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Anti-implantation effect of droloxifene in rats and its relationship with anti-estrogenic activity

Acta Pharmacologica Sinica 2005年第10期26卷 1243-1247页

作者： yong huang, yu shen, ying feng, lin cao, ying leng~2 shanghai institute of materia media, shanghai institute for biological sciences, chinese academy of sciences, graduate school of the chinese aeademy of sciences, shanghai 201203, china shanghai institute of materia media Shanghai Institute for Biological Sciences Chinese Academy of Sciences Graduate School of the Chinese Academy of Sciences Shanghai China

Aim: To investigate the anti-implantation effect of droloxifene and study the possible relationship between the anti-estrogenic activity of droloxifene and its antiimplantation effect. Methods: Pregnant rats were treated orally with droloxifene at 10:00 AM on d 2 at doses of 1.25-20 mg/kg to observe anti-implantation effects, and then doses of 14 mg/kg or 2.5 mg/kg were given at different time on d 2 to d 5 to determine the optimal administration time for anti-implantation effects. Pregnant rats were treated with a combination of droloxifene (2.5 mg/kg, ig) and E2 (0.5-8.0μg/kg, sc) on the optimal administration time to observe the antagonistic effect of external estrogen on the anti-implantation effect of droloxifene. Serum estrogen and progesterone levels were measured by carrying out radioimmunoas says on d 1 to d 6 in droloxifene-treated and control rats to determine the surge time for nidatory estrogen and the effect of droloxifene on ovary function. Results: Droloxifene has anti-implantation effects in rats. The optimal oral administration time was at 22:00 PM on d 4, which was after the surge time for nidatory estrogen (on d 4 at 10:00 AM). This suggests that the anti-implantation effect of droloxifene is not attributable to antagonism of the surge in secretion of nidatory estrogen. External estrogen did not antagonize the anti-implantation effect of droloxifene. Droloxifene had no effect on the serum levels of estrogen and progesterone on d 5 or d 6 when administered on d 4 at 22:00 PM. Conclusion: Droloxifene has an anti-implantation effect in rats, and the effect appears to be not completely due to its anti-estrogenic activity.

关键词： 3-hydroxytamoxifen implantation estrogen progesterone rats

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Development of a complex scintillation proximity assay for highthroughput screening of PPAR7 modulators

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Acta Pharmacologica Sinica 2005年第3期26卷 339-344页

作者： Bin WU Jie GAO Ming-wei WANG~2 The National Center for Drug Screening,shanghai institute of materia Medica,shanghai institutes for biological sciences,chinese academy of sciences graduate school of chinese academy of sciences,shanghai 201203,china The National Center for Drug Screening Shanghai Institute of Materia Medica Shanghai Institutes for Biological Sciences Chinese Academy of Sciences graduate school of chinese academy of sciences Shanghai China

Aim:To develop a complex high-throughput screening （HTS） assay based onscintillation proximity assay （SPA） technology for identification of novel peroxi-some proliferator-activated receptor gamma （PPARγ） ***:Full-length PPARγ and retinoid X receptor alpha （RXRα）,biotinylated PPAR responseelement （PPRE）,[3H]BRL49653 and streptavidin-coated FlashPlate or microbeadwere used to develop an HTS assay based on SPA ***‘ABCDE’method was validated against conventional hydroxyapatite （HA） assay and ap-plied to large-scale screening of 16 000 synthetic compounds and natural ***:（1） IC50values of positive control compounds （BRL49653 andtroglitazone） obtained from the‘ABCDE’method and HA assay were compa-rable and consistent with those reported elsewhere;（2） Approximately 178compounds,showing more than 70% competitive inhibition on BRL49653 bind-ing to PPARγ,were identified initially by the‘ABCDE’method （microbead）;（3）Secondary screening using FlashPlate and cross-reactivity studies with RARα,β,γ and RXRα,β,γ confirmed that 12 compounds possessed specific PPARγ bind-ing properties including 2 with IC50values less than 0.5 μmol/L and novel chemi-cal ***:The‘ABCDE’method using either FlashPlate ormicrobead,is a highly efficient,automatable,and robust tool to screen potentialPPARγ modulators in HTS *** application may be expanded to othernuclear receptors that form heterodimers upon activation.

