Search Results (470)

Lemon peel, which contains a wide variety of antioxidant compounds and biopolymers, is an interesting byproduct for valorization. In this study, pectin and cellulose were obtained from lemon peel with 36% and 23% extraction yields. Meanwhile, when evaluating the extraction of secondary metabolites using various enzymes, it was found that their concentrations increased the most in the case of pectin methylesterase, by up to 21.7% for eriocitrin, although the solid residue was not affected spectroscopically by the enzymatic activity. In contrast, enzyme mixes with β-glucosidase activity showed no presence of the O-glycosylated flavonoids, suggesting their hydrolysis into the aglycones. Full article

Glycosylation serves as an effective strategy to enhance the solubility, bioavailability, and pharmacological activity of polyhydroxyphenols. In this study, we explored the glycosylation of natural and natural-inspired phenolic compounds using the glycosyltransferase AbCGT and evaluated the anti-renal fibrotic potential of the resulting glycosides. Among them, 1,3,5,8-tetrahydroxyxanthone 5-O-β-D-glucopyranoside (2-1a), synthesized via the regioselective 5-O-glycosylation of demethylbellidifolin, demonstrated significant anti-renal fibrotic activity. In contrast, its homologous glycosyltransferase, UGT73AE1, predominantly glycosylated demethylbellidifolin at the 3-OH position. Molecular docking studies revealed the structural basis for this regioselectivity difference. To enhance the production of 2-1a, we established a UDP-glucose (UDPG) recycling system by coupling AbCGT with Glycine max sucrose synthase (GmSuSy) and subsequently optimized the reaction conditions. Furthermore, targeted mutagenesis of AbCGT informed by molecular docking analysis identified a F138A mutant that enhanced glycosylation yield by 2.3-fold. This work develops a novel glycosyltransferase-based catalytic system and identifies a new compound with potential anti-renal fibrotic activity. Full article

A novel steviol glycoside, Rebaudioside D17, was identified from the leaf extract of Stevia rebaudiana Bertoni. This compound features a rare β-1→4 glycosidic linkage between two glucose units at the C19 position, distinguishing it from its structural isomer, Rebaudioside D. The aim of this study was to isolate and characterize Rebaudioside D17 and investigate its biosynthetic origin. The compound was isolated and structurally characterized using comprehensive NMR spectroscopy including ¹H, ¹³C, COSY, NOESY, Heteronuclear Single Quantum Coherence–Distortionless Enhancement by Polarization Transfer (HSQC-DEPT), Heteronuclear Multiple Bond Correlation (HMBC), Heteronuclear Single Quantum Coherence–Total Correlated Spectroscopy (HSQC-TOCSY), along with mass spectrometry analysis. A tentative biosynthetic pathway is proposed, involving Rebaudioside E19, a putative intermediate bearing the same β-1→4 glycosidic linkage at C19. Rebaudioside E19 may serve as a common precursor to both Rebaudioside D17 and Rebaudioside U3, a minor steviol glycoside previously reported in Stevia rebaudiana leaf extract, which also contains the same β-1→4 glycosidic linkage. The discovery of Rebaudioside D17 expands the known diversity of steviol glycosides and provides new insights into glycosylation patterns in Stevia rebaudiana, which may support the development and production of novel sweeteners with improved sensory and physicochemical properties. Full article

Weed control is mainly carried out using synthetic herbicides, which represent 62.6% of the total pesticides sold. However, some plants produce allelochemicals that inhibit the growth of other plants, and these substances can be isolated and used as natural herbicides. This study aimed to evaluate the allelopathic, cytotoxic, genotoxic, and antigenotoxic potential of the ethanol extract (EE), hexane (HEX), dichloromethane (DCM), ethyl acetate (EA) and hydroethanol (HE) fractions obtained from Tecoma stans flowers. Nuclear magnetic resonance (NMR) was used to characterize the compounds present in the samples. The allelopathic activity was tested using Allium cepa and Lactuca sativa seeds, and the cytotoxicity, genotoxicity and antigenotoxicity were evaluated using A. cepa seeds. The saturated and unsaturated fatty acids ω-3 and ω-6, terpenes, flavonoids, and phenolic acids with coumaroyl or glycosyl derivatives were characterized in the samples. The HEX and DCM fractions significantly inhibited germination and root growth, effects associated with fatty acids and phenolic compounds. The EA fraction exhibits genotoxic potential at higher concentrations tested. The extract and fractions reduced the genotoxicity induced by glyphosate and atrazine, reversing chromosomal abnormalities. These results demonstrate the possible use of the extract and fractions as natural sources of allelochemicals, but safe dosage validation is required. Full article

