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https://www.readbyqxmd.com/read/28636236/assessment-of-silibinin-as-a-potential-antifungal-agent-and-investigation-of-its-mechanism-of-action
#1
Dae Gyu Yun, Dong Gun Lee
Silibinin, which is derived from Silybum marianum (milk thistle), has used as a traditional remedy for liver or biliary disorders and known to have superior antioxidant activity. In addition, silibinin was recently reported to have antifungal effect related to fungal apoptosis against Candida albicans and the interest in the therapeutic effect is increasing. In this study, we found another mode of antifungal action of silibinin and its antibiofilm activity on C. albicans. To investigate influence on fungal plasma membrane, propidium iodide and bis-(1, 3-dibutylbarbituric acid) trimethineoxonol [DiBAC4 (3)] assay were primarily carried out...
June 21, 2017: IUBMB Life
https://www.readbyqxmd.com/read/28636189/discovery-of-alkyl-bis-oxy-dibenzimidamide-derivatives-as-novel-protein-arginine-methyltransferase-1-prmt1-inhibitors
#2
Wei-Yao Zhang, Wen-Chao Lu, Hao Jiang, Zheng-Bing Lv, Yi-Qian Xie, Fu-Lin Lian, Zhong-Jie Liang, Yu-Xi Jiang, Da-Jin Wang, Cheng Luo, Jia Jin, Fei Ye
Protein arginine methylation, a post-translational modification critical for a variety of biological processes, is catalyzed by protein arginine N-methyltransferases (PRMTs). In particular, PRMT1 is responsible for over 85% of the arginine methylation in mammalian cells. Dysregulation of PRMT1 is involved in diverse pathological diseases including cancers. However, most current PRMT1inhibitors are lack of specificity, efficacy, and bioavailability. Herein, a series of alkyl bis(oxy)dibenzimidamide derivatives were identified as selective PRMT1 inhibitors...
June 21, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28636172/a-phos-tag-based-micropipette-tip-method-for-rapid-and-selective-enrichment-of-phosphopeptides
#3
Elena Tianfei Yuan, Yoko Ino, Maho Kawaguchi, Yayoi Kimura, Hisashi Hirano, Emiko Kinoshita-Kikuta, Eiji Kinoshita, Tohru Koike
Phosphorylated peptides are attractive targets in the study of the phosphoproteome. Here, we introduce a simple and convenient micropipette-tip method for the separation of phosphorylated and nonphosphorylated peptides by using a phosphate-binding zinc(II) complex of 1,3-bis(pyridin-2-ylmethylamino)propan-2-olate (Phos-tag). A 200-μL micropipette tip containing 10 μL of swollen agarose beads functionalized with Phos-tag moieties was prepared. All steps in the phosphate-affinity separation (binding, washing, and elution) were conducted by using aqueous buffers at neutral pH values...
June 21, 2017: Electrophoresis
https://www.readbyqxmd.com/read/28636030/base-promoted-deborylative-secondary-alkylation-of-n-heteroaromatic-n-oxides-with-internal-gem-bis-pinacolato-boryl-alkanes-a-facile-derivatization-of-2-2-bipyridyl-analogues
#4
Chiwon Hwang, Woohyun Jo, Seung Hwan Cho
A base-promoted, secondary alkylation of N-heteroaromatic N-oxides using internal gem-bis[(pinacolato)boryl]alkanes as alkylation reagents is reported. The reaction exhibits a broad scope, providing deoxygenated secondary alkylated N-heteroaromatic compounds with high efficiency. The usefulness of the developed protocol is evidenced by the sequential direct alkylation of 2,2'-bipyridine-N-oxide.
