Search Results (8,622)

Leaves of Cucumis callosus, traditionally employed in Ayurvedic medicine for the treatment of urinary disorders, were investigated in depth for their therapeutic potential against bacterially induced urinary tract infection (UTI) for the first time. The present work is the first to explore the antibacterial activity of C. callosus leaf fractions with an integrative in silico, in vitro, and in vivo approach. Through bioassay-guided fractionation, the chloroform fraction (F1) was identified as the most active, exhibiting potent activity against Uropathogenic Escherichia spp. species. Liquid chromatography–mass spectrometry (LC-MS) analysis of F1 revealed the presence of bioactive compounds, including stigmasterol, 1,2,3,4-tetrahydroisoquinoline, lactose, hydroxy(mesityl)acetic acid, and 2,4-di-tert-butylphenol. Molecular docking studies validated the strong binding affinities of these compounds for bacterial resistance enzymes, including AmpC β-lactamase and carbapenemases, thereby providing plausible mechanisms of antimicrobial action. In vivo studies carried out on female rats infected with Escherichia spp. species revealed a dose-dependent reduction in bacterial load, with a significant decrease in urinary tract inflammation upon F1 administration. Histopathological evaluation confirmed the protective effect, with reduced epithelial damage and inflammation in bladder tissues. These findings indicate significant antibacterial and tissue-protective effects of the C. callosus leaf fraction F1, supporting its ethnomedicinal use and establishing it as a promising phytotherapeutic agent for the treatment of urinary tract infections. Full article

Steroidal compounds lie at the crossroads of inflammation and cancer, where modulation of common signaling pathways creates opportunities for dual-action therapeutic intervention. Accumulating evidence indicates that their anti-inflammatory and antitumor activities are frequently interconnected, reflecting shared molecular mechanisms that regulate immune signaling, oxidative stress, cell proliferation, and apoptosis. This review provides a critical and comparative analysis of major classes of bioactive steroids—including furanosteroids, neo-steroids, aromatic steroids, α,β-epoxy steroids, peroxy steroids, cyanosteroids, nitro- and epithio steroids, halogenated steroids (fluorinated, chlorinated, brominated, iodinated), and steroid phosphate esters—with emphasis on their dual anti-inflammatory and anticancer potential. More than one thousand steroidal metabolites derived from plants, fungi, marine organisms, bacteria, and synthetic sources are surveyed. While the majority exhibit either anti-inflammatory or antineoplastic activity alone, only a limited subset displays potent activity in both domains. Comparative evaluation highlights the structural features that favor dual functionality, including epoxide, peroxide, nitrile, nitro, halogen, and phosphate ester moieties, as well as rearranged or heteroatom-enriched steroidal frameworks. Where available, biological data from in vitro and in vivo assays (IC₅₀ values, enzyme inhibition, cytokine modulation, and antiproliferative effects) are summarized and critically compared. Special attention is given to rare natural metabolites—such as polyhalogenated marine steroids, phosphorylated sterols, and heteroatom-containing derivatives—as well as synthetic analogues designed to enhance cytotoxic or immunomodulatory efficacy. Mechanistically, steroids exhibiting dual activity commonly modulate convergent signaling pathways, including NF-κB, JAK/STAT, MAPK, PI3K/AKT, redox homeostasis, and apoptosis regulation. Collectively, these findings underscore the potential of structurally optimized steroids as multifunctional therapeutic agents and provide a framework for the rational design of next-generation anti-inflammatory and anticancer drugs. Full article

