Database : MEDLINE
Search on : glycosides [Words]
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[PMID]: 29523385
[Au] Autor:Kuo GH; Gaul MD; Liang Y; Xu JZ; Du F; Hornby P; Xu G; Qi J; Wallace N; Lee S; Grant E; Murray WV; Demarest K
[Ad] Address:Cardiovascular and Metabolism Research, Janssen Research and Development, L.L.C., Welsh & McKean Roads, Spring House, PA 19477, USA. Electronic address: gkuo@its.jnj.com.
[Ti] Title:Synthesis and biological evaluation of benzocyclobutane-C-glycosides as potent and orally active SGLT1/SGLT2 dual inhibitors.
[So] Source:Bioorg Med Chem Lett;, 2018 Mar 01.
[Is] ISSN:1464-3405
[Cp] Country of publication:England
[La] Language:eng
[Ab] Abstract:Synthesis and biological evaluation of benzocyclobutane-C-glycosides as potent and orally active SGLT1/SGLT2 dual inhibitors are described. Compound 19 showed high inhibitory potency at SGLT1 (IC = 45 nM), and excellent potency at SGLT2 (IC = 1 nM). It also displayed excellent PK profiles in mice, rats, dogs and monkeys (F = 78-107%). In SD rats, compound 19 treatments significantly reduced blood glucose levels in a dose-dependent manner. In ZDF rats, compound 19 displayed anti-hyperglycemic effect up to 24 h. Therefore, compound 19 may serve as valuable pharmacological tool, and potential use as a treatment for metabolic syndrome.
[Pt] Publication type:JOURNAL ARTICLE
[Em] Entry month:1803
[Cu] Class update date: 180310
[Lr] Last revision date:180310
[St] Status:Publisher

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[PMID]: 29522916
[Au] Autor:Yan S; Ren S; Ding N; Li Y
[Ad] Address:School of Pharmacy, Fudan University, Shanghai 201203, China.
[Ti] Title:Concise total synthesis of acylated phenolic glycosides vitexnegheteroin A and ovatoside D.
[So] Source:Carbohydr Res;460:41-46, 2018 Mar 02.
[Is] ISSN:1873-426X
[Cp] Country of publication:Netherlands
[La] Language:eng
[Ab] Abstract:Starting from readily available vanillin and α-D-acetobromo glucose, two natural acylated phenolic glycosides vitexnegheteroin A and ovatoside D were synthesized for the first time in 4 steps with overall yields of 54% and 65%, respectively. The key steps involve the directly regioselective O-6 acylation of vanillin -D-glucopyranoside with acyl chlorides, and simultaneous removal of the allyl protecting groups on the phenolic acid moiety and reduction of the aldehyde in the aglycon moiety by using Pd(PPh) -NaBH system in one pot.
[Pt] Publication type:JOURNAL ARTICLE
[Em] Entry month:1803
[Cu] Class update date: 180309
[Lr] Last revision date:180309
[St] Status:Publisher