关键词： peroxisome proliferator-activated receptor gamma retinoid X receptor alpha scintillation proximity assay high-throughput screening

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Comparative studies of huperzine A,donepezil,and rivastigmine on brain acetylcholine,dopamine,norepinephrine,and 5-hydroxytryptamine lev-els in freely-moving rats

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Acta Pharmacologica Sinica 2006年第9期27卷 1127-1136页

作者： Yan-qi LIANG Xi-can TANG~2 State Key Laboratory of Drug Research,shanghai institute of materia Medica,shanghai Instituties for biological sciences,graduate school of the chinese academy of sciences,chinese academy of sciences,shanghai 201203.china State Key Laboratory of Drug Research Shanghai Institute of Materia Medica Shanghai Instituties for Biological Sciences Graduate School of the Chinese Academy of Sciences Chinese Academy of Sciences Shanghai China

Aim:To assess the effects of cholinesterase inhibitors huperzine A,donepeziland rivastigmine on cerebral neurotransmitters in the cortex and hippocampus infreely-moving ***:Double-probe cerebral microdialysis and HPLC withelectrochemical detection were used to detect ***:Ourresults showed that huperzine A(0.***.0.5,and 0.75μmol/kg,po)dose-depen-dently elevated extracellular acetylcholine(ACh)levels in the medial prefrontalcortex(mPFC)and *** administration of donepezil(5.4μmol/kg)orrivastigmine(1μmol/kg)also elicited significant increases in ACh in the mPFC *** time course of cortical acetylcholinesterase(ACHE)inhibitionwith the 3 inhibitors minored the increases of ACh at the same *** markedelevation of ACh after oral administration of huperzine A(0.5μmol/kg)anddonepezil(5.4μmol/kg)was associated with a significantly increased release ofdopamine(DA)in the mPFC or *** of the 3 inhibitors affectednorepinephrine(NE)and 5-hydroxytryptamine(5-HT)levels in the mPFC *** effects of huperzine A and rivastigmine did not depend on theroute of administration,but donepezil was less efficacious by the oral route thanby ip *** ability of huperzine A to increase ACh levels was unchangedwhen tests were performed after multiple oral administration of the drug at 0.5μmol/kg,once per day for 30 ***:The present findings showed that,inmolar terms,huperzine A had similar potency on increasing mPFC ACh and DAlevels as compared to the 11-and 2-fold dosages of donepezil and rivastigmine,respectively,and had longer lasting effects after oral dosing.

关键词： huperzine A donepezil rivastigmine acetylcholine dopamine norepinephrine 5-hydroxy tryptamine Alzheimer’s disease rats

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Neuroprotective effects of cyclooxygenase-2 inhibitor celecoxib against toxicity of LPS-stimulated macrophages toward motor neurons

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Acta Pharmacologica Sinica 2005年第8期26卷 952-958页

作者： yong huang, Jing LIU, Li-zhen WANG, Wei-yu ZHANG, Xing-zu ZHU~1 Department of Pharmacology, shanghai institute of materia Medica, shanghai institutes for biological sciences, chinese academy of sciences, graduate school of chinese academy of sciences, shanghai 201203, china Department of Pharmacology Shanghai Institute of Materia Medica Shanghai Institutes for Biological Sciences Chinese Academy of Sciences Graduate School of Chinese Academy of Sciences Shanghai China

Aim: To establish an in vitro injured motor neuronal model and investigate the neuroprotective effects and possible mechanism of celecoxib, a selective cyclooxygenase-2 (COX-2) inhibitor, on this model. Methods: After macrophages were stimulated with lipopolysaccharide (LPS)+interferon-γ(IFN-γ) in the pre-sence or absence of celecoxib for 24 h, the cell-free supernatant of LPS-stimulated macrophages was transferred to the culture of NSC34 cells. Viability of NSC34 cells was assessed by MTT assay after a further 24 h and 72 h incubation. After macrophages were stimulated by LPS+IFN-γ for 12 h or 24h, the release of pros-taglandin E2(PGE2), nitric oxide (NO), reactive oxygen species (ROS), tumor necro-sis factor α(TNF-α) and interleukin-1β (IL-1β) from macrophages was measured by radioimmunoassay, Griess assay, fluorescence assay and enzyme-linked immunosorbent assay, respectively. The mRNA levels of COX-2, inducible nitric oxide synthase (iNOS), TNF-α and IL-1β in macrophages were determined by reverse transcription-polymerase chain reaction after macrophages were stimu-lated for 6 h and 12 h. Results: The supernatant of LPS-stimulated mouse mac-rophages induced the death of NSC34 cells and celecoxib protected the NSC34cells against this toxicity. The LPS-induced increases in the release of PGE2, NO,TNF-α and IL-1β from macrophages were attenuated by pre-treatment with celecoxib. However, celecoxib showed no effect on the ROS levels upregulated by LPS+IFN-γin the macrophage supernatant. The mRNA levels of COX-2, iNOS, TNF-α and IL-1β were increased in LPS-activated macrophages and, except COX-2, reduced by pre-treatment with celecoxib. Conclusion: An in vitro injured motor neuronal model was established by using the toxicity of LPS-stimulated mouse macrophages toward motor neuronal NSC34 cells. In this model, celecoxib exerted neuroprotective effects on motor neurons via an inhibition of the neurotoxic secretions from activated macrophages.

