Citations
2 publicationsPublications from researchers using this productDescription
4-Octyl Itaconate (4-OI) is a cell-permeable itaconate derivative. Itaconate and 4-Octyl Itaconate had similar thiol reactivity, making 4-Octyl Itaconate a suitable itaconate surrogate to study its biological function. 4-Octyl Itaconate is reported to alkylate cysteine residues on kelchlike ECH-associated protein 1 (KEAP1) and then activate nuclear factor (erythroid derived 2)-related factor 2 (Nrf2) to exert antioxidant and anti-inflammatory effects. [1]. 4-Octyl Itaconate can halt the progress of various diseases, including ischemiareperfusion injury, osteoclast-related diseases, and renal fibrosis, by reducing oxidative stress and modifying the immune response of macrophages to lipopolysaccharide (LPS) [2].
The inhibitory effect of 4-octyl itaconate extends to the replication of several other pathogenic viruses including Herpes Simplex Virus-1 and-2, Vaccinia virus, and Zika virus through a type I interferon (IFN)- independent mechanism. In addition, 4-Octyl Itaconate limit host inflammatory responses to SARS-CoV2 infection [3].
Treat Vero cells with 4-octyl itaconate enerated before infection with SARS-CoV2 resulted in a 102–104 eduction in SARS-CoV2 RNA levels in a dose dependent manner, while not affecting cell viability, as determined by lactate dehydrogenase (LDH) release assay. The antiviral effect of 4-Octyl Itaconate was also demonstrated in the lung cancer cell line Calu-3, where SARS-CoV2 RNA levels were reduced by >2-logs, while release of progeny virus was reduced by >6-logs. 4-Octyl Itaconate effect SARSCoV2 in primary human airway epithelial (HAE) cultures, also, 4-Octyl Itaconate treatment significantly reduced viral RNA levels. The antiviral effect of 4-Octyl Itaconate was reproduced using a different SARS-CoV-2 isolate [3].
4-Octyl Itaconate (50 mg/ kg) were administered to 57BL/6J mice or vehicle 2 h before intraperitoneal injection of LPS (5 mg/kg). 4-Octyl Itaconate treatment significantly prolonged the survival rate and simultaneously decreased the serum levels of IL-1β, IL-6 and lactate in mice induced by LPS. 4-Octyl Itaconate protects mice against experimental lethal endotoxaemia partly by inhibiting cytokine release and lactate production [1].
References:
[1] Liao, S. T. et al. 4-Octyl itaconate inhibits aerobic glycolysis by targeting GAPDH to exert anti-inflammatory effects. Nat. Commun. 10, 5091, 2019.
[2] Li, Y., Chen, X., Zhang, H., et al. 4-Octyl Itaconate Alleviates Lipopolysaccharide-Induced Acute Lung Injury in Mice by Inhibiting Oxidative Stress and Inflammation. Dddt 14, 5547–5558. 2020. doi:10.2147/DDDT.S280922.
[3] Olagnier, D. et al. SARS-CoV2-mediated suppression of NRF2-signaling reveals potent antiviral and anti-inflammatory activity of 4-octyl-itaconate and dimethyl fumarate. Nat. Commun. 11, 4938, 2020.
Protocol
| Cell experiment [1]: | |
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Cell lines |
C28/I2 chondrocytes |
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Preparation Method |
Cells were stimulated with 10 ng/mL interleukin 1β(IL-1β) for 24 h. CQ (50 μM) was incubated with chondrocytes for 48 h in the CQ group, chondrocytes were pretreated with 4-Octyl Itaconate (100 μM) for 48 h followed by treatment with IL-1β (1 ng/mL) for 24 h in the IL-1β + 4-Octyl Itaconate group, and chondrocytes were pretreated with 4-Octyl Itaconate (100 μM) for 48 h followed by treatment with CQ (50 μM) for 48 h in the CQ + 4-Octyl Itaconate group. The control group was untreated chondrocytes cultured in regular medium. |
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Reaction Conditions |
100μM for 48 hours |
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Applications |
IL-1β (interleukin 1β) treatment significantly inhibited the growth of chondrocytes, but the cell growth of chondrocytes was restored after the pretreatment of 4-Octyl Itaconate. The IL-1β induces chondrocyte apoptosis and participates in the pathogenesis of OA (Osteoarthritis), 4-Octyl Itaconate protected chondrocytes from IL-1β-induced apoptosis. |
| Animal experiment [2]: | |
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Animal models |
Male C57BL/6 mice aged 8–10-weeks-old |
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Preparation Method |
The control group (rats were shamoperated and given saline solution on the first day of every week from the 4th to the12th week following surgery, n = 6), the OA group (subjected to DMM, 100 μLof normal saline treatment injected at the same as in the control group, n = 6), and the OA + OI group (subjected to DMM, 100 μL of OI (100 μM) injected at the same as in the control group, n = 6). |
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Dosage form |
Inject 50 mg/kg or 100 mg/kg |
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Applications |
The histopathology indicated that 4-Octyl Itaconate reduced the LPS-induced pulmonary edema, hemorrhage and inflammatory cell infiltration. The inflammation scores of 4-Octyl Itaconate intervention groups were lower than those of the ALI group. 4-Octyl Itaconate could alleviate acute lung tissue injury induced by lipopolysaccharide. |
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References: [1]. X. Pan, H. Shan, J. Bai et al. Four-octyl itaconate improves osteoarthritis by enhancing autophagy in chondrocytes via PI3K/AKT/mTOR signalling pathway inhibition. Communications Biology, vol. 5, no. 1, p. 641, 2022. [2]. Li, Y., Chen, X., Zhang, H., et al. 4-Octyl Itaconate Alleviates Lipopolysaccharide-Induced Acute Lung Injury in Mice by Inhibiting Oxidative Stress and Inflammation. Dddt 14, 5547–5558. 2020. doi:10.2147/DDDT.S280922 |
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Product Documents
Chemical Properties
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility
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