  3 / 32108 MEDLINE  
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[PMID]: 28934712
[Au] Autor:Stuchlkov LR; Sklov L; Szotkov B; Syslov E; Vokrl I; Vanek T; Podlipn R
[Ad] Address:Department of Biochemical Sciences, Faculty of Pharmacy in Hradec Krlov, Charles University, Heyrovskho 1203, 500 05 Hradec Krlov, Czech Republic. Electronic address: lucie.raisova@faf.cuni.cz.
[Ti] Title:Biotransformation of flubendazole and fenbendazole and their effects in the ribwort plantain (Plantago lanceolata).
[So] Source:Ecotoxicol Environ Saf;147:681-687, 2018 Jan.
[Is] ISSN:1090-2414
[Cp] Country of publication:Netherlands
[La] Language:eng
[Ab] Abstract:Although veterinary anthelmintics represent an important source of environmental pollution, the fate of anthelmintics and their effects in plants has not yet been studied sufficiently. The aim of our work was to identify metabolic pathways of the two benzimidazole anthelmintics fenbendazole (FBZ) and flubendazole (FLU) in the ribwort plantain (Plantago lanceolata L.). Plants cultivated as in vitro regenerants were used for this purpose. The effects of anthelmintics and their biotransformation products on plant oxidative stress parameters were also studied. The obtained results showed that the enzymatic system of the ribwort plantain was able to uptake FLU and FBZ, translocate them in leaves and transform them into several metabolites, particularly glycosides. Overall, 12 FLU and 22 FBZ metabolites were identified in the root, leaf base and leaf top of the plant. Concerning the effects of FLU and FBZ, both anthelmintics in the ribwort plantain cells caused significant increase of proline concentration (up to twice), a well-known stress marker, and significant decrease of superoxide dismutase activity (by 50%). In addition, the activities of four other antioxidant enzymes were significantly changed after either FLU or FBZ exposition. This could indicate a certain risk of oxidative damage in plants influenced by anthelmintics, particularly when they are under other stress conditions.
[Mh] MeSH terms primary: Anthelmintics/toxicity
Fenbendazole/toxicity
Mebendazole/analogs & derivatives
Plantago/drug effects
Veterinary Drugs/toxicity
[Mh] MeSH terms secundary: Animals
Anthelmintics/metabolism
Biotransformation
Fenbendazole/metabolism
Mebendazole/metabolism
Mebendazole/toxicity
Metabolic Networks and Pathways/drug effects
Oxidative Stress/drug effects
Plantago/enzymology
Plantago/growth & development
Veterinary Drugs/metabolism
[Pt] Publication type:JOURNAL ARTICLE
[Nm] Name of substance:0 (Anthelmintics); 0 (Veterinary Drugs); 621BVT9M36 (Fenbendazole); 81G6I5V05I (Mebendazole); R8M46911LR (flubendazole)
[Em] Entry month:1803
[Cu] Class update date: 180309
[Lr] Last revision date:180309
[Js] Journal subset:IM
[Da] Date of entry for processing:170922
[St] Status:MEDLINE

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[PMID]: 29521529
[Au] Autor:Jin M; Zhou W; Jin C; Jiang Z; Diao S; Jin Z; Li G
[Ad] Address:a Key Laboratory of Natural Resources of Changbai Mountain and Functional Molecules, Ministry of Education , Yanbian University College of Pharmacy , Yanji , P. R. China.
[Ti] Title:Anti-inflammatory activities of the chemical constituents isolated from Trametes versicolor.
[So] Source:Nat Prod Res;:1-4, 2018 Mar 09.
[Is] ISSN:1478-6427
[Cp] Country of publication:England
[La] Language:eng
[Ab] Abstract:Twenty-seven compounds including nine triterpenoids (1-9), eight sterols (10-17), two ribonucleotides (18, 19), four phenols (20-23), three glycosides (24-26), and one furan (27) were isolated from the fruiting bodies of Trametes versicolor (L.) Lloyd. This study is the first confirmation of the presence of the 11 compounds (3, 5, 6, 8, 18, 20, 21, 23-25, and 27) isolated from the Polyporaceae family, with six of these (2 and 12-16) from the genus Trametes. Compounds 3, 4, 10, 11, 16 and 17 were found to significantly inhibit the production of NO, TNF-α and IL-6 in a dose-dependent manner.
[Pt] Publication type:JOURNAL ARTICLE
[Em] Entry month:1803
[Cu] Class update date: 180309
[Lr] Last revision date:180309
[St] Status:Publisher
[do] DOI:10.1080/14786419.2018.1446011

