Search Results (111)

Background/Objectives: Type 2 diabetes mellitus (T2DM) is characterized by chronic hyperglycemia and insulin resistance, leading to progressive metabolic dysfunction. Flavonoids, such as astragalin, have reported antidiabetic potential; however, their direct effects on pancreatic β-cell ionic mechanisms and insulin secretion remain unclear. This study aimed to investigate the effects of astragalin on glucose uptake, insulin secretion, and membrane ionic currents in pancreatic β-cell lines. Methods: Murine MIN6 and rat INS-1 pancreatic β-cells were used as experimental models. Following astragalin treatment, glucose uptake was quantified by bioluminescence, and insulin secretion was measured by ELISA. Ionic currents were analyzed using the whole-cell patch-clamp technique. Selective pharmacological blockers targeting ATP-sensitive K⁺ channels (KATP), voltage-dependent K⁺ channels (K_v), and L-type voltage-dependent Ca²⁺ channels were applied to elucidate the underlying mechanisms. Results: Astragalin increased glucose uptake in a time-dependent manner, reaching a plateau between 3 and 5 h. Insulin secretion was significantly enhanced after 1 h of exposure to 100 µM astragalin. Patch-clamp recordings demonstrated that astragalin reduced potassium channel currents in pancreatic β-cells. Pharmacological modulation confirmed the involvement of KATP, K_v, and L-type Ca²⁺ channels. Verapamil attenuated the insulinotropic effect, supporting the role of calcium influx in astragalin-induced insulin exocytosis. Conclusions: Astragalin enhances glucose uptake and stimulates insulin secretion in pancreatic β-cells through modulation of potassium and calcium channels, promoting calcium-dependent exocytosis. These findings support its potential as a candidate for antidiabetic therapeutic strategies. Full article

Diabetes Mellitus is a complex metabolic disorder, primarily characterized by persistent high blood sugar levels, and it is becoming increasingly prevalent with numerous associated complications. The leaves of Cyclocarya paliurus (Batal.) Iljinskja, traditionally prepared as a tea beverage in China, is frequently used in folk medicine for managing metabolic syndromes, particularly diabetes and hyperlipidemia. However, the main active components responsible for its hypoglycemic effect and their underlying mechanisms remain unclear. The current study aimed to clarify the main chemical components of the aqueous extract of C. paliurus leaves and to explore their mechanisms of action. The primary constituents from the aqueous extract of C. paliurus leaves were isolated and identified using macroporous adsorption resin, preparative liquid chromatography, and nuclear magnetic resonance technology. The contents of these identified compounds in the leaves were quantified using HPLC. An integrated approach combining network pharmacology and molecular docking was initially used to predict the potential molecular targets and associated signaling pathways responsible for the hypoglycemic activity of the compounds, with subsequent experimental validation performed in a hyperglycemic zebrafish model. From the aqueous extract, a total of seven compounds were obtained and subsequently identified as Chlorogenic Acid (CA), Quercetin-3-O-β-D-glucuronide (Q3GA), Astragalin, 3,4-Dicaffeoylquinic Acid (3,4-DCA), Afzelin, Quercetin, and Kaempferol. Their contents in C. paliurus leaves, as determined by HPLC, were 24.88 mg/g, 30.87 mg/g, 1.21 mg/g, 1.19 mg/g, 5.24 mg/g, 2.43 mg/g, and 1.34 mg/g, respectively. Network pharmacology analysis identified AKT1, TNF, and IL1B as key targets for the hypoglycemic effects of both the aqueous extract and the seven individual compounds. These findings were further supported by RT-PCR experiments in a zebrafish model, which showed that blood glucose regulation occurs through the downregulation of TNF and IL1B and the upregulation of AKT1 protein. The aqueous extract is rich in Chlorogenic Acid, Quercetin, and their derivatives, all of which display significant hypoglycemic activity. Full article

