Significant Scavenging Effect Research Articles

Anti-Inflammatory and Antioxidant Effects of Liposoluble C60 at the Cellular, Molecular, and Whole-Animal Levels.

Liposoluble carbon-60 (C60) has potential applications in many fields, including cosmetics, medical devices, and medicine, but its specific mechanism of action remains unclear. This study explored whether liposoluble C60 could be delivered to human organs, tissues, and cells through blood, extracellular fluid, and cell culture fluid and whether it exerts anti-inflammatory and antioxidant effects at the molecular, cellular, and whole-animal levels. At the cellular level, we mixed C60 dissolved in grape seed oil with cell culture medium containing 10% serum and investigated its effects on tumor necrosis factor-α (TNF-α) release, migration, phagocytosis, respiratory burst, and apoptosis in freshly isolated human neutrophils. At the molecular level, we mixed a trace amount of C60 dissolved in grape seed oil with aqueous and ethanolic solutions and studied its antioxidant effect. At the animal level, we investigated the inhibitory effect of C60 on the serum inflammatory marker C-reactive protein (CRP) in beagle dogs after oral administration of C60 dissolved in grape seed oil. The results showed that the trace amount of C60 dissolved in grape seed oil significantly inhibited TNF-α release, cell migration, phagocytosis, and respiratory burst in freshly isolated human neutrophils. In addition, the trace amount of C60 dissolved in grape seed oil had a significant scavenging effect on superoxide free radicals and 1,1-diphenyl-2-trinitrophenylhydrazine free radicals. Oral administration of C60 dissolved in grape seed oil markedly reduced the level of the serum inflammatory marker CRP in beagle dogs. In summary, a trace amount of hydrophobic C60 in hydrophilic media effectively produced anti-inflammatory and antioxidant effects in cells and animals. C60 dissolved in grape seed oil is a novel anti-inflammatory and antioxidant drug candidate.

Unsaturated guluronate oligosaccharide used as a stabilizer of oil-in-water nanoemulsions loaded with bioactive nutrients.

Unsaturated guluronate oligosaccharide (GOS) is generated via alginate-derived polyguluronate (PG) degradation by alginate lyase, followed by formation of a double bond between C-4 and C-5 at the nonreducing end. In this study, GOS was first used as a stabilizer to fabricate O/W nanoemulsions loaded with resveratrol (GOS-RES). Our results revealed that both the GOS-RES and normal O/W resveratrol nanoemulsions (water-RES) showed small droplet sizes and narrow size distributions under certain experimental conditions. However, the particle size and stability of the GOS-RES were slightly greater than those of the water-RES in acidic and neutral environments and at high temperatures. Furthermore, the GOS-RES exhibited a better sustained release effect for resveratrol than the water-RES. Moreover, the GOS-RES showed a significant superoxide radical scavenging effect. All these results demonstrated that GOS has good prospects for preparing nanoemulsions to encapsulate hydrophobic nutrients, which could be applied as food-grade components in beverages and other foods.

Antimicrobial, antioxidant and anticancer activity of Ephedra alata growing in East of Libya1

Introduction: The plant Ephedra alata belongs to the Ephederiaceae family. These plants distributed in North Africa, Palestine, Libya, Egypt, Saudi Arabia, and Iraq. Ephedra alata has been commonly used in folk medicine in Libya and most of the Arabian countries for treatment of asthma, hay fever, and the common cold. Aim: This study aimed to investigate the phyto-constituents and to assess its anti-microbial, antioxidant activities, in addition, to study its cytotoxic effect. Methods: The aerial part dried of the plant was subjected to a phytochemical screening and investigated for their antimicrobial activity, antioxidant effect, and cytotoxic effects. Results: The phytochemical investigation of the methanolic extracts of Ephedra alata revealed the presence of alkaloids, carbohydrates, flavonoides, steroids, tannins, and phenolic compounds. The results of anti-microbial activity revealed that; there was a significant antibacterial activity against representatives of Gram positive (Staphylococcus aureus, Bacillus subtilis) and Gram-negative (Escherichia coli, Pseudomonas aeruginosa), while there was no antifungal effect against Aspergillusflavus and Candida albicans. In terms of antioxidant activity, the methanolic extract of Ephedra alata showed a significant scavenging effect on the DPPH radical, compared to gallic acid. The results showed an honest correlation between antioxidant activity and flavonoid content. The plant extract displayed a significant cytotoxic effect on MCF7with IC50 and IC90 comparing with doxorubicin as a positive control. Conclusion: The results indicated that the extract of Ephedra alata had significant antioxidant, and cytotoxic effects in addition to their antimicrobial activity

Protective activity of Malus doumeri leaf extract on H2O2-induced oxidative injury in H9C2 rat cardiomyocytes.

