Bioactive Effects Research Articles

The effect of quercetin and citrulline on cycling time trial performance.

There is growing interest in the use of nutrition and dietary supplements to optimize training and time-trial (TT) performance in cyclists. Separately, quercetin (QCT) and citrulline (CIT) have been used as ergogenic aids to improve oxygen (VO2) kinetics, perceived effort, and cycling TT performance. However, whether the combination of QCT and CIT can provide additive benefits and further enhance cycling performance production is currently unknown. We examined 28-days of QCT + CIT supplementation on TT performance and several performance measures (i.e. mean power, VO2, respiratory exchange ratio (RER), and rate of perceived exertion (RPE)). Forty-eight highly trained cyclists were assigned to one of four supplementation groups: (1) QCT + CIT (QCT: 500 mg, CIT: 3000 g), (2) QCT (500 mg), (3) CIT (3000 mg), or (4) placebo (3500 mg of a zero-calorie flavored crystal light package). Supplements were consumed two times per day for 28 consecutive days. Participants performed a 20-km cycling time-trial race, pre- and post-supplementation to determine the impact of the combined effects of QCT + CIT. There were no potential benefits of QCT +CIT supplementation on TT performance and several performance measures. However, there was an improvement in VO2 from pre-to-post-supplementation in QCT (p = 0.05) and CIT (p = 0.04) groups, but not in the QCT+CIT and PL groups. QCT + CIT does not seem beneficial for 20-km TT performance; further exploration with a focus on an increase in cycling duration or QCT+CIT combined with additional polyphenols may amplify any perceived bioactive or metabolic effects on cycling performance. The efficacy of QCT + CIT supplementation to improve cycling performance remains ambiguous.

Impact of Hyaluronic Acid and Other Re-Epithelializing Agents in Periodontal Regeneration: A Molecular Perspective.

This narrative review delves into the molecular mechanisms of hyaluronic acid (HA) and re-epithelializing agents in the context of periodontal regeneration. Periodontitis, characterized by chronic inflammation and the destruction of tooth-supporting tissues, presents a significant challenge in restorative dentistry. Traditional non-surgical therapies (NSPTs) sometimes fail to fully manage subgingival biofilms and could benefit from adjunctive treatments. HA, with its antibacterial, antifungal, anti-inflammatory, angiogenic, and osteoinductive properties, offers promising therapeutic potential. This review synthesizes the current literature on the bioactive effects of HA and re-epithelializing agents, such as growth factors and biomaterials, in promoting cell migration, proliferation, and extracellular matrix (ECM) synthesis. By modulating signaling pathways like the Wnt/β-catenin, TGF-β, and CD44 interaction pathways, HA enhances wound healing processes and tissue regeneration. Additionally, the role of HA in facilitating cellular crosstalk between epithelial and connective tissues is highlighted, as it impacts the inflammatory response and ECM remodeling. This review also explores the combined use of HA with growth factors and cytokines in wound healing, revealing how these agents interact synergistically to optimize periodontal regeneration. Future perspectives emphasize the need for further clinical trials to evaluate the long-term outcomes of these therapies and their potential integration into periodontal treatment paradigms.

Debittering and antioxidant improvement of soy protein hydrolysates using curcumin as hydrophobic core.

Protein hydrolysates possess various bioactive functions (e.g. antioxidant), but their bitter taste is unacceptable to most consumers. In the present study, a novel approach for debittering was introduced, which involved the utilization of a hydrophobic compound, curcumin (Cur). Soy protein hydrolysates (SPH), prepared through alcalase hydrolysis, served as the research model for this investigation. It was found that bitter intensity of SPH was dominated by the hydrophobic amino acid residues, and the addition of Cur could remarkably reduce bitterness. The debittering mechanism is attributed to the direct binding of Cur to the exposed hydrophobic amino acid residues of SPH via hydrophobic interaction, thereby shielding the hydrophobic bitter groups and hindering their interaction with the bitter taste receptors. Moreover, this debittering strategy leads to the generation of stable nanoparticles with a Cur-core/SPH-shell architecture, which can significantly improve the antioxidant capacity of SPH compared to those using biomacromolecules for encapsulation. Using curcumin as a hydrophobic core is a facile and feasible strategy with bifunction of debittering as well as improving bioactive effect of SPH, which may extend its application in foods. © 2024 Society of Chemical Industry.