Heracleum sosnowskyi is considered to be a dangerous invasive plant species that has successfully naturalized within a variety of plant communities across numerous countries. As a result of its superior competitiveness, the alien species is able to displace the indigenous species from their native habitats, thus changing the ecosystems and decreasing biodiversity. The phytochemicals present in the H. sosnowskyi aqueous extracts were revealed using GC/MS and HPLC/DAD/TOF techniques. Isopsoralen, methoxsalen, (iso)pimpinellin and/or bergapten were determined to be major compounds in the leaf, inflorescence and root extracts. Glutaric, quinic, linolenic, (iso)chlorogenic and other polyphenolic acids were identified in the extracts. Furthermore, a number of furanocoumarins, including hermandiol, bakuchicin, candinols (A and C) and candibirin F, and coumarins, umbelliferone and yunngnins (A and B), were identified in the roots. Additionally, the presence of flavonoids, including astragalin, quercetin 7,3,4-trimethyl ether, nicotiflorin and rutin, has been detected in the flower and leaf extracts. Allelopathic effects of H. sosnowskyi aqueous extracts were tested on four model plants, lettuce (Lactuca sativa L.) and three native Lithuanian meadow herbs, perennial ryegrass (Lolium perenne L.), timothy (Phleum pratense L.) and white clover (Trifolium repens L.), using the Petri dish method. H. sosnowskyi flower and leaf extracts demonstrated the strongest inhibitory effects on the germination and growth of the tested plant seeds. At the highest relative concentrations, 0.5 and 1.0, extracts of Sosnowsky’s hogweed inflorescences inhibited timothy seedling growth by 95.47% (from 19.64 ± 2.57 mm to 0.89 ± 0.73 mm) and 100%, respectively. The leaf extracts exhibited the strongest inhibitory effects on white clover seedlings. The highest relative concentrations tested (0.5 and 1.0) suppressed clover seedling growth by 94.66% (from 41.22 ± 2.53 mm to 2.20 ± 0.63 mm) and 100%, respectively. Additionally, the germination rate and vigor index of model plants were assessed. The research is of significance for the regulation and monitoring of the spreading of aggressive H. sosnowskyi plants. Moreover, it is important for the development of natural herbicides based on active phytotoxic compounds from these plants. Full article

Ptelea trifoliata L. is a perennial plant of the Rutaceae family and contains secondary metabolites with potential biological relevance. Due to limited information on its activity, the objective of this study was to evaluate the biological properties of its flower extracts and to determine their phytochemical composition. Flowers were dried and subjected to ultrasound-assisted extraction using methanol, 60% methanol and water. LC–MS/MS was used for qualitative profiling, HPLC for quantitative determination, and spectrophotometry for measuring total phenolic and flavonoid content. The antioxidative capacity of the extracts was determined using DPPH, CUPRAC, FRAP, and iron chelation assays. Enzymatic inhibition analyses were performed for hyaluronidase, indicative of anti-inflammatory properties, and tyrosinase, associated with pigmentation mechanisms. The wound-healing capacity was evaluated in vitro using a scratch assay. Our research revealed the highest levels of polyphenols in the 60% methanol extract and of flavonoids in the methanol extract. The occurrence of chlorogenic acid, rutin, hyperoside, and astragalin was also demonstrated. Both methanol and 60% methanol extracts demonstrated antioxidant effects. The methanol extract showed the greatest hyaluronidase inhibition, while the 60% methanol extract was the most effective in suppressing tyrosinase activity and promoting wound closure. Principal component analysis showed that the contents of polyphenols or flavonoids were associated with enzyme-inhibitory or antioxidant activities. Moreover, the 60% methanol and water extracts exhibited notable wound healing properties. These results highlight the antioxidant, enzyme-modulating and regenerative potential of P. trifoliata flower extracts, suggesting their possible use in biomedical and dermatological applications. Full article

