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- [VIRTUAL] OPTIMIZATION OF VINYL SULFONE DERIVATIVES AS POTENT NUCLEAR FACTOR ERYTHROID 2‑RELATED FACTOR 2 (NRF2) ACTIVATORS FOR PARKINSON’S DISEASE THERAPY (EXHIBITION HALL) - Jan 6, 2020 - Abstract #AATADPD2020AAT_ADPD_411;
In MPTP-induced PD mice, treatment with 17e was neuroprotective, alleviating loss of DAergic neurons and preventing microglia activation. Conclusions In conclusion, 17e represents a novel therapeutic agent with potential for treating PD.
- | Clinical, Review, Journal: Activators and Inhibitors of NRF2: A Review of Their Potential for Clinical Development. (Pubmed Central) - Jan 5, 2020
This review describes the electrophilic and nonelectrophilic NRF2 activators with clinical projection in various chronic diseases. We also analyze the status of NRF2 inhibitors, which at this time provide proof of concept for blocking NRF2 activity in cancer therapy.
- | Journal: Recent Advances of Natural Polyphenols Activators for Keap1-Nrf2 Signaling Pathway. (Pubmed Central) - Jan 1, 2020
In this view, we summarize the research status of natural polyphenols that have been found with apparent Nrf2 activation and their action modes. On the whole, this review may guide the design of novel Keap1-Nrf2 activator.
- | Preclinical, Journal: Protection against HEMA-Induced Mitochondrial Injury In Vitro by Nrf2 Activation. (Pubmed Central) - Dec 23, 2019
This protective effect on mitochondria could be related to peroxisome proliferator-activated receptor γ coactivator 1α (PGC1α)/nuclear respiratory factor 1 (NRF1) pathway. These results contribute to the understanding of the function of Nrf2 and the development of novel therapies to counteract the adverse effects of dental resin monomers.
- | Journal: HDAC5 Catalytic Activity Suppresses Cardiomyocyte Oxidative Stress and NRF2 Target Gene Expression. (Pubmed Central) - Dec 20, 2019
These results contribute to the understanding of the function of Nrf2 and the development of novel therapies to counteract the adverse effects of dental resin monomers. Histone deacetylase 5 (HDAC5) and HDAC9 are class IIa HDACs that function as signal-responsive repressors of the epigenetic program for pathological cardiomyocyte hypertrophy. The conserved deacetylase domains of HDAC5 and HDAC9 are not required for inhibition of cardiac hypertrophy. Thus, the biological function of class IIa HDAC catalytic activity in the heart remains unknown. Here, we demonstrate that catalytic activity of HDAC5, but not HDAC9, suppresses mitochondrial reactive oxygen species (ROS) generation and subsequent induction of NF-E2 Related Factor 2 (NRF2)-dependent antioxidant gene expression in cardiomyocytes. Treatment of cardiomyocytes with TMP195 or TMP269, which are selective class IIa HDAC inhibitors, or shRNA-mediated knockdown of HDAC5 but not HDAC9, leads to stimulation of NRF2-mediated transcription in a ROS-dependent manner. Conversely, ectopic expression of catalytically active HDAC5 decreases cardiomyocyte oxidative stress and represses NRF2 activation. These findings establish a role for the catalytic domain of HDAC5 in the control of cardiomyocyte redox homeostasis, and define TMP195 and TMP269 as a novel class of NRF2 activators that function by suppressing the enzymatic activity of an epigenetic regulator.
- | Journal: Nrf2 activation mediates tumor-specific hepatic stellate cells-induced DIgR2 expression in dendritic cells. (Pubmed Central) - Dec 15, 2019
Moreover, Nrf2 shRNA or KO attenuated splenic T cell inhibition by tHSCs-stimulated mDCs. Together, we conclude that Nrf2 activation mediates tHSCs-induced DIgR2 expression in mDCs.