In this study, Malus doumeri leaf extract (MDLE) was used to test its anti-oxidation capacity in vitro, it has been preliminarily analyzed for H2O2-induced oxidative damage in H9C2 cells and its main active components. The antioxidant capacity through DPPH (1, 1-Diphenyl-2-Picrylhydrazyl), ABTS+• [2,2,2'-azino-BIS-(3-ethylbenzo-thiazoline-6-sulfonic acid)] radical ion, •OH (hydroxyl radical), and (superoxide anion) were determined in vitro. The proliferation of H9C2 cells was examined by MTT [3-(4,5-Dimethyl-2-thiazolyl)-2,5-diphenyl-2-H-Tetrazolium bromide]. MDA (malondialdehyde), SOD (superoxide dismutase), CAT (catalase), GSH (glutathione), and GSH-Px (glutathione peroxidase) were determined by colorimetry. Apoptosis induced by oxidative damage was detected by flow cytometry. The mRNA expression of antioxidant related genes of SOD, CAT, GSH, and GSH-Px were checked by qRT-PCR (quantitative real-time polymerase chain reaction). The MDLE main active components were analyzed by HPLC (high-performance liquid chromatography). MDLE had significant scavenging effects on DPPH, ABTS+•, •OH, and superoxide anion radicals in a concentration-dependent manner. H2O2 treatment could significantly lead to oxidative stress injury of H9C2 cells, and MDLE treatment significantly improved the degree of H9C2 cell damage, and showed a positive correlation with concentration. MDLE can also reduce apoptosis caused by oxidative damage. MDLE treatment could significantly reduce MDA content and increase CAT, SOD, GSH, and GSH-Px contents and expression. In addition, by HPLC analysis, the following six bioactive components were detected from MDLE: chlorogenic acid, isoquercitrin, quercetin, baicalin, and phloretin. Therefore, MDLE has a good protective effect on myocardial cells.

Network pharmacology, molecular docking and in vivo and in vitro experiments to explore the molecular mechanism of licorice green tea beverage to scavenge oxygen free radicals.

Excessive oxygen free radicals can lead to aging, cancer, and other diseases. Therefore, searching for effective antioxidants to scavenge oxygen free radicals has become the focus of modern medicine. In this study, the molecular mechanism of Licorice Green Tea Beverage (LGTB) in scavenging oxygen free radicals was investigated by means of network pharmacology, molecular docking and experimental verification. Network pharmacology studies have shown that paeonol, eugenol, cinnamaldehyde, swertisin, rutin, glycyrrhetinic acid, oleic, pelargonidin-3-O-glucoside and quercetin, kaferempol were the main active components of LGTB, and SOD and CAT are important targets for LGTB in scavenging oxygen free radicals. The results of molecular docking showed that these representative compounds had good affinity to SOD and CAT target proteins. In vitro free radical scavenging experiments showed that LTGB had significant scavenging effects on both DPPH and ABTS radicals, and had strong total reducing power. In vitro cell experiments showed that LGTB could protect HaCaT cells from oxidative stress induced by H2 O2 . The mechanism of LGTB was related to the increase of SOD and CAT activity. Western blotting showed that LGTB could inhibit PI3K/AKT/HIF-1 signaling pathway and improve the antioxidant capacity of HaCaT cells. In vivo experiments showed that LGTB could significantly increase mouse visceral index, increase serum SOD and GSH-Px activity, decrease the content of MDA, and improve liver and kidney pathological state. This study reported the molecular mechanism of LTGB scavenging oxygen free radicals, which provided scientific basis for the treatment and clinical research of aging and other diseases caused by excessive free radicals. PRACTICAL APPLICATIONS: Free radicals are produced by the normal response of cells during aerobic respiration and perform various functions, such as signaling and providing protection against infection. However, excessive free radicals can lead to aging, cancer, and other diseases. The antioxidant can overcome the harm caused by excessive free radicals. In this study, we investigated the molecular mechanism of scavenging oxygen free radicals of Licorice Green Tea Beverage (LGTB) through network pharmacology and molecular docking, and its efficacy was verified by free radical scavenging experiment in vitro, HaCaT cell oxidative stress injury induced by H2 O2 , D-galactose to establish an aging model in mice and Western blotting experiment. It not only elucidates its mechanism at the system level, but also proves its validity at the biological level. It provides the theoretical basis and experimental evidence for the follow-up research and promotion of the product.