June 21, 2017: Chemical Communications: Chem Comm
https://www.readbyqxmd.com/read/28634226/phostine-pst3-1a-targets-mgat5-and-inhibits-glioblastoma-initiating-cell-invasiveness-and-proliferation
#5
Zahra Hassani, Ali Saleh, Soumaya Turpault, Salim Khiati, Willy Morelle, Jacques Vignon, Jean-Philippe Hugnot, Emmanuelle Uro-Coste, Philippe Legrand, Marcel Delaforge, Séverine Loiseau, Ludovic Clarion, Marc Lecouvey, Jean-Noël Volle, David Virieux, Jean-Luc Pirat, Hugues Duffau, Norbert Bakalara
Glioblastoma multiforme (GBM) is the most common primary malignant brain tumor and accounts for a significant proportion of all primary brain tumors. Median survival after treatment is around 15 months. Remodeling of N-glycans by the N-acetylglucosamine glycosyltransferase (MGAT5) regulates tumoral development. Here, perturbation of MGAT5 enzymatic activity by the small-molecule inhibitor 3-Hydroxy-4,5-bis-benzyloxy-6-benzyloxymethyl-2-phenyl2-oxo-2λ5-[1,2]oxaphosphinane (PST3.1a) restrains GBM growth. In cell based assays it is demonstrated that PST3...
June 20, 2017: Molecular Cancer Research: MCR
https://www.readbyqxmd.com/read/28634178/ascorbate-protects-the-di-heme-enzyme-maug-against-self-inflicted-oxidative-damage-by-an-unusual-antioxidant-mechanism
#6
Zhongxin Ma, Victor L Davidson
Ascorbate protects MauG from self-inactivation that occurs during the autoreduction of the reactive bis -Fe(IV) state of its diheme cofactor. The mechanism of protection does not involve direct reaction with reactive oxygen species in solution. Instead it binds to MauG and mitigates oxidative damage that occurs via internal transfer of electrons from amino acid residues within the protein to the high-valent hemes. The presence of ascorbate does not inhibit the natural catalytic reaction of MauG which catalyzes oxidative posttranslational modifications of a substrate protein that binds to the surface of MauG, and is oxidized by the high-valent hemes via long range electron transfer...
June 20, 2017: Biochemical Journal
https://www.readbyqxmd.com/read/28632963/metal-ion-induced-in-situ-ligand-oxidation-for-self-assembled-clusters-from-bis-5-2-pyridine-2-yl-1-2-4-triazole-3-yl-methane-to-alcohol-or-ketone
#7
Wei-Quan Lin, Yuan-Yuan Peng, Lang Tong, Jian-Hua Jia, Jun-Liang Liu, Yan-Cong Chen, Wen-Bin Chen, Ming-Liang Tong
Hydrothermal reactions of metal nitrates and ligand bis(5-(pyridine-2-yl)-1,2,4-triazol-3-yl)methane (H2L1) on same condition gave three cluster compounds, {Cr2}, {Zn12} and {Fe8}. Notably, methylene group of H2L1 was in situ oxidized either to hydroxymethylated (L2-O)3- in the metallo-ring {Zn12} or to a rigid carbonylated (L3=O)2- in the screw-type {Fe8}. In light of comparative experiment results, NO3- was deduced to be of a catalytic role in ligand oxidation. Metal ions could be regarded as an "induced" tool for clusters generation in self-assembly process...
June 20, 2017: Chemistry, An Asian Journal
https://www.readbyqxmd.com/read/28632383/taking-advantage-of-disorder-small-molecule-organic-glasses-for-radiation-detection-and-particle-discrimination
#8
Joseph S Carlson, Peter Marleau, Ryan A Zarkesh, Patrick L Feng
A series of fluorescent silyl-fluorene molecules were synthesized and studied with respect to their photophysical properties and response toward ionizing neutron and gamma-ray radiation. Optically transparent and stable organic glasses were prepared from these materials using a bulk melt-casting procedure. The prepared organic glass monoliths provided fluorescence quantum yields and radiation detection properties exceeding the highest-performing benchmark materials such as solution-grown trans-stilbene crystals...
