Screening of Inhibitors Targeting Heat Shock Protein 47 Involved in the Development of Idiopathic Pulmonary Fibrosis

Heat shock protein 47 (HSP47), a collagen-specific molecular chaperone, is causally related to fibrotic diseases, including idiopathic pulmonary fibrosis. The identification of Compounds that interfere with the HSP47-collagen interaction is essential for the development of relevant therapeutics. Herein, we prepared human HSP47 as a soluble fusion protein expressed in E. coli and established an assay system for HSP47 inhibitor screening. We screened a natural and synthetic Compound library established at Nagasaki University. Among 1023 Compounds, 13 exhibited inhibitory activity against human HSP47, of which three inhibited its function in a dose-dependent manner. Epigallocatechin-3-O-gallate, one of these three Compounds, is a typical polyphenol Compound derived from tea leaves. Structurally related Compounds were synthesized and examined for their activity, revealing a hydroxyl group at A-ring position 5 as important for its activity. The present findings provide valuable insight for the development of natural product-derived therapeutics for fibrotic diseases, including idiopathic pulmonary fibrosis.     

基于水质模拟的水质在线监测站点布设研究

随着水质监测连续化的需求增加,河流水质在线监测站布设成为不可忽视的问题。本文采用水文模拟模型HSPF对台湾淡水河流域进行水量水质联合模拟。水文模拟以9个测站比对,纳什效率系数多数大于0.7;相关系数r皆大于0.7。水质模拟以27个测站比对,生化需氧量、氨氮、悬浮固体、溶氧的修正平均百分误差多数小于25%。基于水质变化率和水质超标率提出水质敏感河段概念,并以此确定为补充布设水质在线监测站点的优先河段。研究指出,淡水河流域水质在线监测站目前仍缺乏且位置不尽合理,应优先补充三峡河的三峡大桥、景美溪的宝桥、基隆河的江北桥水质在线监测站。     

基于长短期记忆网络的电网故障区域定位与故障传播路径推理

为了在发生故障后维持电力系统的安全稳定,有必要实现对故障区域的快速定位并确定故障冲击的传播路径,提出基于长短期记忆网络(LSTM)的故障区域定位和故障传播路径推理方法.首先,利用LSTM建立2个故障诊断模型分别实现在线检测故障时刻和确定故障区域;然后,通过计算故障点附近线路的端口供给能量确定故障冲击的传播路径;最后,以8机36节点电网为例进行算例验证,结果表明所提模型可在发生故障后短时间内检测到故障,给出故障区域和故障冲击传播的路径,且对噪声有较强的鲁棒性.     

Nephrotoxicity of Herbal Products in Europe—A Review of an Underestimated Problem

Currently in Europe, despite the many advances in production technology of synthetic drugs, the interest in natural herbal medicines continues to increase. One of the reasons for their popular use is the assumption that natural equals safe. However, herbal medicines contain pharmacologically active ingredients, some of which have been associated with adverse effects. Kidneys are particularly susceptible to injury induced by toxins, including poisonous constituents from medicinal plants. The most recognized herb-induced kidney injury is aristolochic acid nephropathy connected with misuse of certain Traditional Chinese herbal medicines. Data concerning nephrotoxicity of plant species of European origin are scarce. Here, we critically review significant data of the nephrotoxicity of several plants used in European phytotherapy, including Artemisia herba-alba, Glycyrrhiza glabra, Euphorbia paralias, and Aloe). Causative mechanisms and factors predisposing to intoxications from the use of herbs are discussed. The basic intention of this review is to improve pharmacovigilance of herbal medicine, especially in patients with chronic kidney diseases.     

Identification of the Catalytic Residues in the Cyclase Domain of the Class IV Lanthipeptide Synthetase SgbL

Lanthipeptides belong to the family of ribosomally synthesized and post-translationally modified peptides (RiPPs) and are subdivided into different classes based on their processing enzymes. The three-domain class IV lanthipeptide synthetases (LanL enzymes) consist of N-terminal lyase, central kinase, and C-terminal cyclase domains. While the catalytic residues of the kinase domains (mediating ATP-dependent Ser/Thr phosphorylations) and the lyase domains (carrying out subsequent phosphoserine/phosphothreonine (pSer/pThr) eliminations to yield dehydroalanine/dehydrobutyrine (Dha/Dhb) residues) have been characterized previously, such studies are missing for LanL cyclase domains. To close this gap of knowledge, this study reports on the identification and validation of the catalytic residues in the cyclase domain of the class IV lanthipeptide synthetase SgbL, which facilitate the nucleophilic attacks by Cys thiols on Dha/Dhb residues for the formation of β-thioether crosslinks.     

