Search Results (51)

Idesia polycarpa is a multipurpose tree species valued for both fruit production and timber and is often referred to as a “beautiful oil reservoir on trees”. However, research has largely focused on fruits, whereas the metabolic composition and potential value of other tissues, such as leaves and shoot tips, remain insufficiently characterized. Here, we employed UPLC–MS/MS-based untargeted metabolomics to compare metabolite profiles and functional components between the leaves and shoot tips of I. polycarpa. In total, 378 differential metabolites were identified, with 105 significantly upregulated in leaves and 273 significantly upregulated in shoot tips. Among these, 32 metabolites were detected exclusively in shoot tips, and 22 were unique to leaves. Leaves were enriched in secondary metabolites, particularly flavonoids and phenolic acids, with scutellarin and catechol as representative compounds. In contrast, shoot tips exhibited higher levels of primary metabolites, including nucleotides and their derivatives as well as amino acids, with catechin and epicatechin being representative compounds. In addition, targeted metabolomics was performed to quantify 53 flavonoids in leaves; scutellarin (2088.1350 μg/g) and apigenin-7-O-glucuronide (1020.9085 μg/g) showed the highest concentrations. Collectively, these results reveal tissue-specific metabolic characteristics in I. polycarpa and provide a data basis for future functional studies and the comprehensive utilization of leaves and shoot tips. Full article

This paper aimed to optimize the ultra-high-pressure extraction process of flavonoids from guanxiang leaves, evaluate their antioxidant capacity, and identify the flavonoids. Methods: Guanxiang leaves were used as the raw material. The extraction process was optimized through single-factor experiments and a response surface methodology. Ascorbic acid (Vc) was employed as a positive control, and the in vitro antioxidant activity of flavonoids was assessed by determining the DPPH radical-scavenging rate, ABTS radical-scavenging rate, and FRAP ferric-reducing ability. Results: The optimal extraction conditions were determined as follows: ethanol concentration of 50%, solid-to-liquid ratio of 1:60 (g/mL), extraction pressure of 300 MPa, and pressure-holding time of 3 min. Under these conditions, the yield of guanxiang leaf flavonoids was found to be 2.21%, better than the solvent extraction method (1.94%). The antioxidant test results indicated that the IC₅₀ values of the extract from the ultra-high-pressure treatment of guanxiang leaves were 11.8 and 50.72 μg·mL⁻¹ on DPPH and ABTS scavenging, which were lower than those of the solvent’s extract (13.40 and 54.29 μg·mL⁻¹). Moreover, the antioxidant ability could also be confirmed by Fe³⁺ ion reduction. Mass spectrometry results indicate that ultra-high-pressure extraction can yield components such as spiraeoside, scutellarin, luteolin, and nepetin, which are not present in solvent extraction methods. Conclusions: Therefore, the ultra-high-pressure extraction method can help to improve the flavonoid yield and antioxidant activity as well as to obtain special product types, including spiraeoside, scutellarin, luteolin, and nepetin, than the solvent extraction method. Full article

Paulownia tomentosa flowers are rich in flavonoids with promising biological activities. However, few studies have investigated their potential for α-glucosidase inhibition. This study compared ultrasound-assisted cellulase extraction and ultrasound-assisted aqueous two-phase extraction for the recovery of flavonoids from Paulownia tomentosa flowers. The aqueous two-phase extraction method demonstrated superior performance, with optimal conditions determined as 17.80% (NH₄)₂SO₄, 12 min ultrasonication, and 44 °C. Purification was efficiently achieved using NKA-9 macroporous resin. Scanning electron microscopy revealed that ultrasonic treatment disrupted the cell walls, facilitating flavonoid release. Ultra-performance liquid chromatography–tandem mass spectrometry identified apigenin-7-glucuronide and scutellarin as the predominant flavonoids. Notably, several compounds—including scutellarin, ombuin, robinetin, and astragalin—were reported for the first time in this plant. The extracted flavonoids exhibited significant α-glucosidase inhibitory activity, with an IC₅₀ value of 0.412 mg/mL, and showed mixed-competitive inhibition. Luteolin 7-O-glucuronide was identified as a major active constituent, exhibiting stronger inhibition than the total flavonoids while sharing the same mechanism. These findings establish a theoretical foundation for the efficient and sustainable extraction of P. tomentosa flavonoids and support their further development for pharmaceutical applications. Full article