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[PMID]: 29521030
[Au] Autor:Mutschlechner B; Rainer B; Schwaiger S; Stuppner H
[Ad] Address:Institute of Pharmacy/Pharmacognosy, University of Innsbruck, and Center for Molecular Biosciences Innsbruck (CMBI), Center for Chemistry and Biomedicine, Innrain 80-82, 6020, Innsbruck, Austria.
[Ti] Title:Tyrosinase Inhibitors from the Aerial Parts of Wulfenia carinthiaca Jacq.
[So] Source:Chem Biodivers;, 2018 Mar 09.
[Is] ISSN:1612-1880
[Cp] Country of publication:Switzerland
[La] Language:eng
[Ab] Abstract:Activity guided isolation of a methanolic extract of the aerial plant parts of Wulfenia carinthiaca Jacq. (Plantaginaceae), using a mushroom tyrosinase assay, resulted in the isolation of five phenylethanoid glucosides and four iridoid glycosides. Two of those, 2'-O-acetylisoplantamajoside and 2',6''-O-diacetylisoplantamajoside, represent new natural products. Evaluation of the inhibitory activity of all isolated compounds revealed that the observed activity is not related to the isolated phenylethanoid glycosides but mainly due to the presence of the iridoid glycoside globularin (IC 41.94 M; CI +/- 16.61/11.89 M). Interestingly, structurally close related compounds (globularicisin, baldaccioside and isoscrophularioside) showed no or only a weak tyrosinase inhibitory activity. This article is protected by copyright. All rights reserved.
[Pt] Publication type:JOURNAL ARTICLE
[Em] Entry month:1803
[Cu] Class update date: 180309
[Lr] Last revision date:180309
[St] Status:Publisher
[do] DOI:10.1002/cbdv.201800014

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[PMID]: 29496527
[Au] Autor:Perucatti A; Genualdo V; Pauciullo A; Iorio C; Incarnato D; Rossetti C; Vizzarri F; Palazzo M; Casamassima D; Iannuzzi L; Iannuzzi A
[Ad] Address:National Research Council (CNR) of Italy, Institute for Animal Production Systems in Mediterranean Environments (ISPAAM), Laboratory of Animal Cytogenetics, Via Argine 1085, 80147 Naples, Italy.
[Ti] Title:Cytogenetic tests reveal no toxicity in lymphocytes of rabbit (Oryctolagus cuniculus, 2n=44) feed in presence of verbascoside and/or lycopene.
[So] Source:Food Chem Toxicol;114:311-315, 2018 Feb 26.
[Is] ISSN:1873-6351
[Cp] Country of publication:England
[La] Language:eng
[Ab] Abstract:Phenylpropanoid glycosides (PPG), like other phenolic compounds, are a powerful antioxidants and the Verbascoside (VB) is one of the most active of them. A previous study, by using in vitro exposure of blood human lymphocytes to Verbascoside, reported a significant increasings of chromosome fragility compared to control. In the present study, four homogeneous groups of rabbits were used to test in vivo the VB and/or Lycopene (LP) by feeding the animals without VB and LP (control), in presence of VB or/and LP for 80 days. Lymphocyte cell cultures were performed in three different times: 0, 40 and 80 days of the experiment and the cytogenetic tests that we used [CA-test (Chromosome Abnormalities in terms of chromosome and chromatid breaks) and Sister Chromatid Exchange (SCE-test)] have revealed no mutagenic effects on chromosomes. Indeed, mean values/cell of CA and SCE decreased during the experiment with some difference among and within groups, with significant decreasing value only for some group. The study shows clear evidence that diets rich in Verbascoside (and/or Lycopene) do not originate any mutagenic activity, resulting no cytotoxic for the animals and, suggesting a possible their use in both animal and human diets.
[Pt] Publication type:JOURNAL ARTICLE
[Em] Entry month:1803
[Cu] Class update date: 180308
[Lr] Last revision date:180308
[St] Status:Publisher

