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A New Flavan-3-ol Glucoside from Daphniphyllum oldhami

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Chinese Chemical Letters 2003年第9期14卷 926-929页

作者： Zhi yu SHAO, Da yuan ZHU, yue Wei GUOstate key laboratory of drug research, institute of materia medica, shanghai institutes for biological sciences, Chinese Academy of sciences, shanghai 200031 state key laboratory of drug research Institute of Materia Medica Shanghai Institutes for Biological Sciences Chinese Academy of Sciences Shanghai 200031

A new flavan-3-ol glucoside, (-)-afzelechin-7-O-β-D-glucopyranoside (1), has been isolated from the stem of Daphniphyllum oldhami. The structure of the new compound was elucidated on the basis of detailed spectroscop... 详细信息

关键词： Daphniphyllum oldhami flavan-3-ol (-)-afzelechin-7-O-β-D-glucopyranoside.

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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 Hangzhou 310058 China Department of state 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

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

Tetrahydroacridine inhibits voltage-dependent Na~+ current in guinea-pig ventricular myocytes

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Acta Pharmacologica Sinica 2004年第9期 36-42页

作者： Wei WANG, Yi-ping WANG, Guo-yuan HUstate key laboratory of drug research, The First Department of Pharmacology, shanghai institute of materia medica, shanghai institutes for biological sciences, Chinese Academy of sciences, shanghai 201203, China

AIM: To study the effects of tetrahydroacridine (tacrine) on voltage-gated Na+ channels in cardiac tissues. METHODS: Single ventricular myocytes were enzymatically dissociated from adult guinea-pig heart. Voltage-depe... 详细信息

关键词： Alzheimer disease cholinesterase inhibitors sodium channels tetrahydroacridine (tacrine) myocardium patch-clamp techniques

Triptolide suppresses CD80 and CD86 expressions and IL-12 production in THP-1 cells

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Acta Pharmacologica Sinica 2005年第2期26卷 223-227页

作者： Jing LIU,Qing-li WU,Yong-hong FENG,Yi-fu YANG,Xiao-yu LI,Jian-ping ZUO~2state key laboratory of drug research,shanghai institute of materia medica,shanghai institutes for biological sciences,Chinese Academyof sciences,shanghai 201203,China statekeylaboratoryofdrugresearch ShanghaiInstituteofMateriaMedicaShanghaiInstitutesforBiologicalSciencesCh

Aim:To investigate the effects of triptolide,a diterpenoid triepoxide fromTripterygium wilfordii Hook F(TWHF),on the co-stimulatory molecule expres-sion and interleukin-12(IL-12)production from THP-1 ***:THP-1 cellswere differentiated into macrophage-like cells by Me2SO,and then cultured withIFN-γ(500kU/L)and lipopolysaccharide(LPS)(1mg/L)with or without *** surface molecule expressions were analyzed on a FACScan flow ***-12p40,IL-12p70 were assayed by ***:Tripolide suppressed CD80and CD86 expressions on IFN-γ(500kU/L)and LPS(1mg/L)activated THP-1 cellsat nontoxic dosages of 2.5-0.625μg/***,the production of IL-12p40and IL-12p70 were also significantly reduced in THP-1 cells exposed to ***:Triptolide impairs the antigen-presenting function by inhibiting CD80and CD86 expressions and decreased IL-12p40 and IL-12p70(bioactive form)pro-ductions from the activated THP-1 cells.

关键词： triptolide CD80 antigens CD86 antigens interleukin-12

Construction of a small peptide library related to inhibitor OM99-2 and its structure-activity relationship to β-secretase

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Acta Pharmacologica Sinica 2006年第12期27卷 1586-1593页

作者： Bin HU Bing XIONG Bei-ying QIU Xin LI Hai-ping yu Kun XIAO Xin WANG Jia LI Jing-kang SHEN~2 state key laboratory of drug research and National Center for drug Screening,shanghai institute of materia medica,shanghai institutes for biological sciences,Chinese Academy of sciences,shanghai 201203,China state key laboratory of drug research and National Center for drug Screening Shanghai Institute of Materia Medica Shanghai Institutes for Biological Sciences Chinese Academy of Sciences Shanghai 201203 China

