Search Results (1,039)

Background: Type 2 diabetes (T2DM) is a chronic metabolic disease closely associated with insulin resistance (IR) and disturbances in glucose and lipid metabolism. Bioactive peptides derived from food are attracting increasing research attention as candidates for nutritional supplements or functional food ingredients that improve metabolic health. This study evaluated the functional food-related properties of YPWTQ (CP4), a novel peptide derived from donkey blood, and its ability to alleviate insulin resistance in HepG2 cells. Methods: CP4 was characterized based on its hemolytic activity, stability under simulated gastrointestinal digestion conditions, inhibitory activity against α-glucosidase and Pancreatic lipase, and free radical scavenging capacity (DPPH·, ABTS⁺·, and O₂⁻·). Its effects on glucolipid metabolism and oxidative stress were examined in a glucosamine-induced insulin-resistant HepG2 cell model. Candidate signaling pathways associated with CP4 treatment were explored through transcriptomic and metabolomic analyses, combined with RT-qPCR technology. Results: CP4 exhibited low hemolytic activity and remained stable after 4 h of simulated gastrointestinal digestion. It inhibited α-glucosidase and Pancreatic lipase and exhibited antioxidant activity. In insulin-resistant HepG2 cells, CP4 increased glucose consumption, glycogen content, and cell survival, while reducing triglyceride accumulation, malondialdehyde levels, and reactive oxygen species (ROS) production. Mult omics analysis indicates that these phenotypic effects may be associated with coordinated changes in the PI3K-Akt, AGE-RAGE, Rap1, and Ras signaling pathways, as well as related genes and metabolites. Conclusions: These findings suggest that CP4, as a food-derived bioactive peptide candidate, warrants further investigation into its potential applications in the field of metabolic health. Full article

Background: This study evaluated the effects of aging and subsequent autoclave treatment on the proton nuclear magnetic resonance (¹H NMR) spectral-feature profile and biological activities of lychee pulp extracts. Methods: Dried lychee (DL), aged lychee (AL), and autoclave-treated aged lychee (ATAL) extracts were compared using ¹H NMR spectroscopy, total phenolic content (TPC), total flavonoid content (TFC), antioxidant assays, carbohydrate-hydrolyzing enzyme inhibitory assays, and endothelial cell viability. Results: Sixteen phytochemical spectral features were putatively annotated, and their relative signal intensities differed among the extracts (p < 0.001). Relative to DL, ATAL exhibited higher signal intensities for most features, including taxifolin (8.32-fold) and procyanidin B2 (7.44-fold), whereas epicatechin was particularly prominent in AL (12.31-fold). TPC increased from 0.53 ± 0.07 mg gallic acid equivalents (GAE)/g extract in DL to 8.39 ± 0.19 and 9.07 ± 0.10 mg GAE/g extract in AL and ATAL, respectively. AL and ATAL also showed higher TFC and antioxidant activities than DL. The α-amylase IC₅₀ values were 247.00 ± 45.00, 129.17 ± 8.56, and 126.27 ± 3.90 mg/mL for DL, AL, and ATAL, respectively, while the corresponding α-glucosidase IC₅₀ values were 187.93 ± 8.20, 66.71 ± 6.84, and 50.30 ± 2.72 mg/mL. No significant reduction in endothelial cell viability was detected after multiplicity adjustment. Exploratory principal component analysis (PCA) explained 99.8% of the total variance and revealed distinct processing-associated spectral-feature profiles. Conclusions: Aging followed by autoclave treatment enhanced the phytochemical profile, antioxidant activity, and in vitro carbohydrate-hydrolyzing enzyme inhibition of lychee pulp extracts. Full article

Digestive enzymes such as pancreatic lipase (PL), α-glucosidase (AG), and α-amylase (AA) play key roles in the hydrolysis of dietary lipids and carbohydrates and are therefore relevant biochemical targets for evaluating compounds with potential to modulate postprandial metabolic responses. Neurolaena lobata (L.) R. Br. ex Cass. (Asteraceae) is a neotropical medicinal species traditionally used for several health-related conditions, including metabolic complaints. This study evaluated the in vitro inhibitory activity of the hydroalcoholic extract, selected VLC fractions, and isolated metabolites from N. lobata leaves against PL, AG, and AA. Enzyme inhibition screening of the extract and VLC fractions was used to select fractions for phytochemical investigation, affording six known metabolites: the sesquiterpene lactones neurolenin B (C1) and lobatin A (C2), the benzoic acid derivatives p-hydroxybenzoic acid (C3) and 3,4-dihydroxybenzoic acid (C4), and the flavonoids 6-hydroxykaempferol 3,7-dimethyl ether (C5) and quercetagetin 3,7-dimethyl ether (C6). The hydroalcoholic extract and the MeOAc and iPrOH fractions inhibited PL, AG, and AA. Among the isolated compounds, C1, C2, C5 and C6 inhibited PL and AG, with IC₅₀ values ranging from 134 to 615 µM and from 170 to 639 µM, respectively, whereas all compounds showed weak AA inhibition. Exploratory kinetic analysis yielded apparent inhibition profiles mainly consistent with competitive behavior; C6 showed an apparent profile consistent with noncompetitive inhibition against AG under the assay conditions used. These findings expand the phytochemical and in vitro bioactivity profile of N. lobata and provide preliminary evidence of digestive enzyme modulation in isolated enzyme systems, without establishing therapeutic efficacy. Full article

