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治疗高血压藥物的研究 Ⅵ.国产蘿芙木中水溶性生物鹼的藥理作用

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生理学报 1959年第1期 54-63页

作者： division of pharmacology, institute OF MATERIA medica,{3.(Shanghai) 中国科学院药物研究所药理组上海

用蘿芙木屬(Rauwolfia)植物的生物鹼来治疗高血压已受到普遍的重视;其中以Reserpine最受注意,它有降低血压作用,并有特殊的鎮靜效能。我国广东、广西、云南諸省出产蘿芙木植物均为Rauwolfia verticillata(Lour.)Baill.,它的化学和藥理... 详细信息

用蘿芙木屬(Rauwolfia)植物的生物鹼来治疗高血压已受到普遍的重视;其中以Reserpine最受注意,它有降低血压作用,并有特殊的鎮靜效能。我国广东、广西、云南諸省出产蘿芙木植物均为Rauwolfia verticillata(Lour.)Baill.,它的化学和藥理均有报导。临床正拟試用国产蘿芙木治疗高血压。刘鑄晋等用离子交换剂获得蘿芙木全鹼,本文是研究它的毒性、降压及中樞鎮靜作用,以便推荐它到临床試用。

关键词：高血压皮下注射升压反应肾上腺素肾上腺能α-受体兴奋药小白鼠水溶性

BASIC FEATURES OF THE GLACIERS OF THE *** LUNGMA REGION,SOUTHERN PART OF THE TIBET AUTONOMOUS REGION,CHINA

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Science in China,Ser.A 1975年第1期 106-130页

作者： division of Glaciology, Lanchow institute of Glaciology, Cryopedology and Desert Research, academia sinica 中国科学院兰州冰川冻土沙漠研究所冰川研究室

As a result of the scientific investigation of Mt. Jolmo Lungma——the world’s highestpeak in 1966-1968, the authors make a detailed discussion on the features of mountainglaciers in the Mt. Jolmo Lungma region, which are developed in low latitudes by intensiveuplifting. Glaciers there are continental ones characterized by rather limited nourishmentand slow melting rate, moderate speed of movement, low ice temperature and slight varia-tion in advancement and retreat. Under the influence of intense solar radiation and otherfactors, ice formation of infiltration and congelation exists extensively from the snowlineto the summit in the Mt. Jolmo Lungma region, and the valley glaciers below the snowlineappear in the form of wonderful forest of ice pyramids. From a comparative study, we havediscovered that the rate of undulatory recessions of the glaciers of this region might be thesmallest among the valley glaciers of the world since the glacial epoch of late *** sculptured by the glaciers have reached a 'mature stage', but the erosion anddeposition of the glaciers are comparatively weak.

关键词： MT

STUDIES ON THE MECHANISMS OF INSULIN ACTION I. THE INTERACTIONS OF INSULIN AND ITS ANALOGS WITH INSULIN RECEPTOR

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Science in China,Ser.A 1974年第6期 779-792页

作者： Insulin Research Group, division of Endocrinology, Peking institute of Zoology, academia sinica and Insulin Research Group, Shanghai institute of Biochemistry, academia sinica 中国科学院北京动物研究所内分泌室胰岛素组中国科学院上海生物化学研究所胰岛素组

The receptor-binding properties of insulin and its analogs with modified C-terminal peptide sequence of the B-chain have been studied in liver cells and fat cells. The results have shown that despentapeptide insulin has the same binding capacity as that of insulin; deshexapeptide insulin and its analog with B23.glycine replaced by D-alanine have definite binding effect; desoctapeptide insulin has a very weak binding effect; the A-chain of insulin, ACTH and glucagon do not bind with insulin receptor. On this basis, the possible involvement of B24 aromatic ring in the binding part has been discussed and it has been proposed that the hydrophobic surface formed by B12, B16, B24 and B25 may be an important element of the binding part and the B20—B23.U turn and A21...B22 salt linkage may have a stabilizing effect on the hydrophobic structure, and that the binding of insulin with the receptor protein may be similar to the formation of the insulin dimer from the two monomers.

