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Anti-inflammatory effect of amurensin H on asthma-like reaction induced by allergen in sensitized mice

Acta Pharmacologica Sinica 2006年第6期27卷 735-740页

作者： Yi-tang LI~2 Chun-suo YAO~3 Jin-ye BAI~2 Man LIN~3 Gui-fang CHENG~(2,4)2 Department of Pharmacology,institute of materia medica,peking union medical college and chinese academy of medical sciences,beijing 100050,china 3 Department of Photochemistry,institute of materia medica,chinese academy of medical sciences and peking union medical college,beijing 100050,china Department of Pharmacology Institute of Materia Medica Peking Union Medical College and Chinese Academy of Medical Sciences Beijing China Department of Photochemistry Institute of Materia Medica Chinese Academy of Medical Sciences and Peking Union Medical College Beijing China

Aim:To explore the anti-inflammatory effects of amurensin H on asthma-like reac-tion induced by allergen in sensitized ***:BALB/c mice were sensi-tized by ovalbumin(OVA,ip)on d 0 and d 14 and challenged with 1% OVA on d 18to *** developed airway eosinophilia,mucus hypersecretion,and elevationin cytokine *** were administered amurensin H orally at the doses of 49,70,or 100 mg/kg once every day from d 15 to the last *** lavagefluid(BALF)were collected at 24 h and 48 h after the last OVA *** tumor necrosis factor-α(TNF-α),interleukin 4(IL-4),interleukin 5(IL-5),andinterleukin 13(IL-13)in BALF were measured using ELISA *** counts of macrophages,lymphocytes,neutrophils and eosinophils were per-formed in 200 cells per slide(one slide per animal).Lung tissue sections of 6-μmthickness were stained with Mayer’s hematoxylin and eosin for assessment of cellinfiltration,mucus production,and tissue ***:Oral administrationof amurensin H significantly inhibited OVA-induced increases in total cell counts,eosinophil counts,and TNF-α,IL-4,IL-5 and IL-13 levels in *** addition,amuresin H dramatically decreased OVA-induced lung tissue damage and ***:Amurensin H may have therapeutic potential for thetreatment of allergic airway inflammation.

关键词： amurensin H asthma ovalbumin tumor necrosis factor-α Th2 cells cytokines

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Synthesis and anti-diabetic activity of(RS)-2-ethoxy-3-{4-[2-(4-trifluoro-methanesulfonyloxy-phenyl)-ethoxy]-phenyl}-propionic acid

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Acta Pharmacologica Sinica 2006年第5期27卷 597-602页

作者： Zhe-feng CAI Quan LIU Ping-ping LI Zong-ru GUO~1 Zhu-fang SHEN institute of materia medica,chinese academy of medical sciences and peking union medical college,beijing 100050,china institute of materia medica Chinese Academy of Medical Sciences and Peking Union Medical College Beijing China

Aim:To synthesize and study the anti-diabetic activity of (RS)-2-ethoxy-3-{4-[2-(4-trifluoromethanesulfonyloxy-phenyl)-ethoxy]-phenyl}-propionic acid(compound Ⅰ).Methods:Compound Ⅰ was prepared in 6 steps,using 4-(2-hy-droxy-ethyl)-phenol as the starting *** in vitro selectivity and potencyof target compound Ⅰ,rosiglitazone and WY-14643 on human PPARα and PPARγwere determined in reporter gene *** vivo,rosiglitazone and compound Ⅰwere administered orally to KKAymice for *** tolerance tests and oralglucose tolerance tests were performed on the 10th and 14th day of treatment,*** the end of the treatment,sera were collected for ***:In vitro,compound Ⅰ significantly activated both PPARα andPPARγ.In vivo,compound Ⅰ corrected the impaired insulin and glucose toleranceof KKAymice,and produced a significant reduction in plasma triglyceride levelsafter 14d of *** effect produced was significant compared with thecontrol ***:Both in vitro and in vivo anti-diabetic activity studiesfor compound Ⅰ were conducted and the data suggest that this compound is apotentially effective anti-diabetic agent.

