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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 Wei LI Jian GU Zhao-jie MENG Sheng-nan WEI Li CHEN Norman Bethune College of Medicine Jilin UniversityChangchun 130021China Norman Bethune College of MedicineJilin UniversityChangchun 130021China College of Chinese Medicinal Materials Jilin Agricultural UniversityChangchun 1300118China

AIM To observe the therapeutic usefulness of Compound K (CK) in type 2 diabetes and its possible *** Type 2 diabetes was induced in male ICR mice by combining of streptozotocin (STZ, 100 mg·kg-1 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-1 were divided into 3 groups (n =12) and treated with vehicle (diabetes model, DM), 30 mg· kg-1 · d-1 of CK and 300 mg·kg-1 ·d-1 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 (OGTI).Moreover, gluconeogenic genes, phosphoenolpyruvate carboxykinase (PEPCK) and glucose-6-phosphatase (GtPase), were decreased in two treatment groups with CK showing greater *** These findings demonstrated the hypoglycemie and insulinsensitizing 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 protopanaxadiol-type ginsenosides type 2 diabetes phosphoenolpyruvate carboxykinase

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Protect effects of Fufangdengzhanhua dripping pill on PC12 cell injury induced by hydrogen peroxide in culture

Protect effects of Fufangdengzhanhua dripping pill on PC12 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： Lei WAN Jing-Xia XU Department of Pharmacology Guiyang Medical CollegeGuiyang 550004China

AIM To investigate protect effect of Fufangdengzhanhua dripping pill (FDD)'s oxidative stress induced by hydrogen peroxide on PC12 *** PC12 cells were divided into six groups in culture: control group, oxidative damage group,different concentration of FDD group (0.763, 3.052, 12.207 mg· L-1), positive drug group (vitamin E, 4.307 mg· L-1).After drug intervention for 24 h, PC12 cells were injured by 300 μmol·L-1 H2O2 except control group for 2 *** the pretreating of FDD at different concentration for 24 h, typical morphological characteristics of PC12 after being exposed to H2O2 could be observed under the inverted *** survival rate of PC12 were detected by *** dehydrogenase (LDH), superoxide dismutase (SOD)and malondialdelyde (MDA) in the culture *** After being exposed to 300 μμnol· L-1 H2O2 for 2 h, FDD can decrease LDH, MDA content and increase SOD activity *** increases the survival rate of PC12 cells according to the results of *** with the model group, there was statistically significant difference (P <0.01).CONCLUSION FDD can protect injury induced by hydrogen peroxide on PC12 cells in *** acting mechanisms may include protecting cell membrance and inhibiting lipid peroxidation.

关键词： FDD PC12 cells H2O2 superoxide dismutase malondialdelyde

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Discovery of anti-sepsis agents from traditional Chinese medicine by utilizing affinity biosensor technology

Discovery of anti-sepsis agents from traditional Chinese med...

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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-Chuan ZHENG~1,Xiu LIU~1,Ning WANG~1,Hong-Wei CAO~1,Guo WEI~1,Yong-Ling LU~1, Hong ZHOU~2,Jiang ZHENG~1 (1.Medical Research Center,Southwest Hospital,2.Department of Pharmacology,College of Pharmacy, the Third Military Medical University,Chongqing 400038,China)

AIM Sepsis is a common and severe complication in trauma,burn and infected patients,and has become the leading cause of death in *** screening,bioactivity-guided isolation and biological evaluation of anti-sepsis agents from traditional Chinese medicine(TCM) were investigated in the present *** The pathogen-associated molecular patterns(PAMPs) containing lipopolysaccharide(LPS) and bacterial DNA were immobilized onto the chip of affinity biosensor,and the extracts of more than 140 TCM were screened and isolated under the direction of affinity ***,the biological activities of isolated compounds were investigated in vitro and in *** affinity constant was determined by using *** neutralization of LPS was evaluated by tachypleus amebocyte lysate(TAL) *** of proinflammatory signal transduction and cytokines production induced by LPS and bacterial DNA were assessed by cellular *** effect against sepsis in a cecal ligation and puncture-induced or heat-killed bacteria-challenged mouse model was evaluated by determination of the survival rate and levels of serum LPS and tumor necrosis factor-alpha(TNF-α).RESULTS More than 10 compounds were found to have potential anti-sepsis ***, a novel dual inhibitor of LPS and bacterial DNA,Kukoamine B,was found from the root bark of Lycium chinense *** vitro, Kukoamine B was found to bind to and neutralize both LPS and bacterial *** could prevent LPS and bacterial DNA from interacting with mouse macrophages,and markedly inhibit LPS and bacterial DNA-induced intracellular signal transduction and over-production of proinflammatory mediators without affecting the signal pathways and cell *** vivo,Kukoamine B significantly improve the survival rate of mice with sepsis,and decrease the circulatory levels of LPS and TNF-α.CONCLUSION Targeting pathogenic molecules to screen and isolate anti-sepsis agents from TCM may provide a promising therapeut

