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Essential oils of Myrtus communis L. produce a non-sedating anxiolytic effect in mice model of anxiety

Essential oils of Myrtus communis L. produce a non-sedating ...

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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： Eyob Hailu Ephrem Engidawork Kaleab Asres Department of Pharmacology and Therapeutics School of PharmacyAddis Ababa UniversityAddis AbabaEthiopia Department of Pharmacognosy and Pharmaceutical Chemistry School of PharmacyAddis Ababa UniversityAddis AbabaEthiopia

AIM The myrtle shrub（Myrtus communis L.,Myritaceae） is rich in essentia]oils that are used in Ethiopian traditional medicine for treatment of a variety of ailments,including *** is a common disorder that attacks many people in society and often accompanied by physiological sensations such as tachycardia,chest pain,shortness of breath,*** present study was undertaken to evaluate the anxiolytic effect of the essential oil of *** using different models of *** AND METHODS Swiss Albino mice of either sex were randomly divided into five ***Ⅰ（control） was administered Tween 80（5%,V/V） in distilled ***Ⅱ（positive control） was given diazepam(0.5 mg·kg,orally),suspended in the ***Ⅲ-Ⅳ（test groups） were given the essential oil at doses of 50,100,200 and 400 mg·kg,*** were then subjected to anxiety models,including elevated plus maze（EPM）,stair case and open field,and parameters,among others,percentage of time spent in each arm and arm entries,number of steps climbed and number of rears,and number of crossings were *** In EPM studies,the extract at both 100 mg·kg（P<0.01） and 200 mg·kg（P<0.05） produced a significant increase in percentage of open arm time as compared to *** the staircase setting,significant reduction of rearing was observed in mice treated with the essential oil at 100 mg·kg（P<0.01） and 200 mg·kg（P<0.05） compared to ***, at doses of 50 and 400 mg·kg no detectable changes were noted on the measured parameters in both EPM and stair case *** total number of entries into open field was comparable in all *** The essential oil of *** showed better anxiolytic activity at 100 mg·kg compared to the standard *** possible mechanism by which the oil showed the activity could be through GABA-related ***,the present work holds up the traditional use of the plant for anxiety.

关键词： anxiety elevated plus maze stair case open field Myrtus communis

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Synergistic antibacterial effect between ASP and β-lactam antibiotics against methicillin-resistant Staphylococcus aureus

Synergistic antibacterial effect between ASP and β-lactam a...

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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： Chun-Hui ZENG~1,Ke YANG~1,Guang WU~2,Zhan-Jing GUO~1,Ming-Guang XU~1,Yi-Qing CHEN~1 (1.Faculty of Pharmacy of Guangxi University of Chinese Medicine,Nanning 530001,China 2.Faculty of Preclinical Medicine of Guangxi University of Chinese Medicine,Nanning 530001,China)

AIM Methicillin-resistant Staphylococcus aureus（MRSA） has been recognized as one of the most important pathogens, which is endemic in hospitals ***（dihydromyricetin） which has been extracted from Ampelopsis grossedentata （Hand-Mazz） *** from Guangxi had been reported antibacterial activity against MSSA and MRSA in vitro and in *** purpose of our study was to investigate the effects and underlying mechanisms of APS alone and in combination withβ-lactam antibiotics on *** Kirby-Bauer and mecA gene test were used to identify 15 MRSA strains isolated from *** MICs of 4 MRSA strains including MSAR-6,MRSA-8,MRSA-9,MRSA-12 and the methicillin-susceptible Staphylococcus,aureus（MSSA） were tested by agar dilution *** synergistic effects of APS with 6β-lactam antibiotics against MRSA-6 were measured by checkerboard method with Fractional inhibitory concentration index（FICI）.To evaluate the protective effect of APS alone and in combination withβ-lactam antibiotics in vivo,MRSA abdominal infection and lung infection mice models were performed with intraperitoneal injection and intranasal inhalation of MRSA-6,*** and transmission electron microscopy were used to observe the ultrastructure of bacterial morphology treating with different concentrate APS alone and in combination withβactam antibiotics against MSSA and *** 4 strain MRSAs were identified with Kirby-Bauer and mecA gene *** MICs of APS alone were 125 mg·*** effect of APS and 5β-lactam antibiotics such as penicillin,oxacillin,cefazolin,tienam,cefoxitin were detected with checkerboard-method to MRSA in vitro except cefepime which showed the additive effect with *** in combination with tienam and cefoxitin can increase the survival rates of abdominal infected mice by MRSA,ED was 3.03 mg·kg and 13.79 mg·kg respectively,decreased 12 and 16.7 times than of tienam and cefoxitin *** dose APS in combination with tienam and cefoxitin

关键词： APS MRSA synergistic antibacterial effect in vivo in vitro

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Genistein induces Nrf2 and HO-1,GCLC gene expression via ERK and PKC pathways and protects against oxidative injury in Caco-2 cells

Genistein induces Nrf2 and HO-1,GCLC gene expression via ERK...