Aim:To develop probes for detecting the binding specificity between β-secretaseand substrate,and provide reliable biological activity data for further researchingencircling substrate-based ***:To prepare the inhibitors,thehydroxyethylene(HE)segment including P1and P1′ was synthesized after multi-step reactions;the combination of all segments was then completed through solidphase *** human β-secretase ectodomain(amino acid resi-dues 1-460)was expressed as a secreted protein with a C-terminal His tag in insectcells using baculovirus infection,and all compounds were evaluated in thisβ-secretase enzyme *** order to understand the interaction in detail,the theoretical methods,namely molecular dynamics(MD)simulation and mo-lecular mechanics-generalized-born surface area(MM-GBSA)analysis,were per-formed on the complex of β-secretase and OM99-2 to obtain the geometrical andenergetical ***:We designed and constructed a positional scan-ning combinatorial library including 16 compounds;all members of the librarywere synthesized based on HE dipeptide ***-activity relationshipstudies at the P4-P1and P1′-P4′ positions led to the discoveries of P and P’sidesbinding specificity and potent inhibitors 14,18,and *** binding free energyon the whole system and every residue were compared to the biological ***:The removal of P4′ yielded inhibitor 22(A3*B2)with highpotency;further truncation of P3′ gave inhibitor 18(A3*B1)with equal activity,implying that the right side of the inhibitors play a less important role and could beeasily simplified,while change on the P side may cause substantial results.

关键词： β-secretase hydroxyethylene OM99-2 Alzheimer’s disease structure-activity relationship

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 Academy of sciences,Graduate School of the Chinese Academy of sciences,shanghai 201203,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(25 mg/kg,50 mg/kg,and 100 mg/kg)the percentage inhibition on edema was 20.7%,52.6%,and 62.6%(for compound 4a)and 27.8%,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

Biphasic firing response of nucleus accumbens neurons elicited by THPB-18 and its correlation with DA receptor subtypes

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Acta Pharmacologica Sinica 2004年第12期25卷 31-39页

作者： yu FU2,3,4, Zi-tao ZHU2,5, Xing-zu ZHU2, Guo-zhang JIN2,6 2state keylaboratory of drug research,shanghai institute ofmateria medica, shanghai institutes for biologicalsciences, ChineseAcademy of sciences, Graduate Schoolof the Chinese Academy of sciences, shanghai 201203, ChinaNow in Department of Pharmacology and Toxicology, Univer-sity of Texas medical Branch, USA.Now in Department of Physiology & Pharmacology, OregonHealth sciences University, USA,5Now in Department of Physiology & Pharmacology, OregonHealth sciences University, USA, state key laboratory of drug research Shanghai Institute of Materia Medica Shanghai Institutes for Biological Sciences Chinese Academy of Sciences Shanghai 201203 China

AIM: To investigate the possibility whether THPB-18 (l-12-shloroscoulerine) possesses the D1 agonist-D2 antago- nist action on meso-accumbens-mPFC DA system. METHODS: Single unit spontaneous firing activity was re- corded in the nucleus accumbens (NAc) neurons of na?ve and unilateral-6-hydroxydopamine (6-OHDA)-lesioned Sprague-Dawley rats. The effects of drugs applied intravenously or iontophoretically were determined by the change of firing rates. RESULTS: Under normal conditions, the systemic administration of THPB-18 produced a decrease-increase biphasic firing pattern in the NAc neurons during cumulative doses. High dose of THPB-18 was capable of reversing the inhibition induced by both D2 agonist LY171555 and D1/D2 agonist APO on NAc firing activity. Spiperone pretreatment could not block the high dose of THPB-18-induced firing rate increase, which was reversed by the D1 selective antagonist SCH23390. The tested NAc neurons were effectively inhibited by iontophoretically applied THPB-18 in 90 % of 6-OHDA-lesioned rats, while THPB-18 caused variable effects on the firing of NAc neurons in the neurons of unlesioned rats. The inhibitory effect of THPB-18 was blocked by iontophoretic application of SCH23390, but not D2 antagonist spiperone. CONCLUSION: Similar to l-stepholidine, THPB-18 also possesses the “D1 agonistic-D2 antagonistic” dual action on the VTA-NAc DA system.4Now in Department of Pharmacology and Toxicology, Univer-sity of Texas medical Branch, USA.5Now in Department of Physiology & Pharmacology, OregonHealth sciences University, USA,4Now in Department of Pharmacology and Toxicology, Univer-sity of Texas medical Branch, USA.5Now in Department of Physiology & Pharmacology, OregonHealth sciences University, USA,5Now in Department of Physiology & Pharmacology, OregonHealth sciences University, USA,

