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Isolation,characterization and cytotoxic activity of benzophenone glucopyranosides from Mahkota Dewa[Phaleria macrocarpa(Scheff.) Boerl]

Isolation,characterization and cytotoxic activity of benzoph...

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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： Yue-Feng BIA School of Pharmaceutical Science Zhengzhou University New Drug Research and Development Center Zhengzhou University

AIM Mahkota Dewa（Phaleria macrocarpa[Scheff.]Boerl）,with effects on antihistamine,anti-oxidation and anticancer, has been used to treat many diseases,including cancer,impotency,haemorrhoids and diabetes *** current study is designed to further understand and develop Mahkota Dewa for cancer treatment *** AND RESULTS Two benzophenone glucopyranosides were isolated from the nut shell part of Mahkota *** structures were identified as 2,4',6-trihydroxy -4-methoxy-benzophenone-2-O-β-D-glucoside（Mahkoside A） and 2,4',6-trihydroxy-4-methoxy-6"-acetyl-benzophenone-2-O-β- D-glucoside（Mahkoside B） NMR,HR-MS and *** B was recognized as a novel ***,a series of benzophenone glucopyranoside derivatives（Compounds 3-18） were *** order to determine the relationship of structure and activity of the compounds above,several cancer cell lines,including esophageal cancer cell lines;EC109 and EC9706,stomach cancer cell line:MGC-803 and prostate cancer cell line:PC-3,were randomly selected and cytotoxic activity was evaluated according to the standard SRB（sulforhodamine B） *** results indicated that Compound 18 has significant cytotoxicity against EC109, EC9706,MGC-803 and PC-3,with IC≤10μmol·L,indicating its potential activity against cancer *** We found that a new derivative of Mahkoside A:Compound 18,demonstrated significant cytotoxicity against cancer cell *** studies will be performed to generate and characterize more derivatives with azotic alkyl group and analyze their structure-effect relationships.

关键词： Mahkota Dewa benzophenone glucopyranoside synthesis bioactivity

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Correlation of Chinese medicine ingredients and over-released neurotransmitters in rats' brain interstitial fluid during cerebral ischemia

Correlation of Chinese medicine ingredients and over-release...

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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： Wen-Ting SONG~1,Jian-Xun LIU~1,Ying ZHANG~1,Jin-Cai HOU~1,Li XU~1 (Experimental Research Center,Xiyuan Hospital,China Academy of Chinese Medical Sciences,Beijing 100091,China)

AIM To study correlation of medicine ingredients and neurotransmitters in brain interstitial fluid（BIF） of cerebral ischemic *** Sprague-Dawley rats（n= 12） were randomized into two *** in SLT（Sailuotong capsule） group were administrated with SLT(150 mg·kg ) by gavage and model rats were administrated with distilled water for 7 d before middle carotid artery occlusion（MCAO）.Rats' BIF samples were collected by microdialysis and rats suffered from permanent cerebral ischemia during sampling under isoflurane ***-MS/MS was employed for medicine ingredients detection while HPLC-ECD system for neurotransmitter *** study was pursued for the correlation of certain endogenous and exogenous substances in rats'*** Three medicine ingredients from SLT were detected by LC-MS/MS,namely bilobalide（BB）,crocin and ginkgolide A（GA）.These ingredients comes from Folium Ginkgo and Stigma Croci,which are two herbs composition of *** neurotransmitters were determined by HPLC-ECD system,namely serotonin（5-HT）,dopamine（DA）,glutamate（Glu）,γ-amino butyric acid（GABA）.Neurotransmitter levels in rats BIF of SLT group were significantly lower than that of model *** correlation analysis showed that dynamic change of BB and GA were highly correlated with four neurotransmitter level changes. CONCLUSION SLT down-regulate both monoamines and amino acids levels,which increase dramatically after rats subjected to *** suggests,maybe,SLT protect ischemic brain by down regulating over-released *** aided correlation study suggests BB and GA are the most likely effective ingredients for regulating the neurotransmitters.

