Search Results (416)

Background/Objectives: Obesity-associated metabolic dysfunction involves oxidative stress, gut barrier impairment, and gut–liver axis disruption. This study evaluated whether enzymatically prepared Solenocera crassicornis peptides (SCPs) provide additional benefits during diet normalization in HFD-induced obese mice and examined associations with antioxidant, microbial, and barrier markers. Methods: SCPs were characterized using UPLC-Q-TOF-MS/MS and amino acid analysis. Peptides underwent bioactivity prediction and Keap1 docking. After 7 weeks of HFD feeding, obese male C57BL/6J mice were switched to a normal diet and administered vehicle, orlistat, or SCPs for 4 weeks. Adipose tissue mass, serum lipid profiles, liver histology, hepatic antioxidant status, barrier-associated histological and biochemical markers, and gut microbiota composition were assessed. A simulated digestion–fecal fermentation model was used to assess the effects of fermentation products generated in the presence of digested SCPs on H₂O₂-induced oxidative injury and MUC2 secretion in LS174T goblet-like cells. Results: SCPs reduced epididymal and perirenal fat, improved serum lipids, improved hepatic steatosis-related morphology and enhanced hepatic antioxidant status. SCPs were also associated with improved intestinal morphology, increased mucin-associated staining, decreased serum diamine oxidase levels and reduced hepatic lipopolysaccharide accumulation. 16S rRNA sequencing showed SCP-associated microbial shifts, with correlations linking taxa to metabolic and barrier markers. Fermentation products generated in the presence of digested SCPs improved oxidative-stress and MUC2-related readouts in LS174T cells. Conclusions: During diet normalization, SCPs were associated with additional improvements in adiposity, lipid profiles, hepatic antioxidant status, intestinal barrier readouts, and gut microbiota. These findings support further investigation of SCPs as standardized marine protein hydrolysates, but active components, causal mechanisms, long-term efficacy, safety, and human relevance remain to be established. Full article

Blue honeysuckle (Lonicera caerulea L.) is a polyphenol-rich berry increasingly recognized as a functional food ingredient for postprandial glycemic management. However, it remains unclear whether its polyphenols can modulate intestinal glucose transport in addition to inhibiting carbohydrate-digesting enzymes. In this study, blue honeysuckle polyphenol extract (BHPE) was characterized by UPLC-QTOF-MS/MS, and its effects on α-glucosidase activity and intestinal glucose transport were evaluated using enzyme kinetics, fluorescence quenching, molecular docking, and differentiated Caco-2 monolayers. A total of 24 phenolic compounds were tentatively identified, with anthocyanins and chlorogenic acid derivatives as the major constituents. BHPE exhibited a mixed-type, static-quenching inhibition of α-glucosidase (IC₅₀ = 75.05 μg/mL). Furthermore, molecular docking revealed that key constituents, including cyanidin-3-O-glucoside, chlorogenic acid, and proanthocyanidin B1, bind the enzyme via hydrogen bonding and hydrophobic interactions. In Caco-2 cell monolayers, BHPE reduced glucose transport by up to 51.56% under simulated postprandial conditions and coordinately downregulated SGLT1 and GLUT2 mRNA expression to 0.58- and 0.51-fold, respectively. These findings extend the bioactivity profile of blue honeysuckle polyphenols from enzyme-level inhibition to functional regulation at the intestinal epithelial barrier, highlighting their potential as multi-target natural ingredients for the attenuation of postprandial hyperglycemia. Full article

