Lupin is a major rotational crop produced abundantly in Australia. Three varieties of sweet lupins are grown in Australia depending on soil types and climatic conditions; these are white lupin ...(Lupinus albus), blue lupin (Lupinus angustifolius), and yellow lupin (Lupinus luteus). In this study, polysaccharides from the three lupin species have been extracted with hot water and a range of their biological activities investigated. The antioxidant activities of lupin polysaccharides have been measured in terms of ABTS
*+
radical and hydroxyl radical scavenging activities, and their affinity to chelate with iron. Immune-enhancing power of the lupin polysaccharides was examined by measuring their capacity to stimulate the macrophages (RAW 264.7) to release TNF-α and nitric oxide. The prebiotic activities were determined against the beneficial probiotics such as Lactobacillus rhamnosus DR20, Lactobacillus acidophilus LAFTI L10, Bifidobacterium lactis DR10, and Bifidobacterium animalis BB-12. Polysaccharides from the three lupin species have exhibited significant antioxidant, immunostimulatory, and prebiotic activities. The results demonstrated that blue lupins displayed the best activities, and therefore are expected to possess high potential to be used as nutraceutical and functional ingredients with significant therapeutic value. FT-IR spectroscopic technique was employed for a preliminary structural characterization. Studies involving surface morphology and thermal behavior have indicated that the lupin polysaccharides are suitable for end product development.
A novel Schiff base, 3-(((1
H
-1,2,4-triazol-3-yl)imino)methyl)-4
H
-chromen-4-one (L) was synthesized and used as ligand for the synthesis of Co(II), Ni(II), Cu(II), Zn(II) and Pd(II) complexes. The ...structural characterization of the ligand and its metal complexes was determined by using various physicochemical and spectroscopic methods. The IR data show that the Schiff base ligand acts as a bidentate donor coordinating through the oxygen atom of the chromone and nitrogen atom of the imine group. Based on all spectral data, tetrahedral geometry has been proposed for all the metal complexes except Cu(II) and Pd(II) complexes. However, square-planar geometry has been proposed for Cu(II) and Pd(II) complexes. DNA binding interaction of the ligand and its metal complexes was investigated by using UV–visible absorption, fluorescence and molecular docking studies. The binding constants were in the order of 10
4
M
−1
suggesting good binding affinity towards CT-DNA. The DNA cleavage activity of the synthesized compounds was investigated by using agarose gel electrophoresis. In vitro antimicrobial activity of the synthesized compounds were screened against two gram-positive bacteria (
Bacillus subtilis, Staphylococcus aureu
) and two gram-negative bacteria (
Escherichia coli, Proteus vulgaris
) and one fungi strain
Candida albicans
using disc diffusion method. Antioxidant activity was carried out by DPPH radical scavenging method. In vitro anti-proliferative activity of the ligand and its metal complexes was also carried on the HEK-293, HeLa, IMR-32 and MCF-7 cancer cell lines using MTT assay.
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A series of new edaravone derivatives 3–7 have been synthesized, characterised using various spectroscopic techniques and screened for their in vitro anti-cancer, antioxidant ...activities. Structure of 5d was further substantiated through single crystal X-ray diffraction. Among the tested, 5l exhibited pronounced activity against PC3 cancer cells. Compounds 5i, 5l, 7c showed potent activity against A549 cancer cells. Products 5k, 6, 7c demonstrated good antioxidant activity with MIC values of 18.60, 16.27, 16.07μg/mL respectively. Further the reported analogues were also tested on normal HEK293T cells and displayed low to good safer profiles. Derivatives 5l and 7c have come out to be safer potent anticancer, antioxidant agents. Additionally, the target products were subjected to their molecular properties prediction and drug likeness by employing Molinspiration and Osiris property explorer toolkits. None of them violated Lipinski’s boundaries classifying the title compounds as potential anticancer and antioxidant agents.
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•1`δ-1`-acetoxyeugenol acetate (DAEA) from A. galanga possesses anti-amnesiac property.•Neurotoxicity was induced by amyloid beta(25–35) injection and treated with DAEA.•AChE ...inhibition, TNF-α inhibition and improved antioxidants indicates neuroprotection.•Regulated biogenic amines and corticosterone implicates the attenuation of stress.•Hypothalamus-pituitary-adrenal axis (HPA-axis) regulation indicates neuroprotection.
The progressive accumulation of amyloid beta (Aβ) peptide is neurotoxic and leads to Alzheimer’s type dementia. Accumulation of Aβ has been associated with dysfunction of hypothalamic-pituitary-adrenal (HPA) axis and elevated pro-inflammatory cytokines. In this study, we investigated the effect of 1`δ-1`-acetoxyeugenol acetate (DAEA), isolated from Alpinia galanga (L.), on Aβ(25–35) induced neurodegeneration in mice. Mice were treated with three different doses of DAEA (12.5 mg/kg, 25 mg/kg and 50 mg/kg) for 28 days. Aβ(25–35) was injected by intracerebroventricular (i.c.v.) injection on the 15th day of 28 days. Open field, water maze and step-down inhibitory tests were performed on the 27th day to determine the habituation memory, spatial learning, and short- and long-term memory, respectively. Acetylcholinesterase (AChE), Corticosterone, biogenic amines (serotonin and dopamine), tumour necrosis factor-α (TNF-α), and antioxidant parameters such as superoxide dismutase, catalase, glutathione peroxidase and vitamin C were evaluated in brain homogenates after behavioural tests to ascertain the cognitive improvement through neuro-immune-endocrine modulation. The DAEA treatment with 25 mg/kg and 50 mg/kg resulted in significant (p < 0.001) improvement of habituation memory and step-down inhibitory avoidance task. In spatial learning, the cognitive improvement was significantly improved (p < 0.001) by reduction in escape latency. In the biochemical study, the significant (p < 0.001) reduction of AChE indicates the preeminent neuroprotection. Corticosterone and TNF-α were significantly (p < 0.01) reduced and biogenic amines were increased with antioxidant markers, which signify the potential influence of DAEA on neuroprotection. Our investigation revealed that the drug DAEA attenuates stress mediated through the HPA axis and regulates the neuroendocrine and neuroimmune function to improve the cognition. DAEA could be a potential lead candidate for the treatment of neurodegeneration.
