ArticleJournal of cellular and molecular medicine2022
4-octyl Itaconate inhibits lipopolysaccharide (LPS)-induced osteoarthritis via activating Nrf2 signalling pathway.
Article in Journal of cellular and molecular medicine, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers.
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Who cites it
23 citing papers in PubMed, 37 citations in OpenAlex.
- Itaconate metabolism in regulated cell death.Molecular and cellular biochemistry · 2026Review
- Itaconate and its derivatives in human health and diseases.Signal transduction and targeted therapy · 2026Review
- Compartmentalized Dual-Drug Injectable Hydrogel for Anti-Inflammatory Activity and Osteoarthritic Cartilage Repair.Small (Weinheim an der Bergstrasse, Germany) · 2026Article
- 4-Octyl itaconate inhibits synovial fibroblast activation by targeting Nrf2 to exert anti-inflammatory effects in rheumatoid arthritis.EULAR rheumatology open · 2026Article
- Targeting the mitochondrial metabolite-dynamics-MDVs-MitoEVs axis: a new frontier in osteoarthritis management.Journal of translational medicine · 2026Review
- The KEAP1/NRF2 axis controls LPS-induced oxidative stress, inflammasome activation and caspase-1 activity in human endothelial cells.PloS one · 2026Article
- Rewiring macrophage immunometabolism in gouty arthritis: from metabolic checkpoints to intelligent nano-delivery.Frontiers in pharmacology · 2026Review
- Intelligent responsive PVA hydrogel loaded with composite MXene nanozyme enables efficient myocardial infarction repair by disrupting the oxidative stress-inflammation cascade.Materials today. Bio · 2025Article
- Metabolic Reprogramming in Stromal and Immune Cells in Rheumatoid Arthritis and Osteoarthritis: Therapeutic Possibilities.European journal of immunology · 2025Review
- Activation of Nrf2 pathway by 4-Octyl itaconate enhances donor lung function in cold preservation settings.Respiratory research · 2025Article
- 4-Octyl itaconate inhibits synovitis in the mouse model of post-traumatic osteoarthritis and alleviates pain.Chinese journal of traumatology = Zhonghua chuang shang za zhi · 2025Article
- Article
- Melatonin Delays Arthritis Inflammation and Reduces Cartilage Matrix Degradation through the SIRT1-Mediated NF-κB/Nrf2/TGF-β/BMPs Pathway.International journal of molecular sciences · 2024Article
- 4-octyl itaconate alleviates cisplatin-induced ferroptosis possibly via activating the NRF2/HO-1 signalling pathway.Journal of cellular and molecular medicine · 2024Article
- Gentiopicroside ameliorates the lipopolysaccharide-induced inflammatory response and hypertrophy in chondrocytes.Journal of orthopaedic surgery and research · 2024Article
- Emerging Roles of Macrophage Polarization in Osteoarthritis: Mechanisms and Therapeutic Strategies.Orthopaedic surgery · 2024Review
- [Effects of VX765 on osteoarthritis and chondrocyte inflammation in rats].Zhongguo xiu fu chong jian wai ke za zhi = Zhongguo xiufu chongjian waike zazhi = Chinese journal of reparative and reconstructive surgery · 2024Article
- Article
- The Abnormal Accumulation of Lipopolysaccharide Secreted by Enriched Gram-Negative Bacteria Increases the Risk of Rotavirus Colonization in Young Adults.Microorganisms · 2023Article
- 4-octyl itaconate improves the viability of D66H cells by regulating the KEAP1-NRF2-GCLC/HO-1 pathway.Journal of cellular and molecular medicine · 2023Article
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Authors and funding
11 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Small molecule drug intervention for chondrocytes is a valuable method for the treatment of osteoarthritis (OA). The 4-octyl itaconate (OI) is a cellular derivative of itaconate with sound cell permeability and transformation rate. We attempted to confirm the protective role of OI in chondrocytes and its regulatory mechanism. We used lipopolysaccharide (LPS) to induce chondrocyte inflammation injury. After the OI treatment, the secretion and mRNA expression of Il-6, Il-10, Mcp-1 and Tnf-α were detected by ELISA and qPCR. The protective effect of OI on articular cartilage was further verified in surgical destabilization of the medial meniscus model of OA. Cell death and apoptosis were evaluated based on CCK8, LDH, Typan blue staining, Annexin V and TUNEL analyses. The small interfering RNAs were used to knockout the Nrf2 gene of chondrocytes to verify the OI-mediated Nrf2 signalling pathway. The results revealed that OI protects cells from LPS-induced inflammatory injury and attenuates cell death and apoptosis induced by LPS. Similar protective effects were also observed on articular cartilage in mice. The OI activated Nrf2 signalling pathway and promoted the stable expression and translocation of Nrf2 into the nucleus. When the Nrf2 signalling pathway was blocked, the protective effect of OI was significantly counteracted in chondrocytes and a mouse arthritis model. Both itaconate and its derivative (i.e., OI) showed important medical effects in the treatment of OA.
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