Evaluation of antioxidant and antibacterial effects of lactobacilli metabolites- preconditioned bone marrow mesenchymal stem cells in skin lesions amelioration

Background and ObjectivesMesenchymal stem cells (MSCs) therapeutically intensify wound-healing. Meanwhile, probiotics are capable to inhibit pathogenic bacteria by secreting antimicrobial and antioxidant agents. They ameliorate more the wounds, by MSCs' synergistic effect. Methods and ResultsThis way, MSCs exposed to probiotics metabolites (the extracts of Lactobacillus plantarum and Lactobacillus casei), become more viable, and the optimum doses of probiotics metabolites were determined by Trypan blue and MTT assays. Then, preconditioned MSCs (pre-MSCs) faced again the oxidative stress (100 µM H2O2), and their survival rate was assessed by MTT assay. Conditioned medium (CM) prepared from pre-MSCs and the expression rate of antioxidant proteins evaluated by Real-time PCR. The antimicrobial activity of the samples was evaluated using the MIC method. Then mice wound models were treated with the mixture of a basal ointment and each CM of pre-MSCs. The proliferation and viability of MSCs improved by the probiotic’s metabolites preconditioning (P ≤ 0.05). pre-MSCs exhibited significant up-regulated in antioxidant genes expression (P ≤ 0.001). Also, probiotics metabolites presented a significant free radical scavenging effect (P ≤ 0.001). CMs of pre-MSCs showed considerably increased antibacterial activity (P ≤ 0.05). Experimental groups compared with the controls revealed that wound contraction was more rapid in groups that received CMs of LP-MSCs, LC-MSCs, MSCs, and then finally mixed probiotics metabolites, respectively. ConclusionsThese results provide a novel insight into the probiotics extract effect on the improvement of MSCs’ potential for wound healing procedures.

Antioxidant and Immune-Modulating Activities of Egg Yolk Protein Extracts.

Egg yolk is widely used to extract lecithin, which is utilized in the food and cosmetics industry. After lecithin is removed, the rest of egg yolk is generated as a by-product. Thus, it is necessary to properly utilize it. In this study, egg yolk protein extracts were produced using ethanol (EYE-E) and water (EYE-W). Their antioxidant and immunomodulatory effects were then evaluated. Antioxidant activities of EYE-E and EYE-W were determined using cellular antioxidant capacity (CAC) assay and comet assay. EYE-E and EYE-W showed significant (p<0.05) scavenging effects on intracellular reactive oxygen species (ROS) in a dose dependent manner. At a concentration of 50 μg/mL, EYE-W showed higher (p<0.05) antioxidant activity than EYE-E. EYE-E and EYE-W also exhibited protective effects against DNA damage caused by oxidative stress. After treatment with EYE-E and EYE-W, DNA damage level of 48.7% due to oxidative stress was decreased to 36.2% and 31.8% levels, respectively. In addition, EYE-E and EYE-W showed immunomodulatory effects by regulating Th1 cytokines (TNF-α and IL-2) and Th2 cytokines (IL-10 and IL-4) in Balb/c mouse splenocytes. These data suggest that EYE-E and EYE-W could be used as functional food ingredients with excellent antioxidant and immunomodulatory activities in the food industry.

Conjugated Dienones from Differently Substituted Cinnamaldehyde as Highly Potent Monoamine Oxidase-B Inhibitors: Synthesis, Biochemistry, and Computational Chemistry.

