Search Results (796)

Cisplatin-induced acute kidney injury (AKI) poses a significant clinical challenge lacking specific therapeutic drugs. Arundina graminifolia, a traditional Dai medicine, exhibits notable renoprotective effects; however, its in vivo pharmacodynamic material basis and molecular mechanisms remain unclear. This study aimed to explore its mechanisms against AKI from the perspective of authentic kidney-migrating components. A cisplatin-induced mouse AKI model was established to evaluate the renoprotective effects of the A. graminifolia extract (BYJ) via biochemical markers and histopathology. UPLC-Q-TOF-MS/MS was employed to comparatively analyze the blood and kidney-migrating components between normal and AKI mice. Network pharmacology and molecular docking were subsequently applied to predict and validate the core signaling pathways based on the specific components detected in the injured kidneys. Results showed that BYJ administration significantly ameliorated renal dysfunction, restored antioxidant capacity, and alleviated tubular necrosis. MS analysis identified 93 chemical components in vitro. In vivo tracking revealed a “pathological targeted recruitment” characteristic: only 6 prototype components entered normal kidneys, whereas 16 prototypes penetrated the AKI kidneys, highly enriched in lipophilic flavonoid aglycones such as kaempferol and apigenin. Network pharmacology predicted that these targeted components could potentially interact with 124 key targets (including AKT1, PIK3CA, and EGFR) to putatively exert anti-apoptotic and anti-inflammatory effects via the PI3K-Akt, TNF, and MAPK pathways. Molecular docking confirmed excellent binding affinities between these aglycones and core target proteins (e.g., kaempferol with PIK3CA at −8.9 kcal/mol). Based on actual in vivo distribution, this study reveals the specific accumulation of polyhydroxy flavonoid aglycones in injured kidneys, providing a reliable scientific basis for defining the pharmacodynamic substances of A. graminifolia. Full article

Dietary polyphenols such as quercetin, resveratrol, and (−)-epigallocatechin-3-gallate (EGCG) have shown neuroprotective effects in epidemiologic and experimental studies of Alzheimer’s disease (AD), although clinical evidence remains limited. This review highlights the importance of investigating glucuronide and sulfate conjugates of these polyphenols, as well as their intestinal microbial metabolites, at bioavailable low nanomolar concentrations, particularly those capable of reaching the brain. Although many in vitro studies use micromolar concentrations of aglycones, the relevance of such concentrations to neuroprotection remains uncertain. While polyphenols are redox-sensitive, their direct antioxidant or prooxidant effects may be limited at nanomolar concentrations. Instead, their neuroprotective actions appear to be mediated through high-affinity interactions with molecular targets such as the 67-kDa laminin receptor (67LR). This receptor binds both aglycones and conjugates at low nanomolar concentrations through a peptide G region containing glycosaminoglycan- and palindromic sequence-related motifs. The same region also binds the prion–amyloid-β complex, suggesting that polyphenols may antagonize amyloid-β binding and thereby prevent its neurotoxicity. The peptide G region may also function as a redox sensor. Binding of polyphenols to 67LR activates cAMP signaling and downstream neuroprotective pathways involving CREB, SIRT1, and protein phosphatase 2A. In addition, nanomolar concentrations of resveratrol and quercetin inhibit quinone reductase 2, an enzyme associated with cognitive decline and reported to be elevated in AD. Given their low bioavailability in the brain and their distinct molecular targets, combining multiple polyphenols at low doses may produce additive or synergistic effects, enhance efficacy, and minimize potential toxicity in the prevention of AD. Full article

Efficient use of agro-industrial residues is central to developing a circular bioeconomy. In this study, apple pomace was used as a feedstock for fermentation with water kefir cultures to investigate the formation of bioactive compounds and evaluate their functional biological effects. The effects of fermentation in a cement tank were compared to a reference fermentation system using a conventional glass vessel, focusing on physicochemical parameters and biological activity. Despite differences in pH evolution, no significant differences between the two fermentation systems were found in antioxidant capacity, total phenolic and carotenoid content, or inhibitory activity against platelet aggregation. Lipid extracts from both systems showed strong antioxidant properties and pronounced inhibitory activity against platelet-activating factor (PAF)- and ADP-induced aggregation, with significantly lower IC₅₀ values for PAF (p < 0.05), indicating enhanced anti-inflammatory specificity. These effects may be attributed to the synergistic interaction of fermentation-derived bioactives, including polar lipids, aglycone flavonoids, and carotenoids. Importantly, fermentation in a cement tank did not compromise biofunctional performance, highlighting its potential as a low-cost and scalable alternative for bioprocessing. Overall, these findings demonstrate that water kefir fermentation can efficiently convert low-value fruit residues into bioactive-rich matrices, providing a sustainable and environmentally friendly approach aligned with EU and UN circular economy frameworks for waste reduction and resource valorization. Full article

