Search Results (26,365)

Barbituric acid is a heterocyclic compound with various pharmacological and biological applications. This review paper provides a comprehensive overview of barbituric acid’s synthesis, reactions, and bio-applications, highlighting its multifaceted role in various fields. Many heterocyclic derivatives were formed based on barbituric acid, for instance, pyrano-fused pyrimidine derivatives, spiro-oxindole derivatives, chrome-based barbituric acid derivatives, and many more via the atom economic method, Michael addition reaction, Knoevenagel condensation reaction, etc. In the context of bio-applications, this review examines the production of a wide range of bioactive drugs like anti-histamine, anti-leprotic, sedative–hypnotic, anti-inflammatory, anti-urease, antiviral, anti-AIDS, antimicrobial, antioxidant, anticonvulsant, anesthetic agent, antitumor, and anticancer drugs using efficient multicomponent reactions. By showcasing the versatility and potential of this compound, it aims to inspire further research and innovation in the field, leading to the development of novel barbituric acid derivatives with enhanced properties and diverse applications, with coverage of the literature relevant up to 2024. Full article

Background: Human milk oligosaccharides (HMOs), which are unique bioactive components in human milk, are increasingly recognized for their multifaceted roles in infant health. A deeper understanding of the nexus between HMOs and the gut–brain axis can revolutionize neonatal nutrition and neurodevelopmental strategies. Methods: We performed a narrative review using PubMed, Embase, and Google Scholar to source relevant articles. The focus was on studies detailing the influence of HMOs on the gut and brain systems, especially in neonates. Articles were subsequently synthesized based on their exploration into the effects and mechanisms of HMOs on these interconnected systems. Results: HMOs significantly influence the neonatal gut–brain axis. Specific concentrations of HMO, measured 1 and 6 months after birth, would seem to agree with this hypothesis. HMOs are shown to influence gut microbiota composition and enhance neurotransmitter production, which are crucial for brain development. For instance, 2′-fucosyllactose has been demonstrated to support cognitive development by fostering beneficial gut bacteria that produce essential short-chain fatty acids. Conclusions: HMOs serve as crucial modulators of the neonatal gut–brain axis, underscoring their importance in infant nutrition and neurodevelopment. Their dual role in shaping the infant gut while influencing brain function presents them as potential game-changers in neonatal health strategies. Full article

Almond okara, a by-product of almond milk production, is rich in bioactive components, such as polyphenols, lipids, and alpha-tocopherol, making it a valuable functional food ingredient. This work aimed to investigate its composition while exploring two main aspects: (i) the impact of extraction time, solid-to-solvent ratio, ethanol concentration, and temperature on polyphenol recovery, and (ii) the quantification of okara’s triglycerides (TG) and alpha-tocopherol contents. The polyphenols’ optimal extraction conditions were 90 min, a 1:30 solid-to-solvent ratio (w/v), 50% ethanol, and 60 °C. These conditions achieved a total polyphenol yield of 523 mg GAE, tannin yield of 340 mg GAE, total flavonoid yield of 548 mg CE, and a total antioxidant capacity of 779 mg AAE per 100 g dry okara. The Peleg model effectively described the extraction kinetics. Additionally, TG levels, quantified by UHE/LPSFC-APCI-MS, in okara were comparable to those in almonds, and alpha-tocopherol levels, quantified by LC-UV, were 14,400 µg/100 g in almonds and 15,600 µg/100 g in okara. These findings highlight the potential of okara as a valuable resource, with a straightforward, scalable, and cost-effective solid-liquid extraction (SLE) method for polyphenols and a supercritical fluid extraction method for TG, for use in the functional food, nutraceutical, and cosmetic industries. Full article

The skin barrier is essential for maintaining the body’s internal homeostasis, protecting against harmful external substances, and regulating water and electrolyte balance. Traditional Chinese Medicine (TCM) offers notable advantages in restoring skin barrier function due to its diverse components, targets, and pathways. Recent studies have demonstrated that active ingredients in TCM can safely and effectively repair damaged skin barriers, reinstating their proper functions. This review article provides a comprehensive overview of the mechanisms underlying skin barrier damage and explores how the bioactive constituents of TCM contribute to skin barrier repair, thereby offering a theoretical framework to inform clinical practices. Full article