Fifteen multiconjugated dienones (MK1–MK15) were synthesized and evaluated to determine their inhibitory activities against monoamine oxidases (MAOs) A and B. All derivatives were found to be potent and highly selective MAO-B inhibitors. Compound MK6, with an IC50 value of 2.82 nM, most effectively inhibited MAO-B, like MK12 (IC50 = 3.22 nM), followed by MK5, MK13, and MK14 (IC50 = 4.02, 4.24, and 4.89 nM, respectively). The selectivity index values of MK6 and MK12 for MAO-B over MAO-A were 7361.5 and 1780.5, respectively. Compounds MK6 and MK12 were competitive reversible inhibitors of MAO-B, with Ki values of 1.10 ± 0.20 and 3.0 ± 0.27 nM, respectively. Cytotoxic studies showed that MK5, MK6, MK12, and MK14 exhibited low toxicities on Vero cells, with IC50 values of 218.4, 149.1, 99.96, and 162.3 μg/mL, respectively, which were much higher than those for their effective nanomolar-level concentrations. Also, MK5, MK6, MK12, and MK14 decreased cell damage in H2O2-induced cells via a significant scavenging effect of reactive oxygen species. Molecular modeling was performed to rationalize the potential inhibitory activities of MK5, MK6, MK12, and MK14 toward MAO-B and their possible binding mechanisms, showing high-affinity binding pocket interactions and conformation perturbations of the compounds with MAO-B, which were interpreted as the conformational dynamics of MAO-B. This study concluded that all the compounds tested were more potent MAO-B inhibitors than the reference drugs, and leading compounds could be further explored for their effectiveness in various kinds of neurodegenerative disorders.

GC-MS Analysis, Molecular Docking and Hepatoprotective Effect of Ethanolic Extract of Capparis zeylanica on CCl4-Induced Hepatotoxicity in Rats

Capparis zeylanica (Capparaceae) is a climbing shrub, commonly known as ‘Asadua’ in Oriya language. Folkloric it is used as anti-inflammatory, anti-rheumatic, hepatitis and liver tonics. The present work aimed to investigate the hepatoprotective activity of Capparis zeylanica root. The ethanolic extract was subjected to GC-MS analysis and quantification of rutin, quercetin and gallic acid by HPLC. In vitro antioxidant study was evaluated by DPPH, nitric oxide radical and hydrogen peroxide assay. Hepatoprotective activity was performed by CCl4 (1.25 ml/kg, I.P) induced Wistar albino rats at dose of 200 and 300 mg/kg using silymarin (100 mg/kg) as standard. The liver tissue homogenate was examined for lipid peroxidation, SOD, CAT and GSH assay. Serum was taken for biochemical analysis and liver for histopathological study. In silico molecular docking study was performed by the indentified compounds. Gallic acid was quantified as highest in HPLC analysis. Fifty compounds were identified by GC-MS analysis. The extract exhibited significant free radical scavenging effect at highest concentration. The level of liver function enzymes (AST, ALT and ALP), bilirubin and protein were significantly improved after the administration of 200 and 300 mg/kg of extract. Alterations in SOD, CAT, GSH and lipid peroxidation levels were significantly checked by extract. Compounds propane, 1, 1-dipropoxy- (-5.2); cis-9-hexadecenal (-6.0); 17-octadecen-14-yn-1-ol (-6.0); 6-butyl-1,4-cycloheptadiene (-6.5) exhibited greater docking score as compared to standard silymarin (-5.1). The hepatoprotective potential of C. zeylanica could be due to its antioxidant effect and the synergistic effect of these compounds.

Artemisinin and Procyanidins loaded multifunctional nanocomplexes alleviate atherosclerosis via simultaneously modulating lipid influx and cholesterol efflux

The development of new reagents combining with nanotechnology has become an efficient strategy for improving the immune escaping ability and increasing local drug concentration for natural compounds with low therapy efficiency. In this study, we prepared biomimetic membrane-coated Prussian blue nanoparticles (PB NPs) for the treatment of atherosclerosis, using the function of Artemisinin (ART) and Procyanidins (PC) on the lipid influx and cholesterol efflux of macrophages, two logical steps involved in the plaque progression. In vitro results indicated that the prepared nanocomplexes have significant scavenging effect on ROS and NO, followed by inhibiting NF-κB/NLRP3 pathway, leading to the suppression of lipid influx. Meanwhile, they can notably reduce the uptake and internalization of oxLDL through significantly enhancing AMPK/mTOR/autophagy pathway, accompanied by promoting cholesterol efflux. In vivo study showed that the improved biocompatibility and immune-escape ability of nanocomplexes allowed less drug clearance during the circulation and high drug accumulation in the atherosclerotic plaque of ApoE−/− mice model. More importantly, the ART and PC co-loaded nanocomplexes showed the high efficacy against atherosclerosis of ApoE−/− mice model with both 8-week low dosage treatment or 1-week high dosage treatment. These findings indicated that ART and PC co-loaded nanocomplexes was promising for the targeted treatment of atherosclerosis.

