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https://www.readbyqxmd.com/read/28502066/ebselen-ameliorates-%C3%AE-amyloid-pathology-tau-pathology-and-cognitive-impairment-in-triple-transgenic-alzheimer-s-disease-mice
#1
Yongli Xie, Yibin Tan, Youbiao Zheng, Xiubo Du, Qiong Liu
Alzheimer's disease (AD) is a progressive neurodegenerative disease which is clinically characterized by memory loss and cognitive decline caused by protein misfolding and aggregation. Imbalance between free radicals and the antioxidant system is a prominent and early feature in the neuropathology of AD. Selenium (Se), a vital trace element with excellent antioxidant potential, is preferentially retained in the brain in Se-limited conditions and has been reported to provide neuroprotection through resisting oxidative damage...
May 13, 2017: Journal of Biological Inorganic Chemistry: JBIC
https://www.readbyqxmd.com/read/28496307/developing-selective-histone-deacetylases-hdacs-inhibitors-through-ebselen-and-analogs
#2
Yuren Wang, Jason Wallach, Stephanie Duane, Yuan Wang, Jianghong Wu, Jeffrey Wang, Adeboye Adejare, Haiching Ma
Histone deacetylases (HDACs) are key regulators of gene expression in cells and have been investigated as important therapeutic targets for cancer and other diseases. Different subtypes of HDACs appear to play disparate roles in the cells and are associated with specific diseases. Therefore, substantial effort has been made to develop subtype-selective HDAC inhibitors. In an effort to discover existing scaffolds with HDAC inhibitory activity, we screened a drug library approved by the US Food and Drug Administration and a National Institutes of Health Clinical Collection compound library in HDAC enzymatic assays...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28485614/design-synthesis-molecular-modeling-and-anticholinesterase-activity-of-benzylidene-benzofuran-3-ones-containing-cyclic-amine-side-chain
#3
Farzad Mehrabi, Yaghoub Pourshojaei, Alireza Moradi, Mohammad Sharifzadeh, Leila Khosravani, Reyhaneh Sabourian, Samira Rahmani-Nezhad, Maryam Mohammadi-Khanaposhtani, Mohammad Mahdavi, Ali Asadipour, Hamid Reza Rahimi, Setareh Moghimi, Alireza Foroumadi
AIM: A series of 2-benzylidene-benzofuran-3-ones were designed from the structures of Ebselen analogs and aurone derivatives and synthesized in good yields. MATERIALS & METHODS: The target compounds were prepared by the condensation reaction between appropriate benzofuranones with amino alkoxy aldehydes and evaluated as cholinesterase inhibitors by Ellman's method. RESULTS: The in vitro anti-acetylcholinesterase (AChE)/butyrylcholinesterase activities of the synthesized compounds revealed that 7e (IC50 = 0...
May 9, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28463038/synergistic-effect-of-ebselen-and-gamma-radiation-on-breast-cancer-cells
#4
Noura M Thabet, Enas M Moustafa
PURPOSE: This study was performed to explore the synergistic effect of a seleno-organic compound Ebselen (Ebs) and/or γ-radiation to exert antitumor effects on human breast cancer (MCF-7) cell line in vitro. MATERIALS AND METHODS: Ebs cytotoxicity at various concentration (10, 25, 50 and 75 μg), cell proliferation and clonogenic assay of Ebs and/or γ-radiation (at 1, 3 and 6Gy), expression of p-IκBα and NF-κB, inflammatory cytokines levels (TNF-α, IL-2, INF-γ, IL-10 and TGF-β), apoptotic factors (Caspase-3, Granzyme-B and TRAIL) and angiogenic factor (VEGF) were investigated...
May 2, 2017: International Journal of Radiation Biology
https://www.readbyqxmd.com/read/28456691/a-new-thioredoxin-reductase-with-additional-glutathione-reductase-activity-in-haemonchus-contortus
#5
Agustín Plancarte, Gabriela Nava, Javier A Munguía
We report, herein, the purification to homogeneity and the biochemical and kinetic characterization of HcTrxR3, a new isoform of thioredoxin reductase (TrxR) from Haemonchus contortus. HcTrxR3 was found to have a relative molecular weight of 134,000, while the corresponding value per subunit obtained under denaturing conditions, was of 67,000. By peptide mass spectrophotometric analysis, HcTrxR3 was determined to have 99% identity with the H. contortus HcTrxR1 although, and most importantly, they are different in their amino acid sequence in two amino acid positions: 48 (isoleucine instead of leucine) and 460 (leucine instead of proline)...