June 20, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/28631930/fluorescent-and-electrochemical-supramolecular-coordination-polymer-hydrogels-formed-from-ion-tuned-self-assembly-of-small-bis-terpyridine-monomer
#9
Xudong Yu, Zengyao Wang, Yajuan Li, Lijun Geng, Jujie Ren, Guoliang Feng
Herein, ditopic ligand DTA comprised of terpyridine and acetylene segments with only one aromatic π-conjugated building block was designed and synthesized. Driven by metal-ligand coordination interactions, we presented that the use of metal salts can direct the self-assembly of DTA in the generation of fluorescent and electrochemical polymers that entrapped water to form ambidextrous hydrogels. These were characterized by several approaches including fluorescent titrations, UV-vis, circular dichroism, and X-ray diffraction spectra as well as scanning electron microscopy and transmission electron microscopy experiments...
June 20, 2017: Inorganic Chemistry
https://www.readbyqxmd.com/read/28631482/carbohydrate-bis-acetal-based-substrates-as-tunable-fluorescence-quenched-probes-for-monitoring-exo-glycosidase-activity
#10
Samy Cecioni, David J Vocadlo
Tunable Förster resonance energy transfer (FRET)-quenched substrates are useful for monitoring the activity of various enzymes within their relevant physiological environments. Development of FRET-quenched substrates for exo-glycosidases, however, has been hindered by their constrained pocket-shaped active sites. Here we report the design of a new class of substrate that overcomes this problem. These Bis-Acetal-Based Substrates (BABS) bear a hemiacetal aglycon leaving group that tethers fluorochromes in close proximity, also positioning them distant from the active site pocket...
June 20, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/28631480/fully-transparent-quantum-dot-light-emitting-diode-with-a-laminated-top-graphene-anode
#11
Li Yao, Xin Fang, Wei Gu, Wenhao Zhai, Yi Wan, Xixi Xie, Wanjin Xu, Xiaodong Pi, Guangzhao Ran, Guogang Qin
A new method to employ graphene as top electrode was introduced, and based on that, fully transparent quantum dot light emitting diodes (T-QLEDs) were sucessfully fabribated through a lamination process. We adopted the widely used wet transfer method to transfer bilayer graphene (BG) on polydimethylsiloxane/polyethylene terephthalate (PDMS/PET) substrate. The sheet resistance of graphene reduced to ~540 Ω/□ through transferring BG for 3 times on the PDMS/PET. The T-QLED has an inverted device structure of glass/Indium tin oxide (ITO)/ZnO nanoparticles (NPs)/(CdSSe/ZnS quantum dots (QDs))/ 1,1-bis[(di-4-tolylamino)phenyl] cyclohexane (TAPC)/MoO3/ graphene/PDMS/PET...
June 20, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28631050/analgesia-nociception-index-ani-monitoring-in-patients-with-thoracic-paravertebral-block-a-randomized-controlled-study
#12
Nurseda Dundar, Alparslan Kus, Yavuz Gurkan, Kamil Toker, Mine Solak
The goal of the study was to evaluate the effectiveness of analgesia nociception index (ANI) monitoring during intraoperative period for patients with thoracic paravertebral block (TPVB) undergoing breast surgery under general anesthesia. This prospective randomized trial was performed after receiving ethics committee approval in 44 patients who were scheduled to undergo breast surgery under general anesthesia. TPVB was performed in the preoperative period using 20 mL of bupivacaine 0.25% at T4 level. Anesthesia maintenance was provided with sevoflurane in O2: air mixture and remifentanil infusion...
June 19, 2017: Journal of Clinical Monitoring and Computing
https://www.readbyqxmd.com/read/28630625/quantification-of-antioxidant-phenolic-compounds-in-a-new-chrysanthemum-cultivar-by-high-performance-liquid-chromatography-with-diode-array-detection-and-electrospray-ionization-mass-spectrometry
#13
Ah-Reum Han, Hyo Young Kim, Yangkang So, Bomi Nam, Ik-Soo Lee, Joo-Won Nam, Yeong Deuk Jo, Sang Hoon Kim, Jin-Baek Kim, Si-Yong Kang, Chang Hyun Jin
The flowers of Chrysanthemum morifolium Ramat. have been used as an herbal tea and in traditional medicine, and the plant has been developed to produce horticultural cultivars of various colors and shapes. In this study, a new chrysanthemum cultivar with dark purple petals (C. morifolium cv. ARTI-Dark Chocolate; ADC) was developed by radiation-induced mutation breeding of its original cultivar with purple striped white petals (C. morifolium cv. Noble Wine, NW). The phenolic profile and antioxidant property of ADC were investigated and compared with NW and the commercially available medicinal herb, C...
