Antioxidant Effects Research Articles

Comprehensive Assessment of Schiff Base Derived from 4-Chloroaniline and 2-Formylphenol: Molecular Architecture, Experimental with Computational Bioactivity Profiling, Emphasizing Anticancer Efficacy Against Pulmonary and Mammary Carcinoma Cell Models

This study thoroughly analyses the structural and biological properties of a Schiff base compound synthesized from the condensation of 2-formyl phenol and 4-chloroaniline. Single crystal X-ray diffraction examination indicated that the compound crystallizes in the monoclinic space group P21/c, with unit cell parameters a = 13.4232(15) Å, b = 5.7860(6) Å, c = 14.699(2) Å, β = 106.048(6) °, and Z = 4. The molecular structure has an E configuration around the C=N double bond, with a bond length of 1.266(2) Å, and includes an intramolecular O—H⋯N hydrogen bond. Hirshfeld surface analysis elucidated intermolecular interactions inside the crystal lattice, emphasizing dominant hydrogen-hydrogen, hydrogen-chlorine, and carbon-hydrogen contacts. The chemical exhibited concentration-dependent antioxidant and anti-inflammatory effects. Studies on DNA interactions indicate van der Waals forces between the ligand and nucleic acid, whereas it demonstrated considerable binding affinity for BSA with a ΔG value of -6.9 kcal/mol. ADME study revealed values within the recommended range, indicating advantageous pharmacokinetic characteristics. PASS filter-based cytotoxicity predictions indicated significant anti-cancer efficacy against breast adenocarcinoma, small cell lung carcinoma, and lung cancer. Toxicological assessments in diverse models indicated no possible irritation to skin and ocular tissues, highlighting its safety profile for therapeutic use. This research advances our comprehension of Schiff bases with halogen substituents and their prospective uses in chemistry and biology.

Dietary Supplements and the Gut–Brain Axis: A Focus on Lemon, Glycerin, and Their Combinations

Dietary supplements are products taken orally, and they contain an ingredient intended to augment the diet. Many studies demonstrate clear alterations in microbe abundances and the production of microbiota-derived metabolites, such as short-chain fatty acids, following dietary changes. This review comprehensively explores the possible interactions among gut microbiota, lemon extracts, glycerin, and their mixture products. Lemon extracts/components are associated with a vast array of health benefits, including anti-inflammation, antioxidant, anti-atherosclerotic, and anti-diabetic effects. They are also associated with increased memory and decreased depression. Glycerin can reduce serum free fatty acids and mimic caloric restriction; its metabolites can function as a broad-spectrum antimicrobial. Additionally, glycerin has a dehydrating effect on the central nervous system and can reduce focal cerebral edema and improve performance by expanding plasma volume. However, it may also have side effects, such as hyperglycemia. Therefore, combined consumption of lemon extracts and glycerin may, in part, mitigate each other’s side effects while exerting their benefits. There is growing evidence that both lemon components and glycerin are metabolized by the gut microbiota and may modulate the intestinal microbiome composition. Therefore, gut microbiome alterations are also explored as an important mechanism in the gut–brain axis regulating various effects of these dietary supplements and their application in various noncommunicable neurological disorders.

Transcriptomic Analysis of the Protective Effect of Piperine on Orlistat Hepatotoxicity in Obese Male Wistar Rats.

Obesity is a risk factor for the development of noncommunicable diseases that impair the quality of life. Orlistat is one of the most widely used drugs in the management of obesity due to its accessibility and low cost. However, cases of hepatotoxicity have been reported due to the consumption of this drug. On the other hand, piperine is an alkaloid found in black pepper that has demonstrated antiobesity, antihyperlipidemic, antioxidant, prebiotic, and hepatoprotective effects. The aim of this study was to evaluate the protective effect of piperine on the toxicity of orlistat in liver tissue. Obese male rats were administered piperine (30 mg/kg), orlistat (60 mg/kg), and the orlistat-piperine combination (30 mg/kg + 60 mg/kg) daily for 6 weeks. It was observed that the orlistat-piperine treatment resulted in greater weight loss, decreased biochemical markers (lipid profile, liver enzymes, pancreatic lipase activity), and histopathological analysis showed decreased hepatic steatosis and reduction of duodenal inflammation. Transcriptomic analysis revealed that the administration of piperine with orlistat increased the expression of genes related to the beta-oxidation of fatty acids, carbohydrate metabolism, detoxification of xenobiotics, and response to oxidative stress. Therefore, the results suggest that the administration of orlistat-piperine activates signaling pathways that confer a hepatoprotective effect, reducing the toxic impact of this drug.

