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Conformational re-analysis of(+)-meptazinol:an opioid with mixed anal-gesic pharmacophores

Acta Pharmacologica Sinica 2006年第9期27卷 1247-1252页

作者： Wei LI~2 Xing-hai WANG~2 Choi-wan LAU~3 Yun TANG~(2,4)Qiong XIE~2 Zhui-bai QIU~(2,5)2 Department of Medicinal Chemistry 3 nmr laboratory,school of pharmacy,fudan university,shanghai 200032,china 4 school of pharmacy,East china university of Science and Technology,shanghai 200237,china Department of Medicinal Chemistry School of Pharmacy Fudan University Shanghai China nmr laboratory School of Pharmacy Fudan University Shanghai China school of pharmacy East China University of Science and Technology Shanghai China

Aim:To further investigate the analgesic pharmacophore of(+)-***:Two different opioid pharmacophores,Pharm-Ⅰ and Pharm-Ⅱ,were es-tablished from structures of nine typical opiates and meperidine by using molecu-lar modeling approaches according to their different structure activity relation-ship *** were further validated by a set of conformationally con-strained *** conformers of(+)-meptazinol(Conformer-Ⅰ and Con-former-Ⅱ)detected in solution were then fitted into the pharmacophores,respectively,by Fit Atoms facilities available in SYBYL,a computational modelingtool kit for molecular design and ***:Conformer-Ⅰ fit Pharm-Ⅰ fromtypical opiates ***,Conformer-Ⅱ fit none of these ***,it was found to be similar to another potent analgesic,benzofuro[2,3-c]pyridin-6-ol,whose pharmacophore was suggested to hold the transitional statebetween the two established *** typical analgesics derivedfrom 4-aryl piperidine(eg,meperidine)with one conformer absolutely overwhelming,the(+)-meptazinol exists in two conformers with similar amounts in ***,both conformers can not transform to each other freely in ordinaryconditions based on our nmr ***:(+)-meptazinol was suggestedto be an opioid with mixed analgesic pharmacophores,which may account for thecomplicated pharmacological properties of meptazinol.

关键词： (+)meptazinol opioid analgesics arylpiperidines Conformational Analysis,pharmacophore.

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Role of Apolipoprotein A-I in Protecting against Endotoxin Toxicity

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Acta Biochimica et Biophysica Sinica 2004年第6期36卷 419-424页

作者： Juan MA, Xue-Ling LIAO, Bin LOU, and Man-Ping WU* Department of Biochemistry, school of pharmacy, fudan university, shanghai 200032, china Department of Biochemistry School of Pharmacy Fudan UniversityShanghai 200032 China

High density lipoprotein (HDL) binds lipopolysaccharide (LPS or endotoxin) and neutralizes its toxicity. We investigated the function of Apolipoprotein A-I (ApoA-I), a major apolipoprotein in HDL, in this process. Mouse macrophages were incubated with LPS, LPS+ApoA-I, LPS+ApoA-I+LFF (lipoprotein-free plasma fraction d>1.210 g/ml), LPS+HDL, LPS+HDL+LFF, respectively. MTT method was used to detect the mortality of L-929 cells which were attacked by the release-out cytokines in LPS-activated macrophages. It was found that ApoA-I significantly decreased L-929 cells mortality caused by LPS treatment (LPS vs. LPS+ApoA-I, P3.20 ± 10.13) h in LPS+ApoA-I group and (46.80 ± 3.79) h in LPS+ApoA-I+LFF group, which were significantly longer than that in LPS group (16.25 ± 17.28) h (P35 ± 3.70) (P3) ApoA-I is the major contributor for HDL anti-endotoxin function.

关键词： Apolipoprotein-I lipopolysaccharide (LPS) macrophages FITC-lipopolysaccharide (FITC-LPS) L-929 cells

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A New Stilbene Tetramer from Caragana rosea

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Chinese Chemical Letters 2003年第10期14卷 1048-1050页

作者： Guo Xun YANG, Chang Qi HU school of pharmacy, fudan university, shanghai 200032 school of pharmacy Fudan University Shanghai 200032 China

Cararosinol A, a new stilbene tetramer, was isolated from Caragana rosea. Its structure has been established on the basis of spectroscopic evidence.

关键词： Caragana rosea Leguminase stilbene tetramer.

