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ABSTRACT Background Aims Methods Results Conclusions Skin barrier health is crucial for preventive and corrective skincare across all skin types. Witch hazel (Hamamelis virginiana) extracts show potential in addressing skin issues, but their efficacy in treating chronic inflammation, improving skin barrier function, and combating UV‐induced oxidation requires further investigation.To evaluate the efficacy of a novel formula containing witch hazel extracts in treating chronic inflammation, improving skin barrier function, and combating UV‐induced oxidation.We employed a novel ex vivo chronic inflammation model to assess anti‐inflammatory effects, measuring key pro‐inflammatory cytokines. Barrier function markers, such as loricrin and transglutaminase‐1, were analyzed. An ex vivo model with UV‐induced Reactive Oxygen Species (ROS) elevation was used to evaluate antioxidant properties, measuring specific ROS markers like 4‐Hydroxynonenal and carbonylated protein.The novel witch hazel formula significantly reduced pro‐inflammatory cytokines in both 2D and ex vivo models, including IL‐6 and IL‐8, demonstrating potent anti‐inflammatory effects. Barrier function markers showed notable improvements compared to the inflamed condition. In the UV‐induced ROS model, the formula remarkably decreased ROS levels, specifically 4‐Hydroxynonenal and carbonylated protein, indicating strong antioxidant properties.Our findings demonstrate that the novel witch hazel formula exhibits potent anti‐inflammatory and antioxidant properties while enhancing skin barrier function. This natural, well‐tolerated ingredient offers a promising treatment option for improving overall skin health, presenting new opportunities in skincare formulation and treatment strategies. [ABSTRACT FROM AUTHOR]

The combination of natural polymers and plant extract attracted much attention thanks to its valuable biological activities. This study presents the preparation and characterization of chitosan (CS) film containing Rhodomyrtus tomentosa leaf extract. In which, the Rhodomyrtus tomentosa leaf extract (SLE) with polyphenol‐rich fractions was extracted by an ultrasonic‐assisted extraction method. The prepared chitosan/polyphenol‐rich fractions film (CSPPF) was characterized using infrared (IR) spectroscopy, mechanical testing, scanning electron microscopy (SEM), and water absorption analysis. Antibacterial and anti‐inflammatory activities of the CSPPF were assessed using the agar well diffusion method and nitric oxide (NO) inhibition assays, respectively. Besides, the release of the extract from the CSPPF as well as the drug release kinetics was also tested. The Rhodomyrtus tomentosa leaf extract enhanced the antibacterial efficacy against Escherichia coli and enhanced the anti‐inflammatory activity as well as the swelling ability of the CSPPF. The CSPPF containing 1 wt.% of SLE can inhibit 77.70 % NO with an IC50 value of 19.40 μg/mL. [ABSTRACT FROM AUTHOR]

ABSTRACT This study focuses on the synthesis, characterization, and evaluation of NiBIDP and CuBIDP mixed‐ligand complexes. Synthesized with high yields in ethanol‐based solutions, these complexes demonstrate exceptional stability and non‐hygroscopic properties, with melting points exceeding 300°C. Solubility tests reveal compatibility with organic solvents such as acetonitrile, DMF, and DMSO, while being insoluble in water. Characterization through UV‐visible, IR, and mass spectrometry confirms octahedral coordination geometries around Ni(II) and Cu(II) centers. Thermal stability assessments indicate robust properties up to 180°C for NiBIDP and 170°C for CuBIDP. Computational analyses reveal significant electron localization and enhanced electron‐accepting capabilities in CuBIDP, as evidenced by its low LUMO value and high electrophilicity index. Molecular electrostatic potential (MEP) analyses identify nucleophilic sites important for protein interactions, underscoring their potential in catalysis and materials science. Biological evaluations show that although the BI and DP ligands exhibit moderate antimicrobial, anti‐inflammatory, and antioxidant activity, their metal complexes, particularly CuBIDP, demonstrate enhanced efficacy. Molecular docking studies further highlight the improved binding affinities of NiBIDP and CuBIDP with target proteins, suggesting their potential as therapeutic agents in drug discovery. In conclusion, this study provides significant insights into the structural, electronic, and biological properties of NiBIDP and CuBIDP complexes, supporting their development as versatile compounds in biomedical and materials science applications. Key outcomes include enhanced stability and bioactivity of metal complexes compared with their ligands, as well as promising therapeutic potential revealed through molecular docking analyses. [ABSTRACT FROM AUTHOR]

Antibiotic resistance microorganisms (ARMs), particularly gram-negative bacteria, pose a global health threat. The effects of fermentation on phytochemicals are numerous, and exploring this potential is the focus of drug development. The study investigated the role of fermentation in modifying V. amygdalina leaf secondary metabolites as an effective antibiotic against Escherichia. coli, Bacillus subtilis and Salmonella typhi. This work showed that fermentation increased the content of lycopene, flavonoid and carotenoid compounds but decreased chlorophyll, soluble protein and phenol. Pearson's correlation heatmap showed a strong correlation between microbial activities and secondary metabolic changes. The methanolic extract of fermented V. amygdalina leaf pulp (at day 9) showed significant antioxidant and anti-inflammatory activities. The GCMS and FTIR results showed unique compounds and structural modifications at different intervals of the fermentation period. In-vitro and in-silico analyses showed that fermentation did not alter the inhibition rate against B. subtilis; however, E. coli and S. typhi were significantly inhibited by fermented V. amygdalina pulp extracts. In-silico analyses showed that 4,6-Cholestadien-3β-ol– a compound present only on the ninth day of fermentation–was responsible for the inhibition of the gram-negative bacteria via the substitution of multiple non-ionic interactions of some key catalytic site residues with non-ionic types, thereby denying ionisation and salt-bridge properties that porins explore to resist antibiotics; and higher binding affinity to OmpC and OmpF than ampicillin. Therefore, this steroid-derived compound may open a new pipeline for developing ion-independent multi-target antibiotics against broad-spectrum multidrug-resistant gram-positive and gram-negative bacteria in food and pharmaceutical purposes. [ABSTRACT FROM AUTHOR]

ABSTRACT A proficient Fe3O4 nanoparticle catalyzed cascade multicomponent synthetic protocol has been established to synthesize the title compounds. 2‐Chloroquinoline‐3‐carbaldehydes, aniline, and substituted benzils were subjected to cascade coupling to produce novel 3‐(1,4,5‐triaryl‐1H‐imidazol‐2‐yl)quinolin‐2‐amine 5k–z under microwave irradiation using Fe3O4 NPs. According to the biological data and the computational analysis, the compounds were found to bind COX‐2 enzyme superior than the COX‐1 enzyme. The molecular docked positions of the compounds (PDB ID: 4O1Z and PDB ID: 5IKR; A chain) were examined, and the results showed that these configurations are similar to those of the highly selective COX‐1 and COX‐2 inhibitors. Compared to mefenamic acid (1.318 μg), the compounds 5k, 5l, 5n, 5p, 5q, 5r, 5s, 5t, 5v, 5x, and 5z Showed IC50 values of 1.172, 1.136, 1.508, 1.0373, 1.186, 1.017, 1.827, 1.008, 1.504, 1.217, 1.440, and 1.832, respectively, making them the most effective and selective COX‐1 and COX‐2 inhibitors. For every significantly active molecule, a selectivity index was calculated. Interestingly, these molecules that worked as COX inhibitors also functioned well and showed promising results for antioxidant activity. [ABSTRACT FROM AUTHOR]

ABSTRACT The COVID‐19 pandemic caused by the SARS‐CoV‐2 virus was arguably one of the worst public health disasters of the last 100 years. As many infectious disease experts were focused on influenza, MERS, ZIKA, or Ebola as potential pandemic‐causing agents, SARS‐CoV‐2 appeared to come from nowhere and spread rapidly. As with any zoonotic agent, the initial pathogen was able to transmit to a new host (humans), but it was poorly adapted to the immune environment of the new host and resulted in a maladapted immune response. As the host‐pathogen interaction evolved, subsequent variants of SARS‐CoV‐2 became less pathogenic and acquired immunity in the host provided protection, at least partial protection, to new variants. As the host‐pathogen interaction has changed since the beginning of the pandemic, it is possible the clinical results discussed here may not be applicable today as they were at the start of the pandemic. With this caveat in mind, we present an overview of the immune response of severe COVID‐19 from a clinical research perspective and examine clinical trials utilizing immunomodulating agents to further elucidate the importance of hyperinflammation as a factor contributing to severe COVID‐19 disease. [ABSTRACT FROM AUTHOR]