The sustainable cultivation of Moringa oleifera is constrained by limited availability of high-quality planting materials. This study established an integrated propagation framework combining seed, cutting, and air-layering methods for the rapid and reliable multiplication of superior genotypes with good morphological traits and elevated astragalin content. Seed pretreatment trials showed that simple soaking for 12 h significantly reduced mean germination time without affecting final germination percentage, while a topsoil–cocopeat–compost mixture enhanced early seedling survival and growth. HPLC profiling identified four genotypes with significantly higher astragalin concentrations (187–281 ppm), linking phytochemical quality with propagation performance. Vegetative propagation experiments revealed that cutting position and girth strongly influenced regeneration success. Cutting position experiments showed clear positional differences, with basal cuttings achieving the highest rooting response. Bottom cuttings produced the highest number of shoots (4.22), nodes (5.00), and thickest shoots (24.65 mm), as well as the highest rooting percentage. Middle cuttings developed the longest shoots (40.21 cm) and the greatest number of roots (32.83), with a rooting percentage of 66.70%. Top cuttings showed the lowest performance across all shoot and root traits. Larger-diameter cuttings produced more shoots but fewer roots while smaller-diameter cuttings produced more roots but fewer shoots. Air-layering with Jiffy-7 pellets achieved the highest root number (43.83) and length (7.23 cm), with 100% survival. Overall, the study provides a robust, mechanism-supported propagation strategy that enables large-scale, uniform production of superior Moringa genotypes, strengthening future programs in clonal improvement, genetic conservation, and sustainable agroforestry development. Full article

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

Gastrodiae Rhizoma (GR) is known to have a medicinal and food-based homology. It is used to treat infantile convulsion, epilepsy, spasm, tetanus, and vertigo. In this study, an ultra-high performance liquid chromatography/tandem mass spectrometry (UHPLC-MS/MS) method was developed and validated to quantify fourteen components (p-hydroxybenzyl alcohol, gastrodin, parishin E, p-hydroxybenzoic acid, parishin C, parishin A, parishin B, nicotinamide, p-hydroxybenzaldehyde, adenosine, 3,4-dihydroxybenzaldehyde, syringaldehyde, dauricine, and nobiletin) of GR in rat plasma. Methanol precipitation was used to prepare the samples with astragalin, serving as the internal standard. In multiple reaction monitoring (MRM) mode, the fourteen components were separated by gradient elution on a Waters ACQUITY UPLC^® HSS T3 column. Under these conditions, all fourteen analytes’ calibration curves demonstrated strong linearity within wide concentration ranges (r > 0.9941). Accuracy for the intra-day and inter-day assessments ranged from −13.74% to 12.76%, and the precision for all analytes remained below 8.88%. The analytes’ extraction recoveries ranged from 66.78% to 114.2%, accompanied by matrix effects ranging from 63.65% to 117.61%. Under the evaluated conditions, stability tests confirmed that the compounds remained stable, with relative standard deviations below 13.83%. Consequently, the UHPLC-MS/MS method was effectively used to determine the pharmacokinetics of fourteen components in rat plasma after oral administration of GR extract. This study provides supportive data for rational application of GR. Full article

Background: Bone metastasis of breast cancer (BC) is a key reason for poor prognosis. Recently, natural ingredients derived from plants have been found to exert a broad anti-tumor effect and are considered to be promising candidates for adjuvant therapy. Astragalin (AS) was found to inhibit the progression of several types of tumors; however, the role of AS in regulating the bone metastasis of BC is still unclear. Methods: The effects of AS on the progression of bone metastasis of BC were detected in vivo through safranin O and fast green staining, in vivo living imaging and microCT. The BrdU assay and Annexin V-PI analysis were used to detect the effects of AS on the growth of BC cells. Furthermore, TRAP staining was performed to examine the formation of osteoclasts regulated by AS. A transcriptome was performed to explore the downstream effects of AS on regulating the growth of BC cells, and the mechanism was further confirmed by Western blot and real-time PCR. Results: Administration of AS could effectively attenuate the bone destruction and the progression of bone metastasis of BC. The growth of BC cells can be inhibited by AS by inducing ER stress-mediated upregulation of Ddit3. In addition, AS can also prevent osteoclastogenesis through inhibiting the activation of the AKT pathway. Conclusions: Our studies suggest that AS could be an ideal adjuvant therapy for attenuating the progression of bone metastasis of BC, since it can directly restrict the growth of tumor, as well as attenuate osteolysis. Full article

