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[PMID]:29342216
[Au] Autor:Narayanaswamy VP; Giatpaiboon SA; Uhrig J; Orwin P; Wiesmann W; Baker SM; Townsend SM
[Ad] Endereço:Synedgen, Inc., Claremont, California, United States of America.
[Ti] Título:In Vitro activity of novel glycopolymer against clinical isolates of multidrug-resistant Staphylococcus aureus.
[So] Source:PLoS One;13(1):e0191522, 2018.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The incidence of multidrug-resistant (MDR) organisms, including methicillin-resistant Staphylococcus aureus (MRSA), is a serious threat to public health. Progress in developing new therapeutics is being outpaced by antibiotic resistance development, and alternative agents that rapidly permeabilize bacteria hold tremendous potential for treating MDR infections. A new class of glycopolymers includes polycationic poly-N (acetyl, arginyl) glucosamine (PAAG) is under development as an alternative to traditional antibiotic strategies to treat MRSA infections. This study demonstrates the antibacterial activity of PAAG against clinical isolates of methicillin and mupirocin-resistant Staphylococcus aureus. Multidrug-resistant S. aureus was rapidly killed by PAAG, which completely eradicated 88% (15/17) of all tested strains (6-log reduction in CFU) in ≤ 12-hours at doses that are non-toxic to mammalian cells. PAAG also sensitized all the clinical MRSA strains (17/17) to oxacillin as demonstrated by the observed reduction in the oxacillin MIC to below the antibiotic resistance breakpoint. The effect of PAAG and standard antibiotics including vancomycin, oxacillin, mupirocin and bacitracin on MRSA permeability was studied by measuring propidium iodide (PI) uptake by bacterial cells. Antimicrobial resistance studies showed that S. aureus developed resistance to PAAG at a rate slower than to mupirocin but similar to bacitracin. PAAG was observed to resensitize drug-resistant S. aureus strains sampled from passage 13 and 20 of the multi-passage resistance study, reducing MICs of mupirocin and bacitracin below their clinical sensitivity breakpoints. This class of bacterial permeabilizing glycopolymers may provide a new tool in the battle against multidrug-resistant bacteria.
[Mh] Termos MeSH primário: Antibacterianos/farmacologia
Glucosamina/análogos & derivados
Staphylococcus aureus Resistente à Meticilina/efeitos dos fármacos
Polímeros/farmacologia
Polissacarídeos/farmacologia
[Mh] Termos MeSH secundário: Antibacterianos/química
Farmacorresistência Bacteriana Múltipla
Glucosamina/química
Glucosamina/farmacologia
Glicosídeos
Seres Humanos
Técnicas In Vitro
Resistência a Meticilina
Staphylococcus aureus Resistente à Meticilina/isolamento & purificação
Staphylococcus aureus Resistente à Meticilina/metabolismo
Testes de Sensibilidade Microbiana
Mupirocina/farmacologia
Permeabilidade/efeitos dos fármacos
Polímeros/química
Polissacarídeos/química
Propídio/farmacocinética
Infecções Estafilocócicas/tratamento farmacológico
Infecções Estafilocócicas/microbiologia
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Glycosides); 0 (Polymers); 0 (Polysaccharides); 0 (pinocembrin 7-O-apiosyl(1-5)apiosyl(1-2)glucopyranoside); 0 (poly-N (acetyl, arginyl)glucosamine); 36015-30-2 (Propidium); D0GX863OA5 (Mupirocin); N08U5BOQ1K (Glucosamine)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180302
[Lr] Data última revisão:
180302
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180118
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0191522


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[PMID]:29025664
[Au] Autor:Tsai W; Tsai H; Wong Y; Hong J; Chang S; Lee M
[Ad] Endereço:Department of Medical Laboratory Science and Biotechnology, Kaohsiung Medical University, Taiwan.
[Ti] Título:Preparation and characterization of gellan gum/glucosamine/clioquinol film as oral cancer treatment patch.