Polyphenols act in humans through authentic metabolites, including regio-isomeric glucuronides/sulphates, O-methylated forms, and microbiota products (urolithins, γ-valerolactones, equol), that reach targets by spatiotemporally gated exposure. Vectorial transport (MRP2/BCRP/P-gp), enterohepatic cycling, and β-glucuronidase hubs create early, surface-proximal microbursts of aglycone/catechol, whereas microbiota metabolites arrive systemically 6–24 h later. Signalling emerges from a continuum of weak noncovalent modulation, conditionally gated electrophile/redox relays (catechol → o-quinone, reversible Michael adduction plus signalling-range H₂O₂), and PTM cascades (phosphorylation → acylation → proteostasis) that reprogram NRF2/Keap1, NF-κB/IKK, AMPK/MAPK/PI3K-Akt, SIRT1/HDACs, PPARγ, AhR, and TFEB according to where and when metabolites appear. We provide methods and standards to dose isomer-resolved metabolites at physiological free concentrations (nM-low µM) in transport-competent systems, with PK-informed sampling across seconds–minutes, 15/60/240 min, and 6–24 h, and we outline a research agenda (reference panels, spatial exposure atlases, metabotype-stratified trials, safety windows). Framed this way, polyphenols shift from vague “antioxidants” to programmable dietary signals that enable precision nutrition targeting transcription-factor and proteostasis programmes in vivo. Full article

Grape seeds are a major by-product of grape processing and a rich source of polyphenolic compounds, yet their value remains underutilized. In this study, 12 lactic acid bacteria (LAB) strains were evaluated in a grape seed-based fermentation system to compare their tolerance, metabolic performance, and ability to promote polyphenol release. Among them, Lactiplantibacillus plantarum FBL002 showed the best overall performance. The strain maintained strong viability and metabolic activity at 5% grape seed concentration and released polyphenols more effectively than the other tested strains. The resulting fermentation broth also showed pronounced intracellular antioxidant activity. To clarify the basis of this phenotype, we further combined metabolomic, genomic, and transcriptomic analyses. Fermentation caused substantial shifts in phenolic metabolites, characterized by a decrease in glycosylated forms and an increase in more bioactive aglycones. Genome annotation revealed an enrichment of β-glucosidase-related genes in FBL002, and transcriptomic analysis showed that these genes were markedly upregulated during fermentation. This pattern was closely associated with the enhanced release of polyphenols. Together, these findings identify β-glucosidase as a key driver of grape seed polyphenol biotransformation by FBL002 and support the sustainable, high-value use of grape seeds in functional foods and cosmetic applications. Full article

Canarium luzonicum (Blume) A. Gray, a tree endemic to the Philippines, is the source of Manila elemi, an oleoresin shown to have anti-infective properties owing to its rich terpenoid content. However, its leaves have not yet been subjected to in-depth phytochemical studies. C. luzonicum leaf compounds were isolated by multiple chromatographic techniques and elucidated by 1D and 2D NMR, MS, Polarimetry, IR, CD, and chemical reaction techniques. As a result, four new megastigmane glycosides, canariluzoniosides A–D (1–4), and two new monoterpenoid glycosides, canariluzoniosides E and F (5–6), were identified along with 29 additional known compounds. Canariluzonioside A (1) was a unique megastigmane featuring a tricyclic ring system. The new glycosides’ sugar moieties were obtained by acid hydrolysis and confirmed by HPLC-OR. Aglycones were liberated by enzymatic hydrolysis and were structurally characterized, one of which was the new compound, named canariluzonol A (1a). Finally, most compounds were screened for cytotoxicity against A549 human lung cancer cell line and for inhibition against Leishmania major promastigotes. Notable bioactivity was observed in known 3,4-seco-A-ring triterpenoids such as canaric acid and nyctanthic acid, for which revision of spectroscopic data is also proposed. Full article

