ReferenceID 2678
Pristimerin protects against inflammation and metabolic disorder in mice through inhibition of NLRP3 inflammasome activation
Acta Pharmacol Sin
Excessive activation of NLRP3 inflammasome is associated with the pathogenesis of inflammatory diseases. Pristimerin (Pri) is a quinonoid triterpene derived from traditional Chinese medical herb Celastraceae and Hippocra
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Record Fields
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- Reference Id
- 2678
- Evidence Id
- 19268
- Core Evidence Id
- 19268
- Source Reference Id
- 5354
- Herb2 Reference Id
- HBREF006151
- Subject Paper Key
- HBIN040737_32989235
- Pubmed Id
- 32989235
- Doi
- 10.1038/s41401-020-00527-x
- Paper Title
- Pristimerin protects against inflammation and metabolic disorder in mice through inhibition of NLRP3 inflammasome activation
- Paper Abstract
- Excessive activation of NLRP3 inflammasome is associated with the pathogenesis of inflammatory diseases. Pristimerin (Pri) is a quinonoid triterpene derived from traditional Chinese medical herb Celastraceae and Hippocrateaceae. Pri has shown antifungal, antibacterial, antioxidant, and anticancer activities. In this study we investigated whether NLRP3 inflammasome was associated with the anti-inflammatory activity of Pri. We showed that Pri (0.1-0.4 muM) dose-dependently blocked caspase-1 activation and IL-1beta maturation in LPS-primed mouse bone-marrow-derived macrophages (BMDMs). Pri specifically inhibited NLRP3 inflammasome activation, had no visible effects on NLRC4 and AIM2 inflammasome activation. Furthermore, we demonstrated that Pri blocked the assembly of the NLRP3 inflammasome via disturbing the interaction between NEK7 and NLRP3; the alpha, beta-unsaturated carbonyl moiety of Pri was essential for NLRP3 inflammasome inactivation. In LPS-induced systemic inflammation mouse model and MSU-induced mouse peritonitis model, preinjection of Pri (500 mug/kg, ip) produced remarkable therapeutic effects via inhibition of NLRP3 inflammasome in vivo. In HFD-induced diabetic mouse model, administration of Pri (100 mug kg-1 d-1, ip, for 6 weeks) reversed HFD-induced metabolic disorders via suppression of NLRP3 inflammasome activation. Taken together, our results demonstrate that Pri acts as a NLRP3 inhibitor, suggesting that Pri might be useful for the treatment of NLRP3-associated diseases.
- Journal
- Acta Pharmacol Sin
- Publish Year
- 2021
- Experiment Subject
- mouse; lps-primed mouse bone-marrow-derived macrophages
- Experiment Type
- Animal Experiment
- Phenotype Related
- Metabolic Disorders; Diabetic; Inflammatory Diseases
- Paper Title Cn
- Paper Title En
- Pristimerin protects against inflammation and metabolic disorder in mice through inhibition of NLRP3 inflammasome activation
- Bilingual Status
- semi_complete