Search Results (1,057)

Background/Objectives: The increasing global prevalence of chronic diseases has intensified the search for potential natural therapeutic agents. Fagonia arabica is a medicinal plant widely used in traditional medicine; however, comparative information on the phytochemical composition and biological activities of its leaves and seeds remains limited. To the best of our knowledge, this study represents the first comparative investigation of the phytochemical profiles and bioactivities of methanolic leaf (FALE) and seed (FASE) extracts of F. arabica collected from Riyadh, Saudi Arabia. Methods: Methanolic extracts were analyzed by gas chromatography–mass spectrometry (GC–MS), and their total phenolic content (TPC), total flavonoid content (TFC), antioxidant, antimicrobial, anticancer, and antidiabetic activities were evaluated using standard in vitro assays. Results: GC–MS analysis identified 60 and 68 compounds in FALE and FASE, respectively, with (9Z,12Z,15Z)-octadeca-9,12,15-trienoic acid, hexadecanoic acid, dimethyl-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-3-ol, and (1R,3aR,5aR,5bR,7aR,9S,11aR,11bR,13aR,13bR)-3a,5a,5b,8,8,11a-Hexamethyl-1-(prop-1-en-2-yl)-1,2,3,4,5,6,7,7a,9,10,11,11b,12,13,13a,13b-hexadecahydrocyclopenta[a]chrysen-9-ol as major constituents. FASE exhibited higher TPC and TFC values (104.13 mg GAE/g and 62.16 mg QE/g, respectively) than FALE. Both extracts demonstrated antioxidant activity, with FASE showing greater potency against DPPH and ABTS radicals (IC₅₀ = 63.3 and 42.4 μg/mL, respectively). FASE also displayed broad-spectrum antimicrobial activity, particularly against Staphylococcus aureus (MIC = 7.81 μg/mL). Furthermore, FASE exhibited stronger concentration-dependent cytotoxicity against MCF-7 and HepG2 cells, with IC₅₀ values of 106.8 and 89.5 μg/mL, respectively, compared with 112.5 and 103.1 μg/mL for FALE. Apoptosis induction in MCF-7 and HepG2 cells was associated with upregulation of caspase-3, caspase-8, caspase-9, and Bax, alongside downregulation of Bcl-2 and Bcl-xL. In addition, FASE exhibited potent α-amylase and α-glucosidase inhibitory activities (IC₅₀ = 61.62 and 67.38 μg/mL, respectively), comparable to acarbose. Conclusions: These findings highlight F. arabica seed extract as a promising source of multifunctional bioactive compounds with potential pharmaceutical application. Full article

Flavones are natural substances widely distributed in fruits and vegetable. Their compounds are characterized by a broad spectrum of activities, including antioxidant activity. Their most interesting biological effect, however, is antihyperglycemic activity, mediated by the inhibition of α-glucosidase. A series of 7-hydroxyflavone derivatives was synthesized and comprehensively characterized using nuclear resonance magnetic spectroscopy. The biological potential of the synthesized derivatives was assessed through antioxidant (DPPH) and α-glucosidase inhibitory assays. The physicochemical and pharmacokinetic properties were analyzed using in silico methods. Finally, molecular docking studies were performed to elucidate the binding mode of compounds within the catalytic site of α-glucosidase. Full article

1-Deoxynojirimycin (DNJ), a well-characterized α-glucosidase inhibitor, remains an important target for dose-reduction and formulation strategies. In the present study, we evaluated the individual and combined α-glucosidase inhibitory activities of nine dietary flavonoids with DNJ, quantified synergistic effects using the combination index (CI) method, and elucidated the molecular mechanism through integrated enzyme kinetics, multi-spectroscopic techniques and molecular docking. (+)-Catechin exhibited the strongest inhibitory activity (IC₅₀ = 33.7 ± 2.7 μM), and its combination with DNJ produced synergistic inhibition across all doses (CI < 0.7). Kinetic analysis confirmed that DNJ acted as a competitive inhibitor, while (+)-catechin functioned as a non-competitive inhibitor. Fluorescence quenching assays revealed that (+)-catechin pre-incubation increased the binding affinity of DNJ to α-glucosidase by 393%. Circular dichroism spectroscopy showed that (+)-catechin induced a marked β-sheet-to-α-helix conformational conversion, and co-incubation of both inhibitors produced more secondary structural changes than either inhibitor alone. Molecular docking further confirmed their distinct binding sites. These findings demonstrate that (+)-catechin synergistically potentiates DNJ activity through allosteric conformational modulation, providing an experimental basis for optimizing DNJ-containing formulations. Full article