Obesity has emerged as a significant global public health challenge, yet the clinical utility of existing anti-obesity drugs is often constrained by limited efficacy and adverse safety profiles. Rheum tanguticum Maxim. ex Balf., a traditional medicinal plant, has shown potential in modulating glucose and lipid metabolism; however, its specific anti-obesity mechanisms remain poorly characterized. In this study, the chemical profile of the 60% ethanol-eluted fraction of R. tanguticum (RTE) was characterized via UPLC-QTOF/MS, followed by network pharmacology analysis to predict regulatory targets and enriched pathways. Subsequently, a high-fat diet (HFD)-induced obese mouse model was established to evaluate the anti-obesity effects of RTE by monitoring body weight, Lee’s index, fat-to-body weight ratio, serum lipid profiles, and liver histopathological changes. A total of 14 major compounds, primarily anthraquinone glycosides, were identified. Integrated network analysis identified 10 hub targets, including TNF, EGFR, and TP53. In vivo experiments demonstrated that RTE significantly attenuated body weight gain and reduced Lee’s index, fat-to-body ratios, and serum levels of TC, TG, and LDL-C. Furthermore, RTE treatment markedly alleviated hepatic steatosis and inflammatory infiltration in obese mice. These findings suggest that RTE exerts potent anti-obesity effects through a multi-target and multi-pathway mechanism that regulates lipid metabolism and suppresses inflammation. This study improves our understanding of the pharmacological value of R. tanguticum and provides a scientific basis for its development as a functional food ingredient or therapeutic agent against obesity. Full article

Marine-derived collagen peptides exhibit potent intestinal barrier protection; however, their gastrointestinal fate and molecular targets remain unclear, limiting their practical applications. This study investigated the digestive stability and transepithelial transport of GPSGPQGSR, a mucoprotective peptide from Alaska pollock (Gadus chalcogrammus) skin, using simulated gastrointestinal digestion, a Caco-2 cell transport model, and an UPLC-QTOF-MS/MS. The results showed that GPSGPQGSR was a digestion-resistant peptide that reached the intestinal epithelium intact. Although brush border membrane enzymes partially hydrolysed the peptide, 42.16% of intact GPSGPQGSR remained in the luminal compartment after 2 h of incubation. No intact peptide was detected in the basolateral compartment. Molecular docking and 100 ns molecular dynamics simulations identified TLR2 (−14.936 kcal/mol) and PAR2 (−10.154 kcal/mol) as high-affinity extracellular targets of GPSGPQGSR, with stable peptide–receptor interactions and extensive hydrogen bonding networks between the peptide and each receptor (RMSD of 1.8 Å and 2.2 Å, respectively). Pharmacological blockade of TLR2 or PAR2 abolished the protective effects of GPSGPQGSR. These findings demonstrate that GPSGPQGSR acts as a digestion-resistant extracellular signalling peptide that reaches the intestinal epithelium intact and protects barrier function through apical TLR2 and PAR2, providing a mechanistic basis for the rational development of marine collagen peptides for improving intestinal health. Full article

To address the lack of a comprehensive quality control system for Ganoderma lucidum, we developed an integrated evaluation strategy across four varieties and three growth stages. This system integrates the targeted screening of anti-benign prostatic hyperplasia (BPH) triterpenoids acting on 5α-reductase type 2 (SRD5A2) with a chemical consistency assessment utilizing systematic quantitative fingerprint method (SQFM) and chemometrics. UPLC-Q-TOF-MS/MS identified 85 triterpenoids in the samples. An orthogonal partial least squares (OPLS) regression was utilized to screen seven chromatographic peaks that positively correlated with SRD5A2 inhibitory activity. Three principal bioactives were structurally identified as ganoderic acids DM and B, and ganoderenic acid A, which demonstrated significant in vitro SRD5A2 inhibition rates of 61.16 ± 1.87%, 36.41 ± 1.10%, and 41.82 ± 2.09%, respectively. Molecular dynamics simulations and averaged weak interaction analysis revealed that these compounds exert potent enzyme inhibition via hydrogen bonds and hydrophobic interactions with distinct SRD5A2 amino acid residues. The SQFM-chemometrics quality system confirmed ten samples reached Grade 6 or above, identifying the H3 variety at the initial stage as possessing the highest active ingredient content and optimal overall quality. This integrated framework enables rapid bioactive discovery and robust standardization for G. lucidum-based functional foods, thereby facilitating their industrial development. Full article

