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- | erastin - Whitehead Institute for Biomedical Research, Dana / Farber Cancer Institute, Columbia University, Prolexys, Caplyta (lumateperone) - Intra / Cellular Therapies
FDA event, Journal: Identifying eleven new ferroptosis inhibitors as neuroprotective agents from FDA-approved drugs. (Pubmed Central) - Apr 15, 2024
1176 drugs have been screened against erastin-induced ferroptosis in HT22 cells, resulting in 89 ferroptosis inhibitors...The most active ferroptosis inhibitor is lumateperone tosylate at nanomolar level...Notably, the active properties of some drugs were firstly revealed here. These ferroptosis inhibitors increase the chemical diversity of ferroptosis inhibitors, and offer new therapeutic possibilities for the treatments of related neurological diseases.
- | Journal: Bioactive Fractions Isolated from Harungana madagascariensis Lam. and Psorospermum aurantiacum Engl. Regulate Collagen and Melanin Biosynthesis Gene Expression in UVB-Irradiated Cells with Additional Anti-Inflammatory Potential. (Pubmed Central) - Mar 15, 2024
These ferroptosis inhibitors increase the chemical diversity of ferroptosis inhibitors, and offer new therapeutic possibilities for the treatments of related neurological diseases. Overall, the hexane fraction of HM and methanol fraction of PA displayed effective anti-aging activities, with additional anti-inflammatory effects.
- utreloxastat (PTC857) / PTC Therap
CARDINALS: A Phase 2, Randomized, Double-blind, Placebo-controlled, Parallel-group Study to Evaluate the Efficacy and Safety of Utreloxastat (PTC857) in Patients with Amyotrophic Lateral Sclerosis (Colorado Convention Center | Exhibit Hall B-E) - Mar 8, 2024 - Abstract #AAN2024AAN_3126;
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Overall, the hexane fraction of HM and methanol fraction of PA displayed effective anti-aging activities, with additional anti-inflammatory effects. Utreloxastat is currently under evaluation in CARDINALS, a clinical trial in patients with ALS.
- | Journal: Integrated computational and experimental evaluation of phenolic constituents of Apricot fruit L. for antiqourum sensing, antibiofilm, antioxidant, and 15-lox inhibitory properties. (Pubmed Central) - Feb 12, 2024
It was therefore determined that compounds 1 and 3 had the highest biofilm inhibitory activity, whereas compounds 4 and 5 were potent 15-lipoxygenase inhibitors with potentially anti-inflammatory properties. Future investigations are suggested for the characterization and formulation development.
- | Journal: A game of networks: Do different lipids interact to orchestrate inflammatory homeostasis? (Pubmed Central) - Dec 27, 2023
Future investigations are suggested for the characterization and formulation development. In this issue of Cell Chemical Biology, Peltner et
- || Review, Journal: Dual COX-2/15-LOX inhibitors: A new avenue in the prevention of cancer. (Pubmed Central) - Oct 21, 2023
Various structural families of dual inhibitors are illustrated. This study discloses various structural families of dual 15-LOX/COX-2 inhibitors, thus pave the way to design potentially-active anticancer agents with balanced dual inhibition of these enzymes.
- | Journal: 12/15-lipoxygenase inhibition attenuates neuroinflammation by suppressing inflammasomes. (Pubmed Central) - Oct 12, 2023
These results suggest that 12/15-LOX inhibition suppresses ischemia-induced inflammation in the acute and subacute phases of stroke via suppressing inflammasome activation. Understanding the mechanisms underlying lipid peroxidation and its associated pathways, like inflammasome activation, may have broader implications for the treatment of stroke and other neurological diseases characterized by neuroinflammation.
- | Journal, IO biomarker: Investigating the Anti-tumor and Apoptosis-inducing Effects of Coumarin Derivatives as Potent 15-Lipoxygenase Inhibitors on PC-3 Prostate Cancer Cells. (Pubmed Central) - Aug 28, 2023
On the other hand, the cytotoxic effects of 8-IC might be due to the inhibition of other signaling pathways in PC-3 cells. However, further in vivo experiments are required to determine the exact mechanisms involved in the anticancer effects of these coumarin compounds.