Background: Pain and inflammation are the major medical condition commonly addressed with traditional remedies. Acacia seyal is a traditional herb widely used in Ethiopian folk medicine for pain management. However, its effectiveness has yet to be validated through scientific or experimental research. Therefore, the current study aims at evaluating the in vivo analgesic and anti-inflammatory effects of 80% methanolic stem bark extract of Acacia seyal in rodent models. Methods: After successful extractions of the stem barks of Acacia seyal with 80% methanol, the pain relieving effects of 100, 200 and 400 mg/kg extract were evaluated using acetic acid-induced writhing test and hot plate method whereas the anti-inflammatory profile was determined by carrageenan induced paw-edema model and cotton pellet induced granuloma technique. Results: The 80% methanol Acacia seyal stem bark extract exhibited substantial (p < 0.001) analgesic effect in acetic acid induced writing test (p < 0.001). The plant extract also witnessed significant central analgesic effect in hot plate method beginning at 30 min with maximum % elongation time occurred at 120 min. Furthermore, the acacia stem bark extract produced anti-inflammatory effect against carrageenan induced paw-edema model. In cotton pellet induced granuloma model, the 200 and 400 mg/kg doses of the current plant material appeared to inhibit granuloma mass formation and exudate reduction significantly (p < 0.001). Conclusion: The collective findings of the current study revealed that 80% methanol extracts of Acacia seyal exhibited considerable analgesic and anti-inflammatory activities, supporting the plant's traditional use for management of pain and inflammatory disorders. [ABSTRACT FROM AUTHOR]

Plant sterols encompass phytosterols and phytostanols, with over 250 identified types. They've garnered attention in the food industry due to their potential hypocholesterolemic effects. This manuscript offers a current view phytosterols content in foods, their bioaccessibility, bioavailability, and metabolic benefits based on existing preclinical and clinical data. Published articles from 2016 to 2023 regarding the effect of sitosterol, sitostanol, campesterol, campestanol, stigmasterol, and mixed phytosterols on preclinical models and clinical trials were included. Food and technology-related issues were also discussed. Phytosterols's bioavailability in food is limited, exhibiting vulnerability to oxidation, low water solubility, and a distinctive taste. Nevertheless, various technological approaches have been devised to enhance its inclusion in food, ensuring adequate doses for harnessing its cholesterol-lowering potential. This effect has been extensively researched, alongside its hypoglycemic and anti-inflammatory properties. There's a need to create novel functional foods enriched with phytosterols to attain the daily dosage required to leverage its hypercholesterolemic, hypoglycemic, anti-inflammatory, and other ongoing beneficial effects. [ABSTRACT FROM AUTHOR]

Ethyl pyruvate (EP) has emerged as a promising compound with potential therapeutic benefits attributed to its anti-inflammatory and antioxidant properties. This study aimed to understand the effects of EP on plasma metabolites and immune cells in horses, utilizing advanced liquid chromatography-mass spectrometry (LC-MS)-based metabolomics, quantitative polymerase chain reaction (qPCR), and blood chemistry analyses. Our comprehensive analysis detected 2,366 ions, and 126 metabolites were accurately identified. Remarkably, EP administration induced significant changes in 28 metabolites at 1 h and 11 metabolites at 8 h, highlighting its time-dependent impact on metabolic pathways such as phenylalanine and arginine biosynthesis. Moreover, EP significantly lowered the expression of inflammatory markers interleukin (IL)-6 and heme oxygenase (HO)-1, indicating its potential as an anti-inflammatory agent. Blood chemistry analysis revealed notable reductions in glucose and triglyceride levels. These findings demonstrate that EP is a substance with potential effects on pathways associated with inflammation, oxidative stress, and metabolic processes. [ABSTRACT FROM AUTHOR]

This study aimed to meticulously assess the effectiveness of hyaluronic acid (HA) in mitigating symptoms associated with monosodium iodoacetate (MIA)-induced osteoarthritis (OA) symptoms in rodent models and to investigate the underlying mechanistic pathways. Eight-week-old rats were randomly allocated to a normal control group and three experimental groups (n = 10 per group). The normal group did not undergo any treatment. The experimental groups were administered MIA for 1 week to induce osteoarthritis, and orally administered distilled water (control group), 2 mg/kg indomethacin (INDO group), or 20 mg/kg HA (HA20 group) daily for 4 weeks. The HA20 group showed a significant improvement in hind-paw weight-bearing distribution after 4 weeks compared to the control group. HA suppressed inflammatory responses by reducing the overproduction of prostaglandin E2 and leukotriene B4 and protected the vital components of the articular ECM, including glycosaminoglycans and aggrecan. HA treatment effectively reduced inflammation, protected cartilage by inhibiting MMP expression, and suppressed inflammatory mediator production. This study demonstrates that HA has potential to alleviate OA symptoms in a rodent model stimulated with MIA, rendering it a promising therapeutic agent for OA. [ABSTRACT FROM AUTHOR]

Autoimmune diseases encompass a wide range of disorders characterized by disturbed immunoregulation leading to the development of specific autoantibodies, which cause inflammation and multiple organ involvement. However, its pathogenesis remains unelucidated. Furthermore, the cumulative medical and economic burden of autoimmune diseases is on the rise, making these diseases a ubiquitous global phenomenon that is predicted to further increase in the coming decades. Coumarins, a class of aromatic natural products with benzene and alpha-pyrone as their basic structures, has good therapeutic effects on autoimmune diseases. In this review, we systematically highlighted the latest evidence on coumarins and autoimmune diseases data from clinical and animal studies. Coumarin acts on immune cells and cytokines and plays a role in the treatment of autoimmune diseases by regulating NF-κB, Keap1/Nrf2, MAPKs, JAK/STAT, Wnt/β-catenin, PI3K/AKT, Notch and TGF-β/Smad signaling pathways. This systematic review will provide insight into the interaction of coumarin and autoimmune diseases, and will lay a groundwork for the development of new drugs for autoimmune diseases. [ABSTRACT FROM AUTHOR]

Introduction: Garlic (Allium sativum L.), has been cultivated in various countries and is valued for its medicinal and culinary properties. It contains bioactive compounds such as phenolic compounds, organic sulfides, polysaccharides, and saponins, with allicin being a particularly studied compound. These compounds have been shown to possess antioxidant, antimicrobial, antiviral, anticancer, anti-inflammatory, anti-hyperlipidemic and antihypertensive effects. Garlic has been used for over 5000 years as a curative plant and has potential applications in food science, medicine, and nutraceuticals. Aim of the Study: The aim of the study is to provide a comprehensive review of the overall impact of Allium sativum L. on human health and in order to draw attention to the benefits of regular consumption. Materials and methods: A comprehensive review of scientific and medical literature was conducted utilizing PubMed and Google Scholar databases. Searching terms were: garlic, Allium sativum L., garlic antiinflammatory, garlic anticancer, garlic health effects. Conclusion: Allium sativum L. is associated with a comprehensive range of beneficial effects on the human body. These include anti-inflammatory and antioxidant properties, positive influence on lipid profile, cardiovascular system, and the anticancer activity among others by stimulation of tumor apoptosis. As a result, garlic and its bioactive compounds hold promise as functional foods or nutraceuticals for the prevention and treatment of various diseases. [ABSTRACT FROM AUTHOR]

Eight new caffeyl hydrazide derivatives (4a–4h) were synthesised via a convenient esterification of caffeic acid with some substituted aryl acid hydrazides. The synthesised caffeyl derivatives were evaluated for their inhibitory effects on lipopolysaccharide (LPS)-induced nitric oxide (NO) production in RAW264.7 macrophages. The fluorobenzoylhydrazide derivatives 4f, 4 g and 4h were found to be the most powerful anti-inflammatory compounds with IC50 values ranging from 11.90 to 24.17 μM, which were more potent than the reference compound L-NMMA (IC50 32.8 μM). Additionally, synthesised compounds have been rationalised by using molecular docking studies which were performed in order to understand insights on the action mechanism of newly synthesised inhibitors against inflammatory mediator (iNOS). Obtained data indicate that compounds 4f, 4h, 4a and 4 g were observed to effectively bind to iNOS receptor with dock score values of −11.62, −10.81, −10.78 and −10.51 kcal/mol, respectively. [ABSTRACT FROM AUTHOR]