Background: The fruits of Rosa laxa Retz. (FRL) is a traditional medicinal and edible fruit widely used in Xinjiang for its potential health benefits. Its chemical variations across geographical origins remain poorly understood, as do the molecular mechanisms underlying its anti-hyperlipidemic effects. This study aimed to characterize the chemical profile of FRL extract (FRLE) from different origins, identify its bioactive constituents and metabolites in vivo, and evaluate its efficacy and potential mechanisms against HLP. Methods: UPLC-QTOF-MS was employed for qualitative and quantitative profiling, combined with PCA to differentiate samples from five origins. An HLP mouse model was established to evaluate the pharmacodynamic effects, while acute and sub-chronic toxicity tests assessed safety. Serum pharmacochemistry was used to track absorbed constituents and metabolites. Finally, network pharmacology, molecular docking, and Western blot were integrated to elucidate the underlying mechanisms. Results: A total of 60 compounds were identified in FRLE, with 20 key components quantified via the TOF-MRM mode. PCA indicated that the Yamalike Mountain samples possessed the most diverse chemical profile and the highest response of active markers. Pharmacodynamic results showed that FRLE (extraction yield 24.19%) significantly improved TC, LDL-C, and corrected abnormal HDL-C levels in HLP mice, while H&E staining confirmed the alleviation of hepatic steatosis. Safety evaluations revealed no significant acute or cumulative toxicity at the maximum feasible dose of 16.6 g/kg. In rat plasma, 15 prototypes and 14 metabolites were identified. FRLE acted on the “Lipid and Atherosclerosis” pathway by modulating key targets, including NFE2L2, CYP1A1, NOS3, and MAPK1. Conclusions: Our findings demonstrate that FRLE is a safe and effective candidate for the management of hyperlipidemia. This study establishes a link between the material basis and biological mechanisms of FRL, thereby providing a scientific foundation for its further resource development and clinical application. Full article

Cisplatin-induced acute kidney injury (AKI) poses a significant clinical challenge lacking specific therapeutic drugs. Arundina graminifolia, a traditional Dai medicine, exhibits notable renoprotective effects; however, its in vivo pharmacodynamic material basis and molecular mechanisms remain unclear. This study aimed to explore its mechanisms against AKI from the perspective of authentic kidney-migrating components. A cisplatin-induced mouse AKI model was established to evaluate the renoprotective effects of the A. graminifolia extract (BYJ) via biochemical markers and histopathology. UPLC-Q-TOF-MS/MS was employed to comparatively analyze the blood and kidney-migrating components between normal and AKI mice. Network pharmacology and molecular docking were subsequently applied to predict and validate the core signaling pathways based on the specific components detected in the injured kidneys. Results showed that BYJ administration significantly ameliorated renal dysfunction, restored antioxidant capacity, and alleviated tubular necrosis. MS analysis identified 93 chemical components in vitro. In vivo tracking revealed a “pathological targeted recruitment” characteristic: only 6 prototype components entered normal kidneys, whereas 16 prototypes penetrated the AKI kidneys, highly enriched in lipophilic flavonoid aglycones such as kaempferol and apigenin. Network pharmacology predicted that these targeted components could potentially interact with 124 key targets (including AKT1, PIK3CA, and EGFR) to putatively exert anti-apoptotic and anti-inflammatory effects via the PI3K-Akt, TNF, and MAPK pathways. Molecular docking confirmed excellent binding affinities between these aglycones and core target proteins (e.g., kaempferol with PIK3CA at −8.9 kcal/mol). Based on actual in vivo distribution, this study reveals the specific accumulation of polyhydroxy flavonoid aglycones in injured kidneys, providing a reliable scientific basis for defining the pharmacodynamic substances of A. graminifolia. Full article