Agricultural and horticultural by-products represent an underexploited source of valuable bioactive compounds that can contribute to the development of more sustainable production systems. This study investigated the chemical composition and biological activities of the essential oil obtained from the horticultural byproducts of Artemisia dracunculus. The waste aerial biomass was subjected to steam distillation, and the essential oil was characterized by gas chromatography–mass spectrometry. Its antioxidant, α-amylase and α-glucosidase inhibitory, phytotoxic, antibacterial, and antibiofilm activities were subsequently evaluated. The essential oil was characterized as an estragole-rich chemotype (70.17%), with trans-β-ocimene and cis-β-ocimene as other main constituents. The essential oil showed moderate antioxidant activity and measurable enzyme inhibitory activity and, despite showing limited effects on seed germination, it significantly inhibited radical elongation in selected plant species. Furthermore, it demonstrated excellent antibiofilm activity, significantly reducing the metabolic activity of mature cells of bacteria associated with biofilm formation: Listeria monocytogenes, Pseudomonas aeruginosa, Escherichia coli, Acinetobacter baumannii, Klebsiella pneumoniae and Staphylococcus aureus. The results demonstrate how horticultural by-products from A. dracunculus maintain a chemical profile comparable to conventional plant material and represent a valuable source of bioactive compounds with promising potential for sustainable agri-food applications. Full article

Dietary interventions using probiotics actively regulate metabolism in obesity and type 2 diabetes. This study aimed to characterize two novel co-isolated strains, P. pentosaceus BGI-N8 and P. acidilactici BGI-N9, using an integrated genome–phenotype approach. Whole-genome sequencing established their preliminary safety and functional genotypes, followed by in vitro assays measuring gastrointestinal tolerance, adhesion, and metabolic enzyme activity. Genomic analysis revealed that both strains achieved genome-based safety levels, and no high-confidence transferable AMR determinants and canonical virulence factors were identified. Functional annotation showed that BGI-N8 and BGI-N9 contain essential genes for gastrointestinal adaptation, including F0F1-ATPase, the dltA-D operon, and the opp transport system. Phenotypically, BGI-N9 exhibited superior acid resistance (79.3% survival at pH 2.0), while both strains showed robust auto-aggregation (>70%) and high adhesion to HT-29 cells (ranged from 5.4 to 5.9 adherent bacteria per cell). Furthermore, the strains displayed inhibitory activity against selected indicator pathogens (88.6–97.6% inhibition). Notably, BGI-N8 and BGI-N9 showed comparable α-glucosidase inhibitory activities, with inhibition rates of 44.53% and 39.94%, respectively, Both strains also exhibited comparable cholesterol-removal capacities under the tested conditions, with removal rates of 68.76% and 74.49%. Overall, these genomic and phenotypic results supported the potentials of BGI-N8 and BGI-N9 as candidate probiotic strains with distinct complementary strengths in glycolipid regulation, providing a theoretical basis for their synergistic application. Further mechanistic, safety, and in vivo studies are required to validate their metabolic-health-related relevance. Full article

Diabetic nephropathy (DN) is a major complication of diabetes, yet effective dietary interventions remain limited. Xanthoceras sorbifolium Bunge leaf extract (XBL) has shown promising bioactivities, but its active components and mechanisms are not well understood. In this study, a comprehensive investigation including chemical profiling, network pharmacology, in vivo validation, and renal multi-omics was conducted. The results show a diverse composition dominated by flavonoids, which were identified as key bioactive contributors. In the streptozotocin-induced DN rat model, XBL administration significantly improved metabolic disorders and renal injury. Integrated metabolomic and transcriptomic analyses demonstrated that XBL alleviates DN by coordinately regulating metabolic reprogramming and inflammation-related signaling pathways. Additionally, representative flavonoids showed α-glucosidase inhibitory activity, supporting their potential role in glucose metabolic regulation. The results from this study suggest that XBL is a promising functional food ingredient for DN intervention. Full article

