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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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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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Chemopreventive effect of dimethyl dicarboxylate biphenyl on malignant transformation of WB-F344 rat liver epithelial cells

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Acta Pharmacologica Sinica 2005年第11期26卷 1339-1344页

作者： Hua SUN, Geng-tao LIU~2 ~2 department of Pharmacology, institute of materia medica, peking union medical college & chinese academy of medical sciences, beijing 100050, china department of Pharmacology Institute of Materia Medica Peking Union Medical College & Chinese Academy of Medical Sciences Beijing China

Aim: To study the potential chemopreventive effect of dimethyl dicarboxylate biphenyl (DDB), an anti-hepatitis drug, on hepatocarcinogenesis in vitro. Methods: The anti-carcinogenesis effect of DDB was assessed on a two-stage chemical oncogenesis model induced by 3-methylcholanthrene and 12-0-tetradecanoyl phorbol 13-acetate (TPA) with WB-F344 rat liver epithelial cells (WB-F344 cells) in vitro. A soft-agar colony formation assay was used to determine the tumorigenic potential of the transformed WB-F344 cells. The gap junctional intercellular communication (GJIC) was detected using the scrape loading/ dye transfer technique. Results: DDB at 1 μmol/L, 2 μmol/L, and 4 μmol/L significantly prevented the malignant transformation of WB-F344 cells induced by 3-methylcholanthrene and TPA. The average number of transformed foci decreased dramatically by 10.0%, 37.2%, and 47.4%, respectively. In soft agar, a remarkable decrease in colony numbers was observed in transformed cells treated with 2 μmol/L and 4 μmol/L DDB. DDB at 1 μmol/L, 2 μmol/L, and 4 μmol/L inhibited the downregulation of GJIC induced by TPA in a dose-dependent manner. The GJIC recovered to 25.6%, 34.6%, and 44.9%, respectively, of the control WB-F344 cells by DDB. Conclusion: DDB has a potential chemopreventive effect on hepatocarcinogenesis induced by carcinogens in vitro.

关键词： dimethyl dicarboxylate biphenyl liver neoplasm: cell transformation chemoprevention epithelial cell gap junctions

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High-throughput screening for monoamine oxidase-A and monoamine oxidase-B inhibitors using one-step fluorescence assay

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Acta Pharmacologica Sinica 2006年第6期27卷 760-766页

作者： Hong-mei GUANG Guan-hua DU~2 institute of materia medica,peking union medical college and chinese academy of medical sciences,beijing 100050,china institute of materia medica Peking Union Medical College and Chinese Academy of Medical Sciences Beijing China

Aim:To develop high-throughput screening(HTS)assays for monoamine oxi-dase(MAO)-A and MAO-B ***:A fluorescence probe basedmethod measuring MAO-A and MAO-B activity was established and optimized,with its sensitivity,stability and specificity *** conditions in-cluding enzyme sources,substrate concentrations,incubation volume and reac-tion time in 384-well format were optimized to achieve sensitive and low consump-tive ***:In optimized conditions,dynamic parameters of MAO-A andMAO-B were *** Kmvalue of serotonin to MAO-A was 1.66μmol/L,while that of benzylamine to MAO-B was 0.80 μmol/*** IC50value of clorgylineto MAO-A was 2.99 nmol/L,and that of deprenyl to MAO-B was 7.04 nmol/L,matching those obtained from traditional spectrometric *** testedsamples,one compound exerted an inhibitory effect on MAO-A activity with IC50as 0.36 μmol/L,and three compounds had an inhibitory effect on MAO-B activitywith IC50as 0.13,0.19,and 0.13 μmol/*** Z′ factor was 0.71±0.03 and 0.75±0.03in MAO-A-inhibitor and MAO-B-inhibitor HTS system,***:The established assays can be well applied to MAO-A and MAO-B inhibitorscreening with high quality,precision and reproducibility.

