Search Results (16,680)

Allicin, as a natural antibacterial active substance from plants, has great medical and health care value. However, due to its poor stability, its application in the field of food and medicine is limited. So, in this paper, allicin–zein–sodium caseinate composite nanoparticles (zein–Ali–SC) were prepared by antisolvent precipitation and electrostatic deposition. Through the analysis of the particle size, ζ-potential, encapsulation efficiency (EE), loading rate (LC) and microstructure, the optimum preparation conditions for composite nanoparticles were obtained. The mechanism of its formation was studied by fluorescence spectrum, Fourier infrared spectrum (FTIR), X-ray diffraction (XRD) and thermogravimetric analysis (TGA). The stability study results showed that the particle size of composite nanoparticles was less than 200 nm and its PDI was less than 0.3 under different NaCl concentrations and heating conditions, showing good stability. When stored at 4 °C for 21 days, the retention rate of allicin reached 61.67%, which was 52.9% higher than that of free allicin. After freeze-drying and reheating, the nanoparticles showed good redispersibility; meanwhile, antioxidant experiments showed that, compared with free allicin, the nanoparticles had stronger scavenging ability of free radicals, which provided a new idea for improving the stability technology and bioavailability of bioactive compounds. Full article

Diabetes-related ulcers and slow-healing wounds pose a significant health risk to individuals due to their uncertain causes. Mortality rates for diabetes foot ulcers (DFUs) range from 10% after 16 months to 24% after five years. The use of bioactive phytochemicals can play a key role in healing wounds in a predictable time. Recent literature has demonstrated that various natural substances, including flavonoids, saponins, phenolic compounds, and polysaccharides, play key roles at different stages of the wound-healing process through diverse mechanisms. These studies have categorized the compounds according to their characteristics, bioactivities, and modes of action. In this study, we evaluated the role of natural compounds derived from plant sources that have been shown to play a crucial role in immunomodulation. Macrophages are closely involved in immunomodulation within the wound microenvironment and are key players in efferocytosis, inflammation resolution, and tissue regeneration, all of which contribute to successful wound healing. Phytochemicals and their derivatives have shown capabilities in immune regulation, including macrophage migration, nitric oxide synthase inhibition, lymphocyte and T-cell stimulation, cytokine activation, natural killer cell enhancement, and the regulation of NF-κβ, TNF-α, and apoptosis. In this review, we have studied the role of phytochemicals in immunomodulation for the resolution of diabetic wound inflammation. Full article

The use of nutraceuticals, mainly phytogenics, is increasingly widespread in animal nutrition, especially in dogs. The materials typically used to provide these very diverse natural compounds come from plants, but lately algae and fungi have also been used. In animal nutrition, these compounds are applied to obtain better results in the production and stability of feed and also as biofunctional substances with benefits for animal health. Polyphenols are natural compounds from the secondary metabolism of plant matter present in animal food (e.g., seeds and nuts, fruits, vegetables, herbs/aromatic plants, spices, cereals, and vegetable oils, among others). Most of the biological effects of these compounds associated with health benefits have been attributed to their antioxidant potential because they can protect cellular elements against oxidative injury, reducing the risk of dysfunctions and diseases associated with oxidative processes. Polyphenols are constituted by multiple families of substances with wide applications in pet therapy and nutrition. In this work, we review the most relevant phytogenic polyphenols, exploring their characteristics, sources, and implications for canine health. Our focus includes the effects on gastrointestinal functions and its microbiota, as well as aspects such as obesity, diabetes, and fat metabolism. Additionally, we examine their impact on cardiovascular, neurological, and immunological systems, along with their potential anti-oncogenic role. Finally, we discuss the overall role of polyphenols in dog diets and their future implications. Full article