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

AIM Genistein is a member of the flavoniod *** have well-known antioxidant,anti-inflammatory and anti-cancer *** this work,we examined whether genistein affect HO-induced oxidative injury and the possible mechanism involved in the colon cancer *** focused on concerted effects on the expression of Nrf2 and phaseⅡenzymes pathway components. METHODS Caco-2 cells were treated for 3 h with different concentrations of genistein before being exposed to 10 mmol·L *** was used to measure cell *** of 2',7'-dichlorodihydrofluorescin diacetate（HDCFDA） was used to measure production of intracellular ROS in Caeo-2 *** and HO-induced Nrf2,HO-1 and GCLC mRNA and protein levels were assessed using RT-PCR and Western ***-induced phosphorylation of PKC and ERKl/2 was visualized using Western blot. RESULTS Treatment with genistein markedly attenuated HO-induced peroxide formation,and this amelioration was reversed by Buthionine sulfoximine（GCLC inhibitor） and zinc protoporphyrin（HO-1 inhibitor）.Genistein dose dependently increased HO-1 and GCLC mRNA and protein *** treatment activated the ERK1/2 and PKC signaling pathway and increased Nrf2 mRNA and protein *** roles of the ERK1/2 as partly as PKC signaling pathway were determined by using PD98059 （ERK1/2 inhibitor） and GF109203X（PKC inhibitor） and RNA interference directed against *** inhibitors and siNrf2 abolished genistein-induced HO-1 and GCLC protein *** results suggested the involvement of ERKl/2 and PKC and Nrf2 in the induction of HO-1 and GCLC by *** Genistein up-regulated HO-1 and GCLC expression through the EKR1/2 and PKC/Nrf2 pathway against oxidative stress.

关键词： gnistein Nrf2,phase Ⅱ enzymes oxidative stress

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SCM-198 attenuates lipopolysaccharide-induced inflammation in microglia and improves cognitive impairment caused by β-amyloid protein fragment 1 -40 in rats

SCM-198 attenuates lipopolysaccharide-induced inflammation i...

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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： Zhen-Yi HONG,Xue-Ru SHI,Kai ZHU,Ting-Ting WU,Yi-Zhun ZHU~* (Department of Pharmacology,School of Pharmacy,Fudan University,Shanghai 201203,China)

AIM Chronic inflammation in central nervous system（CNS） is a conspicuous hallmark in neurodegenerative diseases, including Alzheimer's disease（AD） and microglia activation is now widely accepted as a key factor in neuroinflammatory responses. Leonurine,also called SCM-198,is an alkaloid extracted from Herba *** the present study,we investigated its possible anti-inflammatory therapeutic effects both in vitro and in *** Immortalized murine BV-2 microglial cell line and purified rat primary microglia were incubated with lipopolysaccharide（LPS） 1 mg·L or were preincubated with different concentrations (0.01 - 10μmol·L ) of SCM198 2 h before LPS was *** viability,nitric oxide production,proinflammatory cytokine release were measured by MTT assay,Griess reaction and ELISA,***-time PCR and Western blot were used to analyze gene and protein expressions and immunocytochemistry staining were performed for NF-κB translocation in ***,microglia/ neuron co-culture system was used to determine whether SCM-198 could protect neuron indirectly via inhibition the activation of microglia. For in vivo study,bilateral intrahippocampalβ-amyloid protein fragment 1 -40(Aβ) injections were selected as model;60 male Sprague-Dawley rats were randomly divided into six groups;sham group,Aβ group,Aβ+ SCM198 15,30 and 60 mg·kg groups,Donepezil group(DON,1.0 mg·kg as a positive control)（n = 10,respectively）.Cognitive performance was evaluated by novel object recognition task（NOR） and Morris water maze（MWM）,microglia activation was detected by immunohistochemistry;gene and protein expressions were analyzed by real-time PCR,ELISA,Western *** SCM-198 could reduce nitric oxide production from LPS-activated microglia and could inhibit iNOS,TNF-α,IL-1βmRNA and protein expressions both in vitro and in ***,LPS-induced NF-κB translocation in BV-2 cells was effectively inhibited by ***, suppression of IκBαdegradation,

关键词： Alzheimer's disease SCM-198 microglia lipopolysaccharide

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Dose ratio-dependent,antagonistic effects of the combination of gallic acid and methyl gallate in human lung adenocarcinoma A549 cells

Dose ratio-dependent,antagonistic effects of the combination...