Integrating Network Pharmacology and Experimental Verification to Explore the Pharmacological Mechanisms of Cordycepin against Pulmonary Arterial Hypertension in Rats.

Pulmonary Arterial Hypertension (PAH) is a fatal disease with high morbidity and mortality. Cordycepin has anti-inflammatory, antioxidant and immune enhancing effects. However, the role of Cordycepin in the treatment of PAH and its mechanism is not clear. The Cordycepin structure and PAH-related gene targets were obtained from public databases. The KEGG and GO enrichment analysis of common targets was performed in DAVID. PPI networks were also mapped using the STRING platform. AutoDock Vina, AutoDockTools, ChemBio3D and Pymol tools were selected for molecular docking of key targets. The therapeutic effects of Cordycepin on PAH were observed in Monocrotaline (MCT)-induced PAH rats and platelet-derived growth factor BB (PDGFBB)-induced rat pulmonary artery smooth muscle cells (PASMCs). The right ventricular systolic pressure (RVSP) was detected. HE staining, Western Blot, Scratch assay, EDU and TUNEL assays were used, respectively. Through Network Pharmacology and molecular docking, the Cordycepin-PAH core genes were found to be TP53, AKT1, CASP3, BAX and BCL2L1. In MCT-induced PAH rats, the administration of Cordycepin significantly reduced RVSP, and inhibited pulmonary vascular remodeling. In PDGFBB-induced PASMCs, Cordycepin reduced the migration and proliferation of PASMCs and promoted apoptosis. After the Cordycepin treatment, the protein expressions of TP53, Cleaved CASP3 and BAX were significantly increased, while the protein expressions of p-AKT1 and BCL2L1 were significantly decreased in MCT-PAH rats and PDGFBB-induced PASMCs. This study identified that TP53, AKT1, CASP3, BAX, and BCL2L1 were the potential targets of Cordycepin against PAH by ameliorating pulmonary vascular remodeling, inhibiting the abnormal proliferation and migration of PASMCs and increasing apoptosis of PASMCs. which provided a new understanding of the pharmacological mechanisms of Cordycepin in the treatment of PAH.

Molecular mechanisms involved in therapeutic effects of natural compounds against cisplatin-induced cardiotoxicity: a review.

Cisplatin is a widely used chemotherapeutic agent for the treatment of various cancers. However, the clinical use of cisplatin is limited by its cardiotoxic side effects. The primary mechanisms implicated in this cardiotoxicity include mitochondrial dysfunction, oxidative stress, inflammation, and apoptotic. Numerous natural compounds (NCs) have been introduced as promising protective factors against cisplatin-mediated cardiac damage. The current review summarized the potential of various NCs as cardioprotective agents at the molecular levels. These compounds exhibited potent antioxidant and anti-inflammatory effects by interaction with the PI3K/AKT, AMPK, Nrf2, NF-κB, and NLRP3/caspase-1/GSDMD pathways. Generally, the modulation of these signaling pathways by NCs represents a promising strategy for improving the therapeutic index of cisplatin by reducing its cardiac side effects.

Modern aspects of therapy of metabolic associated liver disease in patients with type 2 diabetes mellitus

