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Chinese Journal of Natural Medicines 2015年第8期13卷 618-627页

作者： CHEN Ji-Chao duan wen-Li BAI Ren-Ren YAO He-Quan WU Xiao-Ming SHANG Jing XU Jin-Yi State Key Laboratory of Natural Medicines China Pharmaceutical University Department of Medicinal Chemistry China Pharmaceutical University Center for Drug Screening China Pharmaceutical University

In the present study, a series of 13-β-elemene ester derivatives were designed and prepared, and their antioxidant activity was investigated in the H2O2-treated human umbilical vein endothelial cells(HUVECs). Among the test compounds, the dimer compounds 5v and 5w exhibited the most potent antioxidant activity with significant ROS suppression being observed. Both compounds markedly inhibited the H2O2-induced changes in various biochemical substances, such as superoxide dismutase(SOD), malonyldialdehyde(MDA), nitric oxide(NO), and lactic dehydrogenase(LDH), which were superior to that of the positive control vitamin E. Furthermore, they did not produce any obvious cytotoxicity, but increased the viability of HUVECs injured by H2O2 in a dose-dependent manner. Additionally, compound 5w, designed as a prodrug-like compound, showed improved stability relative to compound 4 in vitro.

关键词： β-Elemene Antioxidant HUVECs ROS Stability

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工程造价改革与发展研究

建筑技术 2024年第7期55卷 893-896页

作者：刘刚宁耿辉强王伟段文博王焱张云中国市政工程西南设计研究总院有限公司成都610081 北京住总第二开发建设有限公司北京100011

本研究对工程造价改革方案的总体思路和五项工作任务进行了梳理和详细解读,同时也分析了各地试点省市相关方案的关键内容,并指出各地深化造价改革方案存在的差异。对于造价改革的关注重点与改革方向也进行了深入解读,并提出了相应的观... 详细信息

本研究对工程造价改革方案的总体思路和五项工作任务进行了梳理和详细解读,同时也分析了各地试点省市相关方案的关键内容,并指出各地深化造价改革方案存在的差异。对于造价改革的关注重点与改革方向也进行了深入解读,并提出了相应的观点。在后资质时代工程造价业的发展现状下,对行业存在的核心问题进行了深入剖析,探讨了工程造价在高质量发展要求背景下未来的发展趋势。该研究旨在通过对工程造价改革及未来发展的全面理解,促进行业高质量发展。

关键词：工程造价改革方案监管

Design,synthesis and biological evaluation of O-linked indoles as VEGFR-2 kinase inhibitors(Ⅰ)

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Chinese Chemical Letters 2015年第9期26卷 1165-1168页

作者： Guo-Rui Gao Meng-Yuan Li Lin-Jiang Tong Li-Xin Wei Jian Ding Hua Xie wen-Hu duan School of Pharmacy East China University of Science & Technology Division of Anti-tumor Pharmacology State Key Laboratory of Drug ResearchShanghai Institute of Materia MedicaChinese Academy of Sciences Pharmacology and Safety Evaluation Key Laboratory of Tibetan Medicine in Qinghai Province Northwest Institute of Plateau BiologyChinese Academy of Sciences Department of Medicinal Chemistry Shanghai Institute of Materia MedicaChinese Academy of Sciences

Inhibition of VEGFR-2 signaling pathway has already become one of the most promising approaches for the treatment of *** this study,we describe the design,synthesis,and biological evaluation of a series of O-linked indoles as potent inhibitors of *** these compounds,18 showed significant anti-angiogenesis activities via VEGFR-2 in enzymatic proliferation assays,with IC50 value of3.8 nmol/L Kinase selectivity profiling revealed that 18 was a multitargeted inhibitor,and it also exhibited good potency against VEGFR-1,PDCFR-α and β.

