Search Results (2,128)

Inonotus obliquus, a medicinal mushroom valued for its bioactive compounds, has not been previously characterized from Romanian sources. This study presents the first comprehensive chemical and biological screening of I. obliquus, introducing novel polymer-based encapsulation systems to enhance the stability and bioavailability of its bioactive constituents. Two distinct delivery systems were designed to enhance the functionality of I. obliquus extracts: (i) microencapsulation in maltodextrin (MIO) and (ii) a sequential approach involving preparation of silver nanoparticle-loaded I. obliquus (IO–AgNPs), followed by microencapsulation to yield the hybrid MIO–AgNP system. Comprehensive metabolite profiling using GC–MS and ESI–QTOF–MS revealed 142 bioactive constituents, including terpenoids, flavonoids, phenolic acids, amino acids, coumarins, styrylpyrones, fatty acids, and phytosterols. Structural integrity and successful encapsulation were confirmed by XRD, FTIR, and SEM analyses. Both IO–AgNPs and MIO–AgNPs demonstrated potent antioxidant activity, significant acetylcholinesterase inhibition, and robust antimicrobial effects against Staphylococcus aureus, Bacillus cereus, Pseudomonas aeruginosa, and Escherichia coli. Cytotoxicity assays revealed pronounced activity against MCF-7, HCT116, and HeLa cell lines, with MIO–AgNPs exhibiting superior efficacy. The synergistic integration of maltodextrin and AgNPs enhanced compound stability and bioactivity. As the first report on Romanian I. obliquus, this study highlights its therapeutic potential and establishes polymer-based nanoencapsulation as an effective strategy for optimizing its applications in combating microbial resistance and cancer. Full article

Developing a rapidly gel-forming, in situ sprayable hydrogel with wound dressing functionality is essential for enhancing the wound healing process. In this study, a novel sprayable hydrogel-based wound dressing was developed by combining thermo- and pH- responsive polymers including Pluronic F127 (PF127) and N-succinyl chitosan (NSC). NSC was prepared by modifying chitosan with succinic anhydride, as confirmed by Fourier-transform infrared spectroscopy and nuclear magnetic resonance spectroscopy. The NSC synthesized using a succinic anhydride-to-chitosan molar ratio of 5:1 exhibited the highest degree of substitution, resulting in a water-soluble polymer effective over a broad pH range. The formulation process of the PF127:NSC sprayable hydrogel was optimized and evaluated based on its sol–gel phase transition behavior, clarity, gelation time, liquid and moisture management, stability, and cytotoxicity. These properties can be suitably tailored by adjusting the concentrations of PF127 and NSC. Moreover, the antioxidant capacity of the hydrogels was enhanced by incorporating Azadirachta indica (neem) extract, a bioactive compound, into the optimized sprayable hydrogel. Both neem release and antioxidant activity increased in a dose-dependent manner. Overall, the developed sprayable hydrogel exhibited favorable sprayability, appropriate gelation properties, controlled drug release, and antioxidant activity, underscoring its promising translational potential as a wound dressing. Full article

Resveratrol is a natural stilbene known for its wide range of biological activities, including antioxidant, anti-inflammatory, and anti-aging effects. However, its application in cosmetics and dermatology is limited by poor stability and bioavailability. Azelaic acid is a natural carboxylic acid employed in cosmetics for its tyrosinase inhibition activity and for cutaneous hyperpigmentation disorders. In this work, we report a concise chemoenzymatic procedure for the synthesis of a novel hybrid molecule combining acetylated resveratrol and azelaic acid. This methodology offers a valuable route for the development of new bioactive compounds for potential cosmetic and dermatological applications. Full article

The emergence of SARS-CoV-2 variants highlights the urgent need for novel therapeutic strategies, particularly entry inhibitors that could efficiently prevent viral infection. Medicinal herbs and herbal combination formulas have long been recognized for their effects in treating infectious diseases and their antiviral properties, thus providing abundant resources for the discovery of antiviral candidates. While many candidates have been suggested to have antiviral activity against SARS-CoV-2 infection, few have been validated for their mechanisms, including possible effects on viral entry. This study aimed to identify SARS-CoV-2 entry inhibitors from medicinal herbs and herbal formulas that are known for heat-clearing and detoxifying properties and/or antiviral activities. A SARS-CoV-2 pseudoparticle (SARS-CoV-2pp) system was used to assess mechanism-specific entry inhibition. Our results showed that the methanol extract of Anemarrhena asphodeloides rhizome, as well as the water extracts of Cimicifuga foetida rhizome, Xiao Chai Hu Tang (XCHT), and Sheng Ma Ge Gen Tang (SMGGT), have substantial inhibitory effects on the entry of SARS-CoV-2pps into host cells. Given the observation that Cimicifuga foetida exhibited the most potent inhibition and is a constituent of SMGGT, we further investigated the major compounds of the herb and identified caffeic acid as a bioactive component for blocking SARS-CoV-2pp entry. Entry inhibition of Cimicifuga foetida and caffeic acid was validated on both wild-type and the currently dominant JN.1 strain SARS-CoV-2pp systems. Moreover, caffeic acid was able to both inactivate the pseudoparticles and prevent their entry into pretreated host cells. The results support the traditional use of these herbal medicines and underscore their potential as valuable resources for identifying active compounds and developing therapeutic entry inhibitors for the management of COVID-19. Full article

