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Function and Inhibition of Prolyl Dipeptidases

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Function and Inhibition of Prolyl Dipeptidases

第五届海峡两岸细胞生物学学术研讨会

作者： Xin Chen Division oj Biotechnology and Pharmaceutical Research, national Health Research institutes, Miaoli,Taiwan

Prolyl dipeptidase family contains DPP-Ⅳ, FAP, DPP8, DPP9 and DPP-Ⅱ.They cleave specifically at the peptide bond of the penultimate proline residue. These proteases play important roles in vivo: DPP-Ⅳ is a drug target for type Ⅱ diabetes, and FAP is the cancer marker for the epithelial cancer types. We are interested in (1) understanding the

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In vitro and in vivo evaluation of a novel oral insulin formulation

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Acta Pharmacologica Sinica 2006年第10期27卷 1382-1388页

作者： Er-li MA Hong MA Zheng LIU Chang-xue ZHENG Ming-xing DUAN~2 State Key Laboratory of Bio-membrane and Biotechnology,Department of Biological Sciences and Biotechnology,Tsinghua University beijing 100084,china State Key Laboratory of Bio-membrane and Biotechnology Department of Biological Sciences and Biotechnology Tsinghua University Beijing 100084 China

Aim:To develop a stable self-emulsifying formulation for oral delivery of ***:Caco-2 cell line and diabetic beagles were used as in vitro and in vivomodels to study the absorption mechanism and the hypoglycemic efficacy of *** addition,various physicochemical parameters of the formulationsuch as droplet size,insulin encapsulation efficiency and stability were ***:This formulation enabled changes in barrier properties of Caco-2monolayers,as referred by transepithelial electrical resistance(TEER)and appar-ent permeability coefficients(Papp)of the paracellular marker ranitidine(20-foldgreater than control)but not transcellular marker propranolol,suggesting that theopening of tight junctions was *** diabetic beagle dogs,the bioavailabilityof this formulation was up to 15.2% at a dose of 2.5 IU/kg in comparison with thehypoglycemic effect of native insulin(0.5 IU/kg)delivered by ***:This formulation,recently approved by the china Statefood and drug Administration to enter clinical trials,was stable,degradation-protected and absorption-enhanced,and provided a promising formulation fororal insulin delivery.

关键词： insulin oral delivery Caco-2 diabetic beagles

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

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

第十五届国际药理学大会

作者： Yang YU,Wei-xing SHI Guo-zhang JIN State Key Laboratory of drug Research,Shanghai Institute of Materia Medica,Shanghai institutes for Biological Sciences,Chinese Academy of Sciences,Shanghai 20120 china

＜正＞ Aim: 1 - Stepholidine （SPD） is a lead compound of tetrahydroprotoberberines （THPBs）. This work investigated the influence of SPD on Dopamine D3 receptor （D3R） and adenosine A2a receptor （A2aR）. Methods: PC12 cells with endogenous A2aR were transfected with pIRES - D3R plasmids by Lipofectamine?2000 transfection kit. Protein expression was assessed by Western blot. mRNA was detected by Real - time polymerase chain reaction. The accumulation of cyclic AMP from cells was measured by HitHunter cAMP II Assay kit. Results: Incubation of PC12 cells expressed D3R with SPD resulted in a little decrease of D3 receptors in protein expression. SPD can decrease of D3R and A2aR mRNA level in PC12 cells which stably expressed D3R. SPD or D3 receptor agonist counteracted the A2aR receptor agonist - mediated increase in cAMP levels. Blockade of D3R with the D3R antagonist increased both basal and A2aR receptor agonist - stimulated cAMP levels. Conclusion: These results suggest SPD is a agonist for D3R stably expressed in PC12 cells. The D3R can modulate A2a receptors at the level of gene transcription and the generation of second messengers.