Anti-Obesity Effects of Adzuki Bean Saponins in Improving Lipid Metabolism Through Reducing Oxidative Stress and Alleviating Mitochondrial Abnormality by Activating the PI3K/Akt/GSK3β/β-Catenin Signaling Pathway.

Obesity is a chronic and complex disease defined by the excessive deposition of fat and is highly associated with oxidative stress. Adzuki bean saponins (ABS) showed anti-obesity activity in our previous in vivo study; however, the active saponins of adzuki beans and potential mechanisms are still unclear. This research aims to elucidate the anti-obesity effects of ABS in improving lipid metabolism and oxidative stress, exploring the effective ingredients and potential molecular mechanisms through UHPLC-QE-MS analysis, network pharmacology, bioinformatics, and in vitro experiments both in the 3T3-L1 cell line and HepG2 cell line. The results indicate that ABS can improve intracellular lipid accumulation, adipogenesis, oxidative stress, and mitochondrial damage caused by lipid accumulation including ROS generation, abnormal mitochondrial membrane potential, and ATP disorder. Fifteen saponin components were identified with the UHPLC-QE-MS analysis. The network pharmacology and bioinformatics analyses indicated that the PI3K/Akt signaling pathway is associated with the bioactive effect of ABS. Through Western blotting and immunofluorescence analysis, the anti-obesity effect of ABS is achieved through regulation of the PI3K/Akt/GSK3β/β-catenin signaling pathway and activation of downstream transcription factor c-Myc in the lipid accumulation cell model, and regulation of β-catenin signaling and inhibition of downstream transcription factor C/EBPα in the adipocyte cell model. These results illustrate the biological activity of ABS in improving fat metabolism and oxidative stress by restoring mitochondrial function through β-catenin signaling, the PI3K/Akt/GSK3β/β-catenin signaling pathway, laying the foundation for its further development.

Symposium Review: The Impact of Fatty Acids as Bioactive Nutrients on the Development of Offspring

Fatty acids (FA) are normally considered a source of energy; however, some FA are essential nutrients with different biological functions such as ligands to membrane and nuclear receptors, and upon binding they modify cell function and transcript expression. The bioactive effects of the FA depend on the FA type and family (i.e., n-6 vs n-3). The FA effects on developmental programming have been studied in cattle and sheep with some similarities in the outcomes between species. Feeding n-3 FA during late gestation improves offspring production performance (i.e., milk yield in dairy cows and growth in beef cattle and sheep) compared with the offspring of dams supplemented with mono- and unsaturated FA or with offspring of dams with no FA supplementation. Also, there is a sexual dimorphism in the outcomes of n-3 FA supplementation, where the increase in growth due to n-3 FA seems to be more evident in males; but it might decrease growth in females. There are multiple assumptions as to how this physiological process occurs. Based on published literature, the developmental effect does not appear to be due to changes in hypothalamic regulations of dry matter intake and energy expenditure or liver and adipose tissue functions. The changes in offspring growth can be attributed to changes in gastrointestinal tract physiology, changes in immune response, or both, probably due to epigenetic changes in those tissues. Feeding n-3 FA in late gestation to the pregnant dam increases expression of amino acid transporters (mRNA and protein) in the offspring's duodenum, associated with changes in DNA methylation. Regarding immune function, the increase in offspring performance has been associated with decreased haptoglobin after weaning in calves or increases in lipid mediators, such as resolvin-D1 at birth. Omega-3 supplementation during late gestation affects offspring growth; changes in the offspring's gut and immune system biology can explain the sexual dysmorphism observed in changed body weight; however, we are unaware which of these basic mechanisms is responsible for the observed changes in biology.