[So] Source:Mater Sci Eng C Mater Biol Appl;82:317-322, 2018 Jan 01.
[Is] ISSN:1873-0191
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:To administer cancer drugs with improved convenience to patients and to enhance the bioavailability of cancer drugs for oral cancer therapy, this study prepared gellan gum/glucosamine/clioquinol (GG/GS/CQ) film as the oral cancer treatment patch. GG/GS/CQ film fabricated through the EDC-mediated coupling reactions (GG/GS/CQ/EDC film). The film of the physicochemical properties and drug release kinetics were studied. The effectiveness of GG/GS/CQ/EDC film as oral cancer treatment patch were evaluated with the animal model. The results confirmed that CQ can be incorporated via EDC-mediated covalent conjugation to gellan gum/glucosamine. Mechanical testing revealed that the maximum tensile strength and elongation percentage at break were 1.91kgf/mm and 5.01% for GG/GS/CQ/EDC film. After a drug release experiment lasting 45days, 86.8% of CQ was released from GG/GS/CQ/EDC film. The Huguchi model fit the GG/GS/CQ/EDC drug release data with high correlation coefficients (R =0.9994, respectively). The effect of the CQ dose on oral cancer cells (OC-2) was tested, and the IC of CQ alone and CQ with 10µM CuCl were 9.59 and 2.22µM, respectively. The animal testing indicated that GG/GS/CQ/EDC film was decreased epidermal growth factor receptor (EGFR) expression and suppress tumor progression. These findings provide insights into a possible use for GG/GS/CQ/EDC film for oral ca in clinical practice. The GG/GS/CQ/EDC film is suitable as the dressing for use in the treatment of early-stage cancer or as wound care after surgery in late-stage of oral cancer treatment.
[Mh] Termos MeSH primário: Antineoplásicos/química
Clioquinol/química
Portadores de Fármacos/química
Glucosamina/química
Polissacarídeos Bacterianos/química
[Mh] Termos MeSH secundário: 9,10-Dimetil-1,2-benzantraceno/toxicidade
Animais
Antineoplásicos/uso terapêutico
Antineoplásicos/toxicidade
Carbodi-Imidas/química
Linhagem Celular Tumoral
Sobrevivência Celular/efeitos dos fármacos
Clioquinol/uso terapêutico
Clioquinol/toxicidade
Cobre/química
Cobre/toxicidade
Cricetinae
Modelos Animais de Doenças
Liberação Controlada de Fármacos
Seres Humanos
Neoplasias Bucais/induzido quimicamente
Neoplasias Bucais/tratamento farmacológico
Neoplasias Bucais/patologia
Receptor do Fator de Crescimento Epidérmico/metabolismo
Espectroscopia de Infravermelho com Transformada de Fourier
Resistência à Tração
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Carbodiimides); 0 (Drug Carriers); 0 (Polysaccharides, Bacterial); 141650-20-6 (1-ethyl-3-(3-dimethylaminoethyl)carbodiimide); 57-97-6 (9,10-Dimethyl-1,2-benzanthracene); 7593U09I4D (gellan gum); 789U1901C5 (Copper); 7BHQ856EJ5 (Clioquinol); EC 2.7.10.1 (Receptor, Epidermal Growth Factor); N08U5BOQ1K (Glucosamine)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180205
[Lr] Data última revisão:
180205
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171014
[St] Status:MEDLINE


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[PMID]:29045474
[Au] Autor:Nakamura S; Kunikata T; Matsumoto Y; Hanaya T; Harashima A; Nishimoto T; Ushio S
[Ad] Endereço:R&D Center, Hayashibara Co., Ltd., Okayama, Japan.
[Ti] Título:Effects of a non-cyclodextrin cyclic carbohydrate on mouse melanoma cells: Characterization of a new type of hypopigmenting sugar.