关键词： 1 - Stepholidine dopamine D3 receptor adenosine A2a receptor

drug candidates from traditional Chinese medicines

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Drug candidates from traditional Chinese medicines

药用植物化学与中药有效成分分析研讨会

作者： Jing-Fang Wang~2,Dong-Qing Wei~(1**) (1.College of Life Science and Biotechnology,Shanghai Jiaotong University,Shanghai 200240,china 2.Bioinformatics Center,Key Lab of Systems Biology,Shanghai institutes for Biological Sciences,Chinese Academy of Sciences,Shanghai 200031,china)

Good progress has been made to modernize traditional Chinese medicines by obtaining active components from natural *** the current case,some recent works on drug design using modern drug design tools have been *** some well defined targets,traditional Chinese medicine databases have been screened so as to identify leading compounds whose potential as a drug candidate was not known *** these excellent works,two have been selected as examples to be discussed in ***,new anti-HIV candidates have been detected,namely leucovorin and agaritine derivatives. Subsequently,GTS-21 is proved to be a good candidate for Alzheimer’s *** these findings may provide a good way to find effective drug candidates with lower cost.

关键词： drug candidates Traditional Chinese Medicine Natural herbs Modern drug design tools

Aristolochic acid I targeted to adenine nucleotide translocator sensitizes mitochondrial permeability transition pore opening in vitro:a possible mechanism for toxicity of aristolochic acid I

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Aristolochic acid I targeted to adenine nucleotide transloca...

第十五届国际药理学大会

作者： Jin REN,Xin-ming QI,Ying Xiao,Yan Cai State Key Laboratory of drug Research,Shanghai Institute of Materia Medica,Shanghai institutes for Biological Sciences,Chinese Academy of Sciences,Shanghai 201203,china

＜正＞ Aristolochic acid （AA） is an extract derived from nature manshuriensis. To study the mechanism of nephrotoxicity and possible hepatotoxicity. fifty C57BL/6J mice were used to test LD50. HepG2 cell line was used to test the cellular toxicity and rat liver mitochondria was isolated to detect mitochondria function. The LD50 of AA in mice was 29mg/kg. Kidney and liver injury were shown by quantification of plasma transaminase activities and histological analysis. For the mitochondria study, a lower AA concentration （5 - 25uM） strongly induced cyclosporin A - sensitive mitochondrial swelling. AA promoted both calcium and GSH release from the matrix of isolated mitochondria. AA also decreased greatly the mitochondrial membrane potential （ΔΨm）. In addition. AA significantly inhibited mitochondrial adenine nucleotide translocator （ ANT）. This inhibition of ANT likely facilitates the AA - induced MPT pore opening which mimicked the effect of atractyloside. a specific inhibitor of ANT. induced clear mitochondrial swelling. It is suggested that inhibition of ANT may mediate, in part, the AA induced MPT pore opening, which may be an important mechanism for AA toxici-

关键词： aristolochic acid (AA) MPT ANT

Design,synthesis,and evaluation of a biotinylated photoaffinity probe for labeling functional GABAB receptors on living cells

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Design,synthesis,and evaluation of a biotinylated photoaffin...

中国药理学会第十次全国学术会议

作者： Xin Lin,Ming Jiang,Xin Li,Fa-Jun Nan,Jian-Feng Liu (Key Laboratory of Molecular Biophysics of Ministry of Education,School of Life Science and Technology,Huazhong UniVersity of Science and Technology,1037 Luo Yu Road,Wuhan,Hubei,china,430074 national Center for drug Screening,State Key Laboratory of drug Research,Shanghai Institute of Materia Medica,Shanghai institutes of Biological Sciences, Chinese Academy of Sciences,189 Guo Shou Jing Road,Shanghai 201203,china)

γ-amidobutyric acid(GABA) is the major inhibitory neurotransmitter in the mammalian central nervous system,exerts its effects through both ionotropic(GABA) and metabotropic(GABA) *** receptors mediate both presynaptic inhibition of neurotransmitter release and post-synaptic inhibition of neuronal excitability. Functional GABA receptor is composed of GABA and GABA subunits,each of which is unable to form a functional GABAB receptor in its own *** the qualitative analysis of functional GABA receptors on living cells,we have designed an activity-based photoaffinity biotinlyted probe based on CGP64213,a GABA selective high-affinity *** probe labels the functional GABA receptor on the cell surface with high specificity in the activity *** probe not only specifically binds GABA which heterodimerizes with GABA to form the functional GABAB receptor,but also indirectly fished out the GABAB2 which also form the functional GABAB receptor with *** results,therefore revealed that the feasibility of the probe we designed as a tool to qualitatively detect functional GABA receptor,as well as other important signal protein which interact with functional GABA receptor in living cells.