A platform chemical from soybean hulls: Unveiling the bioactive effects of levoglucosenone derivatives

Soybean is one of the most extensively cultivated crops globally, and the soybean oil industry produces a significant amount of hulls annually. Utilizing this by-product to generate levoglucosenone through acid-catalyzed pyrolysis represents an environmentally friendly strategy to maximize the use of this crop and increase the value of the residue.This study explored the pyrolysis of soybean hulls to obtain the target enone and its application in the generation of new antifungal compounds. Halogenated derivatives were synthesized in a simple and straightforward manner and evaluated for antifungal activity against several Candida and Cryptococcus strains. Mechanistic studies investigated their interactions with ergosterol, impact on fungal cell wall synthesis, and inhibition of virulence factors. Biofilm formation assays were also conducted. Our results showed that the chloro derivative demonstrated the highest antifungal activity, exhibiting a remarkable minimum inhibitory concentration (MIC) and efficacy against both susceptible and resistant strains. It was also showed that the mode of action does not involve ergosterol bonding nor inhibition of cell wall synthesis. This study provides valuable insights into utilizing agricultural waste for developing bioactive compounds with pharmaceutical applications, contributing to the sustainable utilization of biomass resources in pharmaceutical research and development.

The Application of Untargeted Metabolomic Approaches for the Search of Common Bioavailable Metabolites in Human Plasma Samples from Lippia citriodora and Olea europaea Extracts.

Lippia citriodora and Olea europaea are known for their shared common bioactivities. Although both matrices are rich in similar families of bioactive compounds, their specific phytochemical compounds are mostly different. Since these compounds can be metabolized in the organism, this study hypothesized that common bioavailable metabolites may contribute to their similar bioactive effects. To test this, an acute double-blind intervention study in humans was conducted with blood samples collected at multiple time points. Using an untargeted metabolomic approach based on HPLC-ESI-QTOF-MS, 66 circulating metabolites were detected, including 9 common to both extracts, such as homovanillic acid sulfate and glucuronide derivates, hydroxytyrosol sulfate, etc. These common metabolites displayed significantly different Tmax values depending on the source, suggesting distinct metabolization pathways for each extract. The study highlights how shared bioavailable metabolites may underlie similar bioactivities observed between these two plant sources.

A One-Week Elderberry Juice Intervention Augments the Fecal Microbiota and Suggests Improvement in Glucose Tolerance and Fat Oxidation in a Randomized Controlled Trial.

Obesity is a costly and ongoing health complication in the United States and globally. Bioactive-rich foods, especially those providing polyphenols, represent an emerging and attractive strategy to address this issue. Berry-derived anthocyanins and their metabolites are of particular interest for their bioactive effects, including weight maintenance and protection from metabolic aberrations. Earlier findings from small clinical trials suggest modulation of substrate oxidation and glucose tolerance with mediation of prospective benefits attributable to the gut microbiota, but mixed results suggest appropriate anthocyanin dosing poses a challenge. The objective of this randomized, placebo-controlled study was to determine if anthocyanin-dense elderberry juice (EBJ) reproduces glucoregulatory and substrate oxidation effects observed with other berries and if this is mediated by the gut microbiota. Overweight or obese adults (BMI > 25 kg/m2) without chronic illnesses were randomized to a 5-week crossover study protocol with two 1-week periods of twice-daily EBJ or placebo (PL) separated by a washout period. Each treatment period included 4 days of controlled feeding with a 40% fat diet to allow for comparison of measurements in fecal microbiota, meal tolerance testing (MTT), and indirect calorimetry between test beverages. Eighteen study volunteers completed the study. At the phylum level, EBJ significantly increased Firmicutes and Actinobacteria, and decreased Bacteroidetes. At the genus level, EBJ increased Faecalibacterium, Ruminococcaceae, and Bifidobacterium and decreased Bacteroides and lactic acid-producing bacteria, indicating a positive response to EBJ. Supporting the changes to the microbiota, the EBJ treatment significantly reduced blood glucose following the MTT. Fat oxidation also increased significantly both during the MTT and 30 min of moderate physical activity with the EBJ treatment. Our findings confirm the bioactivity of EBJ-sourced anthocyanins on outcomes related to gut health and obesity. Follow-up investigation is needed to confirm our findings and to test for longer durations.

