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Antitumor activity of a novel recombinant mutant human tumor necrosis factor-related apoptosis-inducing ligand

Acta Pharmacologica Sinica 2005年第11期26卷 1373-1381页

作者： fang fang~2, ai-ping wang~2, shi-fang yang~3 ~2 institute of materia medica, chinese academy of medical sciences and peking union medical college, beijing 100050 ~3 beijing Sunbio Biotech LTD, beijing 100081, China institute of materia medica Chinese Academy of Medical Sciences and Peking Union Medical College Beijing China beijing Sunbio Biotech LTD Beijing China

aim: To investigate the antitumor activity and safety of a novel recombinant mutant human tumor necrosis factor-related apoptosis-inducing ligand (rmh TRaiL). Methods: Antitumor activity of rmh TRaiL was evaluated by using several tumor cell lines by MTT assay in vitro, and by using a mouse xenograft model in vivo, rmh TRaiL-induced apoptosis in tumor cells was detected by cell death enzyme-linked immunosorbent assay (ELISA), TdT-mediated dUTP nick-end labeling (TUNEL) assay and flow cytometry. The safety of rmh TRaiL was also evaluated in several normal human cell lines. Results: At the concentration of 0.32-1 000 ng/mL, rmh TRaiL remarkably inhibited the proliferation of 5 tumor cell lines from lung, colon, and breast cancer compared with wild type (wt TRaiL) in vitro, whereas at the concentration of 1 ng/mL-10 μg/mL, rmh TRaiL showed no or mild cytotoxicity in the normal cell lines, rmh TRaiL (3,15 mg/kg, ip, once daily for 10 d) exerted a significant inhibition on the growth of xenograft tumor NCI-H460 in nude mice compared with the saline group (PaiL, a positive control. The apoptosis of NCI-H460 cells was markedly induced in a concentration-dependent and time-dependent manner after rmh TRaiL treatment. The percentage of apoptotic cells induced by rmh TRaiL in NCI-H460 cells was significantly higher than that by wt TRaiL. Conclusion: rmh TRaiL provided potent antitumor activity in vivo and in vitro, whereas most normal human cells were resisitant to rmh TRaiL. The results suggested that rmh TRaiL might be a useful anticancer agent in future.

关键词： antineoplastic agents tumor necrosis factorrelated apoptosis-inducing ligand apoptosis flow cytometry NCI-H460 cells

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Protective effects of compound FLZ onβ-amyloid peptide-(25-35)-induced mouse hippocampal injury and learning and memory impairment

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Acta Pharmacologica Sinica 2006年第6期27卷 651-658页

作者： fang fang Geng-tao LIU~2 Department of Pharmacology,institute of materia medica,peking union medical college and chinese academy of medical sciences,beijing 100050.China Department of Pharmacology Institute of Materia Medica Peking Union Medical College and Chinese Academy of Medical Sciences Beijing China

aim:To study the protective effects of compound FLZ,a novel synthetic ana-logue of natural squamosamide,on learning and memory impairment and lesionsof the hippocampus caused by icv injection of β-amyloid25-35(Aβ25-35)in ***:Mice were icv injected with the Aβ25-35(15 nmol/mouse),and thentreated with oral administration of 75 mg/kg or 150 mg/kg of FLZ once daily for 16consecutive *** impairment of learning and memory in mice were testedusing step-down test and Morris water maze *** content of malondialdehyde(MDA)and the expressions of acetylcholinesterase(ACHE),Bax,and Bcl-2 in theCA1 region of the mouse hippocampus were measured by biochemical and immu-nohistochemical analysis,*** pathological damages of hippocam-pus were observed using a ***:FLZ(75 mg/kg,150 mg/kg)significantly attenuated Aβ25-35-induced impairment of learning and memory in thestep-down test and Morris water maze *** also reduced pathological dam-ages to the hippocampus induced by Aβ25-35Furthermore,FLZ prevented theincrease of AChE and Bax,and the decrease of Bcl-2 immunoreactive cells in theCA1 region of the hippocampus,and reduced the increase of MDA content in thehippocampus in mice injected with Aβ***:FLZ has protective ac-tion against the impairment of learning and memory and pathological damage tothe hippocampus induced by icv injection of Aβ25-35in mice.