关键词： berberine dopamine D1 receptors dopamine D2 receptors nucleus accumbens

(5R)-5-hydroxytriptolide inhibits IFN-γ-related signaling

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Acta Pharmacologica Sinica 2006年第12期27卷 1616-1621页

作者： Ru ZHOU~2 Jun-xia WANG~2 Wei TANG~2 Pei-lan HE~2 Yi-fu YANG~2 yuan-chao LI~3 Xiao-yu LI~2 Jian-ping ZUO~(2,4)2 laboratory of Immunopharmacology and 3 laboratory of Chemistry,state key laboratory of drug research,shanghai institute of materia medica,shanghai institutes for biological sciences,Chinese Academy of sciences,shanghai 201203,China laboratory of Immunopharmacology State Key Laboratory of Drug Research Shanghai Institute of Materia Medica Shanghai Institutes for Biological Sciences Chinese Academy of Sciences Shanghai 201203 China laboratory of Chemistry State Key Laboratory of Drug Research Shanghai Institute of Materia Medica Shanghai Institutes for Biological Sciences Chinese Academy of Sciences Shanghai 201203 China

Aim:(5R)-5-hydroxytriptolide(LLDT-8)displayed anti-arthritis and anti-allogenictransplantation rejection activities in our previous ***,we aim to furtherclarify the effect of LLDT-8 on the pro-inflammatory cytokine IFN-γ.Methods:Tcells were activated with anti-CD3 antibody or concanavalin A(ConA).The ex-pression of cell surface molecules was detected with flow *** werelabeled with carboxyfluorescein diacetate succinimidyl ester(CFSE)to test ***-γ production was determined by enzyme-linked *** proliferation was evaluated by[~3H]-thymidine *** wereimmunized with ovalbumin to assess the in vivo immune ***-PCR andReal-time PCR were applied to determine the mRNA *** protein phos-phorylation levels were detected by Western immunoblot ***:LLDT-8 at 100 nmol/L did not change the CD25,CD69,and CD154 expressions in anti-CD3-stimulated T ***-8 markedly blocked the cell division of CD4 andCD8 T cells after ConA ***-8 inhibited T cell-derived IFN-γ***,LLDT-8 suppressed the ovalbumin-specific T cell prolif-eration and IFN-γ *** anti-CD3-activated T cells,LLDT-8 abrogated themRNA expression of signal transducer and activator of transcriptionl(STAT1),T-box transcription factor,IL-12 receptor β2,STAT4,and interferon regulatory fac-tor 1 in the IFN-γ expression *** blot analysis showed that LLDT-8 blocked the phosphorylation levels of extracellular signal-regulated kinase,stress-activated protein kinase(SAPK)/c-Jun N-terminal kinase,and p38 mitogen-activated protein kinase in anti-CD3 plus anti-CD28-activated T *** addition,LLDT-8 reduced the transcripts of macrophage inflammatory protein(Mip)-1α,Mip-1β,regulated upon activation normally T-cell expressed and secreted,induc-ible protein-10,IFN-inducible T cell a chemoattractant,and monokine induced byIFN-7 in IFN-γ-stimulated murine macrophage cell line Raw 264.7 ***:LLD

关键词： (5R)-5-hydroxytriptolide IFN-γ MAPK chemokine

1-Stepholidine,Adenosine A2A Receptor and Dopamine D3 Receptor Interactions

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1-Stepholidine,Adenosine A2A Receptor and Dopamine D3 Recept...