Sound Pharma News - LARVOL Sigma

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|||||||||| ebselen (SPI-1005) / Sound Pharma
Journal: New cyclophilin D inhibitor rescues mitochondrial and cognitive function in Alzheimer's disease. (Pubmed Central) - May 3, 2024
Inhibition of CypD by Ebselen protects against sporadic AD- and amyloid beta (A?)-induced mitochondrial and glycolytic perturbation, synaptic and cognitive dysfunction, together with suppressing neuroinflammation in the brain of AD mouse models, which is linked to CypD-related mPTP formation. Thus, CypD inhibitors have the potential to slow the progression of neurodegenerative diseases, including AD, by boosting mitochondrial bioenergetics and improving synaptic and cognitive function.

|||||||||| ebselen (SPI-1005) / Sound Pharma
Journal: Ebselen analogues with dual human neutrophil elastase (HNE) inhibitory and antiradical activity. (Pubmed Central) - Apr 26, 2024
The most active compounds 4d, 4f, and 4j exhibited a good balance between anti-HNE (IC50 = 0.9-1.4 ?M) and antiradical activity (IC50 = 0.05-0.7 ?M). Additionally, the solid-state structure of 4d was determined and compared to that of the similar compound N-propionyl-1,2-benzisoselenazol-3(2H)-one.

|||||||||| ebselen (SPI-1005) / Sound Pharma
Preclinical, Review, Journal: Brief Review and Perspective: Antioxidants for early treatment of Type 2 Diabetes in Rodents and Humans: Lost in Translation? (Pubmed Central) - Apr 22, 2024
Prdxs detoxify hydrogen peroxide and reduce lipid peroxides. This suggests that pharmacologic development of more potent, beta cell specific antioxidants could be valuable as a treatment for oxidative stress due to post-prandial hyperglycemia in early type 2 diabetes in humans.

|||||||||| ebselen (SPI-1005) / Sound Pharma
The Effects of Ebselen on Brain Neurochemistry in Depressed Patients on Antidepressants (Griffin Hall) - Apr 14, 2024 - Abstract #SOBP2024SOBP_376;
This suggests that pharmacologic development of more potent, beta cell specific antioxidants could be valuable as a treatment for oxidative stress due to post-prandial hyperglycemia in early type 2 diabetes in humans. In patients with treatment-resistant depression, as in healthy volunteers, ebselen reduces inositol and glx levels potentially via inositol monophosphatase and glutaminase inhibition, respectively.

|||||||||| ebselen (SPI-1005) / Sound Pharma
Journal: The small molecule CBR-5884 inhibits the Candida albicans phosphatidylserine synthase. (Pubmed Central) - Apr 8, 2024
Three of these, ebselen, LOC14, and CBR-5884, exhibited antifungal effects against C. albicans cells, with fungicidal inhibition by ebselen and fungistatic inhibition by LOC14 and CBR-5884...The significance of our research is that we developed a high-throughput target-based assay and identified the first Cho1 inhibitor, CBR-5884, which acts both on the purified protein and its function in the cell. This molecule acts as a competitive inhibitor with a Ki value of 1,550

|||||||||| ebselen (SPI-1005) / Sound Pharma
Journal: Bioinspired Selenium-Nitrogen Exchange (SeNEx) Click Chemistry Suitable for Nanomole-Scale Medicinal Chemistry and Bioconjugation. (Pubmed Central) - Apr 3, 2024
This molecule acts as a competitive inhibitor with a Ki value of 1,550 We report the first selenium-nitrogen exchange (SeNEx) click reaction between benzoselenazolones and terminal alkynes (Se-N to Se-C), which is inspired by the biochemical SeNEx between Ebselen and cysteine (Cys) residue (Se-N to Se-S)...Besides, this reaction is characterized by modular, predictable, high-yielding, fast kinetics (k2

|||||||||| ebselen (SPI-1005) / Sound Pharma
Preclinical, Journal: N-3-Methylbutyl-benzisoselenazol-3(2H)-one Exerts Antifungal Activity In Vitro and in a Mouse Model of Vulvovaginal Candidiasis. (Pubmed Central) - Mar 27, 2024
In the present work, we evaluated the antifungal activities of two novel ebselen analogs, N-allyl-benzisoselenazol-3(2H)-one (N-allyl-bs) and N-3-methylbutylbenzisoselenazol-3(2H)-one (N-3mb-bs)...We then utilized the N-3mb-bs compound (12.5 mg/kg) in the mouse VVC model and observed that it significantly reduced the vaginal fungal burden, histopathological changes in vagina tissue, and expression of myeloperoxidase (MPO). All in all, the present work has identified a potentially promising drug candidate for VVC treatment.