- || Biomarker, Clinical, Journal: Senescent Phenotype Induced by p90RSK-NRF2 Signaling Sensitizes Monocytes and Macrophages to Oxidative Stress in HIV Individuals: Implications for Atherogenesis. (Pubmed Central) - Dec 8, 2019
cART increased monocyte/macrophage sensitivity to ROS in HIV individuals by suppressing NRF2-ARE activity via p90RSK-mediated ERK5 S496 phosphorylation, which coordinately elicited senescent phenotypes and pro-inflammatory responses. As such, our report underscores the importance of p90RSK regulation in monocytes/macrophages as a viable biomarker and therapeutic target for preventing CVD, especially in HIV patients treated with cART.
- | Preclinical, Journal: Sulforaphane improves endothelial function and reduces placental oxidative stress in vitro. (Pubmed Central) - Dec 6, 2019
As such, our report underscores the importance of p90RSK regulation in monocytes/macrophages as a viable biomarker and therapeutic target for preventing CVD, especially in HIV patients treated with cART. In reducing placental and endothelial oxidative stress, sulforaphane may offer a new adjuvant therapeutic approach for the treatment of preeclampsia.
- | Preclinical, Journal: Use of Primary Mouse Embryonic Fibroblasts in Developmental Toxicity Assessments. (Pubmed Central) - Nov 29, 2019
After collection, MEFs were pretreated with the Nrf2 activator, dithiol-3-thione (D3T; 10 μM) for 12 h, and then treated with either hydrogen peroxide (0-2000 μM) or mercury (0-100 μM) for another 24 h. Viability was measured via MTT assay after 24 h of treatment.
- | Journal: Nrf2 activation in osteoblasts suppresses osteoclastogenesis via inhibiting IL-6 expression. (Pubmed Central) - Nov 27, 2019
The Nrf2 activator acts not only on osteoclasts but also on osteoblasts, in other word, Nrf2 activation indirectly suppresses osteoclastogenesis. In conclusion, the Nrf2 activator exhibits dual inhibitory effects via direct action on osteoclast and indirect action on osteoclast supporting cells.
- | Vincerinone (vatiquinone) / Sumitomo Dainippon, PTC Therapeutics
Journal: New developments in pharmacotherapy for Friedreich ataxia. (Pubmed Central) - Nov 24, 2019
These trials have been directed at the augmentation of mitochondrial function and/or alleviation of symptoms and are not regarded as potential cures in FRDA. Either a combination of therapies or a drug that replaces or increases the pathologically low levels of frataxin better represent potential cures in FRDA.
- | Licensing / partnership, Review, Journal: Therapeutic targeting of the NRF2 and KEAP1 partnership in chronic diseases. (Pubmed Central) - Nov 14, 2019
One NRF2 activator has received clinical approval and several electrophilic modifiers of the cysteine-based sensor KEAP1 and inhibitors of its interaction with NRF2 are now in clinical development. However, challenges regarding target specificity, pharmacodynamic properties, efficacy and safety remain.
- | omaveloxolone (RTA 408) / AbbVie, Reata
Journal, Orphan drug: Orphan Drugs In Development For The Treatment Of Friedreich's Ataxia: Focus On Omaveloxolone. (Pubmed Central) - Nov 8, 2019
Friedreich's Ataxia (FRDA) is a devastating and progressive ataxia, marked by mitochondrial dysfunction and oxidative stress. Nrf2 activators such as omaveloxolone (Omav) modulate antioxidative mechanisms, and thus may be viable therapeutic agents in FRDA.
- Tecfidera (dimethyl fumarate) / Biogen
Genetic Activation of NRF2 By KEAP1 Inhibition Induces Fetal Hemoglobin Expression and Triggers Anti-Oxidant Stress Response in Erythroid Cells (W414AB, Level 4 (Orange County Convention Center)) - Nov 7, 2019 - Abstract #ASH2019ASH_1574;
Additionally, treatment with CDDO-Me, an NRF2 activator compound, resulted in a 4-fold induction in γ-globin mRNA levels in primary SCD patient derived CD34+ cells (by ddPCR), a 2.5-fold induction in HbF (by flow cytometry), and a 2.5-fold up-regulation in both Aγ and Gγ globin levels (by ultra-performance liquid chromatography)...In conclusion, KEAP1 inhibition in erythroid cell lineage and subsequent NRF2 activation leads to HbF induction and improvement in the antioxidant stress enzymes . Overall these data demonstrate a multi-faceted potential benefit of NRF2 activation in sickle cell disease.