关键词： amyotrophic lateral sclerosis celecoxib macrophage NSC34 cell lipopolysaccharide cyclooxygenase-2 prostaglandin E2 nitric oxide reactive oxygen species

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Magnesium lithospermate B ameliorates renal cortical microperfusion in rats

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Acta Pharmacologica Sinica 2006年第2期27卷 217-222页

作者： Chun-guang CHEN~(2,3) Yi-ping WANG~(2,4) ~2State Key Laboratory of Drug Research.shanghai institute of materia Medica,shanghai institutes for biological sciences graduate school of the chinese academy of sciences,chinese academy of sciences,shanghai 201203,china State Key Laboratory of Drug Research Shanghai Institute of Materia Medica Shanghai Institutes for Biological Sciences Shanghai China graduate school of the chinese academy of sciences Chinese Academy of Sciences Shanghai China

Aim:To investigate the effects of magnesium lithospermate B（MLB）isolatedfrom Salviae miltiorrhizae on renal microcirculation,and renal and systemic he-modynamics in Sprague-Dawley ***:MLB（10,30,and 60 mg/kg）wasinjected intravenously and renal blood flow（RBF）,renal cortical microperfusion（RCM）,and systemic hemodynamic function parameters including heart rate（HR）,mean arterial pressure（MAP）,left ventricular systolic pressure（LVSP）,left ven-tricular end-diastolic pressure（LVEDP）,and maximal velocity of pressure increase(dp/dtmax)were measured for 45 min after ***:IntravenousMLB at doses of 10,30,and 60 mg/kg increased RCM significantly,but had noobvious effects on RBF or systemic *** effect of MLB on RCMreached its peak 15 rain after injection and returned to baseline after 45 *** to60 mg/kg MLB increased RCM by 62.4%±20.2%（changes from baseline,Pline）and renal vascular resistance（-1.4%±9.1%vs baseline）did not obviously ***:These results indicate thatMLB ameliorates renal microcirculation in a dose-dependent manner,which maybe related to the renoprotective effects of MLB.

关键词： magnesium lithospermate B hemodynamics renal blood flow renal cortical microperfusion

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Expression and purification of lipoprotein-associated phospholipase A2,a key enzyme involved in atherosclerosis

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Acta Pharmacologica Sinica 2006年第6期27卷 679-684页

作者： Fu-jun ZHANG~(2,4)Mao-jun CAI~3 Jing-kang shen~3 Yi-ping WANG~(2,5)2 State Key Laboratory of Drug Research.3 Department of Medicinal Chemistry,shanghai institute of materia Medica,shanghai institutes for biological sciences,chinese academy of sciences.shanghai 201203,china 4 graduate school of the chinese academy of sciences.chinese academy of sciences,shanghai 201203.china State Key Laboratory of Drug Research Chinese Academy of Sciences Shanghai China graduate school of the chinese academy of sciences Chinese Academy of Sciences Shanghai China Department of Medicinal Chemistry Shanghai Institute of Materia Medica Shanghai Institutes for Biological Sciences Chinese Academy of Sciences Shanghai China

