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Down regulation of cyclooxygenase-2 is involved in delayed neuroprotec-tion by ischemic preconditioning in rats

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Acta Pharmacologica Sinica 2005年第4期26卷 441-446页

作者： liang XIAO Fei-li ZHAO xing-zu zhu~1 department of pharmacology II,shanghai institute of materia medica,shanghai institutes for biological sciences,chinese academy of sciences,shanghai 201203,china departmentofpharmacologyII ShanghaiInstituteofMateriaMedicaShanghaiInstitutesforBiologicalSciencesChineseA

Aim:To examine whether the prostaglandins(PGs)pathway is involved in trigger-ing delayed neuroprotection by ischemic preconditioning(IPC)and evaluate theeffects of IPC on cyclooxygenase-2(COX-2)expression following focal cerebralischemia and reperfusion in ***:IPC was induced by 10 min of salineinfusion into the left internal carotid artery with the right common carotid arteryclamped at the same *** cerebral artery occlusion(MCAO)and reperfusionmodel was produced using intraluminal filament ***:IPC 48 h priorto MCAO significantly reduced infarct area as compared with MCAO *** inhibitor of COX indomethacin(3 mg/kg ip)applied 1 h prior to or 1 hafter IPC failed to affect its protective *** had no direct effect on thecortex COX-2 mRNA and protein expression 72 h later,but decreased the expres-sion of COX-2 mRNA and protein following ischemia and reperfusion ***:PGs pathways was not involved in triggering delayed neuroprotectionby IPC,and IPC induced down-regulation of COX-2 following focal cerebral is-chemia and reperfusion in rats in vivo.

关键词： ischemic preconditioning brain ischemia prostaglandins cyclooxygenase-2

Neuroprotective effects of cyclooxygenase-2 inhibitor celecoxib against toxicity of LPS-stimulated macrophages toward motor neurons

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Acta Pharmacologica Sinica 2005年第8期26卷 952-958页

作者： Yong HUANG, Jing liU, li-zhen WANG, Wei-yu ZHANG, xing-zu zhu~1 department of pharmacology, shanghai institute of materia medica, shanghai institutes for biological sciences, chinese academy of sciences, Graduate School of chinese academy of sciences, shanghai 201203, china department of pharmacology Shanghai Institute of Materia Medica Shanghai Institutes for Biological Sciences Chinese Academy of Sciences Graduate School of Chinese Academy of Sciences Shanghai 201203 China

Aim: To establish an in vitro injured motor neuronal model and investigate the neuroprotective effects and possible mechanism of celecoxib, a selective cyclooxygenase-2 (COX-2) inhibitor, on this model. Methods: After macrophages were stimulated with lipopolysaccharide (LPS)+interferon-γ(IFN-γ) in the pre-sence or absence of celecoxib for 24 h, the cell-free supernatant of LPS-stimulated macrophages was transferred to the culture of NSC34 cells. Viability of NSC34 cells was assessed by MTT assay after a further 24 h and 72 h incubation. After macrophages were stimulated by LPS+IFN-γ for 12 h or 24h, the release of pros-taglandin E2(PGE2), nitric oxide (NO), reactive oxygen species (ROS), tumor necro-sis factor α(TNF-α) and interleukin-1β (IL-1β) from macrophages was measured by radioimmunoassay, Griess assay, fluorescence assay and enzyme-linked immunosorbent assay, respectively. The mRNA levels of COX-2, inducible nitric oxide synthase (iNOS), TNF-α and IL-1β in macrophages were determined by reverse transcription-polymerase chain reaction after macrophages were stimu-lated for 6 h and 12 h. Results: The supernatant of LPS-stimulated mouse mac-rophages induced the death of NSC34 cells and celecoxib protected the NSC34cells against this toxicity. The LPS-induced increases in the release of PGE2, NO,TNF-α and IL-1β from macrophages were attenuated by pre-treatment with celecoxib. However, celecoxib showed no effect on the ROS levels upregulated by LPS+IFN-γin the macrophage supernatant. The mRNA levels of COX-2, iNOS, TNF-α and IL-1β were increased in LPS-activated macrophages and, except COX-2, reduced by pre-treatment with celecoxib. Conclusion: An in vitro injured motor neuronal model was established by using the toxicity of LPS-stimulated mouse macrophages toward motor neuronal NSC34 cells. In this model, celecoxib exerted neuroprotective effects on motor neurons via an inhibition of the neurotoxic secretions from activated macrophages.