This study investigated the content differences of major active ingredients in red, yellow, and white flowers of Carthamus tinctorius L. from Yumin County, Xinjiang, and evaluated their α-glucosidase inhibitory effects using high-performance liquid chromatography (HPLC), network pharmacology, molecular docking, and in vitro enzyme assays. HPLC analysis revealed that red safflower had the highest content of Hydroxysafflor yellow A (HSYA), while white safflower exhibited the highest levels of kaempferol and kaempferol-3-O-rutinoside. Network pharmacology identified 21 core targets and multiple pathways related to type 2 diabetes and insulin resistance. Molecular docking indicated that kaempferol-3-O-rutinoside had the lowest binding energy (−9.3 kcal/mol). However, in vitro assays showed that kaempferol exhibited the strongest α-glucosidase inhibition (half maximal inhibitory concentration (IC₅₀) = 0.1768 mg/mL), followed by HSYA and kaempferol-3-O-rutinoside. Among extracts, white safflower demonstrated the highest inhibitory activity (IC₅₀ = 0.5485 mg/mL). In conclusion, flower color significantly influences the chemical composition and hypoglycemic potential of safflower. White safflower extract exhibited the strongest α-glucosidase inhibitory activity among the three flower color extracts. This study identifies kaempferol as the key active ingredient for safflower’s α-glucosidase inhibitory activity, providing a scientific basis for developing Yumin safflower as hypoglycemic functional food. Full article

Tsuan-Kan tea (TKT) is a solid-state-aged mixture of citrus and tea leaves. This study examined how aging temperature, humidity, and time affect the properties of TKT. Solid-state aging (SSA) enriched active ingredients (total phenol content: 1.25–2.51-fold; total flavonoid content: 1.29–2.52-fold; DPPH radical scavenging activity: 7.16–18.35-fold; ferric-reducing antioxidant power: 5.06–11.96-fold) by avoiding traditional processing losses. Flavanone glycosides (narirutin: 2.81 mg/g; hesperidin: 37.33 mg/g), 5-hydroxymethylfurfural (0.20 mg/g), and tea polyphenols (catechin: 109.80 mg/g; theaflavin: 1.82 mg/g) increased substantially under high-temperature and humidity. Fourier-transform infrared spectroscopy suggested that hydrothermal environments promoted glycosidic bond cleavage (1078 cm⁻¹) and enhanced π–π stacking between polyphenols and flavanone glycosides, improving solubility. During SSA, aroma profiles shifted from fruity and floral to woody and aged. Partial least squares regression revealed that nonenzymatic browning products, particularly 5-HMF (variable importance in projection [VIP] = 1.806), strongly correlated with α-glucosidase inhibition. Although naphthalene exhibited statistical collinearity (VIP = 2.300) and theoretical binding affinity in molecular docking, its potential toxicity as a thermal processing byproduct designates it as a quality control marker for process intensity. Overall, SSA enriches functional phytochemicals (e.g., polyphenols and 5-HMF) via non-enzymatic pathways, providing preliminary in vitro evidence for developing functional beverages. Full article

This study aimed to evaluate the efficacy of crude polysaccharide extraction from Thai-cultivated oats (Avena sativa L.) utilizing hot water extraction (HW) and ultrasound-assisted water extraction (UW) methods. Optimal conditions were determined by a response surface methodology (RSM). The influence of solid-to-liquid ratio, temperature or %amplitude, and extraction time on %yield and beta glucan content was investigated. Under optimal conditions, UW produced a superior %yield (82.72 ± 2.19%) and beta glucan content (1.75 ± 0.87 g/100 g extract) compared to HW (41.32 ± 0.98% and 1.25 ± 0.27 g/100 g extract). This finding may occur from acoustic cavitation, which effectively dismantles the cellular wall structure, supported by FTIR analysis finding more distinct β-glycosidic linkage peaks. SEM analyses indicated a greater surface area dispersion and porosity in UW extract relative to HW extract. Analysis of monosaccharide composition supported the properties of both crude extracts, demonstrating glucose as the predominant component. However, the functional and bioactive characterization demonstrated a distinct trade-off between the two extraction methods. HW extract demonstrated superior swelling capacity (6.2 vs. 2.7 g/g at pH 6.5), enhanced antioxidant activity compared to both ABTS (0.67 ± 0.04 vs. 0.58 ± 0.06 μmol TE/g), DPPH (0.53 ± 0.06 vs. 0.35 ± 0.06 μmol TE/g), and FRAP (0.05 ± 0.02 vs. 0.03 ± 0.01 μmol TE/g), total phenolic content (98.33 ± 7.68 vs. 87.79 ± 3.07 mg GAE/g). The crude extracts from the two methods had selective enzyme inhibitory activity, exhibiting considerable inhibition of α-glucosidase and markedly reduced inhibition of α-amylase. UW demonstrated slightly superior inhibitory activity compared to HW for both enzymes. The findings indicate that the determination of crude polysaccharides should principally take into account the purpose of the final product. UW is preferable for optimizing %yield and beta glucan content. Nevertheless, if the emphasis is on functional attributes like water absorption and antioxidant efficacy, HW has advantages that merit a consideration. This research provides a framework for identifying optimal extraction methods aimed at extracting crude polysaccharides from Thai-cultivated oats for use as a functional ingredient in health food products. Full article

