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To predict the binding of compound 16 to IAPP and α-glucosidase protein complexes, molecular docking studies were performed. Altogether, our results support that the 2-phenylbenzofuran derivatives could represent a promising candidate for developing molecules able to modulate multiple targets involved in diabetes mellitus disorder.Lemon waste after industrial juice extraction encompasses of valuable bio-components that stimulated the development of novel and biodegradable films. Lemon waste powder (LWP) based nanobiocomposite films were prepared by incorporating different concentrations of cellulose nanofiber (CNF) (3 and 6% w/w) and savory essential oil (SEO) (1.5 and 3% w/w) in order to modify physical, mechanical and antimicrobial properties of the films. The fabricated film samples were characterized in terms of FTIR, XRD, FE-SEM and DSC analyses as well as mechanical, water vapor permeability and antimicrobial properties. PF-04418948 FTIR and FE-SEM results indicated a good compatibility between LWP matrix and incorporated CNF and SEO. Physical and thermal analysis showed a significant effect of incorporating SEO and CNF on enhancing glass transition temperature, tensile strength and water barrier properties of the film samples. SEM analysis revealed non-uniform dispersion of CNF at higher concentration, while SEO incorporation improved the structure of the films. In addition, the LWP based films significantly showed antimicrobial properties against five food borne pathogens and this effect improved considerably by elevating the SEO loading concentration. In conclusion, LWP based nanobiocomposite films containing 3% CNF and 3% SEO could be introduced as a good candidate for development of active food packaging.Laccases are enzymes able to catalyze the oxidation of a wide array of phenolic and non-phenolic compounds using oxygen as co-substrate and releasing water as by-product. They are well known to have wide substrate specificity and in recent years, have gained great biotechnological importance. To date, most well studied laccases are from fungal and mesophilic origin, however, enzymes from extremophiles possess an even greater potential to withstand the extreme conditions present in many industrial processes. This research work presents the heterologous production and characterization of a novel laccase from a thermoalkaliphilic bacterium isolated from a hot spring in a geothermal site. This recombinant enzyme exhibits remarkably high specific activity (>450,000 U/mg) at 70 °C, pH 6.0, using syringaldazine substrate, it is active in a wide range of temperature (20-90 °C) and maintains over 60% of its activity after 2 h at 60 °C. Furthermore, this novel spore-coat laccase is able to biodecolorize eight structurally different recalcitrant synthetic dyes (Congo red, methyl orange, methyl red, Coomassie brilliant blue R250, bromophenol blue, malachite green, crystal violet and Remazol brilliant blue R), in just 30 min at 40 °C in the presence of the natural redox mediator acetosyringone.γD-crystallin is among the most abundant γ-crystallins in the human eye lens which are essential for preserving its transparency. Aging, and environmental changes, cause crystallins to lose their native soluble structure and aggregate, resulting in the formation of cataract. Current treatment of cataract is surgical removal which is costly. Pharmaceutical therapeutics of cataract is an unmet need. We report a screen for small molecules capable of inhibiting aggregation of human γD-crystallin. Using a highly amyloidogenic hexapeptide model 41GCWMLY46 derived from the full-length protein, we screened a library of 68 anthraquinone molecules using ThT fluorescence assay. A leading hit, the cochineal Carmine, effectively reduced aggregation of the model GDC6 peptide in dose dependent manner. Similar effect was observed toward aggregation of the full-length γD-crystallin. Transmission electron microscopy, intrinsic Tryptophan fluorescence and ANS fluorescence assays corroborated these results. Insights obtained from molecular docking suggested that Carmine interaction with monomeric GDC6 involved hydrogen bonding with Ace group, Cys, Met residues and hydrophobic contact with Trp residue. Carmine was non-toxic toward retinal cells in culture. It also reduced ex vivo the turbidity of human extracted cataract material. Collectively, our results indicate that Carmine could be used for developing new therapeutics to treat cataract.Anti-TNF inhibitors are efficacious in the treatment of chronic inflammatory diseases such as rheumatoid arthritis (RA), Crohn's disease (CD), juvenile idiopathic arthritis (JIA), and ankylosing spondylitis (AS). However, more and more clinical case reports revealed that anti-TNF inhibitors could increase the risk of viral, fungal, and bacterial (especially intracellular) infection. In this study, based on Immune Epitope Database (IEDB) online B cell epitope prediction and the knowledge of TNF three dimensional (3D) structure we developed a novel vaccine (DTNF114-TNF114) that targeting TNF epitope 1-14, which produced antibodies only partially binding to trans-membrane TNF (tmTNF), therefore partially sparing tmTNF-TNFR1/2 interaction. Immunization with DTNF114-TNF114 significantly protected and prolonged the survival rate of mice challenged with lipopolysaccharide (LPS); and in the mCherry expressing Mycobacterium bovis Bacillus Calmette-Guérin (mCherry-BCG) infection model, DTNF114-TNF114 immunization significantly decreased soluble TNF (solTNF) level in serum, meanwhile did not suppress host immunity against infection. Thus, this novel and infection concern-free vaccine provides a potential alternative or supplement to currently clinically used anti-TNF inhibitors.Cerebral ischemia, a common cerebrovascular disease, is one of the great threats to human health. Nowadays, many drugs used in the treatment of cerebral ischemia such as clot busting drugs, antiplatelet drugs, and neuroprotective drugs have limits. It is urgent finding new effective treatments for the patients. Researches have confirmed that many kinds of polysaccharides from natural resources possess therapeutic effects on cerebral ischemia, but are still lack of a comprehensively understanding. In this paper, based on the pathophysiology of cerebral ischemic injury, we summarize the latest discoveries and advancements of 29 kinds of polysaccharides, focusing on their ameliorating effects on cerebral ischemia and the underlying mechanisms. Several mechanisms are involved, mainly including antioxidant activities, anti-inflammatory activities, regulating neuron apoptosis, as well as resisting nitrosative stress injury. Besides, polysaccharides show protective effects through certain signaling pathways including PI3K/Akt, MAPK, and NF-κB, PARP-1/AIF, JNK3/c-Jun/Fas-L, and Nrf2/HO-1 signaling pathways.
Read More: https://www.selleckchem.com/products/pf-04418948.html
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