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https://www.readbyqxmd.com/read/29778464/peroxiredoxin-2-deficiency-accelerates-age-related-ovarian-failure-through-the-reactive-oxygen-species-mediated-jnk-pathway-in-mice
#1
Sun-Ji Park, Jung-Hak Kim, Dong Gil Lee, Jin-Man Kim, Dong-Seok Lee
Reactive oxygen species (ROS) produced in biological reactions have been shown to contribute to ovarian aging. Peroxiredoxin 2 (Prx2) is an antioxidant enzyme that protects cells by scavenging ROS; however, its effect on age-related, oxidative stress-associated ovarian failure has not been reported. Here, we investigated its role in age-related ovarian dysfunction and 4-vinylcyclohexene diepoxide (VCD)-induced premature ovarian failure using Prx2-deficient mice. Compared to those in wildtype (WT) mice, serum levels of anti-Müllerian hormone, 17β-estradiol, and progesterone and numbers of follicles and corpora lutea were significantly lower in 18-month-old Prx2-/- mice...
May 17, 2018: Free Radical Biology & Medicine
https://www.readbyqxmd.com/read/29742915/redox-regulation-of-hexokinases
#2
Petr Heneberg
Significance Hexokinases are key enzymes that are responsible for the first reaction of glycolysis, but they also moonlight other cellular processes, including mitochondrial redox signaling regulation. Modulation of hexokinase activity and spatiotemporal location by reactive oxygen and nitrogen species as well as other gasotransmitters serves as the basis for a unique, underexplored method of tight and flexible regulation of these fundamental enzymes. Recent advances Redox modifications of thiols serve as a molecular code that enables the precise and complex regulation of hexokinases...
May 10, 2018: Antioxidants & Redox Signaling
https://www.readbyqxmd.com/read/29733976/ebselen-protects-mitochondrial-function-and-oxidative-stress-while-inhibiting-the-mitochondrial-apoptosis-pathway-after-acute-spinal-cord-injury
#3
Zhi-Qiang Jia, San-Qiang Li, Wei-Qiang Qiao, Wen-Zhong Xu, Jian-Wu Xing, Jian-Tao Liu, Hui Song, Zhong-Yang Gao, Bing-Wen Xing, Xi-Jing He
Ebselen is a fat-soluble small molecule and organic selenium compound that regulates the activity of glutathione peroxidase to alleviate mitochondrial oxidative stress and improve mitochondrial function. In the present study, we aimed to investigate the effects of ebselen on mitochondrial oxidative stress response, mitochondrial apotosis, and motor behaviors after spinal cord injury (SCI). We found that ebselen significantly increased the BBB score in motor behavior, thus suggesting a rescue effect of ebselen on motor function after SCI in rats...
May 4, 2018: Neuroscience Letters
https://www.readbyqxmd.com/read/29703933/the-cysteine-reactive-small-molecule-ebselen-facilitates-effective-sod1-maturation
#4
Michael J Capper, Gareth S A Wright, Letizia Barbieri, Enrico Luchinat, Eleonora Mercatelli, Luke McAlary, Justin J Yerbury, Paul M O'Neill, Svetlana V Antonyuk, Lucia Banci, S Samar Hasnain
Superoxide dismutase-1 (SOD1) mutants, including those with unaltered enzymatic activity, are known to cause amyotrophic lateral sclerosis (ALS). Several destabilizing factors contribute to pathogenicity including a reduced ability to complete the normal maturation process which comprises folding, metal cofactor acquisition, intra-subunit disulphide bond formation and dimerization. Immature SOD1 forms toxic oligomers and characteristic large insoluble aggregates within motor system cells. Here we report that the cysteine-reactive molecule ebselen efficiently confers the SOD1 intra-subunit disulphide and directs correct SOD1 folding, depopulating the globally unfolded precursor associated with aggregation and toxicity...
April 27, 2018: Nature Communications
https://www.readbyqxmd.com/read/29687124/a-protein-structure-guided-covalent-scaffold-selectively-targets-the-b1-and-b2-subclass-metallo-%C3%AE-lactamases
#5
Cheng Chen, Yang Xiang, Ke-Wu Yang, Yuejuan Zhang, Wen-Ming Wang, Jian-Peng Su, Ying Ge, Ya Liu
We report the discovery of ebselen-based dual covalent inhibitors of metallo-β-lactamases. Fluorescence and MALDI-TOF analysis suggested that the scaffold could bind to NDM-1 by forming a S-Se bond with Cys221 and an amide bond with Lys224 of NDM-1, thereby exhibiting selective inhibition and labeling against B1 and B2 subclass enzymes in vitro and in vivo.
