预约演示

更新于：2025-05-07

RXRs x NF-κB x PPAR x MAPK

更新于：2025-05-07

基本信息

关联

项与 RXRs x NF-κB x PPAR x MAPK 相关的药物

Forsythiaside A

连翘苷A

靶点

MAPK x NF-κB x PPAR x RXRs

作用机制

MAPKs抑制剂 [+3]

在研机构

成都中医药大学

原研机构-

在研适应症

急性肺损伤 [+1]

非在研适应症-

最高研发阶段临床前

首次获批国家/地区-

首次获批日期1800-01-20

100 项与 RXRs x NF-κB x PPAR x MAPK 相关的临床结果

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100 项与 RXRs x NF-κB x PPAR x MAPK 相关的转化医学

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0 项与 RXRs x NF-κB x PPAR x MAPK 相关的专利（医药）

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项与 RXRs x NF-κB x PPAR x MAPK 相关的文献（医药）

2023-11-17·Medicine

Network pharmacology-based research on the effect of Scutellaria baicalensis on osteosarcoma and the underlying mechanism

Article

作者: Tian, Yushi ; Fan, Heng ; Wang, Jingbo ; Deng, Shuangjiao ; Zhang, Lijuan

To explore the anti-tumor effects of Scutellaria baicalensis on osteosarcoma and its mechanism. Network pharmacology and molecular docking techniques were applied to investigate the effect and mechanism of Scutellaria baicalensis on osteosarcoma (OS). We analyzed the protein-protein interaction (PPI) network for potential targets of Scutellaria baicalensis for treating osteosarcoma and identified hub targets. We used KM curves to screen for hub targets that could effectively prolong the survival time of OS patients. We systematically performed gene ontology (GO) and Kyoto encyclopedia of genes and genomes (KEGG) enrichment analysis of the Scutellaria baicalensis potential targets and predicted the Scutellaria baicalensis molecular mechanism and function in treating osteosarcoma. Through molecular docking, the binding process between the hub targets, which could prolong the survival time of sarcoma patients, and Scutellaria baicalensis was simulated. PPI network analysis of potential therapeutic targets discriminated 12 hub targets. The KM curves of the hub targets showed that upregulation of RXRA, RELA, ESR1, TNF, IL6, IL1B, and RB1 expression, and downregulation of MAPK1, VEGFA, MAPK14, CDK1, and PPARG expression were effective in improving the 5-year survival rate of OS patients. GO and KEGG enrichment demonstrated that Scutellaria baicalensis regulated multiple signaling pathways of OS. Molecular docking results indicated that Scutellaria baicalensis could bind freely to the above hub target, which could prolong the survival time of sarcoma patients. Scutellaria baicalensis acted on osteosarcoma by regulating a signaling network formed by hub targets connecting multiple signaling pathways. Scutellaria baicalensis appears to have the potential to serve as a therapeutic drug for osteosarcoma and to prolong the survival of OS patients.

2023-03-01·Current Drug Targets

Protective Roles and Mechanism of Action of Plant Flavonoids against Hepatic Impairment: Recent Developments

Article

作者: Boniface, Pone Kamdem ; Paumo, Hugues Kamdem ; Katata-Seru, Lebogang Maureen ; Fabrice, Fekam Boyom

Background:The liver is one of the crucial organs in humans and is responsible for the regulation of diverse processes, including metabolism, secretion, and detoxification. Ingestion of alcohol and drugs, environmental pollutants, and irradiation are among the risk factors accountable for oxidative stress in the liver. Plant flavonoids have the potential to protect the liver from damage caused by a variety of chemicals.Objective:The present study aims to summarize up-to-date information on the protective roles of plant flavonoids against liver damage.Methodology:The literature information on the hepatoprotective plant flavonoids was assessed through various databases, which were searched from their respective inception until March 2022.Results:More than 70 flavonoids with hepatoprotective activity against a variety of models of liver toxicity have been reported across the literature. Among these are flavones (19), flavonols (30), flavanones (9), isoflavonoids (5), and biflavonoids (2). Several hepatoprotective mechanisms of action were reported in various classes of flavonoids, including flavones and flavonols (upregulation of the pro-survival ERK1/2 pathway; downregulation of apoptotic proteins, including Bax, Bcl-2, Bax, BH3, caspase-3, 8, 9, etc.), flavanones (downregulation of NF-κB, TNF-α, IL-1 β, IL-6, iNOS, etc.), isoflavonoids (downregulation of lipogenesis genes, such as SREBP-1c, LXRα, RXRα, PPARγ and ACC2, with concomitant upregulation of genes involved in β-oxidation, including AMPK and PPARα; inhibition of CYPs, such as CYP1A1, CYP1A2, CYP2B1, CYP2D6, CYP2E1 and CYP3A1/2).Conclusion:The present work demonstrated the effectiveness of plant flavonoids against hepatic damage. However, more studies need to be performed regarding the cytotoxicity, pharmacokinetics, and mechanisms of action of these very important cytoprotective flavonoids.

2023-01-01·Pharmacological Research

Anti-inflammatory effects and improved metabolic derangements in ob/ob mice by a newly synthesized prenylated benzopyran with pan-PPAR activity

Article

作者: Duplan, Isabelle ; Vila, Laura ; Piqueras, Laura ; Enriz, Ricardo D ; Staels, Bart ; Cabedo, Nuria ; Garibotto, Francisco ; Collado, Aida ; Marques, Patrice ; Hennuyer, Nathalie ; García, Ainhoa ; Villarroel-Vicente, Carlos ; Dacquet, Catherine ; Cortes, Diego ; Sanz, María-Jesús

BACKGROUND AND PURPOSESelective peroxisome proliferator-activated receptors (PPARs) are widely used to treat metabolic complications; however, the limited effect of PPARα agonists on glucose metabolism and the adverse effects associated with selective PPARγ activators have stimulated the development of novel pan-PPAR agonists to treat metabolic disorders. Here, we synthesized a new prenylated benzopyran (BP-2) and evaluated its PPAR-activating properties, anti-inflammatory effects and impact on metabolic derangements.EXPERIMENTAL APPROACHBP-2 was used in transactivation assays to evaluate its agonism to PPARα, PPARβ/δ and PPARγ. A parallel-plate flow chamber was employed to investigate its effect on TNFα-induced leukocyte-endothelium interactions. Flow cytometry and immunofluorescence were used to determine its effects on the expression of endothelial cell adhesion molecules (CAMs) and chemokines and p38-MAPK/NF-κB activation. PPARs/RXRα interactions were determined using a gene silencing approach. Analysis of its impact on metabolic abnormalities and inflammation was performed in ob/ob mice.KEY RESULTSBP-2 displayed strong PPARα activity, with moderate and weak activity against PPARβ/δ and PPARγ, respectively. In vitro, BP-2 reduced TNFα-induced endothelial ICAM-1, VCAM-1 and fractalkine/CX₃CL1 expression, suppressed mononuclear cell arrest via PPARβ/δ-RXRα interactions and decreased p38-MAPK/NF-κB activation. In vivo, BP-2 improved the circulating levels of glucose and triglycerides in ob/ob mice, suppressed T-lymphocyte/macrophage infiltration and proinflammatory markers in the liver and white adipose tissue, but increased the expression of the M2-like macrophage marker CD206.CONCLUSION AND IMPLICATIONSBP-2 emerges as a novel pan-PPAR lead candidate to normalize glycemia/triglyceridemia and minimize inflammation in metabolic disorders, likely preventing the development of further cardiovascular complications.

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