The n-butanol extract of Stachys arvensis (L.) L. aerial parts (BESA) was analysed by LC-HRMS/MS. 43 Polyphenols, including flavonoids, cinnamic acid derivatives, phenylethaoids, chromones, gallotannins, coumarins and chalcones with hyperoside (13.85%), panasenoside (10.31%), myricitrin (7.89%) and sayaendoside (7.16%), as the major compounds, were identified. High total phenolics (470.21 ± 1.22 mg GAE/g extract) and total flavonoids (189.05 ± 0.72 mg QE/g extract) contents were measured. In addition, the BESA exhibited a higher antioxidant effect in CUPRAC (A0.5:0.45 ± 0.03 μg/mL), DPPH (IC50:4.51 ± 0.16 μg/mL) and ABTS (IC50:7.10 ± 0.18 μg/mL) assays than the standards BHA and α-Tocopherol. Moreover the extract showed a good inhibitory effect against BChE (IC50: 145.02 ± 0.03 μg/mL) and α-amylase (IC50:2.66 ± 0.0024 mg/mL). The BESA exhibited an excellent anti-inflammatory activity (IC50:416 ± 0,056 μg/mL) which was close to that of acetylsalicylic acid, used as a control. The BESA was toxic towards T. molitor larvae and it possessed a good antibacterial activity against gram (+) and gram (-) tested strains. [ABSTRACT FROM AUTHOR]

A series of para -quinone methide derivatives were evaluated their anti-inflammatory activity. Through the screening of the lipopolysaccharide (LPS)-induced inflammatory cell model in Raw264.7 cells, it was found that the inhibitory activity of meta -substituted derivatives on NO production was superior to that of ortho - and para -substituted derivatives. Among them, in the inflammatory cell model, the meta -trifluoromethyl substituted para -quinone methide derivative 1i had the best activity in inhibiting LPS-induced excess generation of NO. And 1i could effectively inhibit the increase of ROS in inflammatory cells, the expression of iNOS related to the production of NO, and the expressions of inflammation related initiating protein TLR4, pro-inflammatory cytokines IL-6 and TNF-α, inflammasome NLRP3 and Caspase1. In the dextran sulfate sodium (DSS)-induced ulcerative colitis (UC) mouse model, the active derivative 1i could inhibit DSS-induced colon shortening, and reverse DSS-induced pathological changes in colon tissue, such as inflammatory infiltration, structural destruction and crypt disappearance. 1i could effectively inhibit oxidative stress, inflammation and apoptosis in UC mice. Moreover, through the determination of serum biochemical indicators, tissue pathologies and tissue organ indexes, 1i could effectively reverse the damage to mouse liver and kidney caused by DSS, playing a protective role in liver and kidney of mice. In summary, 1i was an effective anti-inflammatory reagent and could be developed as a potential drug for anti-UC. [ABSTRACT FROM AUTHOR]

Syzygium aqueum is widely used in folk medicine. A polyphenol-rich extract from its leaves demonstrated a plethora of substantial pharmacological properties. The extract showed solid antioxidant properties in vitro and protected human keratinocytes (HaCaT cells) against UVA damage. The extract also reduced the elevated levels of ALT, AST, total bilirubin (TB), total cholesterol (TC) and triglycerides (TG) in rats with acute CCl4 intoxication. In addition to reducing the high MDA level, the extract noticeably restored GSH and SOD to the normal control levels in liver tissue homogenates and counteracted the deleterious histopathologic changes in liver after CCl4 injection. Additionally, the extract exhibited promising anti-inflammatory activities in vitro where it inhibited LOX, COX-1, and COX-2 with a higher COX-2 selectivity than that of indomethacin and diclofenac and reduced the extent of lysis of erythrocytes upon incubation with hypotonic buffer solution. S. aqueum extract also markedly reduced leukocyte numbers with similar activities to diclofenac in rats challenged with carrageenan. Additionally, administration of the extract abolished writhes induced by acetic acid in mice and prolonged the response latency in hot plate test. Meanwhile, the identified polyphenolics from the extract showed a certain affinity for the active pockets of 5-lipoxygenase (5-LOX), cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) explaining the observed anti-inflammatory activities. Finally, 87 secondary metabolites (mostly phenolics) were tentatively identified in the extract based on LC-MS/MS analyses. Syzygium aqueum displays good protection against oxidative stress, free radicals, and could be a good candidate for treating oxidative stress related diseases. [ABSTRACT FROM AUTHOR]

Introduction: Safflower, a traditional Chinese medicine, is rich in chemical components including flavonoids, polysaccharides, and alkaloids. It exhibits pharmacological effects such as antioxidant, anti-inflammatory, anti-tumor, and anti-thrombosis properties, making it a valuable resource in the medical field. Furthermore, due to its antioxidant and anti-inflammatory effects, safflower is increasingly being utilized in the cosmetics industry. Methods: In this study, yeast was employed to ferment safflower, and the optimal fermentation conditions were established through single-factor experiments and response surface methodology. Subsequently, the antioxidant and anti-inflammatory efficacy of the safflower fermentation solution was assessed using both cellular and zebrafish models. Finally, the safety of the safflower fermentation solution was evaluated through a cosmetic eye irritation test. Results: From a total of 20 yeast strains, YF-5 was identified as the dominant strain for safflower fermentation. By optimizing the fermentation conditions, it was established that the optimal parameters for YF-5 fermentation of safflower are as follows: a fermentation temperature of 36.55°C, a material-to-liquid ratio of 1:20.46, a fructose concentration of 6.20%, a fermentation duration of 72 h, and an inoculum volume of 4%. The biological activities of safflower, including its antioxidant and anti-inflammatory properties, were enhanced through yeast fermentation. In HaCaT cell and zebrafish oxidative damage assays, safflower fermentation solution inhibits the production of malondialdehyde (MDA) and increases superoxide dismutase (SOD) activity as well as total antioxidant capacity (T-AOC). In the RAW264.7 cell inflammatory damage assays, a 20% safflower fermentation solution was found to inhibit the release of TNF-α and NO in the inflammatory model, with inhibition rates of 30.94 and 28.86%, respectively. In the zebrafish inflammatory damage assays, the quantity of fluorescent neutral proteins in the 5% safflower fermentation solution was 0.7 times that observed in the dexamethasone (0.1 mg/mL) positive control group, indicating that its anti-inflammatory activity is comparable to that of dexamethasone (0.1 mg/mL). In the chicken embryo chorionic membrane experiment, it was observed that the safflower fermentation solution did not cause significant damage to the blood vessels of the chorionic allantoic membrane (CAM). This finding demonstrates that the safflower fermentation solution possesses a certain degree of safety. Discussion: Safflower fermentation solution has antioxidant and anti-inflammatory bioactivities, and it has passed cosmetic safety evaluations. It can be used as a new natural cosmetic ingredient added to cosmetic products. [ABSTRACT FROM AUTHOR]

Schiff bases possess a range of unique physical, chemical and medicinal properties, which contribute to their potency as biological agents. A Schiff base was synthesized, which consisted of 4-chloro aniline and vanillin. The successful formation of the compound was confirmed by their comparable FTIR, UV–Vis, 1HNMR and 13CNMR spectra. The compound was analyzed using X-ray crystallography, which revealed that it crystallizes in the monoclinic system with the space group P21/c. The Hirshfeld surface analysis revealed valuable information about the intermolecular interactions present in the crystal lattice. The most common contacts observed were between hydrogen and hydrogen, as well as carbon and hydrogen. The obtained fluorescence values of 375 nm and 412 nm at excitation wavelength 322 nm strongly indicated the luminescent nature of the compound. The thermal stability of the compound was assessed through thermogravimetric analysis (TGA). DFT was used to optimize the geometry using the B3LYP/cc-pVDZ basis set. The compound exhibited an energy gap of 2.35 electron volts (eV). According to the analysis of molecular electrostatic potential, C and O atoms were found to be electrophilic. According to Mulliken charge analysis, C atoms possess both positive and negative charges, hydrogen atoms exclusively carry positive charges, and Cl, O and N atoms exclusively carry negative charges. Upon analysis of the molecule, the electron localization function discovered that the atoms of carbon, nitrogen and chlorine exhibited delocalized electron density. Also, the localized orbital locator identified the localized orbital positions in the hydrogen atoms. The reduced density gradient (RDG) maps exhibit a wide range of noncovalent interactions. In comparison to the standard amoxicillin, the synthesized compound demonstrated moderate antimicrobial efficacy against the gram-positive bacteria Klebsiella pneumoniae and the fungi Candida albicans. The compound’s concentration-dependent antioxidant and anti-inflammatory properties were demonstrated through in vitro biological evaluation using 2,2-diphenyl-1-picrylhydrazyl and human red blood cell (HRBC) methods. The compound was docked using the proteins 7BYE and 4LEB were chosen from both organisms. The lowest binding attractions obtained were -3.40 kcal/mol for 7BYE and -4.51 kcal/mol for 4LEB. To investigate the stability of the protein–ligand complex, molecular dynamic simulation was employed. The ligands in silico toxicity potentialities were analyzed using seven toxicity models and the results indicated that the ligand is biocompatible. [ABSTRACT FROM AUTHOR]

