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| 1 | Development of a complex scintillation proximity assay for highthroughput screening of PPAR7 modulators显示文摘Aim: To develop a complex high-throughput screening (HTS) assay based on scintillation proximity assay (SPA) technology for identification of novel peroxisome proliferator-activated receptor gamma (PPARγ) modulators. Methods: Fulllength PPARγand retinoid X receptor alpha (RXRα), biotinylated PPAR response element (PPRE), [^3H]BRL49653 and streptavidin-coated FlashPlate or microbead were used to develop an HTS assay based on SPA technology. This ‘ABCDE' method was validated against conventional hydroxyapatite (HA) assay and applied to large-scale screening of 16 000 synthetic compounds and natural product extracts. Results: (1) IC50 values of positive control compounds (BRL49653 and troglitazone) obtained from the ‘ABCDE' method and HA assay were comparable and consistent with those reported elsewhere; (2) Approximately 178 compounds, showing more than 70% competitive inhibition on BRL49653 binding to PPARγ, were identified initially by the ‘ABCDE' method (microbead); (3) Secondary screening using FlashPlate and cross-reactivity studies with RARα, β,γand RXRα,β,γconfirmed that 12 compounds possessed specific PPARγbinding properties including 2 with IC50 values less than 0.5μmol/L and novel chemical structures. Conclusions: The ‘ABCDE' method using either FlashPlate or microbead, is a highly efficient, automatable, and robust tool to screen potential PPARγmodulators in HTS setting. Its application may be expanded to other nuclear receptors that form heterodimers upon activation. | Bin WU Jie GAO Ming-wei WANG~2 The National Center for Drug Screening,Shanghai Institute of Materia Medica,Shanghai Institutes for Biological Sciences,Chinese Academy of Sciences Graduate School of Chinese Academy of Sciences,Shanghai 201203,China | 2005 | Acta Pharmacologica Sinica2005，26，3： | 12 |
| 2 | 英国大肠癌筛查预试验首轮结果显示文摘目的:评价在英国国家医疗体系(National Health Service,NHS)中推行以便隐血试验为基础的全国大肠癌筛查项目的可行性。 | UK Colorectal Cancer Screening Pilot Group 胡恩坦 | 2004 | 英国医学杂志中文版2004，7，6： | 7 |
| 3 | Pharmacokinetic Study of Baicalein and Its Major Metabolites after iv Administration in Dogs显示文摘Objective To develop and validate a simple,rapid,sensitive,and reproducible HPLC method for simultaneous determination of baicalein and its metabolite baicalin in dog plasma and for the subsequent pharmacokinetic study after iv administration to dogs.Methods An accurate and reproducible HPLC-UV method was developed and validated for simultaneous determination of baicalein and baicalin in dog plasma,using luteolin as internal standard.The analytes were separated by an Agilent Zorbax SB-C18 column(250 mm × 4.6 mm,5 μm) and the column temperature was maintained at 40 ℃.The mobile phase was a binary mixture of acetonitrile and water(27:73) ,containing 0.05% phosphoric acid in water,with a flow rate of 1.0 mL/min.The UV detector was set at 276 nm.Results Linear relationships were validated over the range of 0.05-25 μg/mL for baicalein and 0.05-20 μg/mL for baicalin.The intra-and inter-day precision values for all samples were within 8.0%,using relative standard deviation.This method was successfully applied to the pharmacokinetic studies in dogs after iv administration of baicalein.Baicalein was converted to baicalin quickly.Cmax values were 21.13 μg/mL at 0.05 h for baicalein and 1.57 μg/mL at 0.5 h for baicalin,areas under the plasma concentration-time curve were 4.97 h·μg/mL for baicalein and 0.63 h·μg/mL for baicalin,and the elimination half-life is 0.50 h for baicalein and 0.75 h for baicalin,respectively.Conclusion The method is able and sufficient to be used in drug metabolism and pharmacokinetic studies of baicalein. | TIAN Shuo1,DU Li-da2,WANG Shou-bao1,HE Guo-rong1,YANG Tao1,LI Xiao-xiu1,GUO Jing1,DU Guan-hua1 1.National Centre for Pharmaceutical Screening,Institute of Materia Medica,Chinese Academy of Medical Sciences and Peking Union Medical College,Beijing 100050,China 2.School of Pharmacy,China Pharmaceutical University,Nanjing 210009,China | 2011 | Chinese Herbal Medicines2011，3，3： | 5 |