[So] Source:PLoS One;12(10):e0186640, 2017.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Cyclic nigerosyl nigerose (CNN) is a cyclic tetrasaccharide that exhibits properties distinct from other conventional cyclodextrins. Herein, we demonstrate that treatment of B16 melanoma with CNN results in a dose-dependent decrease in melanin synthesis, even under conditions that stimulate melanin synthesis, without significant cytotoxity. The effects of CNN were prolonged for more than 27 days, and were gradually reversed following removal of CNN. Undigested CNN was found to accumulate within B16 cells at relatively high levels. Further, CNN showed a weak but significant direct inhibitory effect on the enzymatic activity of tyrosinase, suggesting one possible mechanism of hypopigmentation. While a slight reduction in tyrosinase expression was observed, tyrosinase expression was maintained at significant levels, processed into a mature form, and transported to late-stage melanosomes. Immunocytochemical analysis demonstrated that CNN treatment induced drastic morphological changes of Pmel17-positive and LAMP-1-positive organelles within B16 cells, suggesting that CNN is a potent organelle modulator. Colocalization of both tyrosinase-positive and LAMP-1-positive regions in CNN-treated cells indicated possible degradation of tyrosinase in LAMP-1-positive organelles; however, that possibility was ruled out by subsequent inhibition experiments. Taken together, this study opens a new paradigm of functional oligosaccharides, and offers CNN as a novel hypopigmenting molecule and organelle modulator.
[Mh] Termos MeSH primário: Ciclodextrinas/farmacologia
Glucanos/farmacologia
Hipopigmentação/patologia
Melanoma Experimental/patologia
[Mh] Termos MeSH secundário: Animais
Western Blotting
Linhagem Celular Tumoral
Glucosamina/farmacologia
Imuno-Histoquímica
Lisossomos/efeitos dos fármacos
Lisossomos/metabolismo
Melaninas/biossíntese
Melanoma Experimental/metabolismo
Melanossomas/efeitos dos fármacos
Melanossomas/metabolismo
Camundongos
Monofenol Mono-Oxigenase/metabolismo
Pressão Osmótica
Estresse Fisiológico/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Cyclodextrins); 0 (Glucans); 0 (Melanins); 0 (cyclic nigerosylnigerose); EC 1.14.18.1 (Monophenol Monooxygenase); N08U5BOQ1K (Glucosamine)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171031
[Lr] Data última revisão:
171031
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171019
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0186640


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[PMID]:28898238
[Au] Autor:Xu X; Lin J; Zhao Y; Kirkman E; So YS; Bahn YS; Lin X
[Ad] Endereço:Center for Experimental Medicine, The First Affiliated Hospital of Nanchang University, Nanchang, Jiangxi, China.
[Ti] Título:Glucosamine stimulates pheromone-independent dimorphic transition in Cryptococcus neoformans by promoting Crz1 nuclear translocation.
[So] Source:PLoS Genet;13(9):e1006982, 2017 Sep.
[Is] ISSN:1553-7404
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Morphotype switch is a cellular response to external and internal cues. The Cryptococcus neoformans species complex can undergo morphological transitions between the yeast and the hypha form, and such morphological changes profoundly affect cryptococcal interaction with various hosts. Filamentation in Cryptococcus was historically considered a mating response towards pheromone. Recent studies indicate the existence of pheromone-independent signaling pathways but their identity or the effectors remain unknown. Here, we demonstrated that glucosamine stimulated the C. neoformans species complex to undergo self-filamentation. Glucosamine-stimulated filamentation was independent of the key components of the pheromone pathway, which is distinct from pheromone-elicited filamentation. Glucosamine stimulated self-filamentation in H99, a highly virulent serotype A clinical isolate and a widely used reference strain. Through a genetic screen of the deletion sets made in the H99 background, we found that Crz1, a transcription factor downstream of calcineurin, was essential for glucosamine-stimulated filamentation despite its dispensability for pheromone-mediated filamentation. Glucosamine promoted Crz1 translocation from the cytoplasm to the nucleus. Interestingly, multiple components of the high osmolality glycerol response (HOG) pathway, consisting of the phosphorelay system and some of the Hog1 MAPK module, acted as repressors of glucosamine-elicited filamentation through their calcineurin-opposing effect on Crz1's nuclear translocation. Surprisingly, glucosamine-stimulated filamentation did not require Hog1 itself and was distinct from the conventional general stress response. The results demonstrate that Cryptococcus can resort to multiple genetic pathways for morphological transition in response to different stimuli. Given that the filamentous form attenuates cryptococcal virulence and is immune-stimulatory in mammalian models, the findings suggest that morphogenesis is a fertile ground for future investigation into novel means to compromise cryptococcal pathogenesis.