Drimenol, a phytochemical with a distinct odor is found in edible aromatic plants, such as Polygonum minus (known as kesum in Malaysia) and Drimys winteri. Recently, drimenol has received increasing attention owing to its diverse biological activities. This review offers the first extensive overview of drimenol, covering its sources, bioactivities, and derivatives. Notably, drimenol possesses a wide spectrum of biological activities, including antifungal, antibacterial, anti-insect, antiparasitic, cytotoxic, anticancer, and antioxidant effects. Moreover, some mechanisms of its activities, such as its antifungal effects against human mycoses and anticancer activities, have been investigated. However, there are still several crucial issues in the research on drimenol, such as the lack of experimental understanding of its pharmacokinetics, bioavailability, and toxicity. By synthesizing current research findings, this review aims to present a holistic understanding of drimenol, paving the way for future studies and its potential utilization in diverse fields. Full article

Skin, the largest organ of the human body, accounts for protecting against external injuries and pathogens. Despite possessing inherent self-regeneration capabilities, the repair of skin lesions is a complex and time-consuming process yet vital to preserving its critical physiological functions. The dominant treatment involves the application of a dressing to protect the wound, mitigate the risk of infection, and decrease the likelihood of secondary injuries. Pursuing solutions for accelerating wound healing has resulted in groundbreaking advancements in materials science, from hydrogels and hydrocolloids to foams and micro-/nanofibers. Noting the convenience and flexibility in design, nanofibers merit a high surface-area-to-volume ratio, controlled release of therapeutics, mimicking of the extracellular matrix, and excellent mechanical properties. Core-shell nanofibers bring even further prospects to the realm of wound dressings upon separate compartments with independent functionality, adapted release profiles of bioactive agents, and better moisture management. In this review, we highlight core-shell nanofibers for wound dressing applications featuring a survey on common materials and synthesis methods. Our discussion embodies the wound healing process, optimal wound dressing characteristics, the current organic and inorganic material repertoire for multifunctional core-shell nanofibers, and common techniques to fabricate proper coaxial structures. We also provide an overview of antibacterial nanomaterials with an emphasis on their crystalline structures, properties, and functions. We conclude with an outlook for the potential offered by core-shell nanofibers toward a more advanced design for effective wound healing. Full article

Sphaerococcenol A is a cytotoxic bromoditerpene biosynthesized by the red alga Sphaerococcus coronopifolius. A series of its analogues (1–6) was designed and semi-synthesized using thiol-Michael additions and enone reduction, and the structures of these analogues were characterized by spectroscopic methods. Cytotoxic analyses (1–100 µM; 24 h) were accomplished on A549, DU-145, and MCF-7 cells. The six novel sphaerococcenol A analogues displayed an IC₅₀ range between 14.31 and 70.11 µM on A549, DU-145, and MCF-7 malignant cells. Compound 1, resulting from the chemical addition of 4-methoxybenzenethiol, exhibited the smallest IC₅₀ values on the A549 (18.70 µM) and DU-145 (15.82 µM) cell lines, and compound 3, resulting from the chemical addition of propanethiol, exhibited the smallest IC₅₀ value (14.31 µM) on MCF-7 cells. The highest IC₅₀ values were exhibited by compound 4, suggesting that the chemical addition of benzylthiol led to a loss of cytotoxic activity. The remaining chemical modifications were not able to potentiate the cytotoxicity of the original compounds. Regarding A549 cell viability, analogue 1 exhibited a marked effect on mitochondrial function, which was accompanied by an increase in ROS levels, Caspase-3 activation, and DNA fragmentation and condensation. This study opens new avenues for research by exploring sphaerococcenol A as a scaffold for the synthesis of novel bioactive molecules. Full article

Accessing plant resources to extract compounds of interest can sometimes be challenging. To facilitate access and limit the environmental impact, innovative cultivation strategies can be developed. Forskolin is a molecule of high interest, mainly found in the roots of Coleus forskohlii. The aim of this study was to develop aeroponic cultivation methods to provide a local source of Coleus forskohlii and to study the impact of abiotic stress on forskolin and bioactive metabolite production. Three cultivation itineraries (LED lighting, biostimulant, and hydric stress) along with a control itinerary were established. The forskolin content in the plant roots was quantified using HPLC-ELSD, and the results showed that LED treatment proved to be the most promising, increasing root biomass and the total forskolin content recovered at the end of the cultivation period threefold (710.1 ± 21.3 mg vs. 229.9 ± 17.7 mg). Statistical analysis comparing the LED itinerary to the control itinerary identified stress-affected metabolites, showing that LEDs positively influence mainly the concentration of phenolic compounds in the roots and diterpenes in the aerial parts of Coleus forskohlii. Moreover, to better define the phytochemical composition of Coleus forskohlii cultivated in France using aeroponic cultivation, an untargeted metabolomic analysis was conducted using UHPLC-HRMS/MS analysis and molecular networks on both the root and aerial parts. This study demonstrates that aeroponic cultivation, especially with the application of an LED treatment, could be a very promising alternative for a local source of Coleus forskohlii leading to easy access to the roots and aerial parts rich in forskolin and other bioactive compounds. Full article