Metabolic associated fatty liver disease (MAFLD) is currently the most common liver disease. The main risk factors for its development are poor nutrition, sedentary lifestyle and obesity. MAFLD is associated with various cardiometabolic conditions – lipid metabolism disorders, cardiovascular pathology and carbohydrate metabolism disorders. The association of MAFLD and type 2 diabetes mellitus (DM) is common among patients, since these diseases have a common pathogenesis link – insulin resistance. The combination of these diseases has a mutual negative effect on each other and increases the risks of cardiovascular diseases, hospitalizations, as well as the risks of liver fibrosis progression. Therefore, the detection of MAFLD and its treatment in type 2 DM are extremely important to improve the patient’s prognosis. Diagnostics of MAFLD includes laboratory and instrumental research methods. The “gold standard” of diagnostics is considered to be liver biopsy, but due to the fact that this method is invasive, it is rarely used and only for differential diagnostics of MAFLD with other liver pathologies. The most accessible instrumental method for detecting liver steatosis is ultrasound. Treatment of MAFLD primarily involves lifestyle changes (rational nutrition with limitation of simple carbohydrates and animal fats, adequate physical activity) and weight loss. Also, hypoglycemic drugs used to treat type 2 diabetes (metformin, pioglitazone, glucagon-like peptide-1 agonists) can have a certain positive effect on MAFLD. Essential phospholipids, which have membrane-stabilizing, antioxidant and antifibrotic effects, are also an important component of MAFLD treatment. A number of domestic and foreign studies have shown the high efficiency of Essential Phospholipids both in relation to biochemical parameters in patients with a combination of type 2 diabetes and MAFLD, and in relation to ultrasound signs, improving the function and structure of the liver in MAFLD, as well as slowing the progression of liver fibrosis.

Research Progress of Maillard Reaction and its Application in Processing of Traditional Chinese Medicine

The Maillard reaction, also known as the ‘non-enzymatic browning reaction’, involves a reaction between reducing sugars and amino compounds, including amino acids and proteins. The Maillard reaction has been increasingly used in the production of traditional Chinese medicine and food. This study thoroughly examines the mechanism of the reaction, the factors that influence it and the techniques used for extracting, separating and purifying Maillard reaction products (MRPs) in food and Chinese medicine processing. Additionally, the article explores the physiological functions of MRPs, highlighting their antioxidant, hepato-protective, antibacterial, immune-boosting, anti-mutagenic, anti-inflammatory, health-promoting, detoxifying and antiviral effects. MRPs have diverse outcomes because of various influencing factors; they can contain trace amounts of potentially harmful constituents, such as acrylamide, 5-hydroxymethylfurfural and advanced glycosylation products. The study also includes a comparative analysis of common methods used for the separation and purification of concentrated MRPs. These methods consist of ultrafiltration, macroporous resin, gel chromatography, ion exchange chromatography and dialysis. Results indicate that each method has advantages and disadvantages, and thus careful consideration should be placed on specific applications. Furthermore, a future outlook for the research and development of Maillard reaction and its products is proposed. Given that the physiological activities of MRPs are diverse, thorough qualitative and quantitative analysis of the reaction mechanisms, influencing factors and pharmacologically active ingredients is needed. This study offers valuable insights into the advancement of MRPs for industries involved in food and traditional Chinese medicinal material processing. These insights can be effectively utilised in healthcare and clinical practice, offering innovative ideas for scientific and technological professionals involved in research and development.

Rosa indica Leaf Contains Molecules with Promising Antioxidant, Antimicrobial and Anticancer Effects in vitro with Strong Interaction with Human VEGFR2 in silico

Rosa indica Leaf Contains Molecules with Promising Antioxidant, Antimicrobial and Anticancer Effects in vitro with Strong Interaction with Human VEGFR2 in silico

DES/O microemulsion for solubilizing and delivering curcumin via the nasal administration to treat acute asthma

As a natural small molecule drug derived from turmeric, curcumin is known for its good biosafety and a range of beneficial effects, including anti-inflammatory, anti-spasmodic, antioxidant, antibacterial, anti-tumor, and neuroprotective effects. Even though, its insolubility in water and instability severely limit its bioavailability and clinical applications. The present study developed a deep eutectic solvent (DES) in oil microemulsion (DES/O-ME) system loaded with Cur for intranasal administration, aiming to enhance both the solubility and permeability of Cur to significantly increase its bioavailability. The project first constructed and screened the optimal choline chloride-based DES. Subsequently, the DES/O-ME system was prepared and optimized to achieve uniform particle size and stability using a pseudo-ternary phase diagram and electrical conductivity measurements. The resulting DES/O-ME system was thoroughly evaluated for its solubilization efficacy, permeability, mucosal cytotoxicity, and stability. Additionally, the therapeutic efficacy of the Cur-DES/O-ME was assessed in vivo using a murine model of allergic asthma. This comprehensive evaluation highlights the potential of the DES/O-ME system as a promising intranasal drug delivery platform to overcome the limitations of curcumin’s bioavailability and clinical application.

