NRF2 activator 
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  • ||||||||||  chloroquine phosphate / Generic mfg.
    Preclinical, Journal:  CDDO-Im ameliorates osteoarthritis and inhibits chondrocyte apoptosis in mice via enhancing Nrf2-dependent autophagy. (Pubmed Central) -  Jul 8, 2022   
    Moreover, we confirmed that CDDO-Im (1-20 nM) dose-dependently activated Nrf2 pathway in TNF-α-treated chondrocytes, and its chondroprotective and autophagy-enhancing effects were significantly diminished when Nrf2 signaling was blocked by Nrf2 inhibitor ML385 (20 μM) or siRNA-mediated Nrf2 knockdown. Together, our results demonstrate that CDDO-Im exhibits prominent chondroprotective and anti-OA activities owing to its Nrf2 activation and autophagy-enhancing properties, which might provide new insights into the strategies of OA clinical prevention and treatment.
  • ||||||||||  Journal:  Cyclo(-Phe-Phe) alleviates chick embryo liver injury via activating the Nrf2 pathway. (Pubmed Central) -  Jul 8, 2022   
    Mechanistically, CPP upregulated the mRNA and protein expression of heme oxyense-1 (HO-1) and NADPH quinone oxidoreductase 1 (NQO1) in vivo and in vitro, along with promoting the translocation of nuclear factor erythroid 2-related factor 2 (Nrf2) while inhibiting its degradation through binding with Kelch-like ECH-associated protein 1 (Keap1). In conclusion, this study proposes a potential peptide drug for the treatment of hepatic damage induced by oxidative stress and also unravels its mechanism of action.
  • ||||||||||  Journal:  Maackiain Prevents Amyloid-Beta-Induced Cellular Injury via Priming PKC-Nrf2 Pathway. (Pubmed Central) -  Jul 6, 2022   
    Moreover, calphostin C attenuated the antioxidant and anti-inflammatory capabilities of Maackiain in PC12 cells. Collectively, Maackiain promoted Nrf2 activation through the PKC signaling pathway, thus preventing PC12 cells from Aβ-induced oxidative stress and cell injury, suggesting that Maackiain is a potential drug for AD treatment.
  • ||||||||||  Journal:  Protecting Effect of Bacillus coagulans T242 on HT-29 Cells Against AAPH-Induced Oxidative Damage. (Pubmed Central) -  Jul 6, 2022   
    coagulans T242 positively regulated the expression of the nuclear factor erythroid 2-relatedfactor 2/Kelch-like ECH-associated protein-1 (Nrf2/Keap1) pathway-related proteins (Nrf2, Keap1, heine oxygenase-1 (HO-1)); increased antioxidant enzymes (glutathione peroxidase (GSH-Px), catalase (CAT), superoxide dismutase (SOD)); reduced the content of malondialdehyde (MDA) level; decreased the expression of inflammatory-related cytokines interleukin-6 (IL-6), interleukin-8 (IL-8), and tumor necrosis factor-α (TNF-α); and thus increased the survival rate in 2,2'-azobis (2-methylpropionamidine) dihydrochloride (AAPH)-damaged HT-29 cells. This study proved that B. coagulans T242 exerted antioxidative effects by quenching oxygen free radicals and activating the Nrf2 signaling pathway in HT-29 cells.
  • ||||||||||  Journal:  Cyclodextrin-mediated conjugation of macrophage and liposomes for treatment of atherosclerosis. (Pubmed Central) -  Jul 3, 2022   
    In addition to anti-inflammation effects of QT, MP-QT-NP efficiently regresses atherosclerotic plaques from both murine aorta and human carotid arteries via CD-MP mediated cholesterol efflux, due to the binding of cholesterol by excess membrane β-CD. Transcriptome analysis of atherosclerotic murine aorta and human carotid tissues reveal that MP-QT-NP may activate NRF2 pathway to inhibit plaque inflammation, and simultaneously upregulate liver X receptor to promote cholesterol efflux.