- Targeted Therapy of Acute Chest Syndrome with Recombinant Heme Oxygenase-1 Revealed By the Resistance of Young Transgenic Sickle Cell Mice to Heme-Induced Acute Lung Injury (Valencia BC (W415BC), Level 4 (Orange County Convention Center)) - Nov 7, 2019 - Abstract #ASH2019ASH_1373;
In conclusion, we have determined that HO-1 activity in blood plasma declines with aging in SCD patients and identify this phenomenon as the basis of poor survival among adult SS mice with induced ALI/ACS . Furthermore, we provide proof-of-principle in mice that a novel human recombinant HO-1 protein can attenuate lung injury and improve survival from ALI/ACS in SCD.
- | Journal: A novel Nrf2 activator, RS9, attenuates secondary brain injury after intracerebral hemorrhage in sub-acute phase. (Pubmed Central) - Nov 6, 2019
These protective effects were cancelled by the ZnPP co-treatment. Our results suggest that the activation of Nrf2 by RS9 exerts neuroprotective effects that are mediated by the attenuation of oxidative stress, and also that RS9 is an effective therapeutic candidate for the treatment for SBI after ICH.
- | Journal: Interleukin-17D and Nrf2 mediate initial innate immune cell recruitment and restrict MCMV infection. (Pubmed Central) - Nov 2, 2019
Interestingly, we were able to artificially induce innate leukocyte infiltration by applying the Nrf2 activator tert-butylhydroquinone (tBHQ), which rendered mice less susceptible to MCMV infection. Our results implicate the Nrf2/IL-17D axis as a sensor of viral infection and suggest therapeutic benefit in boosting this pathway to promote innate antiviral responses.
- | Tecfidera (dimethyl fumarate) / Biogen
Journal: Dimethyl fumarate accelerates wound healing under diabetic condition. (Pubmed Central) - Oct 29, 2019
However, in spite of the activation of NRF2, DMF lost this capability under the NG condition. The findings of this study demonstrate that ROS activate the protective effect of DMF on the diabetic wound healing.
- | Journal: Astrocyte-specific overexpression of Nrf2 protects against optic tract damage and behavioural alterations in a mouse model of cerebral hypoperfusion. (Pubmed Central) - Oct 18, 2019
In particular, complement components (C4 and C1q) were increased in wild type hypoperfused mice but expressed at levels similar to controls in hypoperfused GFAP-Nrf2 mice. This study provides evidence that overexpression of Nrf2 in astrocytes exerts beneficial effects through repression of inflammation and supports the potential use of Nrf2-activators in the amelioration of cerebrovascular-related inflammation and white matter degeneration.
- | Journal: Optimization of Vinyl Sulfone Derivatives as Potent Nuclear Factor Erythroid 2-Related Factor 2 (Nrf2) Activators for Parkinson's Disease Therapy. (Pubmed Central) - Oct 18, 2019
In a 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-induced mouse model of PD, 17e significantly attenuated loss of tyrosine hydroxylase (TH)-immunopositive dopaminergic (DAergic) neurons, suppressed microglial activation, and alleviated PD-associated motor dysfunction. Thus, 17e is a novel Nrf2 activator with excellent drug-like properties and represents a potential therapeutic candidate for PD.
- | Journal: Replacement of a Naphthalene Scaffold in Kelch-like ECH-Associated Protein 1 (KEAP1)/Nuclear factor (erythroid-derived 2)-like 2 (NRF2)Inhibitors. (Pubmed Central) - Oct 18, 2019
Paying particular attention to aqueous solubility, metabolic stability, potency, and mutagenicity, we modified a previously known, naphthalene-based non-electrophilic NRF2 activator to give a series of non-naphthalene and heterocyclic scaffolds. We found that, compared to previously reported naphthalene-based compounds, a 1,4-isoquinoline scaffold provides a better mutagenic profile without sacrificing potency, stability, or solubility.