关键词： VEGFR-2 Inhibitor Indole

S1B-2 Therapeutics and Biomarker Development in Huntington’Disease

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神经药理学报 2018年第4期8卷 28-29页

作者： duan wen-zhen Laboratory of Translational Neurobiology Division of NeurobiologyDepartment of Psychiatry and Behavioral SciencesDepartment of NeuroscienceJohns Hopkins University School of Medicine.BaltimoreMarylandUSA

Most neurodegenerative diseases,including Alzheimer’s,Parkinson’s,and Huntington’s disease(HD),have converging pathogenesis,such as formation of abnormal protein aggregates and mitochondrial ***,despite tremendous efforts by many scientists and increasing knowledge about disease mechanisms,we still lack disease-modifying treatments for any of these *** discovery has been revolutionized in the past *** technological advances as a result of substantial investment,the number of new drug approvals remains stagnant and the cost of bringing a drug to market is higher than *** highlights the persistence of a model of drug development that has not adapted to changes in science and public perception of drug *** these diseases affect different areas of the brain and are distinct at the cellular and molecular levels,they share many underlying ***,development of treatment for any of these diseases may provide clues to accelerate the path to the treatment for other neurodegenerative *** into potential therapies for HD is particularly attractive because it is a genetically homogeneous disease for which well-established models *** HD gene encodes the protein huntingtin(Htt),whose polyglutamine expansion is believed to mediate the cytotoxic effects of ***,HD also serves a model for polyglutamine *** is a monogenic neurodegenerative disorder caused by mutation of the gene *** lowering(gene silencing)strategies,including antisense oligonucleotides,shRNA,miRNA et al,have shown great preclinical promise,and the first HTT lowering clinical trial is *** key to success of these trials will be to know where and when to intervene,since these reagents do not penetrate the blood-brain-barrier,and must be delivered directly to the *** is notable for preferential atrophy of the striatum but also involves degeneration in cortex,subcortical white matter,and specif

关键词： experimental promise treatment cellular contribute effects circuit mutation

三黄泻心汤抑制α-淀粉酶及α-葡萄糖苷酶活性成分研究

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时珍国医国药 2024年第4期35卷 795-798页

作者：方鹏霞赵磊段文达武晓玉续艳丽张启立王洁禄国花甘肃中医药大学药学院甘肃兰州730000 西北中藏药省部共建协同创新中心甘肃兰州730000 甘肃省高校中(藏)药化学与质量研究省级重点实验室甘肃兰州730000 甘肃省道地药材质量标准化研究与推广工程实验室甘肃兰州730000 陇药产业创新研究院甘肃兰州730000 兰州市食品药品检验检测研究院甘肃兰州730000

目的筛选三黄泻心汤抑制α-淀粉酶和α-葡萄糖苷酶抑制活性的有效部位,并研究其活性成分。方法三黄泻心汤水煎液采用大孔树脂分段洗脱得到水部位、30%乙醇部位、60%乙醇部位、95%乙醇部位,对水煎液及4个洗脱部位进行α-淀粉酶和α-葡萄... 详细信息

目的筛选三黄泻心汤抑制α-淀粉酶和α-葡萄糖苷酶抑制活性的有效部位,并研究其活性成分。方法三黄泻心汤水煎液采用大孔树脂分段洗脱得到水部位、30%乙醇部位、60%乙醇部位、95%乙醇部位,对水煎液及4个洗脱部位进行α-淀粉酶和α-葡萄糖苷酶体外活性抑制试验,筛选最佳活性部位,再通过高效液相色谱分析其活性成分,并进行方法学考察与含量测定。结果筛选得到抑制α-淀粉酶活性最佳部位为30%乙醇部位,IC50为1.707mg·mL^(-1),活性成分主要有黄芩苷,小檗碱,汉黄芩苷,黄芩素,芦荟大黄素,大黄酸,大黄素,其中黄芩苷含量最高(177.588 mg·g^(-1)),汉黄芩苷次之(30.546 mg·g^(-1));抑制α-葡萄糖苷酶活性最佳部位为60%乙醇部位,IC50为0.0123mg·mL^(-1),活性成分有黄芩苷,小檗碱,汉黄芩苷,黄芩素,芦荟大黄素,大黄酸,大黄素,大黄酚,大黄素甲醚,其中黄芩苷含量最高(181.631mg·g^(-1)),小檗碱次之(71.724 mg·g^(-1))。结论三黄泻心汤在一定程度上对α-淀粉酶及α-葡萄糖苷酶均有活性抑制作用,对α-葡萄糖苷酶的抑制作用优于α-淀粉酶,对开发α-葡萄糖苷酶抑制剂具有一定参考价值。