[Mh] Termos MeSH primário: Cryptococcus neoformans/genética
Proteínas Fúngicas/genética
Glucosamina/metabolismo
Morfogênese/genética
[Mh] Termos MeSH secundário: Calcineurina/metabolismo
Núcleo Celular/genética
Núcleo Celular/metabolismo
Cryptococcus neoformans/crescimento & desenvolvimento
Citoplasma/genética
Citoplasma/metabolismo
Proteínas Fúngicas/metabolismo
Hifas/genética
Hifas/crescimento & desenvolvimento
Proteínas Quinases Ativadas por Mitógeno/genética
Feromônios/genética
Feromônios/metabolismo
Transporte Proteico/genética
Transdução de Sinais
Fatores de Transcrição/genética
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Fungal Proteins); 0 (Pheromones); 0 (Transcription Factors); EC 2.7.11.24 (Mitogen-Activated Protein Kinases); EC 3.1.3.16 (Calcineurin); N08U5BOQ1K (Glucosamine)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171009
[Lr] Data última revisão:
171009
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170913
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pgen.1006982


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[PMID]:28754801
[Au] Autor:Runhaar J; Rozendaal RM; van Middelkoop M; Bijlsma HJW; Doherty M; Dziedzic KS; Lohmander LS; McAlindon T; Zhang W; Bierma Zeinstra S
[Ad] Endereço:Department of General Practice, Erasmus University Medical Center Rotterdam, Rotterdam, The Netherlands.
[Ti] Título:Subgroup analyses of the effectiveness of oral glucosamine for knee and hip osteoarthritis: a systematic review and individual patient data meta-analysis from the OA trial bank.
[So] Source:Ann Rheum Dis;76(11):1862-1869, 2017 Nov.
[Is] ISSN:1468-2060
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:OBJECTIVE: To evaluate the effectiveness of oral glucosamine in subgroups of people with hip or knee osteoarthritis (OA) based on baseline pain severity, body mass index (BMI), sex, structural abnormalities and presence of inflammation using individual patient data. METHODS: After a systematic search of the literature and clinical trial registries, all randomised controlled trials (RCTs) evaluating the effect of any oral glucosamine substance in patients with clinically or radiographically defined hip or knee OA were contacted. As a minimum, pain, age, sex and BMI at baseline and pain as an outcome measure needed to be assessed. RESULTS: Of 21 eligible studies, six (n=1663) shared their trial data with the OA Trial Bank. Five trials (all independent of industry, n=1625) compared glucosamine with placebo, representing 55% of the total number of participants in all published placebo-controlled RCTs. Glucosamine was no better than placebo for pain or function at short (3 months) and long-term (24 months) follow-up. Glucosamine was also no better than placebo among the predefined subgroups. Stratification for knee OA and type of glucosamine did not alter these results. CONCLUSIONS: Although proposed and debated for several years, open trial data are not widely made available for studies of glucosamine for OA, especially those sponsored by industry. Currently, there is no good evidence to support the use of glucosamine for hip or knee OA and an absence of evidence to support specific consideration of glucosamine for any clinically relevant OA subgroup according to baseline pain severity, BMI, sex, structural abnormalities or presence of inflammation.