Bioactive Self-Polymerizing Resin with Surface Pre-Reacted Glass Ionomer Fillers for Suppressed Enamel Demineralization.

The treatment of damaged enamel surfaces involves modification of the enamel surface with artificial materials or the development of a pseudo-enamel, with research focusing on bioactive and biomimetic materials. In this study, a bioactive auto-polymerizing resin (APR) was developed by adding surface-pre-reacted glass ionomer (S-PRG) fillers of different quantities to APR. Its bioactive effects were evaluated via pH neutralization, ion release, and inhibition of enamel demineralization studies. The pH and fluoride ion release were measured using ion-specific electrodes, revealing that the APR disk with the S-PRG filler immediately neutralized the lactic acid solution (pH 4.0) through ion release. Inductively coupled plasma atomic emission spectrometry revealed that the Sr ion release peaked on the first day, with the other ions following the order F > B > Si > Al > Na, exhibiting a weekly decrease in the same order. Scanning electron microscopy was used to examine the enamel block morphology of the disks after 7 d of incubation, revealing enamel demineralization in disks without the S-PRG filler, whereas no demineralization occurred in disks with the S-PRG filler. APR containing the S-PRG filler demonstrated acid buffering suppressed enamel demineralization and bioactive properties.

Insights into inhibitory action and interaction of bisdemethoxycurcumin on tyrosinase: Spectroscopic and docking analysis

Bisdemethoxycurcumin (BDMC), a demethoxy derivative of curcumin, has garnered interest for its potential anti-tyrosinase properties, which are crucial for applications in food preservation and cosmetic industries. Despite its recognized bioactive effects, the detailed inhibitory action and interaction of BDMC on tyrosinase and its application in anti-browning processes remain unclear. This study aims to dissect the molecular interactions of BDMC with tyrosinase, elucidate its inhibition mechanism, and assess its efficacy in preventing browning, thereby underpinning its potential as a natural anti-browning agent. Employing a battery of spectroscopic techniques, we characterized the interaction of BDMC with tyrosinase. The anti-browning properties of BDMC were evaluated on fresh-cut apples, and its effect on enzymatic activities related to browning was also investigated. The results indicate that BDMC interacts with tyrosinase in a reversible mixed-type inhibition manner with an IC50 value of 12.5 ± 0.2 μM. Surface Plasmon Resonance (SPR) results indicated that BDMC presented good binding affinity toward tyrosinase. Fluorescence quenching results showed that BDMC could quench the fluorescence of tyrosinase in a static process. Synchronous fluorescence, circular dichroism spectra, and three-dimensional fluorescence results indicated that interaction of BDMC against tyrosinase resulted in changes of tyrosinase on microenvironment and conformation, thus causing decrease of tyrosinase activity. Copper-chelating results presented that BDMC could chelate to copper with stoichiometric ratio of 1: 2. Molecular docking provided intricate details of how BDMC interacted with tyrosinase. Moreover, BDMC exhibited anti-browning capability on fresh cut apples, and could regulate PPO, POD, and APX activities. The comprehensive analysis proposed in this study consolidated the theoretical basis of BDMC as a tyrosinase inhibitor and supported its potential anti-browning application.

Multifunctional Nanoemulsified Clinacanthus nutans Extract: Synergistic Anti-Pathogenic, Anti-Biofilm, Anti-Inflammatory, and Metabolic Modulation Effects against Periodontitis.