|||||||||| ebselen (SPI-1005) / Sound Pharma
Journal: Fingerprints of Chalcogen Bonding Revealed Through 77Se-NMR. (Pubmed Central) - Mar 20, 2024
77Se-NMR is used to characterise several chalcogen bonded complexes of derivatives of the organoselenium drug ebselen, exploring a range of electron demand...A single crystal NMR experiment was conducted using one of the co-crystals, affording the absolute orientation of the chemical shift tensor within the crystal. This showed that the selenium nucleus is strongly shielded in the direction of the chalcogen bond, and strongly deshielded in the perpendicular direction, consistent with the presence of a second ?-hole which is not participating in a chalcogen bond.

|||||||||| Legalon (silibinin) / Viatris, ebselen (SPI-1005) / Sound Pharma, Xocova (ensitrelvir) / Shionogi
Journal: Improved fluorescence-based assay for rapid screening and evaluation of SARS-CoV-2 main protease inhibitors. (Pubmed Central) - Mar 8, 2024
Moreover, our results revealed that ensitrelvir is a potent Mpro inhibitor, but baicalein, chloroquine, ebselen, echinatin, and silibinin are not. Therefore, this robust ddRFP assay provides a faithful avenue for rapid screening and evaluation of Mpro inhibitors to fight against COVID-19.

|||||||||| ebselen (SPI-1005) / Sound Pharma
Journal: Attenuation of phytofungal pathogenicity of Ascomycota by autophagy modulators. (Pubmed Central) - Mar 4, 2024
We identified ebselen (EB) and its analogs ebselen oxide (EO) and 2-(4-methylphenyl)-1,2-benzisothiazol-3(2H)-one (PT) as inhibitors of fungal pathogens Botrytis cinerea and Magnaporthe oryzae ATG4-mediated ATG8 processing...Treatment with EB and its analogs significantly reduced fungal pathogenicity. Our findings provide molecular insights to develop the next generation of antifungal compounds by targeting autophagy in important fungal pathogens.

|||||||||| ebselen (SPI-1005) / Sound Pharma
Journal: Advances in drug structure-activity-relationships for the development of selenium-based compounds against HIV. (Pubmed Central) - Feb 5, 2024
Ebselen, which acts as an HIV capsid inhibitor, serves as a valuable probe compound for the discovery of novel HIV integrase inhibitors. Furthermore, it is crucial not to underestimate the potential toxicity associated with organic selenium compounds despite no reported instances of severe toxicity.

|||||||||| ebselen (SPI-1005) / Sound Pharma
Journal: Repurposing ebselen as an inhalable dry powder to treat respiratory tract infections. (Pubmed Central) - Jan 29, 2024
The deposition of the dry powder in the respiratory tract is dependent on its physicochemical properties and this properties can be modulated to target the intended site of infection (upper and/or lower respiratory tract). Further studies will allow the development of similar formulations of individual and/or combination of antimicrobials that could be used to inhibit a number of respiratory pathogens.

|||||||||| Zyclara (imiquimod) / Mochida, Viatris, Bausch Health, ebselen (SPI-1005) / Sound Pharma
Review, Journal: Novel Therapeutic Hybrid Systems Using Hydrogels and Nanotechnology: A Focus on Nanoemulgels for the Treatment of Skin Diseases. (Pubmed Central) - Jan 22, 2024
Developed formulations revealed adequate droplet size, PDI, viscosity, spreadability, pH, stability, drug release, and drug permeation and/or retention capacity, having more advantageous characteristics than current marketed formulations. In vitro and/or in vivo studies established the safety and efficacy of the developed formulations, confirming their therapeutic potential, and making them promising platforms for the replacement of current therapies, or as possible adjuvant treatments, which might someday effectively reach the market to help fight highly incident skin or systemic diseases and conditions.