关键词： amyotrophic lateral sclerosis celecoxib macrophage NSC34 cell lipopolysaccharide cyclooxygenase-2 prostaglandin E2 nitric oxide reactive oxygen species

Insulin-sensitizing effects of a novel α-methyl-α-phenoxylpropionate derivative in vitro

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Acta Pharmacologica Sinica 2007年第3期28卷 417-422页

作者： Hao-shu WU~(2,4) Juan-hong YU~(3,4) Ying-yin li~2 Yu-she YANG~3 Qiao-jun HE~2 Yi-jia LOU~(2,5) Ru-yun JI~3 ~2department of pharmacology and Toxicology,College of Pharmaceutical sciences,Zhejiang University,Hangzhou 310058,china ~3State Key Laboratory of Drug Research,shanghai institute of materia medica,shanghai institutes for biological sciences,Graduate School of the chinese academy of sciences,shanghai 201203,china department of pharmacology and Toxicology College of Pharmaceutical Sciences Zhejiang University

Aim:To examine the insulin sensitizing effects of a novel α-methyl-α-phenoxylpropionate derivative YY20 in insulin-sensitive cell ***:Theperoxisome proliferator-activated receptor γ（PPARγ）agonist bioactivities of YY20were detected by a preadipocyte differentiation ***-PCR and Westernblotting analysis were used to detect the expression of the target gene or *** effects of YY20 on insulin-mediated glucose consumption were determined inthe HepG2 human hepatocellular carcinoma ***:YY20 could enhancethe differentiation of preadipocytes to adipocytes and upregulate the gene ex-pression of PPARγ2,as well as the protein expression of insulin receptor sub-strate-1（IRS-1）,glucose transporter-4（GLUT4）,and adiponectin（ACRP30）.Theeffects on GLUT4 and ACRP30 could be reversed by the PPARγ inhibitor ***,YY20 efficiently reduced glucose consumptions in HepG2 cells after24 h culture,and the effects were related to insulin and YY20 ***:YY20,a potential insulin-sensitizing agent like rosiglitazone,couldenhance glucose consumption in HepG2 cells in a concentration-and insulin-dependent *** may improve the insulin resistance associated with type 2diabetes.

关键词： YY20 peroxisome proliferator-activated receptor y insulin sensitivity glucose consumption

Design,synthesis and antitumor evaluation of a new series of N-substi-tuted-thiourea derivatives

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Acta Pharmacologica Sinica 2006年第9期27卷 1259-1271页

作者： Jian li~2 Jin-zhi TAN~2 li-li CHEN~2 Jian ZHANG~2 Xu SHEN~(2,3)Chang-lin MEI~(4,6)li-li FU~4 li-ping liN~5 Jian DING~5 Bing XIONG~2 Xi-shan XIONG~4 Hong liU~(2,6)Xiao-min LUO~(2,6)Hua-liang JIANG~(2,3)2 Drug Discovery and Design Centre,State Key Laboratory of Drug Research,shanghai institute of materia medica,shanghai institutes for biological sciences,chinese academy of sciences,shanghai 201203.china 3 School of Pharmacy.East china University of Science and Technology,shanghai 200237,china 4 Division of Nephrology,department of Internal Medicine,Changzheng Hospital,Second Military medical University,shanghai 200003,china 5 Division of Antitumor pharmacology,shanghai institute of materia medica,shanghai 201203.china 2Drug Discovery and Design Centre State Key Laboratory of Drug Research Shanghai Institute of Materia Medica Shanghai Institutes for Biological Sciences Chinese Academy of Sciences Shanghai 201203 China 2Drug Discovery and Design Centre State Key Laboratory of Drug Research Shanghai Institute of Materia Medica Shanghai Institutes for Biological Sciences Chinese Academy of Sciences Shanghai 201203 China 2Drug Discovery and Design Centre State Key Laboratory of Drug Research Shanghai Institute of Materia Medica Shanghai Institutes for Biological Sciences Chinese Academy of Sciences Shanghai 201203 China 2Drug Discovery and Design Centre State Key Laboratory of Drug Research Shanghai Institute of Materia Medica Shanghai Institutes for Biological Sciences Chinese Academy of Sciences Shanghai 201203 China 3School of Pharmacy East China University of Science and Technology Shanghai 200237 China 3School of Pharmacy East China University of Science and Technology Shanghai 200237 China 4Division of Nephrology Department of Internal Medicine Changzheng Hospital Second Military Medical University Shanghai 200003 China 5Division of Antitumor pharmacology Shanghai Institute of Materia Medica Shanghai 201203 China 5Division of Antitumor pharmacology Shanghai Institute of Materia Medica Shanghai 201203 China 2Drug Discovery and Design Centre State Key Laboratory of Drug Research Shanghai Institute of Materia Medica Shanghai Institutes for Biological Sciences Chinese Academy of Sciences Shanghai 201203 China 4Division of Nephrology Department of Internal Medicine Changzheng Hospital Second Military Medical University Shanghai 200003 China 2Drug Discovery and Design Centre State Key Laboratory of Drug Research Shanghai Institute of Materia Medica Shanghai Institutes for Biological Sciences Chinese Academy of Sciences Shanghai 201203 China 2Drug Discovery and Design Centre State Key Laboratory of Drug Research Shanghai Institute of Materia Medica Shanghai Institutes for Bi

