Itaconate derivative eye drops deploy anti-inflammatory effect in treating dry eye models
Zimeng Zhai1, Yiteng Lu1, Xujiao Zhou1
1Department of Ophthalmology, Eye & ENT Hospital, State Key Laboratory of Brain Function and Disorders, MOE Frontiers Center for Brain Science, Fudan University, Shanghai, China.
Advances in Ophthalmology Practice and Research
|May 7, 2026
Summary
4-Octyl itaconate (4-OI) eye drops effectively treat dry eye disease (DED) by reducing inflammation. This itaconate derivative shows promise as a safe therapeutic option for DED patients.
Area of Science:
- Ophthalmology
- Immunology
- Pharmacology
Background:
- Dry eye disease (DED) is a prevalent ocular condition characterized by inflammation.
- Itaconate (ITA) is an endogenous immunomodulator with anti-inflammatory properties.
- 4-Octyl itaconate (4-OI) is a derivative of ITA being investigated for therapeutic potential.
Purpose of the Study:
- To evaluate the therapeutic efficacy and safety of 4-Octyl itaconate (4-OI) for treating dry eye disease (DED).
- To investigate the anti-inflammatory mechanisms of 4-OI in an in vivo DED model.
Main Methods:
- In vitro assessment of 4-OI cytotoxicity and anti-inflammatory effects on human corneal epithelial cells (HCECs).
- Induction of DED in C57BL/6 mice and treatment with 4-OI eye drops or intraperitoneal injection.
- Evaluation of corneal epithelial defects, tear secretion, and molecular mechanisms (qPCR, Western blotting, mRNA sequencing, TUNEL, H&E staining).
Main Results:
- 4-OI eye drops significantly reduced corneal epithelial defects and increased tear secretion in DED mice.
- mRNA sequencing revealed downregulation of key inflammatory pathways, including IL-1, TNF, and IL-17 signaling.
- Molecular assays confirmed reduced expression of pro-inflammatory mediators (IL-1β, IL-17A, TNF-α, NFKBIZ) without significant toxicity.
Conclusions:
- 4-Octyl itaconate (4-OI) demonstrates significant therapeutic potential for dry eye disease.
- 4-OI acts as a safe and effective anti-inflammatory agent by suppressing ocular inflammatory pathways.
- This ITA derivative offers a promising new treatment strategy for DED.
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