Search Results (352)

This study optimized supercritical fluid extraction (SC-CO₂) parameters for Boswellia sacra leaves to evaluate how extraction thermodynamics influence subsequent pharmacological bioactivity. Using a multi-parametric approach, extracts obtained at 40 °C and 80 °C (100 bar) were profiled via HPLC-DAD and evaluated using in vitro antimicrobial, pancreatic lipase inhibition, and Caco-2 cell antiproliferative assays. HPLC analysis revealed that the 40 °C threshold preserved chemical diversity (17 active peaks, retaining higher caffeic acid and rutin concentrations), whereas 80 °C conditions caused severe compound degradation. Consequently, the 40 °C extracts exhibited significantly enhanced biomedical potencies over the 80 °C variants, demonstrating superior microbiostatic activity against Gram-positive bacteria and Candida albicans (MIC = 15.62 µg/mL), stronger porcine pancreatic lipase inhibition (IC₅₀ = 17.21 µg/mL), and greater antiproliferative efficacy against human colorectal adenocarcinoma cells (IC₅₀ = 109.47 µg/mL). Ultimately, maintaining low thermal thresholds during green extraction is critical to preserving the integrated polyphenolic architecture of B. sacra required for multi-targeted antimicrobial, anti-obesity, and anticancer therapeutics. Full article

Background: Staphylococcus aureus is a major cause of life-threatening infections, and increasing antimicrobial resistance necessitates alternative therapeutic strategies. This study evaluated the antiquorum sensing and antivirulence activities of selected nonsteroidal anti-inflammatory drugs (NSAIDs) against S. aureus clinical isolates by targeting the accessory gene regulator (agr). Methods: Antimicrobial susceptibility and virulence factor production were evaluated in 56 S. aureus clinical isolates. The MICs of six NSAIDs (Diclofenac, ketoprofen, ketorolac, meloxicam, indomethacin and celecoxib) were determined by broth microdilution, and the effects of sub-MICs (½ and ¼ MIC) on virulence factors were assessed. The expression of agrA, hlb, and hld was analyzed by qRT-PCR, and molecular docking was performed to evaluate interactions with AgrA receptor. Results: Among the isolates, high resistance rates were accompanied with cefoxitin, ceftazidime, and cefepime. Hemolysin, protease, and lipase production were detected in 42.86%, 89.28%, and 94.64% of isolates, respectively. Meloxicam and celecoxib at sub-MIC levels significantly reduced hemolysin, protease, and lipase activities. Additionally, both drugs markedly downregulated agrA expression by 88.9–95.3% and significantly reduced hlb and hld expression by 90.5–99.9% without affecting bacterial growth. Molecular docking demonstrated favorable binding interactions with AgrA. Conclusions: Meloxicam and celecoxib could be promising adjunctive therapies against S. aureus through suppression of the Agr-regulated virulence traits. Full article

Elizabethkingia species have emerged as important nosocomial pathogens associated with multidrug resistance and persistent infections. This study aimed to characterize clinical Elizabethkingia isolates from Northern Thailand regarding antimicrobial susceptibility, virulence-associated phenotypes, and biofilm formation, and to evaluate the antimicrobial and anti-biofilm activity of dialdehyde cellulose (DAC) film. A total of 49 clinical isolates were identified by MALDI-TOF mass spectrometry, with species identification confirmed by 16S rRNA gene sequencing. Antimicrobial susceptibility was determined against 12 agents. Virulence traits (protease, lipase, lecithinase, and hemolysin production) and biofilm formation were assessed using standard phenotypic assays. DAC films were evaluated against selected resistant isolates. Elizabethkingia anophelis predominated, and most isolates exhibited multidrug or extensive drug resistance, with high resistance to carbapenems and cephalosporins. Piperacillin–tazobactam, levofloxacin, and trimethoprim–sulfamethoxazole showed the greatest activity. All isolates demonstrated protease production and time-dependent hemolysis, while lipase and lecithinase activities were absent. Biofilm formation varied among isolates, while DAC films inhibited bacterial growth and prevented detectable biofilm formation in the tested isolates. No significant difference was observed between DAC and DAC supplemented with meropenem in inhibition zone diameters (p = 0.555). Clinical Elizabethkingia isolates demonstrated extensive antimicrobial resistance with conserved virulence traits and heterogeneous biofilm formation. DAC films demonstrated antimicrobial activity and prevented detectable biofilm formation under the experimental conditions. Further studies are warranted to evaluate their mechanism of action and potential applications. Full article