Aim:To design and synthesize a novel class of protein tyrosine kinase inhibitors,featuring the N-(2-oxo-1,2-dihydroquinolin-3-yl-methyl)-thiourea ***:First,compounds 1 and 2 were identified using the virtual screeningapproach in conjunction with binding assay based on surface plasmon ***,3 regions of compounds 1 and 2 were selected for chemical *** compounds were characterized potent inhibitory activities toward thehuman lung adenocarcinoma cell line SPAC ***:Forty new compounds(1-2,3a-g,4a-w,and 5a-l)were designed,synthesized and *** com-pounds(1,3e,41,4w,5a,and 5b)were found to show promising inhibitory activityagainst the SPAC1 tumor cell *** inhibitory activity of compound 5aincreases approximately 10 times more than that of the original compound ***:This study provides a promising new template with potential antitu-mot activity.

关键词： N-substituted-thiourea derivatives antitumor SPAC1 tyrosine kinase inhibitor virtual screening

Modulating effect of adenosine deaminase on function of adenosine A1 receptors

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Acta Pharmacologica Sinica 2005年第2期26卷 160-165页

作者： Wan-chun SUN,Yan CAO,Lei JIN,li-zhen WANG,Fan MENG~2,xing-zu zhu~3department of pharmacology,shanghai institute of materia medica,shanghai institutes for biological sciences,chinese academy of sciences,shanghai 201203,china ~2department of Psychiatry,University of Michigan,The Psychiatry/MHRI Microarray Laboratory,205 Zina Pitcher Place,Ann Arbor,MI 48109-0720,USA department of pharmacology Shanghai Institute of Materia Medica Shanghai Institutes for Biological Sciences Chinese Academy of Sciences Shanghai 201203 China

Aim:To study the modulating effect of adenosine deaminase（ADA）on yheadenosine A1receptor（A1R）in HEK293 cells stably expressing the human ***:cDNA was amplified by RT-PCR using total RNA from human embryobrain tissue as the *** PCR products were subcloned into the plasmidpcDNA3 and cloned into the plasmid *** cloned A1R cDNA wassequenced and stably expressed in HEK293 *** modulating effect of ad-enosine deaminase on A1R was studied by using[3H]DPCPX binding assay andan intracellular calcium ***:HEK293 cells stably expressing humanA1R were *** studies showed that the KDvalue and Bmaxvalueof[3H]DPCPX were 1.6±0.2 nmol/L and 1.819±0.215 nmol/g of protein respectively,in the absence of ecto-ADA respectively,and 1.3±0.2 nmol/L and 1.992±0.130nmol/g of protein in the presence of ecto-ADA respectively,suggesting that theKDvalue and Bmaxvalue of[3H]DPCPX were unaffected by *** the caseof[3H]DPCPX competition curves obtained from intact cells or membranes,A1Ragonist CCPA/[3H]DPCPX competition curve could be fitted well to a one-sitemodel in the absence of ecto-ADA and a two-site model in the presence of ecto-ADA with a KHvalue of 0.74（0.11-4.8）nmol/L（intact cells）or 1.8（0.25-10）nmol/L（membrane）and a KLvalue of 0.94（0.62-1.41）μmol/L（intact cells）or 0.77（0.29-0.99）μmol/L（membrane）.The KLvalue is not significantly different from the IC50value of 0.84（0.57-1.23）μmol/L（intact cells）or 0.84（0.63-1.12）μmol/L（membrane）obtained in the absence of *** results were obtained from theCPA/[3H]DPCPX competition curve in the absence or presence of ecto-ADA onintact cells or *** calcium assay demonstrated that the EC50value of CPA were 10（5-29）nmol/L and 94（38-229）nmol/L in the presence orabsence of ecto-ADA,***:A1R stably expressed in theHEK293 cells display a low affinity for agonists in the absence of ADA and highand low affinities for agonists in the presence of *** pr