关键词： hypoglycemic agents peroxisome proliferator-activated receptors agonists

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High-throughput fluorescence polarization method for identifying ligands of LOX-1

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Acta Pharmacologica Sinica 2006年第4期27卷 447-452页

作者： Tian-tai ZHANG~2 Zhen-tai HUANG~3 Ying DAI~2 Xiu-ping CHEN~2 Ping ZHU~3 Guan-hua DU~(2,4) ~2National Centre for Pharmaceutical Screening,institute of materia medica,chinese academy of medical sciences and peking union medical college,beijing 100050,china:~3Department of Natural Product Biosynthesis,institute of materia medica,chinese academy of medical sciences and peking union medical college,beijing 100050,china National Centre for Pharmaceutical Screening Institute of Materia Medica Chinese Academy of Medical Sciences and Peking Union Medical College Beijing China Department of Natural Product Biosynthesis Institute of Materia Medica Chinese Academy of Medical Sciences and Peking Union Medical College Beijing China

Aim: To develop and optimize a competitive fluorescence polarization(FP)method,and use it as a high-throughput screening(HTS)assay for drug ***: Human lectin-like oxidized low-density lipoprotein receptor-1(hLOX-1)and oxidized low-density lipoprotein(oxLDL)were used to establish a high-throughput fluorescence polarization assay to screen ligands of human LOX-1. A96-well plate assay was performed with a fast plate reader. Three fluoresceinisothiocyanate-labeled hLOX-1 concentrations(100, 200, and 400 nmol/L)wereselected to be titrated by oxLDL(from 0.05 nmol/L to 100 μmol/L)in order to obtainoptimal reactive concentrations. The concentration of Me2SO used(0%, 1%, 3%,5%) and incubation time(15 min, 30 min, 1 h, 2 h)were optimized. The Z’factor wascalculated to estimate the quality of FP-based HTS. Results: Concentrations of200 nmol/L for human LOX-1 and 50 μmol/L for oxLDL were used in the actualassay. Concentrations of 0% to 5% Me2SO and different reaction times did notaffect the FP-based HTS. The Z’value was 0.66. By using this detection andscreening system, 12 700 compounds were screened and 3 ligands with an IC50ofless than 4.5 μmol/L were found. Conclusion: The established competitive FP-based assay is sensitive, stable, highly reproducible and robust, and suitable forHTS for ligands of the hLOX-1 receptor.

关键词： high-throughput screening fluorescence polarization assay LDL receptors oxidized low density lipoprotein

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Comparison of antioxidant activities between salvianolic acid B and Ginkgo biloba extract(EGb 761)

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Acta Pharmacologica Sinica 2006年第9期27卷 1137-1145页

作者： Chang-suo LIU Yong CHENG Jin-feng HU Wei ZHANG Nai-hong CHEN Jun-tian ZHANG~2 Department of Neuropharmacology,institute of materia medica,chinese academy of medical sciences and peking union medical college,beijing 100050.china Department of Neuropharmacology Institute of Materia Medica Chinese Academy of Medical Sciences and Peking Union Medical College Beijing China

Aim:To investigate and compare the antioxidant activities of salvianolic acid B(SalB)and Ginkgo biloba extract(EGb 761)in aqueous solution,rat microsomesand the cellular ***:Superoxide anion(O2~-)was generated usingxanthine/xanthine oxidase system and phenazine methosulate/NADH system,andthe effects of SalB and EGb 761 on the generation of O2~- were achieved by spectro-photometric measurement of the product formed on reduction of nitro *** different methods were used to assess the scavenging effects ofthe extracts on hydroxyl radical(.OH):HPLC method was used for quantitation *** by oxy-radical trapping of 5,5-dimethyl- 1-pyrroline-N-oxide(DMPO)to formDMPO-OH adducts in Fe2+-*** confirm the HPLC data,.OHwas also measured by spectrophotometry using a commercial detection ***-lipid peroxidation effects of the extracts in microsomes of rat brain,liver andkidney induced by ascorbate-NADPH were determined by thiobarbituric acid(TBA)*** protective effects of the extracts on peroxide hydrogen(H2O2)-induced oxidative damage in SH-SY5Y cells were investigated by assessing cellviability assay,the level of lipid peroxidation,and the lactate dehydrogenase(LDH)***:Both SalB and EGb 761 were able to scavenge O2~- ***,inhibit lipid peroxidation of microsomes,and protect SH-SY5Y ceils againstH2O2-induced oxidative ***,the concentration of SalB was far lowerthan that of EGb 761 when a similar effect was ***:The antioxi-dant efficiency of SalB was greater than that of EGb *** results suggestthat SalB,like EGb 761,has promising potential in treating oxidative damage-derived neurodegenerative disorders.