碳酸锂在水和NaCl-KCl溶液体系中溶解度的在线测定

碳酸锂溶解度在工业结晶生产中是十分重要的基础数据。采用浸入式红外探头和拉曼探头在线监测溶液体系中CO₃^2-和碳酸锂的特征峰峰强的变化,依据Lambert-Beer定律得出溶液体系中实时在线测定碳酸锂的溶解度。通过在线测定,测得碳酸锂在氯化钠-氯化钾溶液（c_NaCl=0.446 6 mol/L,c_KCl=0.015 8 mol/L）中的溶解度高于在水中的溶解度值。实验测试出的水中碳酸锂的溶解度数据还能与Van′t Hoff方程较好地关联,进一步测算碳酸锂在其他温度下水中的溶解度值。此外,该方法测定的碳酸锂在水中的溶解度数据比文献值中采用重量分析法测试出的溶解度数据偏小,是因为测试装置不同造成的。     

连铸高铝氮积齿轮钢第三脆性区形成机制与控制

钢中的Al、N含量对连铸及其后续加工热塑性和奥氏体晶粒度控制有重要影响,这也是高温渗碳钢与各种Al脱氧钢广泛关注的问题。使用Gleeble 3800热/力学模拟试验机测定了一种轨道交通用高铝氮积齿轮钢(SCM420H)的高温热塑性,并结合差示扫描量热仪(DSC)分析、AlN析出热力学模型以及Schwerdtfeger热塑性特征值计算模型揭示了其第三脆性区的形成机制与调控途径。结果表明,高铝氮积齿轮钢第三脆性区低谷温度范围为750~850 ℃,这是由应力诱导先共析铁素体膜的产生与AlN粒子的大量析出共同导致的。Schwerdtfeger热塑性特征值计算模型可以较准确地预测高铝氮积齿轮钢第三脆性区的上限温度与最小面缩率,但由其预测的热塑性曲线下限温度偏高,应进一步考虑先共析铁素体膜析出的影响,并依据Ar3温度对其进行修正。高Al高N齿轮钢第三脆性区的下限温度取决于其先共析铁素体开始析出温度,主要与钢种成分和铸坯冷却速率相关,连铸生产中可控性有限;但其上限温度则与铸坯应变速率、冷却速率以及钢中的Al、N含量和AlN析出行为均有关联,调控空间较大,应该是连铸生产中合理控制铸坯热塑性与表面裂纹倾向的正确途径。     

在线监测结晶器调宽换向阀阀芯卡阻方法的实现

对某炼钢厂铸机结晶器在线调宽液压系统的工作原理进行了分析,并重点分析了调宽过程中换向阀阀芯卡阻的问题,针对该问题对其液压系统进行了改进,改进后可以在线监测换向阀阀芯是否卡阻。该改进的实施在减少结晶器在线调宽时发生漏钢故障方面起到了重要作用。     

宝钢高速线材轧机的产品现状及展望

介绍了具有当前国际线材生产先进水平的宝钢高速线材轧机的产品特点，及该轧机自投产至今的产品开发情况，并对今后新产品开发工作进行了展望。     

牙科钛及钛合金表面烤瓷研究进展

介绍了中国钛工业发展的历史，钛的资源和钛的应用情况以及钛合金发展所取得的进展，中国钛工业经历了４０余年的研究和发展，目前产能已达到年产３６５０ｔ海绵钛和２８００ｔ钛加工材的生产能力，并建立了一个从海绵钛生产到钛锭熔炼，铸造，加工及钛设备制造的完整的钛工业体系，钛材已被广泛用於化学，宇航，航空等各个工业部门。中国已成长为世界上一个重要的钛工业国，同时还总结了中国钛工业发展的经验和教训；展望了中国钛工