Background/Objectives: This retrospective study evaluated and compared the cephalometric effects of an elastodontic bioactivator and conventional high-pull headgear in growing patients with hyperdivergent Class II malocclusion. Methods: Patients aged 7–11 years were divided into two groups according to the appliance used for the orthodontic treatment performed: elastodontic device (ED) and high-pull headgear (HPHD). Cephalometric measurements were recorded at baseline (T0) and after 18 months of treatment (T1). The data were subjected to statistical analysis, descriptive statistics were calculated, and an ANOVA test and post hoc Tukey test were performed (repeated measures correction was applied for intragroup comparisons). Linear regressions were conducted. Significance was predetermined as p < 0.05 for all the tests performed. Results: 40 patients were included, 20 belonging to the ED group and 20 to the HPHD group. Both groups showed a significant increase in SNB (p < 0.05), suggesting favorable mandibular positional changes. SNA and ANB did not show significant intra- or intergroup variations (p > 0.05). Regarding vertical skeletal parameters, no significant intra- or intergroup changes were observed at T0 and T1, indicating that both devices preserved vertical stability without worsening the hyperdivergent pattern. Dentoalveolar and soft-tissue effects were limited. Conclusions: Both ED and HPHD are effective in managing hyperdivergent Class II growing patients. The two appliances provide comparable improvements in mandibular positioning. Both devices seem to preserve vertical skeletal dimensions, avoiding further mandibular clockwise rotation. Both appliances are associated with minimal undesirable effects on the soft tissues. Full article

Eugenia pyriformis Cambess., popularly known as uvaia, is a native Brazilian species belonging to the Myrtaceae family that has attracted pharmacological interest due to its richness in bioactive secondary metabolites. Previous studies have reported antimicrobial and antioxidant activities of the essential oil obtained from its leaves, reinforcing its therapeutic potential. In this context, the present study aimed to extract and characterize the essential oil from E. pyriformis leaves cultivated in the mountainous region of Rio de Janeiro, Brazil, and to evaluate its anti-inflammatory potential through in vitro and in vivo models. Gas chromatography mass spectrometry (GC–MS) analysis revealed a predominance of sesquiterpene hydrocarbons, mainly γ-muurolene, δ-cadinene, and β-caryophyllene. The oil exhibited significant anti-edematogenic activity in carrageenan-, prostaglandin E₂-, and bradykinin-induced paw edema models in adult female Swiss mice, suggesting modulation of inflammatory mediators, possibly through inhibition of the cyclooxygenase (COX) pathway. Conversely, no effect was observed in the compound 48/80-induced model, indicating the absence of activity on histamine- and serotonin-mediated processes. In vitro assays demonstrated that the oil reduced TNF-α and IL-1β gene expression in RAW 264.7 macrophages, confirming its ability to modulate pro-inflammatory cytokines. Taken together, these findings demonstrate that the essential oil of E. pyriformis exerts anti-inflammatory activity through multiple targets. Full article

Sustainable strategies for revalorizing food industry by-products are increasingly relevant in the development of modern experimental dermato-cosmetic formulations. In this study, two semisolid cosmetic creams (R10 and EM-R10) were designed using recycled palm oil—physically purified after intensive frying—as the lipid phase. The recycled oil was incorporated strictly within a controlled experimental framework and does not imply cosmetic-grade regulatory compliance. The formulations incorporated distinct bioactive profiles: R10 combined apricot and pineapple extracts with lime essential oil, while EM-R10 integrated fir bud and green tea extracts alongside the same essential oil. Both preparations contained Fragard as a preservative and niacinamide and panthenol as vitaminic components. The physicochemical properties of the formulations were assessed through rheology, confocal microscopy, ATR-FTIR, SEM, DSC, and contact angle measurements. Antimicrobial activity was evaluated against Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, and Candida albicans using disk diffusion and broth microdilution assays. The results demonstrate that, despite partial thermal degradation, recycled palm oil retains modified structural features that influence formulation-related properties relevant to topical systems. EM-R10 showed superior spreadability, adhesion, stability, and diffusion-related performance, as well as improved antimicrobial activity, within the investigated experimental conditions, highlighting recycled palm oil as a promising sustainable lipid phase for experimental dermato-cosmetic formulations, pending further purification, toxicological evaluation, and regulatory compliance assessment. Full article

