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https://www.readbyqxmd.com/read/29779240/synthesis-characterization-and-reactivity-of-3-mercaptopyruvic-acid
#1
Erwan Galardon, Jean-Chrstophe Lec
A synthesis of the sulfur metabolic compound 3-mercaptopyruvic acid (3-MPH) is reported and allowed its isolation and characterization for the first time. Detailed kinetic, thermodynamic and spectroscopic studies of its complex behaviour in solution are discussed.
May 20, 2018: Chembiochem: a European Journal of Chemical Biology
https://www.readbyqxmd.com/read/29778820/synthesis-of-bioactive-compounds-from-vermicast-isolated-actinomycetes-species-and-its-antimicrobial-activity-against-human-pathogenic-bacteria
#2
R Balachandar, N Karmegam, M Saravanan, R Subbaiya, P Gurumoorthy
The present study aimed to evaluate the antimicrobial activities of bioactive compounds synthesized from vermicast isolated actinomycetes species. Specifically, the synthesized bioactive compounds were evaluated for their antimicrobial activity against selected Gram + ve and Gram-ve human pathogenic bacteria including Staphylococcus aureus, Bacillus circulans, Bacillus subtilis, Pseudomonas aeruginosa, and Escherichia coli. Interestingly, a total of five different actinomycetesspecies were recovered from vermicasts...
May 17, 2018: Microbial Pathogenesis
https://www.readbyqxmd.com/read/29777813/polyphenolic-polysaccharide-conjugates-from-flowers-and-fruits-of-single-seeded-hawthorn-crataegus-monogyna-jacq-chemical-profiles-and-mechanisms-of-anticoagulant-activity
#3
Izabela Pawlaczyk-Graja
The polyphenolic-polysaccharide conjugates were isolated from flowers and fruits of medicinal plant Crataegus monogyna Jacq. (Lindm.) by the alkaline extraction, followed by neutralization, partitioning with organic solvents and dialysis against water. The isolates from flowers as well as from fruits were homogenous macromolecular compounds, with a molecular weight over 760 × 103  g/mol and 970 × 103  g/mol, respectively, what was assessed in HPGPC analysis. Both products were characterized spectrophotometrically, and by GLC-MS, FT-IR and NMR techniques...
May 16, 2018: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/29775685/phenotypic-and-genetic-resistance-traits-in-pseudomonas-aeruginosa-strains-infecting-cystic-fibrosis-patients-a-french-cohort-study
#4
Nathalie Courtois, Yvan Caspar, Max Maurin
Pseudomonas aeruginosa is responsible for chronic respiratory tract colonisation and acute exacerbations in cystic fibrosis (CF) patients. This Gram-negative bacterium often develops multidrug resistance, which represents a therapeutic challenge. Our objective was to characterize the phenotypic and genetic β-lactam resistance traits of P. aeruginosa strains isolated from CF patients followed at Grenoble Alpes university hospital. The susceptibility to β-lactam compounds of 123 P. aeruginosa strains collected from the lower respiratory tract of 45 CF patients, between 2010 and 2014, was evaluated...