Forsythia suspensa leaves black tea (FSLBT) is a fermented herbal tea traditionally consumed in Northern China, yet its bioactive constituents and antioxidant basis remain insufficiently understood. In this study, a phytochemical investigation of FSLBT led to the isolation and structural identification of nine compounds, including five lignans and four pentacyclic triterpenic acids, whose structures were elucidated by ¹H-NMR, ¹³C-NMR, and HRESIMS spectral analysis. Notably, epipinoresinol and pinoresinol monomethyl ether were isolated from Forsythia suspensa leaves (FSL) for the first time. Among the isolated lignans, phillygenin, epipinoresinol, pinoresinol monomethyl ether, and pinoresinol were further evaluated for antioxidant activity using DPPH•, ABTS•+, and FRAP assays. The four lignans exhibited concentration-dependent antioxidant activities, with IC₅₀ (half maximal inhibitory concentration) values ranging from 20.32 to 46.40 μg/mL for DPPH• scavenging and 37.29 to 72.71 μg/mL for ABTS•+ scavenging, while FRAP EC₅₀ (half maximal effective concentration) values ranged from 1.53 to 1.90 mg/mL. Quantitative HPLC analysis showed that the contents of phillygenin, epipinoresinol, pinoresinol monomethyl ether, and pinoresinol in FSLBT were 3.48 ± 1.12 wt%, 0.39 ± 0.21 wt%, 0.26 ± 0.20 wt%, and 0.18 ± 0.07 wt%, respectively. These results indicate that FSLBT is enriched in lignan aglycones, particularly phillygenin, and that these major lignans possess measurable chemical antioxidant activities, providing a phytochemical basis for further investigation of the functional properties of this fermented herbal tea. Full article

The flavonoids constitute a class of secondary metabolites distributed in plants, occurring in free form (aglycone) or conjugated sugars (glycosides), and are notable for their recognized pharmacological potential. This study investigated flavonoids isolated from the leaves of Erythroxylum rimosum, correlating their chemical structures with biological activities evaluated in vitro assays. The flavonoids did not show significant cytotoxicity in mammalian cells (CC₅₀ > 100 μM), while flavonoids 4 and 5, glycosylated with six-carbon sugar, inhibited the promastigote forms of L. braziliensis with IC₅₀ of 10.34 ± 0.70 μM and 10.14 ± 0.50 μM, respectively. In intracellular infection models, they reduced ~43% of parasitized cells and ~40% of amastigotes. Scanning electron microscopy demonstrated changes in promastigotes, including loss of membrane integrity and flagellum shortening. A molecular docking study with L. mexicana arginase suggested enzyme inhibition as a possible mechanism of action, influenced by sugar chirality. In the antioxidant evaluation, using the DPPH and β-carotene methods, quercetin showed the best inhibitory concentration value (IC₅₀ = 0.22 ± 0.94 mg/mL), followed by glycoside 5 (IC₅₀ = 0.42 ± 0.09 mg/mL). In addition, the flavonoids glycosylated with five-carbon sugar inhibited the acetylcholinesterase enzyme. Full article

Background: Dragon’s blood (dried resin of Dracaena cochinchinensis (Lour.) S.C.Chen) is a classic traditional medicine for treating ischemic stroke, yet its bioactive components capable of penetrating the blood–brain barrier (BBB) remain ill-defined. This study aims to elucidate its material basis and the synergistic mechanism of Borneol as a “guide drug.” Methods: A systematic strategy integrating UHPLC-Q-TOF-MS/MS and metabolomics was employed to map the chemical profile of dragon’s blood and identify its migrating constituents in rats. Results: A total of 96 compounds were characterized in vitro. In vivo analysis of the cerebrospinal fluid (CSF) revealed a brain-penetrating profile that was significantly enriched by Borneol, with the number of detected constituents increasing from 11 in the DB group to 16 in the DB + B group. The results demonstrated that demethylation, glycoside hydrolysis, and oxidation are primary metabolic pathways, validating a “pro-drug” mechanism where aglycones and hydroxylated derivatives act as the central effectors. Notably, Borneol not only enhanced the BBB permeability of lipophilic flavonoids but also facilitated unique metabolic transformations, such as the cyclization of berberrubine to coptisine. Conclusions: This study elucidates the brain-penetrating material basis of dragon’s blood and reveals the dual synergistic mechanism of Borneol involving both physical permeation enhancement and metabolic modulation, offering scientific evidence for its clinical application in central nervous system diseases. Full article