关键词：三黄泻心汤 α-淀粉酶 α-葡萄糖苷酶抑制作用活性成分

基于AHP/QFD/TRIZ理论的手机包装创新设计

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绿色包装 2024年第4期 153-156页

作者：卢首博马开平李振宇段文浩南京农业大学江苏南京210031

本研究目的为丰富手机包装的应用,扩展使用功能,优化传统手机包装设计,满足当今用户日益多样化的需求。通过问卷调查获取用户需求,利用AHP层次分析法计算各项用户需求综合权重,通过QFD质量功能展开构建用户需求与质量特性的质量屋模型,... 详细信息

本研究目的为丰富手机包装的应用,扩展使用功能,优化传统手机包装设计,满足当今用户日益多样化的需求。通过问卷调查获取用户需求,利用AHP层次分析法计算各项用户需求综合权重,通过QFD质量功能展开构建用户需求与质量特性的质量屋模型,利用TRIZ创新理论提出创新方案解决矛盾。基于AHP/QFD/TRIZ集成理论提出了手机包装创新设计方法,得到了手机包装创新方案,为相关产品的创新设计提供了思路和理论参考。

关键词： AHP TRIZ QFD 创新设计手机包装

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Rh^(III)-Catalyzed heteroarylation of N-2,6-difluoro-phenyl arylamides with heteroaryl boronate esters

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Organic Chemistry Frontiers 2022年第4期9卷 1077-1084页

作者： Jia-Xue Wu Qing-Xia Yao wen-Zeng duan Da-Cheng Li Xian-Qiang Huang Jian-Min Dou Huai-Wei Wang Shandong Provincial Key Laboratory of Chemical Energy Storage and Novel Cell Technology School of Chemistry and Chemical EngineeringLiaocheng UniversityLiaocheng 252000China

Herein,an efficient strategy to achieve aryl-heteroaryl formation via Rh^(III)-catalyzed ortho-C(sp^(2))–H heteroarylation of(hetero)arenes with heterocyclic boronates using a readily removable N-2,6-difluoro-phenyl arylamide directing group has been disclosed.A variety of heteroaromatic boronates as the coupling partners were shown to be able to participate in this protocol,providing the desired hetero-arylated products with high reactivity and good tolerance of functional groups.

关键词： boron esters heterocyclic

化学老化对Zn改性生物炭性质及吸附Pb^(2+)的影响

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中国环境科学 2024年第2期44卷 803-813页

作者：吴宇茜韩琳希钱敏朱自洋王丽段文焱陈芳媛昆明理工大学环境科学与工程学院云南省土壤固碳与污染控制重点实验室云南昆明650500

本文采用60及90℃非生物化学老化方法,对ZnSO_(4)浸渍改性生物炭(PRZn)进行了为期6个月的老化试验.通过元素分析仪,比表面积分析仪,X射线光电子能谱法和傅里叶红外光谱等手段明确老化后生物炭性质的变化特点,并利用等温吸附实验比较老化... 详细信息