May 15, 2018: International Journal of Antimicrobial Agents
https://www.readbyqxmd.com/read/29775541/molecular-characterization-and-bioactivity-of-coumarin-derivatives-from-the-fruits-of-cucumis-bisexualis
#5
Qin-Ge Ma, Rong-Rui Wei, Ming Yang, Xiao-Ying Huang, Fang Wang, Zhi-Pei Sang, Wen-Min Liu, Qing Yu
Cucumis bisexualis (Cucurbitaceae) is known as "mapao egg" or "muskmelon egg", which has been widely used as a wild melon in Chinese folk. Nine new coumarin derivatives (1-9), named 7-hydroxy-3-(4',6'-dihydroxy-5'-isopropyl-3'',3''-dimethyl-2H-chromen)-6-prenyl-2H-chromen-2-one (1), 7-hydroxy-3-(5'-prenyl-3'',3''-dimethyl-2H-chromen)-6-prenyl-2H-chromen-2-one (2), 3-(6'-hydroxy-5'-prenyl-3'',3''-dimethyl-2H-chromen)-6-prenyl-2H-chromen-2-one (3), 3-(5'-ethyl-3'',3''-dimethyl-2H-chromen)-6-prenyl-2H-chromen-2-one (4), 3-(4',6'-dihydroxy-5'-dimethylallyl-3'',3''-dimethyl-2H-chromen)-6-prenyl-2H-chromen-2-one (5), 3-[4',6'-dihydroxy-5'-(2-propenyl)-3'',3''-dimethyl-2H-chromen]-14,15-dimethyl-pyrano-chromen-2-one (6), 3-(6'-dihydroxy-5'-isopropanol-3'',3''-dimethyl-2H-chromen)-14,15-dimethyl-pyrano-chromen-2-one (7), 3-(5'-isopentenol-3'',3''-dimethyl-2H-chromen)-14,15-dimethyl-pyrano-chromen-2-one (8), 3-(4',6'-dihydroxy-5'-prenyl-3'',3''-dimethyl-2H-chromen)-14,15-dimethyl-pyrano-chromen-2-one (9), together with twelve known compounds (10-21), were isolated and identified by spectroscopic analysis and references from the active site (EtOAc soluble fraction) of the fruits of C...
May 18, 2018: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/29775474/the-cryptococcus-neoformans-titan-cell-is-an-inducible-and-regulated-morphotype-underlying-pathogenesis
#6
Ivy M Dambuza, Thomas Drake, Ambre Chapuis, Xin Zhou, Joao Correia, Leanne Taylor-Smith, Nathalie LeGrave, Tim Rasmussen, Matthew C Fisher, Tihana Bicanic, Thomas S Harrison, Marcel Jaspars, Robin C May, Gordon D Brown, Raif Yuecel, Donna M MacCallum, Elizabeth R Ballou
Fungal cells change shape in response to environmental stimuli, and these morphogenic transitions drive pathogenesis and niche adaptation. For example, dimorphic fungi switch between yeast and hyphae in response to changing temperature. The basidiomycete Cryptococcus neoformans undergoes an unusual morphogenetic transition in the host lung from haploid yeast to large, highly polyploid cells termed Titan cells. Titan cells influence fungal interaction with host cells, including through increased drug resistance, altered cell size, and altered Pathogen Associated Molecular Pattern exposure...
May 2018: PLoS Pathogens
https://www.readbyqxmd.com/read/29775304/sesquiterpenoids-from-chloranthus-anhuiensis-with-neuroprotective-effects-in-pc12-cells
#7
Jian Xu, Hui-Lin Zhu, Jie Zhang, Tao Du, Er-Yan Guo, Wen-Yuan Liu, Jian-Guang Luo, Feng Ye, Feng Feng, Wei Qu
Glutamate-induced excitotoxicity plays a vital role in neurodegenerative diseases. Neuroprotection against excitotoxicity has been considered as an effective experimental approach for preventing and/or treating excitotoxicity-mediated diseases. In the present study, six new sesquiterpenoids (1-6) and 26 known compounds of this type (7-32) were isolated and characterized from the whole plants of Chloranthus anhuiensis. Chlorantolide A (1) is the first example of a 5,6- seco-germacrane-type sesquiterpenoid, while phacadinane E (2) is a rare 4,5- seco-cadinane-type sesquiterpenoid...
May 18, 2018: Journal of Natural Products
https://www.readbyqxmd.com/read/29775053/uranyl-tri-bis-silyl-amide-alkali-metal-contact-and-separated-ion-pair-complexes
#8
Philip J Cobb, David J Moulding, Fabrizio Ortu, Simon Randall, Ashley J Wooles, Louise S Natrajan, Stephen T Liddle
We report the preparation of a range of alkali metal uranyl(VI) tri- bis(silyl)amide complexes [{M(THF) x }{(μ-O)U(O)(N″)3 }] (1M) (N″ = {N(SiMe3 )2 }- , M = Li, Na, x = 2; M = K, x = 3; M = K, Rb, Cs, x = 0) containing electrostatic alkali metal uranyl-oxo interactions. Reaction of 1M with 2,2,2-cryptand or 2 equiv of the appropriate crown ether resulted in the isolation of the separated ion pair species [U(O)2 (N″)3 ][M(2,2,2-cryptand)] (3M, M = Li-Cs) and [U(O)2 (N″)3 ][M(crown)2 ] (4M, M = Li, crown = 12-crown-4 ether; M = Na-Cs, crown = 15-crown-5 ether)...
