Search Results (912)

Procyanidins are oligomeric flavonoids with several bioactive properties. Their antidiabetic potential is related to their capacity to inhibit enzymes responsible for the absorption of dietary carbohydrates, such as pancreatic α-amylase. Procyanidins possess great structural diversity, including types of monomers and interflavanic bonds (A- or B-), and the degree of polymerization. However, there is a lack of evidence that systematically analyzes the effect of these structural features on their α-amylase inhibitory activity. In this paper, the activity of a mammalian pancreatic α-amylase was assessed using two different substrates, and the inhibitory activity of five commercially available procyanidins and three monomeric flavonoids was compared. The enzyme-binding sites of the eight compounds were predicted by in silico analysis to help explain the different enzyme-inhibitory activities. The inhibitory activity of procyanidins and monomeric flavonoids depended on the substrate used. A-type dimers presented the best activity against a polymeric substrate, while a B-type dimer was the best inhibitor for an oligomeric substrate. The predicted binding site for dimers and monomers was close to the active site. For the B-type trimer, the binding site was on the back side (approximately 180°) of the catalytic triad. In silico predictions suggested that dimeric procyanidins, especially A-type, could better enter the active site cavity, which could explain their superior inhibitory activity. We may conclude that inhibition of pancreatic α-amylase by procyanidins is mainly related to the type of interflavanic bond and the degree of polymerization. Dimers could be the most effective procyanidins to mildly inhibit this enzyme and present antidiabetic potential. Full article

Background/Objectives: Although several studies have been reported on the modulation of Cytochrome P450 by resveratrol, inconsistencies in the results obtained require further investigation. Here, we report the results of in vivo and in vitro experiments investigating the effect of resveratrol on CYP1A2, which participates in the biotransformation of several drugs used for the treatment of human malignancies. Methods: Male Wistar rats were exposed to resveratrol through diet (1%) for 30 days, and the hepatic CYP1A2 activity and protein concentration were assayed at the end of the treatment. Additionally, the capacity of the phytochemical to interfere with the induction of CYP1A2 by benzo[a]pyrene (50 mg/kg body weight) was also studied. The inhibition of CYP1A2 activity in rat liver microsomal and recombinant human enzymes by resveratrol, as well as its inhibitory kinetics and type of inhibition, were compared. Results: No significant increase in the protein concentration of hepatic CYP1A2 was found in resveratrol-treated rats, but it induces CYP1A2 activity and enhances the induction effect of benzo[a]pyrene. In silico and in vitro experiments demonstrated that resveratrol binds to the active site of human CYP1A2 through hydrophobic interactions with PHE125, PHE226, PHE260, and ALA317, and hydrogen bonds with SER122 and ASP313. It inhibits human recombinant CYP1A2 activity as well as that in rat liver microsomes, with IC₅₀ values of 46 µM and 485 µM, respectively. Resveratrol showed a mixed type of inhibition of recombinant human protein and a competitive inhibition of rat liver microsomal CYP1A. Conclusions: We can conclude that resveratrol is an in vitro inhibitor of CYP1A2, but it increases the benzo[a]pyrene CYP induction effect in vivo. Full article

