Novel 1,3,5-Triazinyl Aminobenzenesulfonamides Incorporating Aminoalcohol,Aminochalcone and Aminostilbene Structural Motifs as Potent Anti-VRE Agents,and Carbonic Anhydrases I,II, VII,IX, and XII Inhibitors

A series of 1,3,5-triazinyl aminobenzenesulfonamides substituted by aminoalcohol, aminostilbene, and aminochalcone structural motifs was synthesized as potential human carbonic anhydrase (hCA) inhibitors. The compounds were evaluated on their inhibition of tumor-associated hCA IX and hCA XII, hCA VII isoenzyme present in the brain, and physiologically important hCA I and hCA II. While the test compounds had only a negligible effect on physiologically important isoenzymes, many of the studied compounds significantly affected the hCA IX isoenzyme. Several compounds showed activity against hCA XII; (E)-4-{2-[(4-[(2,3-dihydroxypropyl)amino]-6-[(4-styrylphenyl)amino]-1,3,5-triazin-2-yl)amino]ethyl}benzenesulfonamide (31) and (E)-4-{2-[(4-[(4-hydroxyphenyl)amino]-6-[(4-styrylphenyl)amino]-1,3,5-triazin-2-yl)amino]ethyl}benzenesulfonamide (32) were the most effective inhibitors with K_Is = 4.4 and 5.9 nM, respectively. In addition, the compounds were tested against vancomycin-resistant Enterococcus faecalis (VRE) isolates. (E)-4-[2-({4-[(4-cinnamoylphenyl)amino]-6-[(4-hydroxyphenyl)amino]-1,3,5-triazin-2-yl}amino)ethyl]benzenesulfonamide (21) (MIC = 26.33 µM) and derivative 32 (MIC range 13.80–55.20 µM) demonstrated the highest activity against all tested strains. The most active compounds were evaluated for their cytotoxicity against the Human Colorectal Tumor Cell Line (HCT116 p53 +/+). Only 4,4’-[(6-chloro-1,3,5-triazin-2,4-diyl)bis(iminomethylene)]dibenzenesulfonamide (7) and compound 32 demonstrated an IC₅₀ of ca. 6.5 μM; otherwise, the other selected derivatives did not show toxicity at concentrations up to 50 µM. The molecular modeling and docking of active compounds into various hCA isoenzymes, including bacterial carbonic anhydrase, specifically α-CA present in VRE, was performed to try to outline a possible mechanism of selective anti-VRE activity.     

A comparative study of the purification of betanin

Betanin is a natural pigment with antioxidant properties used as a food colourant. This work describes the spectrophotometric and chromatographic quantification of betanin (2S/15S) and its epimer isobetanin (2S/15R) in fresh beetroot juice, food-grade beetroot powder and betanin standard diluted in dextrin. Absorption spectra of all three samples were deconvoluted using a mixed three-function model. Food-grade beetroot powder has the largest amount of violet-red impurities, probably formed during processing. The purification of betanin from these complex matrices was carried out by seven different methods. Ion exchange chromatography was the most efficient method for the purification of betanin from all samples; however, fractions contain high amounts of salt. Reversed-phase HPLC as well as reversed-phase column chromatography also produced good results at a much faster rate. The longer retention time of isobetanin when compared to betanin in reversed-phase conditions has been investigated by means of quantum-mechanical methods.     

人乳与牛乳N-链寡糖组对小鼠肠道菌群的影响

目的:探究人乳N-链寡糖组(human milk N-glycome,HMN)与牛乳N-链寡糖组(bovine milk N-glycome,BMN)对小鼠肠道菌群的影响.方法:以C57BL/6J雄性小鼠为对象,首先在体外测定粪便菌群中与N-链寡糖相关的糖苷酶活性,并模拟粪便菌群对HMN与BMN的利用;然后将小鼠随机分...     

STRNet:Triple-stream Spatiotemporal Relation Network for Action Recognition

Learning comprehensive spatiotemporal features is crucial for human action recognition.Existing methods tend to model the spatiotemporal feature blocks in an in...     

Sulfur in wheat gluten: In situ analysis by X-ray absorption near edge structure (XANES) spectroscopy

The sulfur containing gluten proteins largely determine the baking quality of wheat. In order to probe the speciation of sulfur, gluten proteins [gliadin, high molecular weight (HMW) and low molecular weight (LMW) subunits of glutenin], stored glutenin subunits as well as flour were investigated in situ by S K-edge X-ray near edge absorption structure (XANES) spectroscopy. The spectra confirmed the existence of disulfide bonds in oxidised (oxygen stream) glutenin subunits, supporting their significance for the formation of gluten networks. Additionally, glutenin subunits, which were stored under ambient air and temperature conditions, predominantly contained sulfur of higher oxidation states (sulfoxide, sulfonic acid). The disulfide state and also sulfoxide and sulfonic acid states were detected after reoxidation of glutenin subunits with potassium bromate.     

Silver-Sodium Exchange in Sodium Galliosilicate Glasses

The silver-sodium interdiffusion coefficients of several glasses in the sodium galliosilicate system were determined. The compositional dependence of the interdiffusion coefficient is compared to that observed in the self-diffusion coefficients calculated from dc electrical conductivity data. The observed trends are discussed in terms of a structural model proposed for these glasses.     

The impact of sulfur on the performance of a solid oxide fuel cell (SOFC) system operated with hydrocarboneous fuel gas

The impact of thiophene in the fuel gas of a commercial solid oxide fuel cell (SOFC) system is investigated for concentrations up to 400 ppmV. Based on the measured voltage–current curves, an empiric correlation for the estimation of the expectable power output of the investigated SOFC system when operated with sulfur containing fuel gases is derived. An interrelation between the open circuit voltage (OCV) and the sulfur concentration of the investigated hydrocarboneous fuel gas is presented and discussed based on corresponding model simulations. The reduction of the steam reforming (STR) activity of the anode cermet material and of the catalytic partial oxidation catalyst used for the fuel gas processing in the investigated SOFC system are found important factors regarding the power output reduction induced by sulfur traces in the fuel gas of SOFCs.     

Micro-CT-based identification of double porosity in fired clay ceramics

Optimizing thermal and mechanical properties of clay block masonry requires detailed knowledge on the microstructure of fired clays. We here identify the macro- and microporosity stemming from the use of three different pore-forming agents (expanded polystyrene, sawdust, and paper sludge) in different concentrations. Micro-CT measurements provided access to volume, shape, and orientation of macropores, and in combination with X-ray attenuation averaging and statistical analysis, also to voxel-specific microporosities. Finally, the sum of micro- and macroporosity was compared to corresponding data gained from two statistically and physically independent methods (namely from chemical analysis in combination with weighing, and from mercury intrusion porosimetry). Satisfactory agreement of all these independently gained experimental data renders our new concept for identifying the pore spaces of fired clay as a very promising tool supporting the further optimization of clay blocks.