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[PMID]: 29441576
[Au] Autor:Kumar H; Agrawal R; Kumar V
[Ad] Address:Department of Pharmacy, School of Chemical Sciences and Pharmacy, Central University of Rajasthan, Ajmer, India.
[Ti] Title:Barleria cristata: perspective towards phytopharmacological aspects.
[So] Source:J Pharm Pharmacol;70(4):475-487, 2018 Apr.
[Is] ISSN:2042-7158
[Cp] Country of publication:England
[La] Language:eng
[Ab] Abstract:OBJECTIVES: Barleria cristata (Family: Acanthaceae), commonly known as Philippine violet, is used in different ethnomedical systems for the treatment of a wide range of ailments. This review aimed to provide a scientific overview of B.cristata with reference to its ethnobotanical aspects, geographical distribution, medicinal uses, phytochemistry and pharmacological activity, and critical analyses research gaps and future research opportunities for investigations on this plant. KEY FINDINGS: Ethnomedical uses of the plant have been observed in lungs disorders, inflammatory conditions, toothache, anaemia, snake bite, diabetes and tuberculosis. The exhaustive bibliographic research carried out on this plant revealed that the plant parts are rich in various phytochemical constituents including triterpenes, phenolic compounds, glycosides and flavonoids type phenolic compounds. Furthermore, the plant was also investigated in terms of its anti-inflammatory, antibacterial, antidiabetic, antifungal, hepatoprotective and antioxidant activity. CONCLUSIONS: This review confirms that B.cristata is a potential herb for the treatment of a wide range of diseases especially lung disorders and inflammatory conditions. Modern pharmacological studies have also validated many ethnobotanical uses of B.cristata, though data regarding many aspects of this plant such as mechanism of action, adverse effects of extracts and active compounds are still limited which call for additional studies.
[Pt] Publication type:JOURNAL ARTICLE; REVIEW
[Em] Entry month:1802
[Cu] Class update date: 180309
[Lr] Last revision date:180309
[St] Status:In-Process
[do] DOI:10.1111/jphp.12881

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[PMID]: 29513486
[Au] Autor:Khandy MT; Titova MV; Konstantinova SV; Kochkin DV; Ivanov IM; Nosov AM
[Ti] Title:[Formation of protodioscin and deltoside isomers in suspension cultures of Nepal yam (Dioscorea deltoidea Wall.) cells].
[So] Source:Prikl Biokhim Mikrobiol;52(6):614-20, 2016 Nov-Dec.
[Is] ISSN:0555-1099
[Cp] Country of publication:Russia (Federation)
[La] Language:rus
[Ab] Abstract:Changes in the content of the furostanol glycosides protodioscin and deltoside, particularly that of the (25S)-isomers of the glycosides, during suspension cultivation of different lines of Nepal yam (Dioscorea deltoidea Wall.) cells of the strain IFR-DM-0.5 has been investigated. The composition of furostanol glycosides has been characterized, and the dynamics of the accumulation of individual glycosides during lengthy subcultivation of cells maintained in flasks or in a barbotage bioreactor has been analyzed. A positive correlation between the growth and accumulation of substances that belonged to the class of furostanol glycosides has been demonstrated for cultured dioscorea cells, whereas the content of some of the individual glycosides varied considerably between the lines of the strain, cultures maintained under different conditions, and even between cells in different phases of the growth cycle. The increased content of (25R)-forms of the glycosides (protodioscin and deltoside) was correlated with a decrease in the cellular growth rate, whereas an increase in culture growth intensity occurred concomitantly to an increase of the amount of (25S)-isomers. This may be indicative of the specific stimulatory effect of (25S)-glycosides, but not the (25R)-forms, on cell proliferation in vitro. Thus, the concentration of (25S)-forms may increase due to the autoselection of cells capable of intensive division during prolonged cultivation.
[Pt] Publication type:JOURNAL ARTICLE
[Em] Entry month:1803
[Cu] Class update date: 180307
[Lr] Last revision date:180307
[St] Status:In-Process

