Search Results (551)

Astragalus species have long been recognized for their pharmacological relevance, yet the antidiabetic properties of Astragalus cruciatus Link (Ac) remain poorly explored. This study aimed to investigate the antidiabetic potential of A. cruciatus Link and to elucidate possible underlying mechanisms. The ethanolic extract of Ac (AcEE) was prepared and analyzed for phenolic and flavonoid content. Antioxidant activity was assessed through a series of in vitro assays. The in vitro inhibition of α-amylase and α-glucosidase was assessed, followed by molecular docking to probe ligand-enzyme interactions. LC-ESI-MS analysis revealed a polyphenol-rich profile, with rutin (953.54 µg/g extract) and quinic acid (797.18 µg/g of extract) identified as main compounds. The AcEE showed significant inhibitory activity against both α-amylase and α-glucosidase (IC₅₀ = 239.30 ± 7.40 and 192.60 ± 15.51 μg/mL, respectively). Moreover, low cytotoxic effects were observed in hepatic cell lines. Computational analysis revealed stable interactions between rutin and both enzymes (−12.935 and −8.073 Kcal/mol, respectively). Network pharmacology revealed that AcEE may modulate key targets, including IL-6, TNF-α, IL-1β, Akt-1, STAT3, EGFR, and INSR as well as pathways related to insulin resistance, AGE-RAGE, and inflammation. These findings suggest that AcEE exerts significant antidiabetic effects through multitarget modulation, highlighting its potential as a natural therapeutic agent for T2DM. Full article

This study introduces a novel food-grade protein–β-glucan nanoparticle system based on Fusarium venenatum protein isolate and Fuscoporia torulosa β-glucans, designed as a multifunctional ingredient for improving the physicochemical stability, bioaccessibility, and functional performance of peach juice beverages. Therefore, this study aimed to develop and evaluate a functional peach juice enriched with protein–β-glucan nanoparticles and to investigate their effects on physicochemical stability, gastrointestinal behavior, metabolic enzyme inhibition, antioxidant retention, and sensory acceptance. Protein–β-glucan nanoparticles produced from Fusarium venenatum protein isolate and Fuscoporia torulosa β-glucans were incorporated into peach juice formulations (V1–V4) and characterized using dynamic light scattering, zeta potential analysis, transmission electron microscopy (TEM), and Fourier-transform infrared spectroscopy (FTIR). In vitro gastrointestinal digestion was performed to assess β-glucan bioaccessibility, protein digestibility, antioxidant activity, and release kinetics, while α-amylase and α-glucosidase inhibition assays, sensory evaluation, digital sensory analysis, principal component analysis (PCA), and exploratory multivariate analysis were used to evaluate relationships among formulation characteristics and functional performance. The nanoparticles formed stable colloidal systems with mean particle sizes ranging from 176 to 229 nm and maintained structural integrity during 28 days of refrigerated storage. Nanoparticle-enriched formulations exhibited higher β-glucan bioaccessibility, improved antioxidant retention, and stronger α-amylase and α-glucosidase inhibitory activities, with the greatest effects observed in V4. Protein digestibility remained high across all formulations, while sensory evaluation revealed improved overall liking and purchase intention. PCA indicated that nanoparticle concentration was the main factor differentiating the formulations based on their physicochemical and functional characteristics. Overall, protein–β-glucan nanoparticles enhanced the physicochemical, functional, and sensory properties of peach juice, supporting their application as multifunctional ingredients for functional beverage development. Full article