April 24, 2018: Chemical Communications: Chem Comm
https://www.readbyqxmd.com/read/29604593/ebselen-can-protect-male-reproductive-organs-and-male-fertility-from-manganese-toxicity-structural-and-bioanalytical-approach-in-a-rat-model
#6
Amany Tharwat Mohammed, Lamiaa L M Ebraheim, Mohamed M M Metwally
Ebselen (EBS) is a versatile compound that can protect the cellular components from oxidative and free radical-mediated damage. In the present study, we investigated the protective effect of EBS against manganese (Mn) toxicity on male reproductive organs. Thirty-two male rats were assigned into four groups, namely, negative control, EBS (15 mg/kg body weight (bw), as a single protective IP injection), MnCl2 (50 mg/kg bw, orally for 30 consecutive days), and EBS + MnCl2 (as mentioned before). The results showed that EBS ameliorated the alterations caused by MnCl2 in the testicular, epididymal, and seminal vesicle tissues...
March 28, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29600321/can-ebselen-prevent-cisplatin-induced-ovarian-damage
#7
Zeynep Soyman, Hafize Uzun, Nihan Bayindir, Mukaddes Esrefoglu, Birtan Boran
PURPOSE: The occurrence of ovarian damage is a major shortcoming in treating tumors with cisplatin (CP). The present study investigates the beneficial effects of ebselen-a seleno-organic compound with antioxidant and antiinflammatory properties-vis-à-vis CP-induced ovarian damage. METHODS: Twenty-eight adult female rats were divided into four study groups. Group 1 received no treatment. The rats in Groups 2, 3, and 4 were intraperitoneally administered CP (2 mg/kg/day) twice per week, for 5 weeks...
March 29, 2018: Archives of Gynecology and Obstetrics
https://www.readbyqxmd.com/read/29584939/the-aglycone-ebselen-and-%C3%AE-d-xyloside-primed-glycosaminoglycans-co-contribute-to-ebselen-%C3%AE-d-xyloside-induced-cytotoxicity
#8
Yang Tang, Siqi Zhang, Yajing Chang, Dacheng Fan, Ariane de Agostini, Lijuan Zhang, Tao Jiang
Most of β-D-xylosides with hydrophobic aglycones are non-toxic primers for glycosaminoglycan assembly in animal cells. However, when Ebselen was conjugated to D-xylose, D-glucose, D-galactose, and D-lactose (8A-D), only Ebselen β-D-xyloside (8A) showed significant cytotoxicity in human cancer cells. The following facts indicated that the aglycone Ebselen and β-D-xyloside primed glycosaminoglycans co-contributed to the observed cytotoxicity: 1. Ebselen induced S phase cell cycle arrest whereas 8A induced G2/M cell cycle arrest; 2...
March 27, 2018: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29559968/-in-vitro-efficacy-of-ebselen-and-bay-11-7082-against-naegleria-fowleri
#9
Anjan Debnath, Andrew T Nelson, Angélica Silva-Olivares, Mineko Shibayama, Dionicio Siegel, James H McKerrow
Primary amebic meningoencephalitis (PAM) is a fatal infection caused by the free-living ameba Naegleria fowleri , popularly known as the "brain-eating ameba." The drugs of choice in treating PAM are the antifungal amphotericin B and an antileishmanial miltefosine, but these are not FDA-approved for this indication and use of amphotericin B is associated with severe adverse effects. Moreover, very few patients treated with the combination therapy have survived PAM. Therefore, development of efficient drugs is a critical unmet need to avert future deaths of children...
2018: Frontiers in Microbiology
https://www.readbyqxmd.com/read/29556223/repurposing-auranofin-ebselen-and-px-12-as-antimicrobial-agents-targeting-the-thioredoxin-system
#10
REVIEW
Holly C May, Jieh-Juen Yu, M N Guentzel, James P Chambers, Andrew P Cap, Bernard P Arulanandam
As microbial resistance to drugs continues to rise at an alarming rate, finding new ways to combat pathogens is an issue of utmost importance. Development of novel and specific antimicrobial drugs is a time-consuming and expensive process. However, the re-purposing of previously tested and/or approved drugs could be a feasible way to circumvent this long and costly process. In this review, we evaluate the U.S. Food and Drug Administration tested drugs auranofin, ebselen, and PX-12 as antimicrobial agents targeting the thioredoxin system...
