The interaction of the novel quinazoline (E)-4-(2-(pyridin-2-ylmethylene)hydrazinyl)quinazoline (L) with Zn2+ was performed in the absence or presence of the non-steroidal anti-inflammatory drug ...sodium diclofenac (Nadicl) and resulted in the formation of complexes Zn(L)2(NO3)2·MeOH (1·MeOH) and Zn(L)(dicl-O)2·MeOH (2·MeOH), respectively. The two complexes were characterized by IR and 1H NMR spectroscopy and by single-crystal X-ray crystallography. In these complexes, L was tridentately coordinated to Zn(II) via the quinazoline, hydrazone and pyridine nitrogen atoms. Further studies concerning the behavior of the compounds towards calf-thymus (CT) DNA and supercoiled circular pBluescript KS II plasmid DNA (pDNA) have been performed. The complexes may bind to CT DNA via intercalation, with complex 1 showing higher binding affinity than 2. The complexes may cleave pDNA in the absence or presence of irradiation with UVA, UVB or visible light and the most active pDNA-cleavager is compound 1. The binding constants of the compounds for bovine serum albumin were calculated and the subdomain of the albumin where the compounds prefer to bind was determined. The free radical scavenging ability of the compounds was evaluated towards 1,1-diphenyl-picrylhydrazyl and 2,2΄-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) radicals with complex 2 being the most active compound. Thus, complex of type 1 maybe a lead compound for the development of novel DNA-binders and DNA-cleavers or photo-cleavers for medical and biotechnological “on demand” applications, whereas the structure of complex type 2 may provide novel antioxidants and radical scavengers.
A novel o-pyridine-hydrazone derivative of 4-quinazoline and its Zn(II) complexes in the absence or presence of diclofenac were characterized and evaluated for their affinity to bovine serum albumin, calf-thymus DNA and plasmid-DNA in the absence or presence of irradiation as well as their ability to scavenge free radicals. Display omitted
•A novel quinazoline and its two Zn complexes were prepared and characterized.•Intercalation is the most possible binding mode of the complexes to DNA.•The complexes exhibit noteworthy plasmid DNA photocleavage activity.•The compounds may bind tightly and reversibly to bovine serum albumin.•The antioxidant activity of complexes depends on the presence of diclofenac ligand.
•Properties of two species of walnut oil in China were comparatively investigated.•The oil from Juglans regia showed higher minor composition content and antioxidant capacity than that from Juglans ...sigillate.•C22:1 is the special fatty acid of iron walnut oil.
This study compared the lipid compositions, minor components contents, oxidative stability index, and free radical scavenging capacities of walnut oils from two species in China: Juglans regia (common walnut) and Juglans sigillata (iron walnut). The results showed that iron walnut oil contained lower C16:0 (4.97–5.25%) and special fatty acid (erucic acid C22:1). Common walnut oil provided higher tocopherols (441.03–490.32 mg/kg), phytosterols (1014.49–1211.40 mg/kg), squalene (4.41–5.21 mg/kg), and polyphenols (44.78–64.61 mg GAE/kg) and better antioxidant capacities. The walnut oil of the different walnut species could be distinguished by principal component analysis and hierarchical cluster analysis. In addition, multiple linear regression was employed to evaluate the contributions of minor components to the free radical scavenging capacity of the walnut oils and develop a predictive model for the antioxidant capacity of the oil. This information has important implications for the nutritional value and industrial production of walnut oil in China.
Fluorescent carbon dots (CDs) are prepared from a natural resource Carica Papaya Leaves, by sand bath method. The as-synthesized CDs optical and structural properties were characterized by ...UltraViolet-Visible, FT- IR, and fluorescence spectroscopy. Also the size, shape, and particle size distribution was studied using Transmission electron microscopy technique. These CDs were examined for biomedical applications like free radical scavenging activity using DPPH assay, antioxidant activity using phosphomolybdate assay, and in vitro anti-inflammatory activity using membrane stabilization protocol. The CDs exhibited excellent biological activities at lower concentrations and showed notable half-maximal effective concentration (EC50). The EC50 of free radical scavenging activity (27.6 μg/mL), antioxidant activity (23.00 μg/mL), and in vitro anti-inflammatory activity (15.52 μg/mL) signifies that CDs can be potential therapeutic agents.
•Fluorescent Carbondots (CDs) are prepared from a natural resource Carica Papaya Leaves without usage of external passivating agents.•A facile, economic, and green approach was utilized to synthesize CDs in bulk using sand bath assisted method.•The CDs were examined for radical scavenging activity and antioxidant capacity and in vitro anti-inflammatory activity.•CDs exhibited excellent EC50 for DPPH (27.6 μg/mL), TAC (23.00 μg/mL), and HRBC (15.52 μg/mL) activities.
