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In vitro studies on anti-influenza viral effect and anti-inflammation of flavonoid derivatives

In vitro studies on anti-influenza viral effect and anti-inf...

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第二届世界天然药物和传统药物药理学学术会议

作者： Mian ZU~1,Wei-Ling ZHOU~1,Ai-Lin LIU~(1,2*),Guan-Hua DU~(1,2*) (1.Institute of Materia Medica,Chinese Academy of Medical Sciences & Peking Union Medical College,Beijing 100050,China 2.Beijing Key Laboratory of Drug Target and Screening Research,Beijing 100050,China)

AIM Influenza A virus(IAV) resistance to available antiviral agents urges us to discover new *** flavonoids have been reported for their antiviral *** this paper,the anti-influenza viral and anti-inflammatory effects of a series of synthesized flavonoid derivatives were *** The cellular protective effects of the flavonoid derivatives were evaluated by cytopathic effect(CPE) *** direct antiviral replication effects of "Hits" were studied by neuraminidase(NA) activity reduction assay,a real-time quantitative PCR assay for the intracellular gene expression of viral haemagglutination(HA),and an immunofluorescence assay for the intracellular protein expression of viral NP and ***,their inhibitory effects on the production of proinflammatory cytokines induced by influenza infection were *** More than 100 synthesized flavonoid derivatives were evaluated,J27113 and J27116 from these compounds exhibited the most protective effects in the CPE reduction *** Inhibited the NA activity,and decreased HA gene and NP,M2 protein ***,they showed inhibitory effects on the production of IL-6,IL-8,MCP-1 and *** The inhibition on the replication of influenza virus and their antiinflammatory effects of J27113 and J27116 may be considered as the major components for their cellular protective effects against influenza, which will provide information for novel antiviral drug development.

关键词： antiviral anti-inflammatory influenza flavonoid derivatives

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Perspectives and challenges of traditional Chinese medicines pharmaceutical businesses in Africa

Perspectives and challenges of traditional Chinese medicines...

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第二届世界天然药物和传统药物药理学学术会议

作者： Ernest TAMBO Jean Rousseau DJOUAKA Olalubi OLUWASOGO Ngouakam HERMAN National Institute for Parasitic Diseases Chinese Center for Disease Control and PreventionShanghaiChina Entomology & Pathology Unit International Institute of Tropical AgricultureCalaviRepublic of Benin

AIM To evaluate the perspectives of Traditional Chinese Medicines(TCM) pharmaceutical businesses in Africa continent with the increasing Sino-Africa *** AND METHODS Reviewed publications,Sino-Africa forum proceedings, papers and internet search data from 2001- end 2011 on Sino-Africa cooperation impact on TCM pharmaceutical businesses on healthcare services delivery across *** Similarities in the holistic healing,interconnectness and harmony with the universe of both continents allow successfully acceptability of TCM in the Africa community and have created an unprecedented TCM market reaching US＄100.000 millions in value,*** mounting pressure of population growth makes Africa,the second populous continent after Asia by 2025,coupled with implementation of the health integrated approach with Traditional medicine in diseases management in national health program,increasingly health demands and drugs shortages offer untapped and great opportunities for TCM pharmaceutical markets,which are more *** had acceptability of 81%and of good preventive effect(89%) on the high prevalence hypertension,diabetes and tropical *** findings documented that the disease severity in Africa patients was part consequence of the hihher cost of western medicines and medical *** Practitioner's foreign language proficiency eases local integration and adaptation and understanding of the therapeutic options as firms promote brand building strategy and *** Official incorporated of TCM into the primary health care delivery in whole of Africa by increasing investment flows is urgently needed. The perspectives and challenges of TCM pharmaceutical industries are enlisted in enhancing TCM exportation.

关键词： Perspectives and challenges of traditional Chinese medicines pharmaceutical businesses in Africa

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Alterations in the intracellular Ca2+ concentration and vimentin in endothelial cells following tumor cell-endothelial cell interactions

Alterations in the intracellular Ca2+ concentration and vime...

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第二届世界天然药物和传统药物药理学学术会议

作者： Yan PAN,Xue-Jun LI (State Key Laboratory of Natural and Biomimetic Drugs,Department of Pharmacology,School of Basic Medical Sciences,Peking University and Institute of System Biomedicine,Peking University, Beijing 100191,China)

