Medicarpin Increases Antioxidant Genes by Inducing NRF2 Transcriptional Level in HeLa Cells

Abstract

The nuclear factor erythroid-derived 2-related factor 2 (NRF2) plays a pivotal role in the regulation of genes involved in oxidative stress and drug detoxification. Therefore, it is important to find NRF2 inducers to protect cells from excessive oxidative damage. Here, we investigated the effect of medicarpin isolated from the root of Robinia pseudoacacia L. on the activity of NRF2 in HeLa cells. Medicarpin significantly induced the antioxidant response elements (ARE)-luciferase activity in a concentration-dependent manner. Furthermore, medicarpin not only induced HO-1, GCLC, and NQO1 mRNA by translocating NRF2 to the nucleus but also induced the mRNA level of NRF2. To verify the NRF2 induction mechanism by medicarpin, ~2 kb of NRF2 promoter-luciferase assay was executed. As a result, medicarpin significantly induced NRF2-luciferase activity. Moreover, medicarpin strongly inhibited the ubiquitin-dependent proteasomal degradation of NRF2. Thus, medicarpin might protect cells by promoting the NRF2 transcriptional activity.

Network Pharmacology Exploration Reveals Gut Microbiota Modulation as a Common Therapeutic Mechanism for Anti-Fatigue Effect Treated with Maca Compounds Prescription

“…According to the literature reports, the other key compounds also have plentiful biological activities. Phyllanthin [26], 7-Methoxy-2-methyl isoflavone [27], medicarpin [28], and N-benzyl-9-oxo-10E,12Z-octadecadienamide [29] displayed anti-inflammatory, antioxidant, neuroprotective, and anti-cancer effects. These studies suggest that the MCP has strong support in fatigue management via network pharmacology.…”

Identification of mulberry leaf flavonoids and evaluating their protective effects on H2O2-induced oxidative damage in equine skeletal muscle satellite cells

“…Previous studies have established a robust connection between flavonoids and the mitigation of oxidative stress through the Nrf2-ARE pathway in various cellular models ( Kim et al, 2022 ). Specifically, flavonoid compounds in pre-treatments activate Nrf2 activity ( Khan et al, 2020 ), which transcriptionally activate antioxidant and detoxifying enzymes, including SOD, glutathione peroxidase, and thioredoxin reductase ( Yi et al, 2020 ; Kitaoka, 2021 ).…”

Bioprospecting microbes and enzymes for the production of pterocarpans and coumestans

“…Medicarpin chemical structure is composed of a pterocarpan core with a hydroxyl group on position C-3 and a methyl group on position C-9. Besides its function as a natural antioxidant, medicarpin is a promising neuroprotective agent for Alzheimer's disease, and also as a bone regeneration agent to treat osteoporosis (Dixit et al, 2015;Kim et al, 2022). Medicarpin also has potential uses in the agricultural sector.…”