Exploration of Antimicrobial Ingredients in Psoralea corylifolia L. Seed and Related Mechanism against Methicillin-Resistant Staphylococcus aureus

With the abuse of antibiotics, bacterial antibiotic resistance is becoming a major public healthcare issue. Natural plants, especially traditional Chinese herbal medicines, which have antibacterial activity, are important sources for discovering potential bacteriostatic agents. This study aimed to develop a fast and reliable method for screening out antimicrobial compounds targeting the MRSA membrane from Psoralea corylifolia Linn. seed. A UPLC-MS/MS method was applied to identify the prenylated flavonoids in major fractions from the extracts of Psoralea corylifolia Linn. seed. The broth microdilution method was used to determine the minimum inhibitory concentrations (MICs) of different fractions and compounds. The morphological and ultrastructural changes of MRSA were determined by scanning electron microscopy (SEM). The membrane-targeting mechanism of the active ingredients was explored by membrane integrity assays, membrane fluidity assays, membrane potential assays, ATP, and ROS determination. We identified eight prenylated flavonoids in Psoralea corylifolia Linn. seed. The antibacterial activity and mechanism studies showed that this type of compound has a unique destructive effect on MRSA cell membranes and does not result in drug resistance. The results revealed that prenylated flavonoids in Psoralea corylifolia Linn. seeds are promising candidates for the development of novel antibiotic agents to combat MRSA-associated infections.     

Synthesis of Potential Antiviral Agents for SARS-CoV-2 Using Molecular Hybridization Approach

We synthesized a set of small molecules using a molecular hybridization approach with good yields. The antiviral properties of the synthesized conjugates against the SAR-CoV-2 virus were investigated and their cytotoxicity was also determined. Among all the synthesized conjugates, compound 9f showed potential against SARS-CoV-2 and low cytotoxicity. The conjugates’ selectivity indexes (SIs) were determined to correlate the antiviral properties and cytotoxicity. The observed biological data were further validated using computational studies.     

New 11-Methoxymethylgermacranolides from the Whole Plant of Carpesium divaricatum

Eight new 11-methoxymethylgermacranolides (1–8) were isolated from the ethanol extract of the whole plant of Carpesium divaricatum. The planar structures and relative configurations of the new compounds were determined by detailed spectroscopic analysis. The absolute configuration of 1 was established by electronic circular dichroism (ECD) spectrum and X-ray crystallographic analysis, and the stereochemistry of the new compounds 2–8 were determined by similar ECD data with 1. The absolute configurations of 5 and 7 were further confirmed by using quantum chemical electronic circular dichroism (ECD) calculations. Compound 4 exhibited weak cytotoxicity against MCF-7 cells. Compound 8 could potently decrease PGE2 productions in LPS-induced RAW 264.7 cells.     

基于Kr工质的离子推力器栅极PIC仿真

Kr是新型低成本离子推力器的优选工质之一。采用三维PIC粒子模拟方法对Kr等离子体在栅极系统中的输运过程进行仿真,并与Xe工质仿真结果进行对比,分析工质类型对束流分布、离子通过率、发散角损失和推力等参数特性和分布的影响。结果表明：相比于Xe工质,Kr工质条件下,屏栅上游鞘层区域更大,屏栅离子通过率略有上升;Kr+在加速栅孔轴向速度较大,径向位移小,撞击加速栅几率小,加速栅电流相对较小;Kr工质和Xe工质的发散角损失相当,但Kr工质工作电流区域更高;相比于Xe工质,相同功率条件下Kr工质的推力值约降低20%。     

中能电子成像仪探头的设计

利用小孔成像原理对中能电子成像仪探头的机械结构进行了设计,为保证探头单元暴露于外辐射带辐射环境12年的总剂量小于5 krad,确定其壳体厚度为约3 mm的铜,探头的角分辨率为20;根据带电粒子在硅中的能量损失规律对探测器进行了防质子污染设计,确定了探测器厚度为1000 m,其屏蔽层厚度为10 m等效硅。最后对设计探头的质子污染率进行了计算,结果表明该中能电子成像仪探头的设计满足外辐射带空间中能电子探测的需求,为中能电子成像仪的研制奠定了基础。     

Investigation on effects of new physics in c→(s,d)e+ve transitions

Anomalies in decays induced by b → ce-(v)e(e =e,μ,τ) transitions may imply lepton flavor universality violations,which raises questions on such phenomena in the...     

Growth and raman scattering of aluminium gallium orthophosphate piezoelectric crystals

A new series of non-ferroelectric crystals, the piezoelectric solid solution aluminium gallium orthophosphate Al_1-xGa_xPO₄ (AGP, 0 < x < 1) system has been successfully developed by a hydrothermal method. The AGP crystal with X = 0.10 shows a phase transition temperature T_−β = 587 ± 3 °C with a cell parameters A = b = 0.49386(3) and C = 1.09563(2) nm. Raman spectra including directional dispersion in AGP are similar to those from -AIPO4 and -quartz crystals, indicating all of them belong to an isomorphic family, the short-range interaction being dominant in AGP. Comparison with -AIPO4 crystals, there exists an apparent red shift of the mode frequency and a smaller TO/LO mode splitting of the E species in the AGP crystals.     

Design, synthesis and antitumor activity of 3-substituted quinolone derivatives (Ⅰ)

A series of quinolone derivatives containing benzimidazole, benzoxazole or benzothiazole ring were synthesized. The cytotoxicity of 12 new compounds was evaluated in KB, Be17402, A2780 and HT-29 cell lines. Most of synthesized compounds showed moderate inhibitory activity against cancer cells. The inhibitory activities of 6k, against KB and A2780 tumor cells are comparable to that of topotecan, one of topoisomerase I inhibitors.     

Direct electrochemistry and electrochemical catalysis of immobilized hemoglobin in an ethanol–water mixture

Hemoglobin (Hb) was immobilized on a glassy carbon electrode (GCE) surface by konjac glucomannan (KGM). KGM hydrogel films on GCE have relatively high stabilities in aqueous–ethanol mixtures. The entrapped hemoglobin undergoes fast direct electron transfer reactions in aqueous–organic solvent mixtures. The peak current is bigger, the peak-to-peak separation smaller and the formal potential observed in the cyclic voltammogram is more negative for Hb–KGM/GCE in ethanol–PBS compared to Hb–KGM/GCE in PBS. The electrochemical properties of the Hb in aqueous–organic solution are almost unchanged from with those observed for the purely aqueous solution, suggesting that water pools in the KGM hydrogel play an important role in preventing changes in conformation and making proteins unreactive with polar organic solvents. The immobilized Hb was able to catalyze the reduction of nitric oxide, peroxides (hydrogen peroxide, cumene hydroperoxide, t-butyl hydroperoxide, 2-butanone peroxide), and the dehalogenation of haloethanes (hexachloroethane, pentachloroethane, tetrachloroethane, etc.). The stability and reproducibility of the modified electrode meant that it could be used to determine these substances.