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Insulin-sensitizing effects of a novel α-methyl-α-phenoxylpropionate derivative in vitro

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Acta Pharmacologica Sinica 2007年第3期28卷 417-422页

作者： Hao-shu WU~(2,4) Juan-hong yu~(3,4) Ying-yin li~2 yu-she YANG~3 Qiao-jun HE~2 Yi-jia LOU~(2,5) Ru-yun JI~3 ~2Department of Pharmacology and Toxicology,College of Pharmaceutical sciences,Zhejiang University,Hangzhou 310058,china ~3State Key Laboratory of Drug Research,shanghai institute of materia medica,shanghai institutes for Biological sciences,Graduate School of the chinese academy of sciences,shanghai 201203,china Department of Pharmacology and Toxicology College of Pharmaceutical Sciences Zhejiang University Hangzhou 310058 China Department of State Key Laboratory of Drug Research Shanghai Institute of Materia Medica Shanghai Institutes for Biological Sciences Graduate School of the Chinese Academy of Sciences Shanghai 201203 China

Aim:To examine the insulin sensitizing effects of a novel α-methyl-α-phenoxylpropionate derivative YY20 in insulin-sensitive cell ***:Theperoxisome proliferator-activated receptor γ（PPARγ）agonist bioactivities of YY20were detected by a preadipocyte differentiation ***-PCR and Westernblotting analysis were used to detect the expression of the target gene or *** effects of YY20 on insulin-mediated glucose consumption were determined inthe HepG2 human hepatocellular carcinoma ***:YY20 could enhancethe differentiation of preadipocytes to adipocytes and upregulate the gene ex-pression of PPARγ2,as well as the protein expression of insulin receptor sub-strate-1（IRS-1）,glucose transporter-4（GLUT4）,and adiponectin（ACRP30）.Theeffects on GLUT4 and ACRP30 could be reversed by the PPARγ inhibitor ***,YY20 efficiently reduced glucose consumptions in HepG2 cells after24 h culture,and the effects were related to insulin and YY20 ***:YY20,a potential insulin-sensitizing agent like rosiglitazone,couldenhance glucose consumption in HepG2 cells in a concentration-and insulin-dependent *** may improve the insulin resistance associated with type 2diabetes.

关键词： YY20 peroxisome proliferator-activated receptor y insulin sensitivity glucose consumption

Effects of bilobalide on interleukin-1, tumor necrosis factor-α and nitric oxide production by rat microglia stimulated with lipopolysaccharides in vitro

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Acta Pharmacologica Sinica 1999年第5期 95-96页

作者： DU Ze-Ying, li Xiao-yu(shanghai institute of materia medica, chinese academy ofsciences, shanghai 200031, china)

The effects of bilobalide,a sesquiterpene isolated from Ginkgo biloba, on interelukin-1 (IL-l), tumor necrosis factor-α(TNF-α) and nitric oxide (NO) production in resting and lipopolysaccharide (LPS )-stimulated cultured neonatal rat microglia were studied. Apafant, a platelet activating factor (PAF) antagonist of triazolobenzodiazepine type was ttsed as *** biological activities of IL-1 and TNFαwere tested

关键词： TNF Effects of bilobalide on interleukin-1 and nitric oxide production by rat microglia stimulated with lipopolysaccharides in vitro tumor necrosis factor

Morphine - a Diphasic immunomodifier

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Acta Pharmacologica Sinica 1999年第5期 75-76页

作者： li Xiao-yu, BIAN Tong-Hua(shanghai institute of materia medica, chinese academy ofsciences, shanghai 200031, china)

The central and peripheral neuroimmunomodulating effects of morphine were studied in our laboratory through the following aspects:(1) By giving different doses of morphine and its addiction on mouse and determining T-,B-lymphocyte proliferation and cytokine production; (2) The direct effects of serial concentrations of morphine on the responses of immune competent cells and cytokine production in vitro; (3) By using of microinjection of morphine into rat periaqueductal gray (PAG), the possible central regulating actions on immune responses of morphine were observed. (1) ip Morphine more than 5 mg·kg-1. d-1for 7 d caused addiction in mice while only higher doses of morphine (40, 100

关键词： a Diphasic immunomodifier Morphine PAG

Pharmacokinetics of magnesium lithospermate B after intravenous administration in beagle dogs

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Acta Pharmacologica Sinica 2004年第11期 18-23页

作者： Xiao-chuan li, Chen yu, Wei-kang SUN, Gang-yi liU, Jing-ying JIA, Yi-ping WANGDepartment of Pharmacology, shanghai institute of materia medica, shanghai institutes for Biological sciences, chinese academy of sciences, shanghai 201203 Central Laboratory, shanghai Xuhui Central Hospital, shanghai 200002, china