Comparative assessment of phenolics, antioxidant and antiproliferative activities between Hippophae rhamnoides ssp. sinensis and H. tibetana leaf in Qinghai-Tibet Plateau

Hippophae rhamnoides ssp. sinensis (Rha) and H. tibetana (Tib) are two species of sea buckthorn which distribute in Qinghai-Tibet Plateau. Our results showed that both sea buckthorn leaf exhibited high total phenolic and flavonoid content, and Rha leaf showed much higher level. In addition, 66 phenolic compounds were detected, belonging to classes of benzoic acid derivatives, flavonols, flavanols, flavanones, and so on. Classes of benzoic acid derivatives and flavonols were most abundant, among them ellagic acid and rutin were the most and second abundant phenols. Besides, methyl gallate, 2,6-dihydroxybenzoic acid, 4-hydroxybenzoic acid, gentisic acid, narcissin, astragalin, nicotiflorin, prunin, procyanidin B3, cyanidin 3-O-rutinoside chloride, delphinidin 3-glucoside, gallocatechin, taxifolin, aromadendrin and trans-3,3′,4′,5,5′,7-Hexahydroxyflavanone were the first time to be identified in SBT leaf. Furthermore, significant free radical scavenging effects of ABTS and DPPH, ferric reducing antioxidant ability, cellular antioxidant properties and anti-proliferation activity against HepG2 cells were observed in the aqueous ethanol extracts of sea buckthorn leaf. While Rha showed stronger inhibitory effects, which might due to the higher content of total phenolic and flavonoid profiles. Our finding clearly supported that Rha leaf as a wild and non-pollution plant could be a better choice as a healthy food resource.

Design, preparation and in vitro characterization of biomimetic and bioactive chitosan/polyethylene oxide based nanofibers as wound dressings

Chitosan-based nanofibers (CS-NFs) are excellent artificial extracellular matrices (ECMs) due to the resemblance of CS with the glycosaminoglycans of the natural ECMs. Despite this excellent feature, the poor electrospinnability and mechanical properties of CS are responsible for important limitations in respect to its biomedical applications. To improve the CS's physico-chemical properties, new bioactive and biomimetic CS-NFs were formulated with polyethylene oxide (PEO), having incorporated different active components (ACs) with important beneficial effects for healing. Manuka honey (trophic and antimicrobial effects), propolis (antimicrobial effects), Calendula officinalis infusion (antioxidant effect, reepithelialization stimulating agent), insulin (trophic effect), and L-arginine (angiogenic effect) were selected as ACs. SEM morphology analysis revealed well-alignment, unidirectional arrays, with small diameters, no beads, and smooth surfaces for developed CS_PEO-ACs NFs. The developed NFs showed good biodegradability (NFs mats lost up to 60% of their initial weight in PBS), increased hemocompatibility (hemolytic index less than 4%), and a reduced cytotoxicity degree (cell viability degree more than 90%). In addition, significant antioxidant and antimicrobial effects were noted for the developed NFs which make them suitable for chronic wounds, due to the role of oxidative stress and infection risk in delaying normal wound healing. The most suitable for wound healing applications seems to be CS_PEO@P_C which showed an improved hemolysis index (2.92 ± 0.16%), is non-toxic (cell viability degree more than 97%), and has also significant radical scavenging effect (DPPH inhibition more than 65%). In addition, CS_PEO@P_C presents increased antimicrobial effects, more noticeably for Staphylococcus aureus strain, which is a key feature in preventing wound infection and delaying the healing process. It can be concluded that the developed CS/PEO-ACs NFs are very promising biomaterials for wound care, especially CS_PEO@P_C.

Nutritional significance and therapeutic potential of Moringa oleifera: The wonder plant.