Backgroud: The growing prevalence of diabetes mellitus necessitates the development of safe and effective inhibitors of carbohydrate-metabolizing enzymes, particularly α-amylase and α-glucosidase. Methods: In this study, a series of pyrimidine–oxadiazole derivatives (1–10) was synthesized and structurally characterized using elemental analysis, HREI-MS, and ¹H/¹³C NMR spectroscopy. The compounds were evaluated for in vitro inhibitory activity against both enzymes, with acarbose as the reference drug. Results: IC₅₀ values ranged from 6.70 ± 0.20 to 21.10 ± 0.10 μM for α-amylase and 7.10 ± 0.20 to 21.80 ± 0.40 μM for α-glucosidase. Compounds 2, 3, and 6 displayed superior dual inhibitory activity compared to acarbose (IC₅₀ = 10.10 ± 0.20 and 10.50 ± 0.10 μM, respectively). Structure–activity relationship analysis revealed that electronic effects of aromatic substitutions significantly influenced enzyme inhibition. Molecular docking supported the experimental findings by demonstrating stable binding interactions within the enzyme active sites. Preliminary safety profiling in male Wistar rats showed no observable behavioral changes, hematological abnormalities, or hepatic and renal dysfunction following repeated administration of the lead compound. Conclusions: These results highlight pyrimidine–oxadiazole derivatives as promising and well-tolerated dual enzyme inhibitors for further antidiabetic drug development. Full article

Cardamom represents one of the world’s most famous spices, which is also applied in the traditional medicine of numerous cultures. Modern research aims to elucidate its therapeutic potential in various diseases. The aim of this study was to investigate the chemical composition of essential oil of cardamom seeds, as well as to assess the biological and pharmacological potential of aqueous and ethanolic extracts. The essential oil composition was evaluated using gas chromatography coupled to mass spectrometry. Aqueous and ethanolic extracts were analyzed for the total phenolic and flavonoid content, and further evaluated in vitro regarding antioxidant, anti-inflammatory and antihyperglycemic activity, and additionally antimicrobial activity for the ethanolic extract. The essential oil was abundant in monoterpenes, with α-terpinyl acetate as a predominant compound. The content of total phenolics and flavonoids in extracts was low. Antioxidant potential was moderate. Extracts displayed potent activity in tests of anti-inflammatory potential, with the ethanolic extract being more active. Regarding the antihyperglycemic activity, the extracts displayed inhibitory activity against α-amylase and no activity against α-glucosidase. Antimicrobial activity was observed against Candida albicans and Prototheca zopfii in high concentrations. The present study suggests preliminary in vitro potential of cardamom in mediating carbohydrate metabolism and pro-inflammatory conditions. Full article

Medicinal plants are being investigated as a source of compounds with biological activities related to diabetes. The antidiabetic properties of the plant Carica papaya have been reported in experimental models. This study aimed to evaluate the phytochemical composition, antioxidant activity, and inhibitory activity of extracts from C. papaya leaves against α-glucosidase and pancreatic lipase. Plant material was collected in Tabasco, Mexico, and extracted by sequential maceration with solvents of increasing polarity: hexane, dichloromethane, methanol, and methanol:water. The extracts were fractionated by column chromatography, and the most active fractions were selected for further purification. The phytochemical identification of the active compounds was performed, and their structures were elucidated using spectroscopic and spectrometric techniques. The methanolic extract, rich in phenols and flavonoids, showed the highest antioxidant capacity (DPPH: 8.99 mmol TE/g; ABTS: 35.94 mmol RE/g; FRAP: 48.62 mmol Fe²⁺/g). The hydroalcoholic extract exhibited α-glucosidase inhibitory activity (38.44%), and bioassay-guided fractionation led to the identification of clitorin. The dichloromethane extract showed pancreatic lipase inhibition (52.2%), and the most active fraction contained loliolide. These findings demonstrate that C. papaya leaves contain bioactive compounds with antioxidants and digestive enzyme inhibitory activities, suggesting they could be candidates for further research in the management of diabetes. Full article