Roselle (Hibiscus sabdariffa) leaves are the major by-product after harvesting the commercial calyces, and they contain diverse functional metabolites such as phenolic acids and flavonoids. This study aimed to comprehensively characterize the metabolite profiles of the leaves of two Taiwanese roselle varieties (Taitung No. 6 and Taitung No. 3) and to evaluate their antiproliferative and insulin resistance-ameliorating activities. Extracts prepared with 50% EtOH and n-hexane were analyzed by untargeted and targeted LC-MS/MS and GC-MS, respectively. Results revealed that the 50% EtOH extracts of both varieties were rich in neochlorogenic acid, cryptochlorogenic acid, rutin, and nicotiflorin. Taitung No. 6 uniquely contained higher levels of anthocyanins including delphinidin-3-O-sambubioside and cyanidin-3-O-sambubioside. Acidified 50% EtOH extraction increased flavonoid aglycone and polyamine contents. n-Hexane extracts were identified as potential sources of vitamin E, α-linolenic acid, squalene, and phytol. Both varieties exhibited antiproliferative activity against BxPC-3 pancreatic cancer cells (IC₅₀: 289.2–356.8 μg/mL) and significantly improved the glucose uptake in insulin-resistant HepG2 cells. Neochlorogenic acid and cryptochlorogenic acid were identified as primary active contributors to these bioactivities. This study elucidated the metabolite composition of Taiwanese roselle leaves and provided a scientific basis for the utilization of roselle leaves as a promising functional ingredient. Full article

Silylation of phenyl 1-thio-α-d-mannopyranoside, ethyl 1-thio-α- and β-d-mannopyranosides under different conditions was studied. Low-temperature NMR analysis revealed that the silylated products typically exist as an equilibrium of two chair conformations with a predominance of the axially rich ¹C₄ conformation. The dependence of the ratio of conformers on the anomeric configuration, the type of silyl groups and the nature of the aglycone was established. The fully silylated phenyl 1-thio-α-d-mannopyranoside, ethyl 1-thio-α- and β-d-mannopyranosides were tested as glycosyl donors in the synthesis of di- and trisaccharides, including one-pot synthesis. In all cases, only α-linked oligosaccharides as mixtures of conformers were formed. The obtained deprotected Manp-(1→2)-α-d-Manp-(1→5)-α-d-Araf trisaccharide 2-azidoethyl glycoside, related to the non-reducing terminal fragment of the mannose-capped lipoarabinomannan (ManLAM) of Mycobacterium tuberculosis, can be used for further preparation of conjugates with proteins to provide antigens, which are important for development of new tuberculosis screening assays. Full article

Olive pomace (OP) has been widely reported as a rich source of phenolic compounds with potential application as food additives with health-promoting properties. The aim of this work was to evaluate pressurized liquid extraction (PLE) as a strategy to obtain antioxidant and antimicrobial extracts from OP. Extractions were carried out in laboratory-scale equipment following a combined static/dynamic procedure. The extraction temperature (100, 120 and 140 °C) and the composition of solvent (50, 75 and 100% ethanol in water) were studied as independent variables of the process using a Face Centered Central Composite Design (α = 1). According to the fitted quadratic model (p < 0.05), the maximum Total Phenol Content (TPC) and Trolox Equivalent Antioxidant Capacity (TEAC) values were obtained at 120 °C using ethanol concentrations between 60 and 80%. Chemical characterization by RP/HPLC-Q-TOF MS/MS allowed the tentative identification of 37 compounds, with quinic acid being the most abundant compound under all extraction conditions, followed by elenolic acid, dimethyl-hydroxy-verbascoside, maslinic acid, hydroxy-verbascoside and oleuropein aglycone. Other secoiridoids, secoridoid derivatives, flavonoids, simple phenols and triterpenic acids were also identified. The extract obtained at 120 °C with 75% ethanol was able to protect purified sunflower oil in an accelerated oxidative stability test (Rancimat), increasing its induction period by 2.4-fold when added at 1000 mg/kg. This extract also exhibited antimicrobial activity against S. aureus, B. cereus, S. enterica and S. sonnei with a Minimum Inhibitory Concentration (MIC) of 3.6 mg/mL. These results highlight the potential of PLE olive pomace extracts as natural preservatives for food applications. Full article