- | Vincerinone (vatiquinone) / Sumitomo Pharma, PTC Therap
Preclinical, Journal: Absorption, Distribution, Metabolism and Excretion of C-Vatiquinone in Rats, Dogs and Human Subjects. (Pubmed Central) - Aug 8, 2023
22% dose).Following oral administration, vatiquinone was the dominant circulating component in rats and dogs but was minor in human subjects. There were no plasma metabolites that were more than 10% of total drug related exposures in all species.Following oral administration, vatiquinone was not detectable in urine but was the most prominent component in faeces in rats, dogs, and humans.
- | Journal: Polysaccharides and Bioactive Phenolics from Aconitum septentrionale Roots. (Pubmed Central) - Jun 20, 2023
Magnoflorine (8) and 2-[[2-(?-D-glucopyranosyloxy)-5-hydroxybenzoyl] amino]-5-hydroxy-, methyl ester (12) inhibited 15-lipoxygenase, and bracteanolide A (7) was a moderate inhibitor of xanthine oxidase. This study is the first to describe the diversity of phenolics and polysaccharides from A. septentrionale and their anti-inflammatory and anti-oxidant activities.
- | celecoxib oral / Generic mfg.
Journal: Synthesis of new multitarget-directed ligands containing thienopyrimidine nucleus for inhibition of 15-lipoxygenase, cyclooxygenases, and pro-inflammatory cytokines. (Pubmed Central) - Jun 2, 2023
This study is the first to describe the diversity of phenolics and polysaccharides from A. septentrionale and their anti-inflammatory and anti-oxidant activities. The ester 4 (SI
- Vincerinone (vatiquinone) / Sumitomo Pharma, PTC Therap
Baseline Demographics in MIT-E: Efficacy and Safety Study of Vatiquinone for the Treatment of Mitochondrial Disease Subjects with Refractory Seizure (Foyer 3B, 3rd Floor) - May 29, 2023 - Abstract #EPNS2023EPNS_756;
The ester 4 (SI The MIT-E study will provide data on the effect of vatiquinone on reduction in observable motor seizure frequency in subjects with genetically confirmed mitochondrial disease.
- | Preclinical, Journal: Investigations of p-tolyloxy-1,3,4-oxadiazole propionamides as soybean 15-lipoxygenase inhibitors in comforting with in (Pubmed Central) - Mar 25, 2023
It was found that compounds with more stabilized LUMO orbitals had significant biological activity. The work collectively supports steps taken forward in search for potential 'leads' as anti-inflammatory agents wherein compounds 7a, 7n, 7i, 7j possessed 'lead' like properties for further investigations.Communicated by Ramaswamy H. Sarma.
- | Vincerinone (vatiquinone) / Sumitomo Dainippon, PTC Therap, rosuvastatin / Generic mfg.
Journal: Clinical Drug-Drug Interaction Between Vatiquinone, a 15-Lipoxygenase Inhibitor, and Rosuvastatin, a Breast Cancer Resistance Protein Substrate. (Pubmed Central) - Mar 2, 2023
Mean rosuvastatin apparent elimination half-life was similar between treatment groups. These results demonstrate that vatiquinone has no clinically relevant effect on the pharmacokinetics of rosuvastatin.
- | Journal: Synthesis, Biological Evaluation, and Molecular Dynamics of Carbothioamides Derivatives as Carbonic Anhydrase II and 15-Lipoxygenase Inhibitors. (Pubmed Central) - Dec 24, 2022
Furthermore, MD simulation results confirmed that these ligands are stably bound to the two targets, while the binding energy further confirmed the inhibitory effects of the 3h compound. As these compounds may have a role in particular diseases, the reported compounds are of great relevance for future applications in the field of medicinal chemistry.
- || PTC857 / PTC Therap
P1 data, PK/PD data, Journal: First-in-Human Studies of Pharmacokinetics and Safety of Utreloxastat (PTC857), a Novel 15-Lipooxygenase Inhibitor for the Treatment of Amyotrophic Lateral Sclerosis. (Pubmed Central) - Dec 16, 2022
Utreloxastat showed no marked safety signal following single doses up to 1000 mg and multiple doses over 14 days of 500 mg once daily or 250 mg twice daily. The results support further development of utreloxastat for the treatment of patients with amyotrophic lateral sclerosis at a 250-mg twice-daily dose administered with food.
