ReferenceID 4736
Anti-inflammatory action of betulin and its potential as a dissociated glucocorticoid receptor modulator
Food Chem Toxicol
Although the medical application of betulin has been presented in previous studies, the potential mechanism of the anti-inflammatory action of betulin should be further investigated. This work aims to confirm the hypothe
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Record Fields
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- Reference Id
- 4736
- Evidence Id
- 21326
- Core Evidence Id
- 21326
- Source Reference Id
- 2713
- Herb2 Reference Id
- HBREF003510
- Subject Paper Key
- HBIN018374_34500009
- Pubmed Id
- 34500009
- Doi
- 10.1016/j.fct.2021.112539
- Paper Title
- Anti-inflammatory action of betulin and its potential as a dissociated glucocorticoid receptor modulator
- Paper Abstract
- Although the medical application of betulin has been presented in previous studies, the potential mechanism of the anti-inflammatory action of betulin should be further investigated. This work aims to confirm the hypothesis that betulin has dexamethasone-like anti-inflammatory action through glucocorticoid receptor (GR)-mediated pathway. Firstly, the binding ability of betulin with GR was measured by a fluorescence polarization-based competitive binding assay, with the IC50 value of 79.18 +- 0.30 mM. Betulin could bind to GR and then induced GR nuclear translocation, but lacked GR transcriptional activity in HeLa cells. Hence, betulin exhibited the potential to be a dissociated modulator for GR, with the loss of glucocorticoid response element (GRE)-associated side effects. In addition, betulin downregulated GRE-driven protein expression of G6P involved in gluconeogenesis, namely side effect. The results of pro-inflammatory cytokines analysis showed that betulin exerted anti-inflammatory action in vitro. Both of the hydrophobic and hydrogen-bonding interactions stabilized the binding between betulin and GR during the simulation process. In conclusion, betulin might be a potential dissociated GR modulator with a reduced side effect profile yet keeping its anti-inflammatory action.
- Journal
- Food Chem Toxicol
- Publish Year
- 2021
- Experiment Subject
- Experiment Type
- Cell Experiment
- Phenotype Related
- Paper Title Cn
- Paper Title En
- Anti-inflammatory action of betulin and its potential as a dissociated glucocorticoid receptor modulator
- Bilingual Status
- semi_complete