2018: Frontiers in Microbiology
https://www.readbyqxmd.com/read/29542192/cyclic-seleninate-esters-spirodioxyselenuranes-and-related-compounds-new-classes-of-biological-antioxidants-that-emulate-glutathione-peroxidase
#11
REVIEW
Kai N Sands, Tyler A Tuck, Thomas G Back
Selenium compounds play an important role in redox homeostasis in living organisms. One of their major functions is to suppress the harmful effects of hydrogen peroxide, hydroperoxides and downstream reactive oxygen species that lead to oxidative stress, which has in turn been implicated in many diseases and degenerative conditions. The glutathione peroxidase (GPx) family of selenoenzymes plays a key protective role by catalyzing the reduction of peroxides with glutathione. Considerable effort has been expended toward the discovery of small-molecule selenium compounds that mimic GPx...
March 14, 2018: Chemistry: a European Journal
https://www.readbyqxmd.com/read/29519735/inhibition-of-histone-lysine-methyltransferases-g9a-and-glp-by-ejection-of-structural-zn-ii
#12
Danny C Lenstra, Abbas H K Al Temimi, Jasmin Mecinović
Histone lysine methyltransferases G9a and GLP are validated targets for the development of new epigenetic drugs. Most, if not all, inhibitors of G9a and GLP target the histone substrate binding site or/and the S-adenosylmethionine cosubstrate binding site. Here, we report an alternative approach for inhibiting the methyltransferase activity of G9a and GLP. For proper folding and enzymatic activity, G9a and GLP contain structural zinc fingers, one of them being adjacent to the S-adenosylmethionine binding site...
April 15, 2018: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29516356/neurotoxic-outcomes-of-subchronic-manganese-chloride-exposure-via-contaminated-water-in-adult-male-rats-and-the-potential-benefits-of-ebselen
#13
Walaa M El-Hady, Azza A A Galal
The neurological effects of manganese (Mn) exposure on adults consuming contaminated water remain unclear. Accordingly, the current experiment was planned to explore the neurotoxic consequences of subchronic Mn exposure via contaminated water and to examine whether ebselen (Ebs) improved these outcomes. Rats exposed to oral MnCl2 (50 mg/kg body weight) for 30 successive days exhibited reduced rearing and ambulation. Furthermore, Mn administration increased brain Mn concentrations and induced superoxide dismutase, catalase, and glutathione depletion...
March 7, 2018: Biological Trace Element Research
https://www.readbyqxmd.com/read/29488609/ebselen-suppresses-inflammation-induced-by-helicobacter-pylori-lipopolysaccharide-via-the-p38-mitogen-activated-protein-kinase-signaling-pathway
#14
Ling Xu, Changguo Gong, Guangming Li, Jue Wei, Ting Wang, Wenying Meng, Min Shi, Yugang Wang
Ebselen is a seleno-organic compound that has been demonstrated to have antioxidant and anti-inflammatory properties. A previous study determined that ebselen inhibits airway inflammation induced by inhalational lipopolysaccharide (LPS), however, the underlying molecular mechanism remains to be elucidated. The present study investigated the effect of ebselen on the glutathione peroxidase (GPX)‑reactive oxygen species (ROS) pathway and interleukin‑8 (IL‑8) expression induced by Helicobacter pylori LPS in gastric cancer (GC) cells...
May 2018: Molecular Medicine Reports
https://www.readbyqxmd.com/read/29488218/ebselen-has-lithium-like-effects-on-central-5-ht-2a-receptor-function
#15
I Antoniadou, M Kouskou, T Arsiwala, N Singh, S R Vasudevan, T Fowler, E Cadirci, G C Churchill, T Sharp
BACKGROUND AND PURPOSE: Lithium's antidepressant action may be mediated by inhibition of inositol monophosphatase (IMPase), a key enzyme in Gq protein coupled receptor signalling. Recently, the antioxidant agent ebselen was identified as an IMPase inhibitor. Here we investigated both ebselen and lithium in models of the 5-HT2A receptor, a Gq protein coupled receptor implicated in lithium's actions. EXPERIMENTAL APPROACH: 5-HT2A receptor function was modelled in mice by measuring the behavioural (head-twitches) and cortical immediate early gene (IEG; Arc, c-fos and Erg2 mRNA) responses to 5-HT2A receptor agonist administration...