关键词： fluorescence assay monoamine oxidase preclinical drug evaluation

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Studies on the Preparation of Bioactive Oligomerstilbene by Oxidative Coupling Reaction(Ⅰ)-Preparation of Shegansu B using Silver Oxide as Oxidant

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chinese Chemical Letters 2000年第6期11卷 515-516页

作者： Li Xin ZHOU Mao LIN(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

篢he oxidative coupling reaction of isorhapontigenin using sliver oxide as oxidant afforded a major product, named shegansu B（2）， which was isolated from the roots of Belamcanda chinensis (L．)DC. Both the natural ... 详细信息

关键词： Isorhapontigenin oligomerstilbene shegansu B oxidative coupling reaction silver oxide

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SYNTHESIS OF PEG-DENDRIMERIC PEPTIDE

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chinese Chemical Letters 1996年第8期7卷 693-694页

作者： De Xin WANG and Lei HUANG(institute of materia medica, chinese academy of medical sciences and peking union medical college,beijing 100050) institute of materia medica Chinese Academy of Medical Sciences Peking Union Medical College Beijing 100050

Synthesis of a new macromolecule with MW up to 7.6 KDA is described in the present paper. The ligation between a dendrimeric amino-PEG and unprotected peptides via a site- specific reaction is a useful trial for the p... 详细信息

关键词： PEG SYNTHESIS OF PEG-DENDRIMERIC PEPTIDE

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Lactariolide,a New 14-Membered-Ring Compound from Lactarius Subvellereus

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chinese Chemical Letters 1997年第2期8卷 135-136页

作者： Jing ZHANG Xiao Zhang FENG(institute of materia medica, chinese academy of medical sciences and peking union medical college, beijing, 100050) institute of materia medica Chinese Academy of Medical Sciences Peking Union Medical College Beijing 100050 China

Lactariolide (I), a new 14-membered-ring lactone was isolated from the fruit bodies of Lactarius subvellereus (Russulaceae), and its structure was elucidated as (R)-13-hydroxy-trans-9, 11-octadecadienoic acid lactone ... 详细信息

关键词： Cl Lactariolide,a New 14-Membered-Ring Compound from Lactarius Subvellereus

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Anti-amnestic and anti-aging effects of ginsenoside Rg1 and Rb1 and its mechanism of action

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Acta Pharmacologica Sinica 2005年第2期26卷 143-149页

作者： Yong CHENG Li-hong SHEN Jun-tian ZHANG institute of materia medica,peking union medical college and chinese academy of medical sciences,beijing 100050,china institute of materia medica Peking Union Medical College and Chinese Academy of Medical Sciences Beijing China

In the present paper,we overview the discovery of new biological activitiesinduced by ginsenoside Rg1 and Rb1 and discuss possible mechanisms of *** compounds could increase neural plasticity in efficacy and structure;espe-cially Rg1,as one small molecular drug,can increase proliferation and differentia-tion of neural progenitor cells in dentate gyrus of hippocampus of normal adultmice and global ischemia model in *** finding has great value for treat-ment of Alzheimer’s disease and other neurodegenerative disorders which is char-acterized by neurons *** of expression of brain derived neurotrophicfactor,Bcl-2 and antioxidant enzyme,enhanced new synapse formation,inhibitionof apoptosis and calcium overload are also important neuron protective *** and Rbl have common effects,but there are some differences in pharmacol-ogy and *** differences may attribute to their different ***1 is panaxtriol with two sugars,while Rb1 is panaxtriol with foursugars.

关键词： ginseng ginsenoside-Rg1 ginsenoside-Rb1 learning memory neural progenitor cells apoptosis immunity synaptic plasticity muscarinic cholinergic receptor long-term potentiation

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Studies on Chemical Constituents of Belamcanda Chinensis(L.)DC.(Ⅱ)

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chinese Chemical Letters 1997年第2期8卷 133-134页

作者： Li Xin ZHOU and Mao LIN(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

Nine compounds were isolated from the acetone soluble fraction of ethanolic extract of the roots of Belamcanda chinensis (L.)DC. The structure of new compound I,named shegansu A,has been established as irigenin-5-O-(6'-O-vanillin acid)-β-D-glucoside(Ⅰ) by the use of spectroscopic evidence (UV, IR. FAB-MS.1HNMR, 13CNMR,1H-13CNMR and NOE difference spectrum) and chemical *** well known compounds were identified as isorhapotigenin (Ⅲ),resveratrol(Ⅳ), P-hydroxy benzoic acid (Ⅴ), iridin (Ⅵ), tectoridin (Ⅶ),tectorigenin(Ⅷ) and daucosterol(Ⅸ). Ⅲ-Ⅸ were isolated from the plant for the first time.

关键词： DC OCH

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Total Synthesis of (±)-Cordatolide A and its Anti-HIV Activity

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chinese Chemical Letters 1999年第8期10卷 653-656页

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

The natural product (±)-cordatolide A has been synthesized by a four-step approach starting from phloroglucinol, including Pechmann reaction, Friedel-Crafts acylation, cyclization. chromenylation and Luche reduction.

关键词： Total synthesis (±)-cordatolide A

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