The escalating global challenges of antimicrobial resistance (AMR) and cancer necessitate innovative therapeutic solutions from natural sources. This study investigated the multifaceted therapeutic potential of pigment-enriched plant extracts. We screened diverse plant extracts for antimicrobial and antibiofilm activity against multidrug-resistant bacteria and fungi. Hibiscus sabdariffa emerged as the most promising, demonstrating potent broad-spectrum antimicrobial and significant antibiofilm activity. Sub-inhibitory concentrations of H. sabdariffa robustly downregulated essential bacterial virulence genes and suppressed aflatoxin gene expression. Comprehensive chemical profiling via HPLC identified major anthocyanin glucosides, while GC-MS revealed diverse non-pigment bioactive compounds, including fatty acids and alcohols. Molecular docking suggested favorable interactions of key identified compounds (Cyanidin-3-O-glucoside and 1-Deoxy-d-arabitol) with E. coli outer membrane protein A (OmpA), indicating potential antiadhesive and antimicrobial mechanisms. Furthermore, H. sabdariffa exhibited selective cytotoxicity against MCF-7 breast cancer cells. These findings establish H. sabdariffa pigment-enriched extract as a highly promising, multi-functional source of novel therapeutics, highlighting its potential for simultaneously addressing drug resistance and cancer challenges through an integrated chemical, biological, and computational approach. Full article

Nudibranchs have garnered increasing interest in biomedical research due to their complex chemical defense mechanisms, many of which are derived from their diet, including sponges, cnidarians, tunicates, and algae. Their remarkable ability to sequester dietary toxins and synthesize secondary metabolites positions them as a promising source of biologically active compounds with potential therapeutic applications, particularly in oncology. This study aimed to review and summarize the available literature on the bioactive potential of nudibranch-derived compounds, focusing mainly on their antitumor properties. Although research in this area is still limited, recent studies have identified alkaloids and terpenoids isolated from species such as Dolabella auricularia, Jorunna funebris, Dendrodoris fumata, and members of the genus Phyllidia. These compounds exhibit notable cytotoxic activity against human cancer cell lines, including those from colon (HCT-116, HT-29, SW-480), lung (A549), and breast (MCF7) cancer. These findings suggest that compounds derived from nudibranchs could serve as scaffolds for the development of more effective and selective anticancer therapies. In conclusion, nudibranchs represent a valuable yet underexplored resource for antitumor drug discovery, with significant potential to contribute to the development of novel cancer treatments. Full article

The plant-based oil industry contributes significantly to food waste/by-products in the form of underutilized biomass, including oil pomace, cake/meal, seeds, peels, wastewater, etc. These waste/by-products contain a significant quantity of nutritious and bioactive compounds (phenolics, lignans, flavonoids, dietary fiber, proteins, and essential minerals) with proven health-promoting effects. The utilization of them as natural, cost-effective, and food-grade functional ingredients in novel food formulations holds considerable potential. This review highlights the potential of waste/by-products generated during plant-based oil processing as a promising source of bioactive compounds and covers systematic research, including recent studies focusing on innovative extraction and processing techniques. It also sheds light on their promising potential for valorization as food ingredients, with a focus on specific examples of food fortification. Furthermore, the potential for value creation in the food industry is emphasized, taking into account associated challenges and limitations, as well as future perspectives. Overall, the current information suggests that the valorization of plant-based oil industry waste and by-products for use in the food industry could substantially reduce malnutrition and poverty, generate favorable health outcomes, mitigate environmental concerns, and enhance economic profit in a sustainable way by developing health-promoting, environmentally sustainable food systems. Full article

