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- NLRP3 Inhibition during Cold Preservation Attenuates Prolonged Cold Ischemia-Induced Accelerated Immune Reaction (118-ABC, Level 1) - May 6, 2024 - Abstract #ATC2024ATC_2881;
NLRP3 inhibition during CIT preserved allograft function and prevented innate immune responses within the graft site during the early post-transplant period resulting in promoting graft acceptance induced by costimulation blockade. It could be a promising strategy for inducing transplant tolerance.
- | RGFP966 / BioMarin
Journal, IO biomarker, Epigenetic controller: Histone deacetylase 3-specific inhibitor RGFP966 attenuates oxidative stress and inflammation after traumatic brain injury by activating the Nrf2 pathway. (Pubmed Central) - May 6, 2024
Overall, our findings demonstrate that RGFP966 can mitigate the first brain damage and neurological impairments in TBI. The underlying mechanism involves triggering the Nrf2-mediated AO system and negatively regulating the HMGB1/TLR4-mediated NLRP3 inflammasome pathway.
- | Preclinical, Journal: Anti-inflammatory and uric acid lowering effects of Euodiae fructus on hyperuricemia and gout mice. (Pubmed Central) - May 6, 2024
Taken together, these data indicate that ER, a powerful and specific NLRP3 inhibitor, has multiple anti-HUA, anti-gout and anti-inflammatory effects. Our investigation is designed to experimentally support the conventional use of ER-containing classical herbal formulas in the treatment of HUA-related disorders and may add a new dimension to the clinical application of ER.
- | Journal: pH responsive fabrication of PVA-stabilized selenium nano formulation encapsulated with luteolin to reduce diabetic ureteral injury by decreasing NLRP3 inflammasome via Nrf2/ARE signaling. (Pubmed Central) - May 3, 2024
The LT-SeNPs significantly inhibits the NLRP3 in?ammasome through Nrf2/ARE pathway, which benefits for DUI treatment. The developed LT-SeNPs could be an effective formulation for the DUI therapy.
- NLRP3-inflammasome inhibition reduces stroke induced inflammation and delays infarct growth before recanalization (Room Berlin) - May 3, 2024 - Abstract #EAN2024EAN_165;
The developed LT-SeNPs could be an effective formulation for the DUI therapy. As main finding we show that blocking of NLRP3 mitigates cerebral inflammation and infarct growth already under LVO and partly preserves the ischaemic penumbra,
- A rationally-designed small molecule NLRP3 inflammasome inhibitor ameliorates cocaine-induced neuroinflammation () - May 2, 2024 - Abstract #AIDS2024AIDS_998;
The embargo on all abstracts, including oral abstract, poster exhibition, e-poster and late breakers, will lift on Tuesday, 23 July 2024, at 10:00 am Central European Summer Time (CEST). If an abstract is part of an official AIDS 2024 press conference that occurs before that time, the embargo on that abstract lifts at the start of the official press conference.
- | Journal: Drugs targeting CMPK2 inhibit pyroptosis to alleviate severe pneumonia caused by multiple respiratory viruses. (Pubmed Central) - May 2, 2024
Z25 and Z08 can reduce the expression level of CMPK2 mRNA and protein, thereby inhibiting NLRP3 and alleviating the development of severe viral pneumonia. In conclusion, the inflammatory response mediated by CMPK2 is the common molecular mechanism of severe pneumonia induced by viral infection, and Z25 and Z08 can effectively alleviate viral infection and severe pneumonia through this mechanism.
- | Journal: Omentin-1 May Be One Treatment Factor for Intravenous Thrombolysis of Acute Cerebral Infarction Through the Inhibition of NLRP3 Ubiquitination by AMPK Function: Preliminary Findings. (Pubmed Central) - May 1, 2024
Omentin-1 reduced neuroinflammation and ROS-induced oxidative stress in the mouse model of ACI, which was achieved by inhibiting NLRP3 ubiquitination through regulating AMPK activity. Therefore, omentin-1 may serve as a treatment factor for the intravenous thrombolysis of ACI in further clinical application.