This study investigated the effect of superheated steam (SS) assisted glycosylation modification on the flavor profile of oyster peptides (OP), and explored the correlation between key flavor compounds and glycosylation degree using Gas Chromatography–Ion Mobility Spectrometry (GC-IMS) and nano-scale Liquid Chromatography coupled with High-Resolution Mass Spectrometry (nano-LC/HRMS). The results indicated that SS treatment accelerated the glycosylation process, reduced free amino groups level, and distinguished their unique flavor through E-nose. GC-IMS analysis detected 64 signal peaks including 13 aldehydes, 6 ketones, 7 esters, 6 alcohols, 2 acids, 2 furans and 5 other substances. And it was revealed that SS-mediated glycosylation treatment reduced the levels of fishy odorants like Heptanal and Nonanal, while promoting the pleasant-smelling alcohols and esters. In addition, Pearson correlation showed a positive correlation between excessive glycation and the increase in aldehydes, which might cause the recurrence of undesirable fishy notes. Further nano-LC/HRMS analysis revealed that arginine and lysine acted as the main sites for glycosylation modification. Notably, glycosylated peptides such as KAFGHENEALVRK, DSRAATSPGELGVTIEGPKE, generated by mild SS treatment could convert into ketones and pyrazines in subsequent reactions, thereby contributing to overall sensory enhancement. In conclusion, SS treatment at 110 °C for 1 min significantly improved the flavor quality of OP and sustains improvement in subsequent stages, providing theoretical support for flavor optimization of oyster peptides. Full article

(1) Background: All-trans retinoic acid (ATRA) has transformed the treatment of acute promyelocytic leukemia (APL) by inducing terminal myeloid differentiation. However, its efficacy in non-APL acute myeloid leukemia (AML) is limited. Exploring combination strategies that enhance ATRA-induced differentiation may broaden its therapeutic potential. (2) Methods: A literature search of PubMed using the keywords “ATRA,” “myeloid,” and “differentiation inducer or enhancer” identified more than 500 published papers as of November 2025. Pre-clinical and clinical studies were reviewed, with a focus on mechanisms, combination partners, and translational relevance. (3) Results: Clinical evidence confirms that ATRA combined with arsenic trioxide or epigenetic modulators achieves high remission rates in APL and selected AML subtypes. Pre-clinical studies show synergistic differentiation effects when ATRA is combined with CDK and kinase inhibitors, nucleotide synthesis inhibitors, DNA-damaging agents, Bcl-2/MDM2 inhibitors, proteasome inhibitors, cytokines, glycosylation modifiers, natural products, and antibiotic-derived compounds. Mechanistically, these combinations modulate key signaling pathways (MAPK, Akt, JAK/STAT), stabilize RARα, remodel chromatin, and perturb nucleotide metabolism. Although translation to non-APL AML remains limited, these findings provide a rational basis for future clinical trials. (4) ATRA-based combination therapies represent a promising strategy to extend differentiation therapy beyond APL. This review, authored solely by the investigator, highlights molecular targets and potential enhancers warranting further clinical evaluation in AML. Full article

