NRF2 activator 
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  • ||||||||||  Journal:  NRF2-ARE signaling is responsive to haloacetonitrile-induced oxidative stress in human keratinocytes. (Pubmed Central) -  Aug 6, 2022   
    Additionally, knockdown of NRF2 by lentiviral shRNAs sensitized the HaCaT cells to HANs-induced cytotoxicity, emphasizing a protective role of NRF2 against the cytotoxicity of HANs. These results indicate that HANs cause oxidative stress and activate NRF2-ARE-mediated antioxidant response, which in turn protects the cells from HANs-induced cytotoxicity, highlighting that NRF2-ARE activity could be a sensitive indicator to identify and characterize the oxidative stress induced by HANs and other environmental pollutants.
  • ||||||||||  Journal:  Targeting clock-controlled gene Nrf2 ameliorates inflammation-induced intervertebral disc degeneration. (Pubmed Central) -  Aug 6, 2022   
    These results indicate that HANs cause oxidative stress and activate NRF2-ARE-mediated antioxidant response, which in turn protects the cells from HANs-induced cytotoxicity, highlighting that NRF2-ARE activity could be a sensitive indicator to identify and characterize the oxidative stress induced by HANs and other environmental pollutants. Taken together, our study extends the relationship between peripheral clock and IVD homeostasis and provides a potential therapeutic method for the prevention and recovery of IDD by targeting the clock-controlled gene Nrf2.
  • ||||||||||  Preclinical, Journal:  Premna microphylla Turcz pectin protected UVB-induced skin aging in BALB/c-nu mice via Nrf2 pathway. (Pubmed Central) -  Aug 5, 2022   
    In contrast, application of PMTP-containing cream on mice skin decreased the protein levels of nuclear factor-kappa B (NF-κB), inhibitor kappa B kinase β (IKKβ), and cyclooxygenase-2 (COX-2), and pro-inflammatory cytokines. Taken togethmier, these findings suggest that PMTP might protect UVB-induced skin aging via activating Nrf2 pathway and suppressing NF-κB pathway.
  • ||||||||||  Xenical (orlistat) / Roche, GSK
    Preclinical, Journal, IO biomarker:  Bee bread attenuates the progression of atherosclerosis by activating Nrf2/Keap1 and modulating TNF-α/NF-κβ-associated mast cell migration and a mitochondrial-dependent apoptotic pathway in the obese rat model. (Pubmed Central) -  Aug 5, 2022   
    After 6 weeks, obese rats that received the HFD were treated either with distilled water (Ob group), bee bread at 0.5 g per kg per day (Ob + Bb group), or orlistat at 10 mg per kg per day (Ob + Or group) concomitant with the HFD for another 6 weeks...We have demonstrated that the treatment with bee bread attenuates the progression of atherosclerosis through its inhibition of vascular oxidative stress, and retardation of inflammatory reaction and apoptosis in obese rats, indicating its potential therapeutic targets for obesity-related vascular diseases. This could be partly attributed to the components of vitamins such as vitamins A, C and E that are present in bee bread, which need further study for the exact molecular mechanism of action.
  • ||||||||||  paracetamol / Generic mfg.
    Journal, IO biomarker:  Protective Effect of Fresh/Dry Dandelion Extracts on APAP-Overdose-Induced Acute Liver Injury. (Pubmed Central) -  Aug 4, 2022   
    The mechanism of its effect may be related to the activation of the Nrf2/HO-1/NQO1 antioxidant pathway in vivo of the CHD mice. FDJ pretreatment protects against APAP-induced hepatic injury by activating the Nrf-2/HO-1 pathway and inhibition of the intrinsic apoptosis pathway, and the effect of fresh dandelion extracts was superior to dried dandelion extracts in APAP hepatotoxicity model mice.
  • ||||||||||  Journal:  SARS-CoV-2 virus NSP14 Impairs NRF2/HMOX1 activation by targeting Sirtuin 1. (Pubmed Central) -  Aug 4, 2022   
    Furthermore, both genetic and pharmaceutical evidence corroborated the novel antiviral activity of SIRT1 against SARS-CoV-2. Therefore, our findings reveal a novel mechanism by which SARS-CoV-2 dysregulates the host antioxidant defense system and emphasize the vital role played by the SIRT1/NRF2 axis in host defense against SARS-CoV-2.
  • ||||||||||  methotrexate / Generic mfg.
    Journal:  Role of Nrf2 in Methotrexate-Induced Epithelial-Mesenchymal Transition in Alveolar A549 Cells. (Pubmed Central) -  Aug 3, 2022   
    Finally, in Nrf2 knockdown cells, the MTX-induced enhancement of α-SMA mRNA/protein expression was not observed, indicating that downregulation of Nrf2 may play a critical role in the MTX-induced EMT in A549 cells. These results suggest that Nrf2-regulated transcriptional activity would be associated with the MTX-induced EMT induction.
