ArticleFrontiers in pharmacology2018
A Comparative Study on the Efficacy of NLRP3 Inflammasome Signaling Inhibitors in a Pre-clinical Model of Bowel Inflammation.
Article in Frontiers in pharmacology, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 27 papers.
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Who cites it
27 citing papers in PubMed, 50 citations in OpenAlex.
- P2X4 Receptor Antagonists Exert Anti-Inflammatory Effects via NLRP3 Inflammasome in a Murine Model of Colitis.ACS pharmacology & translational science · 2026Article
- Protein-protein interaction-mediated signaling networks in ischemic stroke: from molecular mechanisms to therapeutic strategies.Acta pharmacologica Sinica · 2026Review
- Targeting pyroptosis in inflammatory bowel disease: A potentially effective therapeutic approach.World journal of gastroenterology · 2025Review
- Unraveling the Converging Roles of ASC-Dependent Inflammasomes, Interleukin-1 Superfamily Members, Serum Amyloid A, and Non-Sterile Inflammation in Disease Pathology and Fibrosis in Inflammatory Bowel Disease and Primary Sclerosing Cholangitis.International journal of molecular sciences · 2025Review
- Ulceroprotective Effects ofCurrent issues in molecular biology · 2025Article
- An anti-complement homogeneous polysaccharide fromActa pharmaceutica Sinica. B · 2025Article
- NLRP3 and beyond: inflammasomes as central cellular hub and emerging therapeutic target in inflammation and disease.Frontiers in immunology · 2025Review
- NLRP inflammasomes in health and disease.Molecular biomedicine · 2024Review
- Therapeutic potential of PANoptosis: innate sensors, inflammasomes, and RIPKs in PANoptosomes.Trends in molecular medicine · 2024Review
- Pharmacological Inhibition of the NLRP3 Inflammasome: Structure, Molecular Activation, and Inhibitor-NLRP3 Interaction.Pharmacological reviews · 2023Review
- Inhibitors of the NLRP3 inflammasome pathway as promising therapeutic candidates for inflammatory diseases (Review).International journal of molecular medicine · 2023Review
- USP14 promotes pyroptosis of human annulus fibrosus cells derived from patients with intervertebral disc degeneration through deubiquitination of NLRP3.Acta biochimica et biophysica Sinica · 2022Article
- Tackling Inflammatory Bowel Diseases: Targeting Proinflammatory Cytokines and Lymphocyte Homing.Pharmaceuticals (Basel, Switzerland) · 2022Review
- Anti-inflammatory Effects of Novel P2X4 Receptor Antagonists, NC-2600 and NP-1815-PX, in a Murine Model of Colitis.Inflammation · 2022Article
- Enteric α-synuclein impairs intestinal epithelial barrier through caspase-1-inflammasome signaling in Parkinson's disease before brain pathology.NPJ Parkinson's disease · 2022Article
- A Novel Inhibitor INF 39 Promotes Osteogenesis via Blocking the NLRP3/IL-1BioMed research international · 2022Article
- Immunology of Inflammatory Bowel Disease: Molecular Mechanisms and Therapeutics.Journal of inflammation research · 2022Review
- Chemical Modulation of the 1-(Piperidin-4-yl)-1,3-dihydro-2Molecules (Basel, Switzerland) · 2021Article
- By Regulating the NLRP3 Inflammasome Can Reduce the Release of Inflammatory Factors in the Co-Culture Model of Tuberculosis H37Ra Strain and Rat Microglia.Frontiers in cellular and infection microbiology · 2021Article
- Palmitoylethanolamide Counteracts Enteric Inflammation and Bowel Motor Dysfunctions in a Mouse Model of Alzheimer's Disease.Frontiers in pharmacology · 2021Article
Corrections and comments
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Authors and funding
13 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Nucleotide-binding oligomerization domain leucine rich repeat and pyrin domain-containing protein 3 (NLRP3) inflammasome is pivotal in maintaining intestinal homeostasis and sustaining enteric immune responses in the setting of inflammatory bowel diseases. Drugs acting as NLRP3 blockers could represent innovative strategies for treatment of bowel inflammation. This study was performed in rats with dinitrobenzenesulfonic acid (DNBS)-induced colitis, to investigate how the direct blockade of NLRP3 inflammasome with an irreversible inhibitor (INF39) compares with Ac-YVAD-cmk (YVAD, caspase-1 inhibitor) and anakinra (IL-1β receptor antagonist), acting downstream on NLRP3 signaling. Animals with DNBS-colitis received YVAD (3 mg/kg) or anakinra (100 mg/Kg) intraperitoneally, and INF39 (25 mg/kg) or dexamethasone (DEX, 1 mg/kg) orally for 6 days, starting on the same day of colitis induction. Under colitis, there was a body weight decrease, which was attenuated by YVAD, anakinra or INF39, but not DEX. All test drugs counteracted the increase in spleen weight. The colonic shortening and morphological colonic alterations associated with colitis were counteracted by INF39, anakinra and DEX, while YVAD was without effects. Tissue increments of myeloperoxidase, tumor necrosis factor and interleukin-1β were more effectively counteracted by INF39 and DEX, than YVAD and anakinra. These findings indicate that: (1) direct inhibition of NLRP3 inflammasome with INF39 is more effective than caspase-1 inhibition or IL-1β receptor blockade in reducing systemic and bowel inflammatory alterations; (2) direct NLRP3 inhibition can be a suitable strategy for treatment of bowel inflammation.
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