关键词： traditional Chinese medicine sepsis affinity biosensor

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Bio-activities of Ophioglossum thermale

Bio-activities of Ophioglossum thermale

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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： Jin-Hwa KIM Geun-Soo LEE Hyeong-Bae PYO Eun-Young SHIN Eung-Gook KIM Department of Biochemistry College of MedicineChungbuk National University410 Sungbong-roGaesin-dongCheongju 361-763Korea

AIM To characterized the in vitro antioxidative and in vivo anti-inflammatory activities of *** Antioxidant fractions from Ophioglossum thermale were extracted with five different polar solvents using Soxhiet type *** total phenolic content of the extracts was determined by Folin-Ciocalteu *** acetate fraction of *** was found to contain maximum *** dried fractions were screened for their antioxidant activity potential using in vitro model systems such as 1,1- diphenyl-2-picryl hydrazyl（DPPH ）,nitroblue tetrazolium（NBT） and lipid-peroxidation reduction at different concentrations. RESULTS This study revealed that the EtOAc fraction exhibited the best performance in DPPH assay,NBT assay and lipid peroxidation. All fractions showed more potent antioxidant capacity than Green tea extract,a well known ***,the EtOAc fraction has the highest total phenolic contents（475.65 mg of EGCG/g）.In addition,EtOAc fraction at 0.005%and 0.01% （g/100 ml） also significantly inhibited UVB irradiation induced ROS generation in human dermal fibroblasts（HDFs）.In carrageenaninduced edema model,EtOAc fraction showed inhibitory effect（21.5%,P<0.05） at 200 mg·kg（po） after 300 min administration. Consequently,3-O-methylquercetin（3MQ） was also isolated from the antioxidative EtOAc *** The data obtained using above in vitro and in vivo test suggest that the antioxidant activity of *** and its anti-inflammatory effect on carrageenan-induced acute inflammation can be attributed to its ameliorating effect on the oxidative damage and thus it has great potential as a source for natural health *** the best of our knowledge,this is the first report on antioxidant activity of different polar extracts from ***.

关键词： Ophioglossum thermale anti-inflammation antioxidant radical scavenging activity

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Exploration for development of anti-ischemic stroke drugs:the discovery of pinocembrin-a novel agent targeting the neurovascular unit based on multi-targets and network regulation

Exploration for development of anti-ischemic stroke drugs:th...

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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： Guan-Hua DU,Mei GAO,Hong-Mei GUANG,Rui LIU,Fan-Rui MENG,Cai-Xia WU,Xi LAN,Yang Lü (Beijing Key Laboratory of Drug Target and Screening Research,Institute of Materia Medica,Chinese Academy of Medical Sciences & Peking Union Medical College,Beijing 100050,China)