[Mh] Termos MeSH primário: Anti-Inflamatórios/administração & dosagem
Glucosamina/administração & dosagem
Osteoartrite do Quadril/tratamento farmacológico
Osteoartrite do Joelho/tratamento farmacológico
[Mh] Termos MeSH secundário: Administração Oral
Adulto
Idoso
Artralgia/tratamento farmacológico
Artralgia/etiologia
Índice de Massa Corporal
Feminino
Articulação do Quadril/efeitos dos fármacos
Articulação do Quadril/patologia
Seres Humanos
Articulação do Joelho/efeitos dos fármacos
Articulação do Joelho/patologia
Masculino
Meia-Idade
Osteoartrite do Quadril/complicações
Osteoartrite do Quadril/patologia
Osteoartrite do Joelho/complicações
Osteoartrite do Joelho/patologia
Ensaios Clínicos Controlados Aleatórios como Assunto
Índice de Gravidade de Doença
Fatores Sexuais
Resultado do Tratamento
[Pt] Tipo de publicação:JOURNAL ARTICLE; META-ANALYSIS; REVIEW
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents); N08U5BOQ1K (Glucosamine)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171023
[Lr] Data última revisão:
171023
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170730
[St] Status:MEDLINE
[do] DOI:10.1136/annrheumdis-2017-211149


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[PMID]:28657529
[Au] Autor:Puente R; Illnait J; Mas R; López E; Mendoza S; Carbajal D; Fernández J; Fernández L; Mesa M; Reyes P; Ruiz D
[Ad] Endereço:Surgical Medical Research Centre (Havana, Cuba).
[Ti] Título:Comparison of the efficacy and tolerability of chondroitin plus glucosamine and D-002 (beeswax alcohols) in subjects with osteoarthritis symptoms.
[So] Source:Rev Fac Cien Med Univ Nac Cordoba;74(2):107-118, 2017.
[Is] ISSN:1853-0605
[Cp] País de publicação:Argentina
[La] Idioma:eng
[Ab] Resumo:BACKGROUND/AIMS: Osteoarthritis (OA), the commonest joint disorder, is a leading cause of disability. Symptomatic slow-acting drugs for OA (SYSADOA), particularly glucosamine plus chondroitin sulphate (GS/CS), are effective for symptom relief, protect joint cartilage and delay OA progression, with a good safety profile. D-002, a mixture of beeswax alcohols that inhibits both cyclooxygenase and 5-lipoxygenase activities, has been effective in experimental and clinical OA studies, showing also a chondroprotective effect. OBJECTIVES: To compare the effects of D-002 and GS/SC administered for 12 weeks on OA symptoms. METHODS: Participants were randomized to GS/CS (375/300 mg) or 50 mg D-002 once daily for 12 weeks. Symptoms were assessed by the Western Ontario and McMaster Individual Osteoarthritis Index (WOMAC) and the Visual Analogy Scale (VAS) scores. The primary outcome was the reduction of the total WOMAC score. Secondary outcomes included WOMAC pain, stiffness and function scores, VAS score and rescue medication consumption. RESULTS: Of 60 randomized patients, 59 completed the study. D-002 and GS/SC reduced significantly total WOMAC score (72.1% and 78.5%, respectively), and pain, joint stiffness and physical function scores versus baseline. VAS scores decreased significantly with D-002 (76.6%) and GS/SC (76.8%). The reductions, significant from the second week, were enhanced over the trial. Rescue medications were consumed by 3/30 D-002 and 4/30 GS/SC patients. No differences between groups were found. Treatments were well tolerated. CONCLUSIONS: D-002 (50 mg/day) administered for 12 weeks was safe and comparable to GS/SC for alleviating OA symptoms (pain, stiffness, and functional limitation) (RPCEC00000180).