Many naturally occurring chemical metabolites with significant cytotoxic activities have been isolated from medicinal plants and have become the leading hotspot of anti-cancer research in recent years. Hyptis rhomboidea Mart. et Gal is used as a folk medicine in South China to treat or assist in the treatment of liver disease, ulcers, and edema. But its chemical constituents have not been fully investigated yet. This study aimed to assess the cytotoxicity of H. rhomboidea, which was chemically characterized by chromatography–mass spectrometry methods. The results showed that the 95% ethanol extract of H. rhomboidea has marked inhibitory effects on five human cancer cell lines (HL-60, A549, SMMC-7721, MDA-MB-231, and SW480), with IC₅₀ values ranging from 15.8 to 40.0 μg/mL. A total of 64 compounds were identified by ultra-high-performance liquid chromatography with quadrupole time-of-flight mass spectrometry (UPLC-QTOF-MS) and gas chromatograph–mass spectroscopy (GC-MS) analysis of H. rhomboidea crude extract. Among them, kaempferol, quercetin, rosmarinic acid, squalene, and campesterol were found to be abundant and might be the major metabolites involved to its bioactivity. The cytotoxic characterization and metabolite profiling of H. rhomboidea displayed in this research provides scientific evidence to support its use as medicinal properties. Full article

This study evaluated the ability of a high-voltage electrostatic field (HVEF) treatment to extend the shelf life of tomatoes. Tomatoes were exposed to HVEF treatment for different lengths of time, and the physicochemical properties of tomatoes and bioactive compounds were monitored during 28 days of storage at 4 °C. The results indicated that the quality parameters of tomatoes were better maintained during storage by the HVEF treatment relative to the control treatment, extending their shelf life by 14–28 days. The HVEF treatment mitigated losses in firmness, weight, color changes, and bioactive substances, such as total phenolic content, total flavonoid content, ascorbic acid, and lycopene. The activity of pectin-degrading enzymes was also inhibited. The best exposure times for the HVEF treatment were 90 and 120 min. While the measured parameters decreased in both the control and HVEF treatment groups, the decrease in all of these measured parameters was significantly less (p < 0.05) in the optimum HVEF treatment groups than in the control. While the physicochemical properties may vary between different tomato varieties, the HVEF treatment of harvested tomatoes for 90 or 120 min can mitigate the degradation of quality parameters and loss of bioactive compounds incurred during the postharvest storage of tomatoes, thus maintaining their commercial value. Full article

The treatment of second-degree burn wounds presents a significant clinical challenge, often characterized by prolonged healing times and risk of complications. In this study, the wound healing potential of bioactive marine sulfated polysaccharides ulvan and carrageenan formulated in gels at concentrations of 1.5%, 5.0%, and 10% w/w was evaluated. Hairless female SKH-hr2 mice (n = 7 per treatment) with burn-inflamed skin were treated with the polysaccharide-based gels, and the therapeutic efficacy was assessed using a comprehensive array of evaluation methods, including a histopathological analysis, clinical observation, photo-documentation, an image analysis, an evaluation of biophysical skin parameters, and FT-IR spectroscopy. Our findings indicate that the 10% w/w carrageenan gel exhibited significant enhancement in wound healing, particularly in the early stages of the healing process. This was evidenced by the restoration of the α-helix structure of collagen and the configuration of glycosaminoglycans, as demonstrated by FT-IR absorption bands of the skin both in vivo and ex vivo. Furthermore, the 5% w/w ulvan gel also demonstrated notable efficacy in promoting wound healing, particularly in the later stages of the healing process. These results suggest that carrageenan and ulvan gels hold promise for improving the efficiency of wound healing in second-degree burn wounds. Our study contributes to the understanding of the therapeutic potential of marine polysaccharides and provides insights into their mechanism of action in promoting wound healing. Full article