关键词： ischemia neurotransmitter bilobalide ginkgolide A

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Nobiletin,a citrus flavonoid improves memory disorder in Alzheimer's disease model animals - its application to functional foods

Nobiletin,a citrus flavonoid improves memory disorder in Alz...

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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： Yasushi OHIZUMI Graduate School of Engineering Tohoku University6-6-07-715 AobaAramakiAoba-kuSendai 980-8579Japan Graduate School of Pharmaceutical Sciences University of Shizuoka52-1 YadaSuruga-kuShizuoka 422-8526Japan Yokohama College of Pharmacy 601 Matano-choTozuka-kuYokohama 245-0066Japan

AIM We have demonstrated for the first time that nobiletin(NB) from citrus peels improves memory impairment in Alzheimer's disease(AD) model *** AND RESULTS Amyloid precursor protein(APP) transgenic(Tg) mice have been extensively used as an indispensable AD model *** markedly improved memory deficits and caused a great decrease in the Aβburden and plaques in the hippocampus in Tg *** the other hand,olfactory-bulbe etomized(OBX) mice have been widely utilized as a useful paradigm that shares some major clinical features of *** rescued greatly memory deficits accompanied by the OBX-indused decrease in the density of AChE-positive *** cultured hippocampal neurons Aβinhibited both CREB phosphorylation and CRE-mediated transcription stimulated by *** antagonized both of the inhibitory effects of *** These results suggest that NB decreases the Aβburden and plaques in the hippocampus and reverses the Ap-induced inhibition of CREB-mediated signaling coupled with CRE-dependent transcription,resulting in improvement of learning *** is also suggested that nobiletin has become a useful natural compound for functional food development for AD.

关键词： nobiletin citrus peels Alzheimer's disease CRE-mediated transcription functional food development

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Hawthorn leaves flavonoids decreases inflammation related to acute myocardial ischemia/ reperfusion in anesthetized dogs

Hawthorn leaves flavonoids decreases inflammation related to...

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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： Yong-Qiu ZHENG,Jian-Hua FU,Peng LI,Xin-Zhi LI,Xiao-Hong SHANG, Jian-Xun LIU (Xiyuan Hospital of China Academy of Chinese Medical Sciences,Beijing 100091,China)

AIM To investigate the effects and mechanisms of hawthorn leaves flavonoids（HLF） on acute myocardial ischemia/ reperfusion in anesthetized *** The acute ischemia models were prepared by ligating left anterior descending（LAD） artery for 60 *** 15 male dogs were divided into 3 groups at random（5 in each group）:blank control(treated with normal saline 3 ml·kg) group,HLF 5 and 10 mg·kg group,with an once injection through a femoral vein 5 min before *** experiments adopted epicardial electrocardiogram（EECG） to measure the scope and degree of myocardial ***, neutrophil infiltration in infarct（Inf） and remote site（RS） of myocardial tissue was measured by myeloperoxidase（MPO） activity *** serum interleukin-1（IL-1） and tumor necrosis factorα（TNF-α） content was quantified by ***, expression of G protein-coupled receptor kinase 2（GRK2） and NF-κB in Inf and RS tissue were detected by Western blotting. RESULTS Ischemia and reperfusion increased the MPO activity and IL-1 and TNF-α*** showed that HLF 10 and 5 mg·kg could significantly decrease the degree and scope of myocardial ischemia;markedly inhibit the increase of MPO activity,and IL-1 and TNF-αcontent induced by myocardial ischemia/***,HLF increased GRK2 expression and inhibited NF-κB expression in Inf *** HLF could improve the situation of acute myocardial ischemia and inhibit the inflammation in dogs,which might be due to its increasing the GRK2 and NF-κB expression.

关键词： hawthorn leaves flavonoids acute myocardial ischemia reperfusion injury inflammation G protein-coupled receptor kinase 2

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Protective effect of Eucalyptus globulus oil on acute and chronic lung inflammation in rats

Protective effect of Eucalyptus globulus oil on acute and ch...

