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Design,synthesis,and anti-inflammatory evaluation of a series of novel amino acid-binding 1,5-diarylpyrazole derivatives

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Acta Pharmacologica Sinica 2005年第7期26卷 865-872页

作者： Ming-hui LI Lin-lin YIN Mao-jun CAI Wei-yu ZHANG Yue HUANG Xin WANG Xing-zu ZHU~1 Jing-kang SHEN~1 State Key Laboratory of Drug Research,Shanghai Institute of Materia Medica,Shanghai Institutes for Biological sciences,chinese {2. of sciences,graduate School of the chinese {2. of sciences,Shanghai 2.12.3,china State Key Laboratory of Drug Research Shanghai Institute of Materia Medica Shanghai Institutes for Biological Sciences Chinese Academy of Sciences Graduate School of the Chinese Academy of Sciences Shanghai 201203 China

Aim:To design and synthesize a series of novel amino acid-binding 1,5-diarylpyrazole derivatives,which are intended to act as prodrugs with better aque-ous solubility than celecoxib,and which will exert potent anti-inflammatory activi-ties after being converted to their parent compounds in ***:To intro-duce an amino acid,celecoxib analogs containing amino or methylamino groupwere synthesized first through multi-step chemical *** the synthesizedcompounds were screened in an intact cell-based assay in vitro and in carrag-eenan-induced mouse paw edema in *** active compounds were selectedfor further evaluation in a carrageenan-induced rat paw edema *** prelimi-nary pharmacokinetics experiments were conducted using high performance liq-uid chromatography/mass spectrometry(HPLC/MS).Results:Celecoxib,6 of the1,5-diarylpyrazole class of celecoxib analogs,and their amino acid derivatives(hydrochloride salts)were *** vitro screening,the hydrochloridesalts showed decreased inhibitory effects on cyclooxygenase(COX)-1 and COX-2.compared with their parent compounds,but some exhibited potent anti-inflam-matory activity in *** 4a was selected for further evaluation,and itsanti-inflammatory effect was equivalent to that of celecoxib after oral administra-tion in the carrageenan-induced rat paw edema *** three doses(2. mg/kg,50 mg/kg,and 100 mg/kg)the percentage inhibition on edema was 2..7%,52.6%,and 62.6%(for compound 4a)and 2..8%,38.4%,and 40.1%(for celecoxib),*** pharmacokinetic evaluations support the hypothesisthat compound 4a was actually converted to its parent compound,compound ***:The compound bound with amino acid acts like prodrug,which canexert anti-inflammatory effect similar to celecoxib after being converted to its par-ent *** finding will be of great benefit in carrying out structuralmodifications of prodrug-like selective COX-2.inhibitors.

关键词： nonsteroidal anti-inflammatory agents cyclo oxygenase inhibitors celecoxib pyrazole sulfonamide prodrugs

样品处理对罗非鱼和银鲫肠道消化酶活性测定的影响

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水产学报 2004年第6期28卷 738-740页

作者：黎军胜李建林吴婷婷南京农业大学食品科技学院中国水产科学研究院无锡淡水渔业研究中心中国水产科学研究院无锡淡水渔业研究中心江苏南京　2.0095 江苏无锡　2.4081

This paper reported the effects of disposal methods of sample on determination of digestive enzyme of tilapia and silver crucian carp. The results showed that activities of digestive enzyme in intestine tissue homogenized for 1 min and 2.min (10000 r·min-1) respectively were not remarkably different, and so did that frozen and melted once. By centrifugation, the activities of digestive enzyme in superstratum of intestine tissue homogenized were 2.8%-7.4% lower than those of initial intestine tissue homogenized. At 4 ℃,the activities of digestive enzyme in intestine tissue homogenized were the most stable in the phase of 3-9 h and 9-18 h for protease and amylase of silver crucian carp respectively after homogenization, and so did that in the phase of 6-9 h for both protease and amylase of tilapia, in the other phase, the activities of digestive enzyme in intestine tissue homogenized decreased at most by 9.0%-18.2. and 11.5%-44.4% for protease and amylase respectively.

关键词：匀浆冻融离心保存

Interactions between rare earths and 3,5,3'-triiodothyronine (T_3)

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chinese Science Bulletin 1997年第17期42卷 1444-1447页

作者： WANG Ruiyao, GAO Feng, NIU Chunji, YANG Kuiyue, Nl Jiazuan, JIN Tianzhu and WANG Xiangyun Laboratory of Rare Earths Chemistry and Physics, Changchun Institute of Applied Chemistry, chinese academy of {2., Changchun 13002., china State Key Laboratory of Rare Earth Materials Chemistry and Applications, Peking university, Beijing 100871, china Laboratory of Rare Earths Chemistry and Physics Changchun Institute of Applied Chemistry Chinese Academy of Sciences Changchun China State Key laboratory of Rare Earth Materials Chemistry and Applications Peking University Beijing China

WHILE rare earths are being used in agriculture, medicine and materials, they are being

关键词： rare earths 3 5 3’-triiodothyronine (T3) complex.