Aim:To express and purify lipoprotein-associated phospholipase A2（Lp-PLA2）,and to establish a screening model for Lp-PLA2inhibitors using the expressed Lp-PLA2,Methods:We cloned the full-length cDNA of Lp-PLA2 from differentiatedTHP-I cells,and subcloned the cDNA into the baculovirus transfer *** addition,we introduced an N-terminal Kozak sequence for high-level translation initiation and a C-terminal sequence of 6 histidine residues forpurification,The fusion enzyme was expressed in Sf9 insect cells and purified byNi2+affinity *** Lp-PLA2activity was measured us-ing[3H]PAF as a substrate,and we examined the enzyme activity of recombinantLp-PLA2pretreated with the known Lp-PLA2inhibitor ***:Wesuccessfully cloned the full-length Lp-PLA2gene from differentiated THP-1 *** fusion enzyme was expressed in Sf9 insect cells at a high level and purifiedefficiently through a 2-step *** recombinant Lp-PLA2activity wasmeasured using[3H]PAF as a substrate,and proved to be enzymatically ***-PLA2inhibitor SB435495 produced a good inhibition curve for inhibition ofrecombinant Lp-PLA2with an IC50of 57±1μmol/***:We expressed andpurified Lp-PLA2at a high level in insect cell-baculovirus expression *** ratio was much greater than that obtained from human plasma and we estab-lished a screening model for Lp-PLA2inhibitors using the expressed Lp-PLA2.

关键词： lipoprotein-associated phospholipase A2 atherosclerosis coronary heart diseases cloning baculovirus purification

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Effect of leukemia inhibitory factor on embryonic stem cell differentiation:implications for supporting neuronal differentiation

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Acta Pharmacologica Sinica 2006年第1期27卷 80-90页

作者： Zhao HE~(2,3) Jing-jing LI~(2,3) Chang-hong ZHEN~(3,4) lin-ying feng~3 Xiao-yan DING~(2,5)2 Laboratory of Molecular and Cell Biology and Laboratory of Stem Cell Biology,institute of Biochemistry and Cell Biology:shanghai institutes for biological sciences,chinese academy of sciences,shanghai 200031,china 3 shanghai institute of materia Medica.chinese academy of sciences.shanghai 201203,china 4 graduate school of the chinese academy of sciences,shanghai 200031,china. Laboratory of Molecular and Cell Biology and Laboratory of Stem Cell Biology Institute of Biochemistry and Cell Biology shanghai institutes for biological sciences Chinese Academy of Sciences Shanghai China shanghai institute of materia Medica Chinese Academy of Sciences Shanghai China graduate school of the chinese academy of sciences Shanghai China

Aim:Leukemia inhibitory factor (LIF),a pleiotropic cytokine,has been used ex-tensively in the maintenance of mouse embryonic stem cell *** thiscurrent work,we examined the effect of the LIF signaling pathway in embryonicstem (ES) cell differentiation to a neural ***:In the presence of LIF(1000U/mL),the production of neuronal cells derived from embryoid bodies (EB)was tested under various culture *** of the LIF pathway wasexamined with specific *** effects of cell apoptosis and proliferationon neural differentiation were *** cell differentiation into three-germlayers was ***:Under various culture conditions,neuronal differ-entiation was increased in the presence of *** the LIF-activated STAT3signaling pathway with specific inhibitors abolished the neuronal differentiationof ES cells,whereas inhibition of the LIF-activated MEK signaling pathway im-paired the differentiation of ES cells toward a glial *** suppressed cellapoptosis and promoted cell proliferation during ES cell *** inhib-ited the differentiation of ES cells to both mesoderm and extraembryonic endo-derm fates,but enhanced the determination of neural ***:These results suggest that LIF plays a positive role during the differentiation ofES cells into neuronal cells.

关键词： leukemia inhibitory factor embryonic stem cells neural fate embryoid bodies

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The cDNA and Genomic DNA Organization of a Novel Toxin SHT-I from Spider Ornithoctonus huwena

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Acta Biochimica et Biophysica Sinica 2004年第10期36卷 656-660页

作者： Peng QIAO, Xiao-Pan ZUO, Zhi-Fang CHAI, and yong-Hua JI* institute of Physiology, shanghai institutes for biological sciences, chinese academy of sciences, graduate school of the chinese academy of sciences, shanghai 200031, china institute of Physiology Shanghai Institutes for Biological Sciences Chinese Academy of Sciences Graduate School of the Chinese Academy of SciencesShanghai 200031 China

In present study the full-length cDNA of a novel toxin from the venom gland of spider Ornithoctonus huwena, named as SHT-I, has been cloned using the strategy of rapid amplification of cDNA ends, and then the whole genomic sequence of SHT-I (Selenocosmia huwena toxin-I) was determined using sequence-specific primers synthesized based on the acquired 3’ and 5’ ends of SHT-I cDNA sequence. It is unexpectedly found that intron was lacking in the genomic sequence of SHT-I. The result might evoke an interesting question whether the gene code of inhibitor cystine-knot peptides from spider venom is distinct from that of those known toxic peptides of scorpion and cone snail.