AIM Up to now,the only currently approved treatment for acute ischemic stroke（AIS） is alteplase,a thrombolytic agent given intravenously within 4.5 h of symptom onset,in an attempt to re-open occluded intracerebral ***,no more than 5%of all AIS patients receive alteplase because of too long symptom-onset-to-hospital ***,this strategy is effective for less than half of the patients treated within the therapeutic *** far there have been no challenges and novel strategies for treatment of ischemic *** Based on the multiparametric interaction within the network in pharmacological system biology,our laboratory has developed novel agents with multiple targets for the treatment of ischemic *** is one of the novel NVU network regulated natural products of great *** In 2008,pinocembrin has been approved by the State Food and Drug Administration of China for clinical use in stroke *** has been clearly confirmed to have protective effects on the neurovascular unit（NVU） in ischemic animal *** compound has a good bioavailability and high BBB *** therapeutic dose-range was demonstrated to be much *** pinocembrin was intravenously injected at 0,8 and 16 h after MCAO,neurological deficit scores and cerebral infarct volumes were preserved from 3 mg·kg to 30 mg·kg at 24 and 48 *** results also suggested that pinocembrin conferred robust neurovascular coupling protection in MCAO *** components of NVU were maintained by the increased fluorescent intensities under confocal microscopy,which was related to the preservation of microvascular integrity and the attenuation of serious neuronal *** rCBF value was gradually recovered from 10.37%to 43.16%of the basic level. The BBB was well protected,and the percentage of cortical microvessels presenting lanthanum ion leakage showed a significant decrease from 28.2%to 35.6%.Further,pinocembrin specially affected RAGE and CRE

关键词： stroke blood-brain barrier neurovascular unit pinocembrin

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Protective effect of scutellarin on myocardial ischemia-reperfusion injury in rats

Protective effect of scutellarin on myocardial ischemia-repe...

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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： Xiao-Ming LIU~1,You-Lan WANG~2,Lei WANG~1,Ya-Juan CHEN~1,Lin LI~3,Tao GUO~3, Chen QING~1,Wei-Min YANG~(1*) (1.School of Pharmaceutical Science & Yunnan Key Laboratory of Pharmacology for Natural Products,Kunming Medical University,Kunming 650500,China 2.Kunming Institute of Medical Science,Kunming 650011, China 3.First Affiliated Hospital of Kunming Medical University,Kunming 650032,China)

AIM Protective effects of scutellarin（SCU） on myocardial ischemia reperfusion（I-R） in rats was evaluated,different SCU treatments were compared and SCU 's effect-time relationship was also investigated in the present *** Myocardial I-R injury model was established by ligation of left anterior descending branch of coronary artery in rats for 40 min,and then carrying on reperfusion for 120 *** left ventricle was isolated and cut into slices,the slices were stained with TTC,observe the change of the ischemic area,and evaluate the protective effect of SCU on myocardial I-R injury in ***①Intravenous infusion of SCU can reduce the ischemic area percentage in myocardial I-R ***(45,90,180 mg·kg ) significantly reduced ischemic *** can decrease the activity of LDH in plasma in myocardial I-R *** with model group,SCU(90,180 mg·kg ) significantly decreased the activity of LDH in plasma in myocardial I-R rats.②SCU pre-treatment,post-treatment and treatment during I-R showed protection in myocardium I-R *** effect is most potent when rats were treated with SCU during I-R,compared with model group,SCU 180 mg·kg significantly reduced ischemic area.③During 0 - 120 min after SCU treatment,protective effect of SCU on myocardial I-R injury in rats wore off with time prolongation.0,30,60 min after SCU 180 mg·kg treatment,SCU significantly reduced ischemic area.120 min after SCU treatment,the effect was not *** SCU treatment attenuated injury in myocardial I-R *** pre-treatment,post-treatment and treatment during I-R had preventative and therapeutic effects in myocardial I-R rats.

关键词： scutellarin myocardial ischemia reperfusion ischemic area

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Activation of AMP-activated protein kinase alleviates high glucose-induced dysfunction of brain endothelial cell tight junction dynamics

Activation of AMP-activated protein kinase alleviates high g...

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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： Chao LIU~1,Ji-Liang WU~1,Ming-Hui ZOU~2 (1.Hubei Province Key Laboratory on Cardiovascular,Cerebrovascular,and Metabolic Disorders,Xianning University, Xianning 437100,China 2.Section of Molecular Medicine,Department of Medicine,University of Oklahoma Health Sciences Center,Oklahoma City,Oklahoma,USA)

