9
Stephanie Harrison-Muñoz, Valentina Rojas-Briones, Sebastián Irarrázaval
Osteoarthritis is the most prevalent chronic articular disease, in which pain is one of the main symptoms and a major determinant of functional loss. Several therapeutic options have been proposed, including glucosamine, but its actual usefulness has not yet been established. To answer this question, we searched in Epistemonikos database, which is maintained by screening multiple databases. We identified 11 systematic reviews including 35 randomized trials answering the question of interest. We extracted data, conducted a meta-analysis and generated a summary of findings table using the GRADE approach...
March 15, 2017: Medwave
https://www.readbyqxmd.com/read/28300590/heparin-depolymerization-by-immobilized-heparinase-a-review
#10
REVIEW
Indu Bhushan, Alhumaidi Alabbas, Jyothi C Sistla, Rashmi Saraswat, Umesh R Desai, Ram B Gupta
Heparin is a member of the glycosaminoglycan (GAG) family composed of glucosamine and uronic acid units containing O-sulfo, N-acetyl and N-sulfo groups, which are alternating in the chain and linked by 1→4 manner. It is a naturally occurring anticoagulant that prevents the formation of clots and their growth within blood. Certain low molecular weight heparins (LMWHs) are considered as better therapeutic agents than natural heparin because of the reduced side effects and smaller risk of bleeding. LMWHs can be produced from heparin by chemical or enzymatic depolymerizations...
March 11, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28294261/asymmetric-organocatalytic-synthesis-of-tertiary-azomethyl-alcohols-key-intermediates-towards-azoxy-compounds-and-%C3%AE-hydroxy-%C3%AE-amino-esters
#11
José A Carmona, Gonzalo de Gonzalo, Inmaculada Serrano, Ana M Crespo-Peña, Michal Šimek, David Monge, Rosario Fernández, José M Lassaletta
A series of peracylated glycosamine-derived thioureas have been synthesized and their behavior as bifunctional organocatalysts has been tested in the enantioselective nucleophilic addition of formaldehyde tert-butyl hydrazone to aliphatic α-keto esters for the synthesis of tertiary azomethyl alcohols. Using the 1,3,4,6-tetra-O-acetyl-2-amino-2-deoxy-β-d-glucosamine derived 3,5-bis-(trifluoromethyl)phenyl thiourea the reaction could be accomplished with high yields (75-98%) and moderate enantioselectivities (50-64% ee)...
March 15, 2017: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/28293289/novel-acinetobacter-parvus-handi-309-microbial-biomass-for-the-production-of-n-acetyl-%C3%AE-d-glucosamine-glcnac-using-swollen-chitin-substrate-in-submerged-fermentation
#12
Tae Il Kim, Kwang Seok Ki, Dong Hyun Lim, Mayakrishnan Vijayakumar, Seong Min Park, Sun Ho Choi, Ki Young Kim, Seok Ki Im, Beom Young Park
BACKGROUND: N-acetyl-β-d-glucosamine (GlcNAc)6 is extensively used as an important bio-agent and a functional food additive. The traditional chemical process for GlcNAc production has some problems such as high production cost, low yield, and acidic pollution. Therefore, to discover a novel chitinase that is suitable for bioconversion of chitin to GlcNAc would be of great value. RESULTS: Here, we describe the complete isolation and functional characterization of a novel exo-chitinase from Acinetobacter parvus HANDI 309 for the conversion of chitin...
2017: Biotechnology for Biofuels
https://www.readbyqxmd.com/read/28284699/incorporated-glucosamine-adversely-affects-the-emulsifying-properties-of-whey-protein-isolate-polymerized-by-transglutaminase
#13
Lin Chen, Niamat Ullah, Chenyi Li, Robert M Hackman, Zhixi Li, Xinglian Xu, Guanghong Zhou, Xianchao Feng
Glucosamine (GlcN) and microbial transglutaminase (Tgase) are used separately or together to improve the emulsifying properties of whey protein isolate (WPI). However, little is known about how the emulsifying properties change when GlcN residues are incorporated into WPI cross-linked by Tgase. We used Tgase as a biocatalyst to cross-link WPI in the presence of GlcN in a liquid system for 12 h at a moderate temperature (25°C). Matrix-assisted laser desorption/ionization time-of-flight mass spectrometry analyses indicated that protein polymerization and GlcN conjugation occurred simultaneously, phenomena also supported by the loss of free amines (9...
March 8, 2017: Journal of Dairy Science
https://www.readbyqxmd.com/read/28282148/alterations-in-the-salivary-proteome-and-n-glycome-of-sj%C3%A3-gren-s-syndrome-patients
#14
Steven C Hall, Maria E Hassis, Katherine E Williams, Matthew E Albertolle, Akraporn Prakobphol, Andrew B Dykstra, Megan Laurance, Katherine Ona, Richard K Niles, Namrata Prasad, Matthew Gormley, Caroline H Shiboski, Lindsey A Criswell, H Ewa Witkowska, Susan J Fisher
We used isobaric mass tagging (iTRAQ) and lectin affinity capture mass spectrometry (MS)-based workflows for global analyses of parotid saliva (PS) and whole saliva (WS) samples obtained from patients diagnosed with primary Sjögren's Syndrome (pSS) who were enrolled in the Sjögren's International Collaborative Clinical Alliance (SICCA) as compared to two control groups. The iTRAQ analyses revealed up- and down-regulation of numerous proteins that could be involved in the disease process (e.g., histones) or attempts to mitigate the ensuing damage [e...