  • ||||||||||  Journal:  Stretch Causes Cell Stress and the Downregulation of Nrf2 in Primary Amnion Cells. (Pubmed Central) -  Jul 2, 2022   
    This work supports stretch as a key modulator of cellular stress and inflammation in the fetal membranes. Our results showed that the modulation of the antioxidant response pathway in the fetal membranes through Nrf2 activation may be a viable approach to improve outcomes in pregnancy.
  • ||||||||||  Venclexta (venetoclax) / Roche, AbbVie
    Journal:  Arsenic Trioxide and Venetoclax Synergize against AML Progenitors by ROS Induction and Inhibition of Nrf2 Activation. (Pubmed Central) -  Jul 2, 2022   
    Using metabolic assays and electron microscopy, we found that the ATO+VEN combination decreased mitochondrial membrane potential, mitochondria size, fatty acid oxidation and oxidative phosphorylation, all of which enhanced apoptosis of LSCs derived from both VEN-sensitive and VEN-resistant AML primary cells. Our results indicate that ATO and VEN cooperate in inducing apoptosis of LSCs through potentiation of ROS induction, suggesting ATO+VEN is a promising regimen for treatment of VEN-sensitive and -resistant AML.
  • ||||||||||  doxorubicin hydrochloride / Generic mfg.
    Journal:  High Levels of Hyaluronic Acid Synthase-2 Mediate NRF2-Driven Chemoresistance in Breast Cancer Cells. (Pubmed Central) -  Jul 1, 2022   
    Herein, we demonstrate that HA production was increased in doxorubicin-resistant breast cancer MCF7 cells (MCF7-DR) via the upregulation of HA synthase-2 (HAS2)...In addition, high HAS2 mRNA levels are associated with increased NRF2 signaling and poor clinical outcome in breast cancer patients. Collectively, these indicate that HAS2 elevation contributes to chemoresistance and sphere formation capacity of drug-resistant MCF7 cells by activating CD44/NRF2 signaling, suggesting a potential benefit of HAS2 inhibition.
  • ||||||||||  Journal:  Phloretin inhibits glucose transport and reduces inflammation in human retinal pigment epithelial cells. (Pubmed Central) -  Jul 1, 2022   
    Subsequent studies revealed that Nrf2, but not the inhibition of glucose uptake or JNK phosphorylation, was the main pathway of phloretin's anti-inflammatory activities. Phloretin was robustly anti-inflammatory in RPE cells and reduced IL-8 secretion via activation of Nrf2 but the evaluation of its potential in the treatment or prevention of AMD requires further studies.
  • ||||||||||  Preclinical, Journal:  Role of Nrf2 Nucleus Translocation in Beauvericin-Induced Cell Damage in Rat Hepatocytes. (Pubmed Central) -  Jun 30, 2022   
    Furthermore, ML385, an Nrf2 inhibitor, partially ameliorated BEA-induced cell injury while CDDO, an Nrf2 activator, aggravated liver damage. The present study emphasizes the role of Nrf2 nuclear translocation in BEA-induced oxidative stress associated with the hepatotoxic nature of BEA.
  • ||||||||||  Journal:  Identification of Nrf2 activators from the roots of Valeriana officinalis. (Pubmed Central) -  Jun 29, 2022   
    This study provides evidence that four valepotriates from the roots of V. officinalis are activators of Nrf2-mediated antioxidant and detoxification pathways. Our data might expand the medical use of this plant beyond its current application as a sleep aid.
  • ||||||||||  acetylcysteine solution / Generic mfg.