- Vincerinone (vatiquinone) / Sumitomo Dainippon, PTC Therap
MIT-E: Efficacy and Safety Study of Vatiquinone for the Treatment of Mitochondrial Disease (MD) Subjects with Refractory Epilepsy () - Nov 29, 2022 - Abstract #AES2022AES_697;
The results support further development of utreloxastat for the treatment of patients with amyotrophic lateral sclerosis at a 250-mg twice-daily dose administered with food. The MIT-E study will provide data on the effect of vatiquinone on reduction in observable motor seizure frequency in subjects with genetically confirmed MD.
- | Journal: Identification of Novel Arachidonic Acid 15-Lipoxygenase Inhibitors Based on the Bayesian Classifier Model and Computer-Aided High-Throughput Virtual Screening. (Pubmed Central) - Nov 25, 2022
The subsequent molecular dynamics simulations confirmed their stable binding to the targets. The findings indicated that the compounds exhibited excellent potential ALOX15 inhibitor capacity, thereby providing novel candidates for the treatment of inflammatory ischemia-related diseases caused by ferroptosis.
- RSL3 / Stanford University
CEPHARANTHINE ATTENUATES EARLY BRAIN INJURY AFTER SUBARACHNOID HEMORRHAGE IN MICE VIA INHIBITING 15-LIPOXYGENASE-1 MEDIATED MICROGLIA AND ENDOTHELIAL CELLS FERROPTOSIS (GALLERY) - Nov 7, 2022 - Abstract #WSC2022WSC_1142;
In summary, to the best of our knowledge, this is the first study demonstrating that ferroptosis occurred in the microglia and endothelium after SAH, and this process was facilitated by increased ALOX15 levels. More importantly, treatment with CEP could inhibit ferroptosis through downregulating the expression of ALOX15.
- | Preclinical, Journal: Evaluation of Major Constituents of Medicinally Important Plants for Anti-Inflammatory, Antidiabetic and AGEs Inhibiting Properties: In Vitro and Simulatory Evidence. (Pubmed Central) - Oct 21, 2022
Quercitrin (65%) and quercetin (62%) showed significant inhibition of 15-lipoxygenase. It was thus concluded that flavonoids and other polyphenols present in plant extracts can be effective in management of diabetes and allied co-morbidities.
- | Journal: Macrophages undergo a behavioural switch during wound healing in zebrafish. (Pubmed Central) - Oct 19, 2022
While inhibition of 15-lipoxygenase using PD146176 or Nordihydroguaiaretic acid (NDGA) decreases the switch from amoeboid to elongated shape, protectin D1 accelerates macrophage reverse migration and favours elongated morphologies. Altogether, our findings suggest that individual macrophages at the wound switch their phenotype leading to important changes in behaviour and shape to adapt to changing environment, and highlight the crucial role of lipid metabolism in the control of macrophage behaviour plasticity during inflammation in vivo.
- | Journal: Anti-Inflammatory, Anti-Diabetic, Anti-Oxidant and Cytotoxicity Assays of South African Herbal Teas and Bush Tea Blends. (Pubmed Central) - Aug 14, 2022
All of the tea samples showed anti-diabetic effects, although with less potency as compared to insulin. The current investigation supports the use of blended herbal teas, and the positive anti-inflammatory effect of special tea warrants further research.
- Effects of methanolic extracts of Mitragyna speciosa on the enzyme 15-lipoxygenase (Virtual-only (Zoom)) - Aug 9, 2022 - Abstract #ACSFall2022ACS_Fall_3639;
The preliminary results indicate all three Kratom species (White, Red & Green) inhibit 15-Lipoxygenase in the range of 75% to 90%. Details of this study and findings will be presented.