Andean crops, including quinoa (Chenopodium quinoa), amaranth species including kiwicha (Amaranthus caudatus), chocho (Lupinus mutabilis), and cañihua (Chenopodium pallidicaule), constitute promising protein matrices for bioactive peptide generation by microbial fermentation and enzymatic proteolysis. These pseudocereals and legumes contain storage proteins, mainly 11S globulins and 2S albumins, enriched in lysine and sulfur-containing amino acids, and therefore provide suitable precursors for multifunctional peptides. In addition, secondary metabolites, such as quinoa saponins and chocho alkaloids, may influence proteolysis, peptide release, and peptide stability during fermentation. This review critically examines LAB fermentation as a food-grade strategy for bioactive peptide production from Andean crops. Evidence from enzymatic hydrolysis and simulated gastrointestinal digestion is included as complementary information and is discussed separately from fermentation-derived evidence. Reported activities include antioxidant, ACE-inhibitory, DPP-IV- and α-glucosidase-inhibitory, antimicrobial and anti-inflammatory activities. Particular attention is given to peptide generation, molecular-weight fractionation, peptidomic characterization, structure–activity relationships, simulated gastrointestinal digestion, and bioaccessibility. Most reported activities were measured in hydrolysates or molecular-weight fractions rather than in defined sequences, and individually validated peptides remain a minority. The strength of evidence differs markedly among crops: fermentation-derived data are more developed for quinoa and amaranth, whereas evidence for chocho and cañihua relies largely on enzymatic hydrolysis. Current limitations, including substrate variability, sensory acceptability, process standardization, peptide identification, bioavailability, and the lack of human validation studies, are also discussed. Andean crop proteins are promising precursors of functional peptide ingredients; however, peptide-specific bioavailability and human efficacy remain largely untested. Full article

Gyrinops vidalii (Thymelaeaceae), a critically endangered agarwood-producing species native to Thailand and Laos and remains phytochemically unexplored. In this study, the chemical constituents and biological activities of the ethyl acetate (EtOAc) fraction of methanol extract of G. vidalii leaves were investigated. Phytochemical analysis led the isolation of mangiferin (1), iriflophenone 3-C-β-D-glucoside (2), aquilarinenside E (3), iriflophenone 2-O-α-L-rhamnoside (4), 5,7,4′-trimethoxyflavone (5), blumenol A (6), loliolide (7), 4-hydroxybenzoic acid methyl ester (8), and 4-hydroxybenzoic acid (9). Compound 1 exhibited potent DPPH radical scavenging activity with an SC₅₀ value of 19.35 μM), whereas iriflophenone (3a), obtained by acid hydrolysis of 3, and 5 showed promising α-glucosidase inhibitory activity with IC₅₀ values 100.06 and 174.57 μM, respectively. Molecular docking demonstrated favorable binding of both compounds within the α-glucosidase active site through hydrogen bonding, aromatic, and hydrophobic interactions, with binding energies of −7.4 and −8.0 kcal/mol, respectively. Predicted ADMET properties further supported the drug-like potential of both compounds, indicating favorable aqueous solubility, high intestinal absorption, and no predicted hepatotoxicity, while differences were observed in their predicted blood–brain barrier permeability. This study represents the first phytochemical investigation of G. vidalii, provides scientific support for its traditional use, and expands the chemotaxonomic knowledge of the closely related genera Gyrinops and Aquilaria. Full article

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

Fucoidans are sulphated polysaccharides from brown macroalgae that have attracted considerable interest due to their diverse biological activities and potential applications in metabolic health. In this study, fucoidan-rich extracts were obtained from three South African brown macroalgal species, Ecklonia maxima, Ecklonia radiata, and Sargassum incisifolium, and comparatively characterised using biochemical and physicochemical analyses. The extracts were evaluated for carbohydrate, sulphate, L-fucose, protein, polyphenol, and uronic acid contents, while molecular weight distribution, Fourier-transform infrared spectroscopy (FTIR), thermogravimetric analysis (TGA), and proton Nuclear Magnetic Resonance (¹H NMR) spectroscopy were used to investigate structural characteristics. All extracts displayed features characteristic of fucoidans, including sulphated fucose-containing polysaccharides. Notable species-dependent differences were observed, with S. incisifolium exhibiting the highest sulphate (~24%) and polyphenol (~6.76%) contents, stronger sulphate-associated FTIR signals, greater molecular weight heterogeneity, and enhanced thermal stability. The fucoidan-rich extracts exhibited concentration-dependent pancreatic lipase and α-glucosidase inhibitory activities, together with DPPH radical-scavenging activity. At 1.0 mg/mL, S. incisifolium demonstrated approximately 66% DPPH radical scavenging and 49% pancreatic lipase inhibition. S. incisifolium and E. radiata exhibited strong α-glucosidase inhibition, with IC₅₀ values of ~29 and ~46 µg/mL, respectively, compared to ~354 µg/mL for acarbose. The findings highlight South African brown macroalgae as promising sources of fucoidans and contribute to understanding the relationships among fucoidan composition, structure, and bioactivity. 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