April 26, 2017: Experimental Parasitology
https://www.readbyqxmd.com/read/28432706/varied-pathological-and-therapeutic-response-effects-associated-with-chchd2-mutant-and-risk-variants
#6
Murni Tio, Rujing Wen, Yih Lin Lim, Zul Haikhel Bin Zukifli, Shaoping Xie, Patrick Ho, Zhidong Zhou, Tong-Wey Koh, Yi Zhao, Eng-King Tan
Mutations and polymorphic risk variant of coiled-coil-helix-coiled-coil-helix domain containing 2 (CHCHD2) have been associated with late-onset Parkinson disease. In vivo pathological evidence of CHCHD2 mutations is currently lacking. Utilizing transgenic Drosophila model, we examined the relative pathophysiologic effect of the pathogenic (c.182C>T, p.Thr61Ile and c.434G>A, p.Arg145Gln) and the risk (c.5C>T, p.Pro2Leu) CHCHD2 variants. All the transgenic models exhibited locomotor dysfunction which could be exacerbated by rotenone exposure, dopaminergic neuron degeneration, reduction in lifespan, mitochondrial dysfunction, oxidative stress and impairment in synaptic transmission...
April 21, 2017: Human Mutation
https://www.readbyqxmd.com/read/28383113/diphenyl-diselenide-protects-against-methylmercury-induced-inhibition-of-thioredoxin-reductase-and-glutathione-peroxidase-in-human-neuroblastoma-cells-a-comparison-with-ebselen
#7
Daiane F Meinerz, Vasco Branco, Michael Aschner, Cristina Carvalho, João Batista T Rocha
Exposure to methylmercury (MeHg), an important environmental toxicant, may lead to serious health risks, damaging various organs and predominantly affecting the brain function. The toxicity of MeHg can be related to the inhibition of important selenoenzymes, such as glutathione peroxidase (GPx) and thioredoxin reductase (TrxR). Experimental studies have shown that selenocompounds play an important role as cellular detoxifiers and protective agents against the harmful effects of mercury. The present study investigated the mechanisms by which diphenyl diselenide [(PhSe)2 ] and ebselen interfered with the interaction of mercury (MeHg) and selenoenzymes (TrxR and GPx) in an in vitro experimental model of cultured human neuroblastoma cells (SH-SY5Y)...
April 6, 2017: Journal of Applied Toxicology: JAT
https://www.readbyqxmd.com/read/28335518/new-chiral-ebselen-analogues-with-antioxidant-and-cytotoxic-potential
#8
Agata J Pacuła, Katarzyna B Kaczor, Jędrzej Antosiewicz, Anna Janecka, Angelika Długosz, Tomasz Janecki, Andrzej Wojtczak, Jacek Ścianowski
New chiral camphane-derived benzisoselenazol-3(2H)-ones and corresponding diselenides have been synthetized using a convenient one-pot procedure. Se-N bond was efficiently converted to an Se-Se bond, which could also be easily re-oxidized to the initial benzisoselenazolone moiety. The antioxidant activity of camphor derivatives was evaluated and compared to the reactivity of a series of N-amino acid benzisoselenazol-3(2H)-ones obtained by a modified procedure involving the improved synthesis and isolation of the diseleno bis(dibenzoic) acid...
March 20, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28285521/exploring-covalent-allosteric-inhibition-of-antigen-85c-from-mycobacterium-tuberculosis-by-ebselen-derivatives
#9
Christopher M Goins, Steven Dajnowicz, Sandeep Thanna, Steven J Sucheck, Jerry M Parks, Donald R Ronning
Previous studies identified ebselen as a potent in vitro and in vivo inhibitor of the Mycobacterium tuberculosis (Mtb) antigen 85 (Ag85) complex, comprising three homologous enzymes required for the biosynthesis of the mycobacterial cell wall. In this study, the Mtb Ag85C enzyme was cocrystallized with azido and adamantyl ebselen derivatives, resulting in two crystallographic structures of 2.01 and 1.30 Å resolution, respectively. Both structures displayed the anticipated covalent modification of the solvent accessible, noncatalytic Cys209 residue forming a selenenylsulfide bond...
May 12, 2017: ACS Infectious Diseases
https://www.readbyqxmd.com/read/28273423/thermal-and-photoinduced-copper-promoted-c-se-bond-formation-synthesis-of-2-alkyl-1-2-benzisoselenazol-3-2h-ones-and-evaluation-against-mycobacterium-tuberculosis
#10
Sandeep Thanna, Christopher M Goins, Susan E Knudson, Richard A Slayden, Donald R Ronning, Steven J Sucheck
2-Alkyl-1,2-benzisoselenazol-3(2H)-ones, represented by ebselen (1a), are being studied intensively for a range of medicinal applications. We describe both a new thermal and photoinduced copper-mediated cross-coupling between potassium selenocyanate (KSeCN) and N-substituted ortho-halobenzamides to form 2-alkyl-1,2-benzisoselenazol-3(2H)-ones containing a C-Se-N bond. The copper ligand (1,10-phenanthroline) facilitates C-Se bond formation during heating via a mechanism that likely involves atom transfer (AT), whereas, in the absence of ligand, photoinduced activation likely proceeds through a single electron transfer (SET) mechanism...