关键词： antioxidant Ginkgo biloba extract 761 free radical salvianolic acid B SH-SY5Y cells

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High performance liquid chromatographic separation of thirteen drugs collected in chinese Pharmacopoeia 2010(Ch.P2010) on cellulose ramification chiral stationary phase

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Journal of Pharmaceutical Analysis 2012年第1期2卷 48-55页

作者： Ying Zhoua,b, Chao Maa, Yan Wanga, Qi-Ming Zhangb, Yi-Ying Zhanga, Jie Fua, Hong Gaoc, Li-Xun Zhaoc aState Key Laboratory of Bioactive Substances and Functions of Natural Medicines, institute of materia medica, chinese academy of medical sciences & peking union medical college, beijing 100050, china bNational institute for the Control of Pharmaceutical and Biological Products, beijing 100050, china cinstitute of Medicinal Biotechnology, chinese academy of medical sciences & peking union medical college, beijing 100050, china State Key Laboratory of Bioactive Substances and Functions of Natural Medicines Institute of Materia Medica Chinese Academy of Medical Sciences & Peking Union Medical College Beijing 100050 China. National institute for the Control of Pharmaceutical and Biological Products Beijing 100050 China. institute of Medicinal Biotechnology Chinese Academy of Medical Sciences & Peking Union Medical College Beijing 100050 China.

The enantiomers separation of thirteen drugs collected in Ch.P2010 was performed on chiral stationary phase of cellulose ramification (chiralpak OD and chiralpak OJ) by high performance liquid chromatographic (HPLC) methods, which included ibuprofen (C1), ketoprofen (C2), nitrendipine (C3), nimodipine (C4), felodipine (C5), omeprazole (C6), praziquantel (C7), propranolol hydrochloride (C8), atenolol (C9), sulpiride (C10), clenbuterol hydrochloride (C11), verapamil hydrochloride (C12), and chlorphenamine maleate (C13). The mobile phase consisted of isopropanol and n-hexane. The detection wavelength was set at 254 nm and the fiow rate was 0.7 mL/min. The enantiomers separation of these thirteen racemates on chiralpak OD column and chiralpak OJ column was studied, while the effects of proportion of organic additives, alcohol displacer and temperature on the separation were studied. And the mechanism of some of racemates was discussed. The results indicated that thirteen chiral drugs could be separated onchiral stationary phase of cellulose ramification in normal phase chromatographic system. The chromatographic retention and resolution of enantiomers could be adjusted by factors including column temperature and the concentration of alcohol displacer and organic alkaline modifier in mobile phase. It was shown that the resolution was improved with reducing concentration of alcohol displacer. When concentration of organic alkaline modifier was 0.2% (v/v), the resolution and the peak shape were fairly good. Most racemates mentioned above had better resolution at column temperature of 25 1C. When racemates were separated, the temperature should be kept so as to obtain stable separation results.

关键词： HPLC Chiral stationary phase Optical enantiomers Cellulose ramification

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Formation of 4'-carboxyl acid metabolite of imrecoxib by rat liver microsomes

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Acta Pharmacologica Sinica 2006年第4期27卷 506-512页

作者： Hai-yan XU~2 Peng ZHANG~2 Ai-shen GONG~3 Yu-ming SUN~2 Feng-ming CHU~4 Zong-ru GUO~4 Da-fang ZHONG~(2,5,6)2 Laboratory of Drug Metabolism and Pharmacokinetics,Shenyang Pharmaceutical University,Shenyang 110016,china 3 Research and Development Center,Shanghai Hengrui Pharmaceutical Co,Shanghai 200245,china:4 institute of materia medica,chinese academy of medical sciences and peking union medical college,beijing 100050,china 5 Shanghai institute of materia medica,chinese academy of sciences,Shanghai 201203,china Laboratory of Drug Metabolism and Pharmacokinetics Shenyang Pharmaceutical University Shenyang China Research and Development Center Shanghai Hengrui Pharmaceutical Co Shanghai China institute of materia medica Chinese Academy of Medical Sciences and Peking Union Medical College Beijing China Shanghai institute of materia medica Chinese Academy of Sciences Shanghai China