- | Tecfidera (dimethyl fumarate) / Biogen
Journal: Nrf2 Suppression Delays Diabetic Wound Healing Through Sustained Oxidative Stress and Inflammation. (Pubmed Central) - Oct 17, 2019
We conclude that Nrf2 activation accelerates impaired wound healing by ameliorating diabetes-mediated oxidative stress and inflammation. This provides a new clinical treatment strategy for diabetic wound healing using Nrf2 activator DMF.
- |||| bardoxolone methyl (RTA 402) / Kyowa Hakko Kirin, Reata, omaveloxolone (RTA 408) / AbbVie, Reata
REATA has investigational drugs bardoxolone and omaveloxolone, Nrf2 activators. Omaveloxolone is being tested in Friedreich’s Ataxia (FA). Today, in a breakthrough for FA, Reata announced positive outcomes. Let’s hope for the same in rare Renal Diseases. https://t.co/pyLM9ZPBDg (Twitter) - Oct 14, 2019
- oltipraz (PMK-N01GI1) / Canopus Biopharma, Pharmaking
Nuclear Factor Erythroid 2-Related Factor 2 (Nrf2) Deficiency Attenuates Hyperglycemia, Hypertension, and Nephropathy via Downregulation of Sodium-Glucose Co-Transporter 2 Expression in db/db Mice (Exhibit Hall, Walter E. Washington Convention Center) - Oct 14, 2019 - Abstract #KIDNEYWEEK2019KIDNEY_WEEK_2706;
In vitro, the effect of oltipraz (Olz, an Nrf2 activator) and overexpression of NRF2 cDNA on SGLT2 expression and SGLT2 promoter activity in human RPTC (HK-2) were assessed...These results identify a novel mechanism by which Nrf2 mediates hyperglycemia-stimulation of Sglt2 expression in diabetes. Funding Government Support - Non-U.S.
- bardoxolone methyl (RTA 402) / Kyowa Hakko Kirin, Reata, Jynarque (tolvaptan) / Otsuka
Tolvaptan and Bardoxolone Methyl Synergistically Activate the Nrf2/HO-1 Pathway (Exhibit Hall, Walter E. Washington Convention Center) - Oct 14, 2019 - Abstract #KIDNEYWEEK2019KIDNEY_WEEK_2578;
Tolvaptan is a potential therapeutic candidate in renal disease. Funding Government Support - Non-U.S.
- Ex Vivo Gene Editing and Pharmacologic Modification of T Cell Keap1/Nrf2 Towards Immunotherapy for Experimental AKI (Exhibit Hall, Walter E. Washington Convention Center) - Oct 14, 2019 - Abstract #KIDNEYWEEK2019KIDNEY_WEEK_2363;
These studies set the stage for immunotherapy treatment for AKI and other immune mediated kidney diseases. Funding NIDDK Support
- bardoxolone methyl (RTA 402) / Kyowa Hakko Kirin, Reata
Activation of the Keap1/Nrf2 Pathway Increases GFR by Increasing Glomerular Effective Filtration Area Without Affecting the Afferent/Efferent Arteriole Ratio (Exhibit Hall, Walter E. Washington Convention Center) - Oct 14, 2019 - Abstract #KIDNEYWEEK2019KIDNEY_WEEK_2094;
Nrf2 activator, Bardoxolone methyl (BARD), increases the estimated glomerular filtration rate (eGFR) in patients with diabetic kidney disease (DKD)...Conclusion The Keap1/Nrf2 pathway plays a pivotal role in regulating GFR and presumably mediates the effects of BARD on GFR. Funding Commercial Support
- | bardoxolone methyl (RTA 402) / Kyowa Hakko Kirin, Reata
Journal: Nrf2 Activator RS9 Suppresses Pathological Ocular Angiogenesis and Hyperpermeability. (Pubmed Central) - Oct 11, 2019
The effects of Nrf2 activators, bardoxolone methyl (BARD) and RS9, were evaluated against vascular endothelial growth factor (VEGF)-induced cell migration in human retinal microvascular endothelial cells (HRMECs)...Furthermore, RS9 showed a tendency toward decreasing CNV lesions, and improved vascular leakage in a CNV monkey model. These data indicate that a Nrf2 activator might be a candidate for treatment of ocular diseases characterized by pathophysiological angiogenesis and hyperpermeability.