March 20, 2017: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/28242720/fluorescence-high-throughput-screening-for-inhibitors-of-tonb-action
#11
Brittany L Nairn, Olivia S Eliasson, Dallas R Hyder, Noah J Long, Aritri Majumdar, Somnath Chakravorty, Peter McDonald, Anuradha Roy, Salete M Newton, Phillip E Klebba
Gram-negative bacteria acquire ferric siderophores through TonB-dependent outer membrane transporters (TBDT). By fluorescence spectroscopic hgh-throughput screening (FLHTS), we identified inhibitors of TonB-dependent ferric enterobactin (FeEnt) uptake through Escherichia coli FepA (EcoFepA). Among 165 inhibitors found in a primary screen of 17,441 compounds, we evaluated 20 in secondary tests: TonB-dependent ferric siderophore uptake and colicin killing and proton motive force-dependent lactose transport. Six of 20 primary hits inhibited TonB-dependent activity in all tests...
May 15, 2017: Journal of Bacteriology
https://www.readbyqxmd.com/read/28212823/cyp-epoxygenase-derived-h2o2-is-involved-in-the-endothelium-derived-hyperpolarization-edh-and-relaxation-of-intrarenal-arteries
#12
Mercedes Muñoz, Maria Elvira López-Oliva, Estéfano Pinilla, María Pilar Martínez, Ana Sánchez, Claudia Rodríguez, Albino García-Sacristán, Medardo Hernández, Luis Rivera, Dolores Prieto
Reactive oxygen species (ROS) like hydrogen peroxide (H2O2) are involved in the in endothelium-derived hyperpolarization (EDH)-type relaxant responses of coronary and mesenteric arterioles. The role of ROS in kidney vascular function has mainly been investigated in the context of harmful ROS generation associated to kidney disease. The present study was sought to investigate whether H2O2 is involved in the endothelium-dependent relaxations of intrarenal arteries as well the possible endothelial sources of ROS generation involved in these responses...
February 14, 2017: Free Radical Biology & Medicine
https://www.readbyqxmd.com/read/28208301/biomolecular-interaction-assays-identified-dual-inhibitors-of-glutaminase-and-glutamate-dehydrogenase-that-disrupt-mitochondrial-function-and-prevent-growth-of-cancer-cells
#13
Min Zhu, Jinzhang Fang, Jingjing Zhang, Zheng Zhang, Jianhui Xie, Yan Yu, Jennifer Jin Ruan, Zhao Chen, Wei Hou, Gensheng Yang, Weike Su, Benfang Helen Ruan
Glutaminase (KGA/isoenzyme GAC) is an emerging and important drug target for cancer. Traditional methods for assaying glutaminase activity are coupled with several other enzymes. Such coupled assays do not permit the direct and stringent characterization of specific glutaminase inhibitors. Ebselen was identified as a potent 9 nM KGA inhibitor in the KGA/glutamate oxidase (GO)/horse radish peroxidase (HRP) coupled assay but showed very weak activity in inhibiting the growth of glutamine-dependent cancer cells...
February 7, 2017: Analytical Chemistry
https://www.readbyqxmd.com/read/28151580/in-vitro-assessment-of-the-growth-and-plasma-membrane-h-atpase-inhibitory-activity-of-ebselen-and-structurally-related-selenium-and-sulfur-containing-compounds-in-candida-albicans
#14
Natalie N Orie, Andrew R Warren, Jovana Basaric, Cesar Lau-Cam, Magdalena Piętka-Ottlik, Jacek Młochowski, Blase Billack
Ebselen (EB, compound 1) is an investigational organoselenium compound that reduces fungal growth, in part, through inhibition of the fungal plasma membrane H(+) -ATPase (Pma1p). In the present study, the growth inhibitory activity of EB and of five structural analogs was assessed in a fluconazole (FLU)-resistant strain of Candida albicans (S2). While none of the compounds were more effective than EB at inhibiting fungal growth (IC50  ∼ 18 μM), two compounds, compounds 5 and 6, were similar in potency...