Spinacia Oleracea: Exploring the Therapeutic Potential in Persian Medicine and Modern Pharmacology.

Spinach is a widely cultivated dark leafy vegetable highly regarded for its medicinal properties in traditional Persian medicine. It is rich in vitamins, minerals, flavonoids, carotenoids, and other bioactive compounds, and this review aims to explore the historical applications of spinach in Persian medicine and juxtapose them with current scientific evidence. Despite its historical significance, there remains a need to comprehensively evaluate and integrate traditional knowledge with modern research on the therapeutic benefits of spinach. To achieve this, a comprehensive search was conducted in Persian medicine references and scientific databases to gather information on the traditional uses, chemical composition, and pharmacological effects of spinach. Studies that met the inclusion criteria were meticulously categorized, and relevant data were analyzed to draw insightful comparisons. Persian medicine describes spinach as a nutrient-rich, laxative, and fast-digesting agent with therapeutic effects on inflammation, lung diseases, back pain, sore throats, jaundice, urinary disorders, joint pain, eye inflammation, insomnia, dementia, and more. Modern studies have substantially corroborated these traditional uses, revealing that spinach possesses antioxidant, anti-inflammatory, anti-cancer, blood sugar-lowering, lipid-lowering, anti-obesity, neurological, ocular, and musculoskeletal effects. Spinach exhibits a wide range of beneficial effects on various health conditions. Its widespread availability, low cost, and exceptional nutritional richness position it as a promising candidate for further investigation. Future studies should explore the clinical effectiveness of spinach in various diseases, while taking into consideration the principles emphasized in Persian medicine to guide research and inform therapeutic strategies.

Phytochemical Characterization and Therapeutic Potential of Leaf of Emilia sonchifolia (L.) DC.: A Comprehensive Study on Functional Groups and Bioactive Compounds.

BackgroundEmilia sonchifolia (L.) DC is an annual herbaceous plant used in the Ayurveda and Unani therapeutic systems. It treats various conditions such as diarrhea, sore throat, night blindness, rashes, fever, measles, earache, eye inflammation, ophthalmia, asthma, malaria, stomach tumors, chest pain, liver diseases, cuts, and wounds. PurposeThis study aimed to assess the functional groups and bioactive compounds present in the leaves of E. sonchifolia using FT-IR and GC-MS analyses and explore their antioxidant, antidiabetic and anticancer effects. Materials and methodsDifferent leaf extracts of E. sonchifolia were subjected to Fourier transform infrared (FT-IR) and gas chromatography-mass spectrometry (GC-MS) analyses to determine the presence of functional groups and for chemical characterization. Biological evaluations such as antioxidant (DPPH and ABTS assays) and antidiabetic (α-amylase enzyme inhibition and glucose uptake using yeast cell assays) and anticancer (HepG2 cell lines) potentials were also analyzed. ResultsFT-IR analysis revealed the presence of various functional groups such as amines, alcohols, alkanes, alkenes, halo compounds, aldehydes, sulfates, esters, phenols, and carboxylic acids. GC-MS analysis revealed the presence of 32 bioactive compounds in different leaf extracts. Among the extracts, petroleum ether (16) contained the highest number of chemical compounds, followed by ethanol (14), chloroform (9), and acetone (4). Lanosterol (17.01%) was the most significant compound in petroleum ether extract, whereas phytol (44.05%) in the acetone extract and 1,2-benzenedicarboxylic acid in the chloroform (82.47%) and ethanol (50.49%) extracts. The ethanol leaf extract showed the highest antioxidant potential in DPPH (63.38±0.46µg/mL) and ABTS (60.74±0.59µg/mL) assays. It also showed better results in antidiabetic activity in both α-amylase enzyme inhibition (135.69±2.08µg/mL) and glucose uptake using yeast cell (114.37±1.71µg/mL) assays. Ethanol leaf extract exhibits good anticancer activity with 59.52±0.76µg/mL against HepG2 cell line. ConclusionFTIR and GC-MS analyses confirmed the presence of bioactive functional groups and phytoconstituents. These results justify the leaves as a traditional remedy in Ayurveda and Unani therapeutic systems. Antioxidant, antidiabetic and anticancer assays suggested that E. sonchifolia leaves have good antioxidant, antidiabetic and anticancer potential compared to standards. Further studies are required to identify the chemical compounds responsible for these activities.