- || Reata Regains Exclusive Worldwide Rights of its Nrf2 Activator Product Platform from AbbVie @AbbVie https://t.co/TZGBH24uB1 (Twitter) - Oct 10, 2019
- || bardoxolone methyl (RTA 402) / Kyowa Hakko Kirin, Reata, omaveloxolone (RTA 408) / AbbVie, Reata
$RETA Reacquires Rights From $ABBV to Develop and Commercialize Bardoxolone Methyl, Omaveloxolone, and All Next-Generation Nrf2 Activators. $RETA to pay $AABV $330M cash - $75M upfront. (Twitter) - Oct 10, 2019
- | Journal: Construction of a novel quinoxaline as a new class of Nrf2 activator. (Pubmed Central) - Oct 3, 2019
It is observed that rat has comparable metabolic profile with human, thus, rat could be used as an in vivo model for prediction of pharmacokinetics and metabolism profiles of NQC in human. NQC is a new class of NRF2 activator with potent in vitro anti-inflammatory activity and good metabolic stability.
- | bardoxolone methyl (RTA 402) / Kyowa Hakko Kirin, Reata
Journal: Glucoraphanin: A broccoli sprout extract that ameliorates obesity-induced inflammation and insulin resistance. (Pubmed Central) - Sep 28, 2019
A recent study demonstrated that glucoraphanin, a precursor of the Nrf2 activator sulforaphane, ameliorates obesity by enhancing energy expenditure and browning of white adipose tissue, and attenuates obesity-related inflammation and insulin resistance by polarizing M2 macrophages and reducing metabolic endotoxemia. Thus, this review focuses on the efficiency and safety of glucoraphanin in alleviating obesity, insulin resistance, and NAFLD.
- | Journal: Neuroprotective effects of an Nrf2 agonist on high glucose-induced damage in HT22 cells. (Pubmed Central) - Sep 27, 2019
Thus, this review focuses on the efficiency and safety of glucoraphanin in alleviating obesity, insulin resistance, and NAFLD. This study suggests that the activation of the Nrf2-ARE signalling pathway might be a therapeutic target for the treatment of diabetic encephalopathy.
- | Preclinical, Journal: ROLE OF NRF2 IN PREVENTING OXIDATIVE STRESS INDUCED CHLORIDE CURRENT ALTERATION IN HUMAN LUNG CELLS. (Pubmed Central) - Sep 26, 2019
Immunochemical and immunocytochemical results showed Nrf2 activation with both substances that lead to prevent OS effect on Cl- current. These data bring new insights on the mechanisms involved in OS induced lung tissue damage , pointing out the role of H2 O2 in chloride current alteration and the ability of Nfr2 activation in preventing this effect.
- Hydralazine protects nigrostriatal dopaminergic neurons from MPP+ and MPTP induced neurotoxicity: Roles of Nrf2-ARE signaling pathway (Les Muses Terrace, Level 3) - Sep 24, 2019 - Abstract #MDSCongress2019MDS_745;
These data bring new insights on the mechanisms involved in OS induced lung tissue damage , pointing out the role of H2 O2 in chloride current alteration and the ability of Nfr2 activation in preventing this effect. This study shows that hydralazine as a potent Nrf2 activator, increases the expression of Nrf2 downstream ARE target genes and confers strong neuroprotection in model of PD both in vitro and vivo in a Nrf2 -independent manner.