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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-Zhen ZHAO,Jian-Ya ZHOU,Wei ZHAO,Yan WANG,Fa-Di TANG (Zhejiang Respiratory Drugs Research Laboratory,College of Medicine,Zhejiang University, Hangzhou 310058,China)

AIM The effects of Eucalyptus globulus oil（EO） were studied on airway inflammation of chronic obstructive pulmonary disease（COPD） and acute lung injury（ALI） in *** COPD was induced by instilling intratracheally with LPS and Klebsiella pneumonia,and ALI was induced by instilling intratracheally with *** were divided into six groups:control（saline）, model group,EO(30,100 and 300 mg·kg,ig),prednisone acetate(10 mg·kg,ig).RESULTS The total leukocyte number in BALF were singnificantly reduced with 300 mg·kg group in acute inflammation of ALI,while in chronic inflammation of COPD,the inflammatory cells in BALF and blood were significantly decreased with 30,100 mg·kg *** is characterized by emphysema and irreversible airway narrowing,and EO group attenuated emphysematous alveolar destruction and thickness of bronchioles. EO 300 mg·kg group obviously decreased expression of activated NF-κB in rat lung tissues of ALI and in vitro inhibited nuclear translocation of NF-κB in alveolar macrophages from ALI *** The most remarkable finding of this study is that EO, characterized by anti-inflammatory and antioxidant property,defended the development of emphysema and remodeling of small airways induced by intratracheal instillation of LPS and Klebsiella pneumonia in *** significantly reduced inflammatory response in both pulmonary and systemic levels,inhibited oxidative stress and regulated antioxidantive transcription factor Nrf2 expression in emphysematous lungs of *** EO protected against LPS-induced inflammatory cell infiltration in lungs of rats possibly through molecular mechanisms of inhibition of NF-κB *** vitro study suggested that EO inhibited nuclear translocation of NF-κB in alveolar macrophages.

关键词： Eucalyptus globulus oil chronic obstructive pulmonary disease acute lung injury inflammation NF-κB

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Effects of an extraction of Rhodiola crenulata on insulin resistance in KKAy mice

Effects of an extraction of Rhodiola crenulata on insulin re...

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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： Fei YE,Jin-Ying TIAN,Xiao-Lin ZHANG,Ling CHEN,Jing HAN,Juan LI,Jian-Yang FU, Pei-Cheng ZHANG,Huan-Ling WEI (Institute of Materia Medica,Chinese Academy of Medical Sciences,Beijing 100050,China)

AIM To investigate the effects of an extraction of Rhodiola crenulata（ERC） on type 2 diabetes mellitus（T2DM） by improving insulin *** The spontaneous T2DM model KKAy mice were treated with *** glucose tolerance was estimated by oral glucose tolerance tests（OGTT）.The insulin resistance was evaluated by insulin tolerance tests（ITT）,the glucose infusion rate（GIR） in hyperinsulinemic-euglycemic clamp tests,the whole-body insulin sensitivity index（ISWBI）,the serum insulin level,and the homeostasis model assessment of insulin resistance（HOMA-IR）,*** hepatic protein expressions were estimated by western *** recombinant human protein tyrosine phosphatase 1B（PTP1B） was prepared and used for the measurement of PTP1B activity in *** The hyperglycemia and glucose intolerance in KKAy mice were improved significantly by the administration of ERC(200 mg·kg) *** the ERC-treated mice,the changes of blood glucose after the insulin loading in ITT were enhanced and its AUC value was reduced by 32.8%;the level of GIR was increased by 2.8 folds;the value of ISWBI was enhanced by 1.7 folds;the levels of serum insulin and HOMA-IR were decreased by 19.1%and 31.5%,respectively, compared with those in KKAy model control *** effects of ERC on insulin resistance was associated with insulin signaling pathway,especially,showed strongly inhibition on PTP1B activity with EC of 1.161 rng·L in vitro and on PTP1B expression in the liver of KKAy mice by 30.0%decrease in *** Targeting on PTPIB,ERC can treat T2DM by improving insulin resistance in KKAy mice.