Cisplatin, the pioneering heavy metal compound, stands out as a potent drug for the treatment of various solid tumors. However, its clinical utility is hampered by notable toxicity and adverse effects, particularly nephrotoxicity. The potency of rutecarpine, a phytochemical, in mitigating cisplatin‐induced nephrotoxicity was assessed in the present study. In this experimental setup, healthy male Wistar rats were grouped into four and Group I rats served as the control group, receiving only vehicle control. Group II rats were subjected to cisplatin treatment alone, administered intraperitoneally at a dosage of 7 mg/kg body weight on the 19th, 20th, and 21st days. Group III and IV rats were orally administered with rutecarpine at doses of 10 and 20 mg/kg body weight, respectively, starting from Day 1 and continuing daily for 21 days. Additionally, they were injected intraperitoneally with cisplatin at the same dosage and schedule as Group II. Relative kidney weight and renal biochemical markers blood urea nitrogen, lactate dehydrogenase, serum urea, and creatinine were measured to assess rutecarpine inhibitory potency against cisplatin toxicity. Markers of oxidative damage and antioxidants levels were quantified in the ruteacarpine‐ and cisplatin‐treated rats. The study investigated the anti‐inflammatory property of rutecarpine in cisplatin‐induced nephrotoxicity by analyzing inflammatory cytokines. Renal tissue levels of monocyte chemoattractant protein‐1, intercellular adhesion molecule‐1, high‐mobility group box 1, and nuclear factor kappa B, key markers of nephrotoxicity, were quantified to assess rutecarpine's potential to mitigate cisplatin‐triggered damage. Histopathological examinations were performed to confirm the impact of rutecarpine against cisplatin‐induced nephrotoxicity. Treatment with rutecarpine notably reduced renal biochemical markers, prevented renal edema, and attenuated oxidative stress‐induced damage in cisplatin‐treated rats. Both inflammatory and nephrotoxicity markers showed significant decreases in rats treated with rutecarpine along with cisplatin. Histological analysis affirmed that rutecarpine pretreatment effectively prevented cisplatin‐induced nephrotoxicity. The study findings demonstrate that rutecarpine ameliorates cisplatin‐triggered nephrotoxicity through its antioxidant and anti‐inflammatory properties, suggesting that rutecarpine supplementation alongside cisplatin treatment could potentially reduce nephrotoxicity in cancer patients. [ABSTRACT FROM AUTHOR]

Background: Green synthesized nanoparticles have recently gained significant medicinal applications and oftentimes outperform their green sources. Selenium is of fundamental importance to human health, stemming from its distinctive physicochemical properties, such as antioxidant activity, inhibition of Lipid peroxidation, stabilization of membrane proteins, maintenance of membrane fluidity and modulation of cell signaling. Though reports have shown some therapeutic potential of Ackee plant parts such as antioxidant, anti-inflammatory, antimicrobial, neuroprotective, very few scientific proofs still exist in support of these effects. Methods: This study synthesized selenium nanoparticles (Se-NPs) from crude methanolic extracts of Ackee leaves (AKL) and Ackee arils (AKA), examined the photo-physical characteristics of the Se-NPs and determined the in-vitro antioxidant, antidiabetic, and anti-inflammatory potentials of AKL, AKA, and their Se-NPs using established protocols. Results: In both leaves and arils Se-NPs: UV spectroscopy revealed a qualitative absorbance at 310 nm; FTIR indicated multiple vibrations around 4000 cm−1- 400 cm−1; SEM images of 5 µm principally showed consistent size distribution of amorphous and granular shape at a magnification of 10,000X; while EDS spectra strongly confirm the presence of atomic Se compound at 30 kV. Various antioxidant activities assays carried out showed a range of approximately 4 to 60 times higher activities of the AKL, AKA, and Se-NPs than Ascorbic acid—the standard drug used. Furthermore, appreciable activities of more than 50% were obtained for alpha-amylase and alpha-glucosidase inhibitory activities, along with highly significant activities of haemoglobin glycosylation, glucose uptake, membrane stabilization, anti-arthritic, anti-haemolysis activities, when AKL, AKA, and Se-NPs were compared with standard drugs. Conclusion: Encouraging the development and utilization of AKL, AKA, and Se-NPs will provide tremendous therapeutic efficacy and bioavailability approaches towards the management of diabetes, inflammation, and other oxidative stress-related diseases. [ABSTRACT FROM AUTHOR]

Background: Achillea fragrantissima (F. Asteraceae) is traditionally used to treat skin infections and inflammation. The present work intended to prepare essential oils (EOs) from A. fragrantissima aerial parts growing widely in Egypt and investigate its antibacterial activity against skin-related pathogens and in vitro cell-based anti-inflammatory activity. Methods: EOs of the fresh aerial parts were extracted by hydrodistillation (HD), microwave-assisted hydrodistillation (MAHD), and head-space (HS), while those of the dried ones were prepared by supercritical fluid (SF). The result EOs were analyzed using GC/MS. The antibacterial activity was evaluated alongside Pseudomonas aeruginosa ATCC 9027, Escherichia coli ATCC 8739, Staphylococcus aureus ATCC 25923, Streptococcus pyogenes ATCC 12344, Clostridium perfringens ATCC 13124 by agar diffusion, microwell dilution, and biofilm formation tests. The anti-inflammatory activity was evaluated by measuring tumor necrosis factor-alpha (TNF-α), interleukin 2 (IL-2), and 6 (IL-6) in lipopolysaccharides (LPS)- stimulated RAW 264.7 cells using ELISA assays in addition, expression of nitric oxide synthase (iNOS) was measured via western blot. Results: The SF method gave the highest EO yield (1.50 mL v/w). Oxygenated components constituted the highest percentage in the four methods, 84.14, 79.21, 73.29 and 33.57% in the HS, HD, MAHD, and SF, respectively. Moreover, variation in the amount of identified compounds was apparent; in HS EO α-thujone (29.37%), artemisia ketone (19.59%), and santolina alcohol (14.66%) are major components, while α-thujone (20.38%) and piperatone (12.09%) were significant in HD. Moreover, (+)-spathulenol (12.22%) and piperatone (10.48%) were significant in MAHD, while piperatone (14.83%) and β-sitosterol (11.07%) were significant in SF EO. HD, MAHD, and SF EOs exhibited susceptibility against P. aeruginosa (IZ = 9–14 mm), E. coli (11–13 mm), and C. perfringens (IZ = 10–14 mm) in agar diffusion assay. MAHD EOs demonstrated potent growth inhibition (MICs = 0.25–2 mg/mL), followed by HD EOs (MICs = 13–52 mg/mL) to all tested microorganisms in well microdilution assay. Also, they exert MBC values equal to or higher than the MICs. Furthermore, SF EOs inhibited the biofilm formation of all tested microorganisms by 65.12—80.84%. Specifically, MAHD and HD EOs efficiently suppress the biofilm of S. pyogenes (77.87%) and P. aeruginosa (60. 29%), respectively. Ultimately, HD and SF EOs showed anti-inflammatory activity by suppressing the TNF-α, IL-2, and IL-6 release and iNOS expression in LPS-stimulated RAW 264.7 macrophages. Conclusion: A. fragrantissima EO is rich in oxygenated volatile compounds with antibacterial and anti-inflammatory activities. It is encouraged as a bioactive agent for adjusting skin infections, though additional studies are essential for their safety in clinical settings. [ABSTRACT FROM AUTHOR]

