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Ebselen

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https://www.readbyqxmd.com/read/29244159/pre-clinical-model-of-severe-glutathione-peroxidase-3-deficiency-and-chronic-kidney-disease-results-in-coronary-artery-thrombosis-and-depressed-left-ventricular-function
#1
Paul Pang, Molly Abbott, Malyun Abdi, Quynh-Anh Fucci, Nikita Chauhan, Murti Mistri, Brandon Proctor, Matthew Chin, Bin Wang, Wenqing Yin, Tzong-Shi Lu, Arvin Halim, Kenneth Lim, Diane E Handy, Joseph Loscalzo, Andrew M Siedlecki
Background: Chronic kidney disease (CKD) patients have deficient levels of glutathione peroxidase-3 (GPx3). We hypothesized that GPx3 deficiency may lead to cardiovascular disease in the presence of chronic kidney disease due to an accumulation of reactive oxygen species and decreased microvascular perfusion of the myocardium. Methods: To isolate the exclusive effect of GPx3 deficiency in kidney disease-induced cardiac disease, we studied the GPx3 knockout mouse strain (GPx3-/-) in the setting of surgery-induced CKD...
December 13, 2017: Nephrology, Dialysis, Transplantation
https://www.readbyqxmd.com/read/29215879/computational-kinetic-modeling-of-the-catalytic-cycle-of-glutathione-peroxidase-nanomimic-effect-of-nucleophilicity-of-thiols-on-the-catalytic-activity
#2
Ramesh Kheirabadi, Mohammad Izadyar, Mohammad Reza Housaindokht
The catalytic cycle of a new derivative of ebselen, 1, was elucidated via three steps by the density functional theory and solvent-assisted proton exchange procedure involving indirect proton exchange through a hydrogen-bonded transfer network. Different behaviors of the aromatic and aliphatic thiols were investigated in the reduction of selenoxide (step 2→3) and selenurane (step 3→1) based on their nucleophilicity. The reduction of selenoxide in the presence of thiophenol (ΔG≠=15.9 kcal.mol-1) is faster than methanethiol (ΔG≠=29...
December 7, 2017: Journal of Physical Chemistry. A
https://www.readbyqxmd.com/read/29212858/decreased-edhf-mediated-relaxation-is-a-major-mechanism-in-endothelial-dysfunction-in-resistance-arteries-in-aged-mice-on-prolonged-high-fat-sucrose-diet
#3
Shannon M Dunn, Kumuda C Das
High-fat sucrose (HFS) diet in aged individuals causes severe weight gain (obesity) with much higher risk of cardiovascular diseases such as hypertension or atherosclerosis. Endothelial dysfunction is a major contributor for these vascular disorders. We hypothesize that prolonged ingestion of HFS diet by aged mice would accentuate endothelial dysfunction in the small resistance arteries. Male C57BL/6J mice at 12 weeks of age were divided into four groups and fed either normal chow (NC) or high-fat sucrose diet (HFS)...
December 2017: Physiological Reports
https://www.readbyqxmd.com/read/29182862/on-the-inhibition-of-mammalian-15-lipoxygenase-by-three-ebselen-like-drugs-a-qm-mm-and-mm-pbsa-comparative-study
#4
Anna Cebrián-Prats, Tiffani Rovira, Patricia Saura, Àngels González-Lafont, José M Lluch
Ebselen is a potent competitive inhibitor of the active form of rabbit 15-lipoxygenase, an enzyme involved in many inflammatory diseases. Light induced Z-to-E isomerization of the ebselen-like 2-(3-benzylidene)-3-oxo-2,3-dihydrobenzo[b]thiophene-7-carboxylic acid methyl ester (BODTCM) molecule was used to convert the weak (Z)-BOTDCM inhibitor into the (E)-isomer with much higher inhibitory capacity. In this study, the binding modes of ebselen, (E)-BOTDCM and (Z)-BOTDCM have been analyzed to provide molecular insights on the inhibitory potency of ebselen and on the geometric-isomer specificity of (E)- and (Z)-BOTDCM inhibitors...
