Journal: The Journal of general virology

Article Title: Oxidative stress specifically inhibits replication of dengue virus

doi: 10.1099/jgv.0.001596

Figure Lengend Snippet: (a) Caco-2 cells were infected with DENV at 10 MOI and treated with 0.5 μM TPEN or TPEN with indicated salts at 1 μM concentration. At 24 h pi, cells were fixed and stained using DENV-envelope by immunofluorescence assay. (b) Viral titres in the supernatants were measured at 24 h pi. (c) Caco-2 cells were treated with TPEN alone and in combination with ebselen and salubrinal at 25 and 50 μM respectively. ROS levels were measured at indicated time points using H2DCFDA by flow cytometry. Graph indicates fold change values in mean fluorescence intensity (MFI) normalized to DMSO. (d) Caco-2 cells were infected with DENV at 10 MOI and treated with TPEN alone and with ebselen or salubrinal as above. Viral titres were measured at 24 h pi. (e) Caco-2 cells were infected at 10 MOI of DENV. After viral adsorption, cells were treated with TPEN alone and in combination with ebselen (EBS) (25 μM), S3QEL 2 (10 μM), l-NAME (100 μM). At 24 h pi, cells were fixed and stained using DENV-envelope antibody using immunofluorescence assay. Data are from at least two independent experiments and error bar represents standard deviation. Scale Bar: 100 μm.

Article Snippet: After viral adsorption, cells were treated with DMSO or TPEN alone or in combination with ebselen (25 μM) (TOCRIS), VAS2870 (10 μM) (Sigma-Aldrich), S3QEL 2 (10 μM) (TOCRIS) and l -NAME (100 μM) (Calbiochem) in serum-free medium.

Techniques: Infection, Concentration Assay, Staining, Immunofluorescence, Flow Cytometry, Fluorescence, Adsorption, Standard Deviation

Journal: Frontiers in Cellular and Infection Microbiology

Article Title: Efficacy of Ebselen Against Invasive Aspergillosis in a Murine Model

doi: 10.3389/fcimb.2021.684525

Figure Lengend Snippet: Susceptibility profile of A. fumigatus reference and clinical strains against ebselen and standard antifungals.

Article Snippet: The following compounds were used for susceptibility tests: ebselen (EbSe; C 13 H 9 NOSe; TargetMol), voriconazole (VOR; Pfizer Incorporated, New York, NY, USA), and amphotericin B (AMB; Sigma-Aldrich, St. Louis, MO, USA).

Techniques:

Journal: Frontiers in Cellular and Infection Microbiology

Article Title: Efficacy of Ebselen Against Invasive Aspergillosis in a Murine Model

doi: 10.3389/fcimb.2021.684525

Figure Lengend Snippet: Fungal burden in the kidney after systemic infection by A. fumigatus (ATCC 64026). Control: mice treated with placebo; ebselen: mice treated with 10 mg.kg –1 (765.8 μmoles per mouse) of ebselen; voriconazole: mice treated with 10 mg.kg –1 (572.5 µmoles per mouse) of voriconazole. All groups were treated intraperitoneally twice daily for 4 days starting 1 day after infection. * p < 0.05. Error bars correspond to the standard deviation.

Article Snippet: The following compounds were used for susceptibility tests: ebselen (EbSe; C 13 H 9 NOSe; TargetMol), voriconazole (VOR; Pfizer Incorporated, New York, NY, USA), and amphotericin B (AMB; Sigma-Aldrich, St. Louis, MO, USA).

Techniques: Infection, Standard Deviation

Journal: Frontiers in Cellular and Infection Microbiology

Article Title: Efficacy of Ebselen Against Invasive Aspergillosis in a Murine Model

doi: 10.3389/fcimb.2021.684525

Figure Lengend Snippet: Histological findings in the kidney of immunocompromised BALB/c mice inoculated with Aspergillus fumigatus after five days of systemic infection. (A) Control: mice treated with placebo; (B) voriconazole: mice treated with 10 mg.kg −1 (572.5 µmoles per mouse); (C) ebselen: mice treated with 10 mg.kg −1 (765.8 µmoles per mouse) of ebselen. The treatments were performed intraperitoneally, twice a day, for four days. Tissues were stained with Grocott–Gomori’s methenamine silver (GMS) and hematoxylin and eosin (H&E); magnification, ×400. Asterisk: coagulative necrosis; arrow’s head: hyphae; arrow: mononuclear cell; star: hemorrhage.

Article Snippet: The following compounds were used for susceptibility tests: ebselen (EbSe; C 13 H 9 NOSe; TargetMol), voriconazole (VOR; Pfizer Incorporated, New York, NY, USA), and amphotericin B (AMB; Sigma-Aldrich, St. Louis, MO, USA).

Techniques: Infection, Staining

Journal: STAR Protocols

Article Title: Fluorogenic in vitro activity assay for the main protease M pro from SARS-CoV-2 and its adaptation to the identification of inhibitors

doi: 10.1016/j.xpro.2021.100793

Figure Lengend Snippet:

Article Snippet: Ebselen , Biosynth Carbosynth , FE75162.

