Anti-fibrosis attributes: UHPLC-MS/MS-based pharmacokinetics profiling of a novel autotaxin inhibitor with excellent in vivo efficacy in rat

3,4-Difluorobenzyl(1-ethyl-5-(4-((4-hydroxypiperidin-1-yl)-methyl)thiazol-2-yl)-1H-indol-3-yl)carbamate (NAI59), a small molecule with outstanding therapeutic effectiveness to anti-pulmonary fibrosis, was developed as an autotaxin inhibitor candidate compound. To evaluate the pharmacokinetics and plasma protein binding of NAI59, a UPLC–MS/MS method was developed to quantify NAI59 in plasma and phosphate-buffered saline. The calibration curve linearity ranged from 9.95 to 1990.00 ng/mL in plasma. The accuracy was −6.8 to 5.9%, and the intra- and inter-day precision was within 15%. The matrix effect and recovery, as well as dilution integrity, were within the criteria. The chromatographic and mass spectrometric conditions were also feasible to determine phosphate-buffered saline samples, and it has been proved that this method exhibits good precision and accuracy in the range of 9.95–497.50 ng/mL in phosphate-buffered saline. This study is the first to determine the pharmacokinetics, absolute bioavailability, and plasma protein binding of NAI59 in rats using this established method. Therefore, the pharmacokinetic profiles of NAI59 showed a dose-dependent relationship after oral administration, and the absolute bioavailability in rats was 6.3%. In addition, the results of protein binding showed that the combining capacity of NAI59 with plasma protein attained 90% and increased with the increase in drug concentration.     

Space-Confined Atomic Clusters Catalyze Superassembly of Silicon Nanodots within Carbon Frameworks for Use in Lithium-Ion Batteries

Incorporating nanoscale Si into a carbon matrix with high dispersity is desirable for the preparation of lithium-ion batteries (LIBs) but remains challenging. A space-confined catalytic strategy is proposed for direct superassembly of Si nanodots within a carbon (Si NDs⊂C) framework by copyrolysis of triphenyltin hydride (TPT) and diphenylsilane (DPS), where Sn atomic clusters created from TPT pyrolysis serve as the catalyst for DPS pyrolysis and Si catalytic growth. The use of Sn atomic cluster catalysts alters the reaction pathway to avoid SiC generation and enable formation of Si NDs with reduced dimensions. A typical Si NDs⊂C framework demonstrates a remarkable comprehensive performance comparable to other Si-based high-performance half LIBs, and higher energy densities compared to commercial full LIBs, as a consequence of the high dispersity of Si NDs with low lithiation stress. Supported by mechanic simulations, this study paves the way for construction of Si/C composites suitable for applications in future energy technologies.     

桉树杂交种与其亲本的近红外光谱判别

研究桉树控制授粉后目标性状的基因作用方式是探索其基因重组规律的重要内容。常规的数量统计分析精度往往不高,而DNA分析的专业要求高,且费时费力。该研究利用近红外光谱(NIRs)研究不同基因型桉树杂交种、亲本及杂交种与亲本间近红外光谱信息的关系,探索NIRs用于桉树杂交种与其亲本判别的可行性和准确性。以控制授粉的桉树亲本及其杂交F1代材料为对象,每种基因型从各自田间试验分别选取10个单株,采集树冠中上部新鲜健康叶片。用手持式近红外仪Phazir Rx(1624)采集桉树杂交种与其亲本叶片的NIRs信息。每单株选10片完全生理成熟的健康叶片,避开叶脉扫描其正面光谱5次,以50条NIRs信息的均值代表单个叶片的NIRs信息,最终每个基因型获得10条NIRs信息。对原始NIRs采用二阶多项式S.G一阶导数预处理。预处理后的NIRs用于多元统计分析,首先对桉树杂交亲本和子代样本进行主成分分析(PCA),直观展示不同基因型的分类情况。然后运用簇类独立软模式(SIMCA)和偏最小二乘判别分析(PLS-DA)两种有监督的判别模式验证NIRs用于桉树杂交种与其亲本树种的分类判别效果。PCA结果显示,不同的亲本间、杂交种间及杂交种与亲本间样本的主因子得分可以清晰地将各基因型分开。SIMCA模式判别分析中,桉树杂交种样本到亲本PCA模型的样本距离显示,待判别样本能够形成单独的聚类,且能直观反映两者的遗传相似。PLS-DA判别结果显示,桉树杂交亲本的PLS模型能通过预测其杂交子代的响应变量将其与亲本准确分开。结果表明,桉树叶片的NIRs信息可以准确地反映桉树杂交子代遗传信息的传递规律,NIRs判别模型可以准确地将各种基因型予以区分。因此,NIRs信息不仅可用于桉树杂交种和纯种的定性判别,还可以分析桉树基因重组过程中加性遗传效应的大小,从而为桉树遗传基础分析及其育种改良研究提供理论支撑。     