Moringaoleiferais a multi-purpose plant and a comprehensive source of dietary components such as proteins, essential amino acids, vitamins, antioxidants, etc. The plant is also a rich source of other bioactive components, including flavonoids, glucosinolates, isothiocyanates, alkaloids, terpenoids, phenolics, etc. Incorporating M. oleifera in diet can improve the nutritional status of pregnant and nursing mothers and helps to combat malnutrition and iron deficiency anemia (IDA) among children. The phytochemicals and secondary metabolites, especially the polyphenolic compounds from Moringa, have a significant free-radical scavenging effect attributed to this plant's therapeutic potential. Investigations targeting to explore M. oleifera for its nutritional makeup, novel bioactive components, and analysis of their health-promoting attributes have received much attention. This review demonstrates an overview of recent (past ten years) advancements and patenting activity in discovering different parts of M. oleifera plant for providing adequate nutritive and bioactive components. The pharmacological potential and action mechanisms of M. oleifera in many diseases like diabetes mellitus, cancer, hypertension, ulcer, etc., are also discussed. PRACTICAL APPLICATIONS: Moringa oleifera is a vital plant that has a varied set of nutritional and therapeutic properties. The indigenous components of Moringa can treat humankind of its diseases and contribute to overall health. The qualitative and functional characteristics of its components indicate possible commercial exploitation of this high-value plant by utilizing its plant parts in many proprietary medicines and nutraceuticals. In conclusion, the Moringa plant needs to be used commercially. It can lead to tremendous economic development if the industries and researchers exploit its potential for highly nutritional super food and therapeutic application by undertaking further research to corroborate earlier studies.

In vitro Screening of Potential Antioxidative and Toxicity of the Stembark Extracts from Sterculia setigera Del.

The current investigation deals with the in vitro antioxidative and toxicity effects of methanol and chloroform extracts from the stem bark of Sterculia setigera . The stem bark of the plant was extracted using organic solvents (methanol and chloroform) to afford methanol extract (ME) and chloroform extract (CE). The extracts were evaluated for antioxidative potentials using 2.2-diphenyl-1-picrylhydraxyl (DPPH) radical, also toxicity effect of the methanol extract was investigated against Artemia salina larvae . The antioxidative effects for the extracts uncovered promising activity on the DPPH with significant scavenging effects of 80.64% and 18.3% at 1000 and 7.813 µg/mL respectively. These values were found to be comparable with those of ascorbic acid (97.80 and 49.62%) and butylated hydroxytoluene (94.44 and 20.98%). The methanol extract was found to be as toxic as the positive control (potassium dichromate) with LC 50 values of 1.64 µg/mL and 1.42 µg/mL, respectively. The antioxidative and cytotoxicity properties of methanol extract from S. setigera supported the ethno-medicinal claims on the plant as a curative agent of different diseases of clinical concern.

Depletion of Macrophages Improves Therapeutic Response to Gemcitabine in Murine Pancreas Cancer.

Background: The tumor microenvironment (TME) is composed of fibro-inflammatory cells and extracellular matrix (ECM) components. However, the exact contribution of the various TME compartments towards therapeutic response is unknown. Here, we aim to dissect the specific contribution of tumor-associated macrophages (TAMs) towards drug delivery and response in pancreatic ductal adenocarcinoma (PDAC). Methods: The effect of gemcitabine was assessed in human and murine macrophages, human pancreatic stellate cells (hPSCs), and tumor cells (L3.6pl, BxPC3 and KPC) in vitro. The drug metabolism of gemcitabine was analyzed by liquid chromatography–tandem mass spectrometry (LC–MS/MS). Preclinical studies were conducted using KrasG12D;p48-Cre and KrasG12D;p53172H;Pdx-Cre mice to investigate gemcitabine delivery at different stages of tumor progression and upon pharmacological TAM depletion. Results: Gemcitabine accumulation was significantly increased in murine PDAC tissue compared to pancreatic intraepithelial neoplasia (PanIN) lesions and healthy control pancreas tissue. In vitro, macrophages accumulated and rapidly metabolized gemcitabine resulting in a significant drug scavenging effect for gemcitabine. Finally, pharmacological TAM depletion enhanced therapeutic response to gemcitabine in tumor-bearing KPC mice. Conclusion: Macrophages rapidly metabolize gemcitabine in vitro, and pharmacological depletion improves the therapeutic response to gemcitabine in vivo. Our study supports the notion that TAMs might be a promising therapeutic target in PDAC.