November 28, 2017: Journal of Physical Chemistry. A
https://www.readbyqxmd.com/read/29168872/organoselenium-compounds-as-mimics-of-selenoproteins-and-thiol-modifier-agents
#5
REVIEW
Nilda V Barbosa, Cristina W Nogueira, Pablo A Nogara, Andreza F de Bem, Michael Aschner, João B T Rocha
Selenium is an essential trace element for animals and its role in the chemistry of life relies on a unique functional group: the selenol (-SeH) group. The selenol group participates in critical redox reactions. The antioxidant enzymes glutathione peroxidase (GPx) and thioredoxin reductase (TrxR) exemplify important selenoproteins. The selenol group shares several chemical properties with the thiol group (-SH), but it is much more reactive than the sulfur analogue. The substitution of S by Se has been exploited in organic synthesis for a long time, but in the last 4 decades the re-discovery of ebselen (2-phenyl-1,2-benzisoselenazol-3(2H)-one) and the demonstration that it has antioxidant and therapeutic properties has renovated interest in the field...
November 23, 2017: Metallomics: Integrated Biometal Science
https://www.readbyqxmd.com/read/29072450/ebselen-mechanisms-of-glutamate-dehydrogenase-and-glutaminase-enzyme-inhibition
#6
Yan Yu, Yanhong Jin, Jie Zhou, Haoqiang Ruan, Han Zhao, Shiying Lu, Yue Zhang, Di Li, Xiaoyun Ji, Benfang Helen Ruan
Ebselen modulates target proteins through redox reactions with selenocysteine/cysteine residues, or through binding to the zinc finger domains. However, a recent contradiction in ebselen inhibition of kidney type glutaminase (KGA) stimulated our interest in investigating its inhibition mechanism with glutamate dehydrogenase (GDH), KGA, thioredoxin reductase (TrxR), and glutathione S-transferase. Fluorescein- or biotin-labeled ebselen derivatives were synthesized for mechanistic analyses. Biomolecular interaction analyses showed that only GDH, KGA, and TrxR proteins can bind to the ebselen derivative, and the binding to GDH and KGA could be competed off by glutamine or glutamate...
November 7, 2017: ACS Chemical Biology
https://www.readbyqxmd.com/read/28889263/chemical-speciation-of-selenium-and-mercury-as-determinant-of-their-neurotoxicity
#7
C S Oliveira, B C Piccoli, M Aschner, J B T Rocha
The antagonism of mercury toxicity by selenium has been well documented. Mercury is a toxic metal, widespread in the environment. The main target organs (kidneys, lungs, or brain) of mercury vary depending on its chemical forms (inorganic or organic). Selenium is a semimetal essential to mammalian life as part of the amino acid selenocysteine, which is required to the synthesis of the selenoproteins. This chapter has the aim of disclosing the role of selenide or hydrogen selenide (Se(-2) or HSe(-)) as central metabolite of selenium and as an important antidote of the electrophilic mercury forms (particularly, Hg(2+) and MeHg)...
2017: Advances in Neurobiology
https://www.readbyqxmd.com/read/28809398/precision-medicine-for-suicidality-from-universality-to-subtypes-and-personalization
#8
A B Niculescu, H Le-Niculescu, D F Levey, P L Phalen, H L Dainton, K Roseberry, E M Niculescu, J O Niezer, A Williams, D L Graham, T J Jones, V Venugopal, A Ballew, M Yard, T Gelbart, S M Kurian, A Shekhar, N J Schork, G E Sandusky, D R Salomon
Suicide remains a clear, present and increasing public health problem, despite being a potentially preventable tragedy. Its incidence is particularly high in people with overt or un(der)diagnosed psychiatric disorders. Objective and precise identification of individuals at risk, ways of monitoring response to treatments and novel preventive therapeutics need to be discovered, employed and widely deployed. We sought to investigate whether blood gene expression biomarkers for suicide (that is, a 'liquid biopsy' approach) can be identified that are more universal in nature, working across psychiatric diagnoses and genders, using larger cohorts than in previous studies...