Background/Objectives: Watermelon (Citrullus lanatus) processing generates substantial quantities of rind, seeds, and residual pulp that are typically discarded despite being rich in polyunsaturated fatty acids, polar lipids, carotenoids, and phenolic compounds. These amphiphilic bioactives are increasingly recognized for their roles in modulating oxidative stress, inflammation, and platelet activation; however, the lipid fraction of watermelon by-products remains insufficiently characterized. This study examined organic watermelon juice and its by-products to isolate, characterize, and evaluate extracts enriched in amphiphilic and lipophilic bioactives, with emphasis on their in vitro antioxidant, anti-inflammatory, and antithrombotic properties. Methods: total lipids were extracted using a modified Bligh–Dyer method and fractionated into total amphiphilic compounds (TAC) and total lipophilic compounds (TLC) via counter-current distribution. Phenolic and carotenoid levels were quantified, and antioxidant capacity was assessed using DPPH, ABTS, and FRAP assays. Anti-platelet and anti-inflammatory activities were evaluated against ADP- and PAF-induced platelet aggregation. Structural characterization of polar lipids was performed using ATR–FTIR, and LC–MS was used to determine fatty acid composition and phospholipid structures. Results and Discussion: Carotenoids were primarily concentrated in the TLC fractions with high ABTS values for antioxidant activity, while phenolics mostly in the juice, the TACs of which showed the strongest total antioxidant capacity based on DPPH. TAC fractions of both samples showed also higher FRAP values of antioxidant activity, likely due to greater phenolic content. TAC extracts also exhibited notable inhibition of PAF- and ADP-induced platelet aggregation, associated with their enriched ω-3 PUFA profiles and favorable ω-6/ω-3 ratios based on their LC-MS profiles. Conclusions: Overall, watermelon products (juice) and by-products represent a valuable and sustainable source of amphiphilic bioactives with significant antioxidant, anti-inflammatory, and anti-platelet potential, supporting their future use in functional foods, nutraceuticals, and cosmetic applications. Full article

Pomegranate is valued for its abundant polyphenolic content and its capacity to promote health. In this study, pomegranate juice or pericarp extracts from two Mediterranean regions (Montenegro and Italy) were systematically and comparatively evaluated for the first time with respect to their polyphenolic composition, antioxidant capacity, and antimicrobial activity. The extraction of juice extracts was accomplished by means of the Kutscher–Steudel liquid–liquid extraction technique, which was employed to selectively recover phenolics. In contrast, the extraction of pericarp extracts from the solid matrix was achieved via Soxhlet extraction. A thorough high-performance liquid chromatography (HPLC) analysis was conducted to identify and quantify the major phenolic compounds present in the sample. This analysis revealed the presence of ellagitannin punicalagin isomers, with concentrations reaching up to 254.75 mg/g of the sample, as well as ellagic acid and gallic acid. The antioxidant potential of the samples was assessed using the antioxidant activity index (AAI) from the 2,2-diphenyl-1-picrylhydrazyl (DPPH) test and by a ferric reducing antioxidant power (FRAP) assay. Juice extracts demonstrated a range of activity levels, with AAI values ranging from 0.17 to 2.12 and FRAP values ranging from 2.49 to 19.41 mmol Fe²⁺/g. In contrast, pericarp extracts exhibited notably higher activity, with AAI values ranging from 0.18 to 27.57 and FRAP values ranging from 2.99 to 372.17 mmol Fe²⁺/g. This study demonstrates the markedly higher functional potential of pericarp extracts compared to juice extracts by linking detailed phenolic profiles with bioactivity data. Antimicrobial testing, inclusive of the determination of minimum bactericidal concentration (MBC), demonstrated that certain pericarp extracts manifested bactericidal properties at low concentrations against selected clinically pertinent strains, including methicillin-resistant Staphylococcus aureus (0.109% p/v), methicillin-sensitive S. aureus (0.109% p/v), carbapenem-resistant Acinetobacter baumannii (0.109% p/v), and Escherichia coli (0.563% p/v). Candida albicans and Klebsiella pneumoniae strains exhibited minimal sensitivity to these extracts. The findings indicate that pomegranate pericarp is a valuable by-product, and they demonstrate the potential of both juice and pericarp extracts as functional ingredients. Full article