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Recombinant Neural Protein PrP Can Bind with Both Recombinant and Native Apolipoprotein E In Vitro

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Acta Biochimica et Biophysica Sinica 2006年第9期38卷 593-601页

作者： Chen GAO~1 Yan-Jun LEI~(1,2. Jun HAN~1 Qi SHI~1 Lan CHEN~(1,3) Yan GUO~(1,4) Yong-Jun GAO~1 Jian-Ming CHEN~1 Hui-Ying JIANG~1 Wei ZHOU~1 Xiao-Ping DONG~1* 1 State Key Laboratory for Infectious Disease Prevention and Control,National Institute for Viral Disease Control and Prevention,chinese Center for Disease Control and Prevention,Beijing 100052.china 2.School of Medicine,Xi'an Jiaotong {2.,Xi'an 710061,china 3 National Laboratory of Medical Molecular Biology,Institute of Basic Medical Science,chinese academy of Medical sciences and Peking Union Medical College,Beijing 100005,china 4 College of Science and Veterinary Medicine,Northwest Agriculture and Forest {2.,Yangling 712.00,china StateKeyLaboratoryforInfectiousDiseasePreventionandControl NationalInstituteforViralDiseaseControlandPreventionChineseCenterforDiseaseControlandPreventionBeijing100052China SchoolofMedicine Xi'anJiaotongUniversity

The most essential and crucial step during the pathogenesis of transmissible spongiformencephalopathy is the conformational change of cellular prion protein （PrPC） to pathologic isoform (PrPSc).Alot of data revealed that caveolae-like domains （CLDs） in the cell surface were the probable place where theconversion of PrP proteins *** E （ApoE） is an apolipoprotein which is considered toplay an important role in the development of Alzheimer's disease and other neurodegenerative diseases byforming protein complex through binding to the receptor located in the clathrin-coated pits of the cell *** this study,a 914-bp cDNA sequence encoding human ApoE3 was amplified from neuroblastoma cell *** human ApoE isomers were expressed and purified from Escherichia ***-specificantiserum was prepared by immunizing rabbits with the purified ***/His pull-down assay,immunoprecipitation and ELISA revealed that three full-length ApoE isomers interact with the recombinantfull-length PrP protein in *** regions corresponding to protein binding were mapped in the N-terminalsegment of ApoE （amino acid 1-194） and the N-terminal of PrP （amino acid 2.-90）.Moreover,the recombinantPrP showed the ability to form a complex with the native ApoE from liver *** data provided directevidence of molecular interaction between ApoE and *** also supplied scientific clues for assessing thesignificance of CLDs on the surface of cellular membrane in the process of conformational conversion fromPrPCto PrPScand probing into the pathogenesis of transmissible spongiform encephalopathy.

关键词： prion disease PrP apolipoprotein E protein interaction caveolae-like domain

BEM Analysis for Galvanic Corrosion of Hot-dip Galvanized Steel in Seawater

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BEM Analysis for Galvanic Corrosion of Hot-dip Galvanized St...

2.06年全国腐蚀电化学及测试方法学术会议

作者： TANG Xiao, LI Yan ( Institute of Oceanology, chinese academy of {2., Qingdao, PRC, 2.6071) (graduate School of the chinese academy of {2., Beijing, PRC, 100039)

A numerical analysis of galvanic corrosion of Hot dip galvanized steel in seawater is presented. The analysis is based on the boundary element methods, by coupling with Newton-Raphson iterative technique of resolution to treat the non-linearity boundary conditions, which were enforced based on the experimentally determined polarization curves. And the Zn/Fe couple was made up of an annular galvanized steel sheet with a con-centric circular defect, where the zinc coating has been removed. Results showing the corrosion potential and current density on the galvanic corrosion symmetrical cell in seawater were obtained. The sacrificial protection of zinc coating on steel substrate reaches overprotection and becomes a latent destructive factor for structural materials. And the anodic galvanic current density concentrates on the boundary of steel substrate and zinc coating. This kind of phenomenon in galvanic corrosion was named as ’Galvanic current boundary concentration’. The probability of metallic invalidation resulted by overprotection augments along with the temperature shifts from 2.℃to 50℃, so does to the defect increscent speed.

关键词： Galvanic corrosion BEM potential distribution current density distribution galvanized steel overprotection

Humoral and cellular immune responses induced by SARS or SARS-like coronavirus 3a DNA vaccine in mice

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Humoral and cellular immune responses induced by SARS or SAR...

中国微生物学会《第二届全国农业微生物研究及产业化研讨会》和《第十一届全国杀虫微生物学术研讨会》暨《湖北省暨武汉市微生物学会和内蒙古微生物学会2.08年会》

作者： Baojing Lu,Ling Tao,Ting Wang,Zhenhua Zheng,Bao Li,Ze Chen,Yi Huang,Qinxue Hu and Hanzhong Wang (State Key Laboratory of Virology,Wuhan Institute of Virology,chinese academy of science, Wnhan 430071,PR {2. 2.graduate university of chinese academy of sciences,Beijing 10004.)

