Given the increasing focus on natural interventions for healthy aging, this research evaluates the longevity-promoting potential of egg-derived peptides (EPs) extracted from American shad (Alosa sapidissima). Using Caenorhabditis elegans as the experimental model, researchers found that 0.15 mg/mL EP supplementation extended lifespan by a remarkable 33.33%. EP also significantly enhanced healthspan, improving physiological metrics such as head thrashing, body bending, and pharyngeal pumping by 24.37%, 22.33%, and 28.81%, respectively. Furthermore, EP reduced aging biomarkers-including lipofuscin and reactive oxygen species (ROS)-by up to 40.34%, while boosting overall antioxidant capacity (SOD increased by 53%, MDA decreased by 30.76%). Transcriptomic analysis identified 2196 differentially expressed genes (DEGs) out of 23 057 total identified genes, providing deep insights into the mechanisms underlying EP-mediated longevity. Crucially, EP upregulated genes responsible for unsaturated fatty acid biosynthesis (fat-7 and elo-4) to optimize cell membrane fluidity. Conversely, it downregulated genes linked to fatty acid β-oxidation (acs-2, acox-1.5, ech-9, hacd-1) and endogenous stress responses (sod-3, hsp-16.1, hsf-1). Validated via qRT-PCR, these shifts indicate that EP extends lifespan by fundamentally remodeling lipid metabolism and maintaining redox homeostasis. Ultimately, these findings highlight EP as a highly promising functional food ingredient for promoting healthy aging.
Natural products rich in phenolic compounds are increasingly investigated as multifunctional agents against oxidative stress and enzyme-related disorders. This study characterized the phytochemical composition and evaluated the antioxidant and enzyme inhibitory activities of methanol and aqueous extracts of Stachys aleurites. Total phenolic and flavonoid contents were determined spectrophotometrically, while selected phenolics were quantified by LC-ESI-MS/MS. Antioxidant and enzyme inhibitory properties were assessed using complementary in vitro assays. The methanol extract contained higher levels of total phenolics (48.86 mg GAE/g) and flavonoids (65.36 mg RE/g) than the aqueous extract. Verbascoside and chlorogenic acid were the predominant compounds in the methanol extract, whereas p-coumaric acid was relatively more abundant in the aqueous extract. The methanol extract exhibited stronger antioxidant activity in most assays and showed greater inhibition of AChE, tyrosinase, α-amylase, and α-glucosidase. In contrast, the aqueous extract displayed slightly higher metal-chelating activity and stronger BChE inhibition. These findings demonstrate solvent-dependent variations in phytochemical composition and bioactivity, highlighting the importance of extraction solvent selection and supporting further studies on the bioactive constituents of S. aleurites.
Two γ-lactone derivatives, alterlactones A-B (1-2), along with one known analogue 3, were isolated from the mangrove endophytic fungus Alternaria sp. HN-17. Their structures were elucidated using comprehensive spectroscopic methods, including 1D and 2D NMR, HRESIMS, and electronic circular dichroism (ECD) calculations. Compounds 1 and 2 showed significant anti-inflammatory activity with IC50 values of 10.2 and 13.5 µM, respectively.
Five Strobilanthes species indigenous to the Kumaun Himalayan region of Uttarakhand, India, have been historically employed in traditional medicine to treat bacterial infections, inflammatory conditions, and respiratory ailments, but remain largely unexplored for aquaculture disease management applications. Dichloromethane extracts of S. glutinosa (SGDE), S. pentastemonoides (SPDE), S. angustifrons (SADE), S. attenuata (SATDE) and S. tomentosa (STDE) were comprehensively analysed by GC-MS for phytochemical profiling, with antioxidant activity quantified using DPPH radical scavenging and ferrozine-based metal chelating assays, and antibacterial efficacy evaluated against Aeromonas salmonicida and Edwardsiella tarda using disc diffusion methodology. Pearson correlation analysis, molecular docking, and ADMET computational modelling were performed to elucidate structure-activity relationships and pharmacokinetic properties. GC-MS analysis identified 42-59 phytochemical constituents per species, with sterols and triterpenes constituting the predominant class. STDE demonstrated superior DPPH radical scavenging activity, while SATDE exhibited optimal metal chelating potential. SGDE and STDE displayed the good antibacterial activities against both pathogens. Pearson correlation analysis identified n-tritriacontane and sclareol associated with antimicrobial activity, while molecular docking revealed superior binding affinities for β-amirone to DNA topoisomerase I and β-amyrin. ADMET assessment identified sclareol, stigmasterol, and 24-epicampesterol as optimal candidates with favorable.
