ReferenceID 5913

Oridonin ameliorates acetaminophen-induced acute liver injury through ATF4/PGC-1α pathway

Drug Dev Res

Acetaminophen (APAP) overdose-induced acute liver injury (ALI) causes hepatocyte cell death, oxidative stress, and inflammation. Oridonin (Ori), a covalent NLRP3-inflammasome inhibitor, ameliorates APAP-induced ALI throu

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Reference Id
5913
Evidence Id
22503
Core Evidence Id
22503
Source Reference Id
5082
Herb2 Reference Id
HBREF005879
Subject Paper Key
HBIN038254_36567664
Pubmed Id
36567664
Doi
10.1002/ddr.22024
Paper Title
Oridonin ameliorates acetaminophen-induced acute liver injury through ATF4/PGC-1α pathway
Paper Abstract
Acetaminophen (APAP) overdose-induced acute liver injury (ALI) causes hepatocyte cell death, oxidative stress, and inflammation. Oridonin (Ori), a covalent NLRP3-inflammasome inhibitor, ameliorates APAP-induced ALI through an unclear molecular mechanism. This study found that Ori decreased hepatic cytochrome P450 2E1 level and increased glutathione content to prevent APAP metabolism, and then reduced the necrotic area, improved liver function, and inhibited APAP-induced proinflammatory cytokines and oxidative stress. Ori also decreased activating transcription factor 4 (ATF4) protein levels and increased peroxisome proliferator-activated receptor-γ coactivator-1α (PGC-1α) to reduce APAP-induced endoplasmic reticulum stress activation and mitochondrial dysfunction. Furthermore, western blot and luciferase assay found that ATF4 inhibited transcription in the PGC-1α promoter -507 to -495 region to reduce PGC-1α levels, while ATF4 knockdown neutralized the hepatoprotective effect of Ori. Molecular docking showed that Ori bound to ATF4's amino acid residue glutamate 302 through 6, 7, and 18 hydroxyl bands. Our findings demonstrated that Ori prevented metabolic activation of APAP and further inhibited the ATF4/PGC-1α pathway to alleviate APAP overdose-induced hepatic toxicity, which illuminated its potential therapeutic effects on ALI.
Journal
Drug Dev Res
Publish Year
2022
Experiment Subject
Experiment Type
Animal Experiment
Phenotype Related
Acute Liver Injury; Inflammation; Hepatocyte Cell Death; Mitochondrial Dysfunction
Paper Title Cn
Paper Title En
Oridonin ameliorates acetaminophen-induced acute liver injury through ATF4/PGC-1α pathway
Bilingual Status
semi_complete