关键词： THE INTERACTIONS OF INSULIN AND ITS ANALOGS WITH INSULIN RECEPTOR STUDIES ON THE MECHANISMS OF INSULIN ACTION ITS

A PERTURBATION SOLUTION FOR NON-NEWTONIAN FLUID TWO-PHASE FLOW THROUGH POROUS MEDIA

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Acta Mechanica sinica 1987年第1期3卷 1-10页

作者： Li Xi Guo Shangping (Lanzhou Research division of Mechanics of Flow Through Porous Media,academia sinica) Lanzhou Research division of Mechanics of Flow Through Porous Media Academia Sinica China

In this paper,the mathematical problem of weak non-Newtonian fluid two-phase flowthrough porous media,including the effect of capillary pressure,is solved by singular perturbation methodin combination with regular perturbation *** asymptotic analytical solutions of the fractional flowfunction and the wetting phase saturation are *** results are verified by numerical calculationsand by classical solutions for corresponding Newtonian *** influences of the non-Newtonian exponentand capillary pressure are discussed.

关键词： non-Newtonian flnid multiphase porous media perturbation

EXOTHERMIC MODEL OF PERCOLATION ZONE IN A GLACIER

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Chinese Science Bulletin 1989年第4期34卷 312-314页

作者：蔡保林匡佩琼 Lanzhou institute of Glaciology and Geocryology Academia Sinica Lanzhou Research division of Mechanics of Flow Through Porous Media Academia Sinica

During the ablation period, the melt-water on the surface of percolation zone of a glacier percolates down through the snow layer when it cools and freezes, the latent heat released causes the temperature of metres of the snow layer to rise to 0℃. However, at the end of ablation period melting stops, the snow layer through which melt-water permeated begins to release heat to the air and the temperature on the surface of snow layer decreases. As a result, the melt-water in the snow layer

关键词： percolation zone permeating depth temperature.

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Design,synthesis,antitumor evaluations and molecular modeling studies of novel 3.5-substituted indolin-2-one derivatives

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Acta Pharmacologica sinica 2007年第1期28卷 140-152页

作者： Hai-hong LI~2 Xiu-hua ZHANG~3.Jin-zhi TAN~2 Li-li CHEN~2 Hong LIU~(2,5) Xiao-min LUO~(2,5) Xu SHEN~(2,4) Li-ping LIN~(3.5) Kai-xian CHEN~2 Jian DING~3.Hua-liang JIANG~(2,4)2 Center for Drug Discovery and Design,State Key Laboratory of Drug Research,Shanghai institute of Materia medica,Shanghai institutes for Biological Sciences,and Graduate School,Chinese Academy of Sciences,Shanghai 201203.China 3.{3. of Anti-tumor pharmacology,Shanghai institute of Materia medica,Shanghai institutes for Biological Sciences,Chinese Academy of Sciences,Shanghai 201203.China 4 School of Pharmacy,East China University of Science and Technology,Shanghai 20023.,China Center for Drug Discovery and Design State Key Laboratory of Drug Research Shanghai Institute of Materia Medica Shanghai Institutes for Biological Sciences and Graduate School Chinese Academy of Sciences Shanghai China division of Anti-tumor pharmacology Shanghai Institute of Materia Medica Shanghai Institutes for Biological Sciences Chinese Academy of Sciences Shanghai China School of Pharmacy East China University of Science and Technology Shanghai China

Aim:To design and synthesize a novel class of antitumor agents,featuring the 3.5-substituted indolin-2-one ***:Based on enzyme binding fea-tures of（Z）-SU5402,introducing a β-pyrrole group at the 3.position of the indolin-2-one core,a series of novel 3.5-substituted indolin-2-ones were designed *** human carcinoma cell lines of A-43.,A-549,MDA-MB-468,and Autosomal Dominant Polycystic Kidney disease were chosen for the cellproliferation ***:Twenty new compounds（1a-t）with E configurationhave been designed,synthesized and *** structural features weredetermined by nuclear magnetic resonance（NMR）spectra,low-and high-resolu-tion mass spectra,and confirmed by X-ray *** the enzymeassay showed a weak inhibition effect against the epidermal growth factor receptor,vascular endothelial growth factor receptor,fibroblast growth factor receptor andplatelet-derived growth factor receptor tyrosine kinases,the cell-based antitumoractivity was *** 1 g and lh showed higher inhibitory activitytoward the A-549 and MDA-MB-468 cell lines with IC50of 0.065-9.4 μmol/***:This study provides a new template for further development ofpotent antitumor drugs.