Abstract: Natural bioactives are mixtures of compounds extracted from plants with physicochemical properties that are usually not favorable for penetrating the skin`s complex barrier. Nanoparticles have important advantages both in dermatology and cosmetology: improved solubility and stability of encapsulated phytocompounds, controlled and sustained skin delivery, and enhanced skin permeation, leading to an improved bioavailability. This review focuses on two generations of lipid-based nanoparticles: solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs). An extensive overview on the recent studies on SLNs and NLCs entrapping essential oils, oils, herbal extracts, and phytocompounds for topical applications is presented, emphasizing their composition, physicochemical characterization, efficacy, and methodologies used to evaluate them. This review also summarizes topical systems containing natural bioactives incorporated into SLNs and NLCs, commercially available products and registered patents in the field. SLNs and NLCs turn out to be effective nanocarriers for skin applications, offering significantly improved encapsulation efficiency, stability, and bioactives delivery. However, their full potential is underexplored. Future applications should study the encapsulation potential of new natural bioactives and show more specialized solutions that address specific requirements; an improved product performance and a pleasant sensory profile could lead to increased customer compliance with the product use. Full article

Meat is known for its high perishability and short shelf life if not properly packaged or stored. Packaging materials play a crucial role in preserving food quality, and there is a growing demand from consumers, industry professionals, and researchers for natural packaging materials that incorporate health-beneficial extracts. Additionally, there is an increasing emphasis on avoiding non-biodegradable plastics in order to reduce environmental pollution. Currently used polymers in food packaging typically feature properties such as oxygen barriers, moisture resistance, and oxidation inhibition, helping to prevent undesirable aromas, flavors, and colors in food. Packaging not only serves as a container for transportation but also prevents physical damage, maintains quality, and ensures food safety. In the pursuit of more sustainable solutions, various compounds are being explored for food packaging, including those derived from proteins, lipids, waxes, and polysaccharides. These materials can be combined with bioactive compounds, such as natural plant extracts, which provide antioxidant, antimicrobial, anti-inflammatory, and anticancer benefits. Different techniques, such as electrohydrodynamic processes and casting methods, are employed in the preparation of these packaging materials. This review highlights the applications and properties of polymers used in meat packaging and promotes the use of biodegradable materials as a viable solution to reduce environmental pollution. Full article

To investigate the characteristics and sources of volatile organic compounds (VOCs) as well as their impacts on secondary organic aerosols (SOAs) formation during high-incidence periods of PM_2.5 pollution, a field measurement was conducted in December 2019 in Hefei, a typical city of the Yangtze River Delta (YRD). During the whole process, the mixing ratios of VOCs were averaged as 21.1 ± 15.9 ppb, with alkanes, alkenes, alkyne, and aromatics accounting for 59.9%, 15.3%, 15.0%, and 9.8% of the total VOCs, respectively. It is worth noting that the contributions of alkenes and alkyne increased significantly during PM_2.5 pollution periods. Based on source apportionment via the positive matrix factorization (PMF) model, vehicle emissions, liquefied petroleum gas/natural gas (LPG/NG), and biomass/coal burning were the main sources of VOCs during the research in Hefei. During pollution periods, however, the contribution of biomass/coal burning to VOCs increased significantly, reaching as much as 47.6%. The calculated SOA formation potential (SOAFP) of VOCs was 0.38 ± 1.04 µg m⁻³ (range: 0.04–7.30 µg m⁻³), and aromatics were the dominant contributors, with a percentage of 96.8%. The source contributions showed that industrial emissions (49.1%) and vehicle emissions (28.3%) contributed the most to SOAFP during non-pollution periods, whereas the contribution of biomass/coal burning to SOA formation increased significantly (32.8%) during PM_2.5 pollution periods. These findings suggest that reducing VOCs emissions from biomass/coal burning, vehicle, and industrial sources is a crucial approach for the effective control of SOA formation in Hefei, which provides a scientific basis for controlling PM_2.5 pollution and improving air quality in the YRD region. Full article

