In vitro evaluation and in vivo performance of lyophilized gliclazide

Enhancement of the dissolution rate of the poorly water-soluble hypoglycemic agent, gliclazide, by the aid of lyophilization was investigated. Mannitol, sodium lauryl sulfate (SLS) and polyvinyl pyrrolidone (PVP-k-30) were employed in different weight ratios (43%, 56% and 64% w/w, respectively) as water-soluble excipients in the formulation. Lyophilized systems were found to exhibit extremely higher in vitro dissolution rate compared to the unprocessed drug powder. Solid state characterization of the lyophilized systems using X-ray powder diffraction, Fourier transform infrared spectroscopy and differential scanning calorimetry techniques revealed that dissolution enhancement was attributable to transformation of gliclazide from the crystalline to an amorphous state in the solid dispersion formed during the lyophilization process. The gastrointestinal absorption and hypoglycemic effect of the lyophilized gliclazide/SLS system were investigated following oral administration to Albino rabbits. C_max and area under the plasma concentration–time curve of gliclazide (AUC_0–12) after administration of the lyophilized formulations were significantly higher than those obtained after administration of the unprocessed gliclazide.     

Porous sunflower plate-like NiFe2O4/CoNi–S heterostructure as efficient electrocatalyst for overall water splitting

Constructing high-efficient and nonprecious electrocatalysts is of primary importance for improving the efficiency of water splitting. Herein, a novel sunflower plate-like NiFe₂O₄/CoNi–S nanosheet heterostructure was fabricated via facile hydrothermal and electrodeposition methods. The as-fabricated NiFe₂O₄/CoNi–S heterostructure array exhibits remarkable bifunctional catalytic activity and stability toward oxygen evolution reaction (OER) and hydrogen evolution reaction (HER) in alkaline media. It presents a small overpotential of 219 mV and 149 mV for OER and HER, respectively, to produce a current density of 10 mA cm^?2. More significantly, when the obtained electrodes are used as both the cathode and anode in an electrolyzer, a voltage of 1.57 V is gained at 10 mA cm^?2, with superior stability for 72 h. Such outstanding properties are ascribed to: the 3D porous network structure, which exposes more active sites and accelerates mass transfer and gas bubble emission; the high conductivity of CoNi–S, which provides faster charge transport and thus promotes the electrocatalytic reaction of the composites; and the effective interface engineering between NiFe₂O₄ (excellent performance for OER) and CoNi–S (high activity for HER), which leads to a shorter transport pathway and thus expedites electron transfer. This work provides a new strategy for designing efficient and inexpensive electrocatalysts for water splitting.     

影响煤层气开发效果的地质因素再认识

地质特征认识对煤层气开发效果起着重要作用。在资源特征相差不大的情况下,发现煤层气相邻井的产量差异仍较大。排除工程因素后,通过选取8类地质参数,细致比对了保德区块低产井与邻井的参数特征,筛查出其关键因素为煤层微幅构造与顶板封盖条件,其中以微幅构造为主。据此,重新认识并划分出区块新的次生褶皱背斜单元、向斜单元和斜坡单元,获得了不同次生褶皱构造单元的开发特征。结果表明,高、低产井分布与次生褶皱背斜、向斜相关性高达92%。其中:高产井主要分布在次生褶皱背斜变化较缓、呈隆起状的“平台”,且煤层顶板以泥岩、碳质泥岩为主,封盖性较好;低产井主要分布在次生褶皱向斜,同一井台各井开发效果差异表现为从向斜条带轴部—向斜条带内—向斜条带外的煤层气井平均单井产量不断增加,到向斜轴部的距离大于向斜曲率半径73.5%的范围为主力产气区,小于向斜曲率半径40.0%范围为产水主力区。这对煤层气新井部署、生产管理、开发调整等,具有一定的指导意义。     

Antitumor Effects of Vitamin D Analogs on Hamster and Mouse Melanoma Cell Lines in Relation to Melanin Pigmentation

Deregulated melanogenesis is involved in melanomagenesis and melanoma progression and resistance to therapy. Vitamin D analogs have anti-melanoma activity. While the hypercalcaemic effect of the active form of Vitamin D (1,25(OH)₂D₃) limits its therapeutic use, novel Vitamin D analogs with a modified side chain demonstrate low calcaemic activity. We therefore examined the effect of secosteroidal analogs, both classic (1,25(OH)₂D₃ and 25(OH)D₃), and novel relatively non-calcemic ones (20(OH)D₃, calcipotriol, 21(OH)pD, pD and 20(OH)pL), on proliferation, colony formation in monolayer and soft-agar, and mRNA and protein expression by melanoma cells. Murine B16-F10 and hamster Bomirski Ab cell lines were shown to be effective models to study how melanogenesis affects anti-melanoma treatment. Novel Vitamin D analogs with a short side-chain and lumisterol-like 20(OH)pL efficiently inhibited rodent melanoma growth. Moderate pigmentation sensitized rodent melanoma cells towards Vitamin D analogs, and altered expression of key genes involved in Vitamin D signaling, which was opposite to the effect on heavily pigmented cells. Interestingly, melanogenesis inhibited ligand-induced Vitamin D receptor translocation and ligand-induced expression of VDR and CYP24A1 genes. These findings indicate that melanogenesis can affect the anti-melanoma activity of Vitamin D analogs in a complex manner.     

