Petterssontorp2251

No toxicity was observed in human epithelial T24 cells treated with hybrid 22 in concentrations up to 560 μM using a lactate dehydrogenase assay.The fortification of animal feed with enzymes in order to optimize feed utilization has become a standard for the meat production industry. A method for measuring levels of active enzymes that can be carried out quickly would ensure that feed has been supplemented with the appropriate amount of enzyme. Phytase is the most widely used feed enzyme and is routinely quantified with an activity assay in a limited number of specialized laboratories. As an alternative, we report here the development of a rapid and easy method to perform a quantitative assay for the phytase from Citrobacter braakii. The method is suitable for use at local sites with a minimum lab setup and will reduce delays and potential interferences due to improper sample storage and shipment. The new assay is based on a lateral flow immunoassay that utilizes magnetic immune-chromatographic test (MICT) technology to quantify the phytase content of a feed extract. After extraction of the phytase from the feed, the sample is simply diluted and added to a reaction tube containing a specific anti-phytase antibody coupled to superparamagnetic particles. The mixture is then applied on an assay cassette, where the formed particle-antibody-phytase complexes are captured by immobilized antibodies on a nitro-cellulose strip housed in a cassette. The cassette is placed in the MICT reader that measures the magnetic signal of the captured particles. Using the calibration information stored in the cassette barcode, the signal is converted to a phytase concentration, given as phytase activity (FYT) per kilogram of feed. The accuracy and robustness of the assay compared to the ISO phytase activity assay were demonstrated through a large validation study including real feed samples from different compositions and origins. The MICT assay is the first quantitative assay for feed enzymes that is fast, reliable, and simple to use outside of a specialized reference laboratory and that is suitable for use in place of the current ISO assay.In this work, to solve the problem of pipeline blockage caused by the accumulation of hydrate particles and wax particles and to explore the interaction characteristics of adhesive force between gas hydrate particles and wax particles as well as droplets, a high-pressure triaxial mobile device was used to measure the adhesion strength between cyclopentane hydrate particles and different commonly seen phases in the pipeline, including cyclopentane hydrate particles themselves, liquid droplets, and wax crystal particles. These experiments were conducted at different temperatures. The results showed that the adhesion between hydrate and wax particles was decreased with the increase in temperature; this is because the wax is amorphous, the heat absorbed when the temperature rises only increases its average kinetic energy, and the stronger the kinetic energy, the lower its viscosity, resulting in reduced adhesion between particles. Meanwhile, this adhesion was also affected by the concentration of wax. As the wax concentration increased from 1 to 5.32 wt % and then to 8.14 wt %, the adhesion between hydrate and wax particles was first decreased and then increased. This was because when the wax crystal concentration was below 5 wt %, a higher wax molecule concentration meant a more hydrophobic surface, which restricted the formation of a capillary liquid bridge between particles and thus reduced the interforce between wax crystal particles and hydrate particles. When the wax crystal concentration was between 5 and 8 wt %, the change of hydrophobicity was no longer the dominating factor, the increase in wax concentration blocked the hydrate molecular diffusion path, which caused a higher hydrate viscosity, therefore leading to a decreased hydrate molecular diffusion rate and a reduced conversion rate of the liquid bridge in hydrates, the lower conversion rate could subsequently lead to the increasing size of micropores in the hydrate shell, and adhesion between particles was increased.A copper-mediated decarboxylative coupling reaction of 3-indoleacetic acids with pyrazolones was described. This protocol realized new functionalization of pyrazolones under simple reaction conditions and exhibited high functional group compatibility and broad substrate scope. Notably, the products displayed antiproliferative activity against cancer cells.Nitroxyl (HNO) is a member of the reactive nitrogen species, and how to detect it quickly and accurately is a challenging task. In this work, we designed and prepared a fluorescent ratiometric probe based on the fluorescence resonance energy transfer (FRET) mechanism, which can detect HNO with high selectivity. The coumarin derivative was used as an energy donor, the rhodol derivative was applied as an energy receptor, and 2-(diphenylphosphine)benzoate was utilized as the recognition group to detect nitroxyl. In the absence of HNO, the rhodol derivative exists in a non-fluorescent spironolactone state, and the FRET process is inhibited. Upon adding HNO, the closed spironolactone form is transformed into a conjugated xanthene structure and the FRET process occurs. This probe could specifically recognize nitroxyl, showing high sensitivity and selectivity. When the HNO concentration was changed from 3.0 × 10-7 to 2.0 × 10-5 mol·L-1, I 543nm/I 470nm exhibited a satisfactory linear correlation with the concentration of HNO. A detection limit of 7.0 × 10-8 mol·L-1 was obtained. In addition, almost no cell toxicity had been verified for the probe. The probe had been successfully applied to the ratiometric fluorescence imaging