- | Journal: Novel Isoalantolactone-Based Derivatives as Potent NLRP3 Inflammasome Inhibitors: Design, Synthesis, and Biological Characterization. (Pubmed Central) - Apr 30, 2024
Mechanistically, we demonstrated that 49 covalently bound to cysteine 279 in the NACHT domain of NLRP3, thereby inhibiting the assembly and activation of NLRP3 inflammasome. These results provided compelling evidence to further advance the development of more potent NLRP3 inhibitors based on this scaffold.
- | doxorubicin hydrochloride / Generic mfg.
Journal: Chinese medicinal formula Fu Xin decoction against chronic heart failure by inhibiting the NLRP3/caspase-1/GSDMD pyroptotic pathway. (Pubmed Central) - Apr 30, 2024
These results provided compelling evidence to further advance the development of more potent NLRP3 inhibitors based on this scaffold. FXD exhibits a cardioprotective effect, improving CHF and alleviating pyroptosis by inhibiting the NLRP3/caspase-1/GSDMD pathway.
- | Journal: Safranal exerts a neuroprotective effect on Parkinson's disease with suppression of NLRP3 inflammation activation. (Pubmed Central) - Apr 29, 2024
FXD exhibits a cardioprotective effect, improving CHF and alleviating pyroptosis by inhibiting the NLRP3/caspase-1/GSDMD pathway. Safranal played a neuroprotective effect on the Parkinson's disease and its mechanism was related to the inhibition of NLRP3 inflammasome activation.
- | Journal: Melatonin suppresses TLR4-mediated RSV infection in the central nervous cells by inhibiting NLRP3 inflammasome formation and autophagy. (Pubmed Central) - Apr 29, 2024
Interestingly, blockade of TLR4 or treatment with exogenous melatonin significantly suppressed TLR4 activation as well as TLR4-mediated apoptosis, autophagy and immune responses. Therefore, we infer that melatonin may act on the TLR4 to ameliorate RSV-induced neuronal injury, which provides a new therapeutic target for RSV infection.
- | Journal: Targeting NLRP3 signaling reduces myocarditis-induced arrhythmogenesis and cardiac remodeling. (Pubmed Central) - Apr 29, 2024
Myocarditis may increase the rate of RVOT arrhythmogenesis, possibly through electrical and structural remodeling. These changes may be mitigated by inhibiting NLRP3 signaling.
- | Journal: Clonal Hematopoiesis of Indeterminate Potential With Loss of Tet2 Enhances Risk for Atrial Fibrillation Through Nlrp3 Inflammasome Activation. (Pubmed Central) - Apr 29, 2024
In a mouse model of AF resulting from hematopoietic-specific inactivation of Tet2, we propose altered calcium handling as an arrhythmogenic mechanism, dependent on Nlrp3 inflammasome activation. Our data are in keeping with previous studies of CHIP in cardiovascular disease, and further studies into the therapeutic potential of NLRP3 inhibition for individuals with TET2 CHIP may be warranted.
- | Journal: Dynasore Alleviates LPS-Induced Acute Lung Injury by Inhibiting NLRP3 Inflammasome-Mediated Pyroptosis. (Pubmed Central) - Apr 29, 2024
Dynasore also downregulated the co-expression of F4/80, caspase-1 and GSDMD in lung tissue. Collectively, these findings demonstrated that dynasore could alleviate LPS-induced ALI by regulating macrophage pyroptosis, which might provide a new therapeutic strategy for ALI/ARDS.
- | Preclinical, Journal: hP-MSCs attenuate severe acute pancreatitis in mice via inhibiting NLRP3 inflammasome-mediated acinar cell pyroptosis. (Pubmed Central) - Apr 28, 2024
Our study demonstrates the regularity and important role of acinar cell pyroptosis during SAP. hP-MSCs attenuate inflammation and inhibit acinar cell pyroptosis via suppressing NLRP3 inflammasome activation, thereby exerting a protective effect against SAP.
- | Twymeeg (imeglimin) / Poxel SA, Roivant, Sumitomo Pharma
Journal: Imeglimin attenuates NLRP3 inflammasome activation by restoring mitochondrial functions in macrophages. (Pubmed Central) - Apr 28, 2024
We demonstrated for the first time that imeglimin reduces LPS-induced NLRP3 inflammasome activation by inhibiting mPTP opening in THP-1 macrophages. These results suggest that imeglimin could be a promising new anti-inflammatory agent for treating diabetic complications.