Antimicrobial resistance (AMR) has severely compromised the clinical utility of classical sulfonamide antibiotics, primarily owing to the emergence of resistance-associated dihydropteroate synthase variants. In this study, sixteen N-(1H-indazolyl) aryl sulfonamide hybrids were evaluated as potential DHPS inhibitors against Escherichia coli and Staphylococcus aureus using disk diffusion, broth microdilution (MIC80), and minimum bactericidal concentration (MBC) assays. Active compounds were characterized by in silico ADME and toxicity profiling, with molecular docking performed against wild-type DHPS and the sulfonamide-resistant Sul1 variant. Antibacterial activity was species-dependent: compound 4 showed the strongest activity against E. coli (MIC = 32 µg/mL), while compounds 11 and 16 were most potent against S. aureus (MIC = 32 µg/mL), outperforming sulfathiazole and sulfisoxazole. All hybrids showed superior docking affinities to sulfamethoxazole (SMX), with compound 11 showing the highest affinity for wild-type DHPS (-7.79 kcal/mol); compound 4 retained favorable binding against Sul1 (-6.83 kcal/mol), suggesting potential resistance resilience. Structure-activity analysis showed antibacterial efficacy is governed by aryl sulfonyl electronic effects, steric balance at the C7 indazole position, and physicochemical properties affecting Gram-negative membrane permeability. These findings support indazole-sulfonamide hybrids as promising scaffolds that may retain predicted binding complementarity toward the Sul1-resistant DHPS variant, warranting validation against resistant isolates and purified DHPS enzymes.
Longgu (fossilized bone), a mineral medicine in traditional Chinese medicine, has been used for centuries to treat symptoms resembling modern anxiety and insomnia. This review evaluates the hypothesis that Longgu's therapeutic effects arise from a synergistic network of its constituent metal ions. We synthesized evidence from chemical analyses, pharmacological studies of Ca, Mg, Zn, Fe, Cu, and Mn, and clinical trials of Longgu-containing formulations. The metal ions form an integrated network exhibiting three emergent properties. First, ionostatic balance is achieved through Ca/Mg-mediated regulation of neuronal excitability. Second, cross-pathway synergy occurs where zinc concurrently modulates neurotransmission and promotes neuroplasticity via BDNF. Third, systemic integration involves zinc and manganese co-regulating the gut-brain axis. Clinical studies demonstrate that Longgu-containing formulations improve outcomes in depression, anxiety, and insomnia, particularly for comorbid conditions, and show synergistic effects when combined with conventional antidepressants. This network pharmacology framework repositions Longgu as a model for developing multi-target therapeutics, offering a strategy to overcome limitations of single-target psychiatric drugs.
The phenolic composition of roots and leaves of Lygeum spartum L., a Mediterranean Poaceae species, was analyzed by HPLC-DAD, revealing an organ-specific distribution of phenolic compounds, with ferulic acid identified as the predominant phenolic compound in the methanolic leaf extract (4.07 mg/g) and higher levels of flavonoids and phenolic acids in leaves than in roots. Antioxidant activity was evaluated using DPPH, ABTS+, and CUPRAC assays, while enzyme inhibitory activity was assessed against acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and tyrosinase using L-DOPA as the substrate. Methanolic extracts, particularly those from leaves, exhibited the highest antioxidant activity among the tested extracts (IC50 = 281.48 µg/mL for DPPH; 105.72 µg/mL for ABTS+; A0.5 = 182.36 µg/mL for CUPRAC), whereas petroleum ether extracts were largely inactive. Enzyme inhibitory activity was generally weak, with all extracts exhibiting little or no inhibition of AChE and BChE, while the methanolic leaf extract showed weak tyrosinase inhibitory activity (IC50 = 310.69 µg/mL). To the best of our knowledge, this is the first study reporting the cholinesterase and tyrosinase inhibitory activities of L. spartum L. These results indicate that L. spartum is a source of phenolic compounds exhibiting moderate antioxidant activity, whereas its enzyme inhibitory effects are limited.