关键词： Ornithoctonus huwena spider cDNA genomic DNA peptide toxin ICK motif

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In Vitro Reassembly of Tobacco Ribulose-1,5-bisphosphate Carboxylase/Oxygenase from Fully Denatured Subunits

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Acta Biochimica et Biophysica Sinica 2006年第10期38卷 737-745页

作者： Zhen-Hua yong Gen-yun CHEN* Jiao-Nai SHI Da-Quan XU institute of Plant Physiology and Ecology,shanghai institutes for biological sciences,chinese academy of sciences,and graduate school of the chinese academy of sciences,shanghai 200032,china institute of Plant Physiology and Ecology Shanghai Institutes for Biological Sciences Chinese Academy of Sciences and Graduate School of the Chinese Academy of SciencesShanghai 200032 China

It has been generally proved impossible to reassemble ribulose-1,5-bisphosphate carboxylase/oxygenase （Rubisco） from fully denatured subunits in vitro in higher plant,because large subunit of fullydenatured Rubisco is liable to precipitate when the denaturant is removed by common methods of directdilution and one-step *** our experiment,the problem of precipitation was resolved by an improvedgradual dialysis method,which gradually decreased the concentration of ***,fully denaturedRubisco subunits still could not be reassembled into holoenzyme using gradual dialysis unless chaperonin 60was *** restored activity of reassembled Rubisco was approximately 8% of natural *** of reassembled Rubisco increased greatly when heat shock protein 70 was present in the *** and Mg2+ were unnecessary for in vitro reassembly of Rubisco,and Mg2+ inhibited the *** reassembly was weakened when ATP,Mg2+ and K+ existed together in the reassembly process.

关键词： Rubisco reassembly gradual dialysis chaperonin 60 Hsp70

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Positive Charges on Lysine Residues of the Extrinsic 18 kDa Protein Are Important to Its Electrostatic Interaction with Spinach Photosystem Ⅱ Membranes

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Acta Biochimica et Biophysica Sinica 2005年第11期37卷 737-742页

作者： Jin-Peng GAO Zhen-Hua yong feng ZHANG Kang-Cheng RUAN Chun-He XU Gen-yun CHEN institute of Plant Physiology & Ecology.shanghai institutes for biological sciences,chinese academy of sciences,shanghai 200032,china Laboratory of Proteomics,institute of Biochemistry and Cell Biology,shanghai institutes for biological sciences,chinese academy of sciences,shanghai 200031,china College of sciences,Zhejiang University.Hangzhou 310029,china graduate school of the chinese academy of sciences,shanghai 200032,china institute of Plant Physiology & Ecology Shanghai Institutes for Biological Sciences Chinese Academy of SciencesShanghai 200032 China graduate school of the chinese academy of sciencesshanghai 200032 China College of sciences Zhejiang UniversityHangzhou 310029 China Laboratory of Proteomics Institute of Biochemistry and Cell Biology Shanghai Institutes for Biological Sciences Chinese Academy of SciencesShanghai 200031 China

To determine the contribution of charged amino acids to binding with the photosystem Ⅱcomplex(PSⅡ),the amino or carboxyl groups of the extrinsic 18 kDa protein were modified with N-succinimidyl propionate(NSP)or glycine methyl ester(GME)in the presence of a water-soluble carbodiimide,*** on isoelectric point shift,4-10 and 10-14 amino groups were modified in the presence of2 and 4 mM NSP,***,3-4 carboxyl groups were modified by reaction with *** of negatively charged carboxyl groups with GME did not alter the binding activity of theextrinsic 18 kDa ***,the NSP-modified 18 kDa protein,in which the positively charged aminogroups had been modified to uncharged methyl esters,failed to bind with the PSⅡ membrane in the presenceof the extrinsic 23 kDa *** defect can not be attributed to structural or conformational alterationsimposed by chemical modification,as the fluorescence and circular dichroism spectra among native,GME-and NSP-modified extrinsic 18 kDa proteins were ***,we have concluded that the positive chargesof lysyl residues in the extrinsic 18 kDa protein are important for its interaction with PSⅡ membranes in thepresence of the extrinsic 23 kDa ***,it was found that the negative charges of carboxylgroups of this protein did not participate in binding with the extrinsic 23 kDa protein associated with PSⅡmembranes.

关键词： extrinsic 18 kDa protein circular dichroism electrostatic interaction chemical modification

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