Porcine reproductive and respiratory syndrome (PRRS) is a highly contagious epidemic caused by the porcine reproductive and respiratory syndrome virus (PRRSV). Characterized by reproductive disorders in pregnant sows and respiratory symptoms in pigs of all ages, it poses a severe threat to the global swine industry. In recent years, the high mutation rate of PRRSV has increasingly limited the effectiveness of vaccines against it, prompting the search for new anti-PRRSV drugs. scutellarin (SCU), a natural flavonoid compound extracted from the medicinal plant Scutellaria baicalensis, possesses multiple biological activities. Its antiviral effects have been demonstrated in numerous studies; however, its inhibitory activity against PRRSV and the underlying mechanism remain unknown. In this study, through in vitro cell experiments, we found that scutellarin significantly inhibits PRRSV infection in PAMs. Furthermore, it directly acts on PRRSV to exert antiviral effects. Transcriptomic analysis suggests that scutellarin may exert its anti-PRRSV effects by regulating host immunity and anti-inflammation through immune-related signaling pathways, including the complement and coagulation cascades, ECM-receptor interaction, Rap1 signaling pathway, and PI3K-Akt signaling pathway. Full article

Liver fibrosis, a progressive condition with limited pharmacotherapies, poses a global health challenge. Scutellarin (SCU), a flavonoid derived from Erigeron breviscapus, has demonstrated anti-fibrotic activity and modulates gut microbiota. Emerging evidence suggests that SCU may also influence the hepatic microbiome. However, its clinical utility is constrained by poor water solubility and low oral bioavailability. Here, we developed an SCU-loaded nanoemulsion (SCE) to enhance solubility and liver-targeted delivery. In vitro, SCE increased SCU uptake in hepatic stellate cells (HSCs) and significantly inhibited TGF-β1-induced fibrogenesis. In a bile duct ligation (BDL) mouse model, oral administration of SCE improved hepatic SCU accumulation and produced superior anti-fibrotic efficacy. SCE treatment attenuated fibrosis and collagen deposition in the liver and improved liver function markers. Mechanistic investigations using 16S rRNA sequencing revealed that SCU treatment was associated with beneficial microbiota changes, although its main therapeutic effects were achieved through enhanced hepatic targeting. Notably, the SCE formulation was well-tolerated, showing no significant toxicity in vitro or in vivo. In conclusion, the SCU-loaded nanoemulsion achieved enhanced hepatic delivery of SCU and exerted potent anti-fibrotic effects via multiple mechanisms, including direct suppression of fibrogenesis and ancillary modulation of the gut–liver microbiome, offering a promising therapeutic strategy for liver fibrosis. Full article

UVB radiation penetrates the epidermis and upper dermis, compromising skin barrier function. This activates pro-inflammatory cells, releasing mediators (e.g., histamine, interleukins) that induce edema. UVB also generates excessive reactive oxygen species (ROS), causing oxidative stress in skin cells. Although the mechanisms of UV-induced skin damage have been extensively studied, the development of effective UV-protective drugs remains a significant challenge. Scutellarin, a flavonoid glycoside predominantly isolated from Erigeron breviscapus, has demonstrated diverse bioactivities including anti-inflammatory, antioxidant, and anti-tumor effects. However, its role in UVB-induced skin damage has not been fully explored. Therefore, we established a UVB-induced skin damage model in mice by irradiating the dorsal skin with a dose of 300 mJ/cm² UVB. Through measurements of transepidermal water loss, detection of barrier-related proteins, assessment of inflammatory factors, and evaluation of oxidative stress indicators, we found that scutellarin can maintain barrier integrity, reduce skin edema, suppress inflammatory responses, and decrease oxidative stress. Moreover, RNA sequencing of mice skin revealed that scutellarin can modulate inflammatory responses and maintain extracellular matrix homeostasis to alleviate skin damage. These findings suggest that scutellarin is a natural compound with potential for UV-protective effects on the skin. Full article