|||||||||| ebselen (SPI-1005) / Sound Pharma
Preclinical, Journal: Carnosic Acid Shows Higher Neuroprotective Efficiency than Edaravone or Ebselen in In Vitro Models of Neuronal Cell Damage. (Pubmed Central) - Jan 15, 2024
Our data indicate that the neuroprotective potential of CA, ED, and EB may be revealed in vitro only under specific conditions, with their rather narrow micromolar concentrations, relevant cellular model, type of toxic agent, and exposure time. Nevertheless, of the three compounds tested, CA displayed the most consistent neuroprotective effects.

|||||||||| ebselen (SPI-1005) / Sound Pharma
Journal: Ebselen Optimized the Therapeutic Effects of Silver Nanoparticles for Periodontal Treatment. (Pubmed Central) - Jan 8, 2024
Moreover, AgNPs and ebselen together declined the release of P. gingivalis-stimulated inflammatory cytokines both in vitro and in vivo, and reduced alveolar bone resorption effectively. AgNPs combined with ebselen would be an effective adjuvant for periodontal treatment owing to their synergistic antibacterial and anti-inflammatory effects.

|||||||||| ebselen (SPI-1005) / Sound Pharma
Journal: Dynamic Covalent Bonds in the Ebselen Class of Antioxidants (Pubmed Central) - Dec 21, 2023
Bond orders and percentage covalency and ionicity estimated from the X-ray wavefunctions, along with localized orbital locator (LOL) and electron localization function (ELF) analyses show that the Se-N bond is unique in its closed shell-like features, despite being a covalent bond. Time-dependent DFT calculations simulate the cleavage of Se-N bonds in ebselen in the excited state, further substantiating their nature as dynamic bonds.

|||||||||| ebselen (SPI-1005) / Sound Pharma
Journal: Synthesis and glutathione peroxidase (GPx)-like activity of selenocystine (SeC) bioconjugates of biotin and lipoic acid. (Pubmed Central) - Dec 18, 2023
The SeC-bioconjugates, SeC-Biotin (1) and SeC-Lipoic acid (2) were synthesized using solid phase peptide synthesis (SPPS) method and were characterized by multinuclear 1D (H, C, Se) and 2D (H-H COSY and H-C TOCSY) NMR spectroscopy, ESI-MS spectrometry, and RP-HPLC. The GPx-like enzyme mimicking activity of the SeC-bioconjugates 1 and 2 has been investigated through the coupled reductase assay method for the catalytic reductions of hydrogen peroxide into water A significant enhancement in GPx-like enzymatic activity was observed for both novel bioconjugates SeC-Biotin (1) and SeC-Lipoic acid (2) as compared to diphenyl diselenide (PhSe), L-selenocystine (SeC), biotin, lipoic acid, and ebselen.

|||||||||| ebselen (SPI-1005) / Sound Pharma
Journal: Computational analysis of the interactions between Ebselen and derivatives with the active site of the main protease from SARS-CoV-2. (Pubmed Central) - Nov 27, 2023
Moreover, this study also reveals that all compounds have the potential to interact closely with the active site of Mpro, providing us with a concept of which derivatives may be promising for in vitro analysis in the future. We propose that these compounds are potential covalent inhibitors of M and that organoselenium compounds are molecules that should be studied for their antiviral properties.

|||||||||| ebselen (SPI-1005) / Sound Pharma, Cu(II)ATSM / Collaborative Medicinal Development, Tyzeka (telbivudine) / Novartis
A polytherapy approach demonstrates therapeutic efficacy in familial SOD1 ALS models (Event Halle, Messe Basel, Ground Floor) - Nov 7, 2023 - Abstract #ALSMND2023ALS_MND_476;
Furthermore, multiple different ratios of the CET treatment) were found to significantly improve survival compared to the highest concentration of CuATSM alone tested (0.5 mM) (p < 0.05), despite using less than half the concentration of CuATSM. In addition, CET treatment significantly reduced the percentage of cells containing inclusions compared to the highest concentration of CuATSM alone.

|||||||||| ebselen (SPI-1005) / Sound Pharma
Journal: Ebselen oxide and derivatives are new allosteric HER2 inhibitors for HER2-positive cancers. (Pubmed Central) - Oct 23, 2023
Finally, ebselen oxide significantly blocked HER2+ breast tumor progression in vivo. Collectively, these data provide evidence that ebselen oxide is a newly identified allosteric inhibitor of HER2 to be considered for therapeutic intervention on HER2+ cancers.