The search for synergies between natural products and commercial antibiotics is a promising strategy against bacterial resistance. This study determined the antimicrobial capacity of Nerol (NE) and Tannic Acid (TA) against 14 pathogenic bacteria, including ESKAPE pathogens. TA exhibited the lowest Minimum Inhibitory Concentrations (MICs) at 162.5 µg/mL against Pasteurella aerogenes and 187.5 µg/mL against Acinetobacter baumannii (WHO priority 1). NE showed its lowest MIC of 500 µg/mL against both Pasteurella aerogenes and Salmonella enterica. A total of 35 combinations of NE and 13 of TA with eight commercial antibiotics were analyzed. For NE, combinations with Streptomycin and Gentamicin were effective against Salmonella enterica, Bacillus subtilis, and Streptococcus agalactiae, with antibiotic MIC reductions between 75.0 and 87.5%. TA showed six synergies with Chloramphenicol, Ampicillin, Erythromycin, and Streptomycin against Acinetobacter baumannii, Streptococcus agalactiae, and Pasteurella aerogenes, with MIC reductions between 75.0 and 93.7%. Additionally, 31 additive effects with antibiotics for NE and 8 for TA were found. Kinetic studies on these synergies showed complete inhibition of bacterial growth, suggesting that natural products enhance antibiotics by facilitating their access to targets or preventing resistance. Given their safety profiles recognized by the EPA and FDA, these natural products could be promising candidates as antibiotic enhancers. Full article

Essential oils (EOs) from various medicinal and aromatic plants are known for their diverse biological activities, including their antimicrobial effects. Citrus aurantium EO is traditionally used for therapeutic benefits due to its high content of bioactive compounds. Therefore, this study focuses on its potential use as a food preservative by investigating the combined antibacterial properties of EOs from leaves (EO1), flowers (EO2), and small branches (EO3) of Citrus aurantium against six bacterial strains by the agar disk diffusion, minimum inhibitory concentration (MIC), and minimum bactericidal concentration (MBC) methods. The chemical compositions of the EOs were analysed by gas chromatography–mass spectrometry (GC-MS) and revealed the presence of numerous compounds responsible for their antimicrobial properties. The MIC values for the EOs were 3.12 mg/mL, 4.23 mg/mL, and 1.89 mg/mL, for EO1, EO2 and EO3, respectively, while the MBC values were 12.5 mg/mL, 6.25 mg/mL, and 6.25 mg/mL, respectively. A simplex centroid design was created to analyse the effect of the individual and combined EOs against E. coli. The combined EOs showed enhanced antibacterial activity compared to the individual oils, suggesting a synergistic effect (e.g., trial 9 with an MIC of 0.21 mg/mL), allowing the use of lower EO concentrations and reducing potential negative effects on food flavour and aroma. Additionally, the practical application of investigated EOs (at concentrations twice the MIC) was investigated in raw chicken meat stored at 4 °C for 21 days. The EOs, individually and in combination, effectively extended the shelf life of the meat by inhibiting bacterial growth (total bacterial count of less than 1 × 10⁴ CFU/g in the treated samples compared to 7 × 10⁷ CFU/g in the control on day 21 of storage). The study underlines the potential of C. aurantium EOs as natural preservatives that represent a sustainable and effective alternative to synthetic chemicals in food preservation. Full article

Onychomycosis is a common fungal infection that affects the nails and accounts for approximately 50% of all nail diseases. The main pathogens involved include dermatophytes, such as Trichophyton rubrum, members of the T. mentagrophytes complex, and emerging pathogens in this infection, T. schoenleinii and T. tonsurans. Tea tree (Melaleuca alternifolia Cheel) essential oil (EO) has been proposed as a promising natural alternative to traditional treatments due to its antimicrobial properties. Among its more than 100 compounds, terpinen-4-ol is one of the main contributors to the antifungal action of this EO. To determine the antifungal activity of tea tree EO against dermatophytes, we designed an in vitro study using EUCAST-AFST protocols to obtain the values of MIC (minimum inhibitory concentration) and MFC (minimum fungicidal concentration) of several commercial M. alternifolia Cheel EOs against three species of dermatophytes isolated from clinical samples with suspected toenail onychomycosis. The results showed that the microorganism most sensitive to the action of the EO was T. rubrum, which had an MIC value more than 13 times lower than the value obtained for T. schoenleinii (0.4% v/v), the most resistant isolate. No differences in antifungal activity were observed by the analysed EOs or between the MIC and MFC values. These in vitro results suggest that tea tree EO is a viable option for the alternative treatment of onychomycosis, although clinical studies are needed to confirm the long-term antifungal activity, safety and efficacy of the oils studied in a clinical context. Full article