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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： Aikebaier MAIMAITI Department of Pharmacology School of Basic Medical SciencesPeking University Health Science Center

AIM Gallic acid(GA) and methyl gallate(MG) derived from grape seeds possess growth-inhibiting and apoptosis- inducing activities in cancer cell lines in *** the present study,we have investigated the impact of defined combinations of GA and MG(ratio 1:1,2:1,3:1,4:1 and 5:1) on cell proliferation and apoptosis induction in cultured A549 lung carcinoma cells and then investigated the possible molecular mechanisms underlying the observed toxic *** Human lung adenocarcinoma A549 cells were treated with a combination of GA and MG in different close ratio,and the changes in cell viability and apoptosis were determined by MTT assay and Annexin V-FITC staining assay,***-related proteins were determined by a Western blot *** malate dehydrogenase,voltage-dependent anion-selective channel protein 1(VDACl ),calreticulin and brain acid soluble protein 1 were measured by two-dimensional gel ***1 siRNA and negative control siRNA were transfected by using lipofectamine-2000 into cell lines according to the *** The percent viability of cells decreased with GA and MG treatment in a dose dependent *** and MG exhibit strong antagonistic interaction on the inhibit proliferation of A549 cells and induction of apoptosis in a dose ratio dependent *** blot analysis also showed that caspase 9 expression decreased and Bcl-2 expression increased in a dose ratio dependent *** were identified using by two dimension electrophoresis, four biomarkers were up-regulated proteins,namely Malate dehydrogenase,VDAC1,calreticulin and brain acid soluble protein 1,*** of these proteins,VDAC1 and calreticulin are associated with *** up-regulated VDAC1 expression in a dose dependent manner and combination of GA and MG down-regulated in a dose ratio dependent *** with VDAC1 siRNA slightly increased the cell viability after treatment of *** and p38 inhibitors did

关键词： gallic acid methyl gallate drug combination apoptosis voltage-dependent anion-selective channel protein 1

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Salvianolic acid A prevents the pathological progress of hepatic fibrosis in rats with type 2 diabetes

Salvianolic acid A prevents the pathological progress of hep...

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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： Li ZHANG~(1,2△),Gui-Fen QIANG~(1△),Xiu-Ying YANG~(1,2),Qi XUAN~3,Li-Li SHI~1,Heng-Ai ZHANG~1, Bai-Nian CHEN~(1,2),Xiao-Xiu LI~(1,2),Mian ZU~(1,2),Dan ZHOU~(1,2), Jing GUO~(1,2),Hai-Guang YANG~(1,2),Guan-Hua DU~(1,2*) (1.Beijing Key Laboratory of Drug Target Identification and Drug Screening,Beijing 100050,China 2 Institute of Materia Medica,Chinese Academy of Medical Sciences and Peking Union Medical College,Beijing 100050, China 3 Xuanwu Hospital,Capital Medical University,Beijing 100053,China)

AIM The aim of the present study was to evaluate the effect of salvianolic acid A（SalA） on the pathological progres- sion of hepatic fibrosis in rats with type 2 diabetes and investigate its liver-protective *** After the animal model of hepatic fibrosis with type 2 diabetes was successfully made with high-sucrose,high-fat diet-fed and low-dose streptozotocin（STZ）, SalA(0.3 mg·kg,i.g) was administered to diabetic rats for four *** hepatic pathological progress and the expression of a-smooth-muscle-actin（α-SMA） and transforming growth factorβ（TGF-β） in liver tissue were *** apoptosis and hepatic mitochondrial respiratory function were *** HE staining and Picro acid - Sirius red staining confirmed that SalA significantly alleviated the lesion of hepatic steatosis and *** expressions of a-SMA and TGF-β in liver tissue were markedly reduced by immunohistochemistry *** desoxynucleotide transferase-mediated dUTP nick end labeling staining showed that SalA reduced hepatocytes *** addition,SalA improved the injured hepatic mitochondrial respiratory function. CONCLUSION The findings suggested that SalA could prevent the pathological progress of hepatic fibrosis in rats with type 2 diabetes. Its liver-protecting mechanism might be involved in reducing oxidative stress,further suppressing the expression of a-SMA and TGF-β, expression,also anti-apoptosis and mitochondria-protective potential.

关键词： salvianolic acid A type 2 diabetes hepatic fibrosis nonalcoholic fatty liver disease

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Identification and quantification of total coumarins from Urtica dentata hand and its roles in promoting immune tolerance via TLR4 -mediated dendritic cell immaturation

Identification and quantification of total coumarins from Ur...

