NRF2 activator 
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  • ||||||||||  Journal:  Flavonolignans and biflavonoids from Cephalotaxus oliveri exert neuroprotective effect via Nrf2/ARE pathway. (Pubmed Central) -  Sep 23, 2022   
    All six undescribed compounds were effective to some degree, and umcephabiflovin B, apigenin 5-O-α-L-rhamnopyranosyl-(1 → 2)-6″-acetyl-β-D-glucopyranoside, and apigenin 7-O-β-D-glucoside exhibited good neuroprotective activity. Umcephabiflovin B protected SH-SY5Y cells against HO-induced neurotoxicity by repressing oxidative stress and apoptosis and by activating the nuclear factor erythroid 2-related factor 2 (Nrf2)/antioxidant-response element (ARE) pathway.
  • ||||||||||  metformin / Generic mfg.
    Preclinical, Journal:  Effects of Rosa roxburghii Tratt glycosides and quercetin on D-galactose-induced aging mice model. (Pubmed Central) -  Sep 22, 2022   
    To investigate the effects of RRT (Rosa roxburghii Tratt) glucosides and quercetin on oxidative stress and chronic inflammation in D-galactose-induced aging mice, 90 mice (8 weeks old) were randomly divided into the normal group (NC), aging model group (D-gal), isoquercitrin group (D-gal+isoquercitrin), quercitrin group (D-gal+quercitrin), quercetin group (D-gal+quercetin) and positive control group (D-gal+Metformin)...RRT glycosides and quercetin were found to protect organ atrophy, liver, and brain tissue in aging mice by regulating oxidative stress and chronic inflammation. It served as the theoretical foundation for the investigation of Rosa roxburghii Tratt as a health product and pharmaceutical raw material.
  • ||||||||||  Preclinical, Journal:  Puffball spores improve wound healing in a diabetic rat model. (Pubmed Central) -  Sep 21, 2022   
    As indicated by wound and serum histology and biochemical analyses, the puffball spores accelerated wound healing by activating Akt/Nrf2 signaling and promoting the expression of its downstream antioxidant genes, markedly stimulating antioxidant activity and enhanceing angiogenesis and collagen deposition. Our findings showed that puffball spores could accelerate diabetic wound healing, enhance antioxidant ability, promote the expression of vascular markers, and suppress inflammation, thus providing a theoretical basis for the treatment of diabetic and refractory wounds.
  • ||||||||||  Journal:  Understanding the role of NRF2 signalling in cancer. (Pubmed Central) -  Sep 20, 2022   
    To decipher the role of NRF2 in tumor formation and progression, large-scale genomic and transcriptomic studies are required to correlate the clinical outcomes with the activity of the NRF2 expression system. This review is an attempt to give insights into the understanding of the role of NRF2 in cancer.
  • ||||||||||  erastin - Whitehead Institute for Biomedical Research, Dana / Farber Cancer Institute, Columbia University, Prolexys
    Journal:  Quercetin Protects against MPP/MPTP-Induced Dopaminergic Neuron Death in Parkinson's Disease by Inhibiting Ferroptosis. (Pubmed Central) -  Sep 20, 2022   
    In this study, we investigated the potential antiferroptotic effects of QCT in cellular models established using specific ferroptosis inducers (Erastin and RSL-3) and MPP...In conclusion, these results demonstrate that ferroptosis is involved in MPP/MPTP-induced PD, and QCT inhibits ferroptosis by activating the Nrf2 protein. Therefore, QCT is a potential agent for preventing the loss of dopaminergic neurons by targeting ferroptosis.
  • ||||||||||  sirolimus / Generic mfg.
    Journal:  Low-dose rapamycin prevents Ang-II-induced toxicity in Leydig cells and testicular dysfunction in hypertensive SHR model. (Pubmed Central) -  Sep 20, 2022   
    Further, rapamycin curbs mitochondrial superoxide generation and depleted mitochondrial membrane potential induced by Ang II through activation of Nrf2-mediated Gpx4 and superoxide dismutase 2 expression. Our results revealed the involvement of ACE2, AT1R, AT2R, PKAc, and oxidative stress in Ang-II-induced testicular toxicity, suggesting low-dose rapamycin could be a potential therapeutic candidate to attenuate testicular toxicity.
  • ||||||||||  tamoxifen / Generic mfg.