Objectives: Bisphenol A (BPA), a prototypical environmental endocrine-disrupting chemical (EDC), is ubiquitously present in environmental matrices and biological fluids. Dietary ingestion and inhalation exposure to BPA can induce testicular oxidative stress and apoptosis. This study aimed to investigate the protective effects and underlying mechanisms of Pfaffia glomerata (Pg), a perennial herb of the Amaranthaceae family, against BPA-induced reproductive system injury. Methods: Potential targets and molecular mechanisms were predicted through network pharmacology. Physiological indicators, histopathological changes, serum biochemical parameters, and Western blot analysis were used to systematically evaluate the ameliorative effects of Pg and elucidate its mechanisms. Results: Our network pharmacology analysis identified core targets of Pg in attenuating reproductive system injury, including PTPN11, PIK3CA, JAK2, PIK3R1, PDGFRB, and others. GO enrichment and KEGG pathway analysis indicated that these key targets primarily regulate steroid metabolism, enhance antioxidant capacity, and modulate signaling pathways such as PI3K-AKT, Fc epsilon RI, and cAMP. In vivo studies demonstrated that all Pg dose groups showed significant improvement in BPA-induced histopathological injury to testicular tissues. BPA exposure increased serum levels of follicle-stimulating hormone (FSH) while decreasing testosterone (T), estradiol (E2), and progesterone (PROG) levels. Furthermore, BPA elevated serum levels of the testicular marker enzymes acid phosphatase (ACP) and lactate dehydrogenase (LDH) but reduced alkaline phosphatase (ALP) levels; all these effects were significantly reversed with Pg treatment. Western blot results showed that compared with the model group, high-dose Pg significantly upregulated the expression of phosphorylated AKT (p-AKT), phosphorylated PI3K (p-PI3K), and Bcl-2, while downregulating Cleaved Caspase-3 and Bax. Conclusions: Our findings indicate that Pg may attenuate BPA-induced reproductive system injury by activating the PI3K/AKT signaling pathway, upregulating the anti-apoptotic protein Bcl-2, and inhibiting the activation of the apoptotic effector Caspase-3. The study provides a new theoretical basis for the development of novel natural drugs or health products. Full article

Ten phyllospheric yeast strains were studied for their potential as biocontrol agents against fruit spoilage mould. The efficacy of these yeasts against Botrytis cinerea and Fusarium fujikuroi was assessed using dual-culture, mouth-to-mouth, radial growth inhibition and post-harvest fruit assays. Additionally, their capacity for producing hydrolytic enzymes was examined. Results from the ten yeasts revealed dual culture antagonism ranging from 41% to 63% against B. cinerea and 23% to 48% against F. fujikuroi, along with radial inhibition ranging from 70% to 100% and 47% to 100%, respectively. Additionally, in vitro inhibition through the production of volatile organic compounds (VOCs) varied from 2% to 46% against B. cinerea and 6% to 64% against F. fujikuroi. Overall, Aureobasidium melanogenum J7, Suhomyces pyralidae Y1117, Dekkera anomala V38, and Rhodotorula diarenensis J43 emerged as the best-performing biocontrol yeasts. Volatile organic compounds produced by the four yeasts were also identified and included in fruit bioassays using pears and tomatoes. Various VOCs, including 1-butanol, 3-methylbutanol, and butyric acid, were linked to the antagonistic properties of the selected yeasts. Lastly, the four chosen yeast strains significantly mitigated post-harvest spoilage caused by B. cinerea and F. fujikuroi in pear and tomato fruits, with D. anomala V38 exhibiting the greatest inhibitory activity. These findings underscore a potential sustainable and efficient approach to reducing mould-induced post-harvest spoilage while reducing reliance on synthetic fungicides. Full article