AIM The aim of this study was to elucidate the molecular mechanisms underlying disruption of the blood-brain-barrier in diabetes and to determine whether activation of AMP-activated protein kinase prevents diabetes-induced blood-brain-barrier dysfunction. METHODS Human brain microvascular endothelial cells（HBMEC） were cultured in endothelial cell media mixed with astrocyteconditioned medium（1:1）.Confluent cells were maintained in 1%fetal calf serum and exposed to normal glucose(NG,5 mmol·L ) or high glucose(HG,D-glucose 25 mmol·L ) for up to 1 week,control groups were exposed to L-glucose(LG,20 mmol·L ) in normal medium containing D-glucose(5 mmol·L ).Intracellular Owas measured using the dihydroethidium（DHE ） fluorescence ***-endothelial electrical resistance（TEER） was determined by the *** the inter related proteins were exam- ined by Western *** HBMEC exposure to HG for 2 h to 1 week significantly increased the permeability of blood-brainbarrier in parallel with lowered expression levels of zonula occludens-1,occludin,and claudin-5,three proteins that are essential to maintain endothelial cell tight *** addition,HG significantly increased generation of superoxide *** overex pression of superoxide dismutase or catalase significantly attenuated the HG-induced reduction of endothelial cell tight junction ***,administration of apocynin reversed the effects of HG on endothelial cell tight junction ***,activation of AMP-activated protein kinase with 5-amino-4-imidazole carboxamide riboside（AICAR） or adenoviral overexpression of constitutively active AMP-activated protein kinase mutants（Ad-AMPK-CA） abolished both induction of NAD（P） H oxidase-derived superoxid anions and tight junction protein degradation induced by *** We conclude that HG increases blood-brain-barrier dysfunction in diabetes through induction of superoxide anions and that the activation of AMP-activated protei

关键词： AMPK NAD(P)H oxidase blood brain barrier tight junctions diabetes

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Carnosic acid prevent hepatic from ischemia-reperfusion injury by silent information regulator 1 pathway

Carnosic acid prevent hepatic from ischemia-reperfusion inju...

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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 HU,Feng ZHANG,Xiao-Mei XU,Xiao-Han ZHAI,Dong-Yan GAO,Ji-Hong YAO~* (Dalian Medical University,Dalian,China)

AIM Silent information regulator 1（Sirt1 ）,a classⅢhistone deacetylase,has been reported to attenuate myocardial and kidney ischemia-reperfusion（I-R） ***,the mechanisms of Sirt1 in hepatic I-R have not been *** acid（CA）,a rosemary phenolic compound,was demonstrated to protect the brain against oxidative stress during middle cerebral artery *** present study was performed to determine CA would reduce hepatic I-R stress and to clarify the molecular mechanisms of CA. METHODS In vivo,rats were randomly exposed to sham-operated group,I-R group（45 min ischemia to 70%of the liver followed by 90 min reperfusion）,CA(60 mg·kg,given 60 min before surgery ),I-R + CA,ischemic preconditioning（IPC）.After reperfusion, pathological alterations,apoptosis index,serum aminotransferases and inflammation factors were *** expressions of Sirt1, P66shc and NF-κB in hepatic were *** vitro,HepG2 cell was treated with CA 2.5,5 and 10μmol·*** this treatment, the expression of Sirt1 was *** In vivo,CA and IPC decreased I-R-mediated the serum levels of aminotransferases, inflammatory response and hepatocellular *** I-R injury was associated with decreased Sirtl,increased P66 and upregulated NF-κB,which were prevented by CA and *** and IPC also significantly attenuated levels of I-R-induced hepatic cell apoptosis. In vitro,CA increased the Sirtl protein level in a dose and time-dependent *** For the first time,we confirm that CA can protect hepatic against inflammation and apoptosis caused by I-R through Sirtl *** results reveal a new protective mechanism elicited by CA-induced SIRT1 activation in I-R tissues and suggest a novel potential therapeutic targets to manage I-R-indueed hepatic dysfunction.

关键词： Sirtl reperfusion,injury carnosic acid inflammation apoptolisis

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PF11 is anti-inflammatory in N9 microglial cells by inactivating nuclear factor-kappa B and inhibiting mitogen-activated protein kinases

PF11 is anti-inflammatory in N9 microglial cells by inactiva...