March 10, 2017: Journal of Proteome Research
https://www.readbyqxmd.com/read/28280336/tumor-targeted-polymeric-nanostructured-lipid-carriers-with-precise-ratiometric-control-over-dual-drug-loading-for-combination-therapy-in-non-small-cell-lung-cancer
#15
Yan Liang, Baocheng Tian, Jing Zhang, Keke Li, Lele Wang, Jingtian Han, Zimei Wu
Gemcitabine (GEM) and paclitaxel (PTX) are effective combination anticancer agents against non-small-cell lung cancer (NSCLC). At the present time, a main challenge of combination treatment is the precision of control that will maximize the combined effects. Here, we report a novel method to load GEM (hydrophilic) and PTX (hydrophobic) into simplex tumor-targeted nanostructured lipid carriers (NLCs) for accurate control of the ratio of the two drugs. We covalently preconjugated the dual drugs through a hydrolyzable ester linker to form drug conjugates...
2017: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/28280335/nanoparticle-abraxane-possesses-impaired-proliferation-in-a549-cells-due-to-the-underexpression-of-glucosamine-6-phosphate-n-acetyltransferase-1-gnpnat1-gna1
#16
Minzhi Zhao, Haiyun Li, Yan Ma, He Gong, Shu Yang, Qiaojun Fang, Zhiyuan Hu
Abraxane (Abr), a US Food and Drug Administration-approved albumin-bound nanoparticle applied for the treatment of non-small-cell lung cancer, has been reported to be more effective than paclitaxel (PTX). To further understand the molecular mechanisms that produce this superior drug efficacy of Abr, a quantitative proteomic approach has been applied to investigate the global protein expression profiles of lung cancer cell A549 treated with Abr and PTX. Only one protein, namely, glucosamine 6-phosphate N-acetyltransferase 1 (GNA1), showed significant differential expression (P<0...
2017: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/28274441/preparation-of-glycosylated-zein-and-retarding-effect-on-lipid-oxidation-of-ground-pork
#17
Xiao-Jie Wang, Xi-Qun Zheng, Xiao-Lan Liu, Narasimha-Kumar Kopparapu, Wan-Suo Cong, Yong-Ping Deng
The focus of the present work was to investigate the glycosylation of zein, partial properties of the glycosylated zein (GZ) and its retarding effect on lipid oxidation of ground pork. Zein was glycosylated with chitosan (MW 1500Da) by microbial transglutaminase, the reaction was verified by FT-IR. Under the optimized conditions, 97.48mg of glucosamine was covalently conjugated to 1g of zein, determined by HPLC. The solubility and the surface hydrophobicity of GZ were significantly improved. In vitro studies of GZ showed a dose-dependent scavenging activity against free radicals of DPPH, superoxide and hydroxyl radical, and the EC50 value for DPPH radical was 1...
July 15, 2017: Food Chemistry
https://www.readbyqxmd.com/read/28267503/a-new-unsaturated-derivative-of-hyaluronic-acid-synthesis-analysis-and-applications
#18
Radovan Buffa, Petra Šedová, Ivana Basarabová, Tomáš Bobula, Pavlína Procházková, Hana Vágnerová, Iva Dolečková, Soňa Moravčíková, Lenka Hejlová, Vladimír Velebný
Hyaluronic acid (HA) containing CC double bond in positions 4 and 5 of N-acetyl-glucosamine ring (ΔHA) is an unique material, which could be used for biomedical applications and cosmetics. The main advantage of the CC double bond is its ability to react with a wide range of oxidation agents. Location of the CC double bond directly on the glucopyranose ring allows to change the chemical capabilities and simultaneously to mimic the intrinsic physical properties of HA without introduction of linkers or other substances...
May 1, 2017: Carbohydrate Polymers
https://www.readbyqxmd.com/read/28267485/three-phase-partitioning-for-efficient-extraction-and-separation-of-polysaccharides-from-corbicula-fluminea
#19
Jing-Kun Yan, Yao-Yao Wang, Wen-Yi Qiu, Ning Shao
Three-phase partitioning (TPP), which is a simple, efficient, and green bioseparation technique, was used to extract and separate polysaccharides from Corbicula fluminea (CFPS). The optimal parameters with a high yield of 9.32% were as follows: mass fraction of (NH4)2SO4, 20.0% (w/v); amount of t-butanol, 9.8mL; temperature, 35.3°C; extraction time, 30min; and pH 6.0. The purified CFPS after TPP consisted of d-glucose, d-glucosamine, and d-mannose in a molar ratio of 57.1: 5.6:1.0 with high purity (86.5%) and different molecular weights (1311...
May 1, 2017: Carbohydrate Polymers
https://www.readbyqxmd.com/read/28267235/red-blood-cells-for-glucose-responsive-insulin-delivery
#20
Chao Wang, Yanqi Ye, Wujin Sun, Jicheng Yu, Jingqiang Wang, David S Lawrence, John B Buse, Zhen Gu
Glucose-responsive delivery of insulin mimicking the function of pancreatic β-cells to achieve meticulous control of blood glucose (BG) would revolutionize diabetes care. Here the authors report the development of a new glucose-responsive insulin delivery system based on the potential interaction between the glucose derivative-modified insulin (Glc-Insulin) and glucose transporters on erythrocytes (or red blood cells, RBCs) membrane. After being conjugated with the glucosamine, insulin can efficiently bind to RBC membranes...
March 7, 2017: Advanced Materials
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