Techniques: Recombinant

Journal: bioRxiv

Article Title: Rational design of a new class of protease inhibitors for the potential treatment of coronavirus diseases

doi: 10.1101/2020.09.15.275891

Figure Lengend Snippet: Inhibition of SARSCoV2 M pro activity in vitro . (A) Left, relative M pro activity in the presence of 2 mM DTT and 150 μM of drugs. GC-376 showed the most inhibition, followed by boceprevir, then telaprevir and narlaprevir. The HIV protease inhibitor ritonavir, ebselen, and disulfiram showed less than 50% inhibiting of enzyme activity, indicating IC 50 > 150 μM in reducing conditions. Right, in the absence of DTT, ebselen and disulfiram showed efficient inhibition of M pro activity. Enzymatic assays were carried out with 100 nM purified SARSCoV2 M pro with an uncleaved C-terminal His 6 -tag, M pro -His 6 (B) IC 50 measurements by inhibitor titrations on 100 nM SARSCoV2 M pro -His 6 (top) or 100 nM fully mature SARSCoV2 M pro (bottom). For ebselen and disulfram, measurements were performed in the absence of DTT, while the assay buffer contained 2 mM DTT for all other drugs. Mean values of 2 to 3 independent experiments are shown. Error bars represent standard deviation.

Article Snippet: All other inhibitors were readily available: boceprevir (Cayman Chemical, ≥ 98%), narlaprevir (AdooQ, ≥ 98%), telaprevir (AdooQ Bioscience, ≥ 98%), GC-376 (AOBIOUS, ≥ 98%), ebselen (Cayman Chemical, ≥ 99%), disulfiram (LKT Laboratories, ≥ 98%), ritonavir (Santa Cruz Biotechnology, ≥ 98%).

Techniques: Inhibition, Activity Assay, In Vitro, Protease Inhibitor, Purification, Standard Deviation

Journal: International Journal of Molecular Sciences

Article Title: SARS-CoV-2 Nucleocapsid Protein Induces Tau Pathological Changes That Can Be Counteracted by SUMO2

doi: 10.3390/ijms25137169

Figure Lengend Snippet: NCAP forms condensates that are modulated by SUMOylation in neuronal cells. ( A ) Quantification of NCAP condensates in N2a cells transfected with NCAP-GFP and treated with drugs that affect SUMOylation, i.e., Ebselen (2 µM) or Ginkgolic acid (10 µM), for 16 h. Modulators of SUMOylation altered the number of NCAP condensates in N2a compared with vehicle alone; one-way ANOVA followed by Tukey’s multiple comparisons test; * p < 0.05, **** p < 0.0001 ( n = 69, from three independent replicates). Scale bar: 20 µm. ( B ) Neural progenitor cells (NPCs) were differentiated into glutamatergic neurons for over 30 days in vitro before transfection with NCAP-GFP and SUMO2. After 5 days from transfection, cells were fixed, and images of transfected NCAP were acquired by confocal microscope. Co-transfection with SUMO2 induced a significant reduction in the size of NCAP-positive granules, unpaired t -test: * p < 0.05 ( n = 10 neurons per condition). Scale bar: 20 µm.

Article Snippet: Ebselen and Ginkgolic acid were purchased from Tocris (Bristol, UK).

Techniques: Transfection, In Vitro, Microscopy, Cotransfection

Journal: Oxidative Medicine and Cellular Longevity

Article Title: Reactive Oxygen Species Evoked by Potassium Deprivation and Staurosporine Inactivate Akt and Induce the Expression of TXNIP in Cerebellar Granule Neurons

doi: 10.1155/2017/8930406

Figure Lengend Snippet: Antioxidants inhibit the expression of TXNIP induced by K5. Primary cultures of rat cerebellar granule neurons (CGN) were cultured with K25 as described in Materials and Methods. After 7 DIV cells were treated with K5 during 4 hours and the levels of TXNIP were evaluated as described. K25 was used as negative control and K5 (4 h) was used as positive control. In K5 (4 h), cells were preincubated with antioxidants EUK-134 (10 and 20 µ M) and Ebselen (10 µ M), as well as with the NOX inhibitors DPI (520 nm) and AEBSF (50 µ M). The immunoblot was performed against TXNIP and GAPDH. GAPDH is the load control. TXNIP: 50 kDa, GAPDH: 37 kDa. Representative blot from 3 independent assays. Eb, Ebselen; AEB, AEBSF.

Article Snippet: Ebselen and EUK-134 were from Cayman Chemical (Ann Arbor, MI, USA).

Techniques: Expressing, Cell Culture, Negative Control, Positive Control, Western Blot, Control

Journal: Oxidative Medicine and Cellular Longevity

Article Title: Reactive Oxygen Species Evoked by Potassium Deprivation and Staurosporine Inactivate Akt and Induce the Expression of TXNIP in Cerebellar Granule Neurons

doi: 10.1155/2017/8930406

Figure Lengend Snippet: Antioxidants inhibit the expression of TXNIP induced by Sts. Primary cultures of rat cerebellar granule neurons (CGN) were cultured with K25 as described in Materials and Methods. After 7 DIV cells were treated with staurosporine (0.5 µ M) during 5.5 hours and the levels of TXNIP were evaluated as described. K25 was used as negative control and Sts (5.5 h) was used as positive control. In Sts (5.5 h), cells were preincubated with antioxidants EUK-134 (10 and 20 µ M) and Ebselen (10 µ M), as well as with the NOX inhibitors DPI (520 nm) and AEBSF (50 µ M). The immunoblot was performed against TXNIP and GAPDH. GAPDH is the load control. TXNIP: 50 kDa, GAPDH: 37 kDa. Representative blot from 3 independent assays. Eb, Ebselen; AEB, AEBSF.

Article Snippet: Ebselen and EUK-134 were from Cayman Chemical (Ann Arbor, MI, USA).

Techniques: Expressing, Cell Culture, Negative Control, Positive Control, Western Blot, Control