Monoacylglycerol lipase (MAGL) is a key enzyme at the interface between the endocannabinoid system and lipid metabolism, playing a pivotal role in the hydrolysis of the endocannabinoid 2-arachidonoylglycerol and in the regulation of lipid mediators involved in inflammation, pain, neurodegeneration and cancer. Owing to its therapeutic relevance, MAGL has emerged as an attractive pharmacological target, stimulating extensive research efforts aimed at the development of potent and selective modulators of its activity. Advances in medicinal chemistry, together with the increasing application of innovative computational approaches and biochemical methods to assess MAGL activity, have significantly expanded the chemical space of compounds capable of modulating this enzyme. This review provides a comprehensive overview of selective MAGL modulators reported in the scientific literature from 2020 to the present, excluding compounds described exclusively in patent literature and MAGL probes, as this area has been recently reviewed elsewhere, ranging from classical enzyme inhibitors to modulators acting through alternative strategies, such as targeted protein degradation. Overall, this review highlights the structural diversity and the main strategies that have emerged in recent years in modulating MAGL and it aims to guide the rational design of next-generation MAGL-targeting agents. Full article

Many bioactive constituents of medicinal plants depend on microbial biotransformation for their pharmacological activity, positioning postbiotics from plant substrates as microbially matured phytomedicines. An emerging framework integrates prebiotic phytochemicals with probiotic strains to modulate gut microbiota and host health. In this study, we explored the functional properties of heat-inactivated Lactobacillus strains following the fermentation of oligosaccharides obtained from sesame hulls (Sesamum indicum L.), underutilised agro-industrial residues. Cell-wall oligosaccharides were obtained by alkaline or enzymatic (Celluclast^® 1.5 L (Novonesis, Copenhagen, Denmark)) extraction with Ultraflo^® L (Novonesis, Copenhagen, Denmark) hydrolysis and fermented with Lactobacillus acidophilus, L. casei, or L. paracasei. Heat-inactivated pre-postbiotic preparations were profiled for antioxidant capacity, inhibition of metabolic enzymes implicated in obesity and type 2 diabetes, and anti-Helicobacter pylori urease activity. Moreover, these preparations were incorporated into a barley malt (Hordeum vulgare L.) beverage. Bioactivity was strain- and substrate-dependent: L. casei-derived postbiotics most strongly inhibited pancreatic lipase (47.82%) and α-glucosidase (52.14%); L. acidophilus most strongly inhibited α-amylase (43.67%); and L. paracasei exhibited the strongest urease inhibition (20.66%). All strains displayed enhanced antioxidant activity, with ABTS scavenging reaching 87.02%. The supplemented beverages improved antioxidant activity by ~20%. The fermentation of these oligosaccharides thus yields a microbially matured phytomedicine with multi-target activity, supporting postbiotics as active mediators of plant-based therapeutics. Full article