Biological Potential and Therapeutic Effectiveness of Artemetin from Traditional to Modern Medicine: An Update on Pharmacological Activities and Analytical Aspects.

Plant products derived from natural sources have been used in medicine as a raw material and newer kinds of drug molecules in pharmaceuticals and other allied health sectors. Phytochemicals have numerous medicinal potentials, including anti- ageing, anti-carcinogenic, anti-microbial, anti-oxidant, and anti-inflammatory activity in medicine. Development and biological application of herbal products in modern medicine signified the value of traditional medicinal plants in health care systems. The objective of the present study was to explore the scientific knowledge of the medicinal importance and therapeutic potential of artemetin in medicine. However, scientific investigations for their pharmacological activities in medicine have been done through scientific data analysis of different scientific research work collected from PubMed, Google, Science Direct and Google Scholar in order to know the biological importance of artemetin in medicine. Moreover, analytical data of artemetin have also been discussed in the present work. The present work and scientific data signified the biological potential of artemetin in medicine. Artemetin has been derived from numerous medicinal plants and dietary herbs, including Artemisia absinthium, Artemisia argyi, Achillea millefolium, and Vitex trifolia. Artemetin has anti-malarial, anti-oxidant, anti-apoptotic, anti-microbial, antitumoral, anti-atherosclerotic, anti-inflammatory, hypotensive and hepatoprotective effects. Further, the biological role of artemetin on lipid oxidation, cytokine production, lipoxygenase, and estrogen-like effects was also investigated in the present work. Analytical data on artemetin in the present paper signified their important role in the isolation, separation, and identification of different classes of pure phytochemicals, including artemetin in medicine. Scientific data analysis of artemetin signified its therapeutic potential in medicine for the development of newer scientific approaches for different human disorders.

Synthesis, highly potent α-glucosidase inhibition, antioxidant and molecular docking of various novel dihydropyrimidine derivatives to treat diabetes mellitus

1,4-dihydropyrimidine-2-thiones were synthesized in five series that include 5-carboxylic acid derivatives of dihydropyrimidine (series A, 6–8), novel 5-carboxamide derivatives of dihydropyrimidine (series B, 9–14), N,S-dimethyl-dihydropyrimidine (series C, 15–20), N-hydrazinyl derivatives of dihydropyrimidine (series D, 21–24) and tetrazolo dihydropyrimidine derivatives (series E, 25–28), and evaluated for anti-diabetic capability. The prepared novel compounds were structurally established by FTIR, 1HNMR, 13CNMR, ESI and HRMS. All of these compounds from series A-E were first time examined for α-glucosidase inhibition as to evaluate their anti-diabetic potential. Most of the compounds for example 8, 11–14, 15, 17–21, 25 and 28 demonstrated greater α-glucosidase inhibitory effects (IC50 = 12.5 ± 0.21 to 47.3 ± 0.23 μM) when compared to deoxynojirimycin as standard (IC50 = 52.02 ± 0.36 μM). Compounds from series B and C found to be highly active however, the compounds from series D found generally less active. The structure–activity relationships demonstrated the importance of C-5 carboxamides, C-5 ethyl ester functionality, and the presence of N,S-dimethyl groups at pyrimidine ring for α-glucosidase inhibition. The docking studies demonstrated that all the active compounds have van der Waal and alkyl bonds interactions with the targeted site of the human lysosomal acid α −glucosidase. All these compounds were also tested for antioxidant potential by DPPH radical scavenging protocol that exhibited significant antioxidant effects (IC50 = 21.4 ± 0.45 to 92.1 ± 0.38 μM) as compared to the standard butylated hydroxyanisol (IC50 = 44.2 ± 0.36 μM). Among all, compound 13, 14 and 19 with potent α-glucosidase inhibition (IC50 = 18.9 ± 0.72, 23.3 ± 0.45 and 21.5 ± 0.16 µM, respectively) along with excellent antioxidant potential in the range of (IC50 = 21.4 ± 0.45 to 31.2 ± 0.23 μM) indicated their ability to use as valuable leads for the development of anti-diabetic drugs with the combined effects of antioxidants.