The rise in multidrug-resistant bacterial strains and persistent infections such as Lyme disease caused by Borrelia burgdorferi highlights the need for novel antimicrobial agents. The present study explores the antioxidant, antibacterial, and cytotoxic properties of extracts from submerged mycelial biomass of Fomitopsis pinicola, cultivated in synthetic and lignocellulosic media. Four extracts were obtained using hot water and 80% ethanol. The provided analysis of extracts confirmed the presence of various bioactive compounds, including flavonoids, alkaloids, and polyphenols. All extracts showed dose-dependent antioxidant activity (IC₅₀: 1.9–6.7 mg/mL). Antibacterial tests revealed that Klebsiella pneumoniae was most sensitive, with the L2 extract producing the largest inhibition zone (15.33 ± 0.47 mm), while the strongest bactericidal effect was observed against Acinetobacter baumannii (MBC as low as 0.5 mg/mL for L1). Notably, all extracts significantly reduced the viability of stationary-phase B. burgdorferi cells, with L2 reducing viability to 42 ± 2% at 5 mg/mL, and decreased biofilm mass, especially with S2. Cytotoxicity assays showed minimal effects on NIH 3T3 cells, with slight toxicity in HEK 293 cells for S2 and L1. These results suggest that F. pinicola extracts, particularly ethanolic L2 and S2, may offer promising natural antimicrobial and antioxidant agents for managing resistant infections. Full article

Background/Objectives: The clinical potential of antimicrobial peptides (AMPs) against dual threats like antimicrobial resistance (AMR) and cancer is often limited by their high host cell toxicity. Here, we focused on brevinin-2OS (B2OS), a novel peptide from the skin of Odorrana schmackeri with potent haemolytic activity. The objective was to study the structure–activity relationship and optimise the safety via targeted modifications. Methods: A dual-modification strategy involving C-terminal truncation and subsequent N-terminal D-amino acid substitution was employed. The bioactivities and safety profiles of the resulting analogues were evaluated using antimicrobial, haemolysis, and cytotoxicity assays. Result: Removal of the rana box in B2OS(1-22)-NH₂ substantially reduced haemolysis while maintaining bioactivities. Remarkably, the D-leucine substitution in [D-Leu²]B2OS(1-22)-NH₂ displayed a superior HC₅₀ value of 118.1 µM, representing a more than ten-fold improvement compared to its parent peptide (HC₅₀ of 10.44 µM). This optimised analogue also demonstrated faster bactericidal kinetics and enhanced membrane permeabilisation, leading to a greater than 22-fold improvement in its therapeutic index against Gram-positive bacteria. Conclusions: The C-terminal rana box is a primary determinant of toxicity rather than a requirement for activity in the B2OS scaffold. The engineered peptide [D-Leu²]B2OS(1-22)-NH₂ emerges as a promising lead compound, and this dual-modification strategy provides a powerful design principle for developing safer, more effective peptide-based therapeutics. Full article

This study presents the development and optimization of a functional soy sauce fermented with Cordyceps militaris (C. militaris), a medicinal fungus known for its high cordycepin and polysaccharide content. Using C. militaris as the sole starter culture, the process aimed to improve both nutritional and functional properties. Response surface methodology was employed to optimize the entire fermentation process. During the koji stage, temperature, aeration, and inoculum concentration were adjusted to maximize protease activity and cordycepin production. In the fermentation stage, temperature, brine concentration, and water-to-material ratio were optimized to increase amino acid nitrogen and bioactive compound levels. Under optimal conditions (24 °C, 679.60 LPM aeration, 9.6% inoculum for koji; 32 °C, 12% brine, 1.53:1 water-to-material ratio for fermentation), the resulting soy sauce contained 1.14 ± 0.05 g/100 mL amino acid nitrogen and 16.88 ± 0.47 mg/100 mL cordycepin. Compared with traditionally fermented soy sauce, the C. militaris product exhibited a darker color, enhanced umami taste, and a distinct volatile profile featuring linoleic acid, methyl palmitate, and niacinamide. These results demonstrate the feasibility of using C. militaris in soy sauce fermentation and its potential as a novel functional condiment with improved bioactivity and sensory quality. Full article

The worldwide increase in antifungal resistance, particularly in Candida sp., requires the exploration of novel therapeutic agents. Natural compounds have been a rich source of antimicrobial molecules, where peptides constitute the class of the most bioactive components. Therefore, this study looks into the target-specific binding efficacy of insect-derived antifungal peptides (n = 37) as possible alternatives to traditional antifungal treatments. Using computational methods, namely the HPEPDOCK and HDOCK platforms, molecular docking was performed to evaluate the interactions between selected key fungal targets, lanosterol 14-demethylase, or LDM (PDB ID: 5V5Z), secreted aspartic proteinase-5, or Sap-5 (PDB ID: 2QZX), N-myristoyl transferase, or NMT (PDB ID: 1NMT), and dihydrofolate reductase, or DHFR, of C. albicans. The three-dimensional peptide structure was modelled through the PEP-FOLD 3.5 tool. Further, we predicted the physicochemical properties of these peptides through the ProtParam and PEPTIDE 2.0 tools to assess their drug-likeness and potential for therapeutic applications. In silico results show that Blap-6 from Blaps rhynchopeter and Gomesin from Acanthoscurria gomesiana have the most antifungal potential against all four targeted proteins in Candida sp. Additionally, a molecular dynamics simulation study of LDM-Blap-6 was carried out at 100 nanoseconds. The overall predictions showed that both have strong binding abilities and are good candidates for drug development. In in vitro studies, Gomesin achieved complete biofilm eradication in three out of four Candida species, while Blap-6 showed moderate but consistent reduction across all species. C. tropicalis demonstrated relative resistance to complete eradication by both peptides. The present study provides evidence to support the antifungal activity of certain insect peptides, with potential to be used as alternative drugs or as a template for a new synthetic or modified peptide in pursuit of effective therapies against Candida spp. Full article