Background: Kidney disorders are strongly related to metabolic disturbances, including obesity and type 2 diabetes. Excessive intake of sugar and saturated fats promotes lipid accumulation, cellular energy issues and inflammatory responses. Cannabigerol (CBG), a non-psychotropic phytocannabinoid, has recently gained attention for its metabolic, anti-inflammatory and potential protective properties. Methods: The present study investigated the effect of two weeks of CBG administration (last 14 days of the experiment) on fatty acid (FA) composition, FA metabolic pathways and FA transporters in rats subjected to a high-fat high-sucrose diet (HFHS) for 6 weeks. Male Wistar rats were divided into four groups: Control, CBG, HFHS, and HFHS+CBG. Kidney tissue and urine samples were analyzed by gas–liquid chromatography (GLC) for lipid fractions and FA profiles, while protein expression of FA transporters and metabolic enzymes was assessed by immunoblotting. Polysaccharides and collagen fibers were visualized using Periodic Acid-Schiff (PAS) and AZAN staining, respectively. ELISA and colorimetric kits were used to measure urinary albumin and creatinine contents. Results: HFHS feeding altered renal lipid homeostasis, increasing saturated and monounsaturated fatty acids (SFA and MUFA, respectively) levels and affecting desaturation and elongation ratios. CBG supplementation affected renal lipid metabolism by lowering triacylglycerol (TAG) accumulation, restoring polyunsaturated fatty acids (PUFA) in phospholipid (PL) and altering FA ratios, suggesting an improvement in lipid balance. CBG also increased the expression of carnitine palmitoyltransferase 1 (CPT1) and lipoprotein lipase (LPL) and decreased the expression of stearoyl-CoA desaturase 1 (SCD1) and fatty acid synthase (FAS), suggesting a shift toward enhanced FA oxidation and reduced lipogenesis. Conclusions: Overall, CBG exerted good effects on renal lipid metabolism and may mitigate early lipid-mediated injury associated with metabolic kidney disorders. Full article

Background/Objectives: Red beetroot (Beta vulgaris L.) is recognized for its antioxidant, anti-inflammatory, and metabolic properties. This study evaluated the effects of two beetroot cultivars (Boldor and Wodan) on blood serum parameters, body composition, and organ weights in male WKY rats fed a low-protein diet (LPD, 8.8% protein). Methods: Five-week-old male rats were maintained on an LPD for 8 weeks and subsequently continued on the LPD diet supplemented with 4% dried beetroot for 45 days. The experimental diets included beetroot from the Boldor and Wodan cultivars, either treated or untreated with a plant growth stimulator during cultivation. Results: Foliar application of the selenium-based plant growth stimulator did not significantly increase selenium or other element concentrations in beet roots. Elemental analysis showed higher levels of Fe, Zn, Cu, Cr, Pb, As, Cd, and Sb in the Wodan group, while Boldor increased Cr, Pb, and As; Ni and Se remained unchanged. Beetroot supplementation significantly affected 14 of the 30 measured biochemical parameters, including biomarkers of liver function (ALT, ALP, total bilirubin, albumin, and total protein), renal function (uric acid), pancreatic activity (amylase and lipase), electrolyte balance (sodium, potassium, and chloride), mineral metabolism (calcium), inflammatory status (CRP), and nutritional metabolism (iron). Conversely, no significant effects were observed on lipid profile parameters or biomarkers of cardiac and skeletal muscle injury. Among the beetroot cultivars evaluated, Wodan exerted distinct effects relative to Boldor, resulting in higher circulating total bilirubin and potassium concentrations, alongside reduced uric acid and lipase levels in treated rats. Boldor supplementation significantly increased body weight gain and fat mass, with a trend toward higher lean mass, and increased kidney weight. Wodan did not significantly affect body weight but increased kidney and spleen mass. Feed intake was similar across groups. No changes in cardiovascular function were observed ex vivo. Conclusions: Beetroot supplementation modulated multiple metabolic and physiological biomarkers in rats fed a low-protein diet, with distinct cultivar-specific effects, underscoring the importance of cultivar selection for optimizing functional dietary interventions. Full article