Background and Objectives: Procalcitonin (PCT), presepsin (PSEP), interferon-λ3 (IFN-λ3), and bioactive adrenomedullin (bio-ADM) are promising sepsis biomarkers. We explored the clinical utility of a multi-marker approach using these four biomarkers in patients with suspected sepsis. Materials and Methods: In a total of 248 patients, the biomarkers were evaluated with the sequential organ failure assessment (SOFA) score. Receiver operating characteristic curves with area under the curve (AUC) were analyzed to diagnose sepsis and predict in-hospital mortality. Survival and reclassification analyses were also used to predict in-hospital mortality. Results: The four biomarkers showed comparable diagnostic performance (AUC = 0.61–0.95, p < 0.001–0.003), and sepsis proportion increased significantly as the number of biomarkers used in the multi-marker approach increased (7.7–91.7%, p < 0.001). The proportion of biomarker quartiles (Q1–Q4) differed significantly according to SOFA score (p < 0.001). The four biomarkers predicted in-hospital mortality (AUC = 0.63–0.84, p < 0.001–0.004). The multi-marker approach performed better than the SOFA score (mortality rate, 58.3% vs. 31.3%; adjusted hazard ratio [HR], 14.7 vs. 4.6), and the addition of biomarkers to the SOFA score increased the performance. The multi-marker approach resulted in a higher HR in patients aged ≥75 years than in the overall population (9.2 vs. 4.2). Conclusions: Each biomarker showed clinical utility in patients with suspected sepsis. The multi-marker approach showed complementary clinical utility in addition to the SOFA score and better prognostic performance in patients aged ≥75 years. The use of biomarkers, alone or in combination, would be a valuable tool in combination with the SOFA score. Full article

Cow’s milk, urine, dung, ghee, and curd possess significant medicinal value in Ayurveda and have been integral to traditional Indian clinical practices for centuries. The cow-derived fermented product (CDFP), a formulation rooted in Ayurvedic tradition, combines these five components as a panchgavya and is believed to offer multifaceted health benefits. In this preliminary single-subject case study, we evaluated the microbial composition of CDFP itself and assessed its effects on the human gut microbiome before and after 7 and 15 days of administration. A single healthy male subject consumed CDFP daily for seven consecutive days. Using 16S rRNA metagenomic sequencing, we observed a prominent increase in gut microbial diversity and a rise in beneficial bacterial genera such as Bifidobacterium, Faecalibacterium, and Akkermansia during and after treatment. Functional profiling revealed significant enhancements in pathways associated with amino acid metabolism, vitamin biosynthesis (e.g., folate, riboflavin), and energy metabolism, along with transient boosts in secondary metabolite synthesis. Metabolomic analysis identified 171 bioactive compounds within CDFP, with 33 exhibiting interactions with human proteins involved in immune modulation, oxidative stress response, and gut barrier integrity. Although conducted on a single participant, this study is the first to elucidate the distinct changes observed in gut microbial composition and function following the seven-day CDFP regimen and provides initial insights that warrant further investigation in larger, controlled studies. These findings highlight the potential of CDFP as a microbiota-targeted intervention with health-supportive properties. Full article

