Mouridsenhammer1261

Here we propose a general strategy to label carbohydrates with N-methyl-anthranilic acid at the anomeric position. Through two examples, we demonstrate that the generated glycoprobes are suitable for fluorescence-based binding/competition assays. Our approach is expected to readily generate series of glycoprobes dedicated to screening assays for the discovery of drugs targeting carbohydrate-protein interactions.An efficient environmentally friendly purely-physical ice-microcrystal pore-forming strategy, consisting of three steps including the water-swelling biomass process utilizing N-methylmorpholine-N-oxide, freeze-drying and one-step carbonization, was developed to prepare a biomass-derived super-flexible high-performance carbon film electrode capable of being repeatedly folded.A highly efficient and asymmetric process to achieve spirocyclic 4-aminopyrazolone derivatives through a cascade Michael addition/cyclization reaction of 4-isothiocyanato pyrazolones with 3-ylideneoxindoles was developed. This reaction forged multicyclic dispiro[pyrazolone-pyrrolidinethione-oxindole] core structures bearing three contiguous stereogenic centers, including two spiro-quaternary stereocenters with excellent diastereo- and enantioselectivities (up to 99% ee, >20  1 dr). The product can be readily diversified to expand the chemical space of spiropyrazolone species. A plausible mechanism to account for the stereochemical course of the cascade process was proposed.Formation of a thermally stiffening microemulsion-based gel showing a nanoconfinement effect of carbohydrates in terms of microviscosity and hydrodynamic diameter of the reverse micelle (specifically with sucrose) is reported. selleckchem The advantage of this gel as an efficient batch bioreactor for entrapped enzymes (horseradish peroxidase and thermophilic α-glucosidase) was shown, and illustrated its potential biocatalytic application at high temperatures.Typically, transition metal catalysis enforces the stereodefined outcome of a reaction. Here we disclose the palladium-catalyzed regio- and stereoselective access to allylic ureas/carbamates and their further exploitation to diverse cyclic structures under operationally simple reaction conditions. This protocol features palladium-catalyzed decarboxylative amidation of highly modular VECs with good to excellent yield, minimal waste production, wide substrate scope, and low catalyst loading. In follow-up chemistry, we demonstrated the debenzylation of vinylic imidazolidinones to N-hydroxycyclic ureas and regioselective derivatization towards the facile synthesis of halohydrins and oxiranes under mild reaction conditions in good to excellent yields.We have prepared several 2,5,8-trialkoxyheptazines starting from the soluble precursor 2,5,8-tris(3,5-diethylpyrazolyl)-heptazine. We present their synthesis along with their promising spectroscopic and electrochemical properties, which demonstrate large band gaps and high reduction potentials altogether. Subsequently, we provide a short assessment of the promising ability of one of these molecules to perform catalytic oxidation test-reactions.Resistance to the platinum-based chemotherapy drug, cisplatin, is a significant setback in ovarian cancer. We engineered fatty acid-like Pt(iv) prodrugs that harness the fatty acid transporter CD36 to facilitate their entry to ovarian cancer cells. We show that these novel constructs effectively kill cisplatin-resistant ovarian cancer cells.In a recent publication [Bergmann et al. Phys. Chem. Chem. Phys., 2018, 20, 5074-5083] we presented a method which enables to investigate the morphology of microgels by superresolution fluorescence microscopy. Here, this method is applied to three microgel species, based on N-isopropylmethacrylamide (NIPMAM), N-n-propylacrylamide (NNPAM) and N-n-propylmethacrylamide (NNPMAM)) with 5, 7.5 and 10 mol% cross-linker, respectively. Super-resolution microscopy reveals differences of the network morphology of the synthesized particles showing the importance of the monomer structure.Electrochemical nanochannel sensors have attracted extensive interest due to their potential applications in biosensing systems. In this work, porous anodized aluminum oxide (AAO) nanochannels are coupled with gold nanoparticles (AuNPs) through a polydopamine (PDA)-induced in situ growth process. It is found that the resulting hybrid nanochannel (denoted as Au-PDA-AAO) can act as both glucose oxidase- and peroxidase-like nanozymes to catalyze the cascade reaction involving glucose. To the best of our knowledge, this is the first report on the synthesis of nanozymes in an AAO nanochannel. Moreover, apart from the nanozyme-catalyzed colorimetric reaction, the Au-PDA-AAO nanochannel could simultaneously serve as a sensitive signal reporter for an electrochemical sensing platform. In such an approach, the glucose oxidation reaction boosts the resistance of the Au-PDA-AAO nanochannel towards ion transport based on the H2O2-mediated size enlargement of AuNPs, resulting in the varied transmembrane ionic current signal of the Au-PDA-AAO nanochannel. On the basis of the changed current-potential properties, the label-free detection of glucose can be achieved with a low detection limit, good reproducibility, and high stability. This work demonstrates the feasibility of the incorporation of versatile nanozymes into AAO nanochannels for mimicking multi-enzymatic catalysis reactions and detecting target analytes.Aristolochic acid I (AA-I) remains a leading cause of aristolochic acid nephropathy (AAN), however few prevention and treatment strategies exist. In this work, the nephroprotective effect of diosgenin, a steroidal saponin distributed abundantly in several plants, on AA-I-induced renal injury and its underlying mechanism were investigated. Sprague-Dawley rats were intragastrically administered with 30 mg kg-1 d-1 diosgenin two hours before exposure to 10 mg kg-1 d-1 AA-I for consecutive four weeks, and the histological change, the renal and liver function, apoptosis, autophagy and the involved pathways were investigated. The results showed that diosgenin relieved AA-I-induced renal histological damage, including mild edematous disorder of renal tubular arrangement and widening of renal tubular lumen. No obvious changes in the hepatic tissue structure were observed in all treatment groups. Moreover, diosgenin up-regulated the expression of Bcl-2 and down-regulated Bax, and subsequently inhibited AIF expression and the cleaved form of Caspase-3, thereby alleviating apoptosis triggered by AA-I.