ArticleBritish journal of pharmacology2018
Liver kinase B1/AMP-activated protein kinase-mediated regulation by gentiopicroside ameliorates P2X7 receptor-dependent alcoholic hepatosteatosis.
Article in British journal of pharmacology, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 39 papers.
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Who cites it
39 citing papers in PubMed, 94 citations in OpenAlex.
- Gentiopicroside alleviates depression-like symptoms in animal models through regulating COX-2-mediated autophagy and inflammation.Metabolic brain disease · 2026Article
- Article
- Gentiopicroside alleviates neuroinflammation in Parkinson's disease by mediating microglial pyroptosis via the NF-κB/NLRP3/GSDMD pathway.Histology and histopathology · 2025Article
- Gentianaceae Family-Derived Bioactive Compounds-Therapeutic Values and Supporting Role in Inflammation and Detoxification.Nutrients · 2025Review
- Gentiopicroside improves DSS-induced ulcerative colitis and secondary liver injury in mice by enhancing the intestinal barrier and regulating the gut microbiome.Scientific reports · 2025Article
- Gentiopicroside ameliorates psoriasis-like skin lesions in mice via regulating the Keap1-Nrf2 pathway and inhibiting keratinocyte activation.Acta pharmacologica Sinica · 2025Article
- Comprehensive insights into potential roles of purinergic P2 receptors on diseases: Signaling pathways involved and potential therapeutics.Journal of advanced research · 2025Review
- The chemical structure, pharmacological activity, and clinical progress of Gentianae Radix et Rhizoma.Frontiers in pharmacology · 2025Review
- Combination of Formononetin and Sulforaphane Natural Drug Repress the Proliferation of Cervical Cancer Cells via Impeding PI3K/AKT/mTOR Pathway.Applied biochemistry and biotechnology · 2024Article
- The significance of lipid metabolism reprogramming of tumor-associated macrophages in hepatocellular carcinoma.Cancer immunology, immunotherapy : CII · 2024Review
- Gentiopicroside improves non-alcoholic steatohepatitis by activating PPARα and suppressing HIF1.Frontiers in pharmacology · 2024Article
- Gentiopicroside-An Insight into Its Pharmacological Significance and Future Perspectives.Cells · 2023Review
- A Study of Gentianae Radix et Rhizoma Class Differences Based on Chemical Composition and Core Efficacy.Molecules (Basel, Switzerland) · 2023Article
- Gentiopicroside alleviates acute myocardial infarction injury in rats by disrupting Nrf2/NLRP3 signaling.Experimental biology and medicine (Maywood, N.J.) · 2023Article
- Gentiopicroside modulates glucose homeostasis in high-fat-diet and streptozotocin-induced type 2 diabetic mice.Frontiers in pharmacology · 2023Article
- The role of liver kinase B1 in tumor progression through regulation of lipid metabolism.Clinical & translational oncology : official publication of the Federation of Spanish Oncology Societies and of the National Cancer Institute of Mexico · 2022Review
- Gentiopicroside targets PAQR3 to activate the PI3K/AKT signaling pathway and ameliorate disordered glucose and lipid metabolism.Acta pharmaceutica Sinica. B · 2022Article
- NMR, LC-MS Characterization ofMolecules (Basel, Switzerland) · 2022Article
- Pharmacological effects of Chinese medicine modulating NLRP3 inflammasomes in fatty liver treatment.Frontiers in pharmacology · 2022Review
- The AMPK pathway in fatty liver disease.Frontiers in physiology · 2022Review
Corrections and comments
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Authors and funding
10 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposeRegulating P2X7 receptor-mediated activation of NLRP3 inflammasomes could be a therapeutic strategy to treat alcoholic hepatosteatosis. We investigated whether this process was modulated by gentiopicroside, the main active secoiridoid glycoside from Gentiana manshurica Kitagawa. EXPERIMENTAL APPROACH: In vivo models of acute and chronic alcoholic hepatosteatosis were established by intragastrically administered ethanol or using chronic plus binge ethanol feeding of Lieber-DeCarli liquid diet to male C57BL/6 mice. In vitro, HepG2 cells were treated with ethanol. RAW 264.7 macrophages and murine bone marrow-derived macrophages (BMDMs) were stimulated with LPS and ATP. KEY
resultsIn both the acute and chronic alcohol-induced mouse hepatosteatosis models, gentiopicroside decreased serum aminotransferases and triglyceride accumulation. Up-regulated SREBP1, down-regulated PPARα and phosphorylated acetyl-CoA carboxylase caused by acute and chronic alcohol feeding were modulated by gentiopicroside, through the elevation of LKB1 and AMPK. Suppression of P2X7 receptor-NLRP3 activation by gentiopicroside inhibited IL-1β production. In ethanol-exposed HepG2 cells, gentiopicroside reduced lipogenesis and promoted lipid oxidation via activation of P2X7 receptor-NLRP3 inflammasomes. Genetic or pharmacological blockade of P2X7 receptors enhanced AMPK activity and reduced SREBP1 expression in ethanol-treated HepG2 cells. Gentiopicroside down-regulated P2X7 receptor-mediated inflammatory responses in LPS/ATP-stimulated RAW 264.7 macrophages and BMDMs. IL-1β from macrophages accelerated lipid accumulation in hepatocytes. Depleting macrophages by clodronate liposomes ameliorated alcoholic hepatosteatosis, and it was further alleviated by gentiopicroside. CONCLUSIONS AND IMPLICATIONS: Activation of LKB1/AMPK signalling by gentiopicroside was mediated by the P2X7 receptor-NLRP3 inflammasome, suggesting the therapeutic value of blocking P2X7 receptors in the treatment of alcoholic hepatosteatosis.
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