AIM: To develop a specific liquid chromatography-tandem mass spectrometry (LC-MS/MS) method for the phar-macokinetic study of magnesium lithospermate B (MLB), and study the pharmacokinetics of MLB after iv administration in beagle dogs. METHODS: Each beagle dog was iv administered MLB 3, 6, and 12 mg/kg random. The serum drug concentration was determined by specific liquid chromatography-tandem mass spectrometry (LC-MS/ MS) assays. The pharmacokinetic parameters were calculated by Drug and Statistics version 1.0 program. RESULTS: The calibration curve for MLB was linear over a range of 16-4096μg/L with coefficients of correlation >0.999. The intra- and inter-day precisions (CV) of analysis were <10 %, and accuracy ranged from 90 % to 113 %. After iv administration of MLB at the doses of 3, 6, and 12 mg/kg, the C0 values for MLB were estimated to be of 24, 47, and 107 mg/L, respectively. The AUC increased with the increasing doses for iv administration, and the mean AUC0-t values were 109.3, 247.9, and 5

关键词： Salvia miltiorrhiza magnesium lithospermate B pharmacokinetics liquid phromatography-tandem mass spectrometry

Synthesis, Characterization and Antitumor Activities of Co, Ni, Cu, Zn Complexes with 1,4,7,10-tetrakis(4-nitrobenzyl)-1,4,7,10 tetraazacyclododecane Macrocyclic ligand

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chinese Journal of Structural Chemistry 2000年第1期19卷 39-47页

作者： KONG De\|yuan a* \ XIE yu\|li a\ XIE yu\|yuan a\ HUANG Xiao\|Ying ba (shanghai institute of materia medica, the chinese academy of sciences, Taiyuan Road 294, shanghai, 200031, P. R. china) b (Department of Chemistry, Rugters University, New Jer 中科院上海药物所上海 2 0 0 0 31 Rugters University 美国 New Jersey 08102

New tetraazamacrocyclic ligand with 1,4,7,10 tetrakis(4 nitrobenzyl) pendent groups (C 36 H 40 N 8O 8, M r =712.76) crystallized in the monoclinic system, P2 1/n space group with unit cell parameters: a=7.834(2), b=22.902(6), c=10\^147(3), β=106.53(2)°, V=1745(1) 3, Z=2, D c =1.356 g/cm 3, λ (Mo Kα )=0.71069; μ =0.92cm -1 , F(000)=752, T =296K. The final R and R w values are 0\^065 and 0.066, respectively. The Cu(Ⅱ), Ni(Ⅱ), Co(Ⅱ), Zn(Ⅱ) complexes with this new ligand have been synthesized and characterized by elemental analyses, IR, UV, ESI MS and molar conductance. The macrocyclic ligand molecular structure is centrosymmetrical. All complexes are in accordance with the general formula: M(L)(NO 3) 2·nH 2O (M=Co, Ni, Cu, n=2; M=Zn, n=4; L=C 36 H 40 \|N 8O 8). The central metal ions coordinate to four nitrogen atoms of azamacrocycle and two oxygen atoms of one nitrate ion. Preliminary pharmacological tests against P 388 and A 549 tumor cell lines showed that all these complexes had considerable activities in vitro.

关键词： synthesis macrocyclic ligand antitumor activity crystal structure

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 201203 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

Magnesium lithospermate B ameliorates microcirculation perfusion in rats by promoting vascular NO production via activating the PI3K/AKT pathway

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Acta Pharmacologica Sinica 2019年第8期40卷 1010-1018页

作者： Ying-luo liu Xiao-yu Zhou li-jiang Xuan State Key Laboratory of Drug Research Shanghai Institute of Materia Medica School of Pharmacy University of Chinese Academy of Sciences