September 2017: Molecular Psychiatry
https://www.readbyqxmd.com/read/28724632/hydrogen-peroxide-produced-by-superoxide-dismutase-sod-2-activates-sperm-in-caenorhabditis-elegans
#9
Taro Sakamoto, Hirotaka Imai
Superoxide dismutase (SOD) is a ubiquitous antioxidant enzyme that catalytically converts the superoxide radical to hydrogen peroxide (H2O2). In mammals, high SOD activity is detectable in sperm and seminal plasma, and loss of SOD activity has been correlated with male infertility; however, the underlying mechanisms of sperm infertility remain to be clarified. Here we report that the deletion of two major SOD genes in Caenorhabditis elegans, sod-1 and sod-2, causes sperm activation defects, leading to a significant reduction in brood size...
September 8, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28716314/safety-and-efficacy-of-ebselen-for-the-prevention-of-noise-induced-hearing-loss-a-randomised-double-blind-placebo-controlled-phase-2-trial
#10
Jonathan Kil, Edward Lobarinas, Christopher Spankovich, Scott K Griffiths, Patrick J Antonelli, Eric D Lynch, Colleen G Le Prell
BACKGROUND: Noise-induced hearing loss is a leading cause of occupational and recreational injury and disease, and a major determinant of age-related hearing loss. No therapeutic agent has been approved for the prevention or treatment of this disorder. In animal models, glutathione peroxidase 1 (GPx1) activity is reduced after acute noise exposure. Ebselen, a novel GPx1 mimic, has been shown to reduce both temporary and permanent noise-induced hearing loss in preclinical studies. We assessed the safety and efficacy of ebselen for the prevention of noise-induced hearing loss in young adults in a phase 2 clinical trial...
July 14, 2017: Lancet
https://www.readbyqxmd.com/read/28703940/ebselen-impairs-cellular-oxidative-state-and-induces-endoplasmic-reticulum-stress-and-activation-of-crucial-mitogen-activated-protein-kinases-in-pancreatic-tumour-ar42j-cells
#11
Patricia Santofimia-Castaño, Alicia Izquierdo-Alvarez, María Plaza-Davila, Antonio Martinez-Ruiz, Miguel Fernandez-Bermejo, Jose M Mateos-Rodriguez, Gines M Salido, Antonio Gonzalez
Ebselen (2-phenyl-1,2-benzisoselenazol-3(2H)-one) is an organoselenium radical scavenger compound, which has strong antioxidant and anti-inflammatory effects. However, evidence suggests that this compound could exert deleterious actions on cell physiology. In this study we have analyzed the effect of ebselen on rat pancreatic AR42J cells. Cytosolic free-Ca2(+) concentration ([Ca(2+) ]c ), cellular oxidative status, setting of endoplasmic reticulum stress and phosphorylation of major mitogen-activated protein kinases were analyzed...
July 13, 2017: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/28673614/ros-dependent-activation-of-rhoa-rho-kinase-in-pulmonary-artery-role-of-src-family-kinases-and-arhgef1
#12
Charles E MacKay, Yasin Shaifta, Vladimir V Snetkov, Asvi A Francois, Jeremy P T Ward, Greg A Knock
The role of reactive oxygen species (ROS) in smooth muscle contraction is poorly understood. We hypothesised that G-protein coupled receptor (GPCR) activation and hypoxia induce Rho-kinase activity and contraction in rat intra-pulmonary artery (IPA) via stimulation of ROS production and subsequent Src-family kinase (SrcFK) activation. The T-type prostanoid receptor agonist U46619 induced ROS production in pulmonary artery smooth muscle cells (PASMC). U46619 also induced c-Src cysteine oxidation, SrcFK auto-phosphorylation, MYPT-1 and MLC20 phosphorylation and contraction in IPA, and all these responses were inhibited by antioxidants (ebselen, Tempol)...
September 2017: Free Radical Biology & Medicine
https://www.readbyqxmd.com/read/28633807/differential-induction-of-atf3-and-ho-1-in-myeloid-cells-and-keratinocytes-via-dimethylfumarate-or-cyclosporine-a
#13
Stefanie Müller, Nikola Smatlik, Marc Burian, Kamran Ghoreschi, Martin Röcken, Amir S Yazdi
BACKGROUND: Chronic inflammatory skin diseases are characterized by controlled proliferation of keratinocytes. Here, activating transcription factor 3 (ATF3) might play a fundamental role. In these inflammatory diseases, proliferation is controlled and only rarely leads to cancer development which can be supported by an inflammatory microenvironment. ATF3 is a dual function protein as it suppresses pro-inflammatory IL-6 and IL-8, but also acts as a pro-oncogenic factor by the suppression of p53...