- | Journal: Anti-inflammatory effect of Trichospira verticillata via suppression of the NLRP3 inflammasome in neutrophilic asthma. (Pubmed Central) - Apr 26, 2024
This study demonstrates that TVE modulates the binding of NLPR3 to NEK7, thereby reporting novel insights into the mechanism by which TVE inhibits NLRP3 inflammasome. These findings suggest TVE as a potential therapeutic of NLRP3 inflammasome-mediated diseases, particularly NA.
- | Journal: Porphyran Attenuates Neuronal Loss in the Hippocampal CA1 Subregion Induced by Ischemia and Reperfusion in Gerbils by Inhibiting NLRP3 Inflammasome-Mediated Neuroinflammation. (Pubmed Central) - Apr 26, 2024
Additionally, the pretreatment significantly inhibited the overexpressions of nucleotide-binding domain, leucine-rich-containing family, pyrin domain-containing protein-3 (NLRP3) inflammasome complex, and pro-inflammatory cytokines (interleukin 1 beta and interleukin 18) induced by IR in the CA1 subregion. Overall, our findings suggest that porphyran exerts neuroprotective effects against brain IR injury, potentially by reducing the reaction (activation) and proliferation of microglia and reducing NLRP3 inflammasome-mediated neuroinflammation.
- | Preclinical, Journal: The prevention effect of pulsed electromagnetic fields treatment on senile osteoporosis in vivo via improving the inflammatory bone microenvironment. (Pubmed Central) - Apr 26, 2024
Furthermore, PEMF also dramatically inhibited NLRP3-mediated low-grade inflammation in the bone marrow, i.e. PEMF inhibited the levels of NLRP3, proCaspase1, cleaved Caspase1, IL-1?, and GSDMD-N. The study demonstrated that PEMF could mitigate the aging-induced bone loss and reverses the deterioration of bone microarchitecture probably through inhibiting NLRP3-mediated low-grade chronic inflammation to improve the inflammatory bone microenvironment in aged rats.
- | dexamethasone / Generic mfg.
Preclinical, Journal: Quanzhen Yiqi decoction attenuates inflammation in mice with smoking-induced COPD by activating the Nrf2/HO-1 pathway and inhibiting the NLRP3 inflammasome. (Pubmed Central) - Apr 26, 2024
QZYQ inhibits ROS production and NLRP3 inflammasome activation by upregulating Nrf2 to reduce lung injury. The anti-inflammatory effects of QZYQ are similar to those of DEX.
- | Preclinical, Journal: Polyphenol Extracts from Ziziphus jujuba Mill. "Junzao" Attenuates Ulcerative Colitis by Inhibiting the NLRP3 and MAPKs Signaling Pathways and Regulating Gut Microbiota Homeostasis in Mice. (Pubmed Central) - Apr 26, 2024
The anti-inflammatory effects of QZYQ are similar to those of DEX. PERJ probably inhibits the development of UC by suppressing the NLRP3 and MAPKs signaling pathways and regulating gut microbiota homeostasis, and can be considered as a potential resource for preventing UC.
- | Journal: Melatonin-induced upregulation of telomerase activity interferes with macrophage mitochondrial metabolism and suppresses NLRP3 inflammasome activation in the treatment of Pneumonia. (Pubmed Central) - Apr 26, 2024
Understanding the molecular mechanisms underlying these effects may lead to the development of novel therapeutic strategies targeting mitochondria and NLRP3 inflammasome activation for the management of pneumonia. Further investigations are warranted to fully uncover the therapeutic potential of melatonin and its implications for pneumonia treatment.
- | Journal: Methylmercury induces inflammatory response and autophagy in microglia through the activation of NLRP3 inflammasome. (Pubmed Central) - Apr 24, 2024
In addition, the inhibition of NLRP3 inflammasome alleviated both cellular inflammation and autophagy, while inhibition of autophagy increased cellular inflammation. Our current research suggests that MeHg might induce BV2 cytotoxicity through inflammatory response and autophagy, which may be mediated by the NLRP3 inflammasome activated by oxidative stress.