关键词： adenosine deaminase adenosine A1 receptor radioligand assay calcium fluorescence diagnosis

Activation of KCNQ potassium channels by small chemical moleculars

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Activation of KCNQ potassium channels by small chemical mole...

Effect of antidepressant duloxetine on stress ulcer

中国神经科学学会第九届全国学术会议暨第五次会员代表大会

作者： Zhaobing GAO~1,Min li~(1,2) 1 State Key Laboratory of Drug Research,shanghai institute of materia medica,shanghai institutes for biological sciences,chinese academy of sciences,555 zu Chong Zhi Road,Zhangjiang Hi-Tech Park,shanghai 201203,china 2 department of Neuroscience,High Throughput Biology Center and Johns Hopkins Ion Channel Center,School of Medicine,Johns Hopkins University,Baltimore,Maryland 21205

＜正＞KCNQ potassium channels play a critical role in controlling membrane *** a typical voltagegated ion channels（Kv）,KCNQ channels undergo closed to open transitions by sensing transmembrane potential changes and mediate inhibitory potassium *** of KCNQ channel activity as results of genetic mutation is causal to a variety of human diseases including epilepsy,arrhythmia and ***,discovery of small compounds to activate voltage-gated ion channels is an important strategy for clinical intervention in human diseases caused by membrane hyperexcitability,including anxiety,epilepsy,arrhythmia and neuropathic *** the binding of these molecules induces a conformational change leading to the opening of these channels,there is also a considerable conceptual interest in understanding the molecular basis of these "gain of a function" *** molecule activators of cation channels are rare;however,several novel compounds have been identified for KCNQ potassium ***,we reported two new molecules which potentiate either cardical or neuronal KCNQ channels and identified molecular determinants for their activity,which provide exciting insights into activation of voltage-gated channels by small molecuars.

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Effect of antidepressant duloxetine on stress ulcer

BCL9 regulates CD226 and CD96 checkpoints in CD8^(+)T cells to improve PD-1 response in cancer

中国神经科学学会第四次会员代表大会暨第八届全国学术会议

作者： Cheng-Xue JI,liang-GUO,Wei-li,Zi-liang liANG,Rui-Ming XU,Jian-Jun ZHANG~* department of pharmacology,institute of materia medica,chinese academy of medical sciences and Peking Union medical College,Beijing 100050,china

＜正＞Objective Previous studies suggested that bad mood and stress predispose to peptic *** duloxetine is dual norepinephrine（NE） and serotonin（5-HT） reuptake *** present study was designed to investigate the effect of duloxetine against stress-induced gastric ulcer,and explore its antiulcer *** The antiulcer effect of duloxetine（20 mg/kg,i.p.,pretreated 30 min before stress） was evaluated in stress-induced gastric ulcer rat *** rat was placed in a restraining cage immersed in water at（21±1 ）℃for 6 h,while control group was free. Rabeprazole（20 mg/kg,i.p.） was used as positive ***-ECD was used to determine the levels of NE,5-HT, dopamine（DA）,and their metabolites[5-hydroxyindoleacetic acid（5-HIAA） and 3,4-dihydroxyphenylacetic acid（DOPAC）] in the rat hypothalamus,hippocampus,cortex,stomach and *** of white blood cell,lymphocyte and neutrophilic granulocyte in the rat blood were quantitated by blood ***（1） Restraint plus waterimmersion induced severe gastric ulcer and hemorrhage in SD *** with model group,duloxetine and rabeprazole decreased significantly both number and severity of gastric ulcer.（2） Compared with control group,NE concentrations in rat hypothalamus and hippocampus significantly decreased in model ***,decrease of DA level in hippocampus,increases of 5-HIAA/5-HT and DOPAC/DA ratio in hypothalamus,hippocampus and cortex（P＜0.05）, decrease of 5-HT in stomach and duodenum（P＜0.05） were *** alterations indicated marked disturbance in the levels of monoamines and *** significantly reversed stress-induced alterations above.（3） Compared with control group,the numbers of white blood cell,lymphocyte and neutrophilic granulocyte significantly increased in model group,which indicated acute bacteria infection *** significantly reversed these alterations. Conclusion Our results indicated that duloxetine exerts pot