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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 XIANG~(1*),Jing-Li LU~1,Yan LAN~1,Guo-Xiao YIN~1,Wen PENG~2 (1.Department of Pharmacology,School of Pharmacy,Tongji Medical College,Huazhong University of Science and Technology,Wuhan,China 2.Department of Geriatrics,Union Hospital,Huazhong University of Science and Technology,Wuhan,China)

AIM Urtica dentata hand(UDH) are traditionally used in the alpine region as a herbal *** goal was to elucidate the cellular and molecular pathway and explore a method to quantify the total coumarins(TC) in *** We established a specific HPLC method to quantify TC in *** mechanism of TC in promoting immune tolerance was studied using dendritic cell(DC) and regulatory cell(Treg).RESULTS We described the ability of TC-conditioned DC,reduced capacity to stimulate effector T cell *** also found that PD-L1(programmed death ligand-1) that plays an inhibitory role in regulating T cell activation in the periphery,were up-regulated on DC by ***,TC-DC-stimulated Treg were superior alloantigenspecific suppressor of T effector response compared with those stimulated by control(CTR)-***,TC-conditioned DC increased levels of Foxp3 and CTLA-4 in the CD25 T cell ***-DC did not down-regulate TLR4 protein expression in response to *** shows that down-regulation of TLR4 in response to TC on DC is a critical signaling pathway that regulate DCs phenotype and *** also established a sensitive and specific high-performance liquid chromatography-diodearray detection-mass spectrometry(HPLC-DAD-MS) for simultaneous identification of its main coumarins,6,6',7,7'-tetramethoxyl-8,8'-biscoumarin(1 ), 7,7'-dihydroxy-6,6'-dimethoxy-8,80-biscoumarin(2),7,7'-dimethoxy-6,6'- biscoumarin(3),scoparone(4).CONCLUSION A demonstration of this mechanism and method for identification and quantification of TC in UDH endorses their potential as tolerance- promoting herbal medicine to prevent or treat transplantation rejection and autoimmune diseases.

关键词： Urtica dentata hand quantification dendritic cell Treg TLR4 signaling

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C-Jun N-terminal kinase/stress-activated protein kinase is critical for growth factors-induced angiogenesis in vitro and in vivo

C-Jun N-terminal kinase/stress-activated protein kinase is 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： Li-Li JI~(1,2*),Kai-Kai SHEN~1,Bin LU~1,Zheng-Tao WANG~(1,2) (1.The MOE Key Laboratory for Standardization of Chinese Medicines and The SATCM Key Laboratory for New Resources and Quality Evaluation of Chinese Medicines,Institute of Chinese Materia Medica,Shanghai University of Traditional Chinese Medicine,Shanghai 201210,China 2 Shanghai R&D Centre for Standardization of Chinese Medicines,Shanghai 201210,China)

AIM The present study was designed to obverse whether c-Jun N-terminal kinase/stress-activated protein kinase (JNK/SAPK) regulates the angiogenesis of human umbilical vein endothelial cells(HUVEC) induced by angiogenic growth factors. METHODS Cell proliferation,migration and tube formation were observed in HUVEC,and in vivo Matrigel plug assay was used. Western-blotting analysis was used to observe the related *** Vascular endothelial growth factor(VEGF) and basic fibroblastic growth factor(bFGF) both stimulated HUVEC proliferation,migration and tube formation in a concentration-dependent *** results showed that VEGF and bFGF induced the activation of JNK/SAPK,p38 kinase and extracellular signal-regulated kinase 1 and 2(ERK1/2),while JNK/SAPK inhibitor SP600125 and specific siRNA both blocked all those angiogenic effects induced by VEGF or ***,in vivo matrigel plug assay showed that SP600125 inhibited VEGF-induced ***, JNK/SAPK inhibitor SP600125 and specific siRNA inhibited VEGF or bFGF-induced JNK/SAPK signal cascade *** results showed that SP600125 and JNK/SAPK siRNA decreased VEGF-induced VEGFR2(Flk-1/KDR) sustained phosphorylation in *** Taken together,all these results indicates that JNK/SAPK signal pathway plays an important role in mediating growth factors-induced angiogenic responses,and thus JNK/SAPK is a potential target for drug development in angiogenesisrelated diseases such as cancer,diabetic retinopathy,etc.

关键词： c-Jun N-terminal kinase/stress-activated protein kinase vascular endothelial growth factor basic fibroblastic growth factor human umbilical vein endothelial cells angiogenesis

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MSL ameliorates cognitive deficits and inhibits inflammatory responses in amyloid β1-42-induced mouse model

MSL ameliorates cognitive deficits and inhibits inflammatory...