In recent decades, the rapid expansion of the food processing industry has led to significant losses and waste, with the fruit and vegetable sector among the most affected. According to the Food and Agriculture Organization of the United Nations (FAO), losses in this category can reach up to 60%. Vegetable waste includes edible parts discarded during processing, packaging, distribution, and consumption, often comprising by-products rich in bioactive compounds such as polyphenols, carotenoids, dietary fibers, vitamins, and enzymes. The underutilization of these resources constitutes both an economic drawback and an environmental and ethical concern. Current recovery practices, including their use in animal feed or bioenergy production, contribute to a circular economy but are often limited by high operational costs. In this context, fermentation has emerged as a promising, sustainable approach for converting vegetable by-products into value-added food ingredients. This process improves digestibility, reduces undesirable compounds, and introduces probiotics beneficial to human health. The present review examines how fermentation can improve the nutritional, sensory, and functional properties of plant-based foods. By presenting several case studies, it illustrates how fermentation can effectively valorize vegetable processing by-products, supporting the development of novel, health-promoting food products with improved technological qualities. Full article

Poor solubility and bioavailability have limited the application of fucoxanthin in drug and functional food processing. In order to encapsulate fucoxanthin in delivery systems, in this study, cellulose was isolated from industrial brown algae residues and high-pressure homogenized into cellulose nanofibrils (CNFs). Then, fucoxanthin was encapsulated into the Pickering emulsion stabilized by the CNFs. The effect of high-pressure homogenization on the characteristics of cellulose and the stability of fucoxanthin emulsion was evaluated. The results indicated that CNFs prepared at 105 MPa had a diameter of 87 nm and exhibited high zeta potential and thermal stability. Encapsulation efficiency peaked at 70.8% with 1.0 mg/mL fucoxanthin, and after three freeze–thaw cycles the encapsulation efficiency was higher than 60%. The DPPH scavenging activity after 12 days’ storage at 4 °C was still 42%. Furthermore, the Pickering emulsion with 1.0 mg/mL fucoxanthin showed high stability and antioxidant activity under different pH values, salinity, temperature, and UV light exposure duration. The CNFs effectively protected fucoxanthin from degradation, offering a novel delivery system for marine bioactive compounds. To the best of our knowledge, this is the first study on the fucoxanthin delivery system of Pickering emulsion stabilized by the CNFs. Such emulsion might benefit the encapsulation and release of bioactive components in marine drugs. Full article

Skin aging is a natural biological process that can be accelerated by free radical induction, leading to a reduction in skin elasticity and the formation of wrinkles due to the depletion of elastin. Eugenia uniflora (dewandaru) is a promising plant believed to possess anti-aging properties, primarily attributed to its major constituents, myricitrin and quercetin. This study aimed to investigate the anti-elastase and antioxidant properties of Eugenia uniflora stem bark, ripe fruit, and seed extracts. Extracts were obtained using an ultrasound-assisted extraction (UAE) method with 70% ethanol. Quantitative phytochemical analysis involved measuring the total phenolic content (TPC), total flavonoid content (TFC), and antioxidant activity. Bioactive constituents were identified using LC-MS analysis, and their interactions with target enzymes were further evaluated through in silico molecular docking. The results demonstrated that the E. uniflora seed extract exhibited the highest antioxidant activity, with an IC₅₀ of 5.23 µg/mL (DPPH assay) and a FRAP value of 3233.32 µmol FeSO₄/g. Furthermore, the ethanolic seed extract showed significant anti-elastase activity with an IC₅₀ of 114.14 µg/mL. Molecular docking predicted strong potential for several compounds as pancreatic elastase inhibitors, including 5-phenylvaleric acid, 2-(3-phenylpropyl)phenol, n-amylbenzene, 2-aminoadipic acid, and traumatin, each showing a prediction activity (PA) value exceeding 0.6. Notably, these compounds also exhibited inhibitory activity against tyrosinase. These findings collectively underscore the significant promise of E. uniflora seed extract as a novel and natural candidate for pharmacocosmeceutical product development, particularly for anti-aging applications. Full article