关键词： protein-tyrosine kinase indolin-2-one antitumor drug screening assays drug design molecular models

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 20023.,China 4 {3. of Nephrology,Department of Internal Medicine,Changzheng Hospital,Second Military medical University,Shanghai 200003.China 5 {3. of Antitumor pharmacology,Shanghai institute of Materia medica,Shanghai 201203.China 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 China School of Pharmacy East China University of Science and Technology Shanghai China division of Nephrology Department of Internal Medicine Changzheng Hospital Second Military Medical University Shanghai China division of Antitumor pharmacology Shanghai Institute of Materia Medica Shanghai China

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(1-2,3.-g,4a-w,and 5a-l)were designed,synthesized and *** com-pounds(1,3.,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

SIMULATION OF MICROWAVE GUN INJECTOR RF LINAC DRIVING INFRARED FREE ELECTRON LASERS

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Journal of Electronics(China) 1992年第2期9卷 153-162页

作者：刘红秀 FEL division IHEP Academia Sinica Beijing

In contrast with the conventional injector consisting of dc gun, chopper, subharmonicbuncher and/or fundamental buncher, a microwave gun can cooperate with an alpha magnet as amore compact high brightness injector for the dedicated rf linear accelerators driving infrared freeelectron lasers (FELs). Such a concept has been put into practice in the MARK III FEL and willbe used in the Beijing Free Electron Laser (BFEL) as well. In this paper, the phase spread, energyspread, energy spread, emittance growth and intensity variation of a single electron microbunchin such an FEL accelerator system are investigated using SUPERFISH and PARMELA.

关键词： Microwave gun injector FEL Linac

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Dispersion of ventricular mRNA of RyR2 and SERCA2 associated with arrhythmogenesis in rats

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Acta Pharmacologica sinica 2004年第6期25卷 36-41页

作者： Hong-lan WANG, De-zai DAI2, Feng GAO3. Yan-pin ZHANG3. Feng LU Research division of pharmacology, China Pharmaceutical University, Nanjing 210009, China 3.aboratorial Center ofMedicine, Southeast University, Nanjing 210009, China Research division of pharmacology China Pharmaceutical University Nanjing 210009 Laboratorial Center of Medicine Southeast University Nanjing 210009

AIM: To investigate the effect of CPU86017 on the changes of mRNA abundance of different calcium handling system in infarcted heart. METHODS: Rats were subjected to left coronary ligation to induce myocardial infarc- tion (MI). The treatment with either propranolol (Pro) 5 mg/kg ip or CPU86017 1, 2, and 4 mg/kg ip was initiated on the next day of operation and continued for 20 d. medication with isoproterenol (Isop) 3.mg/kg sc started on the d 17-21. Ventricular mRNA abundance of ryanodine receptor 2 (RyR2), sarcoplasmic reticulum Ca2+-ATPase (SERCA2), L-type Ca2+ channel, and Na+/Ca2+exchanger (NCX1) were measured. RESULTS: Arrhythmic scores (AS) in the Isop group was raised up to 5.27±1.75 (P3. The AS was depressed by Pro (1.63.1.53. P3.00±1.24, and 1.70±1.85, P<0.01 vs Isop). The significant dispersion of depressed mRNA abundance of RyR2 and SERCA2 was associated with an increase in AS in Isop group, and it was much depressed in the left than the right ventricle. The dispersion and depression of mRNA were restored significantly by Pro and CPU86017, asso- ciated with suppression on AS. In Isop group, the mRNA abundance of L-type Ca2+ channel was not changed; and a moderate increase in the mRNA of NCX1 was seen, the changes were regressed by Pro and CPU86017. CONCLUSION: Isop-induced arrhythmogenesis in MI heart was correlated mainly with a dispersion of depressed mRNA abundance in ventricle likely due to the consequence of PKA over-phosphorylation. A suppression of arrhythmia by Pro and CPU86017 resulted from a regression of the dispersion and depression of RyR2 and SERCA2.

关键词： myocardial infarction isoproterenol arrhythmia calcium 4-chlorobenzyltetrahydroberberine