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The Role of TNF Related Apoptosis-Inducing Ligand in Neurodegenerative Diseases

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Cellular & Molecular Immunology 2005年第2期2卷 113-122页

作者： Y.Huang N.Erdmann H.Peng Y.Zhao ThelaboratoryofNeurotoxicologyattheCenterforNeurovirology＆NeurodegenerativeDisorders ／／Dept.Pharmacology dept.ofSurgery UniversityofNebraskaMedicalCenterOmahaNE68198-5880USA／／InstituteofAnimalResearchChineseAcademyofScienceChina

A hallmark of all forms of neurodegenerative diseases is impairment of neuronal functions,and in many cases neuronal cell death.Although the etiology of neurodegenerative diseases may be distinct,different diseases display a similar pathogenesis,for example abnormal immunity within the central nervous system(CNS),activation of macrophage/microglia and the involvement of proinflammatory cytokines.Recent studies show that neurons in a neurodegenerative state undergo a highly regulated programmed cell death,also called apoptosis.TNF-related apoptosis-inducing ligand(TRAIL),a member of the TNF family,has been shown to be involved in apoptosis during many diseases.As one member of a death ligand family,TRAIL was originally thought to target only tumor cells and was not present in CNS.However,recent data showed that TRAIL was unregulated in HIV-1-infected and immune-activated macrophages,a major disease inducing cell during HIV-1-assoeiated dementia(HAD).TRAIL is also induced on neuron by β-amyloid protein,an important pathogen for Alzheimer's disease.In this review,we summarize the possible common aspects that TRAIL involved those neurodegenerative diseases,TRAIL induced apoptosis signaling in the CNS cells,and specific role of TRAIL in individual diseases.Cellular & Molecular Immunology.2005;2(2):113-122.

关键词： Alzheimer's disease HⅣ-1 associated dementia multiple sclerosis apoptosis TRAIL macrophage

EFFECTS OF QUERCETIN ON MEMBRANE FLUIDITY OF INJURED VASCULAR ENDOTHELIAL CELLS WITH HYPOXIA AND THE LACK OF GLUCOSE

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Journal of Pharmaceutical Analysis 2003年第2期15卷 196-198,201页

作者：林蓉刘俊田甘伟杰 dept. of pharmacology Medical School of Xi ’an Jiaotong University

Objective To study the effects of different concentrations of Quercetin on nitric oxide (NO) production and membrane fluidity of the injured human umbilical vein vascular endothelial cell line(ECV 304) with hypoxia and the lack of glucose. Methods The experiments were performed in the culture of ECV 304 injured with hypoxia and the lack of glucose in vitro. The releases of intracellular lactate dehydrogenase(LDH) of ECV 304 was measured with automatic biochemistry analysis. NO level of ECV 304 was monitored with colorimetry. The membrane fluidity of ECV 304 was measured with the fluorescence polarization method. Results After ECV 304 was cultured in hypoxia and the the lack of glucose for 24 hours, the release of LDH and the membrane fluidity were increased significantly; NO level was decreased. Preincubation of ECV 304 with 20, 80,160 μ mol·L -1  of Quercetin for 24 hours reduced LDH activity, membrane fluidity and increased the level of NO in hypoxia and the lack of glucose induced ECV 304. Conclusion These results demonstrate that Quercetin can produce the protective effect on hypoxia and the lack of glucose induced injury of ECV 304 by increasing release of NO and changing membrane fluidity.

关键词： quercetin(Que) endothelial cells membrane fluidity hypoxia and the lack of glucose

Regulation of expression of drug-metabolizing enzymes by oncogenic signaling pathways in liver tumors: a review

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Acta Pharmaceutica Sinica B 2020年第1期10卷 113-122页

作者： Albert Braeuning Michael Schwarz German Federal Institute for Risk Assessment Dept.Food SafetyBerlin 10589Germany Eberhard Karls University of Tu¨bingen Inst.of Pharmacology and ToxicologyDept.of ToxicologyTu¨bingen 72074Germany

Mutations in genes encoding key players in oncogenic signaling pathways trigger specific downstream gene expression profiles in the respective tumor cell populations.While regulation of genes related to cell growth,survival,and death has been extensively studied,much less is known on the regulation of drug-metabolizing enzymes(DMEs)by oncogenic signaling.Here,a comprehensive review of the available literature is presented summarizing the impact of the most relevant genetic alterations in human and rodent liver tumors on the expression of DMEs with a focus on phasesⅠandⅡof xenobiotic metabolism.Comparably few data are available with respect to DME regulation by p53-dependent signaling,telomerase expression or altered chromatin remodeling.By contrast,DME regulation by constitutive activation of oncogenic signaling via the RAS/RAF/mitogen-activated protein kinase(MAPK)cascade or via the canonical WNT/β-catenin signaling pathway has been analyzed in greater depth,demonstrating mostly positive-regulatory effects of WNT/β-catenin signaling and negativeregulatory effects of MAPK signaling.Mechanistic studies have revealed molecular interactions between oncogenic signaling and nuclear xeno-sensing receptors which underlie the observed alterations in DME expression in liver tumors.Observations of altered DME expression and inducibility in liver tumors with a specific gene expression profile may impact pharmacological treatment options.