AIM Interactions of tumor cells with endothelial cells（EC）,for example tumor cell adhesion and migration through the EC layer,are essential components of tumor *** calcium regulation and cytoskeletal proteins in both tumor cells and EC provide important signaling mechanisms for the growth,angiogenesis and metastasis of tumor *** the present study, we investigated the influence of tumor cell-EC interactions on the intracellular calcium ion concentration([Ca]) and vimentin in ***[Ca] was measured by confocal microscopy in human umbilical vein endothelial cells（HUVEC） before and after the addition of PC-3M prostate carcinoma *** expression and structural organization of vimentin in HUVEC was analyzed by immunofluorescence *** effect of heparin and nifidipine on EC[Ca] and vimentin were ***,a known disruptor of intermediate filaments,was used to induce the collapse of vimentin filaments,and the distribution of calcium ions in ECs was *** PC-3M cells induced a rapid[Ca] elevation and lead to altered vimentin distribution in EC at the sites of tumor cell-EC *** cell-induced[Ca] elevation was significantly inhibited by heparin and nifidipine;however, heparin and nifidipine had no obvious effects on the expression and organization of ***-induced collapse of vimentin filaments shifted the distribution of calcium ions from the cytoplasm to the nucleus and perinuclear field in *** Rapid [Ca] elevation and alterations in vimentin distribution occur in EC at the sites of tumor cell-EC contact;the structural integrity of vimentin is partly related to the intracellular calcium ion distribution and concentration.

关键词： calcium ions vimentin tumor cell-endothelial cell interaction

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Antihypertensive effect of linarin combined with luteolin on spontaneously hypertensive rats

Antihypertensive effect of linarin combined with luteolin on...

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第二届世界天然药物和传统药物药理学学术会议

作者： Gui-Yuan Lü~1,Jie SU~1,Su-Hong CHEN~(2*),Yan-Ping ZHANG~1,Jing LEI~1 (1.Institute of Materia Medica,Zhejiang Chinese Medical University,Hangzhou 310053,China 2.Institute of Chinese Materia Medica,Wenzhou Medical College,Wenzhou 325035,China)

AIM To observe the antihypertensive effect of linarin combined with luteolin on ***①The singledose test:The spontaneously hypertensive rats（SHRs） were given linarin combined with luteolin by intragastric administration（ig） for once and blood pressure of 1,2,4,6 and 9 h were measured by CODA multi-channel non-invasive pressure measuring system to determine the best-effective-time.②The continuous-dose test;The SHRs were given linarin combined with luteolin by gavage 30 d and measuring blood pressure on the 0,1,3,8,12,19 and 30 d at the *** the last treatment,blood samples were collected to detect the levels of Ang H,ALD,ET,PGI,TXB,NO and PRA.③The hemorheology test;The SHRs were given linarin combined with luteolin for 60 *** the 60th day,blood samples were drawn from orbit to detect hemorheology *** linarin combined with luteolin could decrease SBP which might be maintained more than 6 h in *** effect also could be lasted for 30 d in the *** with the model control group,the levels of AngⅡ,PRA,ALD,ET in plasma decreased,and the level of NO in serum ***,it improved the hemorheology *** Linarin combined with luteolin could decrease the blood pressure of SHR and improve the *** mechanism was potentially connected with restraining the RAAS,rising the serum NO content and reducing the plasma ET content.

关键词： linarin luteolin antihypertensive hemorheology

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A novel mouse model of combined hyperlipidemia associated with fatty liver and steatohepatitis generated by schisandrin B/cholesterol/bile salt suspended in olive oil

A novel mouse model of combined hyperlipidemia associated wi...

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第二届世界天然药物和传统药物药理学学术会议

作者： Kam-Ming KO Division of Life Science Hong Kong University of Science & Technology

AIM To create a novel mouse model of combined hyperlipidemia using a modeling agent（MA） made of a mixture of schisandrin B,cholesterol and bile salt(1,2 and 0.5 g·kg ) suspended in olive oil 20 ml·*** Mice were given a single dose of MA via intragastric *** biomarkers and hepatic lipids as well as hepatic weight were determined at 12,24, 48,72,96,or 120 h following the administration of *** Results showed that MA treatment increased serum triglyceride （TG） and total cholesterol（TC）(up to 422 and 100%at 12 -96 h post-treatment,respectively) and hepatic TG and TC（up to 220 and 26%at 12 - 120 h post-treatment,respectively） in a time- and dose-dependent ***,MA treatment elevated the serum high density lipoprotein and low density ***,serum alanine/aspartate aminotransferase and aspartate aminotransferase activity was elevated（up to 198 and 64%,respectively） at 48 and 72 h post-MA *** index,were increased（up to 66%） at 24 - 120 h post-MA *** pretreatment(0.1 g·kg for 4 d) reduced serum TG and TC levels as well as hepatic TG content in MA-treated ***,the combined treatment with MA and fenofibrate showed an increase in liver weight（up to 139%） in an additive *** Oral administration of a mixture of schisandrin B,cholesterol and bile salt could generate an interesting mouse model of combined hyperlipidemia associated with hepatic steatosis and steatohepatitis.

