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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： Miao-Miao WU,Wen-Jie ZHAO,Yu-He YUAN,Nai-Hong CHEN (state key laboratory of bioactive substances and functions of natural medicines,Institute of Materia Medica, Chinese Academy of Medical Sciences,Beijing 100050,China )

AIM To investigate the effects and mechanism of polygalasaponin F（PS-F） on PC12 cellular apoptosis induced by 1-methyl-4-phenylpyridinium ion（MPP ）.METHODS The cell viability was evaluated using MTT *** cell apoptosis rate was analyzed using flow *** reactive oxygen species（ROS） was examined using DCFH-DA,the ATP depletion was examined using a luciferase-coupled quantification ***-1 staining was used to detect the mitochondrial membrane potential（MMP）. Western blot analysis was used to determine cytochrome c and caspase *** PS-F increased the viability of PC12 cells, decreased MPP -induced apoptosis,restored MPP -induced mitochondrial dysfunction and suppressed the expression of cytochrome c and active-caspase ***-F showed a dose-dependent manner in all the *** PS-F protects PC12 cells against MPP -induced apoptosis via ameliorating the mitochondrial ***,PS-F may be a potential bioactive compound for the treatment of Parkinson's disease.

关键词： polygalasaponin F neuroprotection 1-methyl-4-phenyl-pyridinium apoptosis

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A Trip from Basic Study on natural Medicine to Innovative Lipid-regulating Candidate Drug

A Trip from Basic Study on Natural Medicine to Innovative Li...

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2012年中美临床和转化医学国际论坛心脑血管病分会论坛（延吉）暨第十二届全国心血管药理学术会议和中俄药理国际研讨会

作者： Jin Li,Zeqin Lian,Yin Liu,Yao Wang,Haibo Zhu state key laboratory of bioactive substances and functions of natural medicines,& Ministry of Health key laboratory of Biosynthesis of natural Products,Institute of Materia Medica,Peking Union Medical College & Chinese Academy of Medical Sciences,Beijing 100050,China

Background: natural medicine,especially Chinese herbal medicine with specific curative effect,is an important source for new drug research and development. In our previous study,an active substance with lipid-regulati... 详细信息

关键词： Basic A Trip from Basic Study on natural Medicine to Innovative Lipid-regulating Candidate Drug

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JTN,an α-glucosidase inhibitor from Bombyx mori excreta exerts hypoglycemic effects and improves beta cell dysfunction in the IGT mouse models

JTN,an α-glucosidase inhibitor from Bombyx mori excreta exe...

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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： Quan LIU Shuai-Nan LIU Su-Juan SUN Zhu-Fang SHEN (Institute of Materia Medica Chinese Academy of Medical Sciences and Peking Union Medical College state key laboratory of bioactive substances and functions of natural medicines Diabetes Research Center of Chinese Academy of Medical Sciences Beijing 100050 China) Institute of Materia Medica Chinese Academy of Medical Sciences and Peking Union Medical CollegeState Key Laboratory of Bioactive Substances and Functions of Natural MedicinesDiabetes Research Center of Chinese Academy of Medical SciencesBeijing 100050China

＜正＞AIM To evaluate the impact of JTN on beta cell function in mice with impaired glucose tolerance（IGT）. METHODS Two animal models with IGT were chosen to evaluate the effect of JTN on beta cell *** MSG obese mice were induced with L-sodium glutamate,which have certain features of prediabetes,such as obesity,impaired glucose tolerance,beta cell *** mice characterized with impaired glucose tolerance and moderately *** of two IGT mouse models were randomly divided into five *** groups of IGT mice（n = 10） were fed for 45 d either a 50%sucrose diet（control） or a 50%sucrose diet supplemented with JTN 8,12,16 g or acarbose 0.3 g per kilogram *** glucose tolerance test（OGTT） and insulin tolerance test were *** plasma glucose,TG,TCHO and insulin level were measured at the end of the supplementation. Blood pressure and cataracta of eyes in MSG mice were *** beta cell function was quantified using a hyperglycemic *** After 7 weeks of supplementation,JTN flatted blood glucose peak and reduced the AUG during OG’IT compared with the control ***-βindex was significantly higher in JTN *** supplementation of JTN improved insulin sensitivity in both MSG and KKAy *** also decreased the fasting plasma glucose and *** hyperglycemic clamps,JTN increased glucose infusion rate（GIR） with dose-dependent fashion in MSG and KKAy mice,which indicated the improved beta cell insulin secretory *** the end of experiment,JTN also reduced the incidence of cataract in MSG *** These results suggested that JTN showed beneficial effect on glucose,lipid metabolism and the diabetic complication which were due to the improvement in insulin sensitivity and beta cell function.