Background: Lavandula (Lamiaceae) includes numerous species, cultivars, and hybrids widely cultivated for both their ornamental traits and for functional uses in perfumery, nutrition, medicinal, and cosmetic applications. Objectives: This study characterized the phytochemical profiles of three species (Lavandula stoechas L., Lavandula latifolia Medik., and Lavandula angustifolia Mill.), two cultivars (L. stoechas ‘Alba’ L. and L. angustifolia ‘Krajova’ Mill.), and the interspecific hybrid Lavandula × intermedia ‘Alba’ Emeric ex Loisel. Methods: All grown species and cultivars were maintained under uniform environmental and harvested simultaneously, to provide a comparative assessment of their terpene and polyphenol profiles and content, as well as their associated antioxidant activity. Results: HPLC-DAD/QTOF-MS analysis revealed differences in flavonoid and hydroxycinnamic acid content among species and cultivars. The main compounds identified were glycosylated derivatives of coumaric, caffeic, and ferulic acids, along with luteolin and apigenin derivatives. L. latifolia Medik. exhibited the highest hydroxycinnamic acid content (5.306 ± 1.265 mg/g FW), whereas L. stoechas ‘Alba’ L. showed the highest flavonoid concentration (2.537 ± 0.192 mg/g FW). GC-MS analysis indicated that hydrocarbon and oxygenated monoterpenes were the predominant terpene classes, with the highest levels recorded in L. stoechas L. (1922.09 ± 144.12 ng/g FW oxygenated; 945.89 ± 159.26 ng/g FW hydrocarbon monoterpenes). Antioxidant activity, assessed via DPPH and FRAP assays, was significantly correlated with flavonoid content across species, cultivars, and the hybrid. Conclusions: Intraspecific and interspecific variability within the Lavandula genus influences antioxidant activity and determines its suitability for different applications. Full article

The cosmetics industry is experiencing dynamic growth, which poses significant environmental challenges, primarily due to the accumulation of cosmetic ingredients in aquatic and soil ecosystems. In response, sustainable solutions aligned with the principles of the circular economy and the concept of “clean beauty” are increasingly sought. One promising approach is the use of bioferments obtained through the fermentation of plant raw materials from the Asteraceae family as alternatives to conventional extracts in cosmetic formulations. This literature review provides up-to-date insights into the biotechnological transformation of Asteraceae plants into cosmetic bioferments, with particular emphasis on fermentation processes enabling enzymatic hydrolysis of glycosylated flavonoids into aglycones, followed by their conversion into low-molecular-weight phenolic acids. These compounds exhibit improved local skin penetration (i.e., higher local bioavailability within the epidermal barrier) compared to their parent glycosides, thereby enhancing antioxidant activity. The analysis includes evidence-based data on the enzymatic hydrolysis of glycosidic flavonoids into free aglycones and their subsequent conversion into low-molecular-weight phenolic acids, which exhibit improved antioxidant potential compared to unfermented extracts. Furthermore, this narrative review highlights the role of lactic acid bacteria and yeast in producing bioferments enriched with bioactive metabolites, including lactic acid (acting as a natural moisturizing factor and preservative), while emphasizing their biodegradability and contribution to minimizing the environmental impact of cosmetics. This review aims to provide a comprehensive perspective on the technological, dermatological, and environmental aspects of Asteraceae-based bioferments, outlining their potential as sustainable and functional ingredients in modern cosmetics. Full article

Background/Objectives:Pereskia aculeata and Pereskia grandifolia belong to the Cactaceae family, despite their foliar and woody stem characteristics. Both species are commonly known as Ora-pro-nóbis (derived from Latin, meaning “pray for us”), a name rooted in their historical use in colonial Brazil due to their nutritional value, particularly P. aculeata, which is frequently described as a high-protein food source. The goal of the present study was to compare these species based on phytochemical composition and antioxidant capacity. Methods: Both species were investigated for their chemical antioxidant properties (DPPH and phosphomolybdenum complex) and cellular anti-ROS activity using the CACO-2 cell line. A comprehensive phytochemical analysis was performed using LC-MS and GC-MS. Results: P. aculeata exhibited a more abundant content of phenolics and flavonoids, with greater structural variability in phenolic compounds and glycosylated flavonoids than P. grandifolia. Still, P. aculeata showed a more potent chemical antioxidant effect. By contrast, in P. grandifolia, a series of novel saponins was now discovered and characterized. In addition, the compounds from this species exhibited a greater cellular antioxidant activity than those of P. aculeata. Tryptophan-derived alkaloids, such as abrine (N-methyltryptophan), were present in both species, but hypaphorine only in P. aculeata. Conclusions: Both species of Pereskia exhibit potential health benefits, including distinct antioxidant activity, among other unexplored effects, given their significant variability in phytochemicals. These differences could be investigated in greater depth using combined LC-MS and GC-MS, thereby enabling more confident structural investigations of these natural compounds. Full article