Objective: The study investigates the dietary effects of Moringa oleifera leaf powder on obesity, blood biochemical parameters, and organ health in hyperlipidemic zebrafish (Danio rerio). Methodology: Adult hyperlipidemic zebrafish (n = 56/group) were fed for 12 weeks either with a high-cholesterol diet (HCD, 4% w/w) or HCD supplemented with 0.5% (w/w) M. oleifera leaf powder (0.5% MO) or HCD with 1.0% (w/w) M. oleifera leaf powder (1.0% MO). At different time points (0 to 12 weeks), the survivability and body weight (BW) of zebrafish were measured, while various biochemical and histological evaluations were performed after 12 weeks of feeding the respective diets. Additionally, an in silico approach was used to assess the binding interactions of MO phytoconstituents with 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase. Results: Following 12-week supplementation, higher zebrafish survivability was observed in the MO-supplemented groups compared to the survivability of the HCD group. Relative to the initial BW, only 4% BW enhancement was observed post 12 weeks of dietary intake of 1.0% MO, in contrast to 27% BW gain in the HCD group. MO supplementation at both (0.5% and 1.0%) effectively mitigates the HCD-induced dyslipidemia and significantly minimizes the atherogenic coefficient and atherogenic index. Similarly, MO reduces elevated blood glucose levels, the ALT/AST ratio, and augments ferric ion reduction (FRA) and paraoxonase (PON) activity in a dose-dependent manner. Likewise, MO (particularly at 1.0%) effectively restrained HCD-induced steatosis, hepatic interleukin (IL)-6 production, and protected the kidneys, testes, and ovaries from oxidative stress and cellular senescence. The in silico findings underscore that the six phytoconstituents (chlorogenic acid, isoquercetin, kaempferol 3-O-rutinoside, astragalin, apigetrin, and myricetin) of MO exhibited a strong interaction with HMG-CoA reductase active and binding site residues via hydrogen and hydrophobic interactions. Conclusions: The findings demonstrated an antioxidant, anti-inflammatory, and hypoglycemic effect of MO, guiding the events to prevent HCD-induced metabolic stress and safeguard vital organs. Full article

Gynura procumbens is a commonly adopted medicinal plant native to the tropical regions of East and Southeast Asia and is well recognized for its significant therapeutic potential. Traditionally used in herbal medicine, it has been employed to manage various conditions, including hypertension, diabetes, renal disorders, constipation, and inflammation. Its leaves are particularly rich in flavonoids—such as astragalin, kaempferol, quercetin, myricetin, and rutin—which are associated with anti-glycaemic, anticancer, antihypertensive, antimicrobial, and antioxidant activities. These bioactive constituents form the basis of the broad pharmacological profile of the plant. Emerging studies also suggest a potential role for G. procumbens in the management of infertility, further broadening its therapeutic scope. This review provides a concise overview of its phytochemical constituents, taxonomic classification, and current pharmacological evidence, highlighting its potential as a valuable candidate for novel drug development. Full article