Background/Objectives: Sleep deprivation (SD) induces the accumulation of reactive oxygen species (ROS) in the intestine, causing inflammation in the intestine, thereby damaging the intestinal epithelial barrier function. As a traditional Chinese medicine, Dendrobium huoshanense (DHS) modulates intestinal flora, maintains the intestinal mucosal barrier, and promotes gastrointestinal motility and digestive secretion. However, the role and mechanism of DHS in improving SD-induced intestinal injury have not been fully studied. Methods: The SD model was established by subjecting rats to complete SD using a specialised SD instrument. Hematoxylin and eosin (HE) staining was performed to evaluate pathological injury in ileal tissues. Enzyme-linked immunosorbent assay (ELISA) and biochemical methods were used to quantify the main inflammatory cytokines, oxidative stress markers, and hypothalamic–pituitary–adrenal (HPA) axis activity. The expression levels of E-cadherin and Occludin proteins in the ileum tissue were analyzed by Western blotting. Additionally, the pH value of ileal mucus, unit secretion, water content, and dry matter weight were measured. Differential metabolites in rat ileum mucus were profiled using ultra-high-performance liquid chromatography–quadrupole time-of-flight mass spectrometry (UPLC-QTOF-MS). Results: DHS alleviated the pathological injury of the ileum induced by SD. DHS reduced the levels of serotonin (5-HT), interleukin-6 (IL-6), and tumor necrosis factor-α (TNF-α), while increasing interleukin-10 (IL-10) levels, thereby attenuating systemic inflammatory responses. Furthermore, DHS decreased malondialdehyde (MDA) content and elevated glutathione (GSH) and superoxide dismutase (SOD) levels in ileal tissues. DHS also upregulated the protein expression of E-cadherin and Occludin in intestinal tissues. In addition, DHS decreased the pH of ileal mucus, promoted intestinal mucus secretion, and increased dry matter content, facilitating the restoration of the mucus barrier. DHS may alleviate SD-induced ileal injury by modulating steroid hormone biosynthesis. DHS decreased the levels of adrenocorticotropic hormone (ACTH), cortisol (CORT), and corticotropin-releasing hormone (CRH), indicating that DHS suppresses the abnormal activation of the hypothalamic–pituitary–adrenal (HPA) axis. Conclusions: In this study, a comprehensive multi-index evaluation showed that DHS could significantly improve the ileal injury caused by SD in rats. The mechanism involved regulating the balance of serum neurotransmitters and inflammatory factors, reducing oxidative stress in tissues, and improving the physicochemical properties of intestinal mucus. Metabolomic analysis further revealed that these protective effects may be mediated via the regulation of steroid hormone biosynthesis pathways and are associated with the inhibition of abnormal HPA axis activation. Full article

This study is the first to demonstrate fluctuations in major phenolics and biofunctional properties under various extraction conditions of Korean winter spinach (Allseason cultivar) leaves. In contrast to earlier reports on summer- or greenhouse-cultivated spinach, which mainly relied on HPLC-DAD or LC-MS profiling and one or two bioactivity assays, the present work combines UPLC-Q-TOF-MS/MS with NMR-based structural confirmation of three major flavone glucuronides (11–13) and integrates five complementary bioactivity assays (DPPH, ABTS, FRAP, DNA protection, and tyrosinase inhibition) within a single optimization framework. A 50% methanol extract yielded twelve phenolics (patuletin, spinacetin, spinatoside, jaceidin, and methylenedioxyflavone-glucuronide derivatives) elucidated by UPLC-Q-TOF-MS/MS, with the isolated major phenolics 11–13 further verified by NMR. Total phenols and total flavonoids of biofunctional characteristics varied significantly depending on the solvent system. The optimal extraction conditions (50% methanol, 72 h, 35 °C) resulted in the highest phenolic levels of phenolics 11–13 (total: ~6.5 mg/g) and bioactivities (DNA protection > ABTS > tyrosinase inhibition > FRAP > DPPH, at 500 μg/mL). PCA and hierarchical clustering distinguished extraction profiles, with 50–70% methanol extracts forming clear clusters. Among the isolated phenolics, phenolic 12 showed the strongest antioxidant activity (DPPH IC₅₀ = 57.6 μM; ABTS IC₅₀ = 21.9 μM). These findings suggest that spinach leaves are a valuable source of bioactive phenolics for nutraceutical applications under optimized extraction conditions. Full article