本文采用60及90℃非生物化学老化方法,对ZnSO_(4)浸渍改性生物炭(PRZn)进行了为期6个月的老化试验.通过元素分析仪,比表面积分析仪,X射线光电子能谱法和傅里叶红外光谱等手段明确老化后生物炭性质的变化特点,并利用等温吸附实验比较老化对Zn改性生物炭Pb^(2+)吸附性能的差异.结果表明,化学老化过程会生成活性自由基,显著增加生物炭表面含氧官能团的数量,导致500℃制备的PRZn老化后比表面积显著提高(从24.67m^(2)/g提升到85.51m^(2)/g),改性引入的Zn氧化物从晶型结构转化为有机结合态,因此,PRZn经60℃老化后,其对Pb^(2+)的吸附量从31.18mg/g提高至47.70mg/g.但经90℃老化后,700℃制备的PRZn吸附量变化不大,这主要是老化过程中产生的活性氧化物质在90℃下发生自猝灭过程,且700℃制备的PRZn碳结构相对稳定,导致老化后含氧官能团的量没有显著升高而比表面积下降.本研究结果将为改性后老化生物炭在铅污染土壤中的长期利用提供具体理论依据.

关键词： Zn改性生物炭 Pb吸附非生物化学老化长期利用自由基

Effect　of　methylflavonolamine　on　acute　forebrain　is　chemiare　perfusion　in　juryin rat

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中国药理学与毒理学杂志 1996年第2期 10-13页

作者： duan wen-Zhen 1, TANG Yun-Zhao, LIANG Yue-Qin, DUN wen (Department of Pharmacology, Shanxi Medical College, Taiyuan 030001)

用Ｐｕｌｓｉｎｅｌｉ法造成大鼠急性前脑缺血４０ｍｉｎ，然后开夹再灌注１ｈ．在缺血前５ｍｉｎ，再灌前５ｍｉｎ以及再灌３０ｍｉｎ时分别ｉｖ甲基黄酮醇胺（ＭＦＡ）１０和２０ｍｇ·ｋｇ－１．结果表明：ＭＦＡ的两个剂量组均可降... 详细信息

用Ｐｕｌｓｉｎｅｌｉ法造成大鼠急性前脑缺血４０ｍｉｎ，然后开夹再灌注１ｈ．在缺血前５ｍｉｎ，再灌前５ｍｉｎ以及再灌３０ｍｉｎ时分别ｉｖ甲基黄酮醇胺（ＭＦＡ）１０和２０ｍｇ·ｋｇ－１．结果表明：ＭＦＡ的两个剂量组均可降低再灌注引起的脑钙含量增加，减轻脑水肿，抑制脂质过氧化物丙二醛生成，并缓解脑组织中乳酸脱氢酶的释放；同时明显改善脑电图，减轻大脑锥体细胞的变性坏死．提示：ＭＦＡ对大鼠急性脑缺血再灌注损伤有保护作用，其作用可能是通过降低钙在脑组织病理性累积，从而抑制进一步的脂质过氧化等病理生理变化实现的．

关键词：脑缺血再灌注损伤钙甲基黄酮醇胺脑电描记术

Comparative Study of Different SPH Schemes on Simulating Violent Water Wave Impact Flows

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China Ocean Engineering 2014年第6期28卷 791-806页

作者：郑兴马庆位段文洋 College of Shipbuilding Engineering Harbin Engineering University Schools of Engineering and Mathematical Science City University London EC1V 0HB UK

Free surface flows are of significant interest in Computational Fluid Dynamics（CFD）. However, violent water wave impact simulation especially when free surface breaks or impacts on solid wall can be a big challenge for many CFD techniques. Smoothed Particle Hydrodynamics（SPH） has been reported as a robust and reliable method for simulating violent free surface flows. Weakly compressible SPH（WCSPH） uses an equation of state with a large sound speed, and the results of the WCSPH can induce a noisy pressure field and spurious oscillation of pressure in time history for wave impact problem simulation. As a remedy, the truly incompressible SPH（ISPH） technique was introduced, which uses a pressure Poisson equation to calculate the pressure. Although the pressure distribution in the whole field obtained by ISPH is smooth, the stability of the techniques is still an open discussion. In this paper, a new free surface identification scheme and solid boundary handling method are introduced to improve the accuracy of ISPH. This modified ISPH is used to study dam breaking flow and violent tank sloshing flows. On the comparative study of WCSPH and ISPH, the accuracy and efficiency are assessed and the results are compared with the experimental data.

关键词： smoothed particle hydrodynamics(SPH) ISPH water wave impact