2017: International Journal of Analytical Chemistry
https://www.readbyqxmd.com/read/28629933/lignans-from-the-root-of-wikstroemia-indica-and-their-cytotoxic-activity-against-panc-1-human-pancreatic-cancer-cells
#14
Hang Chang, Yuwei Wang, Xue Gao, Zehai Song, Suresh Awale, Na Han, Zhihui Liu, Jun Yin
Six new compounds, wikstronin A (1), wikstronin B (2), wikstresinol (3), acetylwikstresinol (4), bis-5',5'-(+)-matairesinol (5), bis-5,5'-(+)-matairesinol (6), together with 20 known compounds (7-26) were isolated from the CH2Cl2 extract of roots of Wikstroemia indica. Structures of compounds 1-6 were determined by extensive NMR and CD spectroscopic analysis. In vitro preferential cytotoxicity of all the isolates was evaluated against a PANC-1 human pancreatic cell line. Compounds 8 and 12 displayed mild preferential cytotoxicity in the nutrient-deprived medium (NDM) and without causing toxicity in normal nutrient-rich conditions...
June 16, 2017: Fitoterapia
https://www.readbyqxmd.com/read/28629211/effect-of-methoxsalen-on-ca%C3%A2-%C3%A2-%C2%BA-homeostasis-and-viability-in-human-osteosarcoma-cells
#15
Yi-Chau Lu, Chiang-Ting Chou, Wei-Zhe Liang, Chun-Chi Kuo, Shu-Shong Hsu, Jue-Long Wang, Chung-Ren Jan
Methoxsalen is a natural compound found in many seed plants. The effect of methoxsalen on Ca²⁺- related physiology in human osteosarcoma is unclear. This study investigated the effect of methoxsalen on cytosolic free Ca²⁺ concentrations ([Ca²⁺]i) in MG63 human osteosarcoma cells. Methoxsalen induced [Ca²⁺]i rises concentration-dependently. Methoxsalen-induced Ca²⁺ entry was confirmed by Mn²⁺-induced quench of fura-2 fluorescence. This Ca²⁺ entry was suppressed by nifedipine, econazole, and SKF96365...
June 30, 2017: Chinese Journal of Physiology
https://www.readbyqxmd.com/read/28628311/pushing-the-limits-of-oxygen-balance-in-1-3-4-oxadiazoles
#16
Qiong Yu, Ping Yin, Jiaheng Zhang, Chunlin He, Gregory Howard Imler, Damon A Parrish, Jean'ne M Shreeve
Gem-trinitromethyl groups were introduced into a 1,3,4-oxadiazole ring to give the first example of a bifunctionalized single five-membered ring with six nitro groups. 2,5-Bis(trinitromethyl)-1,3,4-oxadiazole (12) has a high calculated crystal density of 2.007 g cm-3 at 150 K and a very high positive oxygen balance (39.12%) which make it a strong candidate as a high energy dense oxidizer. The dihy-droxylammonium and dihydrazinium salts of bis(trinitromethyl)-1,3,4-oxadiazole (5 and 6) exhibit excel-lent detonation properties (5, vD = 9266 m s-1, P = 38...
June 19, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/28628262/catalytic-enantioselective-reaction-of-allenylnitriles-with-imines-using-chiral-bis-imidazoline-s-palladium-ii-pincer-complexes
#17
Masaru Kondo, Masashi Omori, Tsubasa Hatanaka, Yasuhiro Funahashi, Shuichi Nakamura
The first highly enantioselective reaction of allenylnitriles with imines has been developed. Excellent yields and enantioselectivities were observed for the reaction with various imines using chiral Phebim-Pd(II) complexes. This process offers a simple and efficient synthetic route for various functionalized α-vinylidene-β-aminonitriles and their derivatives.