A ZnO/CuO@amoxicillin nanocomposite was synthesized via a sol-gel route and characterized as a biphasic wurtzite ZnO-monoclinic CuO system with crystallite sizes of about 10-12 nm and an optical band gap of 3.30-3.36 eV, indicating defect-rich interfaces favorable for redox activity. In antidiabetic assays, the nanocomposite showed strong inhibitory effects on alpha-amylase (IC50 = 21.57 ± 1.68 mg/mL) and alpha-glucosidase (IC50 = 13.95 ± 0.76 mg/mL), with activities comparable to acarbose, while anti-inflammatory tests yielded low IC50 values of 0.22 ± 0.03 mg/mL for egg albumin denaturation and 0.34 ± 0.07 mg/mL for human serum albumin, approaching the performance of diclofenac. Antioxidant performance was outstanding, with total antioxidant capacity of 298.27 ± 4.70 mg ascorbic acid equivalents per gram and ferric reducing antioxidant power of 311.67 ± 2.53 mM Fe2 +/g, both higher than ascorbic acid, alongside efficient hydrogen peroxide scavenging (IC50 = 0.16 ± 0.04 mg/mL) and protection against H2O2/FeCl3-induced hemolysis at an IC50 of 0.007 ± 0.00 mg/mL; together with moderate but significant acetylcholinesterase inhibition (IC50 = 33.16 ± 3.02 mg/mL vs. 21.80 ± 2.74 mg/mL for donepezil), these results support ZnO/CuO@amoxicillin as a multifunctional nano-platform for managing oxidative stress, inflammation, and metabolic disorders.
Research on molecular systems capable of interacting with DNA through binding, modification, or cleavage remains important in medicinal chemistry. In this study, we report the design and synthesis of a new D-glucamine-based Schiff base containing a triazolyl silatrane probe (6) and its Fe(II) and Cu(II) complexes, followed by investigation of their interactions with calf thymus DNA (CT-DNA). The synthesized ligand and its metal complexes were characterized by elemental analysis, FT-IR, UV-vis spectroscopy, ESI-MS, and NMR spectroscopy (1H and 13C for the free ligand). DNA-binding properties were evaluated by UV-vis absorption spectroscopy, ethidium bromide (EtBr) displacement fluorescence assays, and molecular docking studies. The combined experimental and computational results indicate that ligand 6 interacts predominantly with CT-DNA through groove binding, whereas complexation with Fe(II) or Cu(II) enhances DNA-binding affinity and modulates the interaction toward a mixed groove-binding/intercalative mode. The higher binding constants, enhanced fluorescence quenching, and favorable docking interactions observed for the metal complexes support this metal-induced modulation of DNA-binding behavior. Overall, the findings demonstrate that metal complexation can tune both the strength and mode of DNA binding, highlighting a potential strategy for designing silatrane-based metal complexes with DNA-targeting applications.
Telmisartan is a benzimidazole derivative and a well-known drug to treat hypertension. This is an angiotensin II receptor blocker (ARB) which helps to relax blood vessels. Studies have shown that telmisartan is effective in reducing cardiovascular disease, with a safety and efficacy profile. This review paper provides an overall understanding of telmisartan as an antihypertensive drug. The goal is to highlight the synthetic methodology of telmisartan, from its first synthesis in 1993. This review also discusses its two mechanisms of action: the Renin-Angiotensin-Aldosterone System (RAAS) inhibitor and partial agonist activity at the Peroxisome Proliferator-activated receptor gamma (PPARγ) receptor. Effective repurposing of this drug for various diseases like chronic kidney illness, diabetes, fatty liver, and Alzheimer's has also been discussed.