Aim:Imrecoxib is a novel and moderately selective COX-2 *** aim ofthe present in vitro investigation was to study the formation of the major metabo-lite 4′-carboxylic acid imrecoxib（M2）and identify the enzyme（s）involved in ***:The formation of M2 was studied in rat liver cytosol in theabsence or presence of liver *** formed metabolite was identifiedand quantified by LC/MS~*** addition,to characterize the cytochrome P450（CYP）isozymes involved in M2 formation,the effects of typical CYP inhibitors（such asketoconazle,quinine,α-naphthoflavone,methylpyrazole,and cimetidine）on theformation rate of M2 were ***:The formation of M2 from 4’-hydroxymethyl imrecoxib（M4）was completely dependent on rat liver microsomesand *** kinetic studies demonstrated that the formation rate of M2conformed to monophasic Michaelis-Menten *** experimentsshowed that the formation of M2 was induced significantly by dexamethasoneand lowered by ketoconazole strongly and ***,other CYP inhibitors,such as α-naphthoflavone,cimetidine,quinine,and methylpyrazole had no inhibitory effects on this metabolic ***:These biotransformation studies of M4 and imrecoxib in rat liver atthe subcellular level showed that the formation of M2 occurs in rat liver microsomesand is *** reaction was mainly catalyzed by CYP 3A inuntreated rats and in dexamethasone-induced *** CYP,such as CYP 1A,2C,2D,and 2E,seem unlikely to participate in this metabolic pathway.

关键词： imrecoxib cytochrome P450 metabolism liver microsomes rats

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Drug screening for influenza neuraminidase inhibitors

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Science china(Life sciences) 2005年第1期48卷 1-5页

作者： LIU Ailin, CAO Hongpeng & DU Guanhua institute of materia medica, chinese academy of medical sciences and peking union medical college, beijing 100050, china institute of Medicinal Biotechnology, chinese academy of medical sciences and peking union medical college, beijing 100050, china institute of materia medica Chinese Academy of Medical Sciences and Peking Union Medical College Beijing100050 China institute of Medicinal Biotechnology Chinese Academy of Medical Sciences and Peking Union Medical College Beijing100050 China

Neuraminidase (NA) is one of the most important targets to screen the drugs of anti-influenza virus A and B. After virtual screening approaches were applied to a compound database which possesses more than 10000 compound structures, 160 compounds were selected for bioactivity assay, then a High Throughput Screening (HTS) model established for influenza virus NA inhibitors was applied to detect these compounds. Finally, three compounds among them displayed higher inhibitory activities, the range of their IC5o was from 0.1 μmol/L to 3 μmol/L. Their structural scaffolds are novel and different from those of NA inhibitors approved for influenza treatment, and will be useful for the design and research of new NA inhibitors. The result indicated that the combination of virtual screening with HTS was very significant to drug screening and drug discovery.

关键词： neuraminidase (NA), inhibitor, high throughput screening (HTS), influenza virus, virtual screening.

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Protective effect of tubuloside B on TNFα-induced apoptosis in neuronal cells

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Acta Pharmacologica Sinica 2004年第10期 36-44页

作者： Min DENG, Jin-yuan ZHAO, Xiao-dong JU, Peng-fei TU, Yong JIANG, Zheng-bin LIResearch Center of Occupational Medicine, Department of Orthopaedics, peking University Third Hospital, beijing 100083, china peking University Modem Research Center for Traditional chinese Medicine, beijing 100083, china institute of materia medica, chinese academy of medical sciences, peking union medical college, beijing 100050, china

AIM: To investigate the neuroprotective effect of tubuloside B, one of the phenylethanoids isolated from the stems of Cistanche salsa, on tumor necrosis factor-alpha (TNFα)-induced apoptosis in SH-SY5Y neuronal cells. METHODS: Cell viability was analyzed using MTT assay. Apoptotic cells were detected using Hoechst33342 staining, and confirmed by DNA fragmentation and flow cytometric analysis. The activity of caspase-3 was measured with special assay kit. The concentration of free intracellular calcium was determined with the probe Indo-1 by spectrometer. The level of intracellular reactive oxygen species and the potential of mitochondrial membrane were determined by laser scanning confocal microscopy (LSCM) combined with fluorescence probe H2DCFDA or JC-1 respectively. RESULTS: SH-SY5Y cells treated with TNFa 100 μg/L for 36 h showed typical morphological changes of apoptosis. DNA ladder could be observed by agarose gel electrophoresis. The highest percentage of apoptotic cells accumulated to 37.5 %. F

关键词： tubuloside B apoptosis tumor necrosis factor SH-SY5Y cells mitochondria membrane potential reactive oxygen species caspase-3 calcium

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Role of rat liver cytochrome P450 3A and 2D in metabolism of imrecoxib

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Acta Pharmacologica Sinica 2006年第3期27卷 372-380页