This study investigates the therapeutic potential of Clinacanthus nutans extracts, focusing on the 95% ethanol (95E) extract and its nanoemulsified form, against oral pathogens and their bioactive effects. The findings demonstrate potent antibacterial activity against Streptococcus mutans and Staphylococcus aureus, essential for combating periodontal diseases, and significant anti-biofilm properties crucial for plaque management. Additionally, the extracts exhibit promising inhibitory effects on α-glucosidase enzymes, indicating potential for diabetes management through glucose metabolism regulation. Their anti-inflammatory properties, evidenced by reduced nitric oxide production, underscore their potential for treating oral infections and inflammation. Notably, the nanoemulsified 95E extract shows higher efficiency than the conventional extract, suggesting a multifunctional treatment approach for periodontal issues and metabolic disorders. These results highlight the enhanced efficacy of the nanoemulsified extract, proposing it as an effective treatment modality for periodontal disease in diabetic patients. This research offers valuable insights into the development of innovative drug delivery systems using natural remedies for improved periodontal care in diabetic populations.

Neuroprotective mechanisms and ameliorative activities of quercetin in cisplatin-induced cerebellum neurotoxicity in rat models

Cisplatin (CP) is a highly effective antitumor agent, but its clinical use is limited due to critical adverse reactions including neurotoxicity. Quercetin (QC) is a naturally occurring phytochemical with promising bioactive effects. This study investigated the Neuroprotective mechanisms and ameliorative activities of quercetin in cisplatin-induced cerebellum neurotoxicity in rat models.The rats were randomly divided into five groups of six (n = 6) rats. Group A, served as control. Group B, received a single dose of 10 mg/kg body weight (bwt) of CP (i.p.) on the first day. Group C received 30 mg/kg bwt of QC. Group D received a single dose of 10 mg/kg bwt CP on the first day followed by 30 mg/kg bwt of QC. Group E received 30 mg/kg bwt of QC per day followed by a single dose of 10 mg/kg bwt of CP on the last day. The treatment lasted for 35 days after which the novel-object recognition memory test (NORT) was used to assess non-spatial memory function. Brain neurochemical status was assessed and brain tissues were processed for histology.Quercetin increased weight loss and cognitive performance in CP-treated rats by enhancing the exploration of unfamiliar objects. Quercetin protects the brain from CP-mediated alterations in oxidative status, as well as brain metabolic enzyme indicators. It also decreased IL-6, IL-1, and TNF-α, and NF-ĸB expression, restored brain metabolic enzyme activities, increased neurotransmitters, and prevented neuromorphological alterations.In conclusion, quercetin protects rats’ brains against CP-induced cerebellum neurotoxicity via oxidative stress inhibition and down-regulation of inflammation.

ANALISIS KADAR ALKALOID DAN FLAVONOID SEDUHAN RAMBUT JAGUNG (Zea mays L. ) DENGAN METODE SPEKTROFOTOMETRI UV-VIS

Corn silk is generally a waste of sweet corn plants after being harvested and is rarely used, however, on the other hand, corn silk is also used by the community as herbal medicine and is believed to reduce the risk of hypertension and other types of chronic diseases such as kidney infections. Corn silk is thought to contain metabolite compounds such as flavonoids, essential oils, steroids, and alkaloids. Alkaloid compounds can function as drugs and strong activators for immune cells that can destroy bacteria, viruses, fungi, and cancer cells. Flavonoid compounds are compounds that have various bioactive effects such as anti-inflammatory, antiviral, cardioprotective, anti-diabetic, anti-cancer, anti-aging, and antioxidants. it is necessary to measure the levels of alkaloids and flavonoids from corn silk infusion to determine the levels of alkaloid and flavonoid compounds in corn silk infusion. The method used in this study is the Uv-Vis spectrophotometry method. The alkaloid content was calculated using the regression formula y = 0.0895x - 0.3046, the results obtained in the corn hair infusion extract were 46.36 mg / g extract, and the flavonoid content was calculated using the regression formula y = 0.0144 x - 0.025 and the results obtained in the corn hair infusion extract were 85.42 mg / g extract. So it can be concluded that corn hair infusion contains more flavonoid compounds, namely with alkaloid compound levels of 46.36 mg / g extract and flavonoid compounds of 85.42 mg / g extract.