The rust disease caused by Melampsora apocyni seriously affects the growth of Poacynum hendersonii. However, the defense mechanisms against rust infection remain unclear. This study explored the regulatory mechanisms of P. hendersonii in response to rust disease through combined physiological, biochemical, and transcriptomic analyses. The results showed that with the increase in disease severity, the chlorophyll content of leaves decreased significantly, while the antioxidant and phenylalanine ammonia lyase activities progressively increased. Mild infection triggered an 11.9-fold surge in salicylic acid levels and a sharp decline in abscisic acid compared to controls, as well as increased synthesis of total phenolics, total flavonoids, chlorogenic acid, cryptochlorogenic acid, isoquercetin, hyperoside, rutin, and astragalin. Transcriptome analysis showed that the “plant–pathogen interaction, plant hormone signal transduction and phenylpropanoid biosynthesis” pathways were significantly up-regulated in the mild infection stage, while “glycerophospholipid metabolism, fatty acid degradation and ABC transporters” were activated in the severe infection stage. In summary, P. hendersonii regulates energy metabolism and phenylpropanoid metabolism through salicylic acid signaling and promotes the accumulation of secondary metabolites and the lignification process of leaves, thereby enhancing rust resistance. Key enzyme genes (COMT, POD, CAD, F5H) and metabolites (chlorogenic acid, isoquercitrin, rutin) can be used as important targets for disease resistance breeding. Our research provides important reference for the prevention and control of M. apocyni in P. hendersonii. Full article

Background/Objectives: Oncogenic KRAS drives ~30% of solid tumours, yet the only approved G12C-specific drugs benefit ≈ 13% of KRAS-mutant patients, leaving a major clinical gap. We sought mutation-agnostic natural ligands from Ziziphus lotus, whose stereochemically rich phenolics may overcome this limitation by occupying the SI/II (Switch I/Switch II) groove and locking KRAS in its inactive state. Methods: Phytochemical mining yielded five recurrent phenolics, such as (+)-catechin, hyperin, astragalin, eriodictyol, and the prenylated benzoate amorfrutin A, benchmarked against the covalent inhibitor sotorasib. An in silico cascade combined SI/II docking, multi-parameter ADME/T (Absorption, Distribution, Metabolism, Excretion, and Toxicity) filtering, and 100 ns explicit solvent molecular dynamics simulations. Pharmacokinetic modelling predicted oral absorption, Lipinski compliance, mutagenicity, and acute-toxicity class. Results: Hyperin and astragalin showed the strongest non-covalent affinities (−8.6 kcal mol⁻¹) by forging quadridentate hydrogen-bond networks that bridge the P-loop (Asp30/Glu31) to the α3-loop cleft (Asp119/Ala146). Catechin (−8.5 kcal mol⁻¹) balanced polar anchoring with entropic economy. ADME ranked amorfrutin A the highest for predicted oral absorption (93%) but highlighted lipophilic solubility limits; glycosylated flavonols breached Lipinski rules yet remained non-mutagenic with class-5 acute-toxicity liability. Molecular dynamics trajectories confirmed that hyperin clamps the SI/II groove, suppressing loop RMSF below 0.20 nm and maintaining backbone RMSD stability, whereas astragalin retains pocket residence with transient re-orientation. Conclusions: Hyperin emerges as a low-toxicity, mutation-agnostic scaffold that rigidifies inactive KRAS. Deglycosylation, nano-encapsulation, or soft fluorination could reconcile permeability with durable target engagement, advancing Z. lotus phenolics toward broad-spectrum KRAS therapeutics. Full article

Dodders (Cuscuta spp.) are prominent parasitic plants widely known and exploited in traditional medicine. They are rich in polyphenolics, which determine their strong antioxidant potential. However, comparatively few of the nearly 200 known species have been characterized for their medicinal potential. In the present study, we aimed to explore the antioxidant potential of four of the most widely distributed Cuscuta species in Bulgaria—C. campestris, C. monogyna, C. epithymum, and C. europaea. They differed significantly in polyphenolic content and accordingly differed in their antioxidant properties, although this correlation is not always straightforward, as shown in C. europaeae. Furthermore, we evaluated the host plant species’ influence on the polyphenolic content, antioxidant properties, and flavonoid profile of C. campestris, finding a significant enhancement when the parasite was grown on aromatic plants—rosemary and thyme—compared to a model host—Arabidopsis thaliana. Seven major flavonoids and phenolic acids—chlorogenic acid, kaempferol-3,7-O-diglucoside, quercetin-3-O-galactoside, kaempferol-3-O-galactoside, quercetin-3-O-glucoside, astragalin, and isorhamnetin-7-glucoside—were annotated after HPLC-MS analysis and found to be affected by the host species. In conclusion, it was found that extracts from different Cuscuta species differ in their antioxidant potential, which the host plants might further modify. Full article