关键词： Rhodiola crenulata protein tyrosine phosphatase 1B type 2 diabetes mellitus

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MD-15 inhibiting the contraction effects of isolated intestinal smooth muscle of rat caused by acetylcholine

MD-15 inhibiting the contraction effects of isolated intesti...

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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： Fu-Hou CHANG,Chao LIU,Zhao-Jun CHEN,Tu-Ya BAI,Xiao-Li LU (College of Pharmacy,Inner Mongolia Medical University,Hohhot 010110,China)

AIM To observe the influence of Mongolian traditional medicine DAGEBU-15（MD-15 ） to the contraction effects of isolated intestinal smooth muscle of rat caused by acetylcholine（ACh）.METHODS Isolated intestinal perfusion method was used to record the rat intestinal muscle tension by JH-type 2 and BL-420 biological function ***'s perfusion fluid with gas mixture of 95%O and 5%CO,temperature is（37±1）℃.The semilogarithmic molar concentration cumulative administered method was used. Administering in proper order according to the following sequence of concentration of ACh without or with MD-15,the concentration of MD-15 was 1 mg·L and 10 mg·*** ACh concentrations of Magnus' bath were 1×10 mol·L,1×10 mol·L, 1×l0 mol·L,1×l0 mol·L and 1×l0 mol·L,*** and recorded the changes in contraction after *** solution need not be changed each *** the contraction of intestinal smooth muscle is stable,add the next concentration *** largest percentage of contraction effect caused by ACh was y-coordinate,the logarithm molar concentration of ACh（- lg[D]） was as abscissa and drew dose-response *** MD-15 of each dose group make the cumulative dose-response curve of ACh shifted to the right and the maximum responses were ***-15 was an non-competitive antagonist of *** maximum responses caused by ACh with 1 and 10 mg·L MD-15 was（81.74±11.22）%and（75.90±16.79）%of the maximum responses caused by ACh without MD-15,*** MD-15 can inhibit the contraction effect of small intestinal smooth muscle of rats.

关键词： Mongolian traditional medicine acetylcholine isolated intestinal smooth muscle dose-response curve

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Apigenin enhances sensitization of BEL-7402/ADM cells to therapeutic drugs via inhibiting PI3K-AKT/Nrf2/ARE pathway

Apigenin enhances sensitization of BEL-7402/ADM cells to 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

作者： Ai-Mei GAO~(1,2),Zun-Ping KE~3,Xuan-Bin WANG~2,Jia-Ning WANG~3,Hui CHEN~(1*) (1.Department of Pharmacology,Tongji Medical College,Huazhong University of Science and Technology, Wuhan 430030,China 2.Laboratory of Chinese Herbal Pharmacology,Renmin Hospital, 3.Institute of Clinical Medicine and Department of Cardiology,Hubei University of Medicine,Shiyan 442000,China)

AIM Nuclear factor erythroid 2-related factor 2(Nrf2) is a redox-sensitive transcription factor which regulates the expression of a battery of cytoprotective *** this study,we investigated whether Nrf2 was associated with drug resistant in doxorubicin resistant BEL7402(BEL-7402/ADM) cells,and if apigenin(APG) could reverse drug resistance in BEL-7402/ADM cells. METHODS Reverse of drug resistance was assayed by MTT and fluorometric *** of Nrf2 signaling pathway by APG was detected through real-time quantitative PCR and Western blot *** At physiological concentrations,APG significantly sensitized BEL-7402/ADM cells to doxorubicin,cisplatin,vincristine and ***,knock-down of Nrf2 using siRNA essentially abolished the enhanced sensitivity by APG,implying the importance of inhibiting Nrf2 for its cytotoxic ***, APG increased intracellular drug concentration in a dose-dependent manner by inhibiting Nrf2 ***,APG dramaticly reduced Nrf2 expression at both the mRNA and protein levels through down-regulating PI3K-AKT ***, expression of Nrf2-downstream genes HO-1,AKR1B10,and MRP5 was *** APG can reverse drug resistance via inhibiting PI3K-AKT/Nrf2/ARE pathway,indicating the effectiveness of using APG as a adjuvant sensitizer to combat chemoresistance.