Inhibition of LPS-induced inflammatory response in RAW264.7 cells by natural Chlorogenic acid isomers involved with AKR1B1 inhibition

Inflammation is the physiological response of the immune system to injury or infection, typically manifested by local tissue congestion, swelling, heat, and pain. Prolonged or excessive inflammation can lead to tissue damage and the development of many diseases. The anti-inflammatory effects of natural ingredients have been extensively researched and confirmed. This study investigated the effects of Chlorogenic acid (CGA) isomers —— 3-Caffeolyquninic acid (3-CQA), 4-Caffeolyquninic acid (4-CQA), and 5-Caffeolyquninic acid (5-CQA) —— on the inflammatory response and oxidative stress reaction induced by LPS in RAW264.7 cells. Overall, 3-CQA exhibited the most significant reduction in levels of TNF-α, IL-6, NO, and ROS. 4-CQA showed superior inhibition of TNF-α compared to 5-CQA (p < 0.05), while no significant difference in other parameters. We further used DARTS and CETSA to demonstrate that CGA isomers have stable affinity with AKR1B1. As a positive control, the AKR1B1 antagonist epalrestat exhibited similar effects to the CGA isomers. 3-CQA having the smallest half-inhibitory concentration (IC50) for AKR1B1, while 4-CQA and 5-CQA have similar values. AutoDock simulations of the docking conformations revealed minimal differences in the average binding energies of the CGA isomers. The main differences were that VAL47 formed a hydrogen bond with 3-CQA, whereas GLN49 formed hydrogen bonds with 4-CQA and 5-CQA. Additionally, the number of hydrophobic bonds involving PHE122 and LEU300 varies. Our conclusion is that differences in non-covalent interactions result in the varying inhibitory abilities of CGA isomers on AKR1B1, which further affect the anti-inflammatory and antioxidant effects of CGA isomers.

Demyelination in cuprizone mice is ameliorated by Calycosin mediated through astrocyte Nrf2 signaling pathway

Oxidative stress plays a pivotal role in multiple sclerosis (MS), triggering demyelination predominantly through excessive peroxide production and the depletion of antioxidants. The accumulation of oxidative damage can be caused by dysregulation of astrocytes, which are the brain's main regulators of oxidative homeostasis. Calycosin, an essential bioactive component extracted from Astragalus, is recognized for its neuroprotective properties. Although recent research has highlighted calycosin's neuroprotective capabilities, its role in demyelinating conditions like MS remains unclear. In this work, we examined the possible molecular mechanism of calycosin's neuroprotective effect on cuprizone (CPZ)-induced demylination in mice. According to our research, calycosin successfully reduced demyelination and behavioral dysfuction in CPZ mice. Calycosin also decreased the production of oxidative stress and enhanced the expression of antioxidants in CPZ mice and in astrocytes induced by hydrogen peroxide (H2O2). Furthermore, both in vivo and in vitro experiments demonstrated that calycosin promoted the nuclear translocation of nuclear factor erythroid 2-related factor 2 (Nrf2) along with the upregulation of heme oxygenase 1 (HO-1), NAD(P)H quinone dehydrogenase 1 (NQO1), and superoxide dismutase (SOD). Importantly, the application of all-trans retinoic acid (ATRA), a specific inhibitor of Nrf2, effectively reversed the myelin-protective and antioxidant effects conferred by calycosin. This study suggested that calycosin might exert neuroprotection by inhibiting oxidative stress and reducing demyelination via the activation of astrocyte Nrf2 signaling. These findings indicated that calycosin might be a potential candidate for treating MS.