The present study provides an integrative, targeted phenolic–bioactivity mapping of Hedysarum pestalozzae Boiss., an endemic Fabaceae species from gypsum habitats of Türkiye. Methanolic extracts of flowers, leaves, stems, and roots were comparatively evaluated for their phenolic profiles, antioxidant potentials, and enzyme inhibitory effects. Targeted LC–ESI–MS/MS analysis of selected phenolics revealed organ-dependent chemical profiles, with flowers exhibiting the highest accumulation of flavonols—hyperoside, kaempferol, quercetin—and phenolic acids such as protocatechuic acid, together with the flavanone glycoside hesperidin, while stems and roots were enriched in catechin, verbascoside, vanillin, and eriodictyol. The antioxidant capacities, assessed through multiple assays (CUPRAC, FRAP, DPPH, ABTS, metal chelation), were integrated using the Relative Antioxidant Capacity Index (RACI), ranking flowers as the most active organ, followed by roots, leaves, and stems. Correlation analysis demonstrated strong positive associations between phenolic abundance and electron-transfer assays, whereas metal chelation showed inverse trends, suggesting distinct antioxidant mechanisms. All extracts exhibited moderate inhibition against cholinesterases, tyrosinase, α-amylase, and α-glucosidase, implying multifunctional enzyme-modulating potential. The root extract showed the highest cholinesterase inhibition, and leaf extract was most effective against α-amylase. These findings indicate that H. pestalozzae exhibits organ-dependent chemical diversity and a broad range of biological activities. The present study provides preliminary evidence that H. pestalozzae may represent a promising source of bioactive compounds for future phytochemical and biological investigations, warranting further bioassay-guided fractionation, compound isolation, cellular studies, and in vivo validation. Full article

This study highlights the therapeutic innovation potential of bioactive plant extracts derived from the selected Thai Rejuvenation Remedy 2 (TRJ 2) for antidiabetic applications. By integrating phytochemical profiling with in vitro α-glucosidase inhibition assays and in silico analyses, including molecular docking and density functional theory (DFT), a comprehensive evaluation of the extract’s bioactivity and mechanistic basis was achieved. The findings demonstrate that both the relative abundance and chemical reactivity of constituent compounds contribute to the overall inhibitory effect through synergistic and competitive interactions. Piperine was identified as a potential bioactive metabolite, with a theoretically strong binding affinity and high reactivity toward the target enzyme. Among the tested extracts, the 80% ethanol extract exhibited the highest inhibitory activity (IC₅₀ = 34.32 µg/mL), underscoring the importance of extraction optimization for maximizing therapeutic efficacy. Furthermore, formulation of the extract with cyclodextrin significantly enhanced solubility and improved pharmaceutical characteristics, meeting the quality requirements of the Thai Herbal Pharmacopoeia (THP). However, the detection of cadmium slightly above permissible levels indicates the need for stricter raw material quality control. Overall, TRJ 2 represents a promising source of bioactive plant-derived compounds and a viable candidate for development into innovative, ready-to-use herbal therapeutics for diabetes management. Full article

The interaction with various food matrix constituents can affect the beneficial effects of phenolic compounds in the gastrointestinal tract. In this study, the effect of cellulose on the potential of phenolic compounds from Aronia melanocarpa after simulated gastrointestinal digestion to inhibit activity of enzymes important in carbohydrate digestion in vitro was investigated. Enzyme inhibitory activity was assessed by the inhibition of α-amylase and α-glucosidase. Cellulose was studied at three different levels. Phenolic compounds were released in the stomach (61–69%) and small intestine (58–66%). Cellulose increased recovery in the stomach (p < 0.05) and decreased it in the small intestine (p < 0.05), and the influence was dose-dependent. After digestion, phenolic compounds inhibited α-amylase and α-glucosidase. Cellulose increased the inhibition of α-amylase (p < 0.05), while it did not affect the inhibition of α-glucosidase. In conclusion, phenolic compounds after gastrointestinal digestion in the presence of cellulose can still inhibit α-amylase and α-glucosidase activity. Since the results represent only the in vitro model of digestion, further studies should focus on in vivo studies, and the effects of different food sources of cellulose to confirm the results. Full article