3a gene is a newly identified group-specific open-reading frame(ORF)found in both SARS-CoV and SARS-Like-CoV(SL-CoV).In this study,the immunogenicity of human SARS-CoV and bat SL-CoV 3a DNA vaccines have been *** date...

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Role of Water in Deformed Omphacite in UHP Eclogite from the Dabie Mountains,Eastern china

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Role of Water in Deformed Omphacite in UHP Eclogite from the...

中国科学院地质与地球物理研究所2.03学术年会

作者： SU Wen~1,YOU Zhendong~2.CONG Bolin~1 and YE Kai~1 1 Laboratory of Lithosphere Tectonic Evolution,Institute of Geology and Geophysics, chinese academy of {2.,Beijing 10002. 2.china university of Geo{2.,Wuhan,Hubei 430074

Omphacite grains from UHP eclogite of the Dabie Mountains in eastern china are elongated and show strong lattice preferred orientations(LPOs).Observations by the transmission electron microscopy(TEM) identified not only structures of plastic deformation occurring as free dislocation,dislocation loops and dislocation walls,but also bubbles of water present in the deformed *** bubbles attach to the dislocation loops which are often connected to one another via a common *** infrared spectroscopy(IR),two types of hydrous components are identified as hydroxyl and free-water in the *** analysis of deformation mechanism of microstructure in omphacite suggests that the mineral deformed plastically under UHP metamorphic conditions by dislocation creep through hydrolitic weakening.

关键词： deformation hydrolitic weakening omphacite UHP eclogite Dabie Mountains china

Geological Signature and Possible Position of the North china Block in the Supercontinent Rodinia

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Geological Signature and Possible Position of the North Chin...

中国科学院地质与地球物理研究所2.03学术年会

作者： Mingguo Zhai~(1*),Ji’an Shao~2.Jie Hao~1 and Peng Peng~1 1 Key Laboratory of Mineral Resources,Institute of Geology and Geophysics,chinese academy of {2.,Beijing,10002., china, 2.Department of Geology,Peking university,Beijing,china

Recent studies suggest that the South china Block(SCB) was located at a central position in the Neoproterozoic supercontinent Rodinia between ca.1000 Ma and 800 Ma,but fewer studies dealt with the North china Block(NCB) in the reconstruction of *** NCB was suggested,in general,to be in a stable cratonic setting from ca.1650 Ma to ca.160-140 *** recent study suggests that there were two metamorphic-magmatic events at～1300-1000 Ma and～800-650 Ma in the *** these events were weak,they have been regarded as marking the assembly(Grenville- age orogenic event) and breakup(Neoproterozoic mafic dyke swarm and granitoid intrusive) of the supercontinent Rodinia.A possible Grenvillian ophiolite or convergent margin complex in the NCB exists only in the North Qinling end-Mesoprotcrozoic orogenic *** major mcta-volcanic-scdimcntary rocks in this complex belong to the Kuanping Group and are associated with gabbros and serpentinized *** and post-collisional granites have been recognized along the North Qinling *** and sedimentary rocks along northern margin of the NCB indicate possible continent rift or continental margin *** main rock associations of ca.～800-650 Ma are mafic dyke swarms withε(t) values of enriched ***,this paper suggests that the mafic dykes were possibly related to the breakup of the Rodinian *** tectonostratigraphic constraints and palaeomagnetic reconstruction show that the Proterozoic NCB was different from the SCB,but somewhat similar to *** above features possibly suggest that the NCB,as part of the supercontinent Rodinia,was possibly located in a marginal location not directly connected to the SCB,but likely adjacent to the Siberian Craton.

关键词： North china Baiyan Obo belt North Qinling belt supercontinent Rodinia Grenvillian in china

A Software Quality Evaluation System: JT SQE

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Wuhan university Journal of Natural sciences 2001年第Z1期6卷 511-515页

作者： Shi Xiao ying 1, Yang Lan 2.1.Dept. of Computer Science & Technology, Shanghai Jiao Tong university, Shanghai 2.0030,china 2.Dept. of Computer Science, California State Polytechnic university, Pomona, CA 91768, USA Dept. of Computer Science & Technology Shanghai Jiao Tong University Shanghai China Dept. of Computer Science California State Polytechnic University Pomona USA

JT SQE system is a software quality and measurement system. Its design was based on the chinese national standards of software product evaluation and quality characteristics. The JT SQE system consists of two parts. One is the model for software quality measurement, which is of hierarchical structure. The other is the process of requirements definition, measurement and rating. The system is a feasible model for software quality evaluation and measurement, and it has the advantage of a friendly user interface, simple operation, ease of revision and maintenance, and expansible measurements.

关键词： quality evaluation and measurement quality characteristics sub characteristics quality metrics metric question

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