A New Approach to Develop a Standardized Method for Simultaneous Analysis of Astragaloside IV and Formononetin in Radix Astragali by High-Performance Thin-Layer Chromatography

JPC – Journal of Planar Chromatography – Modern TLC - A new high-performance thin-layer chromatographic (HPTLC) method has been developed for the simultaneous estimation of...     

红外动态场景生成装置空间分辨率的测试

建立了一套基于刀口灰度图红外探测的实验装置,对红外场景生成器的空间分辨率进行了测试。首先通过被测红外场景生成器产生带有刀口标志的红外图像,然后利用红外热像仪采集红外场景生成器所成的红外图像,通过对采集到的红外热图的数据处理,实现了对红外场景生成器空间分辨率的测量。测得的红外场景生成器的空间分辨率为5lp/mm,标准误差为0.04。     

新型4-羟色胺类化合物的合成及生物活性

以4-羟基吲哚为原料,经吲哚环4位乙酰基化、3位亲电取代、酰胺化和还原加氢等反应合成目标化合物7.通过核磁共振氢谱及碳谱对化合物进行结构表征,并对目标化合物进行体外抗氧化生物活性测试.初步生物活性测试结果表明,化合物7a,7b,7c和7d对DPPH·均有很强的清除作用(清除率为85.25%~90.73%),7e,7f,7g,7h作用较差;目标化合物与Vc相比,对·OH的清除作用稍差,最高清除率25.66%(Vc的最高清除率为34.67),但各化合物整体水平相当;在清除O-2·能力上化合物7a,7d,7g,7h最大清除率(分别为19.34,35.35,27.93和31.74)均强于同等浓度的Vc(17.58).     

Cu2O/TiO2-Bi2WO6三元复合催化剂的制备及光催化性能研究

采用水热法制备花状Bi2 WO6,并利用超声分散法制备了Cu2 O/TiO2-Bi2 WO6复合光催化剂,通过FESEM、XRD、XPS、FI-IR、UV-vis DRS和PL对光催化剂进行了分析和表征.表征结果证明:花状Bi2 WO6表面负载着碎片状的TiO2和立方体Cu2 O形成Cu2 O/TiO2-Bi2 WO6复合光催化剂;以短链脂肪酸(SCFAs)为牺牲剂,考察复合光催化剂的光催化产生氢气和烷烃的性能.实验结果表明:Cu2 O/TiO2-Bi2 WO6复合光催化剂以乙酸为牺牲剂,主要产氢气和甲烷,降解率高达91.82;;以丙酸为牺牲剂,产物主要是乙烷和丁烷,降解率高达90.70;;以丁酸为牺牲剂,除了氢气,甲烷,乙烷,丙烷,丁烷外,气体产物还含有一定量的戊烷,其降解率高达91.50;.结合反应液中间产物的成分进行检测,由此推断出光催化反应的可能机理.     

煤直接液化油中混合酚的分离研究

利用分子筛择形特点，对煤直接液化油中的混合酚实施高效分离。本研究选取间甲酚和对甲酚作为分离煤直接液化油馏分段混合酚的模型化合物，采用化学液相沉积法对HZSM-5吸附剂的孔口结构进行改变，分析分子筛硅铝比及颗粒粒径对模型化合物间甲酚和对甲酚吸附分离性能的影响，以获得高性能固相吸附剂，并将其应用于180-190℃馏分段混合酚分离。结果表明，当分子筛硅铝比为25、粒径为3-5 μm时，分子筛的孔口结构调节效果最优；当正硅酸乙酯的最小用量为0.2 mL/g时，固相吸附剂的吸附量为0.03 g/g，对甲酚选择性高于95%。由于外表面沉积物对吸附剂的孔口结构变化，导致对甲酚选择性的提高。进一步采用HZSM-5（1）吸附剂对真实煤直接液化油混合酚的分离中发现，苯酚和对甲酚的选择性均达到100%。