Introduction: Due to its remarkable anti-inflammatory pharmacological activity, Farfarae Flos has gained extensive usage in the treatment of various inflammatory diseases such as bronchitis, pneumonia, prostatitis and colitis. And Farfarae Flos come in two color types depending on the color of the flowers: yellowish-white (YW), and purplish-red (PR). However, the difference in anti-inflammatory activity and metabolic profiles between the two flower colors remains unexplored. Methods: This study aims to explore the difference in the anti-inflammatory potential between YW and PR variants of Farfarae Flos and unravel the mechanisms responsible for the observed differences in anti-inflammatory activity through an integrated approach encompassing untargeted metabolomics and in vivo / vitro experimental studies. Initially, we verified the contrasting effects of YW and PR on the inhibition of the inflammatory factors interleukin-6 (IL-6) and nitric oxide (NO) by utilizing an in vitro RAW 264.7 cell inflammation model. Subsequently, a comprehensive evaluation of the systemic inhibitory capacity of YW and PR on IL-6, Interleukin-10 (IL-10), and tumor necrosis factor- α (TNF- α) was conducted using a validated whole-body mouse model, followed by the analysis of inflammatory factors and histological examination of collected serum, liver, and spleen after 7 days. Furthermore, non-targeted metabolomics profiling was employed to analyze the metabolite profiles of Farfarae Flos with different colors, and quantitative analysis was conducted to identify differential metabolites between YW and PR. The correlation between the anti-inflammatory activities of differentially accumulated metabolites (DAMs) and Farfarae Flos was investigated, resulting in the identification of 48 compounds exhibiting significant anti-inflammatory activity. Additionally, KEGG pathway enrichment analysis was performed to elucidate the underlying mechanisms. Results: Our findings demonstrate that both YW and PR possess anti-inflammatory abilities, with PR exhibiting significantly superior efficacy. The integration of in vivo / vitro experiments and non-targeted metabolomics confirmed the exceptional anti-inflammatory potential of PR and solidified its classification as the "purplish-red better" of Farfarae Flos. Discussion: This study provides valuable insights into the breeding and medical transformation of Farfarae Flos varieties, along with a scientific basis for the establishment of quality standards and the development of new drugs utilizing Farfarae Flos. [ABSTRACT FROM AUTHOR]

Given the unique anatomy and location of inflammatory bowel disease (IBD), oral pharmacological treatment is the mainstay for managing IBD because of its convenience and direct accessibility to the gastrointestinal tract. However, efficient delivery systems must be designed to navigate the harsh gastrointestinal environment during application. Here, an innovative oral drug delivery system was proposed using nanomotor (NM)‐loaded soluble microcapsules for treating IBD. MnO2‐Au‐mSiO2 NMs incorporate partially encapsulated MnO2 antennas that convert reactive oxygen species into oxygen, autonomously propelling the NMs. Astaxanthin (AST), known for its anti‐inflammatory properties, is loaded into the mesoporous silica (mSiO2) of NMs (AST@NMs). AST effectively reduces inflammation and shifts macrophages from a proinflammatory (M1) phenotype to an anti‐inflammatory (M2) phenotype. To protect the nanomotors from harsh digestive conditions and achieve intestinal‐responsive release, using photocurable 3D printing, we fabricated enteric‐coated oral microcapsules (MCs). Additionally, to prevent leakage of AST@NMs, a calcium alginate shell was cured in situ on the surface of the microcapsules (AST@NMs@MCs). In vitro and in vivo, AST@NMs@MCs effectively reduced inflammation, repaired the intestinal barrier, and modulated the gut microbiota. These findings underscore the protective effects of the microcapsules on AST@NM, highlighting their potential as a promising strategy for treating colitis. [ABSTRACT FROM AUTHOR]

Isoalantolactone (ISA) is a sesquiterpene lactone that could be isolated from Inula helenium as well as many other herbal plants belonging to Asteraceae. Over the past 2 decades, lots of researches have been made on ISA, which owns multiple pharmacological effects, such as antimicrobial, anticancer, anti-inflammatory, neuroprotective, antidepressant-like activity, as well as others. The anticancer effects of ISA involve proliferation inhibition, ROS overproduction, apoptosis induction and cell cycle arrest. Through inhibiting NF-κB signaling, ISA exerts its anti-inflammatory effects which are involved in the neuroprotection of ISA. This review hackled the reported pharmacological effects of ISA and associated mechanisms, providing an update on understanding its potential in drug development. [ABSTRACT FROM AUTHOR]

Background: Allergic rhinitis is an inflammatory disease dependent on immunoglobulin E and causes inflammation of the nasal mucosa, leading to decreased quality of life for affected patients. Since common treatments, including corticosteroids and antihistamines, have temporary therapeutic effects and numerous side effects, investigating natural compounds effective in improving allergic rhinitis with low complications and high efficacy can be significant and necessary. Purpose: This study aims to present a comprehensive and critical evaluation of the effect of natural compounds in improving allergic rhinitis. Methods: Studies were identified through systematic searches of ScienceDirect, PubMed, Scopus, and Web of Sciences databases. Eligibility checks were conducted based on predefined selection criteria. Forty-six articles were included in this study. Results and discussion: Phytochemicals, including flavonoids, alkaloids, terpenoids, and other compounds showed significant anti-inflammatory and antihistaminic effects. These compounds alleviate allergic rhinitis symptoms by inhibiting inflammatory mediators, oxidative stress, apoptosis, and key signaling pathways such as MAPK/NFκB and TLR4/MyD88/NF-κB. Conclusion: Phytochemicals exhibit anti-inflammatory and antioxidant properties, making them. [ABSTRACT FROM AUTHOR]

Due to its unique properties and advantageous traits, zinc oxide has garnered significant attention in recent years for the green synthesis of ZnO nanoparticles (ZnO‐NP). This paper is focused on the synthesis of ZnO‐NPs mediated by Adiantum capillus‐veneris L. leaf extract and assesses their potential biological activities. In this study, ZnO‐NP is synthesized using A. capillus‐veneris L. leaf extract. The synthesized nanoparticles are characterized using, UV–vis spectroscopy, energy‐dispersive X‐ray spectroscopy (EDX), (SEM) scanning electron microscopy, X‐ray diffraction (XRD), and Fourier transform infrared (FT‐IR) spectrophotometry. The antibacterial, antifungal, anti‐inflammatory, and antioxidant properties of the formulated ZnO‐NPs are also inspected. The UV–vis, XRD, SEM, EDX, and FTIR confirmed the formation and purity of synthesized ZnO‐NPs. The ZnO‐NPs exhibit efficient antimicrobial potency against Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, Aspergillus niger, and Aspergillus fumigatus. Gram‐positive bacteria, particularly S. aureus, are more susceptible to ZnO‐NPs, with the largest inhibition zone of 32 mm. In contrast, E. coli and P. aeruginosa display smaller inhibition zones of 25 and 27 mm respectively. Anti‐inflammatory tests show that ZnO‐NPs have a significant anti‐inflammatory effect against egg albumin and bovine serum albumin denaturation, possess low toxicity on erythrocytes, and are highly hemocompatible. [ABSTRACT FROM AUTHOR]

The present investigation reports the synthesis and characterization of a novel series of 1,2-dihydroquinoline sulphonamides, developed with the aim of enhancing their pharmacological efficacy. The synthesis involved a multi-step process starting with the preparation of 3-hydroxy Acetanilide, followed by Pechmann condensation to obtain acetylated aminophenol, and subsequent reactions leading to the formation of 1,2-dihydroquinoline derivatives. These derivatives were further reacted with various substituted sulphonyl chlorides to yield the target sulphonamide compounds. The synthesized compounds were characterized using FTIR, 1H NMR, 13C NMR, and LCMS. Their pharmacological activities, including antibacterial, anthelmintic, anti-inflammatory, and antihyperlipidemic properties, were evaluated through in-vitro assays. The results demonstrated that these novel 1,2-dihydroquinoline sulphonamides exhibit promising pharmacological activities, validating their potential as effective therapeutic agents. [ABSTRACT FROM AUTHOR]

This study aimed to develop and evaluate a novel herbal gel formulation containing celecoxib and bioactive compounds of Salai Guggul for effective pain management. Celecoxib, a selective COX-2 inhibitor with anti-inflammatory and analgesic properties, was combined with menthol, safflower oil, and Salai Guggul extract to enhance therapeutic efficacy through synergistic effects. Three gel formulations (CHG I, CHG II, and CHG III) were prepared using varying concentrations of key excipients and evaluated for physicochemical properties, including pH, viscosity, extrudability, spreadability, and in vitro drug diffusion. All formulations exhibited favorable properties with pH values near skin compatibility, acceptable viscosity, and superior extrudability and spreadability. In vitro drug diffusion studies revealed that CHG I provided the highest drug release (97.27%) over 240 minutes. The study demonstrated the potential of this herbal gel formulation as a promising topical treatment for pain management, offering improved skin permeation and prolonged drug release. [ABSTRACT FROM AUTHOR]