[Mh] Termos MeSH primário: Sulfatos de Condroitina/administração & dosagem
Álcoois Graxos/administração & dosagem
Glucosamina/administração & dosagem
Osteoartrite/tratamento farmacológico
[Mh] Termos MeSH secundário: Adulto
Idoso
Idoso de 80 Anos ou mais
Sulfatos de Condroitina/efeitos adversos
Quimioterapia Combinada
Álcoois Graxos/efeitos adversos
Feminino
Glucosamina/efeitos adversos
Seres Humanos
Masculino
Meia-Idade
Índice de Gravidade de Doença
Resultado do Tratamento
Adulto Jovem
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; RANDOMIZED CONTROLLED TRIAL
[Nm] Nome de substância:
0 (D 002); 0 (Fatty Alcohols); 9007-28-7 (Chondroitin Sulfates); N08U5BOQ1K (Glucosamine)
[Em] Mês de entrada:1707
[Cu] Atualização por classe:170726
[Lr] Data última revisão:
170726
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170629
[St] Status:MEDLINE


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[PMID]:28535934
[Au] Autor:Bottelli S; Grillo G; Barindelli E; Nencioni A; Di Maria A; Fossati T
[Ad] Endereço:IBSA Institut Biochimque SA, Via del Piano 29, CH-6915 Pambio-Noranco, Switzerland.
[Ti] Título:Validated high-performance anion-exchange chromatography with pulsed amperometric detection method for the determination of residual keratan sulfate and other glucosamine impurities in sodium chondroitin sulfate.
[So] Source:J Chromatogr A;1505:43-49, 2017 Jul 07.
[Is] ISSN:1873-3778
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:An efficient and sensitive analytical method based on high-performance anion exchange chromatography with pulsed amperometric detection (HPAEC-PAD) was devised for the determination of glucosamine (GlcN) in sodium chondroitin sulfate (CS). Glucosamine (GlcN) is intended as marker of residual keratan sulfate (KS) and other impurities generating glucosamine by acidic hydrolyzation. The latter brings CS and KS to their respective monomers. Since GlcN is present only in KS we developed a method that separates GlcN from GalN, the principal hydrolytic product of CS, and then we validated it in order to quantify GlcN. Method validation was performed by spiking CS raw material with known amounts of KS. Detection limit was 0.5% of KS in CS (corresponding to 0.1µg/ml), and the linear range was 0.5-5% of KS in CS (corresponding to 0.1-1µg/ml). The optimized analysis was carried out on an ICS-5000 system (Dionex, Sunnyvale, CA, USA) equipped with a Dionex Amino Trap guard column (3mm×30mm), Dionex CarboPac-PA20 (3mm×30mm) and a Dionex CarboPac-PA20 analytical column (3mm×150mm) using gradient elution at a 0.5ml/min flow rate. Regression equations revealed good linear relationship (R =0.99, n=5) within the test ranges. Quality parameters, including precision and accuracy, were fully validated and found to be satisfactory. The fully validated HPAEC-PAD method was readily applied for the quantification of residual KS in CS in several raw materials and USP/EP reference substance. Results confirmed that the HPAEC-PAD method is more specific than the electrophoretic method for related substance reported in EP and provides sensitive determination of KS in acid-hydrolyzed CS samples, enabling the quantitation of KS and other impurities (generating glucosamine) in CS.