|||||||||| morphine sulphate / Generic mfg.
Journal: The Endolysosomal Transporter DMT1 is Required for Morphine Regulation of Neuronal Ferritin Heavy Chain. (Pubmed Central) - Oct 22, 2023
This pathway requires the endolysosomal iron transporter DMT1, as pharmacological and genetic inhibitors of the transporter completely block morphine's ability to upregulate FHC. Created with BioRender.com .

|||||||||| ebselen (SPI-1005) / Sound Pharma
Journal: Ebselen Inhibits the Growth of Lung Cancer Cells via Cell Cycle Arrest and Cell Death Accompanied by Glutathione Depletion. (Pubmed Central) - Oct 4, 2023
Z-VAD did not affect ROS levels or GSH depletion in Ebselen-treated A549 or Ebselen-treated Calu-6 cells. In conclusion, Ebselen inhibited the growth of lung cancer and normal fibroblast cells and induced cell cycle arrest and cell death in lung cancer cells with GSH depletion.

||||||||||  ebselen (SPI-1005) / Sound Pharma
Trial completion date, Trial primary completion date:  SPI-1005 Treatment in Severe COVID-19 Patients (clinicaltrials.gov) -  Oct 3, 2023
P2, N=60, Enrolling by invitation,  Sponsor: Sound Pharmaceuticals, Incorporated
In conclusion, Ebselen inhibited the growth of lung cancer and normal fibroblast cells and induced cell cycle arrest and cell death in lung cancer cells with GSH depletion. Trial completion date: Apr 2023 --> Dec 2023 | Trial primary completion date: Apr 2023 --> Dec 2023

||||||||||  ebselen (SPI-1005) / Sound Pharma
Trial completion date, Trial primary completion date:  SPI-1005 Treatment in Moderate COVID-19 Patients (clinicaltrials.gov) -  Oct 3, 2023
P2, N=60, Enrolling by invitation,  Sponsor: Sound Pharmaceuticals, Incorporated
Trial completion date: Apr 2023 --> Dec 2023 | Trial primary completion date: Apr 2023 --> Dec 2023 Trial completion date: Apr 2023 --> Dec 2023 | Trial primary completion date: Apr 2023 --> Dec 2023

|||||||||| ebselen (SPI-1005) / Sound Pharma
Journal: Nanoformulation of a novel potent ebselen analog for treatment of vulvovaginal candidiasis. (Pubmed Central) - Oct 2, 2023
The G20-SNEP formulation significantly reduced vaginal colonization and vaginal inflammation relative to yeast-infected but untreated control mice. G20-SNEP exhibits potent antimycotic activity in a mouse model of vulvovaginal candidiasis.

|||||||||| ebselen (SPI-1005) / Sound Pharma
Preclinical, Journal: Oxidative stress in rat brain during experimental status epilepticus: effect of antioxidants. (Pubmed Central) - Sep 28, 2023
To test central actions of antioxidants, we used the lithium-pilocarpine (Li-Pilo) model of status epilepticus (SE) in the rat in which seizures are accompanied by significant oxidative stress...Six different antioxidants were tested in acute and preventive experiments (vitamin C, vitamin E, ebselen, resveratrol, n-tert-butyl-?-phenylnitrone and coenzyme Q10)...We conclude that preventive treatment with vitamin C or vitamin E ameliorates seizure-induced oxidative damage in the brain. Several well-studied antioxidants were inactive, possibly due to limited brain permeability or a lack of chain-breaking antioxidant activity in hydrophilic compounds.

|||||||||| ebselen (SPI-1005) / Sound Pharma
Journal: Spray-Dried Inhalable Microparticles Combining Remdesivir and Ebselen against SARS-CoV-2 Infection. (Pubmed Central) - Sep 28, 2023
The spray-dried inhalable microparticles retained their limited cytotoxicity and specific antiviral properties. Future in vivo studies are needed to verify the potential use of these remdesivir/ebselen combinational spray-dried inhalable microparticles to block the SARS-CoV-2 replication in the respiratory tract.

|||||||||| ebselen (SPI-1005) / Sound Pharma, Bay11-7082 / Bayer, Torisel (temsirolimus) / Pfizer
Journal: High-Throughput Screening of the Repurposing Hub Library to Identify Drugs with Novel Inhibitory Activity against Candida albicans and Candida auris Biofilms. (Pubmed Central) - Sep 27, 2023
In addition, their in vivo activity was examined in the murine models of hematogenously disseminated C. albicans and C. auris infections. Although promising, further in vitro and in vivo studies are needed to confirm their potential use for the therapy of candidiasis and possibly other fungal infections.