Severe acute pancreatitis (SAP) is a life-threatening inflammatory disorder characterized by high mortality and limited therapeutic options. Alginate oligosaccharide (AOS), a marine-derived bioactive polysaccharide, exhibits prebiotic, anti-inflammatory and antioxidant properties that are effective against various inflammatory diseases. In this study, a mouse model of SAP was established by intraperitoneal injection of cerulein (100 μg/kg) and lipopolysaccharide (5 mg/kg), and the mice were pretreated with AOS (200 mg/kg) by gavage for 4 consecutive weeks to explore the potential protective efficacy and underlying mechanisms. The results shown that AOS attenuated the severity of SAP, as evidenced by reduced serum amylase and lipase levels, as well as alleviated histopathological injury in both pancreatic and ileal tissues. AOS suppressed the overproduction of pro-inflammatory cytokines (IL-1β, IL-6, TNF-α) in serum, pancreas, and ileum at protein or mRNA levels. Moreover, AOS effectively diminished pancreatic and ileal inflammatory infiltration and oxidative stress in SAP mice, accompanied by inhibited the TLR4/MyD88/NF-κB pathway and activated the Nrf2/HO-1 antioxidant axis. Furthermore, AOS restored intestinal barrier integrity, as manifested by upregulated expression of tight junction proteins (claudin-1, occludin, ZO-1), reduced serum diamine oxidase, and decreased bacterial translocation from the gut to the pancreas. It was revealed by 16S rRNA sequencing that AOS ameliorated SAP-induced gut dysbiosis by restoring microbial diversity, normalizing the Firmicutes/Bacteroidetes ratio, enriching beneficial genera (Lactobacillus, Blautia), and enhancing cecal short-chain fatty acid (acetic, propionic, butyric acid) production. Collectively, our findings demonstrate that AOS exerts comprehensive protective effects against SAP through suppression of inflammatory signaling and oxidative stress, as well as restoring gut homeostasis. These results suggest that AOS may serve as a promising prebiotic-based nutritional strategy for the management of SAP. Full article

Obesity and its metabolic complications represent a major global health challenge, and food-derived bioactive peptides are emerging as promising dietary interventions. In this study, two hemp seed protein-derived tetrapeptides with pancreatic lipase (PL) and cholesterol esterase (CE) inhibitory activity, APAM and RLPA, were co-administered with a high-fat diet (HFD) to male C57BL/6J mice at 25 and 100 mg/kg body weight for 10 weeks. Both peptides dose-dependently alleviated HFD-induced body weight gain, visceral fat accumulation, hepatic steatosis, dyslipidemia, hyperglycemia, and systemic inflammation. Mechanistically, both peptides inhibited intestinal PL and CE activities and enhanced fecal lipid excretion, supporting direct suppression of intestinal fat digestion. 16S rRNA gene sequencing revealed partial restoration of HFD-disrupted gut microbiota, with APAM preferentially enriching Bifidobacterium and Roseburia, while RLPA promoted Akkermansia and Lactobacillus, accompanied by differential improvements in fecal short-chain fatty acid (SCFA) profiles. Hepatic transcriptomics identified the PPAR signaling pathway as a shared regulatory hub, and multi-omics integration revealed significant correlations linking gut microbiota, SCFA production, hepatic gene expression, and metabolic phenotypes. These findings suggest a dual-pathway anti-obesity mechanism integrating intestinal lipid digestion inhibition with gut–liver axis modulation, and highlight hemp seed protein-derived peptides as potential functional food ingredients for obesity prevention. Full article

In this study, 20% ethanol elution fraction(PC-20), 40% ethanol elution fraction(PC-40), 60% ethanol elution fraction(PC-60), and 80% ethanol elution fraction (PC-80)of Penthorum chinense polyphenols were obtained using AB-8 macroporous resin . Their in vitro bioactivities were compared to explore potential applications. A comprehensive phytochemical analysis identified 85 compounds, including 16 phenolic acids, 36 flavonoids, 24 hydrolyzed tannins, 7 anthocyanins, and 2 others. The results showed clear ethanol concentration-dependent variations in both compound composition and bioactivity. PC-20 had the highest levels of total polyphenols (418.45 mg/g), proanthocyanidins (84.95 mg/g), and tannins (10.61 mg/g), and also showed the best antioxidant capacity. PC-40 contained the most flavonoids (227.55 mg/g). PC-60 gave the strongest α-glucosidase inhibition (IC₅₀ = 0.79 µg/mL), while PC-20 was most effective against pancreatic lipase (IC₅₀ = 101.06 µg/mL) and also significantly activated the enzymes ADH and ALDH. Overall, PC-20 appears more suitable for applications aimed at antioxidant, anti-obesity, or liver-protective effects, whereas PC-60 is more promising for blood glucose control. This work provides a practical basis for selecting different ethanol fractions of P. chinense polyphenols according to specific functional needs. Full article