  • ||||||||||  Journal:  Antidepressant Mechanism of Kaixinsan and Its Active Compounds Based on Upregulation of Antioxidant Thioredoxin. (Pubmed Central) -  Aug 3, 2022   
    In the HO induced SH-SY5Y cell damage model, this showed kaempferol and ginsenoside rh2 could enhance the activity of the Trx system by upregulation of AKT1 to activate Nrf2 in vitro. Taken together, by comprehensive systems pharmacology approach analysis, we found that KXS and its active compounds might exhibit antioxidant effects by stimulating the AKT1/Nrf2 pathway in the treatment of depression, which might shed new light on innovative therapeutic tactics for the new aspects for depression in traditional Chinese medicine in future studies.
  • ||||||||||  Review, Journal:  The Role of Organosulfur Compounds as Nrf2 Activators and Their Antioxidant Effects. (Pubmed Central) -  Jul 29, 2022   
    Although some individual organosulfur compounds have been reported as Nrf2 activators, there are no papers with a collective analysis of these Nrf2-activating organosulfur compounds which may help to broaden the knowledge of their therapeutic potentials and motivate further research. In line with this fact, for the first time, this review article provides collective and comprehensive information on Nrf2-activating organosulfur compounds and their therapeutic effects against oxidative stress, thereby enriching the chemical and pharmacological diversity of Nrf2 activators.
  • ||||||||||  ALZ002 / AnnJi Pharma, omaveloxolone (RTA 408) / Reata
    Preclinical, Journal:  In Vitro Efficacy and Molecular Mechanism of Curcumin Analog in Pathological Regulation of Spinocerebellar Ataxia Type 3. (Pubmed Central) -  Jul 29, 2022   
    Unlike other nuclear factor erythroid-2-related factor 2 (Nrf2) activators, the mechanism of action of curcumin analog, ASC-JM17 (JM17), in regulating oxidative homeostasis remains unknown...Presently, we compared actions of JM17 with those of known Nrf2 activators, omaveloxolone (RTA-408) and dimethyl fumarate (DMF), using human neuroblastoma SK-N-SH cells with stable transfection of full-length ataxin-3 protein with 78 CAG repeats (MJD78) to clarify the resulting pathological mechanism by assaying mitochondrial function, mutant ataxin-3 protein toxicity, and oxidative stress...It showed that activation of Nrf2 in response to ROS generated in mitochondria could play an import role in the benefit of JM17. This study presents the diversified regulation of JM17 in a pathological process and helped develop more effective therapeutic strategies for SCA3.
  • ||||||||||  Review, Journal:  The Role of KEAP1-NRF2 System in Atopic Dermatitis and Psoriasis. (Pubmed Central) -  Jul 29, 2022   
    Atopic dermatitis (AD) and psoriasis are two common chronic inflammatory skin diseases caused by a defective skin barrier, dysregulated immune responses, genetic predispositions, and environmental factors. This review focuses on the role of the KEAP1-NRF2 system in the pathophysiology of AD and psoriasis and the therapeutic approaches that utilize this system.
  • ||||||||||  GYY4137 / National University of Singapore
    Journal:  Hydrogen Sulfide Donor GYY4137 Rescues NRF2 Activation in Respiratory Syncytial Virus Infection. (Pubmed Central) -  Jul 29, 2022   
    We found that treatment with the HS donor GYY4137 significantly increased NRF2 levels and AOEs gene expression by decreasing KEAP1 levels, and by modulating pathways involved in RSV-induced NRF2 degradation, such as NRF2 ubiquitination, and promyelocytic leukemia (PML) protein levels. These results suggest that the administration of exogenous HS can positively impact the altered redox balance associated with RSV infection, which represents an important determinant of RSV-induced lung disease.
  • ||||||||||  Review, Journal:  The Therapeutic Potential of Carnosine as an Antidote against Drug-Induced Cardiotoxicity and Neurotoxicity: Focus on Nrf2 Pathway. (Pubmed Central) -  Jul 29, 2022   
    Different drug classes such as antineoplastic drugs (anthracyclines, cyclophosphamide, 5-fluorouracil, taxanes, tyrosine kinase inhibitors), antiretroviral drugs, antipsychotic, and immunosuppressant drugs are known to induce cardiotoxic and neurotoxic effects...Cardiotoxic drugs, such as the anthracycline doxorubicin, or neurotoxic drugs, such as paclitaxel, suppress or impair the Nrf2 pathway, whereas the rescue of this pathway counteracts both the oxidative stress and inflammation that are related to drug-induced cardiotoxicity and neurotoxicity...Interestingly, carnosine (β-alanyl-l-histidine), an endogenous dipeptide that is characterized by strong antioxidant, anti-inflammatory, and neuroprotective properties is able to rescue/activate the Nrf2 pathway, as demonstrated by different preclinical studies and preliminary clinical evidence. Starting from these new data, in the present review, we examined the evidence on the therapeutic potential of carnosine as an endogenous antidote that is able to rescue the Nrf2 pathway and then counteract drug-induced cardiotoxicity and neurotoxicity.