Urtica dioica L. is one of the most widely utilized medicinal plants commonly applied in the form of tea, juice, and dietary supplements. This study aimed to assess the effect of the U. dioica ethanol–water extract (UdE) and polyphenolic fraction isolated from the extract (UdF) on normal human colon epithelial cells and to evaluate their protective activity against induced oxidative stress. The cytotoxic potential against human colorectal adenocarcinoma (HT29) and the anti-inflammatory effects were also investigated. UPLC-MS-DAD analysis revealed that both extracts were abundant in caffeic acid derivatives, specifically chlorogenic and caffeoylmalic acids, and therefore, they showed significant protective and ROS scavenging effects in normal human colon epithelial cells. Moreover, they had no negative impact on cell viability and morphology in normal cells and the extracts, particularly UdF, moderately suppressed adenocarcinoma cells. Furthermore, UdF significantly decreased IL-1β levels in HT29 cells. Our research indicates that U. dioica may provide significant health advantages because of its antioxidant and anti-inflammatory effects. [ABSTRACT FROM AUTHOR]

Understanding the complex link between inflammation, gut health, and dietary amino acids is becoming increasingly important in the pathophysiology of inflammatory bowel disease (IBD). This study tested the hypothesis that a leucine-rich diet could attenuate inflammation and improve gut health in a mouse model of IBD. Specifically, we investigated the effects of a leucine-rich diet on dextran sulfate sodium (DSS)-induced colitis in germ-free (GF) SAMP1/YitFC (SAMP) mice colonized with human gut microbiota (hGF-SAMP). hGF-SAMP mice were fed one of four different diets: standard mouse diet (CHOW), American diet (AD), leucine-rich AD (AD + AA), or leucine-rich CHOW diet (CH + AA). Body weight, myeloperoxidase (MPO) activity, gut permeability, colonoscopy scores, and histological analysis were measured. Mice on a leucine-rich CHOW diet showed a decrease in fecal MPO prior to DSS treatment as compared to those on a regular diet (p > 0.05); however, after week five, prior to DSS, this effect had diminished. Following DSS treatment, there was no significant difference in gut permeability, fecal MPO activity, or body weight changes between the leucine-supplemented and control groups. These findings suggest that while a leucine-rich diet may transiently affect fecal MPO levels in hGF-SAMP mice, it does not confer protection against DSS-induced colitis symptoms or mitigate inflammation in the long term. [ABSTRACT FROM AUTHOR]

Propolis, such as is used as bio-cosmetics and in functional materials, is increasing because of its antioxidant medicinal benefits. However, its pharmacological and chemical composition is highly variable, relative to its geography and botanical origins. Comparative studies on three propolis samples collected from different regions in Korea have been essential for linking its provenance, chemical composition, and biological activity, thereby ensuring the efficient utilization of its beneficial properties. Here, we report the chemical composition and biological activities such as the antioxidant, wound healing, and anti-inflammatory effects of the ethanolic extract of Korean propolis collected from two regions. We compared the chemical constituents of three 70% ethanol-extracted (EE) samples, including the Andong, Gongju field (GF), and Gongju mountain (GM)-sourced propolis using Gas chromatography–mass spectrometry (GC–MS). The major and common components of these EE Korean propolis were flavonoids such as pinocembrin (12.0–17.7%), chrysin (5.2–6.8%), and apigenin (5.30–5.84%). The antioxidant property using a 2,2-Diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity assay of EEP showed substantial differences among samples with the highest from Andong. The sample 10% GM levigated in simple ointment was found to be the most active in wound healing activity based on the excision, incision, and dead space wound models. The potential of propolis for wound healing is mainly due to its evidenced properties, such as its antimicrobial, anti-inflammatory, analgesic, and angiogenesis promoter effects, which need further study. The anti-inflammatory activity and NO production inhibitory effect were highest in GM samples. However, GM and GF samples demonstrated similar inhibitory effects on the expression of inflammatory mediators such as iNOS, IL-1β, and IL-6. The presence of a higher concentration of flavonoids in Korean EE propolis might be responsible for their promising wound healing, anti-inflammatory, and antioxidant properties. [ABSTRACT FROM AUTHOR]

• Seventy-eight metabolites were annotated in two Ziziphus species collected from different localities by UPLC-MS/MS. • Samples' segregation in OPLS model was relied on their species type rather than their origin. • The Chinese Z. jujuba was more efficient than piroxicam in downregulating TNF-α levels. • OPLS coefficient plots resulted in identifying the anti-inflammatory biomarkers. Ziziphus is a cosmopolitan genus that has several traditional applications. One of them is alleviation of inflammation. However, Ziziphus mechanisms and exact biomarkers in charge of this effect are not extensively studied. Therefore, the aim of this study is to explore the phytochemical variability between the leaves' extracts of two Ziziphus species gathered from diverse geographic localities, scrutinizing their in vitro anti-inflammatory effects, identifying the mechanisms and exact biomarkers accountable for these effects utilizing UPLC-MS/MS along with an in vitro multivariate statistical approach. Seventy-eight metabolites were annotated by UPLC-MS/MS. These metabolites were found to belong to different chemical classes such as alkaloids, terpenoids, and flavonoids. Multivariate statistical analysis revealed that samples' segregation was relied on their species type rather than their origin. Then, testing the effects of the studied extracts on the gene expression of four pro-inflammatory cytokines (IL-1β, IL-6, TNF-α, and INF-γ) using polymerase chain reaction (PCR) showed that Z. jujuba extract originating from China downregulated TNF-α to levels less than those caused by piroxicam, indicating its higher efficacy. The Orthogonal Projection to Latent Structures (OPLS) coefficient plots indicated that zizybeoside I, zizyphine G and lotusine G were among the most potential metabolites downregulating the inflammatory cytokine TNF-α. However, ebelin lactone, oxyphylline B and zizyvoside I were from the more prominent biomarkers responsible for the downregulation of IL-1β. Furthermore, zizyphursolic acid, oxyphylline B and mauritine H, were strongly correlated with the downregulation of IFN-ɣ and IL-6. This study is the first attempt to decipher the anti-inflammatory metabolites from different Ziziphus species, valorizing their significance as a valuable traditional medicine. [ABSTRACT FROM AUTHOR]

• Rose oil is used for medicinal, pharmaceutical, therapeutical purposes • Pharmacologically Damask Rose serves as an anti-HIV agent, source of antioxidant, antitussive usage, hypnotic uses, and anti-diabetic agent • Rose oil is reported to cure many physiological roles as well as psychological ailments of humans • Rose is prone to a number of pests viz., diseases, insect pests, nematodes, and weeds This review highlights recent advancements in the utilization of rose oil across medicinal, pharmaceutical, therapeutic, and clinical trials, as well as its integration into pest management strategies that significantly contribute to its economic value. The Damask Rose, recognized for its potent pharmacological properties, serves multiple roles including as an anti-HIV agent, antioxidant source, antitussive, hypnotic, anti-diabetic treatment, and tracheal system soother. There is a crucial focus on enhancing the content of aromatic monoterpenes and sesquiterpenes in Rosa damascena L. Clinical studies affirm that rose oil effectively addresses various physiological and psychological conditions such as pain relief, anxiety reduction, depression alleviation, respiratory system improvement, blood oxygenation, pulse regulation, skin temperature control, stress management, menstrual discomfort, and exhibits antifungal, antibacterial properties, and potential as a sex stimulant. Rose cultivation faces challenges from numerous pests including diseases, insects, nematodes, and weeds, which detrimentally affect yield and flower quality. Effective management of these pests ensures optimal returns for rose growers. [ABSTRACT FROM AUTHOR]

Gastric and duodenal ulcers are increasingly becoming global health burdens. The side effects of conventional treatments such as non-steroid anti-inflammatory drugs (NSAIDs), proton pump inhibitors (PPIs), antibiotics, and cytoprotective agents have necessitated the search for new medications. Plants are a rich source of active metabolites and herbal medicines have been used in the treatment of ulcers and cancers. In this study, we used in silico methods like molecular docking and MM-GBSA calculations to evaluate the effects of some anti-ulcer and anti-inflammatory phytochemicals on some key enzymes, cyclooxygenase (COX), and lipoxygenase (LOX), which are implicated in the protection and destruction of the gastric mucosa. The phytochemicals were retrieved from the literature and docked toward the binding sites of the three enzymes (COX-1, COX-2, and 5-LOX). Five compounds, rhamnetin, kaempferol, rutin, rosmarinic acid, and chlorogenic acid were observed to putatively bind to cyclooxygenase 2 (COX-2) and 5-lipoxygenase (5-LOX) but not to cyclooxygenase 1 (COX-1). The interaction mechanisms between these phytochemicals and the target proteins are discussed. The compounds' drug metabolism, pharmacokinetics, and toxicity have been evaluated to assess their suitability as potential next-generation anti-ulcer and anti-inflammatory drugs. [ABSTRACT FROM AUTHOR]