Microcirculation morphologically refers to the blood flow in vessels of less than 150 pm in diameter,including arterioles,capillaries and venules,which provides nutrients and removes metabolic byproducts within *** dysfunction is involved in the pathological progress of many diseases,such as obesity,hypertension,and insulin *** this study we investigated the effects of magnesium lithospermate B(MLB), an active compound of the traditional chinese medicine Slavia miltiorrhiza,on the microcirculation dysfunction in rats and the underlying molecular *** effects of MLB on microcirculation were assessed in vivo by measuring the hindlimb blood perfusion in dextran-induced microcirculation dysfunction rats and mesentery blood flow in anesthetized *** demonstrated that administration of MLB restored the impaired rat hindlimb blood flow and promoted the mesenteric micoperfusion in *** further revealed in these two animal models that MLB treatment significantly increased the production of total nitrite in vascular tissues(mesentery,aorta,and heart),which was confirmed in human microvascular endothelial cells(HMEC-1)treated with MLB in ***,we showed that MLB treatment significantly increased the phosphorylation of endothelium nitric oxide synthase(eNOS)via inducing AKT phosphorylation in vivo and in ***-administration of the eNOS inhibitor L-NAME(20 mg/kg)abolished the protective effects of MLB against dextran-induced microcirculation dysfunction in rats,whereas pretreatment with PI3K inhibitor LY294002(10 μM)prevented eNOS activation in MLBtreated HMEC-1 *** results suggest that MLB can restore the microcirculation dysfunction via activating eNOS,and in turn enhancing the vascular nitric oxide production,which is medicated by MLB-caused activation of the PI3K/AKT pathway.

关键词： traditional chinese medicine Salvia miltiorrhiza magnesium lithospermate B microcirculation dysfunction NO endothelium nitric oxide synthase PI3K/AKT pathway

Design,synthesis,and anti-inflammatory evaluation of a series of novel amino acid-binding 1,5-diarylpyrazole derivatives

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Acta Pharmacologica Sinica 2005年第7期26卷 865-872页

作者： Ming-hui li lin-lin YIN Mao-jun CAI Wei-yu ZHANG yue HUANG Xin WANG Xing-zu ZHU~1 Jing-kang SHEN~1 State Key Laboratory of Drug Research,shanghai institute of materia medica,shanghai institutes for Biological sciences,chinese academy of sciences,Graduate School of the chinese academy of sciences,shanghai 201203,china State Key Laboratory of Drug Research Shanghai Institute of Materia Medica Shanghai Institutes for Biological Sciences Chinese Academy of Sciences Graduate School of the Chinese Academy of Sciences Shanghai 201203 China

Aim:To design and synthesize a series of novel amino acid-binding 1,5-diarylpyrazole derivatives,which are intended to act as prodrugs with better aque-ous solubility than celecoxib,and which will exert potent anti-inflammatory activi-ties after being converted to their parent compounds in ***:To intro-duce an amino acid,celecoxib analogs containing amino or methylamino groupwere synthesized first through multi-step chemical *** the synthesizedcompounds were screened in an intact cell-based assay in vitro and in carrag-eenan-induced mouse paw edema in *** active compounds were selectedfor further evaluation in a carrageenan-induced rat paw edema *** prelimi-nary pharmacokinetics experiments were conducted using high performance liq-uid chromatography/mass spectrometry(HPLC/MS).Results:Celecoxib,6 of the1,5-diarylpyrazole class of celecoxib analogs,and their amino acid derivatives(hydrochloride salts)were *** vitro screening,the hydrochloridesalts showed decreased inhibitory effects on cyclooxygenase(COX)-1 and COX-2 compared with their parent compounds,but some exhibited potent anti-inflam-matory activity in *** 4a was selected for further evaluation,and itsanti-inflammatory effect was equivalent to that of celecoxib after oral administra-tion in the carrageenan-induced rat paw edema *** three doses(25 mg/kg,50 mg/kg,and 100 mg/kg)the percentage inhibition on edema was 20.7%,52.6%,and 62.6%(for compound 4a)and 27.8%,38.4%,and 40.1%(for celecoxib),*** pharmacokinetic evaluations support the hypothesisthat compound 4a was actually converted to its parent compound,compound ***:The compound bound with amino acid acts like prodrug,which canexert anti-inflammatory effect similar to celecoxib after being converted to its par-ent *** finding will be of great benefit in carrying out structuralmodifications of prodrug-like selective COX-2 inhibitors.

关键词： nonsteroidal anti-inflammatory agents cyclo oxygenase inhibitors celecoxib pyrazole sulfonamide prodrugs

STRUCTURAL　ELUCIDATION　AND　SYNTHESIS　OF　ASTERBATANOSIDE　A　FROM　ASTER　BATANFENSIS

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chinese Chemical Letters 1994年第8期5卷 675-678页

作者： yu SHAO yun Long li and Bing Nan ZHOU(shanghai institute of materia medica,Academia sinica shanghai 200031)

A new p-acetylphenyl glycoside,asterbatanoside A has been isolated from the roots of Aster batangensis, and its structure has been elucidated as p-hydroxyacetophenone- -O-α-D-xylopyranosyl-(1,6) -β-D-glucopyranoside by chemical and spectral *** the confirmation of this structure. the synthesis of this compound was also reported in this paper.

关键词： ASTERBATANOSIDE SYNTHESIS BATANFENSIS ELUCIDATION FROM OF AND

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