关键词： GABAB Receptor biotinlyted probe photoaffenity labeling

Synthesis and PTP1B Inhibitory Evaluation of 2-naphthol tyrosine derivatives

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Synthesis and PTP1B Inhibitory Evaluation of 2-naphthol tyro...

2011年全国药物化学学术会议——药物的源头创新

作者： Liang-Peng Sun a,Qiang Shen b,Jia Li b,Hu-Ri Piao a,~* a Key Laboratory of Natural Resources of Changbai Mountain & Functional Molecules,Ministry of Education,Yanbian University College of Pharmacy,Yanji,133000,PR china b national Center for drug Screening,Shanghai Institute of Materia Medica,Shanghai institutes for Biological Science,Chinese Academy of Sciences,Shanghai 201203,china

＜正＞In recent years,a great attention are being payed to protein tyrosine phosphatase 1B（PTP1B） due to its pivotal role in type 2 diabetes and obesity as a negative regulator of the insulin and leptin-signaling pathway[1-2].Therefore,the search for potent small molecule protein tyrosine phosphatase 1B inhibitors is a major thrust area in the management of type 2 diabetes mellitus.

关键词： Protein tyrosine phosphatase 1B(PTP1B) Inhibitor Synthesis

人工智能医疗器械性能评价通用方法专家共识(2023)

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协和医学杂志 2023年第3期14卷 494-503页

作者：浙江大学中国食品药品检定研究院海军军医大学第二附属医院刘士远李静莉吴健不详海军军医大学第二附属医院影像医学与核医学科上海200003 中国食品药品检定研究院医疗器械检定所北京102629 浙江大学公共卫生学院杭州310027

人工智能(artificial intelligence,AI)医疗器械的研发与转化进入活跃期,产品的性能评价方法需要标准化且亟待创新。以促进行业发展、支撑监管、提升人工智能医疗器械产品质量为目标,浙江大学牵头联合中国食品药品检定研究院等多家专业... 详细信息

人工智能(artificial intelligence,AI)医疗器械的研发与转化进入活跃期,产品的性能评价方法需要标准化且亟待创新。以促进行业发展、支撑监管、提升人工智能医疗器械产品质量为目标,浙江大学牵头联合中国食品药品检定研究院等多家专业机构,依托人工智能医疗器械标准化技术归口单位,分析了人工智能医疗器械性能评价的共性问题,对相关测试方法进行了梳理总结。本文在专家组共识的基础上,对各种测试方法及其应用进行具体介绍,同时对相关的测试数据抽样加以阐述,以期在业内形成统一认识,从而促进人工智能医疗器械性能评价方法与流程的标准化,为人工智能医疗器械的高质量发展保驾护航。

关键词：人工智能医疗器械性能评价专家共识测试方法规范测试数据规范

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Dynamic Characteristic Analysis of HIV Mother to Child Transmission in china

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Biomedical and Environmental Sciences 2010年第5期23卷 402-408页

作者： JUN-JIE WANG KATHLEEN HEATHER REILLY HUA HAN ZHI-HANG PENG NING WANG national Center for AIDS/STD control and Prevention Chinese Center for Disease Control and PreventionBeijing 100050China Tulane University Health Sciences Center School of Public Health and Tropical MedicineNew OrleansLAUSA national ASIC Design Engineering Center Institute of AutomationChinese Academy of SciencesBeijing 100190China Department of Epidemiology and Biostatistics Nanjing Medical UniversityNanjing 210029China

Objective to explore dynamic characteristics of the HIV mother to child transmission （MTCT） epidemic in *** A deterministic dynamic transmission model was used to determine the effect of key parameters on the likely long-term trends of the HIV MTCT epidemic in *** 7.0 was used to develop the *** The number of the susceptibles （S）,the transmission rate （β）,and the screening proportion （α） of HIV positive pregnant women have the greatest impact on the HIV MTCT epidemic in *** growth of the MTCT epidemic in china could not be controlled only by decreasing the MTCT transmission *** prevalence of HIV positive women should be reduced and more pregnant women should be tested for *** Prevention of MTCT （PMTCT） should focus not only on the reduction of HIV transmission rates and incidences of HIV among women but also on the increase of HIV testing for pregnant *** most cost-effective PMTCT means for china should be investigated in future studies.

关键词： mother to child transmission dynamic model HIV china

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