June 12, 2017: Journal of Dermatological Science
https://www.readbyqxmd.com/read/28606995/synergistic-antibacterial-effect-of-silver-and-ebselen-against-multidrug-resistant-gram-negative-bacterial-infections
#14
Lili Zou, Jun Lu, Jun Wang, Xiaoyuan Ren, Lanlan Zhang, Yu Gao, Martin E Rottenberg, Arne Holmgren
Multidrug-resistant (MDR) Gram-negative bacteria account for a majority of fatal infections, and development of new antibiotic principles and drugs is therefore of outstanding importance. Here, we report that five most clinically difficult-to-treat MDR Gram-negative bacteria are highly sensitive to a synergistic combination of silver and ebselen. In contrast, silver has no synergistic toxicity with ebselen on mammalian cells. The silver and ebselen combination causes a rapid depletion of glutathione and inhibition of the thioredoxin system in bacteria...
August 2017: EMBO Molecular Medicine
https://www.readbyqxmd.com/read/28605287/prdx1-peroxiredoxin-1-deficiency-reduces-cholesterol-efflux-via-impaired-macrophage-lipophagic-flux
#15
Se-Jin Jeong, Sinai Kim, Jong-Gil Park, In-Hyuk Jung, Mi-Ni Lee, Sejin Jeon, Hyae Yon Kweon, Dae-Yeul Yu, Sang-Hak Lee, Yangsoo Jang, Sang Won Kang, Ki-Hwan Han, Yury I Miller, Young Mi Park, Cheolho Cheong, Jae-Hoon Choi, Goo Taeg Oh
Oxidative stress activates macroautophagy/autophagy and contributes to atherogenesis via lipophagic flux, a form of lipid removal by autophagy. However, it is not known exactly how endogenous anti-oxidant enzymes are involved in lipophagic flux. Here, we demonstrate that the anti-oxidant PRDX1 (peroxiredoxin 1) has a crucial role in the maintenance of lipophagic flux in macrophages. PRDX1 is more highly expressed than other anti-oxidant enzymes in monocytes and macrophages. We determined that Prdx1 deficiency induced excessive oxidative stress and impaired maintenance of autophagic flux in macrophages...
June 12, 2017: Autophagy
https://www.readbyqxmd.com/read/28592405/current-and-emerging-topical-antibacterials-and-antiseptics-agents-action-and-resistance-patterns
#16
REVIEW
Deborah A Williamson, Glen P Carter, Benjamin P Howden
Bacterial skin infections represent some of the most common infectious diseases globally. Prevention and treatment of skin infections can involve application of a topical antimicrobial, which may be an antibiotic (such as mupirocin or fusidic acid) or an antiseptic (such as chlorhexidine or alcohol). However, there is limited evidence to support the widespread prophylactic or therapeutic use of topical agents. Challenges involved in the use of topical antimicrobials include increasing rates of bacterial resistance, local hypersensitivity reactions (particularly to older agents, such as bacitracin), and concerns about the indiscriminate use of antiseptics potentially coselecting for antibiotic resistance...
July 2017: Clinical Microbiology Reviews
https://www.readbyqxmd.com/read/28502066/ebselen-ameliorates-%C3%AE-amyloid-pathology-tau-pathology-and-cognitive-impairment-in-triple-transgenic-alzheimer-s-disease-mice
#17
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...
August 2017: Journal of Biological Inorganic Chemistry: JBIC
https://www.readbyqxmd.com/read/28496307/developing-selective-histone-deacetylases-hdacs-inhibitors-through-ebselen-and-analogs
#18
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
#19
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 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28463038/synergistic-effect-of-ebselen-and-gamma-radiation-on-breast-cancer-cells
#20
Noura M Thabet, Enas M Moustafa
PURPOSE: 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 concentrations (10, 25, 50 and 75 μg), cell proliferation and clonogenic assay of Ebs and/or γ-radiation (at 1, 3 and 6 Gy), 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...
August 2017: International Journal of Radiation Biology
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