Phyllanthus emblica L. is a nutraceutically important medicinal plant; however, the relationship between genetic variation and bioactive potential remains poorly understood. This study integrates genome-wide SNP analysis, phytochemical profiling, and functional bioassays to investigate cross-scale differentiation among fourteen cultivars. Genotyping-by-sequencing (GBS) identified 5644 high-quality SNPs from an initial dataset of 9018 SNPs, revealing moderate but structured genomic divergence (0.0275–0.0845). Phytochemical analysis of five commercial cultivars demonstrated significant variation (p < 0.05) in total phenolic content (6.58–15.53 mg GAE/gDW) and tannin content (284.52–333.81 mg TAE/gDW). Functional assays revealed strong anti-obesity potential, with crude extracts exhibiting superior α-glucosidase inhibition (up to 98.75%), while tannin-enriched extracts showed enhanced pancreatic lipase inhibition (up to 46.26%). Importantly, enzyme inhibition did not correlate directly with total phenolic or tannin content, indicating compound-specific bioactivity. LC-MS/QTOF analysis identified flavonoids (e.g., quercetin and kaempferol), phenolic acids, and other candidate metabolites potentially associated with enzyme inhibitory activity. These findings demonstrate a non-proportional association among genomic variation, metabolite composition, and functional bioactivity, suggesting that bioactivity may be influenced more strongly by compound-specific metabolite composition than by genome-wide similarity alone. Full article

Histamine is a significant risk factor in brown fishmeal and negatively affects histamine-sensitive fish species. The present study aimed to explore the potential protective effects of dietary sanguinarine supplementation against the adverse impacts of excessive dietary histamine on growth and intestinal and hepatic health in American eels. Four experimental diets were formulated: the basal diet (control diet), the basal diet supplemented with 500 mg kg⁻¹ of histamine (HH diet), and the HH diet supplemented with 100 mg kg⁻¹ and 200 mg kg⁻¹ of sanguinarine (HH+SAN100 and HH+SAN200 diets, respectively). After a 10-week feeding trial, both sanguinarine supplementation diets alleviated HH-diet-induced growth retardation, reduced feed utilization, serum dyslipidemia, and hepatic and intestinal structural damage; decreased hepatic and intestinal antioxidant capacity; increased intestinal and hepatic malondialdehyde levels; inhibited intestinal lipase activities; elevated intestinal pro-inflammatory-related gene abundance; and lowered intestinal anti-inflammatory-related gene expression. Furthermore, the HH+SAN100 diet partially ameliorated HH-diet-induced gut microbiota dysbiosis and intestinal metabolic disturbances. Collectively, these findings identify sanguinarine as a functional dietary additive that mitigates histamine-associated growth suppression and intestinal and hepatic injury in American eels, promoting the sustainable utilization of brown fishmeal in American eel culture. Full article