This study presents the phytochemical and biological evaluation of the species Hedysarum yilmazunalii Kandemir, F. Yıldız & H.İ. Turkoğlu. Methanolic extracts from leaves, stems, and roots were characterized by LC-MS/MS, and their antioxidant, enzyme inhibitory, and antiproliferative activities were investigated. The analyses showed organ-specific differences in phenolic composition, with quinic acid as the major compound in leaves together with higher levels of flavonoid glycosides, including astragalin and isoquercitrin. Aerial extracts showed strong enzyme inhibitory activity. Leaf and stem extracts exhibited cholinesterase inhibition, with IC50 values of 5.82 and 6.42 µg/mL for AChE and 5.41 and 5.50 µg/mL for BChE, respectively. The leaf extract showed α-glucosidase inhibitory activity (4.10 µg/mL), comparable to acarbose, and antioxidant activity (DPPH: 6.46 µg/mL), together with the highest phenolic (145.43 mg GAE/g extract) and flavonoid contents (87.20 mg QE/g extract). Antiproliferative assays demonstrated growth inhibition of lung and breast cancer cell lines, with the lowest GI50 values of 1.00 µg/mL for H1650 and 2.34 µg/mL for MDA-MB-231 cells. LDH cytotoxicity remained low (2.25%-12.59%), indicating limited membrane damage in both cancer and normal cells. These findings identify H. yilmazunalii as a source of compounds with antioxidant, neuroprotective, antidiabetic, and anticancer potential.
The chemical composition of 50 individual trunk bark oil samples from plants of Pachylobus klaineanus (Pierre) Guillaumin. collected in eight Ivoirian localities was investigated by GC-FID (50 samples), GC/MS (30 samples), and 13C-NMR (23 samples). Eighty-three compounds were identified. Oil samples are dominated by monoterpenes. The main components were α-pinene (28.8%-76.2%), β-pinene (2.0%-46.3%), limonene (0.9%-13.8%), p-cymene (0%-19.2%), and myrcene (0%-17.9%). The 50 oil compositions were submitted to hierarchical clustering and principal components analyses, which allowed the distinction of two groups within the oil samples. Group II could be divided into two subgroups, IIa and IIb. Group I (23 samples) was characterized by the pre-eminence of α-pinene; subgroup IIa (19 samples) was dominated by α-pinene followed by β-pinene, while IIB (8 samples) is represented by α-pinene and β-pinene in association with monoterpene hydrocarbons (limonene and p-cymene). The trunk bark essential oil of this species was reported for the first time.
An investigation of the chemical constituents of Viburnum macrocephalum f. macrocephalum leaves (VMML) resulted in the purification of five previously unreported iridoids, viburetins D-H (1-5), along with one known analogue (6). Compounds 1-5 were identified by combined spectroscopic and spectrometric techniques, including 1D/2D NMR, HRESIMS, and ECD. Antioxidant assays revealed that compounds 2, 5, and 6 exhibited DPPH (IC50: 36.58-53.90 µM) and ABTS (IC50: 25.96-45.80 µM) free radical scavenging activity, whereas compound 1 was appreciably active in the ABTS assay (IC50 = 58.47 µM). Notably, compound 6 was the most potent antioxidant, showing greater activity than the positive control Trolox in both assays (DPPH: IC50 = 36.58 vs. 41.12 µM; ABTS: IC50 = 25.96 vs. 29.09 µM). These findings have enriched the chemical diversity of iridoids from VMML and provided preliminary evidence for their free radical scavenging activity.
The essential oil (EO) and phenolic composition of Helichrysum italicum (Roth) G. Don from natural populations in east Adriatic were analyzed using gas and liquid chromatography coupled with mass spectrometry. In EOs of the studied populations, 146 compounds were identified, representing, on average, 97.3% of the total oil composition. The essential oils were dominated by sesquiterpenes. γ-Curcumene was among the most abundant compounds in all samples. Twelve compounds were present in concentrations greater than 5% in at least one of the ten populations. In the extracts, 73 phenolic compounds were identified, belonging to four classes. Compound classes included phenolic acids, flavonoid glycosides, flavonoid aglycones, pyranones, and related compounds. Arzanol was the most prominent peak across all samples, and pyranones and related compounds were the most abundant. No correlations between EO and flavonoid aglycone composition and the studied environmental parameters were found, whereas phenolic acids and glycosides showed correlations with temperature and precipitation.