Design, Synthesis and Bioevaluation of Two Series of 3-[(1-Benzyl-1H-1,2,3-triazol-4-yl)methyl]quinazolin-4(3H)-ones and N-(1-Benzylpiperidin-4-yl)quinazolin-4-amines.

Two series of 3-[(1-benzyl-1H-1,2,3-triazol-4-yl)methyl]quinazolin-4(3H)-ones and N-(1-benzylpiperidin-4-yl)quinazolin-4-amines were designed initially as potential acetylcholine esterase inhibitors. Biological evaluation demonstrated that N-(1-benzylpiperidin-4-yl)quinazolin-4-amines significantly inhibited AChE activity. Especially, two compounds of them were found to be the most potent with relative AChE inhibition percentages of 87 % in comparison to donepezil. The docking studies with AChE showed similar interactions between donepezil and four derivatives. N-(1-Benzylpiperidin-4-yl)quinazolin-4-amines also exhibited significant DPPH scavenging effects. The two series of compound also exerted moderate to good cytotoxicity against three human cancer cell lines, including SW620 (human colon cancer), PC-3 (prostate cancer), and NCI-H23 (lung cancer), with 3-[(1-benzyl-1H-1,2,3-triazol-4-yl)methyl]quinazolin-4(3H)-one being the most cytotoxic agent. 3-[(1-Benzyl-1H-1,2,3-triazol-4-yl)methyl]quinazolin-4(3H)-one significantly induced early apoptosis and arrested the SW620 cells at G2/M phase. From this study, two compounds of N-(1-benzylpiperidin-4-yl)quinazolin-4-amines could serve as new leads for further design and AChE inhibitors, while 3-[(1-benzyl-1H-1,2,3-triazol-4-yl)methyl]quinazolin-4(3H)-one could serve as a new lead for the design and development of more potent anticancer agents.

Bio-active mixed ligand Cu(II) and Zn(II) complexes of pyrimidine derivative Schiff base: DFT calculation, antimicrobial, antioxidant, DNA binding, anticancer and molecular docking studies

A new series of bio active Cu(II) and Zn(II) complexes [CuL(phen)](OOCCH3) (1), [ZnL(phen)](OOCCH3) (2), [CuL(bpy)](OOCCH3) (3), [ZnL(bpy)](OOCCH3) (4) have been synthesized using the pyrimidine derivative Schiff base (HL) [HL = 2-(4,6-dimethylpyrimidin-2-ylimino)methyl)-4-nitrophenol], 1,10-phenanthroline (phen), 2,2’-bipyridine (bpy) and acetate salts of Cu(II) and Zn(II). UV-Visible, FT-IR, 1H-NMR, ESR, elemental analysis, molar conductance and EI-MS spectral techniques have been used to endorse the square planar geometry for the complexes 1–4. The optimized molecular structure and the harmonic vibrational frequencies have been scrutinized by DFT methods. The antibacterial and antifungal activity of Schiff base (HL) and complexes 1–4 indicates that complex 1 acts as good antimicrobial agent against microbial strains than HL, complexes 2–4 and standard drugs streptomycin and nystatin. DNA cleavage study of the complexes 1–4 exposes that complexes 1 and 3 spectacle good cleaving agent than complexes 2 and 4. The interaction of complexes 1–4 with CT DNA using absorption, emission and viscometric measurements signifies that complexes 1–4 bind via an intercalation mode. The highest binding constants (K b) for the complex 1 is confirmed as 7.83 × 103 M−1 and 2.98 × 104 M−1 by absorption and emission spectrum respectively. These experimental observations were found to be close to the theoretical observations investigated by the molecular docking technique. Antioxidant property of the complexes 1–4 using DPPH assay clinches that complex 1 produces significant scavenging effect than other compounds. The result of in vitro cytotoxicity of the Schiff base (HL) and complexes 1–4 shows that complex 1 shows better ability to inhibit the growth of cancer cells. Communicated by Ramaswamy H. Sarma

Interaction of nitrocellulose with pentaacyloxyphenyl fullerene derivatives: autocatalytic inhibition in thermal decomposition of nitrocellulose