Cyclamen cyprium Kotschy, an endemic species of Cyprus, remains largely unexplored in terms of its chemical content and biological activity, despite the well-documented effects of other Cyclamen spp. This study aimed to characterize the phytochemical composition and biological activities of leaf extracts from the endemic C. cyprium and to compare them with those of Cyclamen persicum, the most extensively investigated species within the genus, in order to evaluate interspecific variation in phytochemical composition and bioactivity. Plant extracts prepared with methanol, ethanol, and acetone were assessed for total phenolic and flavonoid content. Their antioxidant activity (DPPH, ABTS, and FRAP assays), metal chelating ability, antimicrobial activity, and possible inhibitory effect related to α-amylase, α-glucosidase and acetylcholinesterase were also evaluated. The results demonstrated that solvent type significantly influenced extraction efficiency, with acetone yielding the highest phenolic (127.88 mg gallic acid/g) and flavonoid (110.42 mg rutin/g) content, while methanol extracts exhibited the strongest antioxidant activity (IC₅₀ = 30.18 μg/mL). Overall, C. persicum showed greater antioxidant capacity compared to C. cyprium, although both species demonstrated moderate antimicrobial activity (MIC = 0.31 mg/mL) and enzyme inhibitory activities (IC₅₀ values ranging from 14.07 to 39.64 μg/mL). Present findings highlight the presence of bioactive compounds (such as gallic acid, caffeic acid, rutin, and quercetin) in C. cyprium, supporting their potential as a natural source of antioxidant and pharmacologically relevant agents. Studying both C. cyprium and C. persicum thus provides essential comparative context, revealing species-specific bioactivities and supporting the broader pharmaceutical relevance of the genus. Full article

Background: Combining natural products with conventional antidiabetic agents to inhibit α-glucosidase activity is an effective strategy for preventing postprandial hyperglycemia. Baicalein, a natural flavonoid with well-documented low toxicity, showed potential synergistic effect with acarbose in diabetic models; however, the synergistic performance and mechanisms of the two agents targeting human maltase–glucoamylase (MGAM) remain unclear. Methods: Recombinant human MGAM-C and MGAM-N were expressed in Pichia pastoris for in vitro inhibition assays. Maltose-loaded mice were used to assess the in vivo hypoglycemic activity and intestinal maltase inhibition. Inhibitor–enzyme interactions were investigated by fluorescence spectroscopy, circular dichroism (CD), multiple molecular docking, and molecular dynamics (MD) simulations. Results: Baicalein potently inhibited MGAM-C and MGAM-N with IC₅₀ values of 20.41 ± 4.80 μM and 14.04 ± 0.94 μM, respectively, and demonstrated a synergistic effect when combined with acarbose. In vivo, co-administration significantly reduced blood glucose levels and suppressed small intestinal maltase activity in maltose-loaded mice. Mechanistic studies revealed that baicalein functions as a non-competitive inhibitor by binding to the allosteric site of MGAM-C via stable hydrogen bonds with residues Ile1716 and Trp1749. This interaction induces conformational changes in the enzyme’s secondary structure and optimizes the hydrophobic microenvironment of the active site, thereby enhancing the binding affinity and hydrogen bond stability of acarbose. These molecular events collectively contribute to the synergistic inhibition of MGAM-C hydrolytic activity. Conclusions: This research revealed the synergistic inhibitory effect of baicalein and acarbose on MGAM and the underlying mechanisms, thereby providing a theoretical basis for developing pharmaceutical formulations to enhance acarbose efficacy. Full article

Persicaria odorata (Lour.) contains considerable amounts of phytochemicals, including phenolics and essential oils, which have been reported to inhibit α-glucosidase activity. However, which bioactive compounds play a key role in inhibiting the α-glucosidase activity is unclear. To address this issue, the methanolic extract of P. odorata was assayed via in vitro studies, and forty-four compounds in P. odorata extracts were elucidated using in silico studies. The extract strongly inhibited yeast α-glucosidase with an IC₅₀ value of 0.31 µg/mL, which was 450-fold more potent than acarbose (IC₅₀ = 139.47 µg/mL), under experimental conditions. The Lineweaver–Burk plots indicated that the inhibition type of the extract on α-glucosidase is a noncompetitive inhibitor. Molecular docking demonstrated that procyanidin B (P9) and rutin (P19), which belong to the flavonoids, were predicted by computational approaches to be bioactive compounds that have more favorable binding interactions to yeast α-glucosidase residues compared to forty-four other compounds and acarbose. Molecular dynamics simulations revealed that P9 and P19 complexes with yeast α-glucosidase remained stable during the 500 ns simulations. Moreover, both P9 and P19 were predicted to qualify as α-glucosidase inhibitors with low toxicity. These findings suggest that P. odorata could be used as an alternative edible plant to manage postprandial hyperglycemia in T2DM, and could serve as basic scientific data. Further experimental studies of the pure bioactive compounds are necessary to support these findings. Full article