Developing bio-based and biodegradable materials has become important to meet current market demands, government regulations, and environmental concerns. The packaging industry, particularly for food and beverages, is known to be the world’s largest consumer of plastics. Therefore, the demand for sustainable alternatives in this area is needed to meet the industry’s requirements. This review presents the most commonly used bio-based and biodegradable packaging materials, bio-polyesters, and polysaccharide-based polymers. At the same time, a major problem in food packaging is presented: fungal growth and, consequently, food spoilage. Different types of antifungal compounds, both natural and synthetic, are explained in terms of structure and mechanism of action. The main uses of these antifungal compounds and their degree of effectiveness are detailed. State-of-the-art studies have shown a clear trend of increasing studies on incorporating antifungals in biodegradable materials since 2000. The bibliometric networks showed studies on active packaging, biodegradable polymers, films, antimicrobial and antifungal activities, essential oils, starch and polysaccharides, nanocomposites, and nanoparticles. The combination of the development of bio-based and biodegradable materials with the ability to control fungal growth promotes both sustainability and the innovative enhancement of the packaging sector. Full article

Seagrass meadows consist of angiosperms that thrive fully submerged in marine environments and form distinct ecosystems. They provide essential support for many organisms, acting as nursery grounds for species of economic importance. Beyond their ecological roles, seagrasses and their associated microbiomes are rich sources of bioactive compounds with the potential to address numerous human healthcare challenges. Seagrasses produce bioactive molecules responding to physical, chemical, and biological environmental changes. These activities can treat microbe-borne diseases, skin diseases, diabetes, muscle pain, helminthic diseases, and wounds. Seagrasses also offer potential secondary metabolites that can be used for societal benefits. Despite numerous results on their presence and bioactive derivatives, only a few studies have explored the functional and therapeutic properties of secondary metabolites from seagrass. With the increasing spread of epidemics and pandemics worldwide, the demand for alternative drug sources and drug discovery has become an indispensable area of research. Seagrasses present a reliable natural source, making this an opportune moment for further exploration of their pharmacological activities with minimal side effects. This review provides a comprehensive overview of the biochemical, phytochemical, and biomedical applications of seagrasses globally over the last two decades, highlighting the prospective areas of future research for identifying biomedical applications. Full article

The emergence of multidrug-resistant fungi Candida auris is a worldwide health crisis connected with high rates of mortality. There is a critical need to find novel and unique antifungal compounds for treating infections of multidrug-resistant fungi such as C. auris. This study aimed to illustrate that biosynthetic gene clusters in native bacterial isolates are able to produce antifungal compounds against the multidrug-resistant fungus C. auris. It was successfully achieved using large-scale antifungal activity screening, cytotoxicity analysis, and whole genome sequencing integrated with genome mining-guided analysis and liquid chromatography–mass spectrometry (LC/MS). A list of possible gene candidates was initially identified with genome mining methods to predict secondary metabolite gene clusters of antifungal-compound-producing bacteria. Then, gene clusters present in the antifungal-compound-producing bacteria were identified and aligned with the reference genome using comparative genomic approaches. Bacillus halotolerans AQ11M9 was identified through large-scale antifungal activity screening as a natural compound-producer against multidrug-resistant C. auris, while it was nontoxic to normal human skin fibroblast cells (confirmed using a cell viability assay). The genome (4,197,347 bp) of B. halotolerans AQ11M9 with 2931 predicted genes was first mined for detecting and characterizing biosynthetic gene clusters, which revealed 10 candidate regions with antifungal activity. Clusters of AQ11M9 encoded non-ribosomal peptide synthase (NRPS) (bacilysin, bacillibactin, paenibactin, surfactin, plipastin, and fengycin) and polyketide (macrobrevin). The presence of gene clusters with anti-C. auris activity, and surfactin identified through LC/MS, from AQ11M9 suggests the potential of utilizing it as a source for a novel and powerful anti-C. auris compound. Full article