- | Journal: 4-Chlorophenyl-N-furfuryl-1,2,4-triazole Methylacetamides as Significant 15-Lipoxygenase Inhibitors: an Efficient Approach for Finding Lead Anti-inflammatory Compounds. (Pubmed Central) - Jun 22, 2022
ADME, in silico, and density functional theory studies supported the evidence as yet another class of triazoles with potential lead properties in search for anti-LOX compounds with a safe gastrointestinal safety profile for various inflammatory diseases. Further work is in progress on the synthesis of more derivatives in search for anti-inflammatory agents.
- | Preclinical, Journal: Targeting new N-furfurylated 4-chlorophenyl-1,2,4-triazolepropionamide hybrids as potential 15-lipoxygenase inhibitors supported with in vitro and in silico studies. (Pubmed Central) - Jun 15, 2022
Compounds 7a, 7f, 7d and 7e exhibited 65.58 ± 1.4%, 54.72 ± 1.3%, 58.52 ± 1.2% and 63.56 ± 1.4% blood mononuclear cells viability, respectively. Density functional theory and molecular docking studies further strengthened the studies of the synthesized compounds and these derivatives perceived to be potential 'lead' compounds in drug discovery as anti-LOX.Communicated by Ramaswamy H. Sarma.
- | Journal: Synthesis of novel hybrid pharmacophore of N-((4-sulfamoylphenyl)carbamothioyl)alkanamides as potent carbonic anhydrase-II and 15-lipoxygenase inhibitors. (Pubmed Central) - Jun 4, 2022
Molecular docking studies of most active compounds were carried out against bCA II as well as 15-LOX to rationalize the binding mode and interactions of compound in the active sites. Additionally, the pharmacokinetic properties of the compounds were predicted through computational tools, which reflect that these compounds possess acceptable pharmacokinetic profile and good drug-likeness.
- | RSL3 / Stanford University
Preclinical, Journal: Cepharanthine Attenuates Early Brain Injury after Subarachnoid Hemorrhage in Mice via Inhibiting 15-Lipoxygenase-1-Mediated Microglia and Endothelial Cell Ferroptosis. (Pubmed Central) - Apr 6, 2022
bEend.3 endothelial cells and BV2 microglial cells as well as RSL3 and hemin were used to simulate SAH in vitro...In summary, to the best of our knowledge, this is the first study demonstrating that ferroptosis occurred in the microglia and endothelium after SAH, and this process was facilitated by increased ALOX15 levels. More importantly, treatment with CEP could inhibit ferroptosis through downregulating the expression of ALOX15.
- | Journal: Design, synthesis, and structure-activity relationship study of O-prenylated 3-acetylcoumarins as potent inhibitors of soybean 15-lipoxygenase. (Pubmed Central) - Apr 5, 2022
The hydrophobic cavity of the enzyme was more effectively occupied by the farnesyl moiety of the potent inhibitor 12b rather than other derivatives. Also, with this pose of farnesyl chain in 7-farnesyloxy-3-acetylcoumarins, the acetyl group could be directed to the hydrophilic pocket in the active site.
- | Journal: Allylphenols as a new class of human 15-lipoxygenase-1 inhibitors. (Pubmed Central) - Mar 9, 2022
It was found that the electronic natures of allyl moiety and para substituents play the main role in radical scavenging activity and subsequently LOX inhibition potency of the synthetic inhibitors. Among the synthetic compounds, 2,6-diallyl-4-(hexyloxy)phenol (42) and 2,6-diallyl-4-aminophenol (47) showed the best results for LOX inhibition (IC = 0.88 and 0.80 μM, respectively).
- | Journal: Real-time imaging of asthmatic epithelial cells identifies migratory deficiencies under Type-2 conditions. (Pubmed Central) - Mar 4, 2022
Migration abnormalities contributed to markedly slower wound closure of IL-13 treated cells, which was modestly reversed by 15LO1 inhibition, suggesting its potential as an asthma therapeutic target. These novel methodologies offer new ways to dynamically study cell movements and identify contributing pathologic processes.