This study investigated the extracts and bioactive constituents of the aerial parts of Polygonum aviculare L., a well-known traditional medicine for inflammation and diuresis, through bioactivity-guided investigation and molecular docking analysis. Solvent extracts demonstrated significant antioxidant, anti-α-glucosidase, and anti-inflammatory activities, supporting their value for further pharmacological investigation. Among the isolated compounds, gallic acid (1), quercetin (3), myricetin (4), avicularin (6), and isorhamnetin (7) exhibited excellent antioxidant activity in the DPPH assay (SC₅₀ ≤ 6.50 μM) and were stronger than the positive control BHT (SC₅₀ = 36.99 μM). Kaempferol (9) (IC₅₀ of 4.50 µM) demonstrated the highest α-glucosidase inhibition, surpassing that of the clinically used acarbose (IC₅₀ = 519.7 µM). Additionally, gallic acid and quercetin demonstrated significantly stronger NO inhibition than apigenin, while kaempferol showed comparable activity (IC₅₀ = 15.06 ± 1.50 μM vs. 16.08 ± 1.86 μM for apigenin). Molecular docking analyses supported favorable interactions between the active compounds and α-glucosidase and inducible nitric oxide synthase (iNOS). Kaempferol reduced the expression of iNOS and COX-2 in LPS-stimulated RAW 264.7 macrophages and was associated with increased KLF4 and Arg-1 expression and decreased phosphorylation of p38 MAPK and IκBα, suggesting a potential role in promoting an anti-inflammatory M2-like macrophage phenotype. Structure–activity relationship analysis indicated that flavonoid aglycones and specific hydroxylation patterns contribute to the observed biological activities. Collectively, these findings identify quercetin and kaempferol as highly active constituents of P. aviculare and support their potential for further pharmacological investigation. 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

Chinese yam possesses anti-type 2 diabetes mellitus (T2DM) potential. However, existing research has focused on its polysaccharides rather than its abundant peptide components. Therefore, this study integrated peptidomics with network pharmacology and molecular docking to explore the potential anti-T2DM mechanisms of Chinese yam peptides. Firstly, this study revealed that crude peptides extracted from Chinese yam possessed a potential hypoglycemic activity, with an IC₅₀ of 568.87 μg/mL against α-glucosidase. Secondly, peptidomics identified 558 peptides with the sequences ranging from 3 to 25 residues. Thirdly, network pharmacology was conducted on 15 candidate peptides selected through bioactivity prediction and safety evaluation. These peptides shared 466 common targets with T2DM, with seven core targets identified through topological network analysis: SRC, EGFR, PTPN11, PIK3R1, ESR1, STAT3, and PIK3CA. Enrichment analysis revealed that these targets were significantly associated with PI3K-Akt and MAPK signaling pathways. Fourthly, molecular docking confirmed the strong binding affinities between the 15 bioactive peptides and seven core targets, particularly the high-affinity binding of peptides SIDLYENRL and RAPDDLDTRL to PIK3CA. Collectively, these findings demonstrate that Chinese yam peptides possess potential hypoglycemic activity and may ameliorate T2DM through the regulation of insulin signaling via PI3K-Akt activation and the modulation of inflammation via the MAPK pathway. Full article

Background/Objectives: Morinda lucida Benth is widely distributed throughout Central and West Africa. It has traditionally been used to treat and manage various diseases. However, scientific research on its phytochemical and pharmacological properties remains scarce. This study investigated the phytochemical profiles, antioxidant activities, α-glucosidase inhibitors, and cytotoxic effects of compounds derived from various parts of M. lucida. Methods: Seventy-seven natural compounds were putatively annotated using ¹H-NMR, UHPLC–Q Exactive Orbitrap MS, and molecular networking techniques. The antioxidant activities of the crude extracts were assessed in vitro using DPPH free radical scavenging and reducing power assays, whereas the in vitro α-glucosidase inhibition activity and toxicity of the crude extracts were evaluated using the α-glucosidase inhibition and MTT assays. Molecular docking was used to assess the interactions between the identified glycosides and the α-glucosidase protein. Results: The root extract exhibited the highest DPPH free radical scavenging (IC₅₀ = 7.7550 ± 6.9142 μg/mL) and reducing power capacity (IC_0.5 = 0.0052 ± 0.0025 μg/mL). In contrast, the stem bark extract demonstrated significant inhibition of alpha-glucosidase (IC₅₀ = 79.9 ± 16.1 µg/mL). Sophoricoside, formononetin 7-O-glucoside, and epicatechin identified in the stem bark extract showed notable in silico interactions with the α-glucosidase protein. The stem bark and leaf extracts were more toxic than the root extract at different concentrations. Conclusions: The results of this study demonstrate the therapeutic potential of M. lucida and provide information on its phytochemical composition and pharmacological properties. 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