Background/Objective: Cellular senescence is increasingly recognized as a key mechanism underlying sarcopenia, an age-related muscle disorder with no effective therapeutic. 6,4′-Dihydroxy-7-methoxyflavanone (DMF), a flavonoid isolated from Dalbergia odorifera T. Chen, has shown anti-senescence potential. This study aimed to investigate the protective effects of DMF against myoblasts senescence and elucidate the underlying molecular mechanisms. Method: A cellular model of senescence was established in C2C12 myoblasts using D-galactose (D-gal). The effects of DMF pretreatment were evaluated by assessing senescence phenotypes, myogenic differentiation, and mitochondrial function. The role of Sirtuin3 (SIRT3) was confirmed using siRNA-mediated knockdown. Results: DMF Pre-treatment effectively attenuated D-gal-induced senescence, as indicated by restored proliferation, reduced senescence-associated β-galactosidase activity, decreased DNA damage, and the downregulation of p53, p21^Cip1/WAF1 and p16^INK4a. Furthermore, DMF rescued myogenic differentiation capacity, enhancing the expression of Myoblast determination protein 1, Myogenin, Myosin heavy chain and Muscle-specific regulatory factor 4, and promoting myotube formation. Mechanistically, DMF was identified as a SIRT3 activator. It enhanced SIRT3 expression and activity, leading to the deacetylation and activation of the mitochondrial antioxidant enzyme superoxide dismutase 2. This consequently reduced mitochondrial reactive oxygen species, improved mitochondrial membrane potential and ATP production, and suppressed the NF-κB pathway by inhibiting IκBα phosphorylation and p65 acetylation/nuclear translocation. Crucially, all the beneficial effects of DMF—including oxidative stress reduction, mitochondrial functional recovery, anti-inflammatory action, and ultimately, the attenuation of senescence and improvement of myogenesis—were abolished upon SIRT3 knockdown. Conclusions: Our findings demonstrate that DMF alleviates myoblasts senescence and promotes myogenic differentiation by activating the SIRT3-SOD2 pathway, thereby reducing oxidative stress and NF-κB-driven inflammation responses. DMF emerges as a promising therapeutic candidate for sarcopenia. Full article

Background/Objectives: In recent years, silver complexes have shown strong antibacterial, antifungal, and antitumor activity with high selectivity toward cancer cells. Their cytotoxic effects are mainly linked to apoptosis induction, DNA damage, and enzyme inhibition, while the antitumor activity of silver(I) complexes with S-alkyl thiosalicylic acid derivatives remains unexplored. Methods: Silver(I) complexes with S-alkyl derivatives of thiosalicylic acid (C1–C5) were obtained through the direct reaction of silver(I) nitrate, the corresponding ligand of thiosalicylic acid, and a sodium hydroxide solution. The interactions between the complexes and CT-DNA/BSA were studied using UV-Vis, fluorescence spectroscopy, and molecular docking studies. The cytotoxic capacity of the newly synthesized complexes was assessed by an MTT assay. Results: Complexes C1–C5 exhibited strong cytotoxicity against murine and human breast (4T1, MDA-MB-468), colon (CT26, HCT116), and lung (LLC1, A549) cancer cell lines. The C3 complex significantly diminished tumor progression in an orthotropic mammary carcinoma model while demonstrating good systemic tolerance. Conclusions: The tested complex C3 triggered apoptosis in 4T1 cells by altering the delicate balance between pro- and anti-apoptotic Bcl-2 family members, increasing reactive oxygen species (ROS) levels, and reducing mitochondrial membrane depolarization. Moreover, the C3 arrested the 4T1 cell cycle in G0/G1 phase, decreasing the expression of cyclin D3 and increasing the expression of p16, p21, and p27. Full article

Coffee is among the most consumed beverages worldwide and is recognized for its bioactive compounds, which exert diverse physiological effects. This study evaluated the impact of roasting degree on the in vitro antioxidant activity and digestive enzyme inhibition of brews from four Mexican regions, as well as their in vivo effects on carbohydrate and lipid absorption. Antioxidant capacity was assessed through radical scavenging and lipid peroxidation inhibition, while inhibition of lipase, α-amylase, and α-glucosidase was also determined. Oral starch (OSTT) and lipid (OLTT) tolerance tests were conducted in healthy Wistar rats. Antioxidant activity was strongly influenced by region and roasting degree. All coffee samples exhibited radical scavenging activity and lipid peroxidation inhibition. With respect to enzyme inhibition, all coffees showed ~67–70% inhibition of lipase activity. For amylase, unroasted coffee from Oaxaca displayed the highest inhibition (34%, p < 0.001). For glucosidase, unroasted samples showed low inhibition (~6–19%), which increased substantially at the medium roast degree (~55% across all samples) but decreased again at the high roast degree (~27%). In OSTT, serum glucose levels were reduced after 120 min by ~20%, 21%, and 18% in rats treated with unroasted, medium-roast, and high-roast coffee, respectively, compared with the negative control. In OLTT, serum triglycerides decreased by ~26% (Chiapas), ~58% (Colima), ~32% (Oaxaca), and ~54% (Hidalgo). Crop region and roasting degree influence the phytochemical profile and bioactivity of Mexican coffee. Although unroasted coffees had the highest concentration of bioactive compounds, roasting enhanced specific bioactivities, particularly enzyme inhibition and lipid-lowering effects in vivo. Full article