Background: The sensory quality of melon (Cucumis melo L.) is determined by the complex interplay of metabolites within the fruit. However, the underlying metabolic mechanisms based on consumer sensory experience remain underexplored. Methods: Sensory evaluation was conducted on twelve melon cultivars, recording flesh color and quantitatively scoring acidity, sweetness, firmness, and aroma intensity. Based on the sensory results, eight cultivars were selected to establish two contrasting groups: sweet-type vs. acidic-type and orange-fleshed vs. green-fleshed. Untargeted metabolomics (UPLC-QTOF-MS) was then performed to analyze the samples, and differential metabolites were screened using OPLS-DA combined with univariate analysis. Results: Pathway enrichment analysis revealed that the key distinction between sweet and acidic taste profiles was associated with the specific accumulation of citric acid within the tricarboxylic acid (TCA) cycle in the acidic-type group. Regarding flesh color, the orange-fleshed group was enriched with carotenoid derivatives like β-citraurinene and the oxidized tocopherol product α-tocopherolquinone, whereas the green-fleshed group mainly accumulated phytol, a chlorophyll degradation product, along with more abundant terpenoids. Conclusions: By integrating sensory phenotyping with metabolomic analysis, this study identified key differential metabolites and candidate pathways associated with taste and color in melon, providing metabolic insights and data resources for quality evaluation and regulation. Full article

This study comparatively evaluated how solvent polarity affects the chemical antioxidant capacity, preliminary hyaluronidase inhibition, and supportive chemical features of Buddleja officinalis Maxim. Six extracts prepared with petroleum ether, ethyl acetate, n-butanol, water, 60% ethanol, and 95% ethanol were assessed using DPPH·, ABTS⁺·, ferric reducing power, and hyaluronidase inhibition assays, together with total flavonoid and linarin determinations. The 60% ethanol extract showed the strongest overall radical-scavenging activity, reaching 95% DPPH· scavenging and 95% ABTS⁺· scavenging at 2 mg/mL, whereas the 95% ethanol extract showed the highest ferric reducing power under the tested conditions. Total flavonoid and linarin contents were highest in the ethanol-rich fractions, especially the 95% ethanol and 60% ethanol extracts. In the hyaluronidase assay, both the petroleum ether and 60% ethanol extracts showed relatively strong inhibition at 2.5 mg/mL, with inhibition rates of 74% and 68%, respectively, suggesting that different chemical classes may contribute to this endpoint. Supportive ¹H NMR and UPLC–QTOF–MS data indicated clear polarity-dependent compositional differences; the 60% ethanol extract was enriched in phenylethanoid glycosides and flavonoid glycosides, whereas the petroleum ether extract showed predominantly lipophilic features. Overall, medium-polarity phenolic-rich fractions were more closely associated with chemical antioxidant capacity, while hyaluronidase inhibition may involve contributions from both non-polar and medium-polarity constituents. The present extract-level comparison provides a useful basis for fraction selection, extract standardization, and follow-up activity-guided studies. Full article

The seed oil of Prinsepia utilis is a traditional food-medicine homology used by the Naxi people in Yunnan Province of the Himalayan region. This study explored the potential applications of food-medicine homology in health and wellness. Using untargeted metabolomics, we compared the metabolite profiles of the subcritical extraction method (edible oil as crude oil) (CO) and its improved processing method (medicinal oil as refined oil) (RO) extracted from P. utilis seeds by UPLC–QTOF MS/MS and evaluated their in vivo and in vitro activities. We screened 14 discriminatory metabolites and performed their tentative annotation, including fatty acids, terpenoids, steroids, and quinones. Furthermore, we quantified 12 bioactive compounds in CO samples via targeted chromatographic analysis, which support the promising food-medicine homology applications of the oil. RO exhibited potent antioxidant activity (DPPH radical scavenging rate of 79.7%, representing 65.7% increase over CO), with an ABTS⁺ radical scavenging rate of 95.8% (77.1% improvement over CO). The hyaluronidase inhibition rate for RO was 43.4%, whilst that for CO was 30.8%; the elastase inhibition rate for RO was 69.8%, whilst that for CO was 59.8%, and promoted zebrafish fin regeneration by 15% at 3% concentration. Our results validated the seed oil of P. utilis as a traditional food and its antioxidants, anti-aging, demonstrating that the CO processing method is able to meet with medicine and food homology in health, and the RO processing method may satisfy skin care function. These findings highlight the potential applications of P. utilis seed oil for food-medicine homology in health and wellness properties. Full article

