ArticleScientific reports2015
Rhein antagonizes P2X7 receptor in rat peritoneal macrophages.
Article in Scientific reports, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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Who cites it
20 citing papers in PubMed, 29 citations in OpenAlex.
- P2X7 receptors promote atrial remodeling and atrial fibrillation susceptibility via reactive oxygen species-mediated mitogen-activated protein kinase signaling activation.Journal of cell communication and signaling · 2026Article
- Role of the P2X7 receptor in breast cancer progression.Purinergic signalling · 2025Review
- Adenosine triphosphate-induced cell death in heart failure: Is there a link?World journal of cardiology · 2025Review
- Fibromodulin selectively accelerates myofibroblast apoptosis in cutaneous wounds by enhancing interleukin 1β signaling.Nature communications · 2025Article
- Molecular and metabolic landscape of adenosine triphosphate-induced cell death in cardiovascular disease.World journal of cardiology · 2024Review
- Review
- Super-resolution microscopy reveals nanoscale architecture and regulation of podosome clusters in primary macrophages.iScience · 2022Article
- Effects of Anthraquinones on Immune Responses and Inflammatory Diseases.Molecules (Basel, Switzerland) · 2022Review
- Temperature and pH Stability of Anthraquinones from NativeFoods (Basel, Switzerland) · 2022Article
- Article
- Purinergic receptor ligands: the cytokine storm attenuators, potential therapeutic agents for the treatment of COVID-19.Immunopharmacology and immunotoxicology · 2021Review
- Antagonism of the ATP-gated P2X7 receptor: a potential therapeutic strategy for cancer.Purinergic signalling · 2021Review
- Targeting P2 receptors in purinergic signaling: a new strategy of active ingredients in traditional Chinese herbals for diseases treatment.Purinergic signalling · 2021Review
- Anti-inflammatory Effects and Mechanisms of Rhein, an Anthraquinone Compound, and Its Applications in Treating Arthritis: A Review.Natural products and bioprospecting · 2020Review
- P2X7 Receptors Regulate Phagocytosis and Proliferation in Adult Hippocampal and SVZ Neural Progenitor Cells: Implications for Inflammation in Neurogenesis.Stem cells (Dayton, Ohio) · 2018Article
- Immune regulation effect of lienal polypeptides extract in Lewis lung carcinoma-bearing mice treated with cyclophosphamide.Experimental biology and medicine (Maywood, N.J.) · 2018Article
- CD38 Is Robustly Induced in Human Macrophages and Monocytes in Inflammatory Conditions.Frontiers in immunology · 2018Article
- Systemic blockade of P2X7 receptor protects against sepsis-induced intestinal barrier disruption.Scientific reports · 2017Article
- Rhein exhibits antioxidative effects similar to Rhubarb in a rat model of traumatic brain injury.BMC complementary and alternative medicine · 2017Article
- Anthraquinones and Derivatives from Marine-Derived Fungi: Structural Diversity and Selected Biological Activities.Marine drugs · 2016Review
Corrections and comments
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Authors and funding
8 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
P2X7 receptor plays important roles in inflammation and immunity, and thereby it serves as a potential therapeutic target for inflammatory diseases. Rhein, an anthraquinone derivative, exhibits significant anti-inflammatory and immunosuppressive activities in therapy. However, the underlying mechanisms are largely unclear. Here, we aimed to investigate the effects of rhein on P2X7 receptor-mediated responses in vitro. In HEK293 cells expressing rat P2X7 receptor, we first found that rhein concentration-dependently blocked ATP-induced cytosolic calcium concentration ([Ca(2+)]c) elevation and pore formation of the plasma membrane, two hallmarks of the P2X7 receptor activation. These two inhibitory effects of rhein were also observed in rat peritoneal macrophages. Furthermore, rhein counteracted macrophage phagocytosis attenuation and suppressed reactive oxygen species (ROS) production triggered by ATP/BzATP. Meanwhile, rhein reduced ATP/BzATP-induced IL-1β release in lipopolysaccharide-activated macrophages. Prolonged application of ATP caused macrophage apoptosis, while the presence of rhein suppressed this cell cytotoxicity. Such ATP/BzATP-induced cellular reactions were also inhibited by a well-known rat P2X7 receptor antagonist, brilliant blue G, in a similar way to rhein. Together, our results demonstrate that rhein inhibit ATP/BzATP-induced [Ca(2+)]c increase, pore formation, ROS production, phagocytosis attenuation, IL-1β release and cell apoptosis by antagonizing the P2X7 receptor in rat peritoneal macrophages.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.