of HNO in HepG2 cells.Facile synthesis of molecular hybrids containing a 2,4-dinitrophenyl moiety was achieved via nucleophilic aromatic substitution of the fluoride anion of Sanger's reagent (2,4-dinitrofluorobenzene) with various N, S, and O nucleophiles, considered as bioactive moieties. Antimicrobial evaluation of the new hybrids was carried out using amoxicillin and nystatin as antibacterial and antifungal reference standards, respectively. MIC test results identified the compounds 3, 4, and 7 as the most active hybrids against standard strains and multidrug-resistant strains (MDR) of Staphylococcus aureus, Escherichia coli, and Pseudomonas aurginosa. Most of the hybrids displayed two times the antibacterial activity of AMOX against MDR Pseudomonas aeruginosa, E. coli, and a standard strain of P. aeruginosa (ATCC 29853), while demonstrating a weak antifungal profile against Candida albicans. Selectivity profiles of the promising compounds 3, 4, 6, 7, 8, and 11 on WI-38 human cells were characterized, which indicated that compound 3 is the safest one (CC50 343.72 μM). The preferential anti-Gram-negative activity of our compounds led us to do docking studies on DNA gyrase B. Docking revealed that the potential antimicrobial compounds fit well into the active site of DNA gyrase B. Furthermore, in silico absorption, distribution, metabolism, and excretion (ADME) predictions revealed that most of the new compounds have high gastrointestinal absorption and a good oral bioavailability with no BBB permeability.New push-pull N(9)-alkylated 6-piperidino-2-triazolylpurine and 2-piperidino-6-triazolylpurine derivatives are synthesized, and their optical and optoelectronic properties are comprehensively characterized with experimental and computational methods. The compounds possess intense violet or blue fluorescence with fluorescence quantum yields of up to 91% in solution and 40% in host-free films. Depending on their structural composition, the compounds have ionization energy in the range of 5.25-6.04 eV, electron affinity of 2.18-3.15 eV, and triplet energy of 2.52-2.95 eV. Due to the presence of hole-transporting purine and electron-transporting triazole fragments, compounds exhibit bipolar charge-transportation ability. Despite the favorable emissive properties of the studied push-pull purines, their electroluminescence in thin films is quenched owing to large current densities that are present even at a moderate driving voltage. This marks application directions related to a predominantly charge-transportation functionality as the most suitable for this compound class.Despite various advancements in cancer therapies, treating cancer efficiently without side effects is still a major concern for researchers. Anticancer drugs from natural sources need to be explored as a replacement for chemo drugs to overcome their limitations. In our previous studies, isolation, characterization, and anticancer properties of a novel biosurfactant from Candida parapsilosis were reported. In this study, we report the cytotoxicity of the polymeric nanoparticles of this novel biosurfactant toward breast cancer cells. Biosurfactant-encapsulated polymeric nanoparticles of polylactic acid-poly(ethylene glycol) (PLA-PEG) copolymers were synthesized by the double emulsion solvent evaporation method. Folic acid (FA) was used as a targeting ligand to actively deliver the anticancer cargo to the cancer site. The encapsulation efficiency of nanoparticles was observed as 84.9%, and Fickian diffusion was observed as a kinetic model for the release of biosurfactant from nanoparticles. The controlled delivery of the biosurfactant was noticed when encapsulated in PLA-PEG copolymer nanoparticles. Additionally, it was observed that FA enhanced the uptake and cytotoxicity of biosurfactant-loaded nanoparticles in MDA-MB-231 cancer cells compared to biosurfactant-loaded plain nanoparticles. Induction of apoptosis was observed in cancer cells by these nanoparticles. We explore a potential anticancer agent that can be further analyzed for its efficiency and can be used as an alternative tool.Two imine compounds named as (E)-2-(((3,4-dichlorophenyl)imino)methyl)phenol (DC2H) and (E)-4-(((2,4-dimethylphenyl)imino)methyl)phenol (DM4H) are synthesized, and their crystal structures are verified using the single-crystal X-ray diffraction (XRD) technique. The crystal structures of the compounds are compared with the closely related crystal structures using the Cambridge Structural Database (CSD). The crystal packing in terms of intermolecular interactions is fully explored by Hirshfeld surface analysis. Void analysis is carried out for both compounds to check the strength of the crystal packing. Furthermore, a state-of-the-art dual computational technique consisting of quantum chemical and molecular docking methods is used to shed light on the molecular structure, optoelectronic properties, and bioactivity of indigenously synthesized compounds. The optimized molecular geometries are compared with their counterpart experimental values. Based on previous reports of biofunctions of the indigenously synthesized imine derivatives, they are explored for their potential inhibition properties against two very crucial proteins (main protease (Mpro) and nonstructural protein 9 (NSP9)) of SARS-CoV-2. The calculated interaction energy values of DC2H and DM4H with Mpro are found to be -6.3 and -6.6 kcal/mol, respectively, and for NSP9, the calculated interaction energy value is found to be -6.5 kcal/mol. We believe that the current combined study through experiments and computational techniques will not only pique the interest of the broad scientific community but also evoke interest in their further in vitro and in vivo investigations.