关键词： apigenin Nrf2 hepatocellular carcinoma chemosensitization

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Molecular mechanism of Liu-Wei-Di-Huang decoction improving age-related cognitive deterioration

Molecular mechanism of Liu-Wei-Di-Huang decoction improving ...

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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-Rui CHENG,Sheng YANG,Wen-Xia ZHOU~*,Yong-Xiang ZHANG (Beijing Institute of Pharmacology and Toxicology,Beijing 100850,China)

AIM Data from clinic trials showed Liu-Wei-Di-Huang decoction(LW) enhanced cognitive processing in normal young adults and improved age-related cognitive *** study aims to investigate the molecular mechanism of LW improving learning and memory deterioration empolying senescence accelerated mouse prone 8(SAMP8).METHODS The ability of learning and memory of SAMP8 administrated LW were examed by step up and down test,shuttle-box test,and morris-water maze *** expression was investigated using cDNA microarray and *** techniques were used to analyses biomolecule interaction *** The chronic administration of LW to SAMP8 enhanced the memory registration and retention ability in passive avoidance performance,promoted the spatial memory ability in the water maze test and partially improved the leaning behavior in conditioned avoidance *** are 39 gene expression in hippocampus and 52 genes expression in cerebral cortex regulated by *** genes involved in the biomolecular network with 384 nodes and 383 edges,characteristic path length 4.416 and network heterogeneity *** mainly effected on pathways with nodes RPS6KA1,TICAM2,MAST2,NRXN1,NSF,STUB1 and ***,RPS6KA1,SLC17A7 and FHIT may be direct targets for LW improving age-related with cognitive deterioration. CONCLUSION LW enhanced cognitive processing via regulating the biomolecular network with 384 nodes and 383 edges,and its direct targets may be RPS6KA1,SLC17A7 and FHIT.

关键词： Liu-Wei-Di-Huang decoction senescence accelerated mouse learning and memory biomolecular network

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ZX-1201 inhibits pancreatic cancer cell PANC-1 epithelial-mesenchymal transition by targeting aquaporin-1 and transforming growth factor-β1

ZX-1201 inhibits pancreatic cancer cell PANC-1 epithelial-me...

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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： Yu AN~(1,2),Ye-Fan WANG~(1,2),Yu ZHANG~2,Xue-Jun LI~(1,2) (1.State Key Laboratory oj Natural & Biomimetic Drugs,Department of Pharmacology,School of Basic Medical Sciences,2.Institute of Systems Biomedicine,Peking University,Beijing 100191,China)

AIM Our present study aimed to test the anti-cancer effect of natural product ZX-1201 on pancreatic cancer cell *** After incubation with different concentrations of drug or vehicle,PANC-1 cell viability was measured by MTS assay,and Scratch assay and Transwell assay were utilized to detect PANC-1 cell ***,morphological changes were recorded by light ***-time PCR,immunofluorescence and Western blot were used to examine change of aquaporin-1 （AQP1） and TGF-β related EMT *** addition,we performed AQP1 and TGF-β RNAi and over-expression experiments to elucidate their role in anti migration effect of *** We found ZX-1201 showed significant inhibitory effect on cell migration in a dose-dependent manner,however,slight cell viability suppression was ***,we demonstrated ZX-1201 could prevent PANC-1 cell from epithelial-mesenchymal transition（EMT）,by reducing mesenchymal phenotype,decrease AQP1 and TGF-β expression,and dramatically down-regulating EMT markers and signaling ***,we verified that ZX-1201 reversed EMT by targeting AQP1 and TGF-β,because either AQP1 or TGF-β over-expression abolished the inhibitory effect of ZX-1201 on *** ZX-1201 significantly inhibits pancreatic cancer cell PANC-1 EMT process through an AQP1 and TGF-β targeting manner.

关键词： ZX-1201 pancreatic cancer PANC-1 epithelial-mesenchymal transition aquaporin-1 transforming growth factor-β1

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