    Journal:  Selective Elimination of NRF2-Activated Cells by Competition with Neighboring Cells in the Esophageal Epithelium. (Pubmed Central) -  Sep 20, 2022   
    These results provide insight into the molecular alterations in the epidermis of AD patients and identify potential targets for pharmaceutical intervention. Constitutive NRF2 activation promotes the selective elimination of epithelial cells via cell competition, but this competition induces DNA damage in neighboring KEAP1-normal cells, which predisposes them to chemical-induced ESCC.
  • ||||||||||  RRx-001 / EpicentRx, AiTan (rivoceranib) / HLB Bio Group, erastin - Whitehead Institute for Biomedical Research, Dana / Farber Cancer Institute, Columbia University, Prolexys
    Review, Journal:  Natural and synthetic compounds in Ovarian Cancer: A focus on NRF2/KEAP1 pathway. (Pubmed Central) -  Sep 14, 2022   
    In this review we analyzed the current literature regarding the role of natural and synthetic compounds in modulating NRF2/KEAP1 (Kelch Like ECH Associated Protein 1) pathway in in vitro models of ovarian cancer. In particular, we reported how these compounds can modulate chemotherapy response.
  • ||||||||||  hyoscine butylbromide oral / Generic mfg.
    Journal:  AKR1C1 Protects Corneal Epithelial Cells Against Oxidative Stress-Mediated Ferroptosis in Dry Eye. (Pubmed Central) -  Sep 14, 2022   
    C57BL/6 mice were injected with scopolamine subcutaneously and exposed to desiccating stress to establish a DED mouse model...The expression of AKR1C1 is triggered by NRF2 to decrease ferroptosis-induced cell damage and inflammation in HCECs. These findings may provide potential makers targeting ferroptosis and AKR1C1 for DED therapy.
  • ||||||||||  Journal:  Nrf2 Downregulation Contributes to Epithelial-to-Mesenchymal Transition in Helicobacter pylori-Infected Cells. (Pubmed Central) -  Sep 13, 2022   
    Findings from this study will inform on the optimal dose/schedule and further confirm previously shown efficacy and safety of sapanisertib in patients with metastatic R/R NFE2L2-mutated sqNSCLC and evaluate its activity in NFE2L2-WT sqNSCLC. Our work supports the hypothesis that Nrf2 downregulation upon H. pylori infection participates in EMT, one of the most important events in gastric carcinogenesis.
  • ||||||||||  Preclinical, Journal, IO biomarker:  Protective effect and mechanism of cannabidiol on myocardial injury in exhaustive exercise training mice. (Pubmed Central) -  Sep 12, 2022   
    Molecular docking results also confirmed that CBD had a good binding effect with Keap1/Nrf2/HO-1 signaling pathway proteins. In conclusion, the protective mechanism of CBD on myocardial injury in exhaustive exercise training mice may be to activate Keap1/Nrf2/HO-1 signaling pathway, and then exert anti-inflammatory, anti-apoptosis and inhibition of oxidative stress.
  • ||||||||||  Preclinical, Journal, IO biomarker:  Humanin ameliorates late-onset hypogonadism in aged male rats. (Pubmed Central) -  Sep 10, 2022   
    This study highlights the role of Keap1 in Nrf2 activation under shear stress and indicates that activation of Nrf2 may be deleterious in ECs in the context of acute haemodynamic injury. Humanin might be a promising therapeutic modality in late-onset hypogonadism as it ameliorated some age-related testicular and hormonal adverse effects.
  • ||||||||||  Journal:  AMPK and NRF2: Interactive players in the same team for cellular homeostasis? (Pubmed Central) -  Sep 10, 2022   
    Due to observed overlapping cellular responses upon AMPK or NRF2 activation and common stressors impinging on both AMPK and NRF2 signaling, it is plausible to assume that AMPK and NRF2 signaling may interdepend and cooperate to readjust cellular homeostasis. After a short introduction of the two players this narrative review paints the current picture on how AMPK and NRF2 signaling might interact on the molecular level, and highlights their possible crosstalk in selected examples of pathophysiology or bioactivity of drugs and phytochemicals.
  • ||||||||||  Journal:  Pros and cons of NRF2 activation as adjunctive therapy in rheumatoid arthritis. (Pubmed Central) -  Sep 10, 2022   
    From another perspective, the review presents how NRF2 activation would be decreasing the efficacy of synthetic anti-rheumatic drugs by increasing drug efflux. Future perspectives regarding pharmacologic NRF2 activation in RA are finally proposed.