- | Preclinical, Journal: 15-Lipoxygenase Worsens Renal Fibrosis, Inflammation, and Metabolism in a Murine Model of Ureteral Obstruction. (Pubmed Central) - Feb 15, 2022
These novel methodologies offer new ways to dynamically study cell movements and identify contributing pathologic processes. 15-LO manipulation by genetic or pharmacologic means induces dynamic changes in the inflammatory microenvironment in the UUO-model and appears to be critical in the progression of UUO-induced fibrosis.
- Anti-Inflammatory effects of Salvia Apiana ethanol extracts by studying the inhibition of 15-lipoxygenase. (In-Person Room (Virtual Room)) - Jan 28, 2022 - Abstract #ACSSp2022ACS_Sp_13238;
The preliminary results indicate the percentage of inhibition of 62.21%(+/-7.54), n=4. Further research will be done with similar plant products.
- Effectiveness of herbal extracts as arachidonate 15-lipoxygenase inhibitors (Virtual Room (Marriott Marquis San Diego Marina)) - Jan 28, 2022 - Abstract #ACSSp2022ACS_Sp_10018;
At a final concentration of ~0.91 mg/mL the extracts inhibited the catalytic oxidation of arachidonic acid by lipoxygenase by 81%, 98%, and 95% respectively. Chemical constituents of each plant material will be determined by GC-MS and an exploration of possible active ingredients.
- | Journal: O-prenylated carbostyrils as a novel class of 15-lipoxygenase inhibitors: synthesis, characterization and inhibitory assessment. (Pubmed Central) - Jan 27, 2022
The results showed that position and length of the prenyl moiety play the important role in lipoxygenase inhibitory activity. Amongst all of the synthetic compounds (carbostyril and coumarin derivatives), 6-farnesyloxycoumarin and 8-farnesyloxycarbostyril demonstrated the best inhibitory activity by IC values of 2.1 µM and 0.53 µM respectively.
- | indomethacin / Generic mfg.
Journal: Protective role of resolvin D1, a pro-resolving lipid mediator, in nonsteroidal anti-inflammatory drug-induced small intestinal damage. (Pubmed Central) - Oct 22, 2021
Inhibition of the resolvin D1 receptor, lipoxin A4 receptor /formyl peptide receptor 2, by its specific inhibitors Boc-1 and WRW4 aggravated indomethacin-induced small intestinal damage. Collectively, these results indicate that resolvin D1 produced by 15-lipoxygenase contributes to mucoprotection against NSAID-induced small intestinal damage through its anti-inflammatory effect.
- VLX-1005 / Veralox Therap
[VIRTUAL] Inhibition of 12/15 Lipoxygenase (12/15 LOX) Improves Renal Recovery and Function Post Ischemia-Reperfusion in Male Spontaneous Hypertensive Rats (SHR) () - Oct 17, 2021 - Abstract #KIDNEYWEEK2021KIDNEY_WEEK_1137;
Pre-treatment of male SHR with ML355 reduced IR-induced lipid peroxidation (P IR*TxT =0.02) and ER stress (P IR*TxT =0.05), prevented IR-induced tubular damage (P IR*TxT =0.02) and tubular cell death (P IR*TxT =0.04), and improved renal function (Pcr: P IR*TxT =0.0067; BUN: P IR*TxT =0.042) compared to vehicle-treated IR males 7 days post-IR. Conclusion In conclusion, our data demonstrate that enhanced activation of 12/15-LOX contributes to impaired renal recovery post-IR via ER stress and cell death in male SHR.
- | Journal: Ethnopharmacology, biological activities and chemical compounds of Canarium strictum: An important resin-yielding medicinal tree in India. (Pubmed Central) - Sep 17, 2021
Triterpenoids and procyanidins are the major compounds in C. strictum resin and stem bark, respectively. The high content of triterpenoids might contribute to anti-inflammatory effects and give a rationale for the widespread usage of the resin in India.
- | itraconazole / Generic mfg.
Journal: Itraconazole Increases Resolvin E3 Concentration and 12/15-lipoxygenase Inhibitor Attenuates Itraconazole Cytotoxicity in Cervical Cancer Cells. (Pubmed Central) - Sep 15, 2021
The high content of triterpenoids might contribute to anti-inflammatory effects and give a rationale for the widespread usage of the resin in India. The metabolic pathway of SPMs, including resolving E3, could be proposed as an anticancer target of itraconazole.