Drought stress induced by climate change is a major limiting factor for crop growth. Selenium (Se) is recognized as an important exogenous regulator that can mitigate drought and other abiotic stresses, but the effects of Se application at different growth stages remain unclear. In this study, greenhouse-grown tomato plants were subjected to four Se treatments (T1: control; T2: Se at seedling stage; T3: Se at flowering stage; T4: Se at both stages) combined with three irrigation regimes (W1: 50–55%, W2: 65–70%, W3: 80–85% of field capacity). The impacts of Se timing on antioxidant enzymes, osmotic regulators, and growth parameters were evaluated. Drought stress induced oxidative damage, reduced photosynthesis, and inhibited biomass accumulation, while proline content increased with drought severity. Se application showed clear growth-stage specificity: under mild stress, Se at the flowering stage most effectively enhanced antioxidant activity, regulated proline metabolism, improved photosynthetic performance, and promoted growth. Dual-stage application did not provide additional benefits. These findings indicate that applying Se during the flowering and fruiting stage is optimal for alleviating drought-induced growth inhibition in tomato. The results contribute to understanding Se-mediated drought tolerance and may support the development of stage-specific Se fertilizer management strategies. Full article

Reactive oxygen species (ROS) are formed by the incomplete reduction of oxygen and play a crucial role in both physiological function and pathological process, being controlled by enzymatic and non-enzymatic antioxidant systems. However, excessive ROS production can exceed the body’s antioxidant capacity, resulting in oxidative stress and causing cell death and oxidation of important biomolecules. In this context, the inhibition and/or modulation of ROS has been shown to be effective in reducing pain, oxidative stress, and inflammation. Among ROS, superoxide anion (O₂^•−) is the first free radical to be formed through the mitochondrial electron transport chain (ETC) or by specific enzymes systems, such as the nicotinamide adenine dinucleotide phosphate (NADPH) oxidase (NOX) complex. O₂^•− plays a significant role in the development and maintenance of pain associated with inflammatory conditions through direct or indirect activation of primary nociceptive neurons and, consequently, peripheral and central sensitization. Experimentally, potassium superoxide (KO₂, a O₂^●− donor) is used to initiate O₂^●− mediated inflammatory and nociceptive responses, making it important for studying the mechanisms associated with ROS-induced pain and evaluating potential therapeutic molecules. This review addresses the production and regulation of O₂^•−, highlighting its biosynthesis, redox control, and its physiological and pathological roles in the development of inflammatory pain, as well as the pharmacological therapies under development aimed at its generation and/or action. Full article

Polysaccharides from edible mushrooms are increasingly recognized as bioactive compounds with health-promoting properties. In this study, a polysaccharide-rich fraction Mp-CPS was isolated from fruiting bodies of Macrolepiota procera using ultrasound-assisted extraction. The chemical composition of crude polysaccharides from the parasol mushroom was evaluated using spectrophotometric and electrophoretic methods. Chemical analysis revealed that Mp-CPS is mainly composed of glucose- and galactose-based heteropolysaccharides, with β-glucans as the predominant glucan type. The biological potential of Mp-CPS was evaluated in light of its antioxidant, anti-inflammatory, and anticancer activities. Antioxidant assays (TEAC, ORAC) demonstrated significant radical-scavenging capacity, with higher activity observed in the ORAC test. As revealed by biochemical examination, Mp-CPS also inhibited key pro-inflammatory enzymes: COX-1, COX-2, and LOX. At the same time, in vitro research (MTT and LDH assays) has shown the great chemopreventive abilities of Mp-CPS against human colon cancer cells, which intensified with the degree of cell malignancy. Overall, these results highlight M. procera as a sustainable and valuable source of biologically active polysaccharides with antioxidant, anti-inflammatory, and anticancer potential. The findings support further exploration of Mp-CPS for applications in functional foods and nutraceuticals. Full article