Background/Objectives: Plants inhabiting mediterranean-influenced climatic zones, like Helichrysum stoechas (L.) Moench subsp. stoechas, Lavandula pedunculata (Mill.) Cav., and Thymus mastichina (L.) L. subsp. mastichina, have been scarcely investigated regarding their richness in phenolic compounds, herein explored as sources of skin anti-aging compounds. Methods: In this investigation, Fourier transform infrared spectroscopy (FTIR) in attenuated total reflectance (ATR) mode and high-performance liquid chromatography coupled with diode-array detection and electrospray ionization tandem mass spectrometry (HPLC-DAD-ESI/MSⁿ) were employed to chemically characterize the hydroethanolic extracts (HEs), and their cell-free antioxidant potential was screened. Thereafter, non-toxic concentrations of HEs were determined in human skin cells using Alamar blue^® and Sulforhodamine B assays. The cytoprotective and antioxidant effects of HEs were assessed in tert-butyl hydroperoxide-stimulated fibroblasts, their anti-inflammatory potential was studied in lipopolysaccharide-injured macrophages, and enzymatic inhibition assays were performed. Notably, the irritant effects of HEs were tested according to Test Guideline No. 439 of the Organization for Economic Co-operation and Development (OECD). Results: The major compounds identified in the T. mastichina and L. pedunculata HEs were rosmarinic and salvianolic acid derivatives, while H. stoechas HE was mainly composed of caffeoyl and feruloyl derivatives, and O-glycosylated flavonoids. T. mastichina (≤0.4 mg/mL) exhibited significant cytoprotective, anti-inflammatory, and antioxidant effects, as well as remarkable anti-hyaluronidase activity. Conclusions: Shedding light on the quantitative and qualitative chemical picture of these HEs highlighted T. mastichina as a promising candidate to target skin aging effects, which correlates with its phenolic content. Further investigation is warranted regarding its anti-aging pharmacological activity, which could lead to the development of plant-based skin anti-aging products. Full article

Due to its appealing composition, grape pomace (GP), the major by-product of the wine industry, could be considered an ideal candidate for innovative functional foods development. In this study, a rice/GP-yogurt alternative, also known as gurt, fermented with selected lactic acid bacteria, was designed. An extensive characterization of the gurts led to the selection of the one fermented with Lactiplantibacillus plantarum T0A10. The strains showed good pro-technological performances (fast acidification and growth up to 9 log cfu/g in the specific plant-based composite substrate), as well as the ability to increase DPPH radical scavenging activity compared to the unfermented control (57% against 40%). Then, an in-depth focus on the effect of fermentation on phenolic compounds and their related antioxidant efficacy on human keratinocytes was provided, elucidating a compound/function relationship. Fermentation significantly modified the phenolic profile of the gurt, reducing glycosylated forms of flavonols and phenolic acids and increasing the content of catechin and pyrogallol (more than 100 mg/kg combined). Such modification was responsible for significantly up-regulating (p < 0.05) the expression of the antioxidant enzyme superoxide dismutase 2, thus protecting NCTC 2544 cells against oxidative stress. Overall, these findings provide a foundation for developing value-added products from GP, supporting both circular economy initiatives and functional ingredient innovation. Full article

Glucosidase II (GluII) is a heterodimeric enzyme localized in the endoplasmic reticulum (ER), essential for the sequential trimming of glucose residues during N-linked glycosylation. This critical function facilitates glycoprotein folding via the calnexin/calreticulin chaperone system, maintaining ER homeostasis. Dysregulation or inhibition of GluII has been implicated in various pathological processes, including cancer, viral infections, and glycoprotein misfolding disorders. This review summarizes the current knowledge of GluII’s structure and function, highlights a wide range of natural and synthetic GluII inhibitors—including iminosugar derivatives (e.g., deoxynojirimycin (DNJ), castanospermine (CAST)), non-iminosugar compounds (e.g., bromoconduritol, catechins), and mechanism-based cyclophellitol analogues—and evaluates their biological effects and therapeutic potential. The cellular impact of GluII inhibition is explored in the context of ER stress, unfolded protein response (UPR), tumor cell apoptosis, and viral replication. Key challenges in developing selective GluII inhibitors are discussed, with a focus on strategies to minimize off-target effects, including prodrug design, allosteric modulation, and emerging genetic approaches such as microRNA (miRNA)-mediated downregulation of GluII subunits. Taken together, these insights underscore the therapeutic relevance of GluII as a druggable target and pave the way for the rational design of next-generation inhibitors in oncology, infectious diseases, and metabolic disorders. Full article