关键词： hyerlipidemia fatty liver hepatomegaly steatohepatitis Schisandrin B fenofibrate

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Exploring therapeutic potential of FTY-720 for treating cardiac hypertrophic remodelling

Exploring therapeutic potential of FTY-720 for treating card...

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第二届世界天然药物和传统药物药理学学术会议

作者： Ronald NAUMANN Ludwig NEYSES R.John SOLARO Elizabeth J.CARTWRIGHT Max Planck Institute of Molecular Cell Biology and Genetics Germany Faculty of Life Sciences Manchester Academic Health Sciences CentreThe University of ManchesterUK Department of Physiology and Biophysics and Centre for Cardiovascular Research University of Illinois at ChicagoUSA

AIM Cardiac hypertrophy is regarded as a clinical determinant of heart *** average age of cardiac hypertrophy onset is about 50 years old and the average patient with heart failure is 77 years *** leaves a relatively large time window where a patient displaying early cardiac hypertrophy could be treated to slow or even prevent the progression of hypertrophic remodelling;therefore studies to discover regulatory mechanisms underlying hypertrophic remodelling and to identify potential therapeutic targets for treating heart failure are of paramount *** Over the past few years using genetically modified mouse models and pharmacological agents our group has investigated the roles of a number of intracellular signalling proteins in cardiac hypertrophy, and recently identified a novel anti-hypertrophic molecule,p21-activated kinase-1(Pak-1).RESULTS In the heart our studies demonstrate Pak1 protection against stress-induced hypertrophic remodelling and targeting of Pak-1 in heart muscle by FTY-720 via Gi coupled sphingosine receptors is able to prevent the induction of stress-induced hypertrophy and reserve existing hypertrophy and fibrosis in wild-type mice,without compromising the cardiac ***-720 is known as a sphingosine-like analogue,derived from myriocin,a component of the natural product Isaria *** Our data provides a scientific basis of development of FTY-720 for clinical applications in the treatment of cardiac hypertrophic remodelling.

关键词： FTY-720 p21-activated kinase-1 cardiac hypertrophy heart failure

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Mechanism of dioscin-containing serum against apoptosis of cardiomyocytes induced by hydrogen peroxide

Mechanism of dioscin-containing serum against apoptosis of c...

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第二届世界天然药物和传统药物药理学学术会议

作者： Xin LIU~1,Yi KANG~2 (1.Department of Pathophysiology,2.Department of Pharmacology,Tianjin Medical University, Tianjin 300070,China )

AEVI To study the mechanism of Dioscin against apoptosis of cardiomyocytes induced by hydrogen peroxide through serum pharmacologic ***①The drug-containing serum(0.6 g crude drug/kg) was prepared.②Cardiomyocytes from neonatal SD rats were cultured in *** primary cultured cardiomyocytes were injured by hydrogen peroxide before giving the drug-containing serum with different *** cardiomyocyte viability was determined by MTT method.③Morphological changes of cardiomyocytes were observed by fluorescence microscope after treating with the drug-containing serum at different concentrations.④The anti-apoptotic effect of dioscin was indicated by detecting the activity of caspase 3 and caspase *** protein expression of Bcl-2 and Bax were semi-quantified by Western blot method after treating with the drug-containing ***①The cardiomyocyte viability was elevated(P<0.01) after being treated with different concentrates of drug-containing serum(0.4,0.8, 1.2 g crude drug/kg,prepared from the original drug-containing serum).②Typical apoptotic features of the cardiomyocytes such as membrane blebbing,cell shrinkage and detachment,and nucleus condensation and fragmentation were dose-dependently improved after being treated with drug-containing serum.③The activity of caspase 3 decreased with the increasing concentration of drug.④Western blot approach showed that the Bcl-2 level increased meanwhile the Bax *** Dioscin could increase the viability of the primary cultured cardiomyocytes in hydrogen peroxide induced *** could also decrease the activity of caspase 3, improve nucleus condensation and fragmentation,increase Bcl-2 level and decrease the Bax level.

关键词： dioscin serum pharmacology apoptosis

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Hypoglycemic effect of compound K on type 2 diabetes mice via downregulation of PEPCK and G6Pase expression in liver

Hypoglycemic effect of compound K on type 2 diabetes mice vi...