Machine Learning-Based Nanozyme Sensor Array as an Electronic Tongue for the Discrimination of Endogenous Phenolic Compounds in Food.

The detection of endogenous phenolic compounds (EPs) in food is of great significance in elucidating their bioactivity and health effects. Here, a novel bifunctional vanillic acid-Cu (VA-Cu) nanozyme with peroxidase-like and laccase-like activities was successfully prepared. The peroxidase mimic behavior of VA-Cu nanozyme can catalyze 3,3',5,5'-tetramethylbenzidine (TMB) to generate oxidized TMB (oxTMB). Owing to the high reducing power of EPs, this process can be inhibited, and the degree of inhibition increases with the increase of reaction time. Additionally, owing to the outstanding laccase mimic behavior of the VA-Cu, it can facilitate the oxidation of various EPs, resulting in the formation of colored quinone imines, and the degree of catalysis increases with the increase of reaction time. Based on the interesting experimental phenomena mentioned above, a six-channel nanozyme sensor array (2 enzyme-mimic activities × 3 time points = 6 sensing channels) was constructed, successfully achieving discriminant analysis of nine EPs. In addition, the combination of artificial neural network (ANN) algorithms and sensor arrays has successfully achieved accurate identification and prediction of nine EPs in black tea, honey, and grape juice. Finally, a portable method for identifying EPs in food has been proposed by combining it with a smartphone.

Modulation of regenerative responses by retinoic and ascorbic acids in human apical papilla cells

ObjectiveThis study investigated the bioactive effects of retinoic acid and ascorbic acid on hSCAPs in vitro. DesignCells were obtained from human third molars (n=4) and characterized for mesenchymal stem cell markers by flow cytometry. The experimental groups: control (α-MEM); vehicle control group (α-MEM + 0.17 % DMSO); retinoic acid 0.1, 1, and 10 µM; and ascorbic acid 3, 30, and 300 µM (n=8) were tested for cell viability (alamarBlue; 1, 3, and 7 days), total collagen synthesis (Sirius Red; 1 and 7 days), mineralized matrix formation (Alizarin red; 14 days), and the regulation of gene expression related to mineralization (ALPL and DSPP), cell migration (ITGAV and CXCL12) angiogenesis (VEGFA) and collagen synthesis (COL1A1 and COL3A1; RT-qPCR) on 1 and 7 days. ACTB and GAPDH were used as reference genes. Data were analyzed by ANOVA and complementary tests at a 5 % significance level. ResultsAscorbic acid 300 µM increased viability, and retinoic acid reduced it dose-dependently. Retinoic acid 0.1 µM and ascorbic acid 30 and 300 µM increased mineralized matrix formation and total collagen synthesis, and retinoic acid 10 µM decreased. On day 1, 0.1 µM retinoic acid upregulated the gene expression of COL1A1, COL3A1, VEGFA, CXCL12, ALPL, DSPP e ITGAV, and 300 µM ascorbic acid upregulated COL1A1, COL3A1 and DSPP. However, on day 7, retinoic acid downregulated ALPL, COL3A1, CXCL12, and VEGFA and downregulated ITGAV and VEGFA. ConclusionRetinoic acid 0.1 µM and ascorbic acid 300 µM biostimulated hSCAPs to differentiate into pro-regenerative phenotypes with potential application for REPs.

Optimizing phlorotannins extraction from Fucus vesiculosus using Box-Behnken design: Unveiling techniques for enhanced antioxidant activity and metabolic enzyme inhibition