|||||||||| ebselen (SPI-1005) / Sound Pharma
Journal: Ebselen, Iron Uptake Inhibitor, Alleviates Iron Overload-Induced Senescence-Like Neuronal Cells SH-SY5Y via Suppressing the mTORC1 Signaling Pathway. (Pubmed Central) - Sep 21, 2023
This also suppressed the expression of p53 protein targeting DNA damage response (DDR)/p21 cyclin-dependent kinase (CDK) inhibitor through a mTORC1 signaling pathway. Potentially, ebselen could be a therapeutic agent for treating brain aging and AD by mitigating iron accumulation and restoring senescence in SH-SY5Y cells.

|||||||||| ebselen (SPI-1005) / Sound Pharma
Review, Journal: Should ebselen be considered for the treatment of mercury intoxication? A minireview. (Pubmed Central) - Sep 21, 2023
Potentially, ebselen could be a therapeutic agent for treating brain aging and AD by mitigating iron accumulation and restoring senescence in SH-SY5Y cells. Accordingly, as observed in

|||||||||| ebselen (SPI-1005) / Sound Pharma
Review, Journal: Ebselen: A Review on its Synthesis, Derivatives, Anticancer Efficacy and Utility in Combating SARS-COV-2. (Pubmed Central) - Sep 15, 2023
Allopurinol and ebselen administered orally can be used to suppress renal ototoxicity and nephrotoxicity...Ebselen may also inhibit the activation of endosomal NADPH oxidase of vascular endothelial cells, which is believed to be required for thrombotic complications in COVID-19. In this review, we have included various studies conducted on the anticancer effect of ebselen as well as its inhibition of SARS-CoV-2.

|||||||||| ebselen (SPI-1005) / Sound Pharma
Journal: Molecular characterisation of Entamoeba histolytica UDP-glucose 4-epimerase, an enzyme able to provide building blocks for cyst wall formation. (Pubmed Central) - Sep 7, 2023
The importance of the ability of GalE to interconvert UDP-GalNAc and UDP-GlcNAc may be that the trophozoites can generate precursors for their own cyst wall from the sugar subunits cleaved from host mucins. This finding advances our understanding of the biochemical interactions of E. histolytica in its colonic environment.

|||||||||| ebselen (SPI-1005) / Sound Pharma
Journal: Four new stilbenes and one new flavonoid with potential antibacterial and anti-SARS-CoV-2 activity from Cajanus cajan. (Pubmed Central) - Aug 31, 2023
This finding advances our understanding of the biochemical interactions of E. histolytica in its colonic environment. Among them, the MIC values of compounds 4, 6, and 7 against S. aureus were 1.56, 0.78, and 0.78

|||||||||| ebselen (SPI-1005) / Sound Pharma
Journal: Synthesis, cytotoxicity, antioxidant activity and molecular modeling of new NSAIDs-EBS derivatives. (Pubmed Central) - Aug 22, 2023
The redox properties of the NSAIDs-EBS derivatives prepared herein were conducted by 2, 2-didiphenyl-1-picrylhydrazyl (DPPH), bleomycin dependent DNA damage and glutathione peroxidase (GPx)-like assays. Finally, TrxR1 inhibition activity assay and molecular docking study revealed NSAIDs-EBS derivatives could serve as potential TrxR1 inhibitor.

|||||||||| ebselen (SPI-1005) / Sound Pharma, Kerydin (tavaborole) / Pfizer, Tirazone (tirapazamine) / Teclison, SRI International
Journal: Repurposing High-Throughput Screening Identifies Unconventional Drugs with Antibacterial and Antibiofilm Activities against Pseudomonas aeruginosa under Experimental Conditions Relevant to Cystic Fibrosis. (Pubmed Central) - Aug 21, 2023
The mode-of-action studies revealed ebselen, carmofur, and tirapazamine targeted the cell membrane, increasing its permeability with subsequent cell lysis. These drugs are strong candidates for repurposing for treating CF lung P. aeruginosa infections.

|||||||||| ebselen (SPI-1005) / Sound Pharma
Journal: Exploring the inhibition mechanism of SARS-CoV-2 main protease by ebselen: A molecular docking, molecular dynamics simulation and DFT approach. (Pubmed Central) - Aug 7, 2023
The simulation results show that the behavior of water molecules at the hydrolysis site is crucial to distinguish the two paths energetically. Our simulations, which are in agreement with existing experimental results, provide a theoretical basis for the rational design and mechanism exploration of ebselen-based inhibitors.