关键词： Xenobiotic metabolism Hepatocytes WNT/b-catenin signaling RAS/MAPK signaling Gene mutation Cytochrome P450

SYNTHESIS AND CHARACTERIZATION OF NOVEL OPTICALLY ACTIVE POLY(AMIDE-IMIDE)S AND POLY(ESTER-IMIDE)S CONTAINING CALIX[4]ARENE AND AMINO ACID UNITS WITH BINDING ABILITY TOWARDS ALKALI METAL AND TOXIC HEAVY METAL CATIONS

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Chinese Journal of Polymer Science 2010年第5期28卷 731-743页

作者： Abdol-reza Hajipour Sakineh Habibi Arnold E.Ruoho dept.of pharmacology University of WisconsinMedical SchoolMadison53706-1532WIUSA Pharmaceutical Research Laboratory College of ChemistryIsfahan University of TechnologyIsfahan 84156IR Iran

A novel calix[4]arene derivative 2 with amino functional groups at the lower rim was first prepared via introduction of nitro functional groups and amination of the dinitro derivative of calix[4]arene. The optically active monomers were synthesized by dehydration of L-leucine （and L-isoleucine） and 3,3＇,4,4＇-benzophenonetetracarboxylic- 3,3＇,4,4＇-dianhydride （3） followed by reaction with thionyl chloride to form 5a and 5b. Two methods, polymerization under microwave irradiation and solution polymerization in CH2Cl2/TEA, were then employed to carry out the condensation polymerization of 2 with the optically active monomers 5a and 5b, respectively. The polymerization conditions affected the kind of resulting polymers, poly（amide-imide）s （PAIs） 6a and 6b and poly（ester-imide）s （PEIs） 6a＇ and 6b＇ were obtained selectively in good yields and moderate inherent viscosities. Sorption-extraction experiments were carried out using cram picrate extraction method and verified good binding ability of the resulting calixarene-based polymers towards silver, alkali metal and toxic heavy metal cations. Also thermogravimetric analysis indicated that the resulting PAIs and PEIs were thermally stable.

关键词： Condensation polymerization Ionophores Optically active Toxic heavy metals Polymeric calixarenes Thermal stability.

Prescription pattern of anti-malarial drugs in a tertiary care hospital

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Asian Pacific Journal of Tropical Medicine 2010年第5期3卷 379-381页

作者： Santoshkumar R Jeevangi Manjunath S Sharanabasappa M Awanti dept of pharmacology M.R.Medical CollegeGulbarga-585105Karnataka StateIndia dept of Biochemistry M.R.Medical CollegeGulbarga-585105Karnataka StateIndia

Objective:To evaluate the prescribing pattern of anti malarial drugs in a tertiary care hospital. Methods:A prospective cross-sectional study was conducted for 6 months of patients visiting in Basaveshwar Teaching and General Hospital,Gulbarga.Data were analyzed for various drug use indicators.Results:A total of 212 prescriptions were collected,with 136(64.15%) male and 76(35.85%) female.There were 128(60.37%) Plasmodium vivax cases and 84(39.63%) Plasmodium falciparum cases.All Plasmodium vivax cases were treated with chloroquine alone and among these 16(12.5%) recieved radical treatment with primaquine along with chloroquine.Among 84 patients with Pasmodium falciparum,40 patients received single drug such as quinine/ mefloquinine/artesunate/arteether.Another 44 patients received multidrug regime like,quinine+artesunate(54.54%),quinine+mefloquine(27.27%) and quinine+arteether (18.18%).Chloroquine was not administered to any of the patients with Plasmodium falciparum malaria.The most common adverse effects with chloroquine were anorexia,nausea,vomiting and tinnitus in 9.37% of the cases.With quinine it was nausea and vomiting in 17.64% ,tinnitus in 11.76% and hypoglycemia in 2.1% of cases.Conclusions:Our study found the perennial favorites like chloroquine for Plasmodium vivax and quinine for Plasmodium falciparum were the most effective drug.In the severe Plasmodium falciparum cases the artesunate derivatives and combination of artesunate with quinine/mefloquine were most effective with fewer incidences of side effects.