May 18, 2018: Inorganic Chemistry
https://www.readbyqxmd.com/read/29770548/the-chemistry-of-the-2-phosphaethynolate-anion
#9
Hansjörg Grützmacher, José Goicoechea
Likely the first synthesis of the phosphaethynolate anion, PCO-, was performed already in 1894 when NaPH2 was reacted with CO in an attempt to make Na(CP) under elimination of water. This reaction was repeated only 117 years later when it was discovered that Na(OCP) and H2 are the products of this remarkable transformation. Li(OCP) was synthesized and fully characterized in 1992 but this salt proved to be too unstable to allow a detailed investigation. Remarkably, it needs the heavier analogues of this lithium salt, Na(OCP) and K(OCP), which are remarkably stable and can be even dissolved in water, to fully explore fully the chemistry of this new functional group...
May 17, 2018: Angewandte Chemie
https://www.readbyqxmd.com/read/29769313/a-catalytically-versatile-benzoyl-coa-reductase-key-enzyme-in-the-degradation-of-methyl-and-halobenzoates-in-denitrifying-bacteria
#10
Oliver Tiedt, Jonathan Fuchs, Wolfgang Eisenreich, Matthias Boll
Class I benzoyl-coenzyme A (BzCoA) reductases (BCRs) are key enzymes in the anaerobic degradation of aromatic compounds. They catalyze the ATP-dependent reduction of the central BzCoA intermediate and analogues of it to conjugated cyclic 1,5-dienoyl-CoAs probably by a radical-based, Birch-like reduction mechanism. Discovered in 1995, the enzyme from the denitrifying bacterium Thauera aromatica (BCRTar ) has so far remained the only isolated and biochemically accessible BCR, mainly because BCRs are extremely labile and their heterologous production has largely failed, so far...
May 16, 2018: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/29769246/small-molecule-positive-allosteric-modulators-of-the-%C3%AE-2-adrenoceptor-isolated-from-dna-encoded-libraries
#11
Seungkirl Ahn, Biswaranjan Pani, Alem W Kahsai, Eva K Olsen, Gitte Husemoen, Mikkel Vestrgaard, Lei Jin, Shuai Zhao, Laura M Wingler, Paula K Rambarat, Rishabh K Simhal, Thomas T Xu, Lillian D Sun, Paul J Shim, Dean P Staus, Li-Yin Huang, Thomas Franch, Xin Chen, Robert J Lefkowitz
Conventional drug discovery efforts at the β2 -adrenoceptor (β2 AR) have led to the development of ligands that bind almost exclusively to the receptor's hormone-binding orthosteric site. However, targeting the largely unexplored and evolutionarily unique allosteric sites has potential for developing more specific drugs with fewer side effects than orthosteric ligands. Using our recently developed approach for screening G protein-coupled receptors (GPCRs) with DNA-encoded small molecule libraries, we have discovered and characterized the first β2 AR small molecule positive allosteric modulators (PAMs) - compound-6 [(R)-N-(4-amino-1-(4-(tert-butyl)phenyl)-4-oxobutan-2-yl)-5-(N-isopropyl-N-methylsulfamoyl)-2-((4-methoxyphenyl) thio)benzamide] and its analogs...
May 16, 2018: Molecular Pharmacology
https://www.readbyqxmd.com/read/29767975/cytotoxic-anthracycline-metabolites-from-a-recombinant-streptomyces
#12
Chun Gui, Jie Yuan, Xuhua Mo, Hongbo Huang, Shanwen Zhang, Yu-Cheng Gu, Jianhua Ju
The C7 (C9 or C10)- O-l-rhodosamine-bearing anthracycline antibiotic cytorhodins and their biosynthetic intermediates were recently isolated from Streptomyces sp. SCSIO 1666. Cosmid p17C4 from the Streptomyces lydicus genomic library, which harbors both the biosynthetic genes for l-rhodinose (or 2-deoxy-l-fucose) and its glycosyltransferase (encoded by slgG), was introduced into SCSIO 1666 to yield the recombinant strain Streptomyces sp. SCSIO 1666/17C4. Chemical investigations of this strain's secondary metabolic potential revealed the production of different anthracyclines featuring C7- O-l-rhodinose (or 2-deoxy-l-fucose) instead of the typically observed l-rhodosamine...