- | Journal: Nicotine improves DSS-induced colitis by inhibiting NLRP3 and altering gut microbiota. (Pubmed Central) - Apr 24, 2024
Combined in vivo and in vitro investigations demonstrate that nicotine primarily impedes the assembly of NLRP3, subsequently inhibiting downstream IL-1? secretion.
- | Journal: Curcumin attenuates aflatoxin B1-induced ileum injury in ducks by inhibiting NLRP3 inflammasome and regulating TLR4/NF-?B signaling pathway. (Pubmed Central) - Apr 24, 2024
We found that Cur reversed the effects of AFB1 through modulating both NLRP3 inflammasome and the TLR4/NF-?B signaling pathway. In conclusion, AFB1 can induce inflammatory damage and pyroptosis in duck ileum, while Cur has obviously protective effects on all the above damages.
- | Preclinical, Journal: Intranasal Delivery of Mitochondria Attenuates Brain Injury by AMPK and SIRT1/PGC-1? Pathways in a Murine Model of Photothrombotic Stroke. (Pubmed Central) - Apr 24, 2024
signaling pathway. Thus, intranasal delivery of mitochondria might be considered a new therapeutic strategy for ischemic stroke treatment.
- | MG132 / Jilin University, Dorothy M. Davis Heart and Lung Research Institute
Journal: Dicoumarol attenuates NLRP3 inflammasome activation to inhibit inflammation and fibrosis in knee osteoarthritis. (Pubmed Central) - Apr 23, 2024
Mechanistic studies demonstrated that dicoumarol did not affect NF??B signaling, but it did directly interact with NOD?like receptor protein 3 (NLRP3) to promote its protein degradation, which could be reversed by MG132, but not NH4Cl...Furthermore, the inflammation and fibrosis of the knee joints were inhibited in rats. In conclusion, the present findings demonstrated that dicoumarol could impede the progression of KOA by inhibiting NLRP3 activation, providing a potential treatment strategy for KOA.
- | febuxostat / Generic mfg.
Journal: Febuxostat attenuates secondary brain injury caused by cerebral hemorrhage through inhibiting inflammatory pathways. (Pubmed Central) - Apr 22, 2024
By inhibiting the NLRP3 inflammasome, preconditioning Feb attenuates inflammatory injury after ICH. Our findings may provide new insights into the role of Feb in neuroprotection.
- | Journal: Design, synthesis and biological evaluation of tanshinone IIA derivatives as NLRP3 inflammasome inhibitors. (Pubmed Central) - Apr 22, 2024
In addition, treatment with T10 significantly attenuated inflammatory response in DSS-induced peritonitis. Our work describes a potential tanshinone-based derivative, which needs to be further structurally optimized as NLRP3 inflammasome inhibitors for treating inflammatory disorders.
- | Bay11-7082 / Bayer
Preclinical, Journal: MG53 protects against Coxsackievirus B3-induced acute viral myocarditis in mice by inhibiting NLRP3 inflammasome-mediated pyroptosis via the NF-?B signaling pathway. (Pubmed Central) - Apr 22, 2024
In conclusion, our results suggest that MG53 acts as a negative regulator of NLRP3 inflammasome-mediated pyroptosis in CVB3-induced AVMC, partially by inhibiting the NF-?B signaling pathway. MG53 is a promising candidate for clinical applications in AVMC treatment.
- | Preclinical, Journal: Integrated Proteomics Characterization of NLRP3 Inflammasome Inhibitor MCC950 in Monocytic Cell Line Confirms Direct MCC950 Engagement with Endogenous NLRP3. (Pubmed Central) - Apr 22, 2024
Further cCETSA (c indicates compressed) in live cells mapped the stabilization of NLRP3 inflammasome pathway proteins, highlighting modulation of the targeted pathway. This is the first evidence of direct MCC950 engagement with endogenous NLRP3 in a human macrophage cellular system using discovery proteomics chemical biology techniques, providing critical information for inflammasome studies.
- | Journal: Cucurbitacin B attenuates osteoarthritis development by inhibiting NLRP3 inflammasome activation and pyroptosis through activating Nrf2/HO-1 pathway. (Pubmed Central) - Apr 20, 2024
This action is further mediated through the activation of the Nrf2/HO-1 pathway to inhibit NF-?B/NLRP3 inflammasome activation. Thus, CuB is a potential therapeutic agent for OA.