High fructose intake rapidly induces protein glycation, oxidative stress, inflammation, and disturbances in the cultivable fraction of gut bacteria, contributing to early metabolic impairment. This study examined whether selected plant-derived bioactives and a prebiotic–probiotic formulation could mitigate fructose-induced biochemical and microbial alterations. Male Wistar rats were fed fructose for 45 days, and advanced glycation end product (AGE)-associated fluorescence, oxidative stress markers, and lipid peroxidation were measured to assess metabolic changes. Culture-dependent enumeration of intestinal and fecal bacteria was performed to evaluate shifts in cultivable aerobic and facultative bacterial counts, while limonene, eugenol, and emodin were tested for antibacterial activity against aerobic and facultative bacterial isolates obtained from fructose-fed rats during our previous study. The prebiotic–probiotic formulation was assessed alone and in combination with these bioactives. Fructose feeding increased protein glycation, oxidative stress, lipid peroxidation, and reduced counts of cultivable gut bacteria. Treatment with the bioactives and the formulation lowered glycation-related fluorescence, reduced oxidative stress, and decreased lipid peroxidation. The bioactives exhibited antioxidant and antiglycation activity and inhibited growth of selected cultivable bacterial isolates, including Corynebacterium stationis. While emodin contributed primarily through its known α-glucosidase inhibitory and antiglycation properties rather than antibacterial activity. Combined treatment partially restored cultivable bacterial counts and improved metabolic parameters. Overall, the interventions attenuated fructose-induced biochemical disturbances and modulated the cultivable gut bacterial counts, suggesting a complementary approach to managing early metabolic changes in rats associated with high fructose intake. Full article

In this study, total flavonoids from Polygonum perfoliatum L. (PPTF) were extracted using ionic liquid-assisted ultrasound and purified by macroporous resin. After optimization, the total flavonoid content increased from 33.9% to 71.2%. HPLC identified hyperoside, kaempferol-3-O-rutinoside, and quercetin. In vitro experiments showed that PPTF exhibited good free radical scavenging activity and inhibitory effects on α-glucosidase and α-amylase. Within the concentration range of 3.13–12.50 μg/mL, PPTF was non-toxic to HepG2 cells and improved glucose uptake, promoted glycogen synthesis, and reduced lipid accumulation in insulin-resistant cells in a dose-dependent manner. In a type 2 diabetic mouse model induced by high-fat diet combined with streptozotocin, intragastric administration of PPTF for four weeks significantly lowered fasting blood glucose in the high-dose group, improved oral glucose tolerance and insulin sensitivity, increased hepatic and muscle glycogen, normalized serum lipid profiles, and alleviated pathological damage in the liver and pancreas. PPTF exhibits favorable hypoglycemic and lipid-regulating effects in both cellular and animal models, demonstrating its potential for development as an adjunctive functional product for glycemic management. 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

The global rise in obesity and associated metabolic disorders has fueled the demand for safe, multi-target therapeutics derived from natural sources. In this study, an artificial neural network combined with a genetic algorithm (ANN-GA), was employed to optimize the ultrasound-assisted extraction of loquat leaf extract (LLE). The optimal parameters—0.6% Tween 80, 328 W ultrasonic power, and 49 °C—enhanced extraction efficiency while minimizing energy consumption and surfactant use. In vitro, LLE exhibited potent dose-dependent inhibition of α-glucosidase (IC₅₀ = 3.75 μg/mL, 21.6-fold stronger than acarbose) and pancreatic lipase (IC₅₀ = 78.3 μg/mL), indicating strong inhibitory activity against these digestive enzymes. In high-fat diet-induced obese mice, LLE supplementation dose-dependently reduced body weight gain, serum total cholesterol, triglycerides, low-density lipoprotein cholesterol (LDL-C), and fasting blood glucose while elevating high-density lipoprotein cholesterol (HDL-C). In addition, LLE ameliorated liver injury (decreased ALT/AST) and oxidative stress (lowered MDA, increased SOD). These findings highlight LLE as a promising multi-target natural product for managing obesity and related metabolic disorders. 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

Silybum marianum (SM) is a rich source of flavonolignans with promising antioxidant and antidiabetic properties; however, its therapeutic application is limited by poor stability and bioavailability. This study combined experimental and computational approaches to develop and evaluate SM-loaded chitosan nanoparticles (CS–SM nanoparticles). Microwave-assisted extraction followed by LC-MS/MS profiling identified eleven metabolites, including major flavonolignans characteristic of SM. Nanoparticles prepared by ionic gelation exhibited favorable physicochemical properties, including a particle size of 173–189 nm, a polydispersity index of 0.23, a zeta potential of +41.5 mV, an encapsulation efficiency of 98%, and a drug loading capacity of 50%, indicating the formation of a stable colloidal delivery system. CS–SM nanoparticles showed enhanced antioxidant, anti-inflammatory, and α-amylase inhibitory activities compared with crude extracts. The formulation exhibited an α-amylase IC₅₀ value of approximately 0.40 mg/mL and maintained low hemolytic activity, suggesting favorable preliminary biocompatibility. Molecular docking demonstrated favorable interactions of neosilyhermin A, silibinin, and silyhermin with α-amylase and α-glucosidase active sites. Short-timescale molecular dynamics simulations revealed ligand-dependent behavior within the chitosan–TPP matrix, indicating different release tendencies among the investigated flavonolignans. Overall, the results support CS–SM nanoparticles as a promising platform for the delivery of bioactive phytochemicals with antioxidant and antidiabetic potential. Full article