- |||||||||| acetylcysteine solution / Generic mfg.
Journal, IO biomarker: Coenzyme Q Inhibits NLRP3 Inflammasome Activation through Mitophagy Induction in LPS/ATP-Stimulated Macrophages. (Pubmed Central) - Mar 5, 2022 Notably, when LPS/ATP-stimulated RAW264.7 macrophages were treated with CoQ, Mito-TEMPO (a mitochondrial ROS inhibitor), or N-acetylcysteine (NAC, a ROS inhibitor), there was a significant reduction of LPS/ATP-stimulated NLRP3 inflammasome activation and IL1β expression...Nrf2 knockdown significantly decreased IL1β expression in LPS/ATP-stimulated RAW264.7 macrophages suggesting that CoQ inhibited ROS-mediated NLRP3 inflammasome activation and IL1β expression was suppressed due to the Nrf2 activation. Hence, this study showed that CoQ might be a promising candidate for the therapeutics of inflammatory disorders due to its effective anti-inflammatory as well as antioxidant properties.
- |||||||||| pioglitazone / Generic mfg.
Preclinical, Journal: Effect of parthenolide, an NLRP3 inflammasome inhibitor, on insulin resistance in high-fat diet-obese mice. (Pubmed Central) - Mar 5, 2022 Treatment with PN and pioglitazone (PIO; 30 mg/kg p.o.) attenuated lipopolysaccharide (LPS; 1 ng/ml) - induced elevation of tumor necrosis factor-α and interleukin-1β in mouse peritoneal macrophages in a dose-dependent manner...Thus, PN treatment was also evident with significant improvement in glucose tolerance and peripheral insulin resistance validated through the respective tolerance tests. Therefore, the present study suggests that PN, an NLRP3 inflammasome inhibitor, could be a possible therapeutic agent for attenuating obesity-induced insulin resistance.
- |||||||||| Journal: Intracellular Potassium Ion Measurements by Inductively Coupled Plasma Optical Emission Spectrometer (ICP-OES). (Pubmed Central) - Mar 4, 2022
Therefore, direct measurement of intracellular ion concentration can more truly reflect the role of K flow during the activation of NLRP3. In this chapter, we will provide the rationale and a method to evaluate intracellular K concentration by ICP-OES (Inductively Coupled Plasma Optical Emission Spectroscopy), which helps us understand how disturbances in intracellular K level orchestrates NLRP3 inflammasome activation.
- |||||||||| glibenclamide / Generic mfg.
Journal: CASPorter: A Novel Inducible Human CASP1/NALP3/ASC Inflammasome Biosensor. (Pubmed Central) - Mar 1, 2022 Dox-induced activation of the NLRP3 inflammasome was dose-dependently inhibited by Dox co-treatment with four known CASP1/NLRP3 inhibitors. We have established a cell-based CASP1/NLRP3 inflammasome model, utilizing a fluorescence biosensor as readout for qualitatively observing and quantitatively determining the activation of caspase 1 and NLRP3 inflammasomes in living cells and easily define the inhibitory effect of inhibitors with high efficacy.
- |||||||||| metformin / Generic mfg.
Preclinical, Journal: Metformin reduces chondrocyte pyroptosis in an osteoarthritis mouse model by inhibiting NLRP3 inflammasome activation. (Pubmed Central) - Mar 1, 2022 In addition, in subchondral bone, metformin inhibited osteophyte formation, increased the bone volume fraction (%) and the bone mineral density (g/cm), decreased the trabecular separation (mm) in early stage of osteoarthritis (4 weeks) but the opposite in an advanced stage of osteoarthritis (8 weeks). Overall, metformin inhibited the activation of NLRP3 inflammasome, decreased cartilage degradation, reversed subchondral bone remodelling and inhibited chondrocyte pyroptosis.
- |||||||||| Preclinical, Journal: Anti-hyperlipidemic, Anti-inflammatory, and Ameliorative Effects of DRP1 Inhibition in Rats with Experimentally Induced Myocardial Infarction. (Pubmed Central) - Feb 25, 2022
In coronary artery endothelial cells from the rats, loss of MMP was observed in the HFD-MI, LV-NC, LV-DRP1, and sh-NC groups and concomitantly, the sh-DRP1group showed increased MMP and decreased levels of mitochondrial ROS, cytochrome C, pro-apoptotic proteins, and NLRP3. Inhibition of DRP1 markedly suppressed HL, systematic inflammation, and myocardial injuries induced by HL-MI through partly restoring mitochondrial function and reducing NLRP3 expression.
