Picroside II alleviates DSS-induced ulcerative colitis by suppressing the production of NLRP3 inflammasomes through NF-κB signaling pathway
Abstract
Context Ulcerative colitis (UC) is a common acute or chronic intestinal disease with an imbalance of inflammation. Picroside II (P-II) exerts a protective role in various inflammation-related diseases. However, the effect of P-II on UC is still unclear. Objective To explore the effect of P-II on UC and its potential mechanism. Materials and methods Human monocytic leukemia cell line THP-1 was treated with phorbol ester (PMA) to differentiate into a macrophage. The differentiated THP-1 cells were hatched with LPS combined with ATP or Nigericin to activate the NLRP3 inflammasome in vitro. The UC model was constructed by injection of DSS into mice. Results The maximum nontoxic concentration of P-II on THP-1 cells was 60 μM. LPS combined with ATP or Nigericin stimulated the production of IL-1β, which was antagonized by P-II treatment. Meanwhile, P-II administration interfered with the aggregation of ASC and the assembly of NLRP3 inflammasomes. Also, P-II treatment reduced the LPS and ATP-induced elevation of the relative protein expression of NLRP3, pro-caspase-1, IL-1β and p-p65/p65, and the concentration of TNF-α and IL-6. Besides, the NF-κB specific inhibitor BAY-117082 notably repressed the LPS together with ATP-enhanced the relative protein expression of NLRP3, caspase-1 and IL-1β. Moreover, in vivo results showed that P-II relieved the DDS-induced UC, as evidenced by the improvement of mice weight, DAI and pathological scores. In addition, P-II treatment notably decreased DDS-promoted expression of NLRP3 inflammasomes and inflammatory factors in vivo. Conclusion P-II alleviated DSS-induced UC by repressing the production of NLRP3 inflammasomes via the NF-κB signaling pathway.
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Picroside II downregulates LPS-induced phosphorylated p65 relative to total p65 and the levels of NLRP3, caspase-1, and IL-1β in macrophages.
“The authors reported that picroside II downregulated the LPS-induced expression of phosphorylated p65 (p-p65) relative to total p65, as well as the levels of key inflammatory mediators including NOD-like receptor protein 3 (NLRP3), caspase-1, and interleukin 1β (IL-1β) in macrophages [40].”
From Picroside II as a Potential Anti-Inflammatory Agent (2026) · cites this paper as [40]
Picroside II has potent anti-inflammatory effects mediated through regulation of the MAPK/NF-κB signaling pathway and suppression of NLRP3 inflammasome activation.
“Additionally, research has confirmed the potent anti-inflammatory effects of Picroside II, which are mediated through the regulation of the MAPK/NF-κB signaling pathway and the suppression of NLRP3 inflammasome activation. [38,39].”
From Picroside II suppresses chondrocyte pyroptosis through MAPK/NF-κB/NLRP3 signaling pathway alleviates osteoarthritis (2024) · cites this paper as [39]
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Picroside II as a Potential Anti-Inflammatory Agent
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“In a recent study, Yao et al. [40] investigated the anti-inflammatory effects of picroside II in a mouse model of dextran sodium sulfate (DSS)-induced ulcerative colitis and in lipopolysaccharide (LPS)-stimulated macrophages.”
Influential
- Authors
- Yao, H., Yan, J., Yin, L., & Chen, W.
- Affiliations
- Shanghai Sixth People's Hospital (CN)
- Shanghai Jiao Tong University (CN)
- Corresponding author
- Chen, Wei
- ORCID
- Chen, Wei
- Venue
- Immunopharmacology and Immunotoxicology
- Publisher
- Informa UK Limited
- Published
- 2022-03-23
- Volume
- 44
- Issue
- 3
- Pages
- 437-446
- ISSN
- 0892-3973 (ISSN-L)
- 1532-2513
- OpenAlex
- W4220863565
- Semantic Scholar
- 9ba00833566163763f9a3af04192504900e31930
- Cited by
- 17
- References
- 41
- Citations by year
- 2026: 2 · 2025: 4 · 2024: 4 · 2023: 6 · 2022: 1
- FWCI
- 2.02
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Immunopharmacology and Immunotoxicology (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Genetics › Inflammatory Bowel Disease
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Inflammasome and immune disorders
- Health Sciences › Medicine › Complementary and alternative medicine › Natural Compounds in Disease Treatment
- Keywords
- picroside II, ulcerative colitis, NLRP3 inflammasome, NF-κB signaling, DSS-induced colitis, IL-1β, caspase-1, macrophages, anti-inflammatory activity
- MeSH terms
- NLR Family, Pyrin Domain-Containing 3 Protein, Adenosine Triphosphate, Animals, Cinnamates, Colitis, Ulcerative, Inflammation, Lipopolysaccharides, Nigericin, Signal Transduction, Dextran Sulfate, NF-kappa B, Caspase 1, Mice, Iridoid Glucosides, Inflammasomes
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