Phlorotannins, phenolic compounds found in brown macroalgae, exhibit potential bioactive effects. This study evaluated the extraction of phlorotannins from Fucus vesiculosus using conventional and ultrasound-assisted extraction (UAE) methods, focusing on solvent-material ratio, solvent concentration, extraction time, and sonication power for UAE. The experiments, designed using a Box-Behnken design, measured total phlorotannin content (TPhC), DPPH, FRAP, and ABTS. The conventional method, under optimal conditions, produced TPhC, DPPH, FRAP, and ABTS values of 512.25 ± 14.26 mg PGE/100 g, 29.70 ± 1.40 mg TE/100 g, 589.57 ± 15.06 mg TE/100 g, and 332.73 ± 31.03 mg TE/100 g, respectively. The UAE method, under its optimal conditions, yielded higher values: 954.00 ± 33.65 mg PGE/100 g, 146.35 ± 3.30 mg TE/100 g, 1037.61 ± 32.93 mg TE/100 g, and 809.95 ± 46.58 mg TE/100 g. The extracts were tested for inhibitory effects on α-amylase and α-glucosidase, with the purified UAE extract showing greater inhibition of α-amylase (IC50 = 7.06 ± 0.67 μg/mL) compared to acarbose (IC50 = 14.63 ± 0.28 μg/mL). For α-glucosidase, acarbose had higher activity (IC50 = 11.54 ± 0.04 μg/mL) than the UAE purified extract (IC50 = 15.04 ± 0.07 μg/mL). UHPLC-qTOF-MS analysis identified various phlorotannin derivatives, with Tetrafucotetraphlorethol (m/z 993) only in the UAE purified extract. This study concludes that purified phlorotannin extract from UAE can potentially regulate α-amylase and α-glucosidase, enzymes linked to metabolic disorders like diabetes and obesity.

Water-soluble garlic polysaccharide (WSGP) improves ulcerative colitis by modulating the intestinal barrier and intestinal flora metabolites

WSGP has demonstrated significant potential for various bioactive effects. However, limited research has explored their anti-ulcerative colitis (UC) effects and mechanism on the colonic system and gut microbial metabolites. We evaluated the ameliorative effects of WSGP on the UC mice model. Using H&E to assess histological injury of colon morphology, AB-PAS staining to detect mucin secretion from goblet cells and the mucous layer, IF to evaluate the expression of intercellular tight junction proteins, ELISA to measure inflammatory factors, WB analysis to measure protein expression of inflammatory signaling pathways, RT-qPCR to quantify gene transcription of inflammatory factors, and LC-MS to analyze metabolites in mouse cecum contents. WSGP supplementation increased food intake, body weight, and colon length while reducing disease activity and histological scores in colitis-afflicted mice. WSGP mitigated colonic tissue damage and restored intestinal barrier integrity by suppressing NF-κB/STAT3 signaling, thereby decreasing gene transcription, protein expression of proinflammatory factors, and nitric oxide production. Additionally, WSGP improved UC by altering the variety of intestinal microbial metabolites. This study demonstrates that WSGP supplementation attenuates UC mice by suppressing the NF-κB/STAT3 signaling pathway, enhancing mucosal barrier function, reducing pro-inflammatory cytokines, and modulating gut microbial metabolites.

Enhancing therapy with nano-based delivery systems: exploring the bioactive properties and effects of apigenin.

Apigenin, a potent natural flavonoid, has emerged as a key therapeutic agent due to its multifaceted medicinal properties in combating various diseases. However, apigenin's clinical utility is greatly limited by its poor water solubility, low bioavailability and stability issues. To address these challenges, this review paper explores the innovative field of nanotechnology-based delivery systems, which have shown significant promise in improving the delivery and effectiveness of apigenin. This paper also explores the synergistic potential of co-delivering apigenin with conventional therapeutic agents. Despite the advantageous properties of these nanoformulations, critical challenges such as scalable production, regulatory approvals and comprehensive long-term safety assessments remain key hurdles in their clinical adoption which must be addressed for commercialization of apigenin-based formulations.