- | Journal: Phillygenin Alleviates Arthritis through the Inhibition of the NLRP3 Inflammasome and Ferroptosis by AMPK. (Pubmed Central) - Apr 19, 2024
These findings suggest that Phillygenin may be a potential therapeutic target for preventing arthritis by inhibiting NLRP3 inflammasome and Ferroptosis through AMPK. This indicates that Phillygenin could have disease-modifying effects on arthritis.
- | Journal: Potential Common Mechanisms of Cytotoxicity Induced by Organophosphorus Pesticides via NLRP3 Inflammasome Activation. (Pubmed Central) - Apr 19, 2024
Furthermore, the common molecular mechanism of NLRP3-OPPs was clarified by the presence of toxicity effector groups (benzene ring, nitrogen/oxygen-containing functional group); =O, -O-, or =S (active) groups; and combination residues (Gly271, Asp272). This finding provided valuable insights into exploring the common mechanisms of multiple threats and developing effective therapeutic strategies to prevent OPPs poisoning.
- | Journal: SWI/SNF complex-mediated chromatin remodeling in Candida glabrata promotes immune evasion. (Pubmed Central) - Apr 18, 2024
production, underscoring NF-?B signaling's role in fungal diseases. Altogether, our findings directly link the nucleosome positioning-based chromatin remodeling to fungal immunomodulatory molecule expression.
- | methamphetamine / Generic mfg.
Preclinical, Journal: Methamphetamine Enhancement of HIV-1 gp120-Mediated NLRP3 Inflammasome Activation and Resultant Proinflammatory Responses in Rat Microglial Cultures. (Pubmed Central) - Apr 17, 2024
The Meth-associated effects were attenuated or blocked by MCC950, an NLRP3 inhibitor, or Mito-TEMPO, a mitochondrial superoxide scavenger. These results suggest that Meth enhances gp120-associated microglial NLRP3 activation and the resultant proinflammatory responses via mitochondria-dependent signaling.
- | Journal: Fluoride induces pyroptosis via IL-17A-mediated caspase-1/11-dependent pathways and Bifidobacterium intervention in testis. (Pubmed Central) - Apr 17, 2024
In summary, this study uncovers the mechanism underlying fluorine-induced testicular pyroptosis and illustrates the novel protecting feature of Bifidobacterium against fluoride-induced harm to male reproduction, along with its potential regulatory mechanism. These results provide fresh perspectives on treating male reproductive dysfunction resulting from fluoride or other environmental toxins.
- | Preclinical, Journal, IO biomarker: Nerolidol rescues hippocampal injury of diabetic rats through inhibiting NLRP3 inflammasome and regulation of MAPK/AKT pathway. (Pubmed Central) - Apr 16, 2024
Furthermore, we suggest that nerolidol may inhibit NLRP3 inflammasome and affected the expression of MAPK and AKT. These findings provide a new experimental basis for the use of nerolidol to ameliorate diabetes-induced brain tissue damage and the associated disease.
- | Journal: Isoliquiritigenin reduces experimental autoimmune prostatitis by facilitating Nrf2 activation and suppressing the NLRP3 inflammasome pathway. (Pubmed Central) - Apr 15, 2024
These findings provide a new experimental basis for the use of nerolidol to ameliorate diabetes-induced brain tissue damage and the associated disease. Isoliquiritigenin reduced experimental autoimmune prostatitis by facilitating Nrf2 activation and suppressing the NLRP3 inflammasome pathway.
- | Journal: Discovery of novel biphenyl-sulfonamide analogues as NLRP3 inflammasome inhibitors. (Pubmed Central) - Apr 15, 2024
The results in a mouse acute peritonitis model revealed that H28 effectively inhibit the NLRP3 inflammasome pathway, demonstrating their anti-inflammatory properties. Our findings strongly support the further development of H28 as potential lead compound for treating NLRP3-related diseases.