  • ||||||||||  Review, Journal:  Chalcones as Potential Ligands for the Treatment of Parkinson's Disease. (Pubmed Central) -  Jul 29, 2022   
    Chalcones have been described as promising enzyme inhibitors (MAO B, COMT, AChE), α-synuclein imaging probes, showing anti-neuroinflammatory activity (inhibition of iNOS or activation of Nrf2 signaling), as well as antagonists of adenosine A and/or A receptors. This review focused on the structure-activity relationships of these compounds to determine how a particular substituent or its position in the chalcone ring(s) (ring A and/or B) affects biological activity.
  • ||||||||||  Journal:  Hispolon alleviates oxidative damage by stimulating the Nrf2 signaling pathway in PC12 cells. (Pubmed Central) -  Jul 28, 2022   
    However, the protective effect of His on PC12 cells was easily terminated by Nrf2 knockdown, demonstrating that Nrf2 is a critical component in this cytoprotective process. Taken together, our study showed that His was not only an effective activator of Nrf2 but also a promising candidate for ND treatment.
  • ||||||||||  Journal:  Activation of the JNKs/ATM-p53 axis is indispensable for the cytoprotection of dermal fibroblasts exposed to UVB radiation. (Pubmed Central) -  Jul 28, 2022   
    Although UVB radiation results in intense and prolonged increase of intracellular ROS levels, classical anti-oxidants, such as Trolox, are unable to affect Akt, JNKs, or p53 phosphorylation and to reverse the loss of fibroblasts' viability. Collectively, here we provide evidence that the main viability-regulating UVB-triggered biochemical pathways act synergistically towards the protection of human dermal fibroblasts, with EGFR/Akt and Nrf2 serving as auxiliary anti-apoptotic machineries, while JNKs/ATM-p53 activation and interplay being overriding and indispensable for the perpetuation of cellular defense and the maintenance of cell viability.
  • ||||||||||  midazolam hydrochloride / Generic mfg.
    Journal:  Midazolam Ameliorates Acute Liver Injury Induced by Carbon Tetrachloride via Enhancing Nrf2 Signaling Pathway. (Pubmed Central) -  Jul 27, 2022   
    Further investigations showed that midazolam could strongly up-regulate the expression of both Nrf2 and HO-1 in the mice liver, accompanied by increasing of the levels of antioxidant enzyme SOD and reducing the production of MDA, as well as reducing the pro-inflammatory cytokines (IL-6, TNF-α) secretion. Collectively, our results clearly demonstrate that midazolam can ameliorate CCl-induced acute liver injury and oxidative stress via activating the Nrf2 signaling pathway.
  • ||||||||||  Journal:  Senescence Connects Autophagy Deficiency to Inflammation and Tumor Progression in the Liver. (Pubmed Central) -  Jul 27, 2022   
    Collectively, our results clearly demonstrate that midazolam can ameliorate CCl-induced acute liver injury and oxidative stress via activating the Nrf2 signaling pathway. These results provide the insight that hepatic senescence can occur early in the disease process, triggers inflammation and is enhanced by inflammation, and has long-term effects on liver injury and tumor progression.
  • ||||||||||  Preclinical, Journal:  The β-TrCP-Mediated Pathway Cooperates with the Keap1-Mediated Pathway in Nrf2 Degradation In Vivo. (Pubmed Central) -  Jul 27, 2022   
    These increases in Nrf2 activity induced by the Nrf2 mutation caused severe hyperplasia and hyperkeratosis in the esophageal epithelium but did not cause abnormalities in the other tissues/organs examined. These results indicate that the β-TrCP-mediated pathway cooperates with the Keap1-mediated pathway to regulate Nrf2 activity, which is apparent when the Keap1-mediated pathway is profoundly suppressed.
  • ||||||||||  Preclinical, Journal:  Anti-fatigue and anti-oxidant effects of curcumin supplementation in exhaustive swimming mice via Nrf2/Keap1 signal pathway. (Pubmed Central) -  Jul 27, 2022   
    Curcumin alleviated exercise-induced oxidative stress and significantly enhanced the activities of superoxide dismutase, catalase and glutathione peroxidase by activating the Nrf2 signaling. These findings indicated that curcumin supplementation exerted remarkable anti-oxidant and anti-fatigue effects in mice, providing additional evidence supporting the use of curcumin as functional food, especially by those engaged in sports-related activities.