This work investigated the effects of Moringa oleifera seed lectin (WSMoL) on motor performance, neuroinflammation, and oxidative stress in a rotenone-induced model of Parkinson's disease (PD). Male mice were daily administered rotenone (3 mg/kg, i.p.) 1 h after being treated with WSMoL (1, 2, or 4 mg/kg, i.p.), levodopa (L-DOPA, 10 mg/kg), or vehicle for 10 days. To assess dopaminergic involvement, another group received the D1 receptor antagonist SCH-23390 co-administered with WSMoL (4 mg/kg). The healthy control group received vehicle only. Motor performance was evaluated using the rotarod, cylinder, and open field tests. Brain levels of monoamines and cytokines as well as redox status were measured. WSMoL prevented the rotenone-related deficits in motor performance, which was accompanied by non-depleted dopamine and serotonin levels. WSMoL also mitigated the increase of IL-6, IL-17A, IFN-γ, and TNF-α. In addition, it prevented oxidative stress by avoiding the exacerbation of superoxide production, lipid peroxidation, and NADPH oxidase activity, while maintaining catalase, superoxide dismutase (SOD), and reduced glutathione (GSH) levels. The data show that D1 receptor-mediated signaling contributes to WSMoL effects. In conclusion, WSMoL attenuates motor deficits and neuroinflammation in a PD model, which supports its potential as a neuroprotective agent and warrants further mechanistic and translational studies.
This study characterized the phytochemical composition of a methanolic bark extract of Cinnamomum verum and evaluated its antibacterial, bactericidal, biofilm-biomass-reducing, and preliminary antibiotic-potentiating effects against reference and multidrug-resistant bacterial strains. The extract was characterized by HPLC-MS; MIC and MBC values were determined by broth microdilution; biofilm biomass was assessed using the crystal-violet assay; and antibiotic-extract interactions were screened by disk diffusion. Molecular docking was used as a hypothesis-generating approach to investigate interactions between identified phytochemicals and GyrB, LasA, and PBP1a. Seventeen compounds were identified, with trans-cinnamaldehyde as the predominant quantified constituent, followed by quinic acid, rutin, and protocatechuic acid. The extract inhibited all tested bacteria, with MIC and MBC values of 0.625-5 and 2.5-20 mg/mL, respectively, and MBC/MIC ratios consistent with bactericidal activity. Imipenem-resistant Acinetobacter baumannii isolates were the most susceptible. The extract also reduced biofilm biomass in a concentration-dependent and strain-dependent manner. Disk-diffusion screening identified antibiotic- and isolate-dependent increases in inhibition zones, particularly for cefoxitin and fosfomycin against MRSA and for selected combinations against A. baumannii; however, some combinations were unchanged or produced smaller zones, and pharmacological synergy was not established. Docking prioritized quercetin, 1,3-di-O-caffeoylquinic acid, and quercetin-3-O-rhamnoside as candidates for subsequent target-based validation.
Aesculus hippocastanum L. is a well-established medicinal plant used for the treatment of venous disorders and inflammation. Despite its wide therapeutic application, systematic comparisons of the phytochemical profile of horse chestnut seed extracts prepared according to pharmacopeial extraction protocols remain scarce. Consequently, this study aimed to characterize and compare the metabolite profiles of hydroalcoholic and aqueous fermented seed extracts prepared according to official pharmacopeial procedures. Extracts were analyzed using high-performance liquid chromatography coupled to diode array and electrospray ion-trap mass spectrometric detection (HPLC-DAD-ESI-MSn) and gas chromatography-mass spectrometry (GC-MS). Additionally, a novel approach was developed for the semi-quantification of saponins by tensiometry, which was compared with the quantification of UV-active aescin derivatives by RP-HPLC-DAD. The HPLC-DAD-MSn analyses revealed different phytochemical compositions that include triterpene saponins, flavonoid glycosides, and indoleacetic acid-N-glycosides. GC-MS analyses mainly revealed the presence of fatty acids, monosaccharides, and lactic acid. The hydroalcoholic extract showed higher aescin contents by RP-HPLC-DAD compared to the aqueous fermented extract, indicating better recovery rates with this extraction procedure. These findings underline the importance of process parameters in pharmaceutical manufacturing and support the use of complementary analytical approaches for comprehensive quality evaluation of complex herbal extracts.
