ArticleActa pharmacologica Sinica2021
Pristimerin protects against inflammation and metabolic disorder in mice through inhibition of NLRP3 inflammasome activation.
Article in Acta pharmacologica Sinica, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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18 citing papers in PubMed, 29 citations in OpenAlex.
- Ciclopirox Olamine Inhibits the NLRP3 Inflammasome to Alleviate Inflammatory Diseases.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2026Article
- Potential mechanisms of natural products in improving gouty arthritis: Focusing on NLRP3 inflammasome regulation.Journal of pharmaceutical analysis · 2026Review
- Pristimerin Alleviates Nanoparticulate Titanium Dioxide-Triggered Neurodegeneration in Hippocampal and Cortex by Downregulation of Inflammation and Oxidative Damage.Biological trace element research · 2026Article
- Deciphering the NEK7-NLRP3 inflammasome assembly: from conformational activation to allosteric drug discovery.Frontiers in immunology · 2026Review
- NLRP3 inflammasome in health and disease (Review).International journal of molecular medicine · 2025Review
- From "metabolic storm" to "immune paralysis": the dynamic evolution of macrophages and metabolism reprogramming in ARDS.Frontiers in immunology · 2025Review
- Dimethyl fumarate covalently modifies Cys673 of NLRP3 to exert anti-inflammatory effects.iScience · 2024Article
- The role of inflammasomes in human diseases and their potential as therapeutic targets.Signal transduction and targeted therapy · 2024Review
- Pristimerin suppresses AIM2 inflammasome by modulating AIM2-PYCARD/ASC stability via selective autophagy to alleviate tendinopathy.Autophagy · 2024Article
- Acetylation is required for full activation of the NLRP3 inflammasome.Nature communications · 2023Article
- Natural products in attenuating renal inflammationFrontiers in immunology · 2023Review
- NEK7: a new target for the treatment of multiple tumors and chronic inflammatory diseases.Inflammopharmacology · 2022Review
- Activation and Pharmacological Regulation of Inflammasomes.Biomolecules · 2022Review
- MCC950, a Selective NLRP3 Inhibitor, Attenuates Adverse Cardiac Remodeling Following Heart Failure Through Improving the Cardiometabolic Dysfunction in Obese Mice.Frontiers in cardiovascular medicine · 2022Article
- NLRP3 inflammasome in digestive diseases: From mechanism to therapy.Frontiers in immunology · 2022Review
- The role of NLRP3 inflammasome in inflammation-related skeletal muscle atrophy.Frontiers in immunology · 2022Review
- The role of NLRP3 inflammasome in digestive system malignancy.Frontiers in cell and developmental biology · 2022Review
- Editorial: Application of plant secondary metabolites to pain neuromodulation, volume II.Frontiers in pharmacology · 2022Article
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Authors and funding
8 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
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 μM) dose-dependently blocked caspase-1 activation and IL-1β 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 α, β-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 μg/kg, ip) produced remarkable therapeutic effects via inhibition of NLRP3 inflammasome in vivo. In HFD-induced diabetic mouse model, administration of Pri (100 μg· kg
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