关键词： FLZ Aβ25-35 intracerebroventricular injection hippocampus acetylcholinesterase Bax Bcl-2 malondialdehyde

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

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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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The Ephemeral 10β-OH Trifluoromethanesulfonates of 7-Epi Paclitaxel Analogs─A New Example for Anchimeric Assistance

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chinese Chemical Letters 1998年第1期9卷 29-33页

作者： Wei Shuo fang Qi Cheng fang and Xiao Tian LIANG (institute of materia medica, chinese academy of medical sciences & peking union medical college, beijing 100050 ) institute of materia medica Chinese Academy of Medical Sciences Peking Union Medical College Beijing 100050 China

Two rearranged products, dienone 4 and 10-oxo product 5 were obtained upon attempted 10β-OSO2SO2CF3 formation from 3. The formation of compound 5 can be explained by anchimeric assistance of 7α-OH. Reduction of 4 ... 详细信息

关键词： rearrange anchimeric assistance neighboring group participation

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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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Preliminary Studies on Acylation of 10β-OH and 7α-OH in 7-Epi-10-deacetylpaclitaxel

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chinese Chemical Letters 1997年第10期8卷 847-848页

作者： Wei Shuo fang Qi Cheng fang and Xiao Tian LIANG (institute of materia medica , chinese academy of medical sciences & peking union medical college.beijing 100050) institute of materia medica Chinese Academy of Medical Sciences Peking Union Medical College Beijing 100050 China

10β-OH can be acylated cleanly when 7α-OH is also free, and thus a facile access to semisynthesis of 7-epi-paclitaxel was proposed. A 2's, 3's-oxazoline paclitaxel analog was serendipitously synthesized

关键词： OH in 7-Epi-10-deacetylpaclitaxel TES Preliminary Studies on Acylation of 10

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Total Synthesis of Bilobetin and Isoginkgetin

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chinese Chemical Letters 1997年第8期8卷 701-704页

作者： Xue shi MAO shi ping XU Xiao Tian LIANG(institute of materia medica) (chinese academy of medical sciences & peking union medical college beijing 100050) institute of materia medica Chinese Academy of Medical Sciences Peking Union Medical College Beijing 100050 China

Total synthesis of bilobetin and isoginkgetin has been achieved by Pd(PPh3)(4) catalytic coupling of 8-flavone-boronic acids with iodoflavones.

关键词： OCH II Total Synthesis of Bilobetin and Isoginkgetin HRMS

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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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Mass Spectral Behavior of Some Indole Schiff-Base Derivatives

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chinese Chemical Letters 1999年第9期10卷 763-766页

作者： Li XU shi ping XU(institute of materia medica, chinese academy of Mdical sciencesand peking union medical college, beijing 100050) institute of materia medica Chinese Academy of Mdical Sciences Peking Union Medical College Beijing 100050 China

Twenty-two indole Schiff-base derivatives were synthesized. Two special ways of cleavage were discussed in the formation of the specific fragment ions in the mass spectra(MS).

关键词： Schiff-base cleavage specific fragment ions EI high resolution MS

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Imrecoxib: a novel and selective cyclooxygenase 2 inhibitor with anti-inflammatory effect

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Acta Pharmacologica Sinica 2004年第7期25卷 81-85页

作者： Xiao-hong CHEN, Jin-ye Bai, fang SHEN, ai-ping Bai, Zong-ru GUO, Gui-fang CHENG2 Departmentof Pharmacology, institute of materia medica, chinese academyof medical sciencesand peking union medical college, beijing 100050, China Department of Pharmacology Institute of Materia Medica Chinese Academy of Medical Sciences and Peking Union Medical College 北京 100050 Department of Pharmacology Institute of Materia Medica Chinese Academy of Medical Sciences and Peking Union Medical College Beijing 100050 Department of Pharmacology Institute of Materia Medica Chinese Academy of Medical Sciences and Peking Union Medical College

aiM: To investigate the inhibitory effect of imrecoxib, a synthetic compound of completely new structure, on cyclooxygenase 1 (COX-1) and 2 (COX-2) and its anti-inflammatory effect in vivo. METHODS: The inhibitory effects of imrecoxib on cyclooxygenase 1 and 2 were studied using whole cell assay with murine peritoneal mac- rophages induced by calcimycin and LPS. The inhibitory effects of imrecoxib on mRNA level of COX-1 and COX- 2 in human macrophage cell line U937 were detected by reverse transcription polymerase chain reaction (RT-PCR) analysis. Effects of imrecoxib on acute and chronic inflammation were evaluated in rat carrageenan induced edema model and rat adjuvant-induced arthritis model, respectively. RESULTS: Imrecoxib was found to inhibit COX-1 and COX-2 with IC50 value of 115±28 nmol/L and 18±4 nmol/L, respectively. Imrecoxib was shown to selectively and dose-dependently inhibit COX-2 mRNA level. Imrecoxib effectively inhibited carrageenan-induced acute in- flammation at the doses of 5, 10, and 20 mg·kg-1 ig and adjuvant-induced chronic inflammation at the doses of 10 and 20 mg·kg-1·d-1 ig. CONCLUSION: Imrecoxib is a novel and moderately selective COX-2 inhibitor that pos- sesses anti-inflammatory effect by inhibition of COX-2 mRNA expression.

关键词： imrecoxib cyclooxygenase 1 cyclooxygenase 2 cyclooxygenase inhibitors inflammation

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