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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： Tian-Tai ZHANG,Xi LAN,Chao HUANG,Guan-Hua DU (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 Methyl salicylate 2-O-β-D-lactoside（MSL） is a novel NSAIDs of molecule chemically related to salicylic acid. It is isolated from a kind of traditional Chinese medicine,Gaultheria yunnanensis（FRANCH） *** roles of MSL in AS intracerebroventrical （i.c.v） injected mice model is studied to explore the effects of MSL on learning and memory functions and further study the mechanisms of neuroinflammation in *** ICR mice were pre-oral gavaged with MSL(75,150 and 300 mg·kg ) for 4 weeks,and then intracerebroventrical（i.c.v） injected with Aβ *** water maze and step-through passive avoidance behavior experiments were carried out to test the learning and memory functions of ***,AS secreting and GFAP, which represented for glial activation,were measured by ***,proteins of mice brain were collected to test the APP,iNOS,COX1/2 expression and the activation of NF-κB and MAPK signaling pathway by western *** proteins were used to study the release of pro-inflammatory cytokines level（IL-6,IL-1β,and TNF-α） by *** MSL ameliorates learning and memory deficits in AS treated mice at the dose of 300 mg·***,Aβ and APP expression are decreased significantly by the same dose of *** addition,pre-administrating with the dosage of 300 mg·kg,MSL not only suppresses the expression of GFAP in cortex and hippocampus,also shows a non-selective COX inhibitor activity in AB injected mice ***,it inhibits the phosphorylation of IKK,p38/MAPK and ERKAβ/MAPK and blocks the degradation of IκB, which causes the down regulation of pro-inflammatory cytokines（IL-6,IL-1β,and TNF-α） release and iNOS expression. CONCLUSION Pretreatment of MSL improves learning and memory in an AS injected mouse model and clear AB accumulation by inhibiting neuroinflammatory responses in central nervous system,including glia cells activation,COX1/2 expression and the transduction of NF-κB/ MAPK signaling pathway.

关键词： methyl salicylate 2-O-β-D-lactoside inflammation cognitive deficit NF-κB

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A novel drug binding site of cysteine-46 on IKK-beta kinase is responsible for suppression of IKK-β-NF-κB signaling and inflammation

A novel drug binding site of cysteine-46 on IKK-beta kinase ...

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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： Vincent Kam Wai WONG Yuen-Fan WONG State Key Laboratory of Quality Research in Chinese Medicine Macau University of Science and TechnologyAvenida Wai LongTaipaMacauChina Shum Yiu Foon Shum Bik Chuen Memorial Centre for Cancer and Inflammation Research School of Chinese MedicineHong Kong Baptist University

AIM To further investigate the new binding mode and action of mechanism of a novel IKK-βinhibitor which can specifically interact with new site on IKK-βand then suppress inflammatory conditions in vitro and in *** In vitro and in vivo studies of identification of the anti-inflammatory action and mechanisms of Compound B derived from a medical plant were *** biotinylated DMY(DMY-biotin) was synthesized as tool probe to confirm the direct interaction between DMY and IKK-βprotein,their protein adduct was detected by western blotting using biotin specific streptavidin-HRP ***-βdisplacement binding assay was used to confirm the novel drug binding site of DMY on IKK-β.RESULTS A novel drug binding site of IKK-βkinase at the Cys-46 residue was found,and the Cys-46 residue of IKK-βexhibited strong and unique capability of binding with small-molecule IKK-βinhibitor,Compound B derived from a medical plant,which potently suppressed in vitro and in vivo mouse inflammatory and rat arthritic ***-179 residue and ATP binding site have been known as drug targeting sites for most of the existing IKK-βinhibitors,while the new Cys-46 residue of IKK-βis able to bind with Compound B and then overcome the in vitro drug resistant phenotype of IKK-βmutants with mutations on the Cys-179 residue and ATP binding ***,finding of Cys-46 could provide insights of the new biochemical properties of IKK-βkinase as well as its mechanisms of *** new finding may also provide possibility of establishing a new platform for screening new IKK-β*** of novel kinase inhibitors with different inhibitory mechanisms or with new drug binding property has been evident in highly demand to circumvent the drug-resistant phenotypes of mutant kinases acquired from somatic gene mutations towards highly personalized therapy of ***,a number of gene mutations of IKBKB have been identified in human cancer genomes although with yet unkno

关键词： Cys-46 residue KK-β KK-β-NF-κB signaling Compound B and-inflammation

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