Objectives: Pharmacokinetic issues were the leading cause of drug attrition, accounting for approximately 40% of all cases before the turn of the century. To this end, several high-throughput in vitro assays like microsomal stability have been developed to evaluate the pharmacokinetic profiles of compounds in the early stages of drug discovery. At NCATS, a single-point rat liver microsomal (RLM) stability assay is used as a Tier I assay, while human liver microsomal (HLM) stability is employed as a Tier II assay. We experimentally screened and collected data on over 30,000 compounds for RLM stability and over 7000 compounds for HLM stability. Although HLM stability screening provides valuable insights, the increasing number of hits generated, along with the time- and resource-intensive nature of the assay, highlights the need for alternative strategies. One promising approach is leveraging in silico models trained on these experimental datasets. Methods: We describe the development of an HLM stability prediction model using our in-house HLM stability dataset. Results: Employing both classical machine learning methods and advanced techniques, such as neural networks, we achieved model accuracies exceeding 80%. Moreover, we validated our model using external test sets and found that our models are comparable to some of the best models in literature. Additionally, the strong correlation observed between our RLM and HLM data was further reinforced by the fact that our HLM model performance improved when using RLM stability predictions as an input descriptor. Conclusions: The best model along with a subset of our dataset (PubChem AID: 1963597) has been made publicly accessible on the ADME@NCATS website for the benefit of the greater drug discovery community. To the best of our knowledge, it is the largest open-source model of its kind and the first to leverage cross-species data. Full article

Xanthohumol (1) is a major prenylated flavonoid in hops (Humulus lupulus L.) which exhibits a broad spectrum of health-promoting and therapeutic activities, including anti-inflammatory, antioxidant, antimicrobial, and anticancer effects. However, due to its lipophilic nature, it is poorly soluble in water and barely absorbed from the gastrointestinal tract, which greatly limits its therapeutic potential. One method of increasing the solubility of active compounds is their conjugation to polar molecules, such as sugars. Sugar moiety introduced into the flavonoid molecule significantly increases polarity, which results in better water solubility and often leads to greater bioavailability. Entomopathogenic fungi are well known for their ability to catalyze O-glycosylation reactions. Therefore, we investigated the ability of selected entomopathogenic filamentous fungi to biotransform xanthohumol (1). As a result of the experiments, one aglycone (2) and five glycosides (3–7) were obtained. The obtained (2″E)-4″-hydroxyxanthohumol 4′-O-β-D-(4‴-O-methyl)-glucopyranoside (5) has never been described in the literature so far. Interestingly, in addition to the expected glycosylation reactions, the tested fungi also catalyzed chalcone–flavanone cyclization reactions, which demonstrates chalcone isomerase-like activity, an enzyme typically found in plants. All these findings undoubtedly indicate that entomopathogenic filamentous fungi are still an underexploited pool of novel enzymes. Full article

Lung cancer is among the most clinically challenging tumors because of its aggressive proliferation, metastasis, and the presence of cancer stem cells (CSCs). Natural bioactive substances have been used for cancer prevention, and, in particular, resveratrol (RSV), a stilbene-based compound with wide biological properties, has been proposed for chemoprevention. Its lesser-known analogue 4,4’-dihydroxy-trans-stilbene (DHS) has demonstrated superior activity both in cell-based assays and in mouse and zebrafish in vivo models. The present study analyzed the effects of DHS and RSV on A549 lung cancer cells, with a particular focus on stemness features and CSCs, isolated by sorting of the side population (SP). The results show that both stilbenes, especially DHS, strongly inhibited cell cycle progression. A reduction in the S phase was induced by DHS, whereas an increase in this phase was obtained with RSV. In addition, 50% reductions in the clonogenicity and soft agar colony formation were observed with the DHS treatment only. Finally, both stilbenes, especially DHS, reduced stemness marker expression in A549 cells and their sorted SP fraction. Spheroid formation, higher in SP cells than in the main population (MP), was significantly reduced after pretreatment with DHS, which was found to decrease SOX2 levels more than RSV. These findings indicate that stilbenes, and particularly DHS, affect stemness features of A549 cells and the SP fraction, suggesting their potential utility as anticancer agents, either alone or combined with chemotherapeutic drugs. Full article