作者： Hai-yan XU~2 Zhi-yong XIE~2 Peng ZHANG~2 Jin SUN~3 Feng-ming CHU~4 Zong-ru GUO~4 Da-fang ZHONG~(2,5) ~2Laboratory of Drug Metabolism and Pharmacokinetics ~3Department of Biopharmaceutics,Shenyang Pharmaceutical University,Shenyang 110016,china ~4institute of materia medica,chinese academy of medical sciences and peking union medical college,beijing 100050,china Laboratory of Drug Metabolism and Pharmacokinetics Shenyang Pharmaceutical University Shenyang China Department of Biopharmaceutics Shenyang Pharmaceutical University Shenyang China institute of materia medica Chinese Academy of Medical Sciences and Peking Union Medical College Beijing China

Aim:To investigate the in vitro metabolism of imrecoxib in rat liver microsomesand to identify the cytochrome P450(CYP)forms involved in its ***:Liver microsomes of Wistar rats were prepared using an *** in vitro metabolism of imrecoxib was studied by incubation with rat *** characterize the CYP forms involved in the 4'-methyl hydroxyla-tion of imrecoxib,the effects of typical CYP inducers(such as dexamethasone,isoniazid and β-naphthoflavone)and of CYP inhibitors(such as ketoconazole,quinine,α-naphthoflavone,methylpyrazole,and cimetidine)on the formation rateof 4'-hydroxymethyl imrecoxib were ***:Imrecoxib was me-tabolized to 3 metabolites by rat liver microsomes:4'-hydroxymethyl imrecoxib(M4),4'-hydroxymethyl-5-hydoxyl imrecoxib(M3),and 4'-hydroxymethyl-5-car-bonyl imrecoxib(M5).Over the imrecoxib concentration range studied(5-600μmol/L),the rate of 4'-methyl hydroxylation conformed to monophasic Michaelis-Menten *** significantly induced the formation of *** markedly lowered the metabolic rate of imrecoxib in a concentra-tion-dependent ***,a significant inhibitory effect of quinine onthe formation of M4 was observed in microsomes obtained from control rats,isoniazid-induced rats,and β-naphthofiavone-induced *** contrast,α-naphthoflavone,cimetidine,and methylpyrazole had no inhibitory effects on thismetabolic ***:Imrecoxib is metabolized via 4'-methyl hydroxy-lation in rat liver microsomes,The reaction is mainly catalyzed by CYP ***2D also played a role in control rats,in isoniazid-induced rats and in β-naphthoflavone-induced rats.

关键词： imrecoxib cytochrome P450 metabolism liver microsomes

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Beneficial effects of melatonin in experimental models of Alzheimer disease

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Acta Pharmacologica Sinica 2006年第2期27卷 129-139页

作者： Yong CHENG~2 Zheng FENG~3 Qing-zhu ZHANG~4 Jun-tian ZHANG~(2.5) ~2Department of Pharmacology,institute of materia medica,chinese academy of medical sciences and peking union medical college,beijing 100050,china:~3Department of Anesthesiology,University of California,San Diego,and Veterans Affairs medical Center,3350 La Jolla Village Drive,San Diego,CA 92161,USA:~4Department of Pharmacology,college of Pharmacy,Shandong University,Jinan 250012,china Department of Pharmacology Institute of Materia Medica Chinese Academy of Medical Sciences and Peking Union Medical College Beijing China Department of Anesthesiology University of California San Diego Veterans Affairs medical Center San Diego USA Department of Pharmacology College of Pharmacy Shandong University Jinan China

Alzheimer’s disease(AD),a progressive degenerative disorder,is characterizedby the presence of amyloid deposits,neurofibrillary tangles and neuron *** evidence indicates that antioxidants could be useful either for the pre-vention or treatment of *** has been shown that melatonin is a potent antioxi-dant and free radical ***,melatonin stimulates severalantioxidative enzymes and improves mitochondrial energy *** find-ings led us to study amyloid precursor protein transgenic mice,ovariectomizedrats,and pheochromocytoma and astroglioma cell lines,to observe whether mela-tonin had any effect on Alzheimer’s symptoms or pathological *** foundthat melatonin had many beneficial effects in experimental models of AD,includ-ing improvement of cognitive function,anti-oxidative injury,anti-apoptosis,inhi-bition of β-amyloid(Aβ)deposition and Aβ fiber *** groups haveshown that melatonin has an inhibitory effect on tau protein *** actions may potentially slow down or stop the progression of dementia.

关键词： melatonin Alzheimer disease beta-amyloid protein calcium overload APP transgenic mice ovariectomized rats tau protein hyperphosphorylation

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