The Antibacterial Drug Candidate SBC3 is a Potent Inhibitor of Bacterial Thioredoxin Reductase

Antibiotic resistance is a growing problem for public health and associated with increasing economic costs and mortality rates. Silver and silver-related compounds have been used for centuries due to their antimicrobial properties. In this work, we show that 1,3-dibenzyl-4,5-diphenyl-imidazol-2-ylidene silver(I) acetate/NHC*-Ag-OAc (SBC3) is a reversible, high affinity inhibitor of E. coli thioredoxin reductase (TrxR; K_i=10.8±1.2 nM). Minimal inhibition concentration (MIC) tests with different E. coli and P. aeruginosa strains demonstrated that SBC3 can efficiently inhibit bacterial cell growth, especially in combination with established antibiotics like gentamicin. Our results show that SBC3 is a promising antibiotic drug candidate targeting bacterial TrxR.     

Microstructural,mechanical properties and strengthening mechanism of DLP produced β-tricalcium phosphate scaffolds by incorporation of MgO/ZnO/58S bioglass

The inherent brittleness of bioceramics restricts their applications in load-bearing implant, although they possess good biocompatibility and bioactivity. ZnO, MgO and 58S bioglass (BG) were incorporated as additives to further improve the mechanical properties and biocompatibility of β-TCP and ZnO/MgO/BG-β-TCP composite scaffolds were manufactured via digital light processing (DLP). The composite with the best comprehensive performance was selected for degradation behavior and biocompatibility evaluation. The effects of different proportions of ZnO/MgO/BG on mechanical strength were analyzed and ZnO0·5/MgO1/BG2-β-TCP (ZMBT) samples exhibited superior mechanical strength. The improvement by 272% and 99% respectively was achieved in fracture toughness and compressive strength with the optimal recipe. The enhancement effect is realized through phase transition, alterative sliding actions and transgranular fracture to effectively prevent the load transfer combining the functions of bioglass and metal oxide. ZMBT scaffolds exhibited a more desirable pH environment and an enhanced ability of apatite-mineralization formation, meanwhile Si⁴⁺, Mg²⁺ and Zn²⁺ were gradually released from scaffolds. Furthermore, in vitro evaluation indicated that ZMBT scaffolds presented not only excellent cell attachment, proliferation, alkaline phosphatase (ALP) activity, but they up-regulated osteogenic gene (ALP, OCN, Runx2). These results suggest that the addition of ZnO/MgO/BG to DLP-printed β-TCP scaffolds offer a smart strategy to fabricate porous scaffolds with conspicuously better biological and physicochemical properties including compressive strength, bioactivity, osteogenesis and osteogenesis-related gene expression. Metal-oxide and BG synergistically enhanced the mechanical and biological properties which make the ZMBT scaffolds a strong candidate for bone repair applications.     

Changes in the content and antioxidative activity of β-carotene and its metabolite vitamin A during gastrointestinal digestion and absorption and optimisation of HPLC-based detection

The β-Carotene (BC), an important precursor of vitamin A (VA), possesses antioxidant activity but is fat-soluble and has low bioavailability. In previous in-vitro assays evaluating antioxidant and 2,2′-azobis(2-amidinopropane) dihydrochloride (AAPH) free radical scavenging, both BC and VA showed a strong ability to scavenge radicals and protected cells from oxidative stress. Here, we used artificially simulated gastrointestinal digestion and Caco-2 cell absorption models to evaluate the bioavailability of the BC during gastrointestinal digestion and absorption using high-performance liquid chromatography (HPLC) analysis. We observed high absorptive and transfer rates of BC and detected retinol metabolites (Vitamin A). Therefore, BC can be detected in the acidic gastrointestinal environment using HPLC. Optimised method provided better separation of BC and VA in the column, improving the accuracy of the test results.     

Synergistic effect of high-intensity ultrasound and β-cyclodextrin treatments on browning control in apple juice

This work evaluated the synergistic effects of combined high-intensity ultrasound (HIU) with β-cyclodextrin (β-CD) treatments on inhibiting browning of apple juice and explored the mechanism through simulation system. The combined treatment of 300 W HIU with 0.006 g mL⁻¹ β-CD had a synergistic impact on maintaining juice colour, resulting in a 39.06% reduction in browning degree, only a 36.64% decrease in total phenolic content, and a 17.82% reduction in PPO activity. The inhibition of enzymatic browning in simulated system revealed that HIU suppressed the enzyme (Polyphenol oxidase, PPO) and β-CD inhibited enzyme (PPO) and embedded substrate (polyphenol). The results of spectroscopic analysis showed that the particle-size distribution of PPO narrowed, the content of α-helix in the secondary structure increased, the fluorescence intensity increased, and the maximum wavelength was red-shifted after HIU and β-CD treatment. Changes in structure could further result in PPO activity loss. Hence, the combined treatment could synthetically alleviate the browning of apple juice.     