Screening bioactive compounds from Fangji Huangqi decoction for treating rheumatoid arthritis via COX-2 magnetic ligand fishing combined with in vivo validation

Ethnopharmacological relevanceFangji Huangqi Decoction (FHD) is a classical Chinese compound formula for treating rheumatoid arthritis (RA) with satisfactory effects. FHD is reputed for its ability to tonify qi with strengthening exterior, and dispel wind while removing dampness, but its mechanisms and bioactive compounds for treating RA remain unclear. Aim of the studyThe aim of this study was to explore the key target and bioactive compounds that were responsible for FHD-mediated improvements in RA. Materials and methodsUsing network pharmacology, we discovered that cyclooxygenase-2 (COX-2) was the key target of FHD against RA. We utilized a ligand fishing technique with COX-2 immobilized magnetic beads to recognize the bioactive components that act on COX-2. Then we carried out an in vitro assay of COX-2 enzyme inhibition and in vivo assay of carrageenan-induced inflammation and collagen-induced arthritis (CIA) to validate the bioactive effects of these captured ingredients. In the CIA assay, micro-CT, hematoxylin‒eosin staining and safranin-O/fast green staining were employed to assess the influence of the captured ligand on bone damage, pathological injury and cartilage destruction, respectively. Immunohistochemistry (IHC) and enzyme-linked immunosorbent assays (ELISAs) were used to detect the expression of COX-2 target in the ankle joint. interleukin-6 (IL-6) levels in the serum were also detected by ELISA. Molecular docking was used to reveal the binding mechanism of the COX-2 protein and the captured ligand. ResultsEleven ligands, including tetrandrine, fangchinoline, cyclanoline, licochalcone B, ononin, calycosin and liquiritin, were specifically bound to the COX-2 protein, as determined by ultrahigh-performance liquid chromatography–mass spectrometry (UPLC–MS), seven of which were present at high levels. One ligand, tetrandrine, not only had a great inhibitory effect on COX-2 enzyme activity but also significantly reduced carrageenan-induced inflammation. In the CIA assay, middle- and high-dose tetrandrine (25 and 50 mg/kg) had effects comparable to those of FHD and celecoxib on ameliorating RA symptoms in CIA mice via the COX-2 target. Furthermore, compared with the low-dose tetrandrine group (12.5 mg/kg), the FHD group exhibited significantly lower arthritis index scores and serum IL-6 expression, although the content of tetrandrine in FHD extract solution was approximately 0.1% of that in the low-dose tetrandrine group. ConclusionsHence, we inferred that tetrandrine was the main bioactive component responsible for the effects of FHD against RA by suppressing the expression of the COX-2 protein and inhibiting the enzyme catalytic activity of COX-2. The reason for these effects may be that tetrandrine can interact with the residue Tyr385 of COX-2, the enzymatic catalytic site of COX-2 to transform arachidonic acid (AA) to prostaglandin E2 (PGE2), and thereby reduce the production of prostaglandins and inflammatory metabolites. Moreover, in addition to tetrandrine, FHD contains other compounds that could supplement the activity of tetrandrine when FHD was used to treat RA, which is manifested the “multi-component” characteristic of how Traditional Chinese Medicine formulas treat diseases.

Bioactives in Nutricosmetics: A Focus on Caffeine from Tea to Coffee

Known for its stimulating effects on the nervous and cardiovascular systems, caffeine has proven remarkable versatile properties. It can be used in a wide range of different products, from anti-aging cosmetics to the pharmaceutical treatment of hair loss. Caffeine is known for its antioxidant properties and is commonly found in moisturising creams recommended as anti-aging or anti-cellulite and also for the treatment of different skin disorders, including androgenic alopecia. This bioactive is also described to be able to enhance the sunscreen scattering effect of well-known ultraviolet (UV) blockers. One of the major challenges remains its penetration capacity into deeper skin layers, which may be achieved by the use of nanosized delivery systems, yet without the risk of transdermal delivery. In this review, we discuss the nutraceutical value of caffeine in cosmetic products, so-called nutricosmetics, which grants this bioactive several advantages in several formulations, in comparison to other potential bioactives of nutricosmetic value. Furthermore, the disclosed effects of bioactives commonly found in coffee, tea, and their by-products are reviewed and discussed. The discussion concludes by highlighting the significant benefits of caffeine in the treatment of skin disorders and its potential to enhance and promote skin health.