Flavonoids of Euphorbia hirta inhibit inflammatory mechanisms via Nrf2 and NF-κB pathways.

IF 1.8 4区 生物学 Q4 BIOCHEMISTRY & MOLECULAR BIOLOGY Cell Biochemistry and Biophysics Pub Date : 2024-11-06 DOI:10.1007/s12013-024-01551-y
Xiaolin Bai, Lijun Li, Yuning Wu, Bai Jie
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Abstract

Euphorbia hirta has anti-inflammatory effects in traditional medicine, but its anti-inflammatory mechanism has not been explored at the cellular and molecular levels. To unravel these mechanisms, the main active components in the 65 and 95% ethanol extracts of Euphorbia hirta were first identified by UPLC-Q-TOF/MS. Subsequently, potential anti-inflammatory targets and signaling pathways were predicted using network pharmacology and experimentally validated using RT-PCR and flow cytometry in a lipopolysaccharide (LPS)-induced inflammation model of RAW264.7 cells. The results revealed flavonoids as the key active components. Network pharmacology uncovered 71 potential anti-inflammation targets, with a protein-protein interaction (PPI) network highlighting 8 cores targets, including IL-6, TNF, NFκB and Nrf2 et al. Furthermore, Euphorbia hirta exerts anti-inflammation effects through modulation of Nrf2 and NF-κB signaling pathways. Specifically, the 65% ethanol extract of Euphorbia hirta (EE65) and quercitrin (HPG) exerted anti-inflammatory activity by inhibiting the expression of inflammatory genes associated with the NF-κB signaling pathway, whereas baicalein (HCS) suppressed cellular inflammation by promoting Nrf2-mediated antioxidant gene expression and enhancing apoptosis of inflammatory cells. The results of the study suggest that Euphorbia hirta has potential for the development of anti-inflammatory drugs.

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大戟的黄酮类化合物通过 Nrf2 和 NF-κB 途径抑制炎症机制
在传统医学中,大戟具有抗炎作用,但其抗炎机制尚未在细胞和分子水平上得到探索。为了揭示这些机制,首先利用 UPLC-Q-TOF/MS 方法鉴定了大戟科植物 65% 和 95% 乙醇提取物中的主要活性成分。随后,利用网络药理学预测了潜在的抗炎靶点和信号通路,并在脂多糖(LPS)诱导的 RAW264.7 细胞炎症模型中利用 RT-PCR 和流式细胞仪进行了实验验证。结果显示黄酮类化合物是关键的活性成分。网络药理学发现了 71 个潜在的抗炎靶点,其中蛋白相互作用(PPI)网络突出了 8 个核心靶点,包括 IL-6、TNF、NFκB 和 Nrf2 等。具体来说,Euphorbia hirta 的 65% 乙醇提取物(EE65)和槲皮素(HPG)通过抑制与 NF-κB 信号通路相关的炎症基因的表达来发挥抗炎活性,而黄芩苷(HCS)则通过促进 Nrf2 介导的抗氧化基因表达和增强炎症细胞的凋亡来抑制细胞炎症。研究结果表明,大戟具有开发抗炎药物的潜力。
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来源期刊
Cell Biochemistry and Biophysics
Cell Biochemistry and Biophysics 生物-生化与分子生物学
CiteScore
4.40
自引率
0.00%
发文量
72
审稿时长
7.5 months
期刊介绍: Cell Biochemistry and Biophysics (CBB) aims to publish papers on the nature of the biochemical and biophysical mechanisms underlying the structure, control and function of cellular systems The reports should be within the framework of modern biochemistry and chemistry, biophysics and cell physiology, physics and engineering, molecular and structural biology. The relationship between molecular structure and function under investigation is emphasized. Examples of subject areas that CBB publishes are: · biochemical and biophysical aspects of cell structure and function; · interactions of cells and their molecular/macromolecular constituents; · innovative developments in genetic and biomolecular engineering; · computer-based analysis of tissues, cells, cell networks, organelles, and molecular/macromolecular assemblies; · photometric, spectroscopic, microscopic, mechanical, and electrical methodologies/techniques in analytical cytology, cytometry and innovative instrument design For articles that focus on computational aspects, authors should be clear about which docking and molecular dynamics algorithms or software packages are being used as well as details on the system parameterization, simulations conditions etc. In addition, docking calculations (virtual screening, QSAR, etc.) should be validated either by experimental studies or one or more reliable theoretical cross-validation methods.
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