检索结果-南通市图书馆

维普期刊数据库

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

在线全文

学校读者我要写书评

暂无评论

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 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

Enhancing immunotherapy efficacy against MHC-I deficient triple-negative breast cancer using LCL161-loaded macrophage membranedecorated nanoparticles

在线全文

同方期刊数据库

学校读者我要写书评

暂无评论

Acta Pharmaceutica Sinica B 2024年第7期14卷 3218-3231页

作者： Wen Zhang Yihui Zhai Ying Cai Xiang Gong yunxuan Jiang Rong Rong Chao Zheng Binyu Zhu Helen He Zhu Hao Wang yaping li Pengcheng Zhang china State institute of Pharmaceutical Industry Shanghai 201203China State Key Laboratory of Drug Research&Center of Pharmaceutics Shanghai Institute of Materia MedicaChinese Academy of SciencesShanghai 201203China School of Biomedical Engineering&State Key Laboratory of Advanced medical materials and Devices ShanghaiTech UniversityShanghai 201210China School of chinese materia medica Nanjing University of Chinese MedicineNanjing 210023China Yantai institute of materia medica Shandong 264000China State Key Laboratory of Oncogenes and Related Genes Renji-Med-X Stem Cell Research CenterDepartment of UrologyRen Ji HospitalSchool of Medicine and School of Biomedical EngineeringShanghai Jiao Tong UniversityShanghai 200127China University of chinese academy of sciences Beijing 100049China

Current cytotoxic T lymphocyte(CTL)activating immunotherapy requires a major histocompatibility complex I(MHC-I)-mediated presentation of tumor-associated antigens,which malfunctions in around half of patients with triple-negative breast cancer(TNBC).Here,we create a LCL161-loaded macrophage membrane decorated nanoparticle(LMN)for immunotherapy of MHC-I-deficient *** on the macrophage membrane helps LMNs recognize CD47-expressing cancer cells for targeted delivery of LCL161,which induces the release of high mobility group protein 1 and proinflammatory cytokines from cancer *** released cytokines and high mobility group protein 1 activate antitumor immunity by increasing the intratumoral density of the phagocytic macrophage subtype by 15 times and elevating the intratumoral concentration of CTL lymphotoxin by 4.6 *** also block CD47-mediated phagocytosis *** inhibit the growth of MHC-I-deficient TNBC tumors,as well as those resistant to combined therapy of anti-PDL1 antibody and albumin-bound paclitaxel,and prolong the survival of animals,during which process CTLs also play important *** macrophage membrane-decorated nanoparticle presents a generalizable platform for increasing macrophagemediated antitumor immunity for effective immunotherapy of MHC-I-deficient cancers.

关键词： MHC-I deficiency Macrophage CD47 Immunotherapy Triple-negative breast cancer Phagocytosis Immune checkpoint Innate immunity

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

维普期刊数据库评论

在线全文

维普期刊数据库

学校读者我要写书评

暂无评论

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 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

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

在线全文

同方期刊数据库

学校读者我要写书评

暂无评论

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 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 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

Space advanced technology demonstration satellite

在线全文

同方期刊数据库

学校读者我要写书评

暂无评论

Science china(Technological sciences) 2024年第1期67卷 240-258页

作者： ZHANG XiaoFeng CHEN Wen ZHU XiaoCheng MENG Na HE JunWang BI XingZi ZHANG YongHe SHI Qi li Fei liU Rui FENG ZhengGong liU liu li JinSong WU HaiChen XU DongXiao li TaiJie HUANG JiangJiang liU Shuo li TianTong yu XianSheng gao Yang ZHOU Heng BAN Hanyu ZHANG Yanli ZHANG yueTing YANG YingQuan HE Tao DUAN Xuliang CHEN Xin WANG YaMin SUN AnTai ZHANG KuoXiang SUN Ying WANG YaoBin FAN ChengCheng XIONG Shaolin li XinQiao WEN XiangYang liNG ZhiXing SUN XiaoJin ZHANG Chen BAI XianYong WANG ZhanShan DENG yuanYong TIAN Hui YANG JianFeng XUE HongBo SANG Peng liU JinGuo ZHENG HuiLong ZHU Xiang HE JianWu li Hui XU LuXiang XU ShuYan CHEN WenWu liU ZhenDong WANG Zhaoli MAO XiangLong gao Rong li ZongXuan DING GuoPeng WANG Xinyu DOU RunJiang WENG LuBin LUO Hao WANG yaping liANG XianFeng FANG ZiRuo Innovation academy for Microsatellites Chinese Academy of SciencesShanghai 201203China institute of High Energy Physics Chinese Academy of SciencesBeijing 100049China National Astronomical Observatory of china Beijing 100101China shanghai institute of Technical Physics Chinese Academy of SciencesShanghai 200083China institute of Precision Optical Engineering School of Physics Science and EngineeringTongji UniversityShanghai 200092China School of Earth and Space sciences Peking UniversityBeijing 100871China Xi’an institute of Optics and Precision Mechanics Chinese Academy of SciencesXi’an 710119China National Space Science Center Chinese Academy of SciencesBeijing 100190China Shenyang institute of Automation Chinese Academy of SciencesShenyang 110016China institute of Engineering Thermophysics Chinese Academy of SciencesBeijing 100190China institute of Mechanics Chinese Academy of SciencesBeijing 100190China shanghai institute of Organic Chemistry Chinese Academy of SciencesShanghai 200032China Hangzhou institute for Advanced Study University of Chinese Academy of SciencesHangzhou 310024China Nanyang Technological University Singapore 569830Singapore Dalian institute of Chemical Physics Chinese Academy of SciencesDalian 116023China Technical institute of Physics and Chemistry Chinese Academy of SciencesBeijing 100049China Changchun institute of Optics Fine Mechanics and PhysicsChinese Academy of SciencesChangchun 130033China institute of Semiconductors Chinese Academy of SciencesBeijing 100083China institute of Automation Chinese Academy of SciencesBeijing 100190China School of Aeronautics and Astronautics Zhejiang UniversityHangzhou 310058China