Either hypoxia in an acute ischemic stroke before thrombolysis or the oxygen-boost after thrombolysis cause a high level of free radicals, resulting in successive injuries to neurocytes. To treat an ...ischemic stroke, it is needed to scavenge free radicals, combining sequentially regulating hypoxia and oxygen-boost microenvironment. Here, we report an engineered nanosponge (Mn3O4@nanoerythrocyte-T7, MNET) that could remodel the microenvironment of a stroke by self-adapted oxygen regulating and free radical scavenging. With a long circulation time in blood due to the stealth effect of the erythrocyte and preferential accumulation in the infarct site by the assisting of T7 peptide, MNET exerts a distinct therapeutic effect in two stages of an ischemic stroke: (i) before thrombolysis, rescue neurocyte via rapid free radical scavenging and timely oxygen supply; (ii) after thrombolysis, suppress oxygen-boost via oxygen storage, as well as scavenge free radical to avoid reperfusion injury. MNET holds an attractive potential for ischemic stroke treatment via phased regulation of pathological microenvironment.
Bi2Se3 nanoparticles (NPs) have attracted wide interests in biological and medical applications. Layer-like Bi2Se3 with high active surface area is promising for free radical scavenging. Here, we ...extended the medical applications of Bi2Se3 NPs further to in vivo protection against ionizing radiation based on their superior antioxidant activities and electrocatalytic properties. It was found that Bi2Se3 NPs can significantly increase the surviving fraction of mice after exposure of high-energy radiation of gamma ray. Additionally, the Bi2Se3 NPs can help to recover radiation-lowered red blood cell counts, white blood cell counts and platelet levels. Further investigations revealed that Bi2Se3 NPs behaved as functional free radical scavengers and significantly decreased the level of methylenedioxyamphetamine. In vivo toxicity studies showed that Bi2Se3 NPs did not cause significant side effects in panels of blood chemistry, clinical biochemistry and pathology.
Layer-like Bi2Se3 with high active surface area can protect mice against ionizing radiation based on their superior antioxidant activities and electrocatalytic properties. Bi2Se3 NPs can significantly increase the surviving fraction of mice up to 70% after exposure of high-energy radiation of gamma ray. Bi2Se3 NPs behaved as functional free radical scavengers and significantly decreased the level of methylenedioxyamphetamine. In vivo toxicity studies showed that Bi2Se3 NPs did not cause significant side effects in panels of blood chemistry, clinical biochemistry and pathology. Display omitted
•Bi2Se3 NPs can significantly increase the surviving fraction of mice up to 70% after Gamma radiation.•Bi2Se3 NPs can help to recover radiation-lowered red blood cell counts, white blood cell counts and platelet levels.•Bi2Se3 NPs behaved as functional free radical scavengers and significantly decreased the level of methylenedioxyamphetamine.
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•SST egg is a promising source of highly nutritious proteins and minerals.•Proteomic analysis showed SST egg proteins containing at least 9 protein families.•Potential antidiabetic ...oligopeptides were released by papain and a total of 16 peptides were identified.•Molecular docking demonstrated the interaction of identified peptides with α-glucosidase.•Three synthetic oligopeptides HNKPEVEVR, ARDASVLK and SGTLLHK strongly inhibited a-glucosidase.
This study aimed to explore nutritional compositions and proteomics of soft-shelled turtle (SST) egg, as well as identify potential antidiabetic oligopeptides with α-glucosidase inhibitory property. Results revealed that SST egg is a promising source of highly nutritious proteins and minerals (54.64% and 5.81% of dry matter, respectively). Further proteomic analysis showed SST egg proteins contained at least 9 protein families, such as transferrin/iron binding protein and immunoregulation-related protein. Hydrolysis by different enzymes, especially papain, remarkably increased α-glucosidase inhibitory activity and scavenging activity for ABTS, DPPH, hydroxyl and oxygen radicals of SST egg proteins. Peptides from papain hydrolysate were fractionated using ultrafiltration followed by reverse phase chromatography, and 16 peptides were identified in the most active fraction by LC-QTOF-MS/MS. Molecular docking revealed that 14 of these peptides could easily dock into the substrate-binding pocket and/or inhibitor binding sites of α-glucosidase with the docking score below −150 kcal/mol, indicating their potential α-glucosidase inhibitory properties. The five most abundant oligopeptides with potent interaction with α-glucosidase were further synthesized, and oligopeptides HNKPEVEVR, ARDASVLK and SGTLLHK strongly inhibited the activity of α-glucosidase (IC50 of 56, 195 and 289 µmol/L, respectively). Therefore, oligopeptides from enzymatic hydrolysate of SST egg protein exhibit potential antidiabetic activity, making it a promising functional food ingredient.
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•(Meth)acrylate and acrylamide monomers based on a protected gallic acid are obtained.•Controlled photo-mediated RAFT polymerization of these original monomers was carried.•Polymers ...with one free gallic acid as lateral substituent per monomer unit are described.•Intrinsic antibacterial and antioxidant properties of these polymers are highlighted.
The development of bio-based thermoplastics is rapidly growing due to the depletion of fossil fuel reserves but also in the hope of obtaining polymers with original properties. Herein, we report the controlled synthesis of original homopolymers derived from gallic acid, one of the well-known natural polyphenols that exhibits various health-promoting effects. More precisely, acrylate, methacrylate and acrylamide monomers based on a protected gallic acid are firstly obtained by a rethought multistep scheme. Then, a controlled photo-mediated RAFT (Reversible Addition Fragmentation chain Transfer) polymerization is carried out before a final deprotection. By this way, original polymers bearing a free gallic acid as a lateral substituent on each monomer unit are described. The intrinsic antibacterial and antioxidant properties of these polymers are highlighted and compared with those of gallic acid.
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