- | Preclinical, Journal: Downregulation of autophagy by 12/15Lipoxygenase worsens the phenotype of an Alzheimer's disease mouse model with plaques, tangles, and memory impairments. (Pubmed Central) - May 15, 2021
Taken together our study supports the hypothesis that the 12/15LO enzymatic pathway by impairing neuronal autophagy plays a functional role in exacerbating AD-related neuropathologies and cognitive impairments. It provides further critical preclinical evidence to justify developing and testing new and selective 12/15LO inhibitors for AD treatment.
- | Journal: Phytochemical and Biological Activity Studies on Nasturtium officinale (Watercress) Microshoot Cultures Grown in RITA Temporary Immersion Systems. (Pubmed Central) - Apr 22, 2021
Moreover, all the studied extracts showed almost similar antibacterial and antifungal potential. Based on these findings, and due to the fact that the growth of in vitro microshoots is independent of environmental conditions and unaffected by environmental pollution, we propose that biomass that can be rapidly grown in RITA bioreactors can serve as an alternative source of bioactive compounds with valuable biological properties.
- | Journal: Design, synthesis, molecular modelling and biological evaluation of novel 3-(2-naphthyl)-1-phenyl-1H-pyrazole derivatives as potent antioxidants and 15-Lipoxygenase inhibitors. (Pubmed Central) - Dec 18, 2020
Catalase (CAT) activity, glutathione (GSH) and malondialdehyde (MDA) levels were assayed in liver of treated rats. Compounds 5b, 5c, and 6e showed significant in vivo antioxidant potentials compared to control group at dose of 100 mg/kg B.W. Molecular docking of compound 6a endorsed its proper binding at the active site pocket of the human 15-LOX which explains its potent antioxidant activity in comparison with standard ascorbic acid.
- | Journal: Synthesis, molecular properties, anti-inflammatory and anticancer activities of novel 3-hydroxyflavone derivatives. (Pubmed Central) - Sep 24, 2020
Molecule description was performed with DFT calculations, the drug likeness and bioactivity scores. The results exhibted that some compounds are in linear correlation with Lipinski's rule of five showing good drug likeness and bioactivity score for drug targets.
- | Journal: Design, synthesis, and SAR study of isopropoxy allylbenzene derivatives as 15-lipoxygenase inhibitors. (Pubmed Central) - Sep 23, 2020
Docking results showed that orientation of the amide and allyl moieties of the inhibitors in the active site pocket is the major factor in inhibitory potency variation. Based on the mentioned orientation, for cycloaliphatic amides, by enlargement of the amide moiety both inhibition potency and calculated binding energy increases.
- | Journal: Curcumin and LOXblock-1 ameliorate ischemia-reperfusion induced inflammation and acute kidney injury by suppressing the semaphorin-plexin pathway. (Pubmed Central) - Sep 1, 2020
Based on the mentioned orientation, for cycloaliphatic amides, by enlargement of the amide moiety both inhibition potency and calculated binding energy increases. The current study reveals the protective effects of Curcumin and LOXblock-1 on acute kidney injury by suppressing SEMA3A as a new biomarker.
- | Journal: Bioprospection of anti-inflammatory phytochemicals suggests rutaecarpine and quinine as promising 15-lipoxygenase inhibitors. (Pubmed Central) - Aug 15, 2020
Further, QUIN and RUT both did not show any inhibition against selected Gram-positive and Gram-negative bacterial species. Thus, based on our present findings, rutaecarpine and quinine may be suggested as promising 15-LOX inhibitor for the prevention of the atherosclerosis development.
- | Journal: A novel 15-Lipoxygenase-1 Inhibitor Protects Macrophages from Lipopolysaccharides-Induced Cytotoxicity. (Pubmed Central) - Jun 26, 2020
In vitro, this inhibitors protected cells from LPS-induced cell death, inhibiting NO formation and lipid peroxidation. Thus, we provide a novel 15-LOX-1 inhibitor that inhibits cellular NO production and lipid peroxidation, which set the stage for further exploration of these mechanisms.