Pyrazole-Thiazole Core-Containing Analogs Exhibit Adjunctive Activity with Meropenem against Carbapenem-Resistant Enterobacteriaceae (CRE)

Pyrazole-thiazole core-containing compound KP-40 and 20 novel derivatives were designed and synthesized through traditional SAR analysis. These molecules displayed adjunctive activity with meropenem against Gram-negative bacteria evidenced by a range of fractional inhibitory concentration (FIC=0.5–0.25) and minimum adjunctive concentration (MAC=128–32 μM) values. Of this series of molecules, four compounds displayed notable adjunctive potential, with FIC and MAC values of 0.25 and 32 μM, respectively. Moreover, the solubility of these compounds was improved to an acceptable range. Further analysis using our “in house” permeation and efflux multi parameter optimization (PEMPO) algorithm revealed key physicochemical properties that may be critical for the development of active Gram-negative antibacterials. Taking PEMPO scores into consideration prior to executing synthesis of analogs may be a simple, yet rapid and effective strategy that can be used in conjunction with traditional SAR approaches to aid in the design of potent Gram-negative antibacterials.     

Compliance-based testing method for fatigue crack propagation rates of mixed-mode I–II cracks

Science China Technological Sciences - Mixed-mode I-II crack-based fatigue crack propagation (FCPI-II) usually occurs in engineering structures; however, no theoretical formula or effective...     

Inorganic Nanoparticles Applied as Functional Therapeutics

Inorganic nanoparticles (NPs) offer significant advantages to the biomedical field owing to their large surface area, controllable structures, diverse surface chemistry, and unique optical and physical properties. Researchers worldwide have shown that inorganic NPs and the released metal ions can act as therapeutic agents in targeted tissues or to cure various diseases without acute toxicity. In this progress report, the recent developments in inorganic NPs with different compositions directly used as therapeutics are discussed. First, the recent convergence of nanotechnology and biotechnology in biomedical applications as well as the unique functions, features, and advantages of inorganic NPs in biomedical applications are summarized. Thereafter, the biological effects of inorganic compositions in NPs which include balancing the intracellular redox environment, regulating the specific cellular signaling and cellular behaviors, and apoptosis are explained. In addition, the emerging therapeutic applications of inorganic NPs in various diseases are exemplified. Finally, the perspectives and challenges for overcoming the weaknesses of inorganic NPs as therapeutics are discussed. By carefully considering and investigating the biological effects of inorganic NPs and metal ions released from NPs, more promising inorganic NPs based therapeutic agents can be developed.     

The effect of alkali metal oxide on the properties of borosilicate fireproof glass: Structure,thermal properties,viscosity, chemical stability

The purpose of the current work was to research the effect of alkali metal oxide on the structure, thermal properties, viscosity and chemical stability in the glass system (R₂O–CaO–B₂O₃–SiO₂) systematically. Because the glass would emulsify when Li₂O was added to the glass batch, this article did not discuss Li₂O. The results showed that when the amount of Na₂O was less than 4 mol.%, there was a higher interconnectivity of borate and silicate sub-networks in glass, as more mixed Si–O–B bonds were present in glass. The glass samples exhibited excellent thermal properties and chemical stabilities. As the amount of Na₂O exceeded 4 mol.%, the interconnectivity of borate and silicate sub-networks was weakened. The thermal properties and chemical stabilities of the glass samples were reduced. The connectivity of the silicate sub-network was weakened slightly as the Na/K ratio varied, and the coefficient of thermal expansion (CTE) of the glass samples gradually increased, and the resistance to thermal shock (RTS) value gradually decreased. Moreover, the viscosity of the glass samples decreased with the ratio of Na/Si and Na/K increased.     

No-reference quality assessment of dynamic sports videos based on a spatiotemporal motion model

This paper proposes an approach to improve the performance of no-reference video quality assessment for sports videos with dynamic motion scenes using an efficient spatiotemporal model. In the proposed method, we divide the video sequences into video blocks and apply a 3D shearlet transform that can efficiently extract primary spatiotemporal features to capture dynamic natural motion scene statistics from the incoming video blocks. The concatenation of a deep residual bidirectional gated recurrent neural network and logistic regression is used to learn the spatiotemporal correlation more robustly and predict the perceptual quality score. In addition, conditional video block-wise constraints are incorporated into the objective function to improve quality estimation performance for the entire video. The experimental results show that the proposed method extracts spatiotemporal motion information more effectively and predicts the video quality with higher accuracy than the conventional no-reference video quality assessment methods.     