May 16, 2018: Journal of Natural Products
https://www.readbyqxmd.com/read/29764947/biological-roles-played-by-sphingolipids-in-dimorphic-and-filamentous-fungi
#13
REVIEW
Caroline Mota Fernandes, Gustavo H Goldman, Maurizio Del Poeta
Filamentous and dimorphic fungi cause invasive mycoses associated with high mortality rates. Among the fungal determinants involved in the establishment of infection, glycosphingolipids (GSLs) have gained increased interest in the last few decades. GSLs are ubiquitous membrane components that have been isolated from both filamentous and dimorphic species and play a crucial role in polarized growth as well as hypha-to-yeast transition. In fungi, two major classes of GSLs are found: neutral and acidic GSLs. Neutral GSLs comprise glucosylceramide and galactosylceramide, which utilize Δ4-Δ8-9-methyl-sphingadienine as a sphingoid base, linked to a C16-18 fatty acid chain, forming ceramide, and to a sugar residue, such as glucose or galactose...
May 15, 2018: MBio
https://www.readbyqxmd.com/read/29763728/in-vitro-and-in-silico-antimicrobial-activity-of-sterol-and-flavonoid-isolated-from-trianthema-decandra-l
#14
R Geethalakshmi, D V L Sarada
Phytochemical study on the leaves of Trianthema decandra leads to the isolation and characterization of two compounds from chloroform extract. The compounds were characterized using HPLC, UV, FT-IR, NMR, LCMS and CHNS. The structure of compounds were elucidated from spectral data and named according to rules laid down in IUPAC nomenclature. A novel sterol was named as 17-(5-ethyl-6-methylheptan-2-yl) -4, 4, 10, 13-tetramethyl-hexadecahydro-1H-cyclopenta (α) phenanthren-3-ol and the flavonoid was named as 2-(3, 4 dihydroxy - phenyl)-3, 5, 7 - trihydroxy-chromen-4 one...
May 12, 2018: Microbial Pathogenesis
https://www.readbyqxmd.com/read/29758934/adipose-tissue-derived-stem-cells-from-affected-and-unaffected-areas-in-patients-with-multiple-symmetric-lipomatosis-show-differential-regulation-of-mtor-pathway-genes
#15
Oliver Felthaus, Teresa Schön, Daniel Schiltz, Thiha Aung, Britta Kühlmann, Friedrich Jung, Alexandra Anker, Silvan Klein, Lukas Prantl
BACKGROUND: Multiple symmetric lipomatosis is a rare disease characterized by the excessive growth of uncapsulated masses of adipose tissue. Although the etiology has yet to be elucidated, a connection to brown adipose tissue has been proposed recently. The mTOR pathway which is found to be regulated in lipomatous tissue as well as associated with brown adipose tissue can be inhibited by a compound called rapamycin. METHODS: We isolated adipose tissue derived stem cells from both affected and unaffected tissue and treated these cells with different concentrations of rapamycin...
2018: Clinical Hemorheology and Microcirculation
https://www.readbyqxmd.com/read/29758007/characterization-of-rhamnolipids-produced-by-an-arctic-marine-bacterium-from-the-pseudomonas-fluorescence-group
#16
Venke Kristoffersen, Teppo Rämä, Johan Isaksson, Jeanette Hammer Andersen, William H Gerwick, Espen Hansen
The marine environment is a rich source of biodiversity, including microorganisms that have proven to be prolific producers of bioactive secondary metabolites. Arctic seas are less explored than warmer, more accessible areas, providing a promising starting point to search for novel bioactive compounds. In the present work, an Arctic marine Pseudomonas sp. belonging to the Pseudomonas (P.) fluorescence group was cultivated in four different media in an attempt to activate biosynthetic pathways leading to the production of antibacterial and anticancer compounds...