Murtilla pomace (the by-product generated during juice production) shows a high phenolic content. Recovering phenolics from murtilla pomace is a sustainable approach towards zero waste. In this study, murtilla pomace was subjected to enzyme-assisted extraction using Viscozyme. The extracts were analyzed for TPC and phenolic profile. Antioxidant activity was evaluated by chemical-based assays and the antioxidant property was demonstrated for the first time in an ozone-induced oxidation process applied to a raw fish model system. Enzymatic pretreatment with Viscozyme increased the total phenolic content by up to 57%. The antioxidant activity also increased upon enzymatic treatment. The concentration of quercetin was positively affected, while the content of rutin decreased upon enzymatic pretreatment, likely reflecting the enzymatic hydrolysis biotransforming rutin glycoside into quercetin aglycone. Phenolics from murtilla pomace obtained upon enzyme-assisted extraction were shown to be effective as natural antioxidants against ozone-induced oxidation in salmon. Therefore, enzyme-assisted extraction may be an environmentally friendly strategy in the recovery of these natural antioxidants. Full article

Environmental pollution from plastics is largely driven by inadequate waste management, particularly in food packaging that relies heavily on petroleum-derived materials. This study utilized gelatin capsule waste (GCW) as a sustainable biopolymer and incorporated yellow peacock flower extract (YPE), obtained via ultrasound-assisted extraction (UAE), at various concentrations (0–2%, w/v) to develop biodegradable films with enhanced functional and antioxidant properties. The main phenolic constituents of YPE were flavonoid aglycones and their glycosylated derivatives. YPE showed total phenolic content of 98.44–129.34 mg GAE/g dry extract, with ABTS, DPPH, and FRAP antioxidant activities ranging from 5.51 to 8.11, 3.17–7.63, and 3.86–5.82 mg TE/g dry extract, respectively. Incorporation of YPE into GCW films significantly improved light barrier properties, thermal stability, mechanical strength, and antioxidant activity, along with a reduction in water vapor permeability and an increase in contact angle, indicating enhanced film hydrophobicity. All films exhibited excellent biodegradability, with complete disintegration within 15 days under soil burial conditions. Films containing 2% YPE (GF4) showed significantly higher thickness, tensile strength, and thermal stability, along with increased opacity, compared with the control (GF0), indicating a reinforcing effect. FTIR analysis revealed the interaction between protein and phenolic compounds from YPE. In a food application model, GF4 film pouches (5 × 5 cm²) effectively delayed oxidative deterioration of dried shrimp during storage at 25 ± 2 °C for 15 days. These findings highlight YPE as a promising bioactive ingredient for biodegradable active packaging and demonstrate the feasibility of GCW as a sustainable biopolymer for eco-friendly films. Full article

Background: Tectoridin is a prominent isoflavone glycoside found in herbs such as Belamcanda chinensis (L.) DC and Iris tectorum Maxim. It has drawn increasing research interest due to its promising pharmacological activities. However, no critical review to date has determined whether its broad pharmacological activity stems from binding to specific targets or from the non-specific, broad-spectrum activity commonly associated with flavonoids. This paper provides a comprehensive review of tectoridin, covering its plant sources, pharmacological effects, pharmacokinetics, and toxicity, alongside an in-depth analysis of the mechanisms underlying its pharmacological effects and strategic recommendations for advancing its clinical translation. Methods: A systematic literature search was conducted in PubMed, Web of Science, Google Scholar, SciFinder, and CNKI for publications from 1968 to 2025 using keywords including tectoridin, tectorigenin 7-O-glucoside, traditional uses, ethnopharmacology, pharmacology, bioactive compounds, biological activity, pharmacokinetics and toxicity. Results: Tectoridin exhibits a broad spectrum of pharmacological activities, including anticancer, anti-inflammatory, hepatoprotective, antidiabetic, antioxidant, cardiovascular, and estrogenic effects. Pharmacokinetic studies have shown rapid tissue distribution and slow elimination; the aglycone metabolite tectorigenin often displays enhanced bioactivity, and chemical modifications may further improve efficacy. Toxicity data suggest relative safety in medicinal food contexts, but comprehensive in vivo studies remain limited. Tectoridin shows promise for treating cancer and inflammatory diseases; however, further research is needed to elucidate its molecular mechanisms, clarify toxicity, and optimize bioactivity. Conclusions: This review bridges natural products and modern therapeutics by focusing on tectoridin, highlighting its therapeutic potential, addressing challenges, and offering new perspectives for treating various diseases. Full article