In this study, we investigated the mechanisms involved in multi-wall carbon particles/nanomaterials (MWCNM) induced cytotoxicity using human embryonic kidney (HEK293) cells and to assess the effect ...of physicochemical properties on the cytotoxicity and oxidative stress induced by the carbon nanomaterials (CNM). To elucidate the possible mechanisms of CNM-induced cytotoxicity, cell viability (3-(4, 5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide MTT assay), cell membrane damage (lactate dehydrogenase enzyme LDH assay), reduced glutathione (GSH), interleukin-8 (IL-8) and lipid peroxidation levels were quantitatively assessed under carbon nanomaterials exposed (48 h) conditions. Exposure of different sizes of four CNM at dosage levels between 3 and 300 μg/mL decreased cell viability in a concentration- and size-dependent manner. Exposure of CNM (10-100 μg/mL) to HEK cells resulted in size-, surface area- and concentration-dependent cell membrane damage, increased production of IL-8, increased thiobarbituric acid reactive substances (TBARS) and decreased intracellular glutathione levels. In summary, the physical properties of carbon nanoparticles may alter the CNM-induced concentration-dependent cytotoxicity and oxidative stress.
A series of substituted (
Z)-5-(
N-benzylindol-3-ylmethylene)imidazolidine-2,4-dione (
3) analogs structurally related to aplysinopsin, and that incorporate a variety of substituents in both the ...indole and
N-benzyl moieties have been synthesized under microwave irradiation and conventional heating methods. These analogs were evaluated for their anti-proliferative activity against MCF-7 and MDA-231 breast cancer cell lines, and A549 and H460 lung cancer cell lines. Two analogs,
3f and
3j had IC
50 values of 4.4 and 5.2
μM, respectively, compared to 5-fluorouracil (IC
50
=
15.2
μM) against MCF-7 cells.
A series of substituted (
Z)-5-(
N-benzylindol-3-ylmethylene)imidazolidine-2,4-dione (
3) analogs structurally related to aplysinopsin, and that incorporate a variety of substituents in both the indole and
N-benzyl moieties have been synthesized under microwave irradiation and conventional heating methods These analogs were evaluated for their anti-proliferative activity against MCF-7 and MDA-231 breast cancer cell lines, and A549 and H460 lung cancer cell lines. Two analogs,
3f and
3j had IC
50 values of 4.4 and 5.2
μM, respectively, compared to 5-fluorouracil (IC
50
=
15.2
μM) against MCF-7 cells.
The roots of Sanguisorba officinalis are used in traditional Chinese medicine for the treatment of diseases such as inflammation and internal haemorrhage. Several scientific investigations involving ...extraction and pharmacological studies of terpenoids and triterpenoid glycosides from this herb have been carried out. However, little is known regarding the immunomodulatory and antioxidant properties of polysaccharides from S. officinalis. Hence the polysaccharides from this herb have been investigated here. The hot water extract of S. officinalis has been fractionated using size-exclusion chromatography to obtain four polysaccharide fractions designated as SOP-1, SOP-2, SOP-3 and SOP-4. The range of molecular masses of these fractions were from 280Da to 2000kDa, and their sugar compositions consisted mainly of fructose, glucose, xylose, arabinose, and rhamnose. The antioxidant activities of the crude polysaccharide fractions were evaluated in a biological assay using Saccharomyces cerevisiae, whereas the radical scavenging activity was measured using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) method. Analysis of the immunomodulatory activities of these polysaccharide fractions were measured by using mouse macrophages. Most of the polysaccharide fractions have stimulated the production of nitric oxide and tumour necrosis factor-α (TNF-α), and also displayed antioxidant activities. These results suggest that the roots of S. officinalis are likely to have therapeutic value for the treatment of cancer.
This proposed work combines R2B, R4B, and R8B using signal delay feedback FFT architecture. R2B SDF FFT architecture has complex and large computations, and many stages are being used. To overcome ...this problem, Radix-4 and Radix-8 FFT are built to increase efficiency and decrease computational steps to incorporate in DUC and DDC filters and OFDM modules of 5G based modules. Signal delay feedback FFT architecture has stages that can have one clock per cycle. Each phase consists of a butterfly-type diagram in which the twiddle factors and rotators are used. In the proposed joined R2B, R4B, and R8B combined FFT, 5 phases of R2B FFT have been used with standard machine learning algorithms. When combined with complex R2B FFT, the combined R2B, R4B, and R8B FFT are less computational than the current technique. In the proposed method, the Xilinx tool is used to execute the introduced model.
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