Enhanced chemiluminescence with sub-1 nanometer CuO-PMA nanosheets for the sensitive detection of quercetin

BackgroundChemiluminescence (CL) analysis, characterized by its simple instrumentation, high signal-to-noise ratio, wide linear range, and minimal background interference, has garnered increasing attention from researchers. Nanomaterials (NMs) have been explored to enhance CL intensity. Notably, sub-1 nanometer scale NMs are considered to hold significant untapped potential due to their size effects. The application of these sub-1 nanometer NMs in enhancing CL is anticipated to yield favorable results. Additionally, the low water solubility and bioavailability of quercetin glycosides lead to their presence in bodily fluids at only trace levels, highlighting the urgent need for efficient and rapid detection methods. ResultsIn this work, phosphomolybdic acid (PMA) was incorporated into CuO to synthesize sub-1 nanometer CuO-PMA nanosheets (SNSs) using a cluster-core co-assembly strategy. Conformational and structural characterization confirmed the successful synthesis of these nanosheets. The CuO-PMA SNSs were employed to enhance the CL emission of the luminol-H2O2 system, resulting in an increase of over 1000 times. The catalytic properties of CuO-PMA SNSs significantly facilitated the decomposition of H2O2, leading to an enhanced production of reactive oxygen species, which in turn induced the CL enhancement. Given that the antioxidant effect of quercetin would consume the reactive oxygen species generated during the catalysis, a decrease in CL intensity was anticipated. A CL sensor for quercetin detection was developed based on the CuO-PMA SNSs-luminol-H2O2 system, demonstrating a strong linear relationship (R2 = 0.9969) and a low detection limit of 0.31 nM. SignificanceThis research provides a strategy to enhance the CL intensity of the luminol-H2O2 system by using CuO-PMA SNSs, offering a highly sensitive assay for detecting quercetin concentrations. The method is characterized as a simple and cost-effective analytical strategy making CL analysis very attractive for chemical analysts.

Anti-diabetic and anti-inflammatory activities of Marrubiin isolated from Marrubium vulgare: Indications of its interaction with PPAR γ

BackgroundThe aerial parts of Marrubium vulgare L. were used for many ailments like catarrh to diabetes in many parts of Latin America and Asia. PurposeIdentifying the active principle responsible for anti-diabetic activity of methanol extract of M. vulgare leaves and to predict the possible targets. Study designAll the activity investigations were conducted simultaneously for the extract, fraction, and isolated compounds to decipher the activity profile in comparison to each other which allowed the identification of an active principle followed by use of in silico methods to identify the possible target/s. MethodsThe aerial parts of M. vulgare were extracted using methanol. A chloroform fraction was prepared. Marrubiin and marrubinone B were isolated from this fraction. The anti-hyperglycemic, hypoglycemic, and postprandial blood glucose lowering activities were investigated using streptozotocin-induced diabetic and non-diabetic rat models. Pro-inflammatory cytokine inhibitory potential was investigated using LPS induced acute-inflammatory mouse model and RAW 264.7 cells. Further, antioxidant activity was investigated using a DPPH assay. The in silico analysis, using the Swiss-target prediction tool, was carried out to predict the probable targets of the isolated molecules. ResultsMarrubiin exhibited anti-hyperglycemic effect in diabetic rats followed by hypoglycemia, and postprandial blood glucose lowering in non-diabetic rats. Methanol extract (Mv extract) and chloroform fraction (Mv fraction) showed anti-hyperglycemic and hypoglycemic effects. Moderate inhibition of IL-1β, TNF-α, and IL-6 was observed for marrubiin, marrubinone B, Mv extract, and Mv fraction, in vitro and in vivo. Neither marrubiin nor marrubinone B could quench the DPPH free radicals while Mv extract and Mv fraction could show 80 % suppression. In silico analysis has predicted that marrubiin can interact with PPAR γ but not marrubinone B. ConclusionsMarrubiin and marrubinone B were responsible for the anti-inflammatory effect of Mv extract and Mv fraction while not contributing to the antioxidant effect. Marrubiin was found to be responsible for the anti-diabetic activity of Mv extract. The predicted interaction propensity of marrubiin with PPAR γ could explain its dual activity observed in the experimental setup.

The Neuroprotective Mechanisms of PPAR-γ: Inhibition of Microglia-Mediated Neuroinflammation and Oxidative Stress in a Neonatal Mouse Model of Hypoxic-Ischemic White Matter Injury.