[Mh] Termos MeSH primário: Sulfatos de Condroitina/química
Cromatografia Líquida de Alta Pressão/métodos
Glucosamina/análise
Sulfato de Ceratano/análise
[Mh] Termos MeSH secundário: Resinas de Troca de Ânions/química
Cromatografia Líquida de Alta Pressão/instrumentação
Glucosamina/isolamento & purificação
Sulfato de Ceratano/isolamento & purificação
Limite de Detecção
[Pt] Tipo de publicação:JOURNAL ARTICLE; VALIDATION STUDIES
[Nm] Nome de substância:
0 (Anion Exchange Resins); 9007-28-7 (Chondroitin Sulfates); 9056-36-4 (Keratan Sulfate); N08U5BOQ1K (Glucosamine)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171016
[Lr] Data última revisão:
171016
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170525
[St] Status:MEDLINE


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[PMID]:28535336
[Au] Autor:Bhattacherjee A; Hrynets Y; Betti M
[Ad] Endereço:Department of Agricultural, Food and Nutritional Science, University of Alberta 410 Agriculture/Forestry Centre, Edmonton AB T6G 2P5, Canada.
[Ti] Título:Transport of the Glucosamine-Derived Browning Product Fructosazine (Polyhydroxyalkylpyrazine) Across the Human Intestinal Caco-2 Cell Monolayer: Role of the Hexose Transporters.
[So] Source:J Agric Food Chem;65(23):4642-4650, 2017 Jun 14.
[Is] ISSN:1520-5118
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The transport mechanism of fructosazine, a glucosamine self-condensation product, was investigated using a Caco-2 cell model. Fructosazine transport was assessed by measuring the bidirectional permeability coefficient across Caco-2 cells. The mechanism of transport was evaluated using phlorizin, an inhibitor of sodium-dependent glucose cotransporters (SGLT) 1 and 2, phloretin and quercetin, inhibitors of glucose transporters (GLUT) 1 and 2, transcytosis inhibitor wortmannin, and gap junction disruptor cytochalasin D. The role of hexose transporters was further studied using downregulated or overexpressed cell lines. The apparent permeability (P ) of fructosazine was 1.30 ± 0.02 × 10 cm/s. No significant (p > 0.05) effect was observed in fructosazine transport by adding wortmannin and cytochalasin D. The presence of phlorizin, phloretin, and quercetin decreased fructosazine transport. The downregulated GLUT cells line was unable to transport fructosazine. In human intestinal epithelial Caco-2 cells, GLUT1 or GLUT2 and SGLT are mainly responsible for fructosazine transport.
[Mh] Termos MeSH primário: Glucosamina/metabolismo
Intestinos/metabolismo
Proteínas de Transporte de Monossacarídeos/metabolismo
Pirazinas/metabolismo
[Mh] Termos MeSH secundário: Transporte Biológico
Células CACO-2
Glucosamina/química
Glucose/metabolismo
Seres Humanos
Proteínas de Transporte de Monossacarídeos/genética
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Monosaccharide Transport Proteins); 0 (Pyrazines); 13121-64-7 (tagatosazine); IY9XDZ35W2 (Glucose); N08U5BOQ1K (Glucosamine)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:170626
[Lr] Data última revisão:
170626
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170524
[St] Status:MEDLINE
[do] DOI:10.1021/acs.jafc.7b01611


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[PMID]:28498332
[Au] Autor:Li FR; Fan ZF; Qi SJ; Wang YS; Wang J; Liu Y; Cheng MS
[Ad] Endereço:Key Laboratory of Structure-Based Drugs Design and Discovery (Ministry of Education), School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China. lifengran_1989@163.com.
[Ti] Título:Design, Synthesis, Molecular Docking Analysis, and Carbonic Anhydrase IX Inhibitory Evaluations of Novel N-Substituted-ß-d-Glucosamine Derivatives that Incorporate Benzenesulfonamides.
[So] Source:Molecules;22(5), 2017 May 12.
[Is] ISSN:1420-3049
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:A series of novel -substituted- -d-glucosamine derivatives that incorporate benzenesulfonamides were designed using a fragment-based drug design strategy. Each derivative was synthesized and evaluated in vitro for its inhibitory activity against human carbonic anhydrase (hCA) IX; several derivatives displayed desirable potency profiles against this enzyme. The molecular docking studies provided the design rationale and predicted potential binding modes for carbonic anhydrase (CA) IX and three target compounds, including the most potent inhibitor, compound (IC = 10.01 nM). Moreover, the calculated Log P (cLog P) values showed that all the compounds tended to be hydrophilic. In addition, topological polar surface area (TPSA) value-based predictions highlighted the selectivity of these carbohydrate-based inhibitors for membrane-associated CA IX.