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Effect of MePEG molecular weight and particle size on in vitro release of tumor necrosis factor-α-loaded nanoparticles

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Acta Pharmacologica Sinica 2005年第2期26卷 242-249页

作者： Chao FANG,Bin SHI,Yuan-ying PEI~2 Department of Pharmaceutics,school of pharmacy,fudan university,shanghai 200032,china Department of Pharmaceutics School of Pharmacy Fudan University Shanghai China

Aim:To study the in vitro release of recombinant human tumor necrosis factor-alpha(rHuTNF-α)encapsulated in poly(methoxypolyethyleneglycol cyanoacry-late-co-n-hexadecyl cyanoacrylate)(PEG-PHDCA)nanoparticles,and investigatethe influence of methoxypolyethyleneglycol(MePEG)molecular weight and par-ticle ***:Three sizes(approximately 80,170,and 240 nm)of PEG-PHDCA nanoparticles loading rHuTNF-α were prepared at different MePEG mo-lecular weights(Mr=2000,5000,and 10000)using the double emulsion *** in vitro rHuTNF-α release was studied in PBS and rat ***:Ahigher burst-release and cumulative-release rate were observed for nanoparticleswith higher MePEG molecular weight or smaller particle size.A decreased cu-mulative release of rHuTNF-α following the initial burst effect was found in PBS,while the particle sizes remained constant and MePEG *** contrast,inrat plasma,slowly increased cumulative-release profiles were obtained after theburst *** a 5-h incubation in rat plasma,more than 50% of the PEG-PHDCA nanoparticles ***:The MePEG molecular weightand particle size had an obvious influence on rHuTNF-α release,rHuTNF-αreleased from PEG-PHDCA nanoparticles in a diffusion-based pattern in PBS,but in a diffusion and erosion-controlled manner in rat plasma.

关键词： tumor necrosis factor-alpha stealth nanoparticles polyethylene glycols poly(methoxypolyethyleneglycol cyanoacrylate-con-hexadecyl cyanoacrylate)

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Hydrogen sulfide:third gaseous transmitter,but with great pharmacological potential

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Acta Pharmacologica Sinica 2007年第11期28卷 1709-1716页

作者： Chang-qing CHEN Hong XIN Yi-zhun ZHU Department Of Pharmacology,school of pharmacy,fudan university shanghai 200032,china Department of Pharmacology School of Pharmacy Fudan University Shanghai China

Hydrogen sulfide (H2S),which is well known traditionally as a toxic gas,has beenproven to be produced endogenously by 3 enzymes in mammalian tissues andplays important roles in physiological and pathophysiological *** thecentral nervous system,H2S functions as not only a neuromodulator,but also aneuroprotectant against oxidative *** the cardiovascular system,H2S re-laxes vascular smooth muscles by the activation of KATPchannels and inhibitssmooth muscle cell proliferation via the mitogen-activated protein kinase signal-ing *** effects are important for maintaining blood pressure andpreventing vessel structural remodeling,and identifies H2S as an important factorin the development of some vascular diseases,such as hypertension.H2S alsoshows cardioprotective effects in ischemic myocardium and septic and *** studies have demonstrated a new mechanism to explain the motoreffect of H2S on the rat detrusor muscle,which is through the activation of thecapsaicin-sensitive primary *** review focuses on the recent researchachievements on H2S and discloses the great potential of H2S as the third gaseoustransmitter in cardiac protection.

关键词： hydrogen sulfide cystathionine β-synthetase cystathionine γ-lyase KATP channels capsaicin

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Identification and Characterization of glnA Promoter and its Corresponding Trans-regulatory Protein GlnR in the Rifamycin SV Producing Actinomycete,Amycolatopsis mediterranei U32

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Acta Biochimica et Biophysica Sinica 2006年第12期38卷 831-843页

作者： Hao YU~(1&) Wen-Tao PENG~1 Yang LIU~1 Ting WU~2 Yu-Feng YAO~1 Ming-Xue CUI~1 Wei-Hong JIANG~1 Guo-Ping ZHAO~(1,3,4*) 1 laboratory of Molecular Microbiology,Institute of Plant Physiology and Ecology,shanghai Institutes for Biological Sciences,Chinese Academy of Sciences,shanghai 200032,china 2 Department of Medicinal Chemistry,school of pharmacy,fudan university,shanghai 200032,china 3 State Key laboratory of Genetic Engineering & Department of Microbiology,school of Life Science,fudan university,shanghai 200433,china 4 laboratory of Disease and Health Genomics,Chinese National Human Genome Center at shanghai,shanghai 201203,china laboratory of Molecular Microbiology Institute of Plant Physiology and Ecology Shanghai Institutes for Biological Sciences Chinese Academy of Sciences Shanghai 200032 China Department of Medicinal Chemistry School of Pharmacy Fudan University Shanghai 200032 China State Key laboratory of Genetic Engineering & Department of Microbiology School of Life Science Fudan University Shanghai 200433 China laboratory of Disease and Health Genomics Chinese National Human Genome Center at Shanghai Shanghai 201203 China