|||||||||| ebselen (SPI-1005) / Sound Pharma
Preclinical, Journal: Ebselen and Diphenyl Diselenide Inhibit SARS-CoV-2 Replication at Non-Toxic Concentrations to Human Cell Lines. (Pubmed Central) - Jul 29, 2023
Importantly, the concentration rates tested on viral replication were not toxic to human PBMCs. Therefore, our findings reinforce the efficacy of Eb and demonstrate (PhSe) as a new candidate to be tested in future trials against SARS-CoV-2 infection/inflammation conditions.

|||||||||| ebselen (SPI-1005) / Sound Pharma
Review, Journal: Ebselen: A promising therapy protecting cardiomyocytes from excess iron in iron-overloaded thalassemia patients. (Pubmed Central) - Jul 19, 2023
In conclusion ebselen can be a promising adjuvant therapy in patients with thalassemia alongside the standard treatment with iron chelators, particularly in severe cases with cardiomyopathy, due to falling iron inflow by inhibiting DMT-1 and increasing ferroportin-1 expression and antioxidant properties. However, clinical studies need to be carried out to reach a definite conclusion.

|||||||||| ebselen (SPI-1005) / Sound Pharma
Journal: Design, Synthesis, and Biological Evaluation of Novel Indanone Derivatives as Cholinesterase Inhibitors for Potential Use in Alzheimer's Disease. (Pubmed Central) - Jul 17, 2023
Molecular docking studies indicated that 5c interacts with AChE in a very similar way to that observed experimentally for donepezil. The introduced indanone-aminopropoxy benzylidenes could be used in drug-discovery development against Alzheimer's disease.

|||||||||| ebselen (SPI-1005) / Sound Pharma
Lipidomic dysfunction accompanied phosphatidylethanolamine deregulation is a potential detection biomarker and drug target for early Alzheimer (Virtual) - Jul 6, 2023 - Abstract #AAIC2023AAIC_7258;
EVs mediated crosstalk between adipose tissue and CNS of obese patients in promoting cognitive impairment and mechanically disturbing lipid quiescent states in the CNS. Maintaining lipid homeostasis, particularly the PE level in the CNS via pharmacology strategy, would open up a new avenue for combating AD.

|||||||||| ebselen (SPI-1005) / Sound Pharma
Lipidomic dysfunction accompanied phosphatidylethanolamine deregulation is a potential detection biomarker and drug target for early Alzheimer (Virtual) - Jul 6, 2023 - Abstract #AAIC2023AAIC_5192;
EVs mediated crosstalk between adipose tissue and CNS of obese patients in promoting cognitive impairment and mechanically disturbing lipid quiescent states in the CNS. Maintaining lipid homeostasis, particularly the PE level in the CNS via pharmacology strategy, would open up a new avenue for combating AD.

|||||||||| ebselen (SPI-1005) / Sound Pharma
Lipidomic dysfunction accompanied phosphatidylethanolamine deregulation is a potential detection biomarker and drug target for early Alzheimer (Virtual) - Jul 6, 2023 - Abstract #AAIC2023AAIC_2946;
EVs mediated crosstalk between adipose tissue and CNS of obese patients in promoting cognitive impairment and mechanically disturbing lipid quiescent states in the CNS. Maintaining lipid homeostasis, particularly the PE level in the CNS via pharmacology strategy, would open up a new avenue for combating AD.

|||||||||| ebselen (SPI-1005) / Sound Pharma
Lipidomic dysfunction accompanied phosphatidylethanolamine deregulation is a potential detection biomarker and drug target for early Alzheimer (Virtual) - Jul 6, 2023 - Abstract #AAIC2023AAIC_726;
EVs mediated crosstalk between adipose tissue and CNS of obese patients in promoting cognitive impairment and mechanically disturbing lipid quiescent states in the CNS. Maintaining lipid homeostasis, particularly the PE level in the CNS via pharmacology strategy, would open up a new avenue for combating AD.