关键词： Bombyx mori excreta impaired glucose tolerance beta cell function hyperglycemic clamp

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Variations in lipoprotein profiles of difference species,analyzed by a fluorescence detection combined FPLC technique

Variations in lipoprotein profiles of difference species,ana...

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中国药理学会第十一次全国学术会议

作者： YANG Liu,ZHU Hai-bo (state key laboratory for bioactive substances and functions of natural medicines,Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College,Beijing 100050,China)

Different animal models have been used to study the pathomechanisms involved in dyslipidemia and evaluate the effect of drugs on serum ***,most of these models differ from human beings in the responses to high-fat and high-cholesterol diet, this may be caused by variations in lipoprotein distribution among different *** profiles of different dyslipidemia animal model have not been explored systematically due to the lack of an appropriate *** ultra-centrifugal lipoprotein separation technique and the commonly used liquid chromatography methods both have their disadvantages in lipoprotein separation,lipoprotein and lipid component quantification. In this study,we combined small volume needed size-exclusion fast protein liquid chromatography（FPLC） and fluorescence lipids measurement,accomplished the determination of serum lipoprotein profiles in C57 BL/6 Mice,ApoE Mice,SD Rats,Golden Hamster,Guinea Pigs,Rabbits,Miniature Pigs and Human *** results demonstrated that there were considerable variations in the FPLC spectrum,lipoprotein distribution and lipoprotein subclasses/lipoprotein ratio among these different *** dyslipi-demia patients,decreased high density lipoprotein（HDL）/lipoprotein ratio and increased low density lipoprotein（LDL）/lipoprotein ratio were observed,but it was found that the changes of HDL/lipoprotein and LDL/lipoprotein ratios in SD Rats after high - fat and high-cholesterol diet were totally different with Human Beings,meanwhile,its HDL/Lipoprotein ratio was increased,and LDL/Lipo-protein ratio was *** Golden Hamster,Miniature Pigs and Human Beings have much in common in lipoprotein distribution and response to high-fat and high-cholesterol *** was the first time that two different size-exclusion columns were combined and used to separate small volume individual serum *** fluorescence detection methods were used to measure lipid components in the eluted lipo

关键词： lipoprotein lipids FPLC dyslipidemia animal models different species atherosclerosis

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Synthesis of Novel D-Seco Paclitaxel Analogues

Synthesis of Novel D-Seco Paclitaxel Analogues

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2011年全国药物化学学术会议——药物的源头创新

作者： Shaorong Wang,Chungang Yang,Weishuo Fang state key laboratory of bioactive substances and functions of natural medicines & Ministry of Health key laboratory of Biosynthesis of natural Products,Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College,Beijing 100050, China

oxetane D ring was initially believed to be essential for the biological activity of Paclitaxel(1).In the Past decade,numerous efforts have been made to delineate its eontribution to the

关键词： Synthesis of Novel D-Seco Paclitaxel Analogues

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Atorvastatin improves pancreaticβ-Cell function and survival in obese C57BL/6J mice

Atorvastatin improves pancreaticβ-Cell function and surviva...

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中国药理学会第十一次全国学术会议

作者： CHEN Zhi-yu,LIU Jing-long,SHEN Zhu-fang (state key laboratory of bioactive substances and functions of natural medicines,Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College,Beijing 100050,China)

OBJECTIVE Atorvastatin is first-line lipid-lowering drug for patients of cardiovascular disease,metabolic syndrome and type 2 diabetes ***,the relation of statins and incidence of diabetes mellitus is controversial through clinical trials. Thus,we examined the effects of Atorvastatin on Obese C57BL/6J mice and possible *** ITT were performed to detect whether insulin resistance were *** clamp was used to explore the function of pancreaticβ-*** mRNA and protein level were determined by Real time PCR and Western *** metabolic activity and apoptosis investigation was done by CCK-8 and flow cytometry,respectively,on the cholesterol induced ER stress model of NIT-1 *** We found that Atorvastatin improved the insulin sensitivity,increased glucose infusion rate(GIR) in the hyperglycemic ***, plasma TG,CHO and pancreas TG were *** mRNA levels of pancreatic and duodenal homeobox 1(PDX-1) and Liver X receptorβ(LXR-β) were *** production of PDX-1 was improved,*** stress markers such as phosphorylation of eukaryotic initiation factor 2α(EIF2α) and activating transcription factor 4(ATF4) protein were *** exhibited beneficial effects on metabolic activity and protected NIT-1 cells from *** In a word,Atorvastatin showed positive effects on insulin sensitivity,insulin secretion,pancreatic proliferation and attenuation of ER ***,it is able to increasesβ-cell survival which provides a supportive data for curing diabetes.