- | Journal: Sodium butyrate alleviates experimental autoimmune prostatitis by inhibiting oxidative stress and NLRP3 inflammasome activation via the Nrf2/HO-1 pathway. (Pubmed Central) - Apr 15, 2024
NaB treatment can alleviates prostatic inflammation and pelvic pain associated with EAP by inhibiting oxidative stress and NLRP3 inflammasome activation via the Nrf2/HO-1 pathway. NaB has the potential as an effective agent in the treatment of EAP.
- | Journal: Gegen Qinlian decoction ameliorates TNBS-induced ulcerative colitis by regulating Th2/Th1 and Tregs/Th17?cells balance, inhibiting NLRP3 inflammasome activation and reshaping gut microbiota. (Pubmed Central) - Apr 15, 2024
NaB has the potential as an effective agent in the treatment of EAP. GQD might alleviate TNBS-induced UC via regulating Th2/Th1 and Tregs/Th17 cells Balance, inhibiting NLRP3 inflammasome and reshaping gut microbiota, which may provide a novel strategy for patients with colitis.
- | Journal: Morinda officinalis polysaccharides inhibit the expression and activity of NOD-like receptor thermal protein domain associated protein 3 in inflammatory periodontal ligament cells by upregulating silent information regulator sirtuin 1. (Pubmed Central) - Apr 14, 2024
Meanwhile, the acetylation level of NLRP3 reduced through deacetylation, leading to the decreased activity of NLRP3. Thus, MOP acted as inflammatory suppressor.
- | Journal: Ascorbyl palmitate ameliorates inflammatory diseases by inhibition of NLRP3 inflammasome. (Pubmed Central) - Apr 10, 2024
Moreover, AP showed more significant preventive effects than AA in LPS-induced systemic inflammation, dextran sulfate sodium (DSS)-induced colitis and experimental autoimmune encephalomyelitis (EAE). Thus, our results suggest that AP is a potential therapeutic combating NLRP3-driven diseases.
- | dapansutrile (OLT1177) / Olatec Therap
Journal: The NLRP3 inhibitor, OLT1177 attenuates brain injury in experimental intracerebral hemorrhage. (Pubmed Central) - Apr 10, 2024
OLT1177 (dapansutrile) could significantly attenuate the brain edema after ICH and effectively alleviate the neurological deficit. This result suggests that the novel NLRP3 inhibitor, OLT1177, might serve as a promising candidate for the treatment of ICH.
- | Journal: Salmonella Enteritidis antitoxin DinJ inhibits NLRP3-dependent canonical inflammasome activation in macrophages. (Pubmed Central) - Apr 10, 2024
and IL-18 in vivo, contributing to S. Enteritidis evading host immune clearance. In summary, our findings provide insights into the role of DinJ in modulating the inflammasome response during S. Enteritidis infection, highlighting its impact on inhibiting inflammasome activation and immune evasion.
- | Journal: Phospholipid transfer protein ameliorates sepsis-induced cardiac dysfunction through NLRP3 inflammasome inhibition. (Pubmed Central) - Apr 8, 2024
Moreover, PLTP could bind to NLRP3 and negatively regulate the activity of the NLRP3 inflammasome/GSDMD signal pathway. This study demonstrated that PLTP can ameliorate SICD by inhibiting inflammatory responses and cardiomyocyte pyroptosis by blocking the activation of the NLRP3 inflammasome/GSDMD signaling pathway.
- | dexamethasone / Generic mfg.
Journal: DT-13 attenuates inflammation by inhibiting NLRP3-inflammasome related genes in RAW264.7 macrophages. (Pubmed Central) - Apr 8, 2024
In comparison to the existing anti-inflammatory drug, dexamethasone, and triterpenoid saponin Rk1, DT-13 more efficiently inhibits inflammation in the applied cell culture model. Therefore, DT-13 may serve as a lead compound for the development of new more effective anti-inflammatory drugs with minimised side effects.
- | Journal: MicroRNA-7 Attenuates Secondary Brain Injury Following Experimental Intracerebral Hemorrhage via Inhibition of NLRP3. (Pubmed Central) - Apr 8, 2024
Therefore, DT-13 may serve as a lead compound for the development of new more effective anti-inflammatory drugs with minimised side effects. The miR-7 suppressed NLRP3 expression in microglia/macrophage to reduce the production of inflammatory cytokines, leading to conducting certain neuroprotection post-ICH in rats.