The Space Advanced Technology demonstration satellite(SATech-01),a mission for low-cost space science and new technology experiments,organized by chinese academy of sciences(CAS),was successfully launched into a Sun-synchronous orbit at an altitude of~500 km on July 27,2022,from the Jiuquan Satellite Launch *** as an experimental platform for space science exploration and the demonstration of advanced common technologies in orbit,SATech-01 is equipped with 16 experimental payloads,including the solar upper transition region imager(SUTRI),the lobster eye imager for astronomy(LEIA),the high energy burst searcher(HEBS),and a High Precision Magnetic Field Measurement System based on a CPT Magnetometer(CPT).It also incorporates an imager with freeform optics,an integrated thermal imaging sensor,and a multi-functional integrated imager,*** paper provides an overview of SATech-01,including a technical description of the satellite and its scientific payloads,along with their on-orbit performance.

关键词： SATech-01 spacecraft design scientific instruments on-orbit performance

维普期刊数据库

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

在线全文

学校读者我要写书评

暂无评论

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 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

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

在线全文

同方期刊数据库

学校读者我要写书评

暂无评论

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 State Key Laboratory of Drug Research Shanghai Institute of Materia Medica Shanghai Institutes for Biological Sciences Chinese Academy of Sciences Shanghai China

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

Oral peptide therapeutics for diabetes treatment: State-of-the-art and future perspectives

在线全文

同方期刊数据库

学校读者我要写书评

暂无评论

Acta Pharmaceutica Sinica B 2024年第5期14卷 2006-2025页

作者： Bingwen Ding Zhu Zhu Cong Guo Jiaxin li Yong Gan Miaorong yu State Key Laboratory of Drug Research and Center of Pharmaceutics Shanghai Institute of Materia MedicaChinese Academy of SciencesShanghai 201203China University of chinese academy of sciences Beijing 100049China School of Pharmacy Henan UniversityKaifeng 475004China NMPA Key Laboratory for Quality Research and Evaluation of Pharmaceutical Excipients National Institutes for Food and Drug ControlBeijing 100050China

Diabetes,characterized by hyperglycemia,is a major cause of death and disability ***,such as insulin and glucagon-like peptide-1(GLP-1)analogs,have shown promise as treatments for diabetes due to their ability to mimic or enhance insulin's actions in the *** to subcutaneous injection,oral administration of anti-diabetic peptides is a preferred ***,biological barriers significantly reduce the efficacy of oral peptide *** advancements in drug delivery systems and formulation techniques have greatly improved the oral delivery of peptide therapeutics and their efficacy in treating *** review will highlight(1)the benefits of oral anti-diabetic peptide therapeutics;(2)the biological barriers for oral peptide delivery,including pH and enzyme degradation,intestinal mucosa barrier,and biodistribution barrier;(3)the delivery platforms to overcome these biological ***,the review will discuss the prospects in this *** information provided in this review will serve as a valuable guide for future developments in oral anti-diabetic peptide therapeutics.

关键词： Oral peptides Diabetes Delivery platforms Insulin Glucagon-like peptide-1 Biodistribution Biological barriers Targeted delivery

Effects of bilobalide on interleukin-1, tumor necrosis factor-α and nitric oxide production by rat microglia stimulated with lipopolysaccharides in vitro

维普期刊数据库评论

在线全文

维普期刊数据库

学校读者我要写书评

暂无评论

Acta Pharmacologica Sinica 1999年第5期 95-96页

作者： DU Ze-Ying, li Xiao-yu(shanghai institute of materia medica, chinese academy ofsciences, shanghai 200031, china)

The effects of bilobalide,a sesquiterpene isolated from Ginkgo biloba, on interelukin-1 (IL-l), tumor necrosis factor-α(TNF-α) and nitric oxide (NO) production in resting and lipopolysaccharide (LPS )-stimulated cultured neonatal rat microglia were studied. Apafant, a platelet activating factor (PAF) antagonist of triazolobenzodiazepine type was ttsed as *** biological activities of IL-1 and TNFαwere tested

关键词： TNF Effects of bilobalide on interleukin-1 and nitric oxide production by rat microglia stimulated with lipopolysaccharides in vitro tumor necrosis factor