Antimicrobial resistance (AMR) is a major global health concern, which complicates treatment of microbial infections and wounds. Conventional therapies are no longer effective against drug resistant microbes; hence, novel antimicrobial approaches are urgently required. Silver nanoparticles (AgNPs) offer stronger antimicrobial activity, and in situ synthesis improves stability, uniformity, cost efficiency, and bioactivity while minimising contamination. These features make AgNPs well-suited for incorporation into textiles and wound dressings. Red wine extract (RW-E), rich in antioxidant and anti-inflammatory compounds was used to hydrothermally synthesise RW-AgNPs and RW-AgNPs-loaded on cotton (RWALC) by optimising pH and RW-E concentration. Characterisation was performed using UV–Vis spectroscopy, dynamic light scattering (DLS), and High Resolution and Scanning electron microscopy (HR-TEM and SEM). Antibacterial activities were evaluated against human pathogens through agar disc diffusion assay for RWALC and microdilution assay for RW-AgNPs. RWALC showed higher potency against both Gram-negative and Gram-positive bacteria, with inhibition zones of 12.33 ± 1.15 to 23.5 ± 5.15 mm, that surpassed those of ciprofloxacin (10 ± 3 to 19.17 ± 1.39 mm at 10 μg/mL). RW-AgNPs exhibited low minimum inhibitory concentrations (MIC: 0.195–3.125 μg/mL) and minimum bactericidal concentrations (MBC: 0.78–6.25 μg/mL). Preincubation with β-mercaptoethanol (β-ME) inhibited the antibacterial activity of RWALC, suggesting that thiolated molecules are involved in AgNPs-mediated effects. This study demonstrated that green-synthesised RW-AgNPs, incorporated in situ into cotton, conferred strong antibacterial properties, warranting further investigation into their mechanisms of action. Full article

Fungal secondary metabolites are valuable sources of natural antioxidants and antimicrobials. This study evaluated the submerged fermentation of Penicillium crustosum OR889307 supplemented with lemon peel as a co-substrate to enhance the production of bioactive compounds. Lemon peel was selected for its phenolic precursors and sustainable availability as an agro-industrial byproduct. Crude extracts, aqueous and organic fractions, and molecular-weight partitions were assessed for antioxidant activity using the DPPH assay and for antimicrobial activity against Escherichia coli, Staphylococcus aureus, methicillin-resistant S. aureus (MRSA), Pseudomonas aeruginosa, and Candida albicans. Semi-purified extracts from co-substrate fermentations exhibited enhanced bioactivity, showing MIC values of 185 µg/mL against P. aeruginosa and 225 µg/mL against MRSA, along with strong ABTS radical-scavenging capacity (238.95 ± 2.17 µmol TE). RP-HPLC-ESI-MS profiling revealed phenolic acids, flavanones, flavonols, and lignans, including ferulic acid 4-O-glucoside, bisdemethoxycurcumin, secoisolariciresinol, and quercetin 3-O-xylosyl-glucuronide. These findings demonstrate that lemon peel supplementation promotes the biosynthesis of antimicrobial and antioxidant metabolites by P. crustosum. This approach supports sustainable agro-waste valorization and offers a promising strategy for obtaining natural bioactive compounds with potential applications in food preservation and health-related formulations. Full article

Capsicum pubescens (rocoto) is an Andean domesticate with notable agronomic and nutraceutical potential, yet it remains underrepresented in chili pepper breeding programs. In this study, 78 accessions from the Peruvian Andes were evaluated in a single field environment during the 2024 growing season for 28 variables spanning plant architecture, phenology and yield, color (CIELAB), weight, fruit morphology, physicochemical variables, and functional phytochemicals, including total phenolics, carotenoids, ascorbic acid, capsaicinoids, and antioxidant activity (FRAP, DPPH, ABTS). Descriptive analyses revealed broad phenotypic diversity in key variables such as yield and bioactive compounds. Spearman correlations uncovered a clear modular structure, with strong within-domain associations across morphological, chromatic, and biochemical variables, and statistically significant but low-magnitude cross-domain associations (e.g., fruit length with pungency, redness with total phenolics). Principal component analysis and hierarchical clustering resolved three differentiated phenotypic profiles: (i) low-pungency accessions with high soluble solids and varied fruit colors; (ii) highly pungent materials with elevated antioxidant capacity; and (iii) large, red-fruited accessions with considerable carotenoid content and high moisture. This multivariate architecture revealed weak cross-block correlations among agronomic, color, and functional traits, enabling selection of promising accessions combining desirable agronomic attributes and favorable bioactive profiles in specific accessions. These results provide a quantitative foundation for future breeding strategies in C. pubescens, opening concrete opportunities to develop improved cultivars that simultaneously meet productivity and functional quality criteria. Full article