||||||||||  ebselen (SPI-1005) / Sound Pharma
Trial completion date, Trial primary completion date:  OxIMP: IMPase in Treatment-resistant Depression (clinicaltrials.gov) -  Jul 6, 2023
P1, N=50, Recruiting,  Sponsor: University of Oxford
Maintaining lipid homeostasis, particularly the PE level in the CNS via pharmacology strategy, would open up a new avenue for combating AD. Trial completion date: May 2023 --> May 2024 | Trial primary completion date: May 2023 --> May 2024

|||||||||| ebselen (SPI-1005) / Sound Pharma
Journal: Molecular responses during bacterial filamentation reveal inhibition methods of drug-resistant bacteria. (Pubmed Central) - Jun 30, 2023
By using a chemical inhibitor, ebselen, to inhibit diguanylate cyclases which catalyzes the synthesis of c-di-GMP, the minimum inhibitory concentration of ceftriaxone against ESBL-E...coli strains and other beta-lactam antibiotics, i.e., ampicillin...coli by knocking out the dgcM gene was used to demonstrate that the inhibition of the antibiotic resistance to beta-lactams by ebselen was mediated through the inhibition of the diguanylate cyclase DgcM and the modulation of c-di-GMP levels. Our study uncovers the molecular changes during bacterial filamentation and proposes a method to inhibit antibiotic-resistant bacteria by combining traditional antibiotics and chemical inhibitors against the enzymes involved in bacterial self-saving responses.

|||||||||| ebselen (SPI-1005) / Sound Pharma
Journal: 2-Benzamide Tellurenyl Iodides: Synthesis and Their Catalytic Role in CO2 Mitigation. (Pubmed Central) - Jun 20, 2023
Ebselen molecule derived from benzamide moiety is the most studied organoselenium...The mechanistic investigation for CO2 mitigation is done by 125Te NMR and HRMS studies. It seems that the reaction proceeds via formation of catalytically active Te-N heterocycle, an ebtellur intermediate which is isolated and structurally characterized.

|||||||||| ebselen (SPI-1005) / Sound Pharma, Evrenzo (roxadustat) / Astellas, AstraZeneca, FibroGen
Journal: Kinetic and inhibition studies on human Jumonji-C (JmjC) domain-containing protein 5. (Pubmed Central) - Jun 9, 2023
The JMJD5 inhibition assays were validated by investigating the effect of reported 2OG oxygenase inhibitors on JMJD5 catalysis; the results reveal that broad-spectrum 2OG oxygenase inhibitors are also efficient JMJD5 inhibitors (e.g. N-oxalylglycine, pyridine-2,4-dicarboxylic acid, ebselen) whereas most 2OG oxygenase inhibitors that are in clinical use (e.g. roxadustat) do not inhibit JMJD5. The SPE-MS assays will help enable the development of efficient and selective JMJD5 inhibitors for investigating the biochemical functions of JMJD5 in cellular studies.

|||||||||| ebselen (SPI-1005) / Sound Pharma
Journal: Mycobacterium tuberculosis CitA activity is modulated by cysteine oxidation and pyruvate binding. (Pubmed Central) - May 30, 2023
A crystal structure of CitA modified by Ebselen was solved, but significant structural changes were lacking. Considering that covalent modification of C143 inactivates CitA and the proximity of C143 to the pyruvate binding site, this suggests that structural and/or chemical changes in this sub-domain are responsible for regulating CitA enzymatic activity.

|||||||||| ebselen (SPI-1005) / Sound Pharma, selenomethionine (SLM) / University of Iowa, Holden Comprehensive Cancer Center
Preclinical, Journal: Antiproliferative Effect of Inorganic and Organic Selenium Compounds in Breast Cell Lines. (Pubmed Central) - May 27, 2023
Selenite had a high SI to the BT cell line; however, the SI of ebselen and diphenyl diselenide was low in both tumoral cell lines. In conclusion, the Se compounds had different effects on the breast cell lines, and additional tests are needed to reveal the antiproliferative effects of Se compounds.

|||||||||| ebselen (SPI-1005) / Sound Pharma
Journal: Chiral 2-azabicycloalkanes bearing 1,2,3-triazole, thiourea, and ebselen moieties - Synthesis and biological activity. (Pubmed Central) - May 24, 2023
2-Azabicycloalkanes: 2-azabicyclo[2.2.1]heptane and 2-azabicyclo[3.2.1]octane were used as a chiral platform for the construction of a set of 1,2,3-triazole, thiourea, and ebselen derivatives. Cytotoxicity and antiviral activity studies revealed the most promising potency for selected thioureas.



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