- | Journal: 2-Methoxy-7-Acetonyljuglone Isolated from Reynoutria japonica Increases the Activity of Nuclear Factor Erythroid 2-Related Factor-2 through Inhibition of Ubiquitin Degradation in HeLa Cells. (Pubmed Central) - Sep 22, 2019
Subsequently, we found that MA significantly enhanced NRF2 stability by inhibiting ubiquitin-dependent proteasomal degradation. Thus, MA might protect cells by enhancing the activity and stability of NRF2 through inhibition of the proteasomal degradation pathway.
- | Journal: Resveratrol, an Nrf2 activator, ameliorates aging-related progressive renal injury. (Pubmed Central) - Sep 14, 2019
Activation of the Nrf2 and SIRT1 signaling pathways ameliorated oxidative stress and mitochondrial dysfunction. Pharmacological targeting of Nrf2 signaling molecules may reduce the pathologic changes of aging in the kidney.
- | Preclinical, Journal: Tert-butylhydroquinone post-treatment attenuates neonatal hypoxic-ischemic brain damage in rats. (Pubmed Central) - Sep 12, 2019
These beneficial effects were accompanied by improved neurological reflex and motor coordination as well as amelioration of spatial learning and memory deficits. Overall, our results provide the first documentation of the beneficial effects of TBHQ in neonatal HI model, in part conferred by activation of Nrf2 mediated antioxidative signaling pathways.
- | Journal: Artocarmitin B enhances intracellular antioxidant capacity via activation of Nrf2 signaling pathway in human lung epithelial cells. (Pubmed Central) - Sep 10, 2019
In terms of activation of Nrf2 pathway, ACB was more potent than ACA and ferulic acid (FA) individually or in combination. Collectively, our results indicate that ACB is a novel Nrf2 activator and enhances intracellular antioxidant capacity in human lung epithelial cells.
- | Journal: Dr. Jekyll and Mr. Hyde: Oxidizable phenol-generated reactive oxygen species enhance sulforaphane's antioxidant response element activation, even as they suppress Nrf2 protein accumulation. (Pubmed Central) - Sep 8, 2019
This unexpected finding reveals the degree to which targets in the ARE pathway downstream of Nrf2 protein accumulation contribute to gene expression. The results presented here provide a model system for significant enhancement of sulforaphane's potency with small molecule co-treatment.
- | Journal: An isopentenyl-substituted flavonoid norartocarpin activates Nrf2 signaling pathway and prevents oxidative insults in human lung epithelial cells. (Pubmed Central) - Sep 8, 2019
Moreover, NOR protected human lung epithelial Beas-2B cells against sodium arsenite [As(III)]-induced cytotoxicity in an Nrf2-dependent manner. Collectively, NOR was firstly identified to be an Nrf2 activator, which demonstrated the capability of preventing oxidative insults in human lung epithelial cells.
- | oxaliplatin / generics
Journal: Luteolin Shifts Oxaliplatin-Induced Cell Cycle Arrest at G₀/G₁ to Apoptosis in HCT116 Human Colorectal Carcinoma Cells. (Pubmed Central) - Sep 6, 2019
Moreover, luteolin treatment was found to reduce oxaliplatin-treated p53-null cell viability and colony counts further, thereby demonstrating an additional effect of luteolin in the killing of human colorectal tumor HCT116 cells not expressing functional p53 protein. The findings suggest that luteolin can induce p53-mediated apoptosis regardless of oxaliplatin treatment and may eliminate oxaliplatin-resistant p53-null colorectal cells.
- ||| Biogen presents the discovery of an orally available non-covalent Nrf2 activator as a tool cpd for validating the benefits of Nrf2 activation for chronic neurodegenerative diseases. #ACSSanDiego (Twitter) - Aug 26, 2019
- | Preclinical, Journal: Contrast media (meglumine diatrizoate) aggravates renal inflammation, oxidative DNA damage and apoptosis in diabetic rats which is restored by sulforaphane through Nrf2/HO-1 reactivation. (Pubmed Central) - Aug 21, 2019
However, silencing Nrf2 using small interfering RNA (siRNA) abolished the cytoprotective effects of sulforaphane. Collectively, the results of this study suggest that Nrf2/HO-1 pathway has a protective role against CIN and support the clinical implication of Nrf2 activators, such as sulforaphane, in CIN particularly in diabetic patients.