Salt stress is a significant environmental factor that inhibits maize growth and development, severely affecting yield formation. Interestingly, nanomaterials, particularly ZnONPs, can enhance resistance to various stresses and support healthy crop growth. However, the effects of ZnONPs on maize under salt stress remain unclear. This study investigates the effect of foliar and seed exposure to zinc oxide nanoparticles (ZnONPs) on reducing NaCl-induced salt stress in two maize inbred lines (NKY298-1 and NKY211). Over a period of seven days, under 120 mM NaCl, we measured growth, reactive oxygen species (ROS), malondialdehyde (MDA), membrane stability index (MSI), water status (relative water content, RWC), photosynthetic pigments and parameters, selected photosynthetic enzymes, and antioxidant enzyme activities. Then, we propose four composite indices, including stress improvement index (SII), alleviation capacity index (ACI), comprehensive improvement effects (CIE), and comprehensive alleviation capacity (CAC), to rank the effectiveness of ZnONP doses. The findings suggested that 50–100 μM ZnONPs significantly mitigate salt damage, with optimal doses varying by genotype (50 μM for NKY211 and 100 μM for NKY298-1). Notably, the study’s originality lies in its side-by-side composite scoring across 26 traits in two maize genotypes’ seedlings. In conclusion, the findings will provide a new idea for research on the molecular mechanism by which exogenous ZnONPs application improves the salt tolerance of maize seedlings. Full article

The spatiotemporal regulatory mechanism underlying silicon (Si)-mediated cadmium (Cd) detoxification in rice (Oryza sativa L.) was investigated using non-invasive micro-test technology (NMT), combined with physiological and biochemical analyses. The results revealed the following: (1) Si significantly inhibited Cd²⁺ influx into rice roots, with the most pronounced reductions in ion flux observed under moderate Cd stress (Cd50, 50 μmol·L⁻¹), reaching 35.57% at 7 days and 42.30% at 14 days. Cd accumulation in roots decreased by 34.03%, more substantially than the 28.27% reduction observed in leaves. (2) Si application enhanced photosynthetic performance, as evidenced by a 14.21% increase in net photosynthetic rate (Pn), a 32.14% increase in stomatal conductance (Gs), and a marked restoration of Rubisco activity. (3) Si mitigated oxidative damage, with malondialdehyde (MDA) and hydrogen peroxide (H₂O₂) levels reduced by 11.29–21.88%, through the upregulation of antioxidant enzyme activities (SOD, APX, CAT increased by 15.34–38.33%) and glutathione metabolism (GST activity and GSH content increased by 60.78% and 51.35%, respectively). (4) The mitigation effects of Si were found to be spatiotemporally specific, with stronger responses under Cd50 than Cd100 (100 μmol·L⁻¹), at 7 days (d) compared to 14 d, and in roots relative to leaves. Our study reveals a coordinated mechanism by which Si modulates Cd uptake, enhances photosynthetic capacity, and strengthens antioxidant defenses to alleviate Cd toxicity in rice. These findings provide a scientific basis for the application of Si in mitigating heavy metal stress in agricultural systems. Full article