Background/Objectives: Understanding metabolome adjustment under saline–alkaline conditions is crucial for enhancing crop tolerance capacity and ensuring food security. Although soil salinization impairs wheat seedlings’ growth, metabolome plasticity under saline–alkaline stress remains poorly understood. Here, we delved into dynamic physiological and metabolome shifts in wheat seedlings grown on SAS (saline–alkaline soil) on the 7th and 15th days post-germination (DPG). Methods: A self-developed and cultivated high-generation salt–alkali wheat variety (011) was grown on SAS and control soil, followed by comparative physiological, biochemical, and metabolomics analyses of seedlings. Results: The seedlings’ saline–alkaline stress responses were developmentally regulated with reduced growth, increasing accumulation of proline and soluble sugars, and differential antioxidant response. LC-MS-based global metabolomics analysis revealed significant metabolite profile differences, with 367 and 485 differential metabolites identified on the 7th and 15th DPG, respectively, between control and treatment. Upregulation of saccharides, flavonoids, organic acids (citrate cycle-related), phenolic acids, amino acids and derivatives, phytohormones, and sphingolipid metabolism was essential for seedlings’ growth on SAS. The key induced metabolites in seedlings grown on SAS include saccharic acid, trehalose, sucrose, glucose, L-citramalic acid, phellodendroside, scutellarin, anthranilate-1-O-sophoroside, lavandulifolioside, N-methyl-L-glutamate, etc. Up-regulated phytohormones include abscisic acid (3.8-fold, 7th DPG and 3.18-fold, 15th DPG), jasmonic acid (1.93-fold, 15th DPG), and jasmonoyl isoleucine (2.03-fold, 15th DPG). Conclusions: Our findings highlight the importance of ABA and jasmonic acid in regulating salt–alkali tolerance in wheat seedlings. Moreover, this study depicts key pathways involved in salt–alkali tolerance in wheat seedlings and unveils key DMs, offering resources for boosting wheat production on SAS. Full article

The occurrence of demyelination in the central nervous system (CNS) causes neurodegenerative lesions. The occurrence and development of demyelination involve multiple pathological mechanisms, including the generation of reactive oxygen species (ROS) caused by mitochondrial dysfunction in microglia and subsequent neuroinflammation. Scutellarin is a natural flavonoid drug with significant neuroprotective effects, including antioxidant, anti-inflammatory, and anti-apoptotic properties, and is widely used in the treatment of neurological diseases. However, the protective effects and mechanisms of scutellarin on demyelination have not yet been elucidated. This study aims to investigate the neuroprotective effects of scutellarin on demyelination and its underlying molecular mechanisms. Our results showed that treatment with scutellarin significantly alleviated Cuprizone-induced myelin damage, neuronal apoptosis, and neurological deficits in mice. In in vitro experiments, scutellarin significantly reduced Cuprizone–copper-induced pro-inflammatory microglia formation and inhibited the secretion of TNF-α, thereby reducing myelin cell damage. Mechanism studies revealed that scutellarin inhibited the secretion of TNF-α by microglia and alleviated myelin cell damage by reducing the excessive production of mitochondrial reactive oxygen species (Mito-ROS), reactive oxygen species (ROS), and malondialdehyde (MDA) induced by Cuprizone–copper in microglia. Finally, scutellarin improved mitochondrial dysfunction in microglia and significantly alleviated myelin cell damage by inhibiting the expression of p38MAPK. In conclusion, our findings demonstrate that scutellarin exerts significant neuroprotective effects on Cuprizone-induced mice by improving mitochondrial dysfunction in microglia, thereby reducing inflammatory responses. This effect is closely associated with the inhibition of the p38MAPK pathway. Full article

Liver fibrosis is a pathological manifestation of chronic liver disease developing to the terminal stage, and there is a lack of effective therapeutic drugs in clinical practice. Scutellarin (SCU) is a flavonoid extracted from Erigeron breviscapus (Vaniot.) Hand.-Mazz., which has significant anti-liver-fibrosis efficacy, but its mode of action remains incompletely understood. A liver fibrosis model was built with male Sprague Dawley rats induced with the disease by CCl₄ to evaluate the therapeutic effect of drugs. 16S rRNA sequencing and metabolomics were used to analyze the regulatory effects of SCU on intestinal flora and host metabolism; antibiotics were administered to eliminate gut microbiota and fecal microbiota transplantation (FMT) experiments were used to verify the mechanism. The mechanistic basis underlying SCU’s hepatic anti-fibrotic effects was screened by network pharmacology combined with transcriptomics, combined with molecular docking, qPCR, and WB verification. The results showed that SCU may play an anti-liver-fibrosis role by correcting the imbalance of gut flora and regulating the linoleic acid and purine metabolic pathways. In addition, SCU can downregulate the levels of proteins and genes related to the PI3K/AKT axis. In summary, SCU alleviates liver fibrosis by reversing intestinal flora imbalance, regulating the metabolic profile, and inhibiting the PI3K/AKT axis. Full article