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第二届世界天然药物和传统药物药理学学术会议

作者： Ming ZHANG~1,Wei LI~(1,2),Jian GU~1,Zhao-jie MENG~1,Sheng-nan WEI~1,Li CHEN~(1*) (1.Norman Bethune College of Medicine,Jilin University,Changchun 130021,China 2 College of Chinese Medicinal Materials,Jilin Agricultural University,Changchun 1300118,China)

AIM To observe the therapeutic usefulness of Compound K（CK） in type 2 diabetes and its possible mechanisms. METHODS Type 2 diabetes was induced in male ICR mice by combining of streptozotocin(STZ,100 mg·kg body weight) and high-fat diet（HFD,45%of energy as fat）.After 4 weeks,mice with fasting（12 h ） blood glucose levels（FBG） between 7.8 and 18 mmol·L were divided into 3 groups（n = 12） and treated with vehicle（diabetes model,DM）,30 mg·kg·d of CK and 300 mg·kg·d of PDG for 4 weeks while continuing on the high-fat *** Hypoglycemic effects of CK and PDG were consistently demonstrated by FBG levels,and insulin-sensitizing effects were seen during oral glucose tolerance testing（OGTT）.Moreover, gluconeogenic genes,phosphoenolpyruvate carboxykinase（PEPCK） and glucose-6-phosphatase（G6Pase）,were decreased in two treatment groups with CK showing greater *** These findings demonstrated the hypoglycemic and insulin- sensitizing capabilities of CK on type 2 diabetes induced by HFD/STZ via down-regulation of PEPCK and G6Pase expression in liver.

关键词： Compound K prolopanaxadiol-type ginsenosides type 2 diabetes phosphoenolpyruvate carboxykinase

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Anti-influenza viral and anti-inflammatory activities of theaflavin derivatives

Anti-influenza viral and anti-inflammatory activities of the...

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第二届世界天然药物和传统药物药理学学术会议

AIM The shortage of anti-viral drugs urge us to look for new lead compounds for developing new anti-influenza viral *** drug screening of influenza viral neuramindase(NA) inhibitors,theaflavin(TF) derivatives all displayed NA *** this paper,their in vitro anti-influenza viral activity and anti-inflammatory activity were *** The in vitro antiviral activities were evaluated by cytopathic effect(CPE) reduction assay,their action mechanisms were studied by NA activity assay,a haemagglutination(HA) inhibition assay and a real-time quantitative PCR(qPCR) assay for gene expression of HA,their anti-inflammatory activity were evaluated by cytokine secretion *** The experimental results showed that TF derivatives all exerted anti-influenza viral activities,their inhibitory effects on the NA of three distinct influenza virus strains,and they also displayed an inhibitory effect on *** addition,they decreased the expression level of the inflammatory cytokine IL-6 during viral infection. CONCLUSION We can concluded that TF derivatives are potential compounds with anti-influenza viral replication and anti-inflammatory properties,which will provide information for novel antiviral drug design and development.

关键词： antiviral anti-inflammatory influenza virus theaflavin derivatives

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Dietary Fructus Schisandrae extracts and fenofibrate regulate the serum/hepatic lipid-profile in normal and hypercholesterolemic mice,with attention to hepatotoxicity

Dietary Fructus Schisandrae extracts and fenofibrate regulat...

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第二届世界天然药物和传统药物药理学学术会议

作者： Kam-Ming KO Division of Life Science Hong Kong University of Science & Technology

AIM To investigate the effects of dietary intake of Fructus Schisandrae chinensis（FSC）,both aqueous and ethanolic extracts（AqFSC,EtFSC）,on serum/hepatic lipid contents in normal diet（ND）- and high-fat/cholesterol/bile salt diet（HFCBD）-fed *** Male ICR mice were fed with ND or HFCBD,supplemented with 1 and 4%of AqFSC and EtFSC,respectively, or 0.1%fenofibrate,for 13 *** were determined according to the manufacture's *** EtFSC,but not AqFSC,significantly elevated hepatic triglyceride（TG） in mice fed with *** mice with HFCBD increased serum total cholesterol （TC）,high density lipoprotein（HDL） and low density lipoprotein（LDL） levels as well as alanine aminotransferase（ALT） *** with AqFSC,EtFSC or fenofibrate significandy reduced hepatic TC and TG ***,AqFSC and EtFSC supplementation increased serum HDL and LDL levels in mice fed with *** increased serum HDL and reduced serum LDL contents in hypercholesterolemic *** reduced,but fenofibrate elevated,serum ALT activity in both normal and hypercholesterolemic *** fenofibrate reduced serum TC,TG,and HDL levels in mice fed with ND,it increased serum HDL and reduced serum LDL,TC,and TG levels in mice fed with *** was found in normal and hypercholesterolemic mice fed with diet supplemented with *** value of AqFSC and EtFSC was estimated to be（43.24±7.79） g·kg and 40.35±6.22,respectively,using the Bliss *** Feeding mice with AqFSC and EtFSC ameliorated the HFCBDinduced hepatic *** addition,EtFSC may offer protection against hepatic injury in hypercholesterolemic mice.

关键词： Fructus Schisandrae Chinensis fenofibrate fatty liver hypercholesterolemia hepatotoxicity hepatomegaly

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