Effects of Z-value on physicochemical and biological properties of β-SiAlONs ceramics

This study evaluated the effects of different Z-values on the physical, chemical, and biological properties of β-SiAlON ceramics. Increasing the Z-value of the β-Si₃N₄ solid solution's main phase resulted in the replacement of Si–N bonds with Al–O bonds. The number of columnar crystals decreased, bulk density increased, and porosity decreased, thus transforming the fine-particle microstructure of β-Si₃N₄ into the columnar structure of β-SiAlON. The compressive strength increased, which facilitated sintering at 1500 °C without sintering auxiliaries. H⁺ and OH⁻ ions in deionized water broke the covalent bonds on the β-SiAlON surface, thereby forming new Si–OH, Al–OH, and N–H bonds on the β-SiAlON surface and producing SiO₄⁴⁻, AlO₂⁻, and NH₄⁺ groups in the solution. Increasing the soaking time changed the compositions of ionized H⁺ and OH⁻ ions, thus increasing the pH. MC3T3-E1 cells were cultured on the β-SiAlON surface, and it was observed that the increase in the Z-value of β-SiAlON had no influence on cell adhesion and spreading, but it may slightly suppress cell proliferation at high Z-values. At low Z-values, the low AlO₂⁻ concentration helps promote osteogenic differentiation and mineralized nodule formation. Thus, β-SiAlON ceramics possess excellent physical, chemical, and biological properties and are considered excellent bone-repairing materials.     

IκB激酶β在肿瘤中的作用及其抑制剂的研究进展

近年来，IκB激酶β（inhibitor kappa B kinaseβ, IKKβ）在肿瘤发生发展过程中的作用逐渐被发现。IKKβ通过作用多种分子通路参与肿瘤细胞增殖、存活等过程，抑制IKKβ已被确定为治疗癌症有希望的手段。研究人员开发一系列IKKβ抑制剂，发现它们能够有效抑制肿瘤的生长，但目前尚无IKKβ抑制剂投入到临床上治疗癌症。在这篇综述中，我们将介绍IKKβ介导肿瘤发生发展及主要IKKβ抑制剂的研究进展。     

Evaluating the profile of myofibrillar proteins and its relationship with tenderness among five styles of dry-cured hams

In order to investigate the relationship between profile of myofibrillar proteins and tenderness among 2 kinds of Chinese hams (Jinhua and Xuanwei) and 3 kinds of European hams (Iberian, Serrano and Parma), shear force, myofibril fragmentation index (MFI), SDS-PAGE, carbonyls content and Raman spectroscopy were investigated. The shear force and salt content of Chinese hams were significantly higher than that of European hams, while moisture content was lower than that of European hams (p < 0.05). MFI values and SDS-PAGE profile revealed that the degradation of myofibrillar proteins in Chinese hams was lower than in European hams. In addition, Chinese hams showed significantly higher carbonyls content and β-sheet content compared with European hams, indicated that proteins aggregation intensively inhibited the degradation of myofibrillar proteins in Chinese hams. These results indicated that the higher shear force in Chinese style hams could be attributed to the lower moisture content and limited proteolysis.     

亲水作用色谱-串联质谱法测定动物源运动食品中3种氨基糖苷类抗生素的残留量

该研究建立了一种亲水交互作用色谱-串联质谱（HILIC-MS/MS）法测定动物源运动食品中潮霉素B、新霉素、安普霉素3种氨基糖苷类抗生素残留量的方法。结果表明，样品经Sielc Obelisc R柱分离，采用0.1%甲酸水溶液-乙腈梯度洗脱，可以实现3种目标物组分的分离。在此条件下，3种氨基糖苷类抗生素在5～500 ng/mL的质量浓度范围内线性关系良好，相关系数R2为0.999 5～0.999 9，检出限均为15 μg/kg，定量限均为50 μg/kg，保留时间的日间和日内相对标准偏差（RSD）分别为3.5%～7.9%和3.5%～4.1%，峰面积的日间和日内RSD分别为3.6%～7.4%和3.2%～3.9%，加标回收率为85.7%～93.6%，回收率试验结果的RSD为3.1%～5.2%。该方法可以满足动物源运动食品中3种氨基糖苷类抗生素的检测需求。