May 14, 2018: Marine Drugs
https://www.readbyqxmd.com/read/29757957/arthroprotective-effects-of-cf-02-sharing-structural-similarity-with-quercetin
#17
Feng-Cheng Liu, Jeng-Wei Lu, Chiao-Yun Chien, Hsu-Shan Huang, Chia-Chung Lee, Shiu-Bii Lien, Leou-Chyr Lin, Liv Weichien Chen, Yi-Jung Ho, Min-Chung Shen, Ling-Jun Ho, Jenn-Haung Lai
In this study, we synthesized hundreds of analogues based on the structure of small-molecule inhibitors (SMIs) that were previously identified in our laboratory with the aim of identifying potent yet safe compounds for arthritis therapeutics. One of the analogues was shown to share structural similarity with quercetin, a potent anti-inflammatory flavonoid present in many different fruits and vegetables. We investigated the immunomodulatory effects of this compound, namely 6-(2,4-difluorophenyl)-3-(3-(trifluoromethyl)phenyl)-2 H -benzo[ e ][1,3]oxazine-2,4(3 H )-dione (Cf-02), in a side-by-side comparison with quercetin...
May 14, 2018: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29757646/inhibition-of-breast-cancer-cell-migration-by-cyclotides-isolated-from-pombalia-calceolaria
#18
Meri Emili F Pinto, Jhenny Z G Najas, Luma G Magalhães, Antonio F Bobey, Jacqueline N Mendonça, Norberto P Lopes, Flávia M Leme, Simone P Teixeira, Marcelo Trovó, Adriano D Andricopulo, Johannes Koehbach, Christian W Gruber, Eduardo Maffud Cilli, Vanderlan S Bolzani
Two new bracelet cyclotides from roots of Pombalia calceolaria with potential anticancer activity have been characterized in this work. The cyclotides Poca A and B (1 and 2) and the previously known CyO4 (3) were de novo sequenced by MALDI-TOF/TOF mass spectrometry (MS). The MS2 spectra were examined and the amino acid sequences were determined. The purified peptides were tested for their cytotoxicity and effects on cell migration of MDA-MB-231, a triple-negative breast cancer cell line. The isolated cyclotides reduced the number of cancer cells by more than 80% at 20 μM, and the concentration-related cytotoxic responses were observed with IC50 values of 1...
May 14, 2018: Journal of Natural Products
https://www.readbyqxmd.com/read/29756660/synthesis-of-azo-dyes-from-mesoionic-carbenes-and-nitrous-oxide
#19
Léonard Y M Eymann, Rosario Scopelliti, Farzaneh Fadaei Tirani, Kay Severin
Covalent adducts of imidazole-based mesoionic carbenes and nitrous oxide (N2 O, "laughing gas") can be converted into azo dyes by reaction with arenes in the presence of AlCl3 or HCl. The azo coupling can be achieved with electron-rich aromatic compounds such as mesitylene, trimethoxybenzene, azulene, or dibenzo-18-crown-6. The latter coupling reaction allows for the easy preparation of a colorimetric sensor for potassium or sodium ions. As a putative intermediate of the reaction with acid, we were able to isolate and structurally characterize a rare diazohydroxide...
May 14, 2018: Chemistry: a European Journal
https://www.readbyqxmd.com/read/29755552/efficacy-of-alpha-glucosidase-inhibitor-from-marine-actinobacterium-in-the-control-of-postprandial-hyperglycaemia-in-streptozotocin-stz-induced-diabetic-male-albino-wister-rats
#20
S R Sathish Kumar, K V Bhaskara Rao
The current study was carried out to evaluate the in-vitro and in-vivo efficiency of alpha glucosidase inhibitor of marine actinobacteria in the control of postprandial hyperglycaemia. Soil samples were collected from salterns, coastal area in Kothapatnam, Ongole, Andhra Pradesh, India. Among the actinobacterial isolates tested for yeastα-glucosidase inhibitory activity, only three isolates showed prominent inhibition. The patient isolate was selected and identified as Streptomyces coelicoflavus SRBVIT13 using 16S r-RNA gene sequencing...
2018: Iranian Journal of Pharmaceutical Research: IJPR
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