Twelve compounds, including four undescribed cytochalasins, xylariachalasins A–D (1–4), four undescribed polyketides (5–8), and four known cytochalasins (9–12), were isolated from the mangrove endophytic fungus Xylaria arbuscula QYF. Their structures and absolute configurations were established by extensive spectroscopic analyses (1D and 2D NMR, HRESIMS), electronic circular dichroism (ECD) calculations, ¹³C NMR calculation and DP4+ analysis, single-crystal X-ray diffraction, and the modified Mosher ester method. Compounds 1 and 2 are rare cytochalasin hydroperoxides. In bioactivity assays, Compound 2 exhibited moderate antimicrobial activities against Staphylococcus aureus and Candida albicans with MIC values of 12.5 μM for both Compound 10 exhibited significant cytotoxic activity against MDA-MB-435 with an IC₅₀ value of 3.61 ± 1.60 μM. Full article

Functional ingredients rich in bioactive compounds can be added to conventional ingredients for the formulation of food to increase its nutraceutical potential. Three prickly pear parts, namely flowers, seeds, and seed cake were utilized in the current work as natural antioxidant resources. The flower extract gave the best amounts of antioxidants as estimated by spectrophotometric methods, which were 68.08 mg GAE/100 g DM for total phenolics; 6.91 mg QE/100 g DM for total flavonoids; 13.05 mg QE/100 g of DM for flavonols; and 0.22 mg/100 g of DM for condensed tannins. The three extracts showed a high proportion of antioxidant effect as determined by DPPH, ABTS, FRAP, and TAA in vitro assays. Chemical analysis and sensory testing were performed on biscuits that were made by adding powdered flowers, seeds, or seed cake. The biscuits made from the seed cake gave a higher protein content (83.97 mg/100 g) and the biscuits made from the seeds had the best ash concentration (3.21%), while the biscuits containing flower powder had the highest anti-radical activity (81.04%). Sensory analysis disclosed the preference for biscuits formulated with flowers or seeds (80%) by the experts. These findings demonstrated that the nutritional value of the biscuits was improved by their enrichment with cactus parts powders, and they were appreciated by tasters. Full article

Ulvan is a water-soluble sulfated polysaccharide extracted from the green algae cell wall. Compared with polysaccharides, oligosaccharides have drawn increasing attention in various industries due to their enhanced biocompatibility and solubility. Ulvan lyase degrades polysaccharides into low molecular weight oligosaccharides through the β-elimination mechanism. The elucidation of the structure, catalytic mechanism, and molecular modification of ulvan lyase will be helpful to obtain high value-added products from marine biomass resources, as well as reduce environmental pollution caused by the eutrophication of green algae. This review summarizes the structure and bioactivity of ulvan, the microbial origin of ulvan lyase, as well as its sequence, three-dimensional structure, and enzymatic mechanism. In addition, the molecular modification of ulvan lyase, prospects and challenges in the application of enzymatic methods to prepare oligosaccharides are also discussed. It provides information for the preparation of bioactive Ulva oligosaccharides through enzymatic hydrolysis, the technological bottlenecks, and possible solutions to address these issues within the enzymatic process. Full article

Flax (Linum usitatissimum L.) is an important crop plant with pharmaceutical significance. It is described in pharmacopoeias (the United States Pharmacopeia and the European Pharmacopoeia), which confirms that it (especially the seeds) is a valuable medicinal product. Similar to flax seeds, which accumulate bioactive compounds, flax in vitro cultures are also a rich source of flavonoids, phenolics, lignans and neolignans. In the present study, flax suspension cultures after treatment of the non-pathogenic Fusarium oxysporum strain Fo47 were established and analyzed. The study examined the suitability of Fo47 as an elicitor in flax suspension cultures and provided interesting data on the impact of these endophytic fungi on plant metabolism and physiology. Two flax cultivars (Bukoz and Nike) and two compositions of media for flax callus liquid cultures were tested. Biochemical analysis revealed enhanced levels of secondary metabolites (total flavonoid and total phenolic content) and photosynthetically active pigments in the flax callus cultures after treatment with the non-pathogenic fungal strain F. oxysporum Fo47 when compared to control, untreated cultures. In cultures with the selected, optimized conditions, FTIR analysis was performed and revealed changes in the structural properties of cell wall polymers after elicitation of cultures with F. oxysporum Fo47. The plant cell wall polymers were more strongly bound, and the crystallinity index (Icr) of cellulose was higher than in control, untreated samples. However, lignin and pectin levels were lower in the flax callus liquid cultures treated with the non-pathogenic strain of Fusarium when compared to the untreated control. The potential application of the non-pathogenic strain of F. oxysporum for enhancing the synthesis of desired secondary metabolites in plant tissue cultures is discussed. Full article