Nitrogen (N) sources critically influence both agronomic performance and secondary metabolism in medicinal plants. Understanding how different forms of nitrogen affect plant growth and the biosynthesis of valuable secondary metabolites is essential for optimizing cultivation practices and enhancing crop medicinal quality. In this study, Erigeron breviscapus (Vant.) Hand.–Mazz., a medicinal herb renowned in traditional Chinese medicine for its bioactive flavonoids such as scutellarin with neuroprotective and cardiovascular therapeutic effects, was cultivated under various N treatments—nitrate (NO₃⁻–N), ammonium (NH₄⁺–N), and urea [CO(NH₂)₂]—and compared to an N-free control. All N treatments significantly enhanced plant height, leaf area, biomass, and overall yield, with nitrate-N providing the most pronounced growth benefits. Metabolomic profiling identified 387 known metabolites, primarily flavonoids, exhibiting distinct accumulation patterns under each N form. Transcriptomic analyses revealed substantial differences in gene expression, with nitrate-N inducing the greatest number of differentially expressed genes (DEGs). Integration of metabolomic and transcriptomic data uncovered co-expression modules linking candidate regulatory genes, such as cytochrome P450s, MYB transcription factors, and glycosyltransferases, to specific flavonoids, including quercetin-3-O-glucoside and apigenin. These findings elucidate how different N sources modulate flavonoid biosynthesis in E. breviscapus, revealing molecular mechanisms underlying N-mediated flavonoid biosynthesis, which can contribute to optimized fertilizer strategies. This research enhances both the medicinal quality and yield of this important medicinal plant by revealing key gene–metabolite networks, thereby offering valuable insights for metabolic engineering and sustainable cultivation practices. Full article

Among all stroke types, ischemic stroke (IS) occurs most frequently, resulting in neuronal death and tissue injury within both the central infarct region and surrounding areas. This study explored the neuroprotective mechanisms of scutellarin, a flavonoid compound, through an integrated strategy that merged in silico analyses (including network pharmacology and molecular docking simulations) with both in vitro and in vivo experimental verification. We identified 1887 IS-related targets and 129 scutellarin targets, with 23 overlapping targets. PPI network analysis revealed five core targets, and molecular docking demonstrated strong binding affinities between scutellarin and these targets. Bioinformatic analyses, including GO functional annotation and KEGG pathway mapping, indicated that the PI3K/AKT cascade represents the primary signaling mechanism. An in vitro experimental system was developed using PC12 cells under oxygen-glucose deprivation conditions to investigate how scutellarin regulates neuronal cell death via the PI3K/AKT pathway. Western blot quantification demonstrated that treatment with scutellarin enhanced the expression of p-PI3K, p-AKT, and Bcl-2 proteins, while simultaneously reducing levels of apoptotic markers Bax and cleaved caspase-3. Furthermore, pharmacological intervention with the selective PI3K inhibitor LY294002 attenuated these molecular alterations, resulting in diminished expression of p-PI3K, p-AKT, and Bcl-2, accompanied by elevated levels of Bax and cleaved caspase-3. In a rat model of middle cerebral artery occlusion, scutellarin administration demonstrated comparable neuroprotective effects, maintaining neuronal survival and modulating apoptotic protein expression via PI3K/AKT pathway activation. Collectively, this study demonstrates the therapeutic potential of scutellarin in cerebral ischemia through PI3K/AKT pathway modulation, suggesting its possible application in treating ischemic disorders. Full article

Type 2 diabetes mellitus (T2DM) and its associated complications represent a significant public health issue affecting hundreds of millions of people globally; thus, measures to prevent T2DM are urgently needed. Chuju has been proven to possess antihyperglycemic activity. However, the bioactive ingredients in chuju that contribute to its antihyperglycemic activity, as well as the relationship between its antihyperglycemic activity and the gut microbiota, remain unclear. To understand the potential effects that it has on T2DM, the glycolipid metabolism and gut microbiota regulation of flavonoid-rich extracts from chuju (CJE) were investigated. The results showed that the top ten flavonoid compounds in CJE are Apigenin 6, 8-digalactoside, Apigenin 6-C-glucoside 8-C-arabinoside, Luteolin-4′-O-glucoside, Isoshaftoside, Scutellarin, Quercetin 3-O-malonylglucoside, Chrysoeriol 7-O-glucoside, Quercetin-3,4′-O-di-beta-glucoside, Luteolin 6-C-glucoside 8-C-arabinoside, and Homoorientin. Furthermore, CJE mitigated hyperglycemia and glycolipid metabolism by reducing the abundance of Faecalibaculum, Coriobacteriaceae, and Romboutsia and increasing the abundance of Alistipes. In addition, the results of Western blot analysis showed that CJE could enhance glycogen synthesis and glucose transport by up-regulating the phosphorylation of IRS1-PI3K-Akt and AMPK-GLUT4. Simultaneously, CJE could decrease gluconeogenesis by down-regulating the phosphorylation of FoxO1/GSK 3β. In conclusion, the findings of this study provide new evidence supporting the hypothesis that CJE can be used as part of a therapeutic approach for treating disturbances in glycolipid metabolism via regulating the gut microbiota and mediating the IRS1-PI3K-Akt-FoxO1/GSK 3β and AMPK-GLUT4 pathways. Full article