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

Background: Bougainvillea species have been used in traditional Mexican medicine, but their bioactive compounds and mechanisms of action are insufficiently studied. This is the first comprehensive evaluation of fractions from the acetone extract of Bougainvillea × buttiana Holtum & Standl (var. Rose), combining phytochemical profiling with in vitro multitarget bioactivity assessment. Methods: Eleven fractions were analyzed for total phenolic (TPC) and flavonoid content (TFC) and antioxidant capacity using the DPPH assay. The most active fractions were further tested for nitric oxide (NO) scavenging, protection of erythrocytes and bovine serum albumin (BSA) from oxidative damage, inhibition of enzymes involved in inflammation (PLA₂, COX, LOX) and carbohydrate metabolism (α-glucosidase, α-amylase, tyrosinase), cytoprotective effects in L929 fibroblasts exposed to hydrogen peroxide, and their main metabolites were qualitatively identified by HPLC-UV-Vis. Results: All fractions showed significant TPC and TFC and concentration-dependent antioxidant activity. The fractions with the highest antioxidant indices were F5, F7, and F9. These effectively scavenged NO, protected erythrocytes and L929 cells (maintaining viability at 82.0%, 75.6%, and 72.0%, respectively), and inhibited key enzymes. Seven major compounds, mainly flavonoids, were identified. Conclusions: These findings showed that flavonoid-enriched fractions from B. × buttiana exhibit coordinated antioxidant, anti-inflammatory, antidiabetic, and cytoprotective effects, suggesting potential to treat oxidative stress-related disorders. 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

Background: Rosmarinus officinalis L. is a medicinally important aromatic plant rich in bioactive secondary metabolites with diverse therapeutic properties. This study aimed to characterize the phytochemical profile of R. officinalis leaf extracts, isolate carnosic acid as a major bioactive diterpene, and evaluate its biological activities. Methods: Leaf extracts were prepared using solvents of increasing polarity and analyzed by phytochemical screening and UHPLC/QTOF-MS. Carnosic acid was isolated by thin-layer chromatography and assessed for antibacterial, antibiofilm, antioxidant, anti-inflammatory, antidiabetic, and antiproliferative activities using in vitro assays. Expression of apoptosis-related genes was also investigated. Results: Methanolic and ethanolic extracts exhibited the highest abundance of phenolic compounds and secondary metabolites, whereas the hexane extract showed lower phytochemical content. UHPLC/QTOF-MS identified seven major metabolites, including phenolic acids, flavonoids, and abietane-type diterpenes. Purified carnosic acid demonstrated potent antibacterial activity (MIC: 10–23 μg/mL) and inhibited biofilm formation by up to 90%. Strong antioxidant activity was observed, with DPPH and ABTS radical-scavenging IC₅₀ values of 125 and 130 μg/mL, respectively. The compound also exhibited notable anti-inflammatory activity and markedly inhibited α-amylase and α-glucosidase activities. Furthermore, carnosic acid exhibited dose-dependent antiproliferative activity against MCF-7, HepG2, and MCF-10A cells, reducing cell viability to 10.8%, 16.9%, and 70.4 ± 1.8%, respectively, at 250 μg/mL, with corresponding IC₅₀ values of 28.3, 37.8, and >250 μg/mL, respectively. Gene expression analysis revealed upregulation of BAX and downregulation of BCL2, indicating activation of mitochondrial-mediated apoptosis. Conclusions:R. officinalis leaves represent a valuable source of multifunctional phytochemicals, particularly carnosic acid. Its broad-spectrum biological activities and apoptosis-inducing potential support its promising application in pharmaceutical, nutraceutical, and biomedical fields. Full article