Journal: Journal of Neuroinflammation

Article Title: Edaravone ameliorates depressive and anxiety-like behaviors via Sirt1/Nrf2/HO-1/Gpx4 pathway

doi: 10.1186/s12974-022-02400-6

Figure Lengend Snippet: Blockade of Sirt1 abolished the antidepressant and anxiolytic effects of EDA. A Schematic timeline of the experimental procedure. B Social interaction test. C Sucrose preference test. D Open field test. E Elevated plus maze test. F Tail suspension test. G Forced swimming test. H Novel object recognition test. All the data are expressed as mean ± SEM ( n = 8 per group). ** p < 0.01, *** p < 0.001 versus the CON group. # p < 0.05, ## p < 0.01, ### p < 0.001 versus the CSDS group. & p < 0.05 versus the CSDS + EDA group

Article Snippet: EX527 (a Sirt1 inhibitor) and ML385 (a Nrf2 inhibitor) were obtained from MedChemExpress (New Jersey, USA).

Techniques: Suspension

Journal: Journal of Neuroinflammation

Article Title: Edaravone ameliorates depressive and anxiety-like behaviors via Sirt1/Nrf2/HO-1/Gpx4 pathway

doi: 10.1186/s12974-022-02400-6

Figure Lengend Snippet: Primer sequences used in the qRT-PCR

Article Snippet: EX527 (a Sirt1 inhibitor) and ML385 (a Nrf2 inhibitor) were obtained from MedChemExpress (New Jersey, USA).

Techniques:

Journal: Journal of Neuroinflammation

Article Title: Edaravone ameliorates depressive and anxiety-like behaviors via Sirt1/Nrf2/HO-1/Gpx4 pathway

doi: 10.1186/s12974-022-02400-6

Figure Lengend Snippet: Effect of EDA on Sirt1/Nrf2/HO-1/Gpx4 and TLR4/NF-κB signaling pathways. A Representative WB bands in the hippocampal region. B – G Statistical graphs of relative protein expression of Sirt1 ( B ), Nrf2 ( C ), HO-1 ( D ), Gpx4 ( E ), TLR4 ( F ), and p-NF-κB ( G ). H Representative WB bands in the mPFC region. I – N Statistical graphs of relative protein expression of Sirt1 ( I ), Nrf2 ( J ), HO-1 ( K ), Gpx4 ( L ), TLR4 ( M ), and p-NF-κB ( N ). Data are presented as mean ± SEM ( n = 4 per group). * p < 0.05, ** p < 0.01, ***p < 0.001 versus the CON + Vehicle group. # p < 0.05, ## p < 0.01, ### p < 0.001 versus the CSDS + Vehicle group

Article Snippet: EX527 (a Sirt1 inhibitor) and ML385 (a Nrf2 inhibitor) were obtained from MedChemExpress (New Jersey, USA).

Techniques: Expressing

Journal: Journal of Neuroinflammation

Article Title: Edaravone ameliorates depressive and anxiety-like behaviors via Sirt1/Nrf2/HO-1/Gpx4 pathway

doi: 10.1186/s12974-022-02400-6

Figure Lengend Snippet: Impact of Sirt1 inhibitor on EDA-induced Sirt1/Nrf2/HO-1/Gpx4 signaling pathway in the Hip of CSDS mice. A Representative WB bands. B – E Protein levels of Sirt1 ( B ), Nrf2 ( c ), HO-1 ( D ), and Gpx4 ( E ) in the Hip. Data are presented as mean ± SEM ( n = 3 per group). * p < 0.05, ** p < 0.01, *** p < 0.001 versus the CON group. ## p < 0.01, ### p < 0.001 versus the CSDS group. && p < 0.01, &&& p < 0.001 versus the CSDS + EDA group

Article Snippet: EX527 (a Sirt1 inhibitor) and ML385 (a Nrf2 inhibitor) were obtained from MedChemExpress (New Jersey, USA).

Techniques:

Journal: Journal of Neuroinflammation

Article Title: Edaravone ameliorates depressive and anxiety-like behaviors via Sirt1/Nrf2/HO-1/Gpx4 pathway

doi: 10.1186/s12974-022-02400-6

Figure Lengend Snippet: Impact of Nrf2 inhibitor on EDA-induced Sirt1/Nrf2/HO-1/Gpx4 signaling pathway in the Hip of CSDS mice. A Representative WB bands. B – E Protein levels of Sirt1 ( B ), Nrf2 ( C ), HO-1 ( D ), and Gpx4 ( E ) in the Hip. Data are presented as mean ± SEM ( n = 3 per group). * p < 0.05, ** p < 0.01, *** p < 0.001 versus the CON group. # p < 0.05, ### p < 0.001 versus the CSDS group. && p < 0.01, &&& p < 0.001 versus the CSDS + EDA group

Article Snippet: EX527 (a Sirt1 inhibitor) and ML385 (a Nrf2 inhibitor) were obtained from MedChemExpress (New Jersey, USA).

Techniques:

Journal: PLoS ONE

Article Title: Synergistic Interactions between HDAC and Sirtuin Inhibitors in Human Leukemia Cells

doi: 10.1371/journal.pone.0022739

Figure Lengend Snippet: Primary AML cells were incubated with or without sirtuin inhibitors (EX527, sirtinol, cambinol) in the presence or absence of VA at the indicated concentrations. Viability was assessed 48 h later by PI cell staining and flow cytometry. CI values refer to the highest drug concentrations used. CI CT s for each drug combination are presented in the lower insets. An effect of 1 corresponds to 100% specific death whereas an effect of 0 corresponds to 0% specific death.