- |||||||||| Journal: Cleavage-Mediated Regulation of Myd88 Signaling by Inflammasome-Activated Caspase-1. (Pubmed Central) - Feb 24, 2022
While Toll/interleukin-1 receptor (TIR) domain released by MyD88 cleavage additionally contributed to the inhibition of signaling, Waldenström's macroglobulinemia associated MyD88 mutation is able to evade the caspase-1-mediated inhibition of MyD88 signaling through the ability of its TIR domain to recruit full length MyD88 and facilitate signaling. The characterization of this mechanism reveals an additional layer of innate immunity regulation.
- |||||||||| dexamethasone injection / Generic mfg.
Journal: Intra-articular Injection of Baicalein Inhibits Cartilage Catabolism and NLRP3 Inflammasome Signaling in a Posttraumatic OA Model. (Pubmed Central) - Feb 19, 2022 In contrast to the administration of baicalein, dexamethasone injection showed similar effects to slow OA progression, while dexamethasone inhibited NLRP3 inflammasome partly through decreasing levels of SOD, GSH, and MDA. This study indicated that baicalein may have the potential for OA prevention and exerts anti-inflammatory effects partly via suppressing NLRP3 inflammasome activation without affecting oxidative stress-associated molecules, and inhibition of cartilage catabolism enzymes in an OA rat model.
- |||||||||| Journal: Ghrelin Ameliorates Diabetic Retinal Injury: Potential Therapeutic Avenues for Diabetic Retinopathy. (Pubmed Central) - Feb 19, 2022
The results indicated that ghrelin reduced ROS generation, inhibited cell apoptosis and the activation of NLRP3 inflammasome, inhibited the apoptosis of retinal cells in diabetic rats, and protected the retina against HG-induced dysfunction. In conclusion, ghrelin may play a role in the treatment of ocular diseases involving diabetic retinopathy.
- |||||||||| The Sphk1/S1P/S1PR2 Signaling Axis Activates the Inflammasome and Promotes Pyroptosis in PASMCs (Area K, Hall F (North Building, Exhibition Level), Moscone Center) - Feb 19, 2022 - Abstract #ATS2022ATS_4735;
These findings suggest that S1P induces pulmonary vascular pro-inflammatory signaling, and that Sphk1/S1P/S1PR2 signaling axis is involved. Activation of the NLRP3 inflammasome and pyroptosis may be a primarily mechanism underlying pulmonary vascular remodeling, which will be a novel target for the treatment of PAH.
- |||||||||| Journal: 1,2,4-Trimethoxybenzene selectively inhibits NLRP3 inflammasome activation and attenuates experimental autoimmune encephalomyelitis. (Pubmed Central) - Feb 15, 2022
In mice with experimental autoimmune encephalomyelitis (EAE), administration of 1,2,4-TTB (200 mg · kg · d, i.g. for 17 days) significantly ameliorated EAE progression and demyelination. In conclusion, our results demonstrate that 1,2,4-TTB is an NLRP3 inflammasome inhibitor and attenuates the clinical symptom and inflammation of EAE, suggesting that 1,2,4-TTB is a potential candidate compound for treating NLRP3 inflammasome-driven diseases, such as multiple sclerosis.
- |||||||||| Farxiga (dapagliflozin) / Ono Pharma, AstraZeneca
Review, Journal: Neuroprotective Effect of SGLT2 Inhibitors. (Pubmed Central) - Feb 12, 2022 Moreover, they may be able to restore the circadian rhythm of mTOR activation, which is quite a novel finding in the field of research on metabolic diseases and cognitive impairment. SGLT2i have a great potential to protect against atherosclerosis and cognitive impairment in patients with type 2 diabetes mellitus.
- |||||||||| Review, Journal: Phytochemical inhibitors of the NLRP3 inflammasome for the treatment of inflammatory diseases. (Pubmed Central) - Feb 10, 2022
By compiling the data of phytochemical inhibitors targeting NLRP3 inflammasome activation, a complex balance between inflammasome activation or inhibition with NLRP3 as central player was pointed out in NLRP3-driven pathological conditions. Phytochemicals represent potential therapeutic leads, enabling the generation of chemical derivatives with improved pharmacological features to treat NLRP3-mediated inflammatory diseases.
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