Investigation of bacterial and fungal communities in indoor and outdoor air of elementary school classrooms by 16S rRNA gene and ITS region sequencing

The advent of high-throughput sequencing methods allowed researchers to fully characterize microbial community in environmental samples, which is crucial to better understand their health effects upon exposures. In our study, we investigated bacterial and fungal community in indoor and outdoor air of nine classrooms in three elementary schools in Seoul, Korea. The extracted bacterial 16S rRNA gene and fungal ITS regions were sequenced, and their taxa were identified. Quantitative polymerase chain reaction for total bacteria DNA was also performed. The bacterial community was richer in outdoor air than classroom air, whereas fungal diversity was similar indoors and outdoors. Bacteria such as Enhydrobacter, Micrococcus, and Staphylococcus that are generally found in human skin, mucous membrane, and intestine were found in great abundance. For fungi, Cladosporium, Clitocybe, and Daedaleopsis were the most abundant genera in classroom air and mostly related to outdoor plants. Bacterial community composition in classroom air was similar among all classrooms but differed from that in outdoor air. However, indoor and outdoor fungal community compositions were similar for the same school but different among schools. Our study indicated the main source of airborne bacteria in classrooms was likely human occupants; however, classroom airborne fungi most likely originated from outdoors.     

Influence of bio-clogging on permeability characteristics of soil

It is necessary to enhance the barrier performance of cutoff walls in order to improve the contamination control level, especially for reconstruction or expansion of existing landfill sites. This paper presents a comprehensive laboratory investigation on the synergistic effects of microorganisms and fibers on the hydraulic conductivity of silty sand to evaluate the applicability to the field condition as an alterative barrier material. Inside the soil, the added carbon fibers not only provided good biocompatibility, but also formed spatial three-dimensional network between soil particles to improve the bacterial adhesion that eventually caused 2–3 orders of magnitude decrease in soil permeability. The resistance of the biofilm to extreme conditions was tested by permeation with solutions of different salinity and pH values, and by subjecting specimens to various hydraulic gradients and soil conditions. Despite the microbial growth inhibition occurred at these conditions, however, biofilm can largely remain intact and continue to reduce k, which due to the gradual adaptation of microorganisms to the extreme environment and the gradual recovery of their activity. Results of these tests demonstrate that biofilm treatment may be a feasible technology for creating waste containment barriers in soil.     

Combination of vegetable soup and glucan demonstrates synergistic effects on macrophage-mediated immune responses

Vegetable soup (VS), a plant-based functional food, has been used as a traditional folk medicine and is attracting attention for its ability to enhance the immune response. β-Glucan, a well-established and effective immunomodulator, has synergistic effects when used in combination with some bioactive compounds. In the present study, we aimed to evaluate the synergistic immunomodulatory effects of the combination of VS and β-glucan on macrophage-mediated immune responses. β-Glucan was demonstrated to synergistically enhance the VS-stimulated immune response, including the production of interleukin-6, tumor necrosis factor-α, and nitric oxide, mainly through the mitogen-activated protein kinase pathway in macrophages. In addition, this combination has the potential for further development in functional foods with immune-enhancing activity.Supplementary InformationThe online version contains supplementary material available at 10.1007/s10068-021-00888-x.     

Dysprosium doped copper oxide (Cu1-xDyxO) nanoparticles enabled bifunctional electrode for overall water splitting

The production of hydrogen, a favourable alternative to an unsustainable fossil fuel remains as a significant hurdle with the pertaining challenge in the design of proficient, highly productive and sustainable electrocatalyst for both oxygen evolution reaction (OER) and hydrogen evolution reaction (HER). Herein, the dysprosium (Dy) doped copper oxide (Cu_1-xDy_xO) nanoparticles were synthesized via solution combustion technique and utilized as a non-noble metal based bi-functional electrocatalyst for overall water splitting. Due to the improved surface to volume ratio and conductivity, the optimized Cu_1-xDy_xO (x = 0.01, 0.02) electrocatalysts exhibited impressive HER and OER performance respectively in 1 M KOH delivering a current density of 10 mAcm^?2 at a potential of ?0.18 V vs RHE for HER and 1.53 V vs RHE for OER. Moreover, the Dy doped CuO electrocatalyst used as a bi-functional catalyst for overall water splitting achieved a potential of 1.56 V at a current density 10 mAcm^?2 and relatively high current density of 66 mAcm^?2 at a peak potential of 2 V. A long term stability of 24 h was achieved for a cell voltage of 2.2 V at a constant current density of 30 mAcm^?2 with only 10% of the initial current loss. This showcases the accumulative opportunity of dysprosium as a dopant in CuO nanoparticles for fabricating a highly effective and low-cost bi-functional electrocatalyst for overall water splitting.     

The peptides in oat and malt extracts that are preferentially absorbed by Lactobacillus plantarum and stimulates its proliferation in milk

Lactobacillus plantarum proliferates inefficiently in milk, mainly because of its lack of cell envelope proteases and its inability to hydrolyse proteins in milk. Our previous study showed that this strain could grow well in milk with the addition of oat and malt extracts. To investigate the usage and preference for polypeptides and oligopeptides for this strain, sodium dodecyl sulphate-polyacrylamide gel electrophoresis (SDS-PAGE), o-phthaldialdehyde (OPA), high-performance liquid chromatography (HPLC), plate counting and other methods were used in this study. The results showed that proteins in fermented milk cannot be absorbed and utilised by L. plantarum, whereas polypeptides and oligopeptides provide available nitrogen sources for their growth. Short-chain peptides were more conducive to absorption and utilisation than long-chain peptides. In particular, peptides with molecular weights in the range of 200–1400 Da in the oat extract and 100–700 Da in the malt extract were preferentially absorbed and utilised.