In this study, the cosmeceutical potential of a 70% ethanol extract of Rosa lucieae was investigated as a multifunctional bioactive ingredient. The extract was systematically evaluated for its antioxidant, anti-melanogenic, and anti-aging properties, and was comprehensively phytochemically profiled using ultra-high-performance liquid chromatography–quadrupole time-of-flight mass spectrometry. The analysis tentatively identified 21 metabolites, including phenolic acids (gallic acid, ellagic acid, and corilagin), flavonoids (catechin, rutin, quercetin, hyperoside, and quercitrin), and glycosidic derivatives (e.g., phlorizin), several of which are well-documented for their skin-protective effects. Quantitative measurements confirmed high polyphenol and flavonoid contents, correlating with strong radical-scavenging and reducing capacities in α-diphenyl-β-picrylhydrazyl, 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid, as well as ferric ion reducing antioxidant power assays. Moreover, the extract inhibited tyrosinase activity and 3,4-dihydroxyphenylalanine oxidation, thereby suppressing melanin biosynthesis. In addition, marked inhibitory effects against collagenase, elastase, and hyaluronidase were observed; these enzymes are critically involved in extracellular matrix degradation and skin aging. Taken together, these results indicate that the biological activities of R. lucieae are supported by a diverse polyphenol- and flavonoid-rich chemical profile, highlighting the potential of this plant as a natural multifunctional ingredient for cosmeceutical, nutraceutical, functional food, and preventive healthcare applications. Full article

The low fertility of tropical Oxisols challenges sustainable agriculture. While biochar-based granular fertilizers (BBGFs) offer a solution, the influence of different organic binders is unclear. This study investigated how BBGFs formulated with bio-oil (BO), pyroligneous extract (PE), and cassava wastewater (CW) impact soil enzyme activities and nutrient dynamics over time. Eucalyptus biochar (B) and natural phosphate (NP) were granulated with three binders at four doses. These treatments, plus controls (unfertilized soil, NP, B with NP, and B alone), were incubated in an Oxisol, assessing soil samples after 10 and 40 days of incubation. All BBGFs significantly enhanced β-glucosidase, acid phosphatase, and arylsulfatase activities over controls, with increases exceeding 8%. While the BBGFs-BO formulation sustained the highest enzymatic activity, BBGFs-PE at 125% maximized acid phosphatase at 10 days, with a subsequent decline, and inhibited arylsulfatase at the 150% dose. BBGFs-CW was most effective for increasing P availability (up to 24.0 mg kg⁻¹). BBGFs-BO and BBGFs-PE also enhanced soil organic carbon and cation exchange capacity by up to 430% and 163%, respectively. The BBGFs-BO at 150% dose is the most effective and stable formulation to enhance nutrient cycling and soil health, offering a viable pathway to convert agricultural residues into high-value fertilizers. Full article

Infusions of the leaves of Ribes magellanicum (Grossulariaceae) are used as a digestive in southernmost South America. This work aimed to assess the composition and activity of infusions and MeOH:H₂O 7:3 extracts of R. magellanicum leaves on enzymes related to metabolic syndrome (α-glucosidase, α-amylase, and pancreatic lipase), as well as their antioxidant capacity. Samples from a longitudinal gradient from central southern Chile to the islands in the Beagle Channel were investigated. Lyophilized infusions and extracts were used for all determinations, including inhibition of the selected enzymes, total phenolic (TP), total flavonoid (TF), total procyanidins (TPC), and antioxidant capacity (DPPH, FRAP, TEAC, and ORAC). The composition of the samples was assessed by HPLC-DAD. Some 99 compounds were tentatively identified by HPLC-MSⁿ. The main phenolics were quantified using calibration curves with reference compounds. Relevant differences exist in the ratio of constituents in infusions compared to hydroalcoholic extracts. The samples were inactive towards α-amylase and pancreatic lipase at 100 and 50 µg/mL, respectively. Assay-guided isolation of α-glucosidase inhibitors led to fractions with high activity (IC₅₀: 0.02–0.05 µg/mL). The strong inhibition of α-glucosidase and antioxidant capacity of the infusion and extracts of R. magellanicum leaves support its traditional use in southern Patagonia. Full article