nrf2/are pathway

Sesaminol is an orally active activator of the Nrf2-ARE signaling pathway, promoting the nuclear translocation of Nrf2 and boosting the expression of NQO1 to enhance cellular defense against oxidative stress. It inhibits 6-OHDA-induced ROS production and apoptosis in SH-SY5Y cells. Sesaminol also provides neuroprotective effects against Rotenone-induced Parkinson's disease.

1. Isoquercetin (3-Glucosylquercetin) is a potential stimulator of bone mineralization used for prophylaxis of osteoporotic disorders. 2. Isoquercetin may be as a potential therapeutic agent against neurodegeneration in Parkinson's disease. 3. Isoquercetin is an inhibitor of Wnt β-catenin and may be as a potential novel anti-tumoral agent, such as against human pancreati,liver cancer related to opioid receptors and to the activation of the mitogen-activated protein kinase (MAPK) signalling pathway. .

Nrf2-ARE hMAO-B QR2 modulator 1, a resveratrol derivative and multi-target-directed ligand (mtdl), activated the NRF2-ARE pathway (CD = 9.83 μM), selectively inhibited hMAO-B and QR2（quinone reductase-2，NQO2) (IC 50 = 8.05 and 0.57 μM), and was able to promote hippocampal neurogenesis and exert neuroprotective and antioxidant effects in an Alzheimer's disease model.

DDO-7263 is a 1,2,4-Oxadiazole derivative that upregulates Nrf2 through binding to Rpn6 to block the assembly of 26S proteasome and the subsequent degradation of ubiquitinated Nrf2. DDO-7263 is a potent Nrf2 activator that activates the Nrf2-ARE signaling pathway and exerts anti-inflammatory activity [1].

Shinorine, a mycosporine-like amino acid (MAA), is a small molecule sunscreen produced in some bacteria. Shinorine ameliorates chromium induced toxicity in zebrafish hepatocytes through the facultative activation of Nrf2-Keap1-ARE pathway. Shinorine is also an analogue of porphyra-344. Both porphyra-334 and shinorine are antioxidants and direct antagonists of Keap1-Nrf2 binding. Shinorine may be a useful agent to prevent or retard the progression of multiple degenerative disorders of ageing. Shinorine is a demethyl-analog of Porphyra 334.

2-HBA, a synthetic analog of curcumin, is an indirect inducer of enzymes that catalyze detoxification reactions through the Keap1-Nrf2-ARE pathway.

(R)-Sulforaphane (L-Sulforaphane) is a potent inducer of the Keap1 Nrf2 ARE pathway.

S21-1011 is a selective butyrylcholinesterase (BChE) inhibitor, demonstrating IC50 values of 0.059 μM for eqBChE and 0.162 μM for hBChE. This compound displays favorable pharmacokinetic properties, including effective blood-brain barrier (BBB) permeability. Furthermore, S21-1011 activates the keap1-Nrf2-ARE pathway, with an EC50 of 23.48 μM for activating the antioxidant element ARE, and has been shown to improve cognitive function in a murine model of Alzheimer's disease.

Tigloylgomisin H represents a potential liver cancer prevention agent, it can significantly induce quinone reductase (QR) activity in Hepa1c1c7 mouse hepatocarcinoma cells, it functions as a novel monofunctional inducer that specifically upregulates phase

Rehmapicrogenin regulates the Nrf2 ARE signaling pathway. Nrf2 ARE signaling pathway is the most important pathway of oxidative stress.

(R)-5-Hydroxy-1,7-diphenylheptan-3-one ((5R)-Dihydroyashabushiketol) is extracted from the rhizomes of Alpinia officinarum, a Chinese medicinal herb, and inhibits melanogenesis in theophylline-stimulated murine B16 melanoma 4A5 cells.