February 27, 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29470101/ebselen-reversibly-inhibits-human-glutamate-dehydrogenase-at-the-catalytic-site
#16
Yanhong Jin, Di Li, Shiying Lu, Han Zhao, Zhao Chen, Wei Hou, Benfang Helen Ruan
Human glutamate dehydrogenase (GDH) plays an important role in neurological diseases, tumor metabolism, and hyperinsulinism-hyperammonemia syndrome (HHS). However, there are very few inhibitors known for human GDH. Recently, Ebselen was reported to crosslink with Escherichia coli GDH at the active site cysteine residue (Cys321), but the sequence alignment showed that the corresponding residue is Ala329 in human GDH. To investigate whether Ebselen could be an inhibitor for human GDH, we cloned and expressed an N-terminal His-tagged human GDH in E...
February 2018: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/29447264/ebselen-alleviates-testicular-pathology-in-mice-with-zika-virus-infection-and-prevents-its-sexual-transmission
#17
Yogy Simanjuntak, Jian-Jong Liang, Si-Yu Chen, Jin-Kun Li, Yi-Ling Lee, Han-Chung Wu, Yi-Ling Lin
Despite the low case fatality, Zika virus (ZIKV) infection has been associated with microcephaly in infants and Guillain-Barré syndrome. Antiviral and vaccine developments against ZIKV are still ongoing; therefore, in the meantime, preventing the disease transmission is critical. Primarily transmitted by Aedes species mosquitoes, ZIKV also can be sexually transmitted. We used AG129 mice lacking interferon-α/β and -γ receptors to study the testicular pathogenesis and sexual transmission of ZIKV. Infection of ZIKV progressively damaged mouse testes, increased testicular oxidative stress as indicated by the levels of reactive oxygen species, nitric oxide, glutathione peroxidase 4, spermatogenesis-associated-18 homolog in sperm and pro-inflammatory cytokines including IL-1β, IL-6, and G-CSF...
February 2018: PLoS Pathogens
https://www.readbyqxmd.com/read/29414105/discovery-of-ebselen-as-an-inhibitor-of-cryptosporidium-parvum-glucose-6-phosphate-isomerase-cpgpi-by-high-throughput-screening-of-existing-drugs
#18
Rana Eltahan, Fengguang Guo, Haili Zhang, Lixin Xiang, Guan Zhu
Cryptosporidium parvum is a water-borne and food-borne apicomplexan pathogen. It is one of the top four diarrheal-causing pathogens in children under the age of five in developing countries, and an opportunistic pathogen in immunocompromised individuals. Unlike other apicomplexans, C. parvum lacks Kreb's cycle and cytochrome-based respiration, thus relying mainly on glycolysis to produce ATP. In this study, we characterized the primary biochemical features of the C. parvum glucose-6-phosphate isomerase (CpGPI) and determined its Michaelis constant towards fructose-6-phosphate (Km  = 0...
April 2018: International Journal for Parasitology, Drugs and Drug Resistance
https://www.readbyqxmd.com/read/29405440/ebselen-inhibits-the-activity-of-acetylcholinesterase-globular-isoform-g4-in-vitro-and-attenuates-scopolamine-induced-amnesia-in-mice
#19
Franciele Martini, Ana P Pesarico, César A Brüning, Gilson Zeni, Cristina W Nogueira
There is a well-known relationship between the cholinergic system and learning, memory, and other common cognitive processes. The process for researching and developing new drugs has lead researchers to repurpose older ones. This study investigated the effects of ebselen on the activity of acethylcholinesterase (AChE) isoforms in vitro and in an amnesia model induced by scopolamine in Swiss mice. In vitro, ebselen at concentrations equal or higher than 10 μM inhibited the activity of cortical and hippocampal G4/AChE, but not G1/AChE isoform...
February 5, 2018: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/29379885/a-novel-fluorescence-based-assay-for-the-measurement-of-biliverdin-reductase-activity
#20
Samuel O Adeosun, Kyle H Moore, David M Lang, Assumpta C Nwaneri, Terry D Hinds, David E Stec
Biliverdin reductase (BVR) is the enzyme responsible for the last step in the production of bilirubin from the breakdown of heme. Bilirubin is one of the most potent antioxidant molecules in the body. Monitoring BVR activity is essential in studying the antioxidant capacity of cells and tissues. Traditional methods of determining BVR activity have relied on the measurement of bilirubin converted from biliverdin using absorbance spectroscopy. The approach has limited sensitivity and requires large quantities of cells or tissues...
2018: Reactive Oxygen Species (Apex, N.C.)
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