In search of new active molecules, a small focused library of novel 1,2,3-triazoles based chalcone derivatives has been efficiently prepared via the click chemistry approach. All the synthesized compounds were characterized with the help of IR, 1H NMR, 13C NMR and mass spectroscopic techniques. The synthesized novel 1,2,3-triazoles based chalcone derivatives evaluated for their anti-inflammatory and antioxidant activity. Furthermore, molecular modeling study could support these outcomes by demonstrating very good binding affinities at the active site of the cyclooxygenase 2 (COX-2) iterating the potential of this scaffold for further optimization. [ABSTRACT FROM AUTHOR]

Microalgae are considered promising sustainable sources of natural bioactive compounds to be used in biotechnological sectors. In recent years, attention is increasingly given to the search of microalgae-derived compounds with antioxidant and anti-inflammatory properties for nutraceutical or pharmacological issues. In this context, attention is usually focused on the composition and bioactivity of algae or their extracts, while less interest is driven to their biological features, for example, those related to morphology and cultivation conditions. In addition, specific studies on the antioxidant and anti-inflammatory properties of microalgae mainly concern Chlorella or Spirulina. The present work was focused on the characterization of the Chlorophyta Neochloris oleoabundans under two combinations of cultivation modes: autotrophy and glucose-induced mixotrophy, each followed by starvation. Biomass for morphological and biochemical characterization, as well as for extract preparation, was harvested at the end of each cultivation phase. Analyses indicated a different content of the most important classes of bioactive compounds with antioxidant/anti-inflammatory properties (lipids, exo-polysaccharides, pigments, total phenolics, and proteins). In particular, the most promising condition able to prompt the production of antioxidant algal biomass with anti-inflammatory properties was the mixotrophic one. Under mixotrophy, beside an elevated algal biomass production, a strong photosynthetic metabolism with high appression of thylakoid membranes and characteristics of high photo-protection from oxidative damage was observed and linked to the overproduction of exo-polysaccharides and lipids rather than pigments. Overall, mixotrophy appears a good choice to produce natural bioactive extracts, potentially well tolerated by human metabolism and environmentally sustainable. [ABSTRACT FROM AUTHOR]

This study aimed to develop a nano-biosystem by covalently binding recombinant laccase from Bacillus licheniformis (rLAC BL) to PEGylated silica-coated magnetic nanoparticles (EMNPs-PEG) and evaluate its cytotoxicity and anti-inflammatory properties on a pro-monocytic cell line. The active rLAC BL was purified from the bacterial culture with a yield of approximately 14 mg/L and purity of about 91 %. The physicochemical characteristics of EMNP-PEG-rLAC BL were confirmed using DLS, UV-Vis spectrum, FTIR, EDS, and SEM. The immobilized rLAC BL exhibited improved kinetic parameters compared to the bare enzyme. The IC 50 value for EMNP-PEG-rLAC BL (58.7 μg/mL) was lower than that of the bare enzyme after 48 hours of treatment on U937 cells. Both EMNP-PEG-rLAC BL and rLAC BL significantly decreased the expression levels of key cytokines (TNF-α, IL-6, IL-17, and IL-23) in LPS-stimulated cells, indicating promising anti-inflammatory properties of rLAC BL. Given the association between chronic inflammation and cancer, this newly developed enzyme-based nanobiomedicine holds potential as a therapeutic option for inflammatory conditions and malignant diseases. However, further research is needed to validate these findings and fully assess the therapeutic potential of LACs before clinical translation can be considered. [Display omitted] • Recombinant laccase (rLAC BL) was produced from Bacillus licheniformis. • The rLAC B was immobilized on PEGylated silica-coated magnetic nanoparticles. • Immobilization of rLAC BL notably enhanced enzyme affinity for its substrate. • Immobilized rLAC BL exhibited anti-inflammatory effects on the U937 cell line. [ABSTRACT FROM AUTHOR]

BACKGROUND: The stem of Abroma augusta contains mucilaginous polysaccharides having numerous ethnomedicinal properties. The present work aimed to develop a scalable ultrasonic‐assisted aqueous Abroma augusta mucilage (AAM) extraction (UAE) method and further explores its emulsifying property and toxicity concern. RESULTS: The combination of ultrasonic power (750 W), solid‐to‐liquid ratio (1:15) and temperature (348 K) gave the highest extraction yield of 2.28% with a diffusivity value of 3.85 × 10−9 m2 s−1, which was higher than aqueous extraction method using a kinetic model based on Fick's second law of diffusion. The extracted polysaccharide showed no toxicity as measured through 3‐(4,5‐dimethylthiazol‐2‐yl)‐2,5‐diphenyltetrazolium bromide (MTT) and lactate dehydrogenase (LDH) assay on RAW cell line. Additionally, the polysaccharide over its critical micelle concentration (400, 500, 600 and 700 μg mL−1) offered emulsifying properties with 0.5%, 1% and 5% oil (v/v). The emulsion with a polysaccharide concentration of 600 μg mL−1 with 5% oil (v/v) provides stability against coalescence for 3 days. CONCLUSION: The overall findings indicated that UAE of AAM polysaccharide can be used for an efficient extraction method, and the obtained polysaccharide is nontoxic in nature and bears emulsifying properties. © 2024 Society of Chemical Industry. [ABSTRACT FROM AUTHOR]

BACKGROUND: Giant salamander protein peptide is a peptide with rich functional properties. Giant salamander protein peptide KGEYNK (KK‐6) is a peptide with both antioxidant and anti‐inflammatory properties. The antioxidant and anti‐inflammatory mechanisms of KK‐6 are still unclear. When we studied the functional mechanism of KK‐6, we found that the antioxidant property of KK‐6 has a synergistic and promoting effect on anti‐inflammatory properties. RESULTS: KK‐6 enhances cellular resistance to LPS via the MAPK/NF‐κB signaling pathway, leading to increased levels of inflammatory factors: interleukin‐1β (764.81 ng mL−1), interleukin‐6 (1.06 ng mL−1) and tumor necrosis factor‐α (4440.45 ng mL−1). KK‐6 demonstrates potent antioxidant properties by activating the Nrf2 signaling pathway, resulting in elevated levels of antioxidant enzymes (glutathione peroxidase: 0.03 μg mL−1; superoxide dismutase: 0.589 μg mL−1) and a reduction in the concentration of the oxidative product malondialdehyde (967.05 μg mL−1). CONCLUSION: Our findings highlight the great potential of KK‐6, a peptide extracted from giant salamander protein, as a remedy for intestinal inflammation. Through its dual role as an antioxidant and anti‐inflammatory agent, KK‐6 offers a promising avenue for alleviating inflammation‐related damage and oxidative stress. This study lays the foundation for further exploration of giant salamander products and highlights their importance in health and novel food development. © 2024 Society of Chemical Industry. [ABSTRACT FROM AUTHOR]

In recent times, there has been a growing exploration of transition metal complexes as potential solutions for significant health challenges, including tuberculosis, microbes infection, and inflammation. Therefore, in our ongoing effort to identify biologically effective agents, Co(II), Ni(II), Cu(II), and Zn(II) metal complexes of H2L1–H2L2 hydrazone ligands were synthesized. The structural features of synthesized compounds were recognized by employing several techniques such as FT‐IR, 1H NMR, 13C NMR, powder x‐ray diffraction (XRD), UV‐Vis, ESR, TG‐DTA, mass spectrometry, and molar conductance measurements. The bonding of ligands via Ophenolic, Oenolic, and Nazomethine donor atoms and the attachment of the three water molecules with metal ion to form the octahedral structure of complexes were corroborated by different spectroscopic techniques. The anti‐tuberculosis, antimicrobial, and anti‐inflammatory activities of the synthesized compounds were assessed using the microplate alamar blue assay, serial dilution, and bovine serum albumin (BSA) methods, respectively, and highlighted the more potency of the complexes than ligands. The synthesized Cu(II) (9) and Zn(II) (10) metal complexes exhibited excellent ability to inhibit the growth of H37Rv strain of Mycobacterium tuberculosis in comparison to standard drug streptomycin. The Cu(II) (6 and 9) and Zn(II) (10) complexes showed superb ability as antimicrobial agents, whereas Cu(II) (5) and Zn(II) (6) complexes exhibited significant anti‐inflammatory ability. The in vitro findings on the antituberculosis activity were reinforced by a significant molecular docking study, which has become a crucial component of computational research utilizing the enzyme Mtb Pks13 thioesterase domain of M. tuberculosis. Additionally, in this research work, the absorption–distribution–metabolism–excretion–toxicity (ADMET) study sparked the compounds' drug‐like behavior. [ABSTRACT FROM AUTHOR]