A facile method for preparation of PGS@ZB‐N and gas‐sol alternating synergistic effect for fire resistance of EVA

Through the simple precipitation of palygorskite (PGS) by zinc borate (ZB) (to make PGS@ZB) and the decoration of PGS@ZB by dodecylamine (N), a novel organic‐inorganic@inorganic hybrid flame retardant of PGS@ZB‐N was prepared and was incorporated with ethylene vinyl acetate copolymer (EVA) to improve its flame retardance. The structure and morphology of PGS@ZB‐N were characterized by Fourier transform infrared (FTIR) spectroscopy, X‐ray diffraction (XRD), and scanning electron microscopy (SEM), and it was confirmed that the PGS@ZB‐N hybrid had been successfully prepared. The flame retardancy and burning behavior of EVA/PGS@ZB‐N/EG (EG = expandable graphite) composite were studied through thermogravimetric analysis (TGA), limiting oxygen index (LOI), UL‐94 (by the vertical burning test), and cone calorimeter test (CCT) characterizations. The prepared EVA/PGS@ZB‐N/EG composite obtained an LOI value of 41.2% with the addition of 30 wt% PGS@ZB‐N/EG. It was found that EVA/PGS@ZB‐N/EG was protected through a gas phase and condensed phase alternating synergistic effect mechanism.     

Influence of the ZrB2 content on the anti-oxidation ability of ZrB2-SiC coatings in aerobic environments with broad temperature range

ZrB₂-SiC coatings with different ZrB₂ contents were prepared by liquid phase sintering. The oxidation processes of coatings were explained according to TG results of ZrB₂-SiC coatings and powders tested from 298 K to 1773 K. Results show that, increasing ZrB₂ content made the weight of the samples changed from weight-loss of 10.04% to weight-gain of 0.14%, while the fastest weight-loss regions were narrowed, whose inflection points reduced from 1310℃ to 1050℃. Increasing ZrB₂ content made the relative oxygen permeability of the ZrB₂-SiC/SiC coatings reduced from 40%–60% to -10%-5%. Increasing ZrB₂ content enhanced high-temperature stability of coatings, making final weight of samples changed from weight-loss of 0.16% to weight-gain of 0.11% after oxidation at 1773 K for 200 h. The peeling and dispersion of Zr-oxides formed Zr-B-Si-O compound glass layer, presenting enhanced stability, dispersion strengthening and pinning effect of Zr-oxides, which were responsible for the excellent anti-oxidation protective effect of coatings in a broad temperature region.     

“Size effect” in the fatigue behavior of Friction Stir Welded plates

Comparative fatigue tests were carried out on Friction Stir Welded specimens of a 2195-T8 aluminum–lithium alloy that differed significantly in width. The width of the larger specimens was over thirteen times greater than that of the small specimens. Fatigue results showed a clear “size effect”, i.e. fatigue life of large specimens was about 40% of the corresponding value of small specimens. The Equivalent Initial Flaw Size methodology was adopted to correlate the two sets of results. Fatigue crack initiation life was disregarded with respect to crack propagation life, and fatigue life was evaluated only as propagation of a small pre-existing defect. Following this methodology, test results of small specimens were used to evaluate the initial equivalent flaw contained in each specimen. It was assumed that this data followed a normal distribution. The equivalent initial flaw in larger specimens was evaluated by simple geometrical considerations. A very good assessment of mean fatigue life and scatter in the fatigue results of large specimens was obtained by simulating the propagation of these defects. Calculations were carried out by taking also welding residual stresses into account, but the results demonstrated that this effect was not significant.     

Facile construction of composition-tuned ruthenium-nickel nanoparticles on g-C3N4 for enhanced hydrolysis of ammonia borane without base additives

Developing high-efficiency and low-cost catalysts for hydrogen evolution from hydrolysis of ammonia borane (AB) is significant and critical for the exploitation and utilization of hydrogen energy. Herein, the in-situ fabrication of well-dispersed and small bimetallic RuNi alloy nanoparticles (NPs) with tuned compositions and concomitant hydrolysis of AB are successfully achieved by using graphitic carbon nitride (g-C₃N₄) as a NP support without additional stabilizing ligands. The optimized Ru₁Ni_7.5/g-C₃N₄ catalyst exhibits an excellent catalytic activity with a high turnover frequency of 901 min^?1 and an activation energy of 28.46 kJ mol^?1 without any base additives, overtaking the activities of many previously reported catalysts for AB hydrolysis. The kinetic studies indicate that the AB hydrolysis over Ru₁Ni_7.5/g-C₃N₄ is first-order and zero-order reactions with respect to the catalyst and AB concentrations, respectively. Ru₁Ni_7.5/g-C₃N₄ has a good recyclability with 46% of the initial catalytic activity retained even after five runs. The high performance of Ru₁Ni_7.5/g-C₃N₄ should be assigned to the small-sized alloy NPs with abundant accessible active sites and the synergistic effect between the composition-tuned Ru–Ni bimetals. This work highlights a potentially powerful and simple strategy for preparing highly active bimetallic alloy catalysts for AB hydrolysis to generate hydrogen.     

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.     

多裂纹混凝土等效断裂模型研究

根据混凝土材料断裂过程区存在尺寸效应这一特点,结合混凝土断裂韧度的尺寸效应规律,对混凝土有效裂缝扩展量进行了研究,得到反映尺寸效应规律的有效裂缝扩展量表达式,进而得到与试件尺寸相关的混凝土多裂纹等效断裂模型,使得多裂纹等效断裂模型更符合断裂过程区的尺寸效应规律。同时,通过与在实际工程中已用的其他模型的计算结果相比较,得出此模型比较可靠的结论。