Food processing techniques are widely used in the food industry to ensure food safety, extend shelf life, and enhance sensory appeal without compromising the product’s nutritional quality. Pearl millet, which is considered a “nutricereal”, features essential content of proteins, soluble and insoluble fibers, minerals (e.g., iron, zinc, and magnesium), bioactive compounds (e.g., phenolic acids, flavonoids, and carotenoids), and antinutritional factors (e.g., phytic acid, C-glycosyl flavones, tannins, and non-digestible oligosaccharides). This nutricereal also undergoes processing methods to improve or maintain its nutritional quality while simultaneously reducing antinutritional factors. Pearl millet processing techniques are categorized into conventional (or traditional) and advanced methods; however, a knowledge gap exists in studies evaluating the post-processing of pearl millet and its impact on metabolic health in in vivo and in vitro experimental models. This study aims to demonstrate the principal conventional and advanced processing techniques used in pearl millet, how they can ensure nutritional quality and reduce antinutritional factors, and how the final post-processing product could impact metabolic health. Full article

Kaempferitrin (KAE) is a natural flavonol dirhamnopyranoside with various pharmacological activities, isolated from the antithrombotic fraction of Celastrus orbiculatus Thunb. This study aimed to investigate the antithrombotic activity and “effective forms” of KAE. The results showed that KAE significantly prolonged rabbit plasma recalcification time in vitro. In the FeCl₃-induced rat arterial thrombosis model, KAE demonstrated antithrombotic effects by inhibiting coagulation, platelet aggregation, and fibrinolysis, with a lesser risk of bleeding compared to aspirin. KAE was orally administered to rats, and a total of 192 metabolites were characterized. These included 25 phase I metabolites, 8 hydroxylated and methylated metabolites, 57 sulfated metabolites, 74 glucuronidated metabolites, 26 sulfated and glucuronidated metabolites, and 2 glycosylated metabolites. Twenty-eight compounds were considered the in vivo “effective forms” of KAE for their antithrombotic activity. Network pharmacology, molecular docking, and molecular dynamics simulations collectively predict that these “effective forms” may exert antithrombotic effects by suppressing the SRC/PI3K/AKT pathway. This study provides a foundation for a better understanding of the in vivo “effective forms” and mechanisms underlying KAE’s antithrombotic activity, which is essential for understanding of “hexue” traditional efficacy of C. orbiculatus. Full article

A series of glycosylated thienopyrimidinone derivatives (7a–e and 8a–e), previously synthesized through a multi-step sequence involving a Gewald reaction, thiocyanate cyclization, functionalization with chloroacetic acid, and subsequent coupling with aldose sugars (glucose, mannose, galactose, xylose, and arabinose), were subjected to comprehensive biological evaluation. Structural confirmation of all compounds was achieved by spectroscopic and elemental analyses. Among them, compound 8e displayed remarkable antioxidant capacity, with radical scavenging activity surpassing standard controls, and demonstrated significant neuroprotective potential through its ability to attenuate oxidative stress, a key driver of neurodegeneration. Furthermore, 8e exhibited notable anti-arthritic and anti-diabetic effects, which may indirectly enhance neuroprotection by alleviating systemic inflammation and metabolic dysfunction—recognized risk factors for neurodegenerative disorders. Molecular docking and molecular dynamics studies revealed favorable binding interactions and structural stability of 8e with multiple biological targets, supporting its promise as a multifunctional neuroprotective candidate against oxidative stress and neurodegeneration. Full article