The genetic requirements for the transcription of glnA,encoding the major glutaminesynthetase in a rifamycin SV-producing Amycolatopsis mediterranei strain,U32,were *** experiments showed that the promoter of U32 glnA （pglnA） was likely to have two transcriptioninitiation sites:P1and P2,located 157 and 45 nucleotides （nt） upstream of the translational start codon,*** mobility shift and DNase I footprinting analyses revealed a 30 bp cis-element locatedat 45 to 75 nt downstream of P1,or 38 to 68 nt upstream of *** sequence of the cis-element displayedhigh similarity to the corresponding regions of pglnA from Streptomyces coelicolor and *** as a reporter gene,the expression levels of U32 pglnA and its deletion derivatives under differentnitrogen-source conditions were analyzed by detecting the catechol dioxygenase activities in ***54,*** J508 and *** FS10 （glnR mutant）.These in vivo studies showed that theactivation of U32 pglnA in *** required GlnR,and its binding to the U32 pglnA was furtherconfirmed by the gel mobility shift *** and heterologous expression of the U32 glnR allowed usto detect the in vitro interaction between the U32 GlnR and the corresponding pglnA *** shown by in vivo glnR inactivation and complementation indicated that GlnR is essential for theactive transcription of glnA in U32.

关键词： glnA promoter cis-element glnR Amycolatopsis mediterranei

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Difference in oral absorption of ginsenoside Rg1 between in vitro and in vivo models

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Acta Pharmacologica Sinica 2006年第4期27卷 499-505页

作者： Min HAN Xiao-ling FANG~1 Department of Pharmaceutics,school of pharmacy.fudan university.shanghai 200032.china Department of Pharmaceutics School of Pharmacy Fudan University Shanghai China

Aim:To clarify the cause of poor oral absorption of ginsenoside Rg1(Rg1),theactive ingredient in Panax notoginseng saponins(PNS)used for ***:Caco-2 cell monolayers were used as an in vitro model tostudy the transport mechanism of Rg1across the intestinal ***,the serum concentration-time profiles after peroral(po),intraduodenal(id),portalvenous(pv)and tail venous(iv)administration of Rg1in rats were compared toevaluate the first-pass effects in the stomach,intestine,and ***:Up-take of Rg1by Caco-2 cell monolayers was temperature-dependent,but was notinfluenced by cyclosporin *** change in the apical pH produced no obviouseffect on the uptake of *** uptake and transport of Rg1was non-saturable;whereas the flux from the apical compartment to the basolateral compartment(A-B)increased in a linear manner with the increase in concentration,indicatingpassive *** apparent permeability coefficient of(2.59±0.17)×10-7cm/s(C0=1 mg/mL)predicted incomplete absorption.A significant difference was ob-served between the po(Fpowas 3.29% at a dose of 1500 mg/kg),id(Fidwas 6.60%at a dose of 1200 mg/kg)and pv(Fpvwas 50.56%)administration methods,and thebarrier function of the intestine was more significant than those of the stomachand liver in the absorption ***:Elimination in the stomach,largeintestine and liver contributed to the low oral bioavailability of Rg1,but low mem-brane permeability might be a more important factor in determining the extent ofabsorption.

关键词： ginsenoside Rgl Panax Caco-2 bioavailability pharmacokinetics

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Preparation of ion-activated in situ gel systems of scopolamine hydrobromide and evaluation of its antimotion sickness efficacy

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Acta Pharmacologica Sinica 2007年第4期28卷 584-590页

作者： Shi-lei CAO Qi-zhi ZHANG Xin-guo JIANG Department of Pharmaceutics,school of pharmacy,fudan university,shanghai 200032,china Department of Pharmaceutics School of Pharmacy Fudan University Shanghai China

Aim:To develop a novel,in situ gel system for nasal delivery of scopolaminehydrobromide (SCOP) and study its efficacy on motion ***:SCOPin situ gels at 0.2%,0.5%,and 1.0% gellan gum concentration (w/v) were prepared,respectively,and characterized in terms of viscosity,in vitro release,and *** photon emission computing tomography technique was usedto evaluate the nasal residence time of gel containing ~99mTc *** antimotionsickness efficacy produced by the in situ gel formulation was investigated in ratsand compared with those achieved after subcutaneous and oral ***:The viscosity of the gellan gum formulations either in solution or in gelincreased with increasing concentrations of gellan *** release in vitro wasmoderate in artificial nasal *** micrographic results showed that in situ gelswere safe,without nasal *** comparison with phosphate buffer saline,a prolonged radioactivity of99mTc in the rabbit nasal cavity was observed afteradministration of the gellan gum *** SCOP in situ gel at a doseof 100 pg/kg decreased symptoms of motion sickness significantly in comparisonwith subcutaneous and oral administration (P<0.01).Conclusion:SCOP nasal insitu gel is a safe and promising therapeutic alternative to existing medications formotion sickness.