Guava (Psidium guajava L.) processing produces peels, seeds, and residual pulp. Previous studies have shown that this fraction contains a significant amount of bioactive molecules (more than in the pulp), such as phenolic compounds, which have demonstrated health-beneficial bioactivities, including antioxidant, anti-obesogenic, and antihyperlipidemic activities, among others. In this study, we aimed to characterize total phenolic compounds, total flavonoids, the phenolic profile, and the in vitro antioxidant and antihyperlipidemic properties of guava byproduct extracts, which were evaluated for their potential use as functional ingredients. Phenolic analysis indicated the total phenolic content (46.45 mg GAE/g), the total flavonoid content (3.86 mg CE/g), and contents of individual phenolic compounds, namely ellagic, syringic, rutin, luteolin, and kaempferol. The extracts showed good antioxidant activity (236.22, 344.89, and 387.1 µmol TE/100 g for TEAC, DPPH, and FRAP, respectively). Moreover, the extracts could bind bile acids (18.50–40.34%) and reduce cholesterol solubility in artificial micelles (53.0–67.6%). Modest pancreatic lipase inhibition (33.33%), stronger cholesterol esterase inhibitory activities (60.22%), and mild HMG-CoA inhibitory potential (16.90%) were recorded. Guava processing byproducts demonstrate the potential to be considered as value-added ingredients in functional foods. Full article

Candida albicans is a yeast found in the oral cavity, gastrointestinal tract, and vaginal mucosa. This species is the most prevalent and virulent in conditions such as oral candidiasis. Myrtenol is a bicyclic monoterpene alcohol recognized for its antioxidant and anti-inflammatory attributes. Its primary source is the essential oil extracted from plants of the Myrtaceae family. This study evaluated the effect of (−)-myrtenol on the virulence factors of Candida albicans. Ten clinical isolates of Candida albicans and one reference strain (ATCC 90028) were used in this study. The virulence factors examined included adhesion, morphogenesis, and lipase production. Assays were conducted in the presence and absence of (−)-myrtenol, using a concentration corresponding to the minimum inhibitory concentration (MIC; 256 µg/mL). Results: The compound reduced the adherence of C. albicans to human oral epithelial cells (92.24 vs. 28.69), and reduced filamentation in liquid (3.17 vs. 2.57) and solid media. Furthermore, (−)-myrtenol inhibited lipase activity (0.68 vs. 1.00). Virulence factors expressed by C. albicans contribute to increased infection rates and, consequently, increased morbidity and mortality. The present findings demonstrate that (−)-myrtenol affects virulence-associated phenotypes of C. albicans in vitro. This compound represents a promising candidate for further investigation, particularly in studies addressing its mechanisms of action, safety, and potential applicability. Full article

Background: This study investigated the effects of increasing levels of salinity on leaf phytochemical composition and the antioxidant, antidiabetic, and anti-obesity activities. Method: Three quinoa accessions grown under escalating NaCl treatments had their leaves exposed to various chemical analyses. Polyphenols, tannins, and flavonoids were among the phenolic substances whose concentrations were measured. The phenolic chemicals in the water extract were identified using HPLC-DAD-ESI-MS/MS. In vitro and in silico methods were used to measure anti-radical (DPPH), anti-alpha glucosidase, anti-alpha-amylase, and anti-lipase activities. Results: The results showed that water and ethanol, due to their polarity, were the most effective solvents for extracting phenolic compounds. Additionally, salt application led to a dose-dependent increase in total phenols (TPC), flavonoids (TFC), and tannins (CT) across all accessions. The accession DE-1 exhibited the highest contents with average values of 1453.03–4398.36 mg EGA/100 g DW, 322.7–1090.7 mg CAE/100 g DW, and 77.9–335.96 mg CAE/100 g DW of TPC, TFC, and Tannins, respectively. HPLC-ESI-DAD-MS/MS profiling of phenolic compounds led to identifying 18 constituents, including five major compounds (p-coumaric acid, caffeic acid, vanillic acid, p-coumaroyl hexose, and HHDP-galloyl glucose). Except for p-coumaroyl hexose and HHDP-galloyl glucose, which were extensively biosynthesized/accumulated in the salt-tolerant accession DE-1, the remaining phenolic compounds showed irregular evolution depending on accession and salt concentration. Moreover, ethanol and water extracts were evaluated for their anti-radical and enzyme-inhibitory activities. Conclusion: Salt-stressed DE-1 water extract showed strong antioxidant and enzyme inhibitory activities, indicating potential antidiabetic and anti-obesity effects. These activities were confirmed by in silico analysis. Full article