| 4 | Atmospheric Precursors of and Response to Anomalous Arctic Sea Ice in CMIP5 Models显示文摘This study examines pre-industrial control simulations from CMIP5 climate models in an effort to better understand the complex relationships between Arctic sea ice and the stratosphere, and between Arctic sea ice and cold winter temperatures over Eurasia. We present normalized regressions of Arctic sea-ice area against several atmospheric variables at extended lead and lag times. Statistically significant regressions are found at leads and lags, suggesting both atmospheric precursors of, and responses to, low sea ice; but generally, the regressions are stronger when the atmosphere leads sea ice, including a weaker polar stratospheric vortex indicated by positive polar cap height anomalies. Significant positive midlatitude eddy heat flux anomalies are also found to precede low sea ice. We argue that low sea ice and raised polar cap height are both a response to this enhanced midlatitude eddy heat flux. The so-called 'warm Arctic, cold continents' anomaly pattern is present one to two months before low sea ice, but is absent in the months following low sea ice, suggesting that the Eurasian cooling and low sea ice are driven by similar processes. Lastly, our results suggest a dependence on the geographic region of low sea ice, with low Barents–Kara Sea ice correlated with a weakened polar stratospheric vortex, whilst low Sea of Okhotsk ice is correlated with a strengthened polar vortex. Overall, the results support a notion that the sea ice, polar stratospheric vortex and Eurasian surface temperatures collectively respond to large-scale changes in tropospheric circulation. | Michael KELLEHER James SCREEN | 2018 | Advances in Atmospheric Sciences2018，35，1： | 4 |
| 5 | Anti-diabetes Agents——I:Tetralone Derivative from Juglans regia显示文摘A new compound, 4-hydroxy-a-tetralone-4-O-b-D-[6-O-(3,4,5-trihydroxybenzoyl) glucopyranoside (1), together with a known compound, 4-hydroxy-a-tetralone (2), has been isolated from the roots of Juglans regia. 2 showed moderate bioactivity against protein tyrosine phosphatase 1B (PTP1B). | Tian Ying AN, Li Hong HU*, Rong Min CHEN, Zhong Liang CHEN, Jia LI, Qiang SHEN Chinese National Center for Drug Screening, Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, Shanghai 200031 | 2003 | Chinese Chemical Letters2003，14，5： | 4 |
| 6 | Newborn screening:toward a uniform screening panel and sys- tem -executive summary显示文摘 | American College of Medical Genetics Newborn Screening Expert Group | 2006 | Pediatrics2006，117，52： | 1 |
| 7 | Cost -effec- tiveness of screening for colorectal cancer: evidence from the Nottingham faecal occult blood trial显示文摘 | Whynes DK Nottingham FOB Screening Trial | 2004 | J Med Screen2004，11，1： | 1 |
| 8 | Dramatic interannual changes of perennial Arctic sea ice linked to abnormal summer storm activity显示文摘 | Screen J A Simmonds I Keay K | 2011 | Journal of Geophysical Research2011，116，15： | 1 |
| 9 | Local and remote controls on observed Arctic warming显示文摘 | Screen J. A. Deser C. Simmonds I | 2012 | EN2012，，1： | 1 |
| 10 | Reduced lung-cancer mortality with low-dose computed tomographic screening显示文摘 | National Lung Screening Trial Research Team Aberle DR Adams AM | 2011 | N Engl J Med2011，365，5： | 1 |
| 11 | Status of NAT screening for HCV, HIV and HBV : experience in Japan显示文摘 | Japanese Red Cross NAT Screening Research Group | 2002 | Dev Biol (Basel)2002，108，： | 1 |
| 12 | Evaluation of screening activity in Iceland显示文摘 | Sigurdsson K: Effect of organized screening on the risk of cervical cancer | 1993 | J Cancer1993，54，4： | 1 |
| 13 | Status of NAT screening for HCV, HIV and HBV: experience in Japan 显示文摘 | Japanese Red Cross NAT Screening Research Group | 2002 | Dev Biol(Basel)2002，108，1： | 1 |
| 14 | The European Group for Colorectal Cancer Screening显示文摘 | Recommendation to include colorectal cancer screening in public health policy | 1999 | J Med Screen1999，6，2： | 1 |
| 15 | Reduced tung- mortality with low dose computed tomographic screening显示文摘 | National Lung Screening Trial Research Team Aberle DR Adams AM el cancer al | 2011 | N Engl J Med2011，365，5： | 1 |
| 16 | Reduced lung-cancer mortality with low dose computed tomographic screening显示文摘 | National Lung Screening Trial Research Team Aberle DR Adams AM | 2011 | N Engl J Med2011，365，2： | 1 |
| 17 | Synthesis and hydrazones, Schiff and mannich bases of isatin derivatives 显示文摘 | Sridhar S K Saravanan M antibacterial screening of Ramesh A | 2001 | European Journal of Medicinal Chemistry2001，36，： | 1 |
| 18 | Newborn screening: toward a uniform screening panel and system-executive summary显示文摘 | American College of Medical Genetics Newborn Screening Expert Group | 2006 | Pediatrics2006，，： | 1 |
| 19 | Hepatitis B e antigen and the risk of hepatocellular carcinoma显示文摘 | Yang HI Lu SN Liaw YF You SL Sun CA Wang LY Hsiao CK Chen PJ Chen DS Chen CJ Taiwan Community-Based Cancer Screening Project Group | 2002 | N Engl J Med2002，347，3： | 1 |
| 20 | Further characterization of cells expressingSTRO-1 in cultures of adult human bone marrow stromal cells 显示文摘 | Stewart K Walsh S Screen J | 1999 | J Bone MinerRes1999，14，8： | 1 |
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