Article Snippet: EX527 was from Tocris Bioscience (Bristol, UK).

Techniques: Incubation, Staining, Flow Cytometry

Journal: PLoS ONE

Article Title: Synergistic Interactions between HDAC and Sirtuin Inhibitors in Human Leukemia Cells

doi: 10.1371/journal.pone.0022739

Figure Lengend Snippet: A, 3×10 6 primary AML cells/well were plated in 6-well plates and incubated in the presence or absence of 50 µM cambinol, 100 µg/ml VA, or their combination. ΔΨ m was monitored at the indicated time points by TMRE staining and flow cytometry. B, 1×10 6 Jurkat cells were plated in 6-well plates and incubated for 48 h in the presence or absence of 100 µg/ml VA. Thereafter, intracellular Bax content was determined by flow cytometry. C, D, Jurkat cells were transduced with either pMIG or pMIG-Bax. Infected cells were FACS sorted, allowed to expand, and subsequently used for flow cytometric detection of intracellular Bax (C) and for viability assays (D). For these, pMIG- or pMIG-Bax-transduced Jurkat were plated in 96-well plates and incubated in the presence or absence of EX527 or cambinol at the indicated concentrations. Viability was determined by PI staining and flow cytometry 48 h later. A–C, one representative experiment out of three is presented. D, Results are means ± SD of three separate experiments.

Article Snippet: EX527 was from Tocris Bioscience (Bristol, UK).

Techniques: Incubation, Staining, Flow Cytometry, Transduction, Infection

Journal: PLoS ONE

Article Title: Synergistic Interactions between HDAC and Sirtuin Inhibitors in Human Leukemia Cells

doi: 10.1371/journal.pone.0022739

Figure Lengend Snippet: A, B, U937 and 697 cells were transduced to either express an anti-EGFP shRNA (EGFP-sh) or a validated anti-Bax shRNA (Bax-sh). Thereafter cells were used for cell lysate preparation and Bax and γ-tubulin were detected by immunoblotting. B, EGFP-sh or Bax-sh 697 cells were incubated with or without 100 µg/ml VA, 75 µM EX527, 50 µM cambinol, or their combinations. Viability was assessed 36 h later by PI staining and flow cytometry. C, D, EGFP-sh or Bax-sh U937 cells were incubated with or without 100 µg/ml VA, 150 µM EX527, 100 µM cambinol, or their combinations. 36 h later, cells were imaged by light microscopy (D) and cell death was determined by flow cytometric quantification of PI-positive cells (C). A, D, one representative experiment out of three is presented. B, C, Results are means ± SD of three separate experiments. *: p<0.05.

Article Snippet: EX527 was from Tocris Bioscience (Bristol, UK).

Techniques: shRNA, Western Blot, Incubation, Staining, Flow Cytometry, Light Microscopy

Journal: Beilstein Journal of Organic Chemistry

Article Title: Azologization and repurposing of a hetero-stilbene-based kinase inhibitor: towards the design of photoswitchable sirtuin inhibitors

doi: 10.3762/bjoc.15.214

Figure Lengend Snippet: Selisistat ( 1 ) and hit compound GW435821X ( 2a ).

Article Snippet: For example, selisistat (EX-527, ), a nanomolar and selective Sirt1 inhibitor, passed phase II clinical trials as a disease-modifying therapeutic for Huntington’s disease (HD) and was acquainted by AOP Orphan Pharmaceuticals AG for phase III trials in 2017 [ – ].

Techniques:

Journal: International Journal of Molecular Sciences

Article Title: Cannabisin F from Hemp ( Cannabis sativa ) Seed Suppresses Lipopolysaccharide-Induced Inflammatory Responses in BV2 Microglia as SIRT1 Modulator

doi: 10.3390/ijms20030507

Figure Lengend Snippet: Cannabisin F increased the expression of SIRT1 and SIRT1 inhibitor EX527 reversed anti-inflammatory action of cannabisin F. ( A and B ) Cannabisin F enhanced expression of SIRT1. BV2 cells were pretreated with cannabisin F (5, 10 and 15 µM) for 1 h prior to stimulation with LPS at 100 ng/mL for 24 h. Cell extracts were harvested and subjected to Western blot with antibodies against SIRT1. β-actin was used as the internal control for normalization. ( C – F ) EX527 reversed the anti-inflammatory activity of Cannabisin F in LPS-stimulated BV2 microglia cells. BV2 cells were pre-treated with EX527 at 10 µM for 1 h, followed by treatment with cannabisin F for 1 h and then stimulation with LPS at 100 ng/mL for 24 h. Culture supernatants were harvested and analyzed for IL-6 ( C ) and TNF-α ( D ) as measured by ELISA. The mRNA levels of IL-6 ( E ) and TNF-α ( F ) were determined by qRT-PCR. The data are presented as mean ± SD from at least three independent experiments. △ p < 0.05, △△△ p < 0.001 as compared to the cells treated with LPS and cannabisin F; * p < 0.05, *** p < 0.001 as compared to the cells treated with LPS; # p < 0.05, ### p < 0.001 as compared to the control.

Article Snippet: A SIRT1 inhibitor EX527 (Selisistat) was purchased from Ark Pharm (Libertyville, IL, USA).

Techniques: Expressing, Western Blot, Activity Assay, Enzyme-linked Immunosorbent Assay, Quantitative RT-PCR