This study evaluates the chemical profile and antifungal efficacy of essential oils from Piper glabratum, Piper friedrichsthalii, and Piper cumanense against the cocoa pathogens Moniliophthora roreri and Phytophthora palmivora. Microwave-assisted hydrodistillation followed by GC-MS analysis identified 80 constituents, predominantly monoterpenes and sesquiterpenes, which exhibited significant mycelial inhibition comparable to commercial fungicides. Beyond basic characterization, a comprehensive chemoinformatic analysis was conducted to elucidate the molecular mechanisms driving this bioactivity. The computed physicochemical landscape reveals a dominant lipophilic profile (average LogP 3.4) and low polarity (TPSA 11.5 Ų), characteristics essential for effective fungal membrane penetration. Structural mining identified conserved benzene and cyclohexene scaffolds alongside specific 1,3-benzodioxole moieties, while Maximum Common Substructure (MCS) analysis uncovered high similarity clusters among phenylpropanoids and sesquiterpenes. These findings suggest a synergistic mode of action where conserved structural backbones and interchangeable diastereomers facilitate membrane destabilization and ion leakage. Consequently, the integrative chemoinformatic profiling elucidates the molecular basis of this efficacy, positioning these Piper essential oils not merely as empirical alternatives, but as sources of rationally defined synergistic scaffolds for next-generation sustainable fungicides. Full article

To improve the oral bioavailability of oleanolic acid (OA), this study developed a menthol–fatty acid-based hydrophobic deep eutectic solvent (HDES) system. Through a comprehensive evaluation using in vitro simulated digestion and Caco-2 cell transport models, the short-chain HDES was found to increase the apparent in vitro bioavailability index of OA by 9.3-fold compared to conventional ethanol systems, with efficacy showing clear fatty acid chain-length dependence. The mechanism was systematically investigated through spectral characterization and cellular studies, revealing a two-stage enhancement process: during the digestion phase, HDES significantly improved OA bioaccessibility to 14.30% compared to 4.90% with ethanol; during the absorption phase, it markedly increased cellular uptake to 25.79% versus 4.71% with ethanol. Molecular analysis indicated that the optimal hydrophobicity and diffusion properties of HDES contributed to this enhancement. This study reveals a fatty acid chain-length-dependent mechanism in HDES-facilitated OA delivery, providing a tunable strategy for enhancing the absorption of hydrophobic bioactive compounds. Full article

This study evaluated the extraction efficiency of two Natural Deep Eutectic Solvents (NADESs), glycerol–urea (1:1) and citric acid–sorbitol (1:2), for recovering phenolic compounds from the different parts of the fruit (pulp, seed-containing pulp, seeds, and peel) of Opuntia robusta and Opuntia ficus-indica in comparison with 50% methanol. Phytochemical profiling was performed using ultra-high-performance liquid chromatography–high-resolution mass spectrometry, alongside antioxidant and enzyme inhibition assessments (acetylcholinesterase, butyrylcholinesterase, tyrosinase, α-glucosidase, and α-amylase). Glycerol–urea performed similarly to methanol in extracting phenolic compounds with notable antioxidant properties. Peel extracts contained the highest levels of bioactive compounds, particularly phenolic acids (525.49 in O. robusta and 362.96 µg/g_DW in O. ficus indica). Enzyme inhibition varied across species and fruit parts, with extracts from both species inhibiting all targeted enzymes. Notably, this study provides the first evidence of tyrosinase inhibitory activity in O. robusta, which exhibited the strongest inhibition. Overall, these results emphasize the potential of cactus fruit extracts, particularly from O. robusta, for valorization, and support the use of NADESs as a sustainable and medium for extracting antioxidant compounds. Furthermore, the potential of fruit peel as waste with nutraceutical applications was demonstrated. Full article