    Counter-regulation of thymosin beta-4 expression and primary cilium formation by nuclear factor (erythroid-derived 2)-like 2 for HeLa cervical cancer cell survival (Poster Area) -  Jun 28, 2022 - Abstract #EACR2022EACR_936;    
    N-acetylcysteine inhibited ROS production following H 2 O 2 treatment or SD, which also decreased PC formation and TB4 transcription...Nrf2 knockdown via expression of Tet-On shNrf2 enhanced ROS production, leading to increased PC formation and decreased TB4 expression; these effects were counteracted by Nrf2 overexpression. Conclusion Our data demonstrate that Nrf2 counter-regulates TB expression and PC formation for CC survival under conditions of SD, suggesting cervical CC survival could be upregulated by PC formation via Nrf2 activation and TB4 expression.
  • ||||||||||  bardoxolone methyl (RTA 402) / Kyowa Kirin, Reata
    Review, Journal:  Nrf2 Activation in Chronic Kidney Disease: Promises and Pitfalls. (Pubmed Central) -  Jun 25, 2022   
    Nrf2 repression relates to high uremic toxin and NF-κB concentrations, and may be related to Kelch-like ECH-associated protein 1 (Keap1)-independent Nrf2 degradation. Furthermore, we review the effects of pharmacological Nrf2 activation by bardoxolone methyl, curcumin, and resveratrol in human CKD and outline strategies for how to adapt future Nrf2-targeted therapies to the requirements of patients with CKD.
  • ||||||||||  acetylcysteine solution / Generic mfg.
    Review, Journal:  Antioxidant Therapy in Cancer: Rationale and Progress. (Pubmed Central) -  Jun 25, 2022   
    Here, we review the rationale for, and recent advances in, pre-clinical and clinical research on antioxidant therapy in cancer, including targeting ROS with nonenzymatic antioxidants, such as NRF2 activators, vitamins, N-acetylcysteine and GSH esters, or targeting ROS with enzymatic antioxidants, such as NOX inhibitors and SOD mimics. In addition, we will offer insights into prospective therapeutic options for improving the effectiveness of antioxidant therapy, which may expand its applications in clinical cancer treatment.
  • ||||||||||  cisplatin / Generic mfg.
    Preclinical, Journal:  Selenium Status in Diet Affects Nephrotoxicity Induced by Cisplatin in Mice. (Pubmed Central) -  Jun 25, 2022   
    Results showed that feeding with a selenium-deficient diet sensitize the mice to cisplatin-induced damage, whereas selenium supplementation increased the activities of selenoenzymes TrxR and glutathione peroxidase (GPx), changed the renal cellular redox environment to a reduced state, and exhibited protective effects. These results demonstrated the correlation of selenoenzymes with cisplatin-induced side effects and provided a basis for the potential approach to alleviate cisplatin-induced renal injury.
  • ||||||||||  acetylcysteine solution / Generic mfg.
    Targeting Lung Adenocarcinoma Cells with a Novel Disulfide Reductase Inhibitor (Exhibit Hall - Hall B) -  Jun 24, 2022 - Abstract #IASLCWCLC2022IASLC_WCLC_958;    
    We are currently investigating why non-responsive cells are less dependent on the glutathione and thioredoxin pathways and how oncogenic transformation, and the inherent oxidative stress that coincides, confer sensitization to dual disulfide reductase pathway inhibition. Through this investigation, we aim to use LCS3 as a tool compound to characterize a cancer dependency that can be exploited for the benefit of lung cancer patients with advanced tumors, for whom treatment is urgently needed.
  • ||||||||||  Journal:  Maackiain protects against sepsis via activating AMPK/Nrf2/HO-1 pathway. (Pubmed Central) -  Jun 22, 2022   
    Moreover, inhibition of AMPK/Nrf2 axis abrogated the anti-inflammatory and anti-oxidant effects of Maackiain both in vitro and in vivo. Collectively, our study indicates that Maackiain treatment inhibits inflammatory response and oxidative stress via activation of AMPK/Nrf2/HO-1 pathway, thus exerting a protective effect against sepsis, providing an alternative option for sepsis prevention.