Background: Caryopteris mongolica Bunge (CM) shows promising potential for managing rheumatoid arthritis (RA) and digestive disorders, attributed to its rich content of bioactive compounds such as polyphenols and flavonoids. Despite its common use in herbal tea, the specific mechanisms underlying CM’s anti-inflammatory and joint-protective effects remain unclear, limiting its development as a functional food. This study investigated the effects of aqueous CM extract on RA in collagen-induced arthritis (CIA) rats and explored the underlying mechanisms. Methods: Forty-eight female Sprague-Dawley rats were randomly assigned to six groups (n = 8): normal control, CIA model, methotrexate (MTX), and CM high-, middle-, and low-dose groups. Anti-inflammatory and joint-protective effects were evaluated using biochemical and histological analyses. To elucidate the mechanisms, we applied metabolomics, network pharmacology, and transcriptomics approaches. Results: The results demonstrated that CM extract effectively suppressed synovial inflammation in CIA rats, reducing joint degradation. CM’s anti-inflammatory effects were mediated through the TNF signaling pathway, modulating glycerophospholipid and amino acid metabolism, including reduced levels of tryptophan, LysoPC, and asparagine. Molecular docking identified scutellarin and apigenin as key bioactive compounds. Additionally, immunofluorescence analysis revealed CM’s therapeutic effects via TNF signaling inhibition and suppression of M1 macrophage polarization. Conclusions: These findings highlight the therapeutic potential of CM for RA and support its development as a functional food or pharmaceutical product. Full article

Vitex negundo has strong antioxidant activity, but its primary antioxidant components are not clear. In this study, the antioxidant components were screened by offline two-dimensional liquid chromatography coupled with electrochemical detection (2D-LC-ECD) and subsequently assessed using liquid chromatography-tandem mass spectrometry (LC-MS/MS) identification, radical scavenging capacity, and molecular docking. Various fractions were isolated from Vitex negundo leaves, and 39 antioxidant components were screened and identified. All of the fractions containing the antioxidant components exhibited certain antioxidant activity. Correlation analysis revealed a strong correlation between the response of LC-ECD and the in vitro antioxidant activity of the fractions. Molecular docking demonstrated that components with high response to LC-ECD exhibited robust interaction with antioxidant-related target proteins. The main antioxidant components of Vitex negundo leaves were isoorientin, chlorogenic acid, agnuside, cynaroside, and scutellarin. The 2D-LC-ECD combined with LC-MS/MS was rapid and effective in screening the antioxidant components in Vitex negundo leaves and could also provide technical support for the discovery of antioxidant components with different polarities and contents in other medicinal and edible plants. Full article

Scutellarein is a key active constituent present in many plants, especially in Scutellaria baicalensis Georgi and Erigeron breviscapus (vant.) Hand-Mazz which possesses both anti-inflammatory and anti-oxidative activities. It also is the metabolite of scutellarin, with the ability to relieve LPS-induced acute lung injury (ALI), strongly suggesting that scutellarein could suppress respiratory inflammation. The present study aimed to investigate the effects of scutellarein on lung inflammation by using LPS-activated BEAS-2B cells (a human bronchial epithelial cell line) and LPS-induced ALI mice. The results showed that scutellarein could reduce intracellular reactive oxygen species (ROS) accumulation through inhibiting the activation of NADPH oxidases, markedly downregulating the transcription and translation of pro-inflammatory cytokines, including interleukin-6 (IL-6), C-C motif chemokine ligand 2 (CCL2), and C-X-C motif chemokine ligand (CXCL) 8 in LPS-activated BEAS-2B cells. The mechanism study revealed that it suppressed the phosphorylation and degradation of IκBα, consequently hindering the translocation of p65 from the cytoplasm to the nucleus and its subsequent binding to DNA, thereby decreasing NF-κB-regulated gene transcription. Notably, scutellarein had no impact on the activation of AP-1 signaling. In LPS-induced ALI mice, scutellarein significantly decreased IL-6, CCL2, and tumor necrosis factor-α (TNF-α) levels in the bronchoalveolar lavage fluid, attenuated lung injury, and inhibited neutrophil infiltration. Our findings suggest that scutellarein may be a beneficial agent for the treatment of infectious pneumonia by virtue of its anti-oxidative and anti-inflammatory activities. Full article