[Mh] Termos MeSH primário: Anidrase Carbônica IX/antagonistas & inibidores
Inibidores da Anidrase Carbônica/farmacologia
Galactosamina/análogos & derivados
Glucosamina/análogos & derivados
Sulfonamidas/síntese química
[Mh] Termos MeSH secundário: Antígenos de Neoplasias/metabolismo
Anidrase Carbônica IX/metabolismo
Desenho de Drogas
Galactosamina/síntese química
Galactosamina/química
Galactosamina/farmacologia
Seres Humanos
Simulação de Acoplamento Molecular
Estrutura Molecular
Relação Estrutura-Atividade
Sulfonamidas/química
Sulfonamidas/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antigens, Neoplasm); 0 (Carbonic Anhydrase Inhibitors); 0 (Sulfonamides); 7535-00-4 (Galactosamine); 98-10-2 (benzenesulfonamide); EC 4.2.1.1 (CA9 protein, human); EC 4.2.1.1 (Carbonic Anhydrase IX); N08U5BOQ1K (Glucosamine)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:170627
[Lr] Data última revisão:
170627
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170513
[St] Status:MEDLINE


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[PMID]:28480412
[Au] Autor:Dai CH; Sun J; Gu XF; Zheng YX
[Ad] Endereço:Luliang County People's Hospital, Qujing City, Yunnan Province 655600, China.
[Ti] Título:USING ARTHROSCOPY TO OBSERVE THE EFFECT OF LIVER-SOFTENING MEDICINE ON KNEE OSTEOARTHRITIS.
[So] Source:Afr J Tradit Complement Altern Med;14(3):12-21, 2017.
[Is] ISSN:2505-0044
[Cp] País de publicação:Nigeria
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Arthroscopy was used to observe the clinical effect of liver-softening medicine for treating knee osteoarthritis (OA). MATERIALS AND METHODS: Forty knee OA patients with cartilage classifications of Outerbridge grade II, III, or II plus III determined via arthroscopy were randomly assigned to a treatment of liver-softening medicine plus glucosamine or a control treatment of glucosamine alone. Clinical observation and determination of the comprehensive effect score were performed at 60, 120, and 180 days. A second arthroscopy was performed at 180 days. RESULTS: Signs and symptoms significantly improved at different time points in the treatment group. The effects in the treatment group were better than those in the control group. When analyzing the cartilage during the second arthroscopy, no further degeneration was observed. CONCLUSIONS: After arthroscopic debridement, the treatment of knee OA with liver-softening medicine in conjunction with glucosamine is a feasible and effective solution.
[Mh] Termos MeSH primário: Artroscopia/métodos
Medicamentos de Ervas Chinesas/administração & dosagem
Glucosamina/administração & dosagem
Fígado/efeitos dos fármacos
Osteoartrite do Joelho/tratamento farmacológico
[Mh] Termos MeSH secundário: Idoso
Desbridamento
Método Duplo-Cego
Quimioterapia Combinada
Estudos de Viabilidade
Feminino
Seres Humanos
Masculino
Meia-Idade
Osteoartrite do Joelho/patologia
Osteoartrite do Joelho/cirurgia
Resultado do Tratamento
[Pt] Tipo de publicação:JOURNAL ARTICLE; RANDOMIZED CONTROLLED TRIAL
[Nm] Nome de substância:
0 (Drugs, Chinese Herbal); N08U5BOQ1K (Glucosamine)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170815
[Lr] Data última revisão:
170815
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170509
[St] Status:MEDLINE
[do] DOI:10.21010/ajtcam.v14i3.2



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