- | Sulforadex (sulforafan alfadex) / Evgen Pharma
Journal: SFX-01 reduces residual disability after experimental autoimmune encephalomyelitis. (Pubmed Central) - Aug 10, 2019
In first-in-man and phase II clinical trials for other indications, SFX-01 was found to be well-tolerated. A trial comparing BG-12 and SFX-01 would address whether SFX-01 can offer RRMS patients a better option with respect to efficacy and tolerability.
- | Preclinical, Journal, IO Biomarker: Olmesartan ameliorates chemically-induced ulcerative colitis in rats via modulating NFκB and Nrf-2/HO-1 signaling crosstalk. (Pubmed Central) - Aug 9, 2019
In conclusion, our data show that OLM is an Nrf2 activator, NFkB inhibitor and apoptosis inhibitor in an experimental model of ulcerative colitis. Overall, the study indicates that OLM shows promise as a potential therapy for the treatment of human inflammatory bowel diseases.
- | low molecular weight dextran sulfate (ILB) / TikoMed
Journal: Berberine upregulates P-glycoprotein in human Caco-2 cells and in an experimental model of colitis in the rat via activation of Nrf2-dependent mechanisms. (Pubmed Central) - Aug 7, 2019
...In this study, we used a dextran sulfate sodium (DSS)-induced colitis rat model to evaluate the effect of berberine on P-gp and explore its mechanism of action...Luciferase assays using Caco-2 cells showed a dose-dependent increase in Nrf2 reporter gene activity following berberine treatment, with a significant twofold elevation at 2.5 μM berberine, suggesting that berberine is a strong Nrf2 activator. These results suggest the possible involvement of Nrf2-mediated upregulation of P-gp in the therapeutic effect of berberine on colitis and highlight the potential of P-gp and/or Nrf2 as new therapeutic targets for IBD.
- | Journal: A combination antioxidant therapy to inhibit NOX2 and activate Nrf2 decreases secondary brain damage and improves functional recovery after traumatic brain injury. (Pubmed Central) - Aug 3, 2019
Whereas, the combo therapy (apocynin + TBHQ) given at either 5 min/24 h or 2 h/24 h improved motor and cognitive function and decreased cortical contusion volume compared to vehicle group. Thus, both the generation and disposal of ROS are important modulators of oxidative stress, and a combo therapy that prevents ROS formation and potentiates ROS disposal concurrently is efficacious after TBI.
- | Journal: Ketone body 3-hydroxybutyrate mimics calorie restriction via the Nrf2 activator, fumarate, in the retina. (Pubmed Central) - Aug 1, 2019
Importantly, the upregulation of nuclear factor erythroid 2 p45-related factor 2 (Nrf2), a regulator of G6PD, and elevation of the tricarboxylic acid cycle's Nrf2 activator, fumarate, were also shared. Together, our findings suggest that CR provides retinal antioxidative defense by 3HB through the antioxidant Nrf2 pathway via modification of a tricarboxylic acid cycle intermediate during 3HB metabolism.
- | Preclinical, Journal: Glyceollins Modulate Tumor Development and Growth in a Mouse Xenograft Model of Human Colon Cancer in a p53-Dependent Manner. (Pubmed Central) - Jul 28, 2019
These results suggest that a high dose of glyceollins possibly promotes the growth of p53 wild-type colon cancer through activation of the Nrf2-mediated signaling pathway and, in particular, strong induction of HO-1 expression. Therefore, the consumption of Nrf2 activators, including glyceollins, should be carefully monitored for patients suffering from certain types of cancer and/or receiving chemotherapy.