The safe storage of nitrocellulose has become challenging due to their requirements of extreme storage environments, and existing stabilizers cannot fully meet the demand. Thus, developing new high-performance stabilizers to improve the stability of nitrocellulose is urgently needed. Considering the stabilizing mechanism of stabilizers and the excellent free radical scavenging ability of fullerenes, two novel fullerene-based stabilizers, pentaacyloxyphenyl fullerene derivatives (PAOP-C60), were designed and synthesized, and their structures were characterized by FTIR, UV–Vis and NMR. The thermal action of PAOP-C60 during thermal decomposition process of nitrocellulose was studied by thermal analysis, which indicating that the thermal stability of nitrocellulose was increased with addition of PAOP-C60 and the PAOP-C60 was found to exhibit superior thermal stability than traditional stabilizer. The results of electron spin resonance showed that fullerene-based stabilizers had a significant scavenging effect on nitrogen oxide radicals, and the IC50 of PAOP-C60 (0.674–0.818 g L−1) was smaller than that of diphenylamine (1.717 g L−1). Moreover, the intermediate product produced by PAOP-C60 and nitrocellulose action was extracted and characterized by FTIR. A possible stabilization mechanism of PAOP-C60, which was different from traditional stabilization mechanism, was proposed.

Ruta graveolens and rutin, as its major compound: investigating their effect on spatial memory and passive avoidance memory in rats

Context There are numerous pharmacological activities for Ruta graveolens and its bioactive constituent, rutin, on learning and memory. Objective This study aimed to examine the effect of R. graveolens and rutin on memory in rats. Materials and methods In this study animals were treated with the hydroalcholic extract of R. graveolens and rutin by IP injection for 10 days. Behavioural and biochemical tests as well as HPLC analysis and antioxidant activity of extract have been evaluated. Results R. graveolens extract and rutin significantly increased learning and improved spatial memory, as well as secondary latency; moreover, there were significant increases in the serum and brain antioxidant capacity as well as the level of TBARS in serum and brain tissues. Results also showed that R. graveolens has significant DPPH radical scavenging effect (IC50: 159.17 ± 1.56 μg/mL). The HPLC analysis of extract showed that caffeic acid (19.92 ± 0.01), rutin (40.15 ± 0.01), and apigenin (0.84 ± 0.01) mg/g of dry extract are the main components of the extract. Discussion and conclusion Regarding the effects of R. graveolens extract and rutin on animal brain cells, memory function, and learning, additional studies, including clinical trials, might be beneficial in producing natural supplementary drugs from this herb.

Concordance of antioxidant and anti-Inflammatory activity in Xylocarpus granatum (Koen)

Xylocarpus granatum, a common mangrove plant is traditionally used for the treatment of diarrhoea, cholera, fever, dyslipidemia, inflammation, etc. The present study was carried out to evaluate the antioxidant and anti-inflammatory potential of the ethanolic extract of X. Granatum by various in vitro methods such as 1,1-diphenyl-2-picryl-hydrazil (DPPH) free radical scavenging assay, reducing power assay, ferric reducing antioxidant power (FRAP) and β-carotene bleaching inhibition assay. Total phenolic and flavonoid content were determined. Anti-inflammatory activity was evaluated by in vitro human RBC membrane stabilizing assay and in vivo mice paw edema test. Ethanolic leaf extract (S2) of X. granatum showed significant scavenging effect on DPPH scavenging with a value of IC50 165.95µg/ml. In addition, it showed significant reducing potential with a value of 59.04 mM of ferrous equivalent per ml in FRAP assay and in reducing power assay the EC50 value was determined as 241.61μg/ml . The ethanolic leaf extracts exhibited 72.3% β-carotene bleaching inhibition. The total phenolic and flavonoid content of the extract were 66μg/ml gallic acid equivalent and 47.66μg/ml quercetin equivalent per gram of dry extract, respectively. The extract also exhibited 52.63% and 51.05% protection of RBC membrane in hypotonicity and heat induced lysis inhibition, respectively. Significant reduction of mice paw edema (36.34% in 20 μg/kg bw concentration) was observed in the extract. The results revealed that the leaf extract of X. granatum possesses strong antioxidant and anti-inflammatory potential.&#x0D; &#x0D; J Bangladesh Agril Univ 17(4): 466–475, 2019