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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： Xiao-Xiao WANG,Si-Qi ZHAO,Chun-Ming WANG,Kuo ZHANG,Chun-Fu WU~*,Jing-Yu YANG~* (Department of Pharmacology,Shenyang Pharmaceutical University,Shenyang 110016,China)

AIM Pseudoginsenoside-F11（PF11 ）,an ocotillol-type saponin,is one of the ingredients of Panax quinquefolium （American ginseng）,previously isolated from leaves of Panax pseudoginseng *** H（Himalayan Panax）,but not in Panax *** previous experiments showed that PF11 could improve the scopolamine-induced memory impairments in *** the present study,we assessed the anti-inflammatory effect of PF11 on the production of pro-inflammatory mediators in lipopolysaccharide （LPS） -stimulated murine N9 *** The effects of PF11 on the NO production in activated microglial cells were assessed by Griess *** blotting was used to detect the protein phosphorylation levels of p38,JNK,ERK,IKKα/β, TAK1 and IκB-α.NF-κB activity was analyzed by using High-Content *** PF11 suppressed production of nitric oxide （NO）,prostaglandin E（PGE） and the pro-inflammatory cytokines,interleukin-1β（IL-1β） in a concentration-dependent manner. PF11 significantly inhibited NF-κB translocation in LPS-stimulated N9 microglia,this was associated with a decrease in the phosphorylation level of inhibitoryκB-α（IκB-α）.Furthermore,PF11 suppressed the phosphorylation of transforming growth factorβactivated kinase-1（TAK1） and inhibitor ofκB kinase（IKK）.Moreover,PF11 blocked signaling upstream of NF-κB activation by inhibiting extracellular signal-regulated kinases 1 and 2（ERK1/2）,c-Jun N-terminal kinase（JNK） and p38 *** Our results demonstrate that suppression of the NF-κB,MAPKs signaling pathways may inhibit LPS-induced NO and PGE production. Therefore,PF11 may have therapeutic potential for neurodegenerative diseases by inhibiting pro-inflammatory mediators and cytokine production in activated microglia.

关键词： PF11 microglia inflammation NF-κB MAPK

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Anti-malarial drug artesunate is an effective drug for allergy and asthma

Anti-malarial drug artesunate is an effective drug for aller...

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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： WS Fred WONG W Eugene HO Department of Pharmacology Yong Loo Lin School of MedicineNUHSSingapore Immunology Program Life Science InstituteNational University of SingaporeSingapore Saw Swee Hock School of Public Health NUHSSingapore

Artesunate is a semi-synthetic derivative of artemisinin,an active component of the medicinal plant Artemisia annua. Artesunate is a clinically effective anti-malarial *** is an acquired hypersensitivity reaction of the immune system mediated by cross-linking of allergen-specific IgE-bound high-affinity IgE receptors,leading to immediate mast cell *** is a chronic airway disorder characterized by airway obstruction,hyperresponsiveness,oxidative damage and *** prevented IgE-mediated cutaneous vascular hyperpermeability,hypothermia,elevation in plasma histamine level and tracheal tissue mast cell degranulation in mice in a dose-dependent *** concentration-dependently blocked IgE-mediated degranulation of RBL- 2H3 mast cells and human culture mast *** was found to inhibit IgE-induced Syk and PLC 1 phosphorylation,production of IP3 and rise in cytosolic Ca level in mast *** dose-dependently inhibited OVA-induced increases in total and eosinophil counts,IL-4,IL-5,IL-13 and eotaxin levels in bronchoalveolar lavage *** attenuated OVA-induced lung tissue eosinophilia and airway mucus production,mRNA expression of E-seleetin,IL-17,IL-33 and Muc5ac in lung tissues,and airway hyperresponsiveness to *** normal human bronchial epithelial cells,artesunate blocked epidermal growth factor-induced phosphorylation of Akt and its downstream substrates tuberin,p70S6 kinase and 4E-binding protein 1,and transactivation of *** damage markers 8-isoprostane,8-hydroxy-2-deoxy-guanosine and 3-nitrotyrosine levels were potently repressed by ***-induced increases in pro-oxidants,iNOS and NADPH oxidase（NOX 1,2,3 and 4） were significantly abated by *** expressions of regulatory subunits of NOX,p22phox and p67phox,were also reduced by *** expressions and activities of antioxidants superoxide dismutase and catalase were substantially restored with arte

关键词： Anti-malarial drug artesunate is an effective drug for allergy and asthma

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