Background: Varicose veins and chronic venous insufficiency are chronic venous disorders involving abnormalities in the venous system. Inflammation, an increase in proteolytic enzymes, and free radicals are important factors that play a role in the varicose vein pathology. Methods: In this study, the antioxidant properties and inhibitor activities of 17 plant extracts used to treat varicose veins in traditional medicine were evaluated against varicose veins-related enzymes (hyaluronidase, elastase, collagenase, lipooxygenase, prolylendopeptidase, and xanthine oxidase). The most effective compounds responsible for the activity of the Helichrysum plicatum subsp. plicatum extract were isolated by open column chromatography techniques. The active compounds were determined to be naringenin, apigenin, and luteolin by spectroscopic methods. In the activity-guided isolation study, the xanthine oxidase enzyme inhibition method was used. Results: The fractions containing naringenin and apigenin (IC₅₀ = 0.269 ± 0.009 µg/mL) and apigenin and luteolin (IC₅₀ = 0.285 ± 0.019 µg/mL) compounds showed synergistic and strong effects against xanthine oxidase and were found to be as active as the positive control allopurinol (IC₅₀ = 0.250 ± 0.006 µg/mL). In the LC-MS/MS analysis of the Helichrysum plicatum extract, quinic acid (22.649 mg compound/g extract), chlorogenic acid (14.573 mg/g extract), isoquercitrin (14.371 mg/g extract), cosmosin (9.885 mg/g extract), and astragalin (11.506 mg/g extract) were detected as the major components. Naringenin, apigenin, and luteolin were detected at concentrations of 1.457, 2.518, and 1.368 mg/g in the extract, respectively. Conclusions: In conclusion, it is predicted that the combination of naringenin, apigenin, and luteolin has a promising use as a conservative treatment option for diseases associated with varicose veins due to their synergistic effects with each other. Full article

Background/Objectives: Bacterial contamination leads to foodborne illnesses, and new antibiotics are required to combat these pathogens. Interest has increased in medicinal plants as targets for new antibiotics. Methods: This study evaluated the antibacterial activity of leaf extracts from Terminalia citrina (Gaertn.) Roxb. ex Fleming against four bacterial pathogens (including a methicillin-resistant Staphylococcus aureus (MRSA) strain) using disc diffusion and liquid microdilution assays. The phytochemical composition of the extracts were determined using ultra-high-performance liquid chromatography–mass spectrometry (UPLC-MS). Results: Both the aqueous and methanol extracts demonstrated noteworthy antibacterial activity against Bacillus cereus (MICs of 468.8 µg/mL and 562.5 µg/mL, respectively). Additionally, the extracts were effective against MRSA (MICs = 625 µg/mL). Strong antibacterial effects were also observed against S. aureus, with MICs of 625 µg/mL (aqueous extract) and 833.3 µg/mL (methanol extract). Twelve combinations of extracts and conventional antibiotics were synergistic against B. cereus and S. flexneri. UPLC-MS analysis revealed two flavonoids, orientin 2″-O-gallate and astragalin, exclusive to the aqueous extract, whilst pinocembrin and gallic acid were only detected in the methanol extract. Both extracts contained vitexin 2″-O-p-coumarate, ellagic acid, orientin, rutin, chebulic acid, terminalin, and quercetin-3β-D-glucoside. Both extracts were determined to be nontoxic. Conclusions: The abundance and diversity of polyphenols in the extracts may contribute to their strong antibacterial properties. Further research is required to investigate the antibacterial effects of the individual extract compounds, including their effects when combined with conventional antibiotics, and the potential mechanisms of action against foodborne pathogens. Full article