关键词： antidepressant antiulcer inflammatory neurotransmitter

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Signal Transduction and Targeted Therapy 2021年第9期6卷 2883-2896页

作者： Mei Feng Zhongen Wu Yan Zhou zhuang Wei Enming Tian Shenglin Mei Yuanyuan zhu Chenglong liu Fenglian He Huiyu li Cao Xie Joy Jin Jibin Dong Dehua Yang Ker Yu Junbin Qian Diether Lambrechts Ming-Wei Wang Di zhu department of pharmacology School of Basic Medical Sciences and School of PharmacyFudan UniversityShanghaiChina School of Pharmacy Fudan UniversityShanghaiChina Key Laboratory of Systems Biology Innovation Center for Cell Signaling NetworkCAS Center for Excellence in Molecular Cell ScienceInstitute of Biochemistry and Cell BiologyShanghai Institutes for Biological SciencesChinese Academy of SciencesShanghaiChina Clinical Translational Research Center Shanghai Pulmonary HospitalSchool of Life Science and TechnologyTongji UniversityShanghaiChina School of Medicine University of California at San FranciscoSan FranciscoCAUSA department of Gynecologic Oncology Women's HospitalZhejiang University School of MedicineHangzhouChina VIB Center for Cancer Biology and Laboratory for Translational Genetics Department of Human GeneticsKU LeuvenLeuvenBelgium School of life Science and Technology ShanghaiTech UniversityShanghaiChina The National Center for Drug Screening and the CAS Key Laboratory of Receptor Research Shanghai Institute of Materia MedicaChinese Academy of Sciences(CAS)ShanghaiChina shanghai Engineering Research Center of Immune Therapy and Key Laboratory of Smart Drug Delivery Fudan UniversityShanghaiChina

To date,the overall response rate of PD-1 blockade remains unsatisfactory,partially due to limited understanding of tumor immune microenvironment(TIME).B-cell lymphoma 9(BCL9),a key transcription co-activator of the Wnt pathway,is highly expressed in *** genetic depletion and pharmacological inhibition of BCL9 in tumors,we found that BCL9 suppression reduced tumor growth.

关键词： BCL tumor CD226

17-Dehydroxyholothurin A, a New Sulfated Triterpene Glycoside from Sea Cucumber Holothuna impatiens

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chinese Chemical Letters 2006年第11期17卷 1454-1456页

作者： Peng SUN Yang Hua YI ling li Min GUI Hai Feng TANG Da Zhi ZHANG Shi Long ZHANG Research Center for Marine Drugs Pharmacy School Second Military Medical University Shanghai 200433 Division of Antitumor pharmacology State Key Laboratory of Drug Research Shanghai Institute of Materia Medica Shanghai Institutes for Biological Sciences Chinese Academy of Sciences Shanghai 201203 department of Pharmacy Xijing Hospital 4th Military Medical University Xi＇an 710032 Departrnent of Organic Chemistry Pharmacy School Second Military Medical University Shanghai 200433

Abstract： A new sulfated triterpene glycoside named as 17-dehydroxyholothurin A 1 was isolated from the sea cucumber Holothuria impatiens. Its structure was elucidated on the basis of spectroscopic data （2D NMR and MS） and chemical evidence. Compound 1 showed cytotoxic activity against cancer cell lines MKN-28, MFC-7, KB, HL-60 and Hep G2 with IC50 values of 1.98, 4.53, 2.01, 4.69 and 2.80 ×10^-6 tool/L, respectively.

关键词： Sea cucumber Holothuria impatiens 17-dehydroxyholothurin A triterpene glycoside.

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