Neuroinflammation and oxidative stress, mediated by microglial activation, hinder the development of oligodendrocytes (OLs) and delay myelination in preterm infants, leading to white matter injury (WMI) and long-term neurodevelopmental sequelae. Peroxisome proliferator-activated receptor gamma (PPAR-γ) has been reported to inhibit inflammation and oxidative stress via modulating microglial polarization in various central nervous system diseases. However, the relationship between PPAR-γ and microglial polarization in neonatal WMI is not well understood. Therefore, this study aimed to elucidate the role and mechanisms of PPAR-γ in preterm infants affected by WMI. In this study, an invivo hypoxia-ischemia (HI) induced brain WMI neonatal mouse model was established. The mice were administered intraperitoneally with either RSGI or GW9662 to activate or inhibit PPAR-γ, respectively. Additionally, an invitro oxygen-glucose deprivation (OGD) cell model was established and pretreated with pcDNA 3.1-PPAR-γ or si-PPAR-γ to overexpress or silence PPAR-γ, respectively. The neuroprotective effects of PPAR-γ were investigated invivo. Firstly, open field test, novel object recognization test, and beam-walking test were employed to assess the effects of PPAR-γ on neurobehavioral recovery. Furthermore, assessment of OLs loss and OL-maturation disorder, the number of myelinated axons, myelin thickness, synaptic deficit, activation of microglia and astrocyte, and blood-brain barrier (BBB) were used to evaluate the effects of PPAR-γ on pathological repair. The mechanisms of PPAR-γ were explored both invivo and invitro. Assessment of microglia polarization, inflammatory mediators, reactive oxygen species (ROS), MDA, and antioxidant enzymes was used to evaluate the anti-inflammatory and antioxidative effects of PPAR-γ activation. An assessment of HMGB1/NF-κB and NRF2/KEAP1 signaling pathway was conducted to clarify the mechanisms by which PPAR-γ influences HI-induced WMI in neonatal mice. Activation of PPAR-γ using RSGI significantly mitigated BBB disruption, promoted M2 polarization of microglia, inhibited activation of microglia and astrocytes, promoted OLs development, and enhanced myelination in HI-induced WMI. Conversely, inhibition of PPAR-γ using GW9662 further exacerbated the pathologic hallmark of WMI. Neurobehavioral tests revealed that neurological deficits were ameliorated by RSGI, while further aggravated by GW91662. In addition, activation of PPAR-γ significantly alleviated neuroinflammation and oxidative stress by suppressing HMGB1/NF-κB signaling pathway and activating NRF2 signaling pathway both invivo and invitro. Conversely, inhibition of PPAR-γ further exacerbated HI or OGD-induced neuroinflammation, oxidative stress via modulation of the same signaling pathway. Our findings suggest that PPAR-γ regulates microglial activation/polarization as well as subsequent neuroinflammation/oxidative stress via the HMGB1/NF-κB and NRF2/KEAP1 signaling pathway, thereby contributing to neuroprotection and amelioration of HI-induced WMI in neonatal mice.

Troxerutin associated with Agaricus blazei Murill polysaccharides in films improves full-thickness wound healing

The present study aimed to associate troxerutin (TRX) with polysaccharides from Agaricus blazei Murill mushroom (PolyAb) in alginate/PVA films and evaluate their effect on wound healing. The physicochemical, mechanical, morphological, and water vapor barrier properties of the films were studied, and their biological potential was analyzed in vivo using the full-thickness wound healing model. The association between TRX and PolyAb present in the polymeric film contributed to increased thermal stability, mechanical resistance, and elasticity when compared to films without TRX, which indicated good miscibility of the excipients. In the in vivo tests, the TRX films promoted greater collagen deposition and repair of epidermis and dermis layers. The 0.25 % TRX film showed an increase in reduced glutathione levels, while the 1.0 % TRX film reduced lipid peroxidation and production of the pro-inflammatory cytokine IL-1β, demonstrating the anti-inflammatory and antioxidant effect of TRX films. Therefore, it is estimated that the film containing 1 % TRX can be used as biocurative for wound dressing applications.

Antioxidant effect and protective effect of Salvia plebeia extract against H2O2-induced oxidative stress in neuronal cell

Antioxidant effect and protective effect of <i>Salvia plebeia</i> extract against H₂O₂-induced oxidative stress in neuronal cell