关键词： Malaria Chloroquine Artesunate Drug utilization Drug use indicators

Identification of Anxiolytic Potential of Niranthin:In-vivo and Computational Investigations

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Natural Products and Bioprospecting 2021年第2期11卷 223-233页

作者： Atul R.Chopade Prakash M.Somade Pratik P.Somade Suraj N.Mali Department of pharmacology Rajarambapu College of PharmacyKasegaonSangliMaharashtra 415404India dept.of Physiology Krishna Institute of Medical SciencesKaradMaharashtraIndia Government College of Pharmacy KaradMaharashtraIndia

Anxiety is an unpleasant state,which can critically decrease the quality of life is often accompanied by nervous behaviour and rumination.Niranthin is a lignan isolated from various Phyllanthus sources.The literature survey on niranthin highlights wide ranges of the therapeutic potentials.In a present study,based on our previous investigations,we evaluated pure,isolated and characterized niranthin as an anxiolytic agent.The niranthin[6-[(2R,3R)-3-[(3,4-dimethoxyphenyl)methyl]-4-methoxy-2-(methoxymethyl)butyl]-4-methoxy-1,3-benzodioxole]was purchased from commercial source and further subjected for assessment of its anxiolytic potentials using popular animal models including Elevated plus-maze model/test(EPM)and Light&Dark Exploration test(L&D).GABA-A receptor mediation was evaluated by pretreating the mice with the GABA-A receptor antagonist Flumazenil before the EPM task.Molecular docking simulation studies(pdb id:4COF)carried out by Vlife QSAR software showed that niranthin(docking score:−62.1714 kcal/mol)have shown comparatively best docking score compared to the standard drug Diazepam(docking score:−63.1568 kcal/mol).To conclude,Niranthin has probable potential in the management of anxiety disorder.Our in-silico and in-vivo analysis(indirectly)indicated the plausible role of GABA mediation for anxiolytic activity.Although,these studies are preliminary,future in depth experimental explorations will be required to use Niranthin as anti-anxiety drug in near future.

关键词： pharmacology Phytoconstituents Niranthin Lignan Anxiolytic activity EPM models

Study on the Heat Conduction of Phase-Change Material Microcapsules

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Journal of Thermal Science 2013年第3期22卷 257-260页

作者： Gangtao Zhao Xiaohui Xu Lin Qiu Xinghua Zheng Dawei Tang dept. of pharmacology General Hospital of Beijing Military Command Chinese People's Liberation Army CN 95824 Troop of Chinese People's Liberation Army CN Institute of Engineering Thermophysics Chinese Academy of Sciences

The 3ω approach was used to measure the effective thermal conductivity of phase-change material microcapsules (PCMMs) based on urea formaldehyde and sliced paraffin. The effective thermal conductivities of PCMMs with different densities were measured within the phase-change temperature range. The relationships between effective thermal conductivity, density and temperature were analysed. The effective thermal conductivity reached peak values within the phase-change temperature range and the temperature peak value was consistent with the peak value of the phase-change temperature. The effective thermal conductivity increased with increasing density due to the decreased porosity of samples and their increased solid-phase conduction.

关键词： 3ω-method, Effective thermal conductivity, Phase-change material microcapsules

三七中人参本醇甙抗心律失常作用的交感神经机理

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中国药理学与毒理学杂志 1990年第3期4卷 161-163页

作者：李学军张宝恒 dept. pharmacology Beijing Medical University Beijing 100083 China

给大鼠三七中人参二醇甙(PTS)150 mg/kgiv能明显抑制交感神经传出放电,减慢心率,暂时降低血压。PTS 75 mg/kg iv仅使血压呈现暂时升高。PTS 200μg/rat icv(约为iv有效量的1/150)也能明显抑制大鼠内脏交感神经传出放电,同时伴有血压降... 详细信息

给大鼠三七中人参二醇甙(PTS)150 mg/kgiv能明显抑制交感神经传出放电,减慢心率,暂时降低血压。PTS 75 mg/kg iv仅使血压呈现暂时升高。PTS 200μg/rat icv(约为iv有效量的1/150)也能明显抑制大鼠内脏交感神经传出放电,同时伴有血压降低和心率减慢,而用该剂量iv则对上述指标无任何影响。给大鼠icv PTS 400μg/rat可明显对抗iv乌头碱诱发的心律失常。上述结果表明PTS对中枢交感神经系统有抑制作用,此作用可能是其抗心律失常的作用机理之一。

关键词：三七人参三醇甙抗心律失常药

PHARMACOLOGICAL RESEARCH ON THE EFFECT OF LICORICE

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Journal of Traditional Chinese Medicine 1988年第4期 307-309页

作者：任骏王振钢 dept.of pharmacology Peking Union Medical College

Licorice is extracted from the roots and sto-lons of Glycyrrhiza uralensis Fisch,a plant initial-ly cultivated for its medical value as describedvery early in“Compendium of Materia Medica”(Li Shizhen).In 1760 a certain George Dunhilladded sugar to licorice,creating a popular con-fection.Licorice is widely used as a flavoringagent in foods,beverages,tobacco and some me-dications.Further studies of its effective com-ponents and mechanisms of action have beenmade only recently,however,with the develop-ment of modem medical techniques.

关键词： PHARMACOLOGICAL RESEARCH ON THE EFFECT OF LICORICE AIDS