June 19, 2017: Angewandte Chemie
https://www.readbyqxmd.com/read/28628103/a-common-haplotype-lowers-pu-1-expression-in-myeloid-cells-and-delays-onset-of-alzheimer-s-disease
#18
Kuan-Lin Huang, Edoardo Marcora, Anna A Pimenova, Antonio F Di Narzo, Manav Kapoor, Sheng Chih Jin, Oscar Harari, Sarah Bertelsen, Benjamin P Fairfax, Jake Czajkowski, Vincent Chouraki, Benjamin Grenier-Boley, Céline Bellenguez, Yuetiva Deming, Andrew McKenzie, Towfique Raj, Alan E Renton, John Budde, Albert Smith, Annette Fitzpatrick, Joshua C Bis, Anita DeStefano, Hieab H H Adams, M Arfan Ikram, Sven van der Lee, Jorge L Del-Aguila, Maria Victoria Fernandez, Laura Ibañez, Rebecca Sims, Valentina Escott-Price, Richard Mayeux, Jonathan L Haines, Lindsay A Farrer, Margaret A Pericak-Vance, Jean Charles Lambert, Cornelia van Duijn, Lenore Launer, Sudha Seshadri, Julie Williams, Philippe Amouyel, Gerard D Schellenberg, Bin Zhang, Ingrid Borecki, John S K Kauwe, Carlos Cruchaga, Ke Hao, Alison M Goate
A genome-wide survival analysis of 14,406 Alzheimer's disease (AD) cases and 25,849 controls identified eight previously reported AD risk loci and 14 novel loci associated with age at onset. Linkage disequilibrium score regression of 220 cell types implicated the regulation of myeloid gene expression in AD risk. The minor allele of rs1057233 (G), within the previously reported CELF1 AD risk locus, showed association with delayed AD onset and lower expression of SPI1 in monocytes and macrophages. SPI1 encodes PU...
June 19, 2017: Nature Neuroscience
https://www.readbyqxmd.com/read/28627751/synthesis-of-gem-dinitromethylated-and-fluorodinitromethylated-derivatives-of-5-5-dinitro-bis-1-2-4-triazole-as-promising-high-energy-density-materials
#19
Qinghua Zhang, Shi Huang, Junjun Tian, Xiujuan Tian, Kangcai Wang
The gem-dinitromethylated and fluorodinitromethylated 5,5'-dinitro-3,3'-bis-1,2,4-triazole (DNBT) (2 and 3) along with seven ionic derivatives (4-9) were successfully synthesized and characterized by NMR and IR spectroscopies, elemental analysis, single crystal X-ray diffraction (XRD), and differential scanning calorimetry (DSC). XRD revealed that compounds 2 and 3 were crystallized in the monoclinic P21/n space group and compound 5 was crystallized in the monoclinic P21/c space group. The physicochemical properties for the as-synthesized compounds 2-9 were investigated and the results indicated that compounds 3, 6 and 7 exhibited a good balance between high energy and low sensitivity, indicating their promise as new high-energy-density materials (HEDMs)...
June 19, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28627565/a-stable-gold-i-enyne-species-obtained-by-alkyne-carboauration-in-a-complex-rearrangement
#20
Jéssica Cámara, M Carmen Blanco, Antonio Laguna, Panče Naumov, M Concepción Gimeno
An unprecedented tetranuclear gold derivative with unusual gold-enyne moieties is prepared by a mild and neat rearrangement of a dinuclear gold complex with a bridging bis(diphenylphosphino)alkyne and terminal alkynyl ligands. The complex originates as a consequence of an intramolecular addition of the AuC[triple bond, length as m-dash]CTol fragment to the internal diphosphine triple bond Ph2PC[triple bond, length as m-dash]CPPh2. The crystal structure of the tetranuclear complex shows a dinuclear metallacycle with a very short AuAu bond interaction and bridging phosphino-enyne ligands...
June 19, 2017: Chemical Communications: Chem Comm
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