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[PMID]: 29210609
[Au] Autor:Buffini M; Goscinny S; Van Loco J; Nugent AP; Walton J; Flynn A; Gibney MJ; McNulty BA
[Ad] Address:a School of Agriculture and Food Science , University College Dublin, UCD Institute of Food and Health , Belfield , Ireland.
[Ti] Title:Dietary intakes of six intense sweeteners by Irish adults.
[So] Source:Food Addit Contam Part A Chem Anal Control Expo Risk Assess;35(3):425-438, 2018 Mar.
[Is] ISSN:1944-0057
[Cp] Country of publication:England
[La] Language:eng
[Ab] Abstract:This research investigated the intakes of six intense sweeteners: acesulfame-K (E950), aspartame (E951), cyclamate (E952), saccharin (E954), sucralose (E955), and steviol glycosides (E960) in the diets of Irish adults, using data from the National Adult Nutrition Survey. A food label survey that included products currently available on the Irish market supplemented the analysis. Sweetener intakes were investigated using three different exposure scenarios; beginning with a crude assessment which assumed that all foods permitted to contain the additives of interest always did contain them, and at their maximum permitted level (Tier 1). Refined assessments estimated intakes of the six sweeteners using food consumption data up to brand level with additive occurrence data from a survey of products currently available on the Irish market (Tier 2) and sweetener concentration data (Tier 3). Results of all exposure assessment scenarios demonstrate that intakes of each of the sweeteners of interest by the total population were below the relevant ADI level (mg kg bodyweight ), even by high consumers (P99). The three sweeteners consumed in highest amounts were acesulfame-k, aspartame, and sucralose. The main sources of these sweeteners in the diet were 'cider and perry', 'energy reduced and no added sugar (ER and NAS) carbonated flavoured drinks', 'table-top sweeteners', 'dairy products', 'solid food supplements', and 'sauces'. Intakes of the six intense sweeteners are currently not a concern among Irish adults. However, exposure to these chemicals should be monitored on a regular basis due to evolving market and consumption patterns.
[Pt] Publication type:JOURNAL ARTICLE
[Em] Entry month:1712
[Cu] Class update date: 180308
[Lr] Last revision date:180308
[St] Status:In-Process
[do] DOI:10.1080/19440049.2017.1411619

  10 / 32108 MEDLINE  
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[PMID]: 29512444
[Au] Autor:Du X; Nyagblordzro M; An L; Gao X; Du L; Wang Y; Ondieki G; Kikete S; He X
[Ad] Address:School of Chinese Materia Medica, Tianjin University of Traditional Chinese Medicine, Nankai District, Tianjin 300193. China.
[Ti] Title:Pharmacokinetic and Toxicological Characteristics of Tripterigium Glycosides and Their Derivatives.
[So] Source:Curr Drug Metab;, 2018 Mar 02.
[Is] ISSN:1875-5453
[Cp] Country of publication:Netherlands
[La] Language:eng
[Ab] Abstract:Tripterigium wilfordii glycosides (TWG) demonstrate paramount bioactive effectiveness in the management of many autoimmune diseases, such as rheumatoid arthritis, psoriasis, and nephrotic syndrome. However, its side effects on the hepatic, nephrotic, reproductive, and cardiovascular systems have limited its immense therapeutic potentials. Triptolide (TP) and Celastrol (CL), the leading bioactive as well as toxic constituents of TWG, have been widely studied. These studies have documented the key mechanisms that trigger the toxic reactions and the precautionary measures that could prevent and reduce such reactions. It has been reported that reactive oxygen species (ROS) generation, mitochondrial respiratory chain inhibition, cauda epididymis sperm structure disruption, and metabolizing enzyme inhibition are the leading factors of the toxic reactions. The bioactive effects and toxicities of TWG are closely related to its metabolic profiles. It has been confirmed that TP and CL inhibit Cytochrome P450 (CYP) and the transporters. This paper reviews and summarizes the pharmacokinetic and toxicological parameters of TWG, some mitigative interventions and several implications of its pharmacokinetic characteristics. Antioxidants, polymeric micelle formulations, topical nanoparticle formulations have exhibited potentials in toxicity circumvention. A thorough understanding of the pharmacokinetic and toxicological characteristics of TWG combined with further in-depth study of its efficacy and toxicity will enhance the efficacy and safety in using TWG, which would augment and improve its clinical application in the future.
[Pt] Publication type:JOURNAL ARTICLE
[Em] Entry month:1803
[Cu] Class update date: 180307
[Lr] Last revision date:180307
[St] Status:Publisher
[do] DOI:10.2174/1389200219666180302152752


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