February 2, 2017: Journal of Biochemical and Molecular Toxicology
https://www.readbyqxmd.com/read/28043795/evaluation-of-substituted-ebselen-derivatives-as-potential-trypanocidal-agents
#15
Heeren M Gordhan, Stephen L Patrick, Maria I Swasy, Amber L Hackler, Mark Anayee, Jennifer E Golden, James C Morris, Daniel C Whitehead
Human African trypanosomiasis is a disease of sub-Saharan Africa, where millions are at risk for the illness. The disease, commonly referred to as African sleeping sickness, is caused by an infection by the eukaryotic pathogen, Trypanosoma brucei. Previously, a target-based high throughput screen revealed ebselen (EbSe), and its sulfur analog, EbS, to be potent in vitro inhibitors of the T. brucei hexokinase 1 (TbHK1). These molecules also exhibited potent trypanocidal activity in vivo. In this manuscript, we synthesized a series of sixteen EbSe and EbS derivatives bearing electron-withdrawing carboxylic acid and methyl ester functional groups, and evaluated the influence of these substituents on the biological efficacy of the parent scaffold...
February 1, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28029457/new-glutathione-peroxidase-mimetics-insights-into-antioxidant-and-cytotoxic-activity
#16
Agata J Pacuła, Katarzyna B Kaczor, Angelika Wojtowicz, Jędrzej Antosiewicz, Anna Janecka, Angelika Długosz, Tomasz Janecki, Jacek Ścianowski
A series of N-alkyl benzisoselenazol-3(2H)-ones has been obtained and transformed to corresponding diselenides by the reduction with sodium borohydride. Additionally, efficient methodology for the oxidative Se-N bond formation by potassium iodate has been presented, new conversion of diselenide to benzisoselenazolone was observed. The GPx-like activity of all synthetized derivatives has been evaluated by NMR. N-Allyl diselenide was up to five times better antioxidant than ebselen. Anticancer capacity towards MCF7 and DU145 cancer cells has been also tested...
January 1, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28003551/response-to-comment-on-a-small-molecule-antivirulence-agent-for-treating-clostridium-difficile-infection
#17
Kristina Oresic Bender, Megan Garland, Matthew Bogyo
Ebselen's antivirulence activity in Clostridium difficile infection is likely due to multiple modes of action, but the contribution of each to its efficacy remains unclear.
December 21, 2016: Science Translational Medicine
https://www.readbyqxmd.com/read/28003550/comment-on-a-small-molecule-antivirulence-agent-for-treating-clostridium-difficile-infection
#18
Greg L Beilhartz, John Tam, Zhifen Zhang, Roman A Melnyk
New insights into the mechanism of action of ebselen, a small-molecule antivirulence agent that reduces disease pathology in a mouse model of Clostridium difficile infection, suggest a different molecular target may be responsible for its efficacy.
December 21, 2016: Science Translational Medicine
https://www.readbyqxmd.com/read/27997177/nitro-azo-and-amino-derivatives-of-ebselen-synthesis-structure-and-cytoprotective-effects
#19
Vijay P Singh, Jia-Fei Poon, Jiajie Yan, Xi Lu, Marjam Karlsson Ott, Ray J Butcher, Paul J Gates, Lars Engman
Novel azo-bis-ebselen compounds 7 were prepared by reduction of 7-nitro-2-aryl-1,2-benzisoselenazol-3(2H)-ones 3 and 6 with sodium benzenetellurolate, NaTeC6H5, and by reaction of 2-bromo-3-nitrobenzamides with Na2Se2. The X-ray structure of 7b showed that the molecule, due to strong intramolecular secondary Se···N interactions, is completely planar. Azo-compounds 7 upon further reaction with NaTeC6H5 were reductively cleaved to provide 2 equiv of the corresponding aromatic amine. The weak Se-N bond was not stable enough to survive the reaction conditions, and diselenides 8 were isolated after workup...
December 20, 2016: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/27983850/computational-modeling-of-the-catalytic-cycle-of-glutathione-peroxidase-nanomimic
#20
Ramesh Kheirabadi, Mohammad Izadyar
To elucidate the role of a derivative of ebselen as a mimic of the antioxidant selenoenzyme glutathione peroxidase, density functional theory and solvent-assisted proton exchange (SAPE) were applied to model the reaction mechanism in a catalytic cycle. This mimic plays the role of glutathione peroxidase through a four-step catalytic cycle. The first step is described as the oxidation of 1 in the presence of hydrogen peroxide, while selenoxide is reduced by methanthiol at the second step. In the third step of the reaction, the reduction of selenenylsulfide occurs by methanthiol, and the selenenic acid is dehydrated at the final step...
December 29, 2016: Journal of Physical Chemistry. A
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