ArticleBritish journal of pharmacology2018
Activating the pregnane X receptor by imperatorin attenuates dextran sulphate sodium-induced colitis in mice.
Article in British journal of pharmacology, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers, 1 of them a synthesis that pooled it.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
19 citing papers in PubMed, 1 synthesis or guideline pooled it, 50 citations in OpenAlex.
- Therapeutic potential of natural coumarins in autoimmune diseases with underlying mechanisms.Frontiers in immunology · 2024Pooled it
- Imperatorin Mitigates Rosacea-Like Inflammation by Modulating the Crosstalk Between JNK1 and STAT1.FASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2026Article
- ALDH3A1-dependent Nrf2/HO-1/GPX4 pathway supports AHR as a promising therapeutic target for ferroptosis and promotes imperatorin-mediated lung protection.Cell death discovery · 2026Article
- Angelica dahurica Polysaccharides Ameliorate Colitis by Reducing the Restriction of Gut Microbiota-Derived Imidazole Propionate on PPAR-γ Signaling Activation.Phytotherapy research : PTR · 2025Article
- 1-methylnicotinamide modulates IL-10 secretion and voriconazole metabolism.Frontiers in immunology · 2025Article
- Natural Product-based Therapies for Inflammatory Bowel Disease: Targeting Key Signaling Pathways.Mini reviews in medicinal chemistry · 2025Review
- Recent advances in anti-inflammatory active components and action mechanisms of natural medicines.Inflammopharmacology · 2023Review
- Natural Coumarin Derivatives Activating Nrf2 Signaling Pathway as Lead Compounds for the Design and Synthesis of Intestinal Anti-Inflammatory Drugs.Pharmaceuticals (Basel, Switzerland) · 2023Review
- Treatment Effects of Natural Products on Inflammatory Bowel Disease In Vivo and Their Mechanisms: Based on Animal Experiments.Nutrients · 2023Review
- Enteric-Coated Cologrit Tablet Exhibit Robust Anti-Inflammatory Response in Ulcerative Colitis-like In-Vitro Models by Attuning NFκB-Centric Signaling Axis.Pharmaceuticals (Basel, Switzerland) · 2022Article
- Ginsenoside Rc attenuates DSS-induced ulcerative colitis, intestinal inflammatory, and barrier function by activating the farnesoid X receptor.Frontiers in pharmacology · 2022Article
- Regulation of PXR Function by Coactivator and Corepressor Proteins: Ligand Binding Is Just the Beginning.Cells · 2021Review
- Gut microbiota accelerates cisplatin-induced acute liver injury associated with robust inflammation and oxidative stress in mice.Journal of translational medicine · 2021Article
- Coumarin Derivatives in Inflammatory Bowel Disease.Molecules (Basel, Switzerland) · 2021Review
- Imperatorin as a Promising Chemotherapeutic Agent Against Human Larynx Cancer and Rhabdomyosarcoma Cells.Molecules (Basel, Switzerland) · 2020Article
- The Protective Effects of Imperatorin on Acetaminophen Overdose-Induced Acute Liver Injury.Oxidative medicine and cellular longevity · 2020Article
- Activation of PXR by alantolactone ameliorates DSS-induced experimental colitis via suppressing NF-κB signaling pathway.Scientific reports · 2019Article
- Pregnane X receptor activation constrains mucosal NF-κB activity in active inflammatory bowel disease.PloS one · 2019Article
- Activating the pregnane X receptor by imperatorin attenuates dextran sulphate sodium-induced colitis in mice.British journal of pharmacology · 2018Article
Corrections and comments
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Authors and funding
13 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposeActivation of the human pregnane X receptor (PXR; NR1I2) has potential therapeutic uses for inflammatory bowel disease (IBD). Imperatorin (IMP), a naturally occurring coumarin, is the main bioactive ingredient of Angelica dahurica Radix, which is regularly used to treat the common cold and intestinal disorders. However, there are no data on the protective effects of IMP against IBD. EXPERIMENTAL APPROACH: The effects of IMP on PXR-modulated cytochrome P450 3A4 (CYP3A4) expression were assessed using a PXR transactivation assay, a mammalian two-hybrid assay, a competitive ligand-binding assay, analysis of CYP3A4 mRNA and protein expression levels and measurement of CYP3A4 activity using a cell-based reporter gene assay and in vitro model. The inhibitory effects of IMP on NF-κB activity were evaluated by a reporter assay and NF-κB p65 nuclear translocation. The anti-IBD effects of IMP were investigated in a dextran sulphate sodium (DSS)-induced colitis mouse model. Colon inflammatory cytokines were assessed by elisa. KEY
resultsIMP activated CYP3A4 promoter activity, recruited steroid receptor coactivator 1 to the ligand-binding domain of PXR and increased the expression and activity of CYP3A4. PXR knockdown substantially reduced IMP-induced increase in CYP3A4 expression. Furthermore, IMP-mediated PXR activation suppressed the nuclear translocation of NF-κB and down-regulated LPS-induced expression of pro-inflammatory genes. Nevertheless, PXR knockdown partially reduced the IMP-mediated inhibition of NF-κB. IMP ameliorated DSS-induced colitis by PXR/NF-κB signalling. CONCLUSIONS AND IMPLICATIONS: IMP acts as a PXR agonist to attenuate DSS-induced colitis by suppression of the NF-κB-mediated pro-inflammatory response in a PXR/NF-κB-dependent manner.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.