关键词： scopolamine gellan gum nasal delivery motion sickness residence time nasal ciliotoxicity

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Artificial pulmonary surfactant as a carrier for intratracheally instilled insulin

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Acta Pharmacologica Sinica 2007年第5期28卷 744-750页

作者： Ying JI,Chen LIU,Yuan-ying PEI~2Department of Pharmaceuties,school of pharmacy,fudan university,shanghai 200032,china Department of Pharmaceutics School of Pharmacy Fudan University Shanghai China

Aim:The relative bioavailabilities and effects on lung injury alleviation of 4 insu-lin-artificial pulmonary surfactant (INS-APS) preparations were studied in *** relationship between the minimal surface tension (γmin) of INS-APS andthe absorption of insulin was also ***:Four formulations ofAPS[1,2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC)/lecithin/palmitic acid(PA),DPPC/1-hexadecanol (Hex)/tyloxapol (Tyl),DPPC/L-α-phosphatidyl-DL-glyc-erol sodium salt (PG),DPPC/Tyl]were prepared by thin-film sonication methodand direct *** γminof 4 APS dispersions was examined with andwithout INS by pulsating with a bubble surface *** vivo experimentswere performed in which serum glucose change and the insulin level were mea-sured by an enzymatic glucose reagent kit and a radioimmunology assay kit afterIT to *** reduction in lung injury by INS-APS following 7 d of consecutiveadministration was evaluated by the pulmonary edema index (the weight ratio ofwet lung to dry lung) and histopathology ***:The γminof allAPS dispersions were below 10 mN/*** was no significant difference (P>0.05) between the γ(min)of APS and the corresponding *** vivo experi-ments showed a significant glucose level decrease and insulin absorptionincrease (P0.05) between INS/DPPC/Tyl,INS/DPPC/PG,and the control *** pulmonary edema indices and histopatho-logical observation indicated that INS-APS could alleviate lung ***:The most potent hypoglycemic effect and insulin absorption increase in this studywere obtained with INS/DPPC/*** to the results,there was a linearcorrelation between the γminand relative bioavailability of INS-

关键词： pulmonary drug delivery system pharmacokinetics pharmacodynamics hypoglycemic effect minimal surface tension absorption pulmonary edema index histopathology examination

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Application of EGFP-EGF fusions to explore mechanism of endocytosis of epidermal growth factor

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Acta Pharmacologica Sinica 2007年第1期28卷 111-117页

作者： Hua JIANG~2 Jie ZHANG~(2,3) Bi-zhi SHI~(2,3) Yu-hong XU~3 Zong-hai LI~(2,3,4) Jian-ren GU~(2,3,4)2 State Key laboratory of Oncogenes and Related Genes,shanghai Cancer Institute,Medical College of fudan university 3 school of pharmacy,shanghai Jiaotong university,shanghai 200032,china State Key laboratory of Oncogenes and Related Genes Shanghai Cancer Institute Medical College of Fudan University Shanghai China school of pharmacy Shanghai Jiaotong University Shanghai China

Aim:To develop a simple method for monitoring protein localization of epidermalgrowth factor(EGF)in living ***:Enhanced green fluorescent protein(EGFP)was used as an autofluorescent tag to label EGF ***-PAGE andWestern blot analysis were used to detect the expression of the EGFP-tagged EGF(EGFP-EGF)*** cell-binding and internalization activity of EGFP-EGFwere analyzed by fluorescence-activated cell sorting(FACS)and confocal ***:EGFP-EGF protein was expressed in Escherichia coli and purified.A cell-binding assay demonstrated that the EGFP-EGF protein could bind effi-ciently to the cells expressing *** binding and internalization of EGFP-EGFcan be visualized even at a very low concentration under confocal *** FACS-based assay for internalization activity indicated the accumulation ofinternalized EGFP-EGF over ***,the results of the competitionassay indicated its EGFR binding *** such a method,it does notneed to label EGF with chemicals and avoid light in the experimental ***:The fusion protein EGFP-EGF has several characters including highsensitivity,stability and convenience for manipulation,and is a powerful tool forthe study of EGF endocytosis.

关键词： receptor epidermal growth factor endocytosis purification expression

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