This work investigates the carboxymethylcellulose (CMC)-dates (Dt) hydrogel films (HFs) for the controlled delivery of hydrophobic drugs, using citric acid (CA) as a nontoxic cross-linking agent. The model drug Econazole (ECN) was loaded into HFs, and drug release was studied at pH 7.4. The HFs were evaluated for β-cyclodextrin (β-CD) content, carboxyl content, swelling ratio, drug loading, drug release, and in vivo anti-inflammatory activity. These films were characterized using ATR-FTIR, thermal gravimetric analysis (TGA), scanning electron microscopy coupled with energy-dispersive x-ray spectroscopy (SEM/EDX), and atomic force microscopy (AFM) for morphological measurements. Results revealed that the HFs with high carboxyl content exhibit maximum swelling and high drug loading. The incorporation of β-CD helped to retard the release of ECN from the HFs. Our findings indicate that HFs F3 and F4 with high Dt concentrations reduce the edematous response by 92% ± 5.07% and 89% ± 3.69%, respectively. Altogether, our findings show that CMC-Dt HFs are suitable for the delivery of non-soluble weak bases and have potential for wound-healing applications. The in vivo investigation demonstrated that the HFs exhibit significant anti-inflammatory characteristics.
The Malpighiaceae family comprises approximately 1,500 species distributed across tropical and subtropical regions and is recognized as a source of bioactive secondary metabolites. However, the metabolomic composition of many species remains poorly characterized. Therefore, this study aimed to characterize and compare the metabolomic profiles of 16 Malpighiaceae species collected from four Brazilian biomes (Amazon Rainforest, Atlantic Forest, Caatinga, and Cerrado). Hydroethanolic leaf extracts were analyzed by ultra-high-performance liquid chromatography coupled to tandem mass spectrometry (UHPLC-MS/MS) and chemometric tools. Principal component analysis (PCA) was applied to investigate metabolomic similarities and differences among species. Fifty metabolites were annotated, mainly flavonoids, anthocyanins, tannins, and phenolic acids, demonstrating the remarkable chemodiversity of the family. Multivariate analysis identified discriminant metabolites, including hexadecanoyl glycerol, quercetin-O-glycoside, epigallocatechin, hydroxyflavanone, isorhamnetin galactoside, ferulic acid, and quercetin-3-O-deoxyhexosyl-pentoside. The results revealed substantial metabolomic variability among species occurring within the same biome and highlighted the phytochemical diversity of Malpighiaceae.
Microwave-assisted green synthesis has become a promising and efficient sustainable method of fabrication of nanomaterials. In the current experiment, the synthesis of bismuth oxide (Bi2O3) nanoparticles was done in the presence of ethanolic extract of Artocarpus heterophyllus (jackfruit) peels as a reducing and stabilizing agent. The detailed characterization was performed by UV-visible spectroscopy, FTIR, XRD, DLS, zeta potential, and SEM. The analyses of the plant extract using GC-MS revealed the presence of bioactive phytochemicals, including phenolics and flavonoids, which are important in the formation and stabilization of nanoparticles. SEM analysis indicated a cauliflower-type granular morphology and a mean particle size of around 97 nm, which was similar to DLS results (99 nm hydrodynamic size). XRD was used to verify that the Bi2O3 nanoparticles were crystalline. The photocatalytic activity of the nanoparticles produced was tested to degrade ciprofloxacin (CIP) and ibuprofen (IBU) during optimized conditions of pH, catalyst dosage, and contact time under natural sunlight. The degradation process was carried out under pseudo-first-order kinetics and obtained high removal efficiencies of 93% and 92% for CIP and IBU, respectively.