The role of medicinal plants in primary healthcare and livelihoods around the world is both ancient and well-documented. Agathosma betulina (P.J. Bergius) Pillans, commonly known as ‘buchu’, has long been utilised in traditional medicine as a household remedy for various ailments and is also valued for its essential oils in the cosmetics and pharmaceutical industries. This study aimed to profile and quantify the secondary metabolites in buchu using ultra-performance liquid chromatography quadrupole time-of-flight combined with mass spectrometry (UPLC-QTOF-MS) techniques, whereby plant material from three distinct locations in the Western Cape Province, Groot Winterhoek, Citrusdal, and Cederberg, was collected. A total of 32 maker compounds were identified from buchu leaves. The results revealed a significant location-dependent variation in the accumulation of multiple classes of phytochemicals, including phenolic acids, flavonoids, saponins, terpenoids, oligosaccharides, vitamins, and steroids. Citrusdal samples had the most bioactive compounds compared to the Cederberg and Groot Winterhoek. Citrusdal had the highest flavonoid levels, while Cederberg samples were the richest in phenolic acids and Groot Winterhoek was dominant in iridoid glycoside levels. Principal component analysis (PCA) revealed distinct clusters corresponding to the three different regions, confirming chemical differences. Elucidating the distribution of secondary metabolites in this species may provide new information for possible medicinal and pharmacological uses, such as the creation of novel and enhanced organic medications and food products. These results will aid in selecting a buchu chemotype with optimal attributes for the intended therapeutic application, helping to protect wild populations from over-exploitation through cultivation. Full article

Anthocyanin stability substantially determines the postharvest storage quality of red Huajiao (Zanthoxylum bungeanum Maxim.). Herein, the composition of red Huajiao anthocyanins (RHAs) was characterized, and the copigmentation performance of seven phenolic compounds with RHAs was comparatively evaluated, together with verifying their practical efficacy in maintaining the overall quality of red Huajiao during frozen storage. UPLC-Q-TOF-MS/MS analysis identified ten anthocyanin monomers in RHAs, among which delphinidin-3,5-diglucoside (D3,5G, 28.23%), and delphinidin-3-O-glucoside (D3G, 14.86%) were verified as the predominant monomers. Naringin (NA) exhibited an optimal copigmentation effect, achieving a maximum color enhancement rate of 19.46% at a 1:40 molar ratio and a pH of 3.0 at 20 °C, while thermodynamic tests verified the excellent stability of the naringin–RHA complex. The copigmentation interactions between RHAs and copigments were largely attributed to hydrogen bonds, π–π stacking, and alkyl hydrophobic interactions. Considering practical application cost and flavor compatibility, chlorogenic acid (CGA) was selected as the preferred alternative copigment. Frozen storage tests suggested that soaking pretreatment with 10 mmol/L CGA effectively delayed color fading and maintained the integrity of the oil gland and the good sensory quality and color attributes of red Hujiao, with no adverse impacts on its inherent flavor and numbing components. Collectively, phenolic-mediated intermolecular copigmentation represents an efficient technical means for stabilizing color and maintaining the commercial quality of postharvest red Huajiao during frozen storage. Full article

This study established an untargeted metabolomic approach based on ultra-performance liquid chromatography/quadrupole time-of-flight mass spectrometry (UPLC-QTOF-MS) to investigate differences in metabolites and lipid composition of lycopene-enriched egg yolk at different enrichment levels and conventional egg yolks. Principal component analysis and hierarchical clustering revealed clear unsupervised discrimination and separation among the control group and two treatment groups. Metabolomic analysis identified 14 differential metabolites, including amino acids, which were associated with 13 metabolic pathways such as cysteine and methionine metabolism. Lipidomic analysis revealed 48 significantly altered lipids, including phospholipids and glycerides. The results demonstrated that lycopene supplementation significantly altered the metabolic and lipid profiles of egg yolks. Specifically, lycopene enrichment upregulated phospholipid synthesis and increased the levels of antioxidant-related metabolites. This study confirms that untargeted metabolomics and lipidomics can effectively identify potential biomarkers in egg yolks with varying lycopene enrichment levels, offering new insights and a scientific basis for nutritional research and metabolic mechanism analysis of functional eggs. Full article