Minor ginsenosides produced by β-glucosidase are interesting biologically and pharmacologically. In this study, new ginsenoside-hydrolyzing glycosidase from Furfurilactobacillus rossiae DCYL3 was cloned and expressed in Escherichia coli strain BL21. The enzyme converted Rb1 and Gyp XVII into Rd and compound K following the pathways: Rb1→Rd and Gyp XVII→F2→CK, respectively at optimal condition: 40 °C, 15 min, and pH 6.0. Furthermore, we examined the cytotoxicity, NO production, ROS generation, and gene expression of Gynostemma extract (GE) and bioconverted Gynostemma extract (BGE) in vitro against A549 cell lines for human lung cancer and macrophage RAW 264.7 cells for antiinflammation, respectively. As a result, BGE demonstrated significantly greater toxicity than GE against lung cancer at a dose of 500 µg/mL but in normal cells showed lower toxicity. Then, we indicated an enhanced generation of ROS, which may be boosting cancer cell toxicity. By blocking the intrinsic way, BGE increased p53, Bax, Caspase 3, 9, and while Bcl2 is decreased. At 500 µg/mL, the BGE sample was less toxic in normal cells and decreased the LPS-treated NO and ROS level to reduce inflammation. In addition, BGE inhibited the expression of pro-inflammatory genes COX-2, iNOS, IL-6, and IL-8 in RAW 264.7 cells than the sample of GE. In conclusion, FrBGL3 has considerable downstream applications for high-yield, low-cost, effective manufacture of minor ginsenosides. Moreover, the study's findings imply that BGE would be potential materials for anti-cancer and anti-inflammatory agent after consideration of future studies. [ABSTRACT FROM AUTHOR]

Alpinia monopleura is one of the endemic plants of Sulawesi, and it has an extensive distribution in the region. Research on chemical compounds and biological activities of A. monopleura is essential to continue as an effort to support the utilization of native plants for medicine. The extract was obtained using the maceration method. The chemical compounds in the extract were identified using Liquid Chromatography Mass Spectrometry (LCMS). Bovine Serum Albumin (BSA) and molecular docking methods were used to evaluate the anti-inflammatory activity. Ten compounds contained in the extract were successfully identified, E-para-coumaric acid (1), trans-ferulaldehyde (2), 3,5,6-trihydroxy-4',7-dimethoxyflavone (3), nevadensin (4), malvalic acid (5), ent-16α,17-hydroxy-19-kauranoic acid (6), 3',5-dihydroxy-7,4'-dimethoxy flavone (7), saurufuran B (8), 5-hydroxy-7,8,2'-trimethoxyflavanone (9) and dehydroabietic acid (10). The anti-inflammatory activity of extracts from rhizomes and stems of A. monopleura were 8.62 and 10.59 mg/L, respectively. Some flavonoids (9 and 7) can bind strongly to specific residues around the COX-2 active site, such as Ser530, thereby interfering with the function of the COX-2 enzyme and reducing the production of pro-inflammatory prostaglandins. Thus, A. monopleura extract has the potential to inhibit inflammatory responses through molecular regulation of the COX-2 enzyme. [ABSTRACT FROM AUTHOR]

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This study was to evaluate the effect of fermented Gardenia jasminoides Ellis by a mixture of Bacillus sp. DU-106 and Lactobacillus plantarum on alcoholic oxidative damage in HepG2 cells. The CCK-8 method was used to explore the optimal alcoholic oxidative damage modelling concentration and the intervention concentration of Gardenia jasminoides Ellis extract. The effect of fermented Gardenia jasminoides Ellis extract on antioxidant capacity indicators such as superoxide dismutase (SOD), catalase (CAT), glutathione peroxidase (GSH-Px) activity, malondialdehyde (MDA), glutathione (GSH) content, as well as the release of transaminase-like enzymes such as alanine aminotransferase (ALT), aspartate aminotransferase (AST), and lactate dehydrogenase (LDH), and indicators of evaluation of hepatic injury, such as pro-inflammatory cytokines (IL-1β, IL-6, and TNF-α), were detected. The results showed that Gardenia jasminoides Ellis extract (GE) and fermented Gardenia jasminoides Ellis extract (FGE) significantly increased the viability of ethanol- induced HepG2 cells (P<0.05), and compared with the model group (MN), GE and FGE significantly increased the cellular antioxidative stress, attenuated lipid peroxidation, reduced GSH depletion, lowered cytokine levels (P<0.01), reduced the release of AST, ALT and LDH in the cells, and improved ethanol-induced damage to HepG2 cell membranes. Among them, FEG had significant antioxidant and anti-inflammatory properties, which were potentially valuable for protecting HepG2 cells from alcoholic oxidative damage, and the present study provided useful clues for the development of food products with hepatoprotective function. [ABSTRACT FROM AUTHOR]

A bioassay-guided isolation on the plant Zanthoxylum armatum DC yielded compounds tambulin (1), and prudomestin (2), from ethyl acetate fraction which showed the highest ROS inhibiting activity (IC50 = 17.8 ± 1.1 µg/mL). Structure elucidation of pure compounds was done using mass and NMR spectroscopic techniques. Compounds 1 and 2 revealed potent ROS inhibition with IC50 = 7.5 ± 0.3 and 1.5 ± 0.3 µg/mL, respectively, as compared to standard ibuprofen (IC50 = 11.2 ± 1.9 µg/mL). Likewise, both compounds 1 and 2 showed potent antioxidant activity with IC50 = 32.65 ± 0.31 and 26.96 ± 0.19 µg/mL, respectively. In vitro studies were supported by molecular docking and drug-likeliness properties. In silico studies of 1 and 2 with cyclooxygenase-2 (COX-2) showed perfect binding affinity with binding energies of −8.4 and −8.6 kcal/mol, respectively, comparable to standard ibuprofen (−7.7 kcal/mol). Drug likeness and ADMET showed higher gastrointestinal absorption of 1 and 2 and no toxic impact. [ABSTRACT FROM AUTHOR]

Bacopa monnieri (L.) Wettst (Plantaginaceae), is traditionally used in many countries as neural tonic and memory enhancer, or to relieve acute pain and inflammation. This study described the isolation and identification of one new, bacomoside D3 (1), and seven known phenyl glycosides (2 − 8). The structures of isolates were established by analysis of their spectroscopic data or hydrolysis followed by HPLC analysis together with a comparison to those reported in the literature. These compounds were evaluated for antioxidant and anti-inflammatory activities. Among them, compounds 4 and 5 exhibited strong DPPH radical scavenging activity with IC50 values of 9.77 ± 0.08 and 3.50 ± 0.04 µM, respectively. Compounds 2 and 5 significantly inhibited TNF-α production in LPS-stimulated RAW264.7 cells with IC50 values of 40.60 ± 3.05 and 38.19 ± 1.75 µM, respectively. Furthermore, the active compounds could be efficient inhibitors of oxidants by interfering with the DPPH activity in silico study. [ABSTRACT FROM AUTHOR]

Inflammatory bowel disease (IBD) is a chronic inflammatory disorder of the gastrointestinal tract which affects millions of individuals worldwide. Despite advancements in treatment options, there is increasing interest in exploring natural interventions with minimal side effects. Cruciferous vegetables, such as broccoli, cabbage, and radishes, contain bioactive compounds known as glucosinolates (GLSs), which have shown promising effects in alleviating IBD symptoms. This review aims to provide a comprehensive overview of the physiological functions and mechanisms of cruciferous GLSs and their metabolites in the context of IBD. Reviewed studies demonstrated that GLSs attenuated all aspects of IBD, including regulating the intestinal microbiota composition, exerting antioxidant and anti-inflammatory effects, restoring intestinal barrier function, and regulating epigenetic mechanisms. In addition, a few interventions with GLS supplementation in clinical studies were also discussed. However, there are still several challenges and remaining knowledge gaps, including variations in animals' experimental outcomes, the bioavailability of certain compounds, and few clinical trials to validate their effectiveness in human subjects. Addressing these issues will contribute to a better understanding of the therapeutic potential of cruciferous GLSs and their metabolites in the management of IBD. [ABSTRACT FROM AUTHOR]