Beneficial Effects of Hordenine on a Model of Ulcerative Colitis
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Hordenine, a phenethylamine alkaloid, is found in a variety of plants and exhibits a broad array of biological activities and pharmacological properties, including anti-inflammatory and anti-fibrotic effects. However, the efficacy and underlying mechanisms of hordenine in treating ulcerative colitis (UC) remain unclear. To address this, we examined the therapeutic effects of hordenine on dextran sodium sulphate (DSS)-induced UC by comparing disease activity index (DAI), colon length, secretion of inflammatory factors, and degree of colonic histological lesions across diseased mice that were and were not treated with hordenine. We found that hordenine significantly reduced DAI and levels of pro-inflammatory factors, including interleukin (IL)-6, IL-1β, and tumor necrosis factor alpha (TNF-α), and also alleviated colon tissue oedema, colonic lesions, inflammatory cells infiltration and decreased the number of goblet cells. Moreover, in vitro experiments showed that hordenine protected intestinal epithelial barrier function by increasing the expression of tight junction proteins including ZO-1 and occludin, while also promoting the healing of intestinal mucosa. Using immunohistochemistry and western blotting, we demonstrated that hordenine reduced the expression of sphingosine kinase 1 (SPHK1), sphingosine-1-phosphate receptor 1 (S1PR1), and ras-related C3 botulinum toxin substrate 1 (Rac1), and it inhibited the expression of phosphorylated signal transducer and activator of transcription 3 (p-STAT3) in colon tissues. Thus, hordenine appears to be effective in UC treatment owing to pharmacological mechanisms that favor mucosal healing and the inhibition of SPHK-1/S1PR1/STAT3 signaling.
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The anti-inflammatory activity of hordenine in the ulcerative colitis model was observed through inhibition of expression of SPHK1, S1PR1, Rac1, and p-STAT3.
“Furthermore, the anti-inflammatory activity of hordenine was observed through the inhibition of expression of SPHK1, S1PR1, Rac1, and p-STAT3.”
Enhanced expression of tight junction proteins ZO-1 and occludin suggests a role for hordenine in colon epithelial cell healing.
“As well, the enhanced expression of tight junction proteins ZO-1 and occludin suggest a role in colon epithelial cell healing [94].”
In an ulcerative colitis mouse model, mice treated with 50 mg/kg hordenine had diminished production of IL-6, IL-1β, and TNF-α.
“They found that mice treated with 50 mg/kg of hordenine had a diminution in production of IL-6, IL-1β, and TNF-α.”
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Self-citationHordenine Protects Against Lipopolysaccharide-Induced Acute Lung Injury by Inhibiting Inflammation
Zhang, X., Du, L., Zhang, J., Li, C., Zhang, J., & Lv, X. (2021) · Frontiers in Pharmacology · doi:10.3389/fphar.2021.712232 · Cited by 17 · see citing works
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Boucher, R., Germain, H., & Desgagné-Penix, I. (2025) · Plants · doi:10.3390/plants14091372 · Cited by 23 · see citing works
- Authors
- Xu, Z., Zhang, Q., Ding, C., Wen, F., Sun, F., Liu, Y., Tao, C., & Yao, J.
- Affiliations
- Jining Medical University (CN)
- Weifang Medical University (CN)
- Corresponding author
- Yao, Jing
- Venue
- Molecules
- Publisher
- MDPI AG
- Published
- 2023-03-21
- Volume
- 28
- Issue
- 6
- Pages
- 2834
- ISSN
- 1420-3049 (ISSN-L)
- PMC
- PMC10054341
- OpenAlex
- W4353072654
- Cited by
- 15
- References
- 3
- Citations by year
- 2026: 5 · 2025: 9 · 2024: 1
- FWCI
- 2.46
- Type
- journal article
- Language
- en
- Update notices
- correction (2023-03-21)
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- Molecules (publishedVersion, cc-by)
- PubMed Central (publishedVersion, cc-by)
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- Funders
- National Natural Science Foundation of China (81603143, 2020Q060, M-2022247, JYHL2021MS30, JYHL2021FMS13, cx2022006z, s202210443013, JYSJ2022B44)
- Shandong Traditional Chinese Medicine Science and Technology Project (81603143, 2020Q060, M-2022247, JYHL2021MS30, JYHL2021FMS13, cx2022006z, s202210443013, JYSJ2022B44)
- Research Fund for Lin He’s Academician Workstation of New Medicine and Clinical Translation in Jining Medical University (81603143, 2020Q060, M-2022247, JYHL2021MS30, JYHL2021FMS13, cx2022006z, s202210443013, JYSJ2022B44)
- Training Program of Innovation and Entrepreneurship for Undergraduates (81603143, 2020Q060, M-2022247, JYHL2021MS30, JYHL2021FMS13, cx2022006z, s202210443013, JYSJ2022B44)
- Scientific Research and Innovation Team of Jining Medical University (Cultivation): Digestive System Inflammation and Tumour Molecular Pharmacology Research Innovation Team (81603143, 2020Q060, M-2022247, JYHL2021MS30, JYHL2021FMS13, cx2022006z, s202210443013, JYSJ2022B44)
- Practical Teaching Education Research Project of Jining Medical University (81603143, 2020Q060, M-2022247, JYHL2021MS30, JYHL2021FMS13, cx2022006z, s202210443013, JYSJ2022B44)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Genetics › Inflammatory Bowel Disease
- Life Sciences › Agricultural and Biological Sciences › Plant Science › Phytochemistry and biological activity of medicinal plants
- Health Sciences › Medicine › Complementary and alternative medicine › Natural Compounds in Disease Treatment
- Keywords
- hordenine, ulcerative colitis, DSS-induced colitis, anti-inflammatory activity, intestinal epithelial barrier, tight junction proteins, sphingosine kinase 1, S1PR1, Rac1, STAT3 signaling, mucosal healing, goblet cells, inflammatory cytokines
- MeSH terms
- Animals, Anti-Inflammatory Agents, Colitis, Colitis, Ulcerative, Colon, Disease Models, Animal, Mice, Inbred C57BL, Tyramine, Interleukin-6, Dextran Sulfate, Mice
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