关键词： statins diabetes mellitus insulin sensitivity pancreaticβ-cell function β-cell survival ER stress

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Effects of Atorvastatin and Pravastatin on Pancreatic β-cell Function and Their Underlying Mechanisms

Effects of Atorvastatin and Pravastatin on Pancreatic β-cel...

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第五届中日基础和临床药理学双边学术会议

作者： Zhiyu Chen,Lei Lei,Sujuan Sun,Shuainan Liu and Zhufang Shen state key laboratory of bioactive substances and functions of natural medicines, Institute of Materia Medica,Chinese Academy of Medical Sciences and Peking Union Medical College,Beijing 100050,P.R.China

Atorvastatin and pravastatin are both 3-hydroxy-3-methylglutaryl coenzyme A reductase *** are used as first-line lipid-lowering drugs for patients of cardiovascular disease,metabolic syndrome and type 2 diabetes *** many researches have shed light on the relations between statins and incidence of diabetes mellitus,the mechanisms onβ-cell function remains ***,we evaluated the effects of the two statins on pancreaticβ-cell function on the high-fat diet induced insulin

关键词： Effects of Atorvastatin and Pravastatin on Pancreatic cell Function and Their Underlying Mechanisms

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Selectivity evaluation method of DPP-Ⅳ inhibitors based on recombinant DPP8

Selectivity evaluation method of DPP-Ⅳ inhibitors based on ...

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第五届中日基础和临床药理学双边学术会议

作者： Jinglong Liu Linyi Li Yi Huan Zhiyu Chen Lei Lei and Zhufang Shen~* state key laboratory of bioactive substances and functions of natural medicines, Institute of Materia Medica,Chinese Academy of Medical Sciences and Peking Union Medical College,Beijing 100050,P.R.China

The dipeptidyl peptidase(DPP)-Ⅳinhibitors are a new class of antihyperglycaemic *** a member of dipeptidyl peptidases in the S9b gene family,DPP8 is more similar in tissue distribution,kinetic and substrate with DPP-Ⅳ.Many data indicate that DPP8 plays physical roles in T-cell activation and other immune *** means nonselective DPP-Ⅳinhibitors will produce potential side effects related to ***,

关键词： Selectivity evaluation method of DPP inhibitors based on recombinant DPP8

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High performance liquid chromatographic separation of thirteen drugs collected in Chinese Pharmacopoeia 2010(Ch.P2010) on cellulose ramification chiral stationary phase

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Journal of Pharmaceutical Analysis 2012年第1期2卷 48-55页

作者： Ying Zhoua,b, Chao Maa, Yan Wanga, Qi-Ming Zhangb, Yi-Ying Zhanga, Jie Fua, Hong Gaoc, Li-Xun Zhaoc astate key laboratory of bioactive substances and functions of natural medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China bNational Institute for the Control of Pharmaceutical and Biological Products, Beijing 100050, China cInstitute of Medicinal Biotechnology, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China State Key Laboratory of Bioactive Substances and Functions of Natural Medicines Institute of Materia Medica Chinese Academy of Medical Sciences & Peking Union Medical College Beijing 100050 China. National Institute for the Control of Pharmaceutical and Biological Products Beijing 100050 China. Institute of Medicinal Biotechnology Chinese Academy of Medical Sciences & Peking Union Medical College Beijing 100050 China.

The enantiomers separation of thirteen drugs collected in Ch.P2010 was performed on chiral stationary phase of cellulose ramification (chiralpak OD and chiralpak OJ) by high performance liquid chromatographic (HPLC) methods, which included ibuprofen (C1), ketoprofen (C2), nitrendipine (C3), nimodipine (C4), felodipine (C5), omeprazole (C6), praziquantel (C7), propranolol hydrochloride (C8), atenolol (C9), sulpiride (C10), clenbuterol hydrochloride (C11), verapamil hydrochloride (C12), and chlorphenamine maleate (C13). The mobile phase consisted of isopropanol and n-hexane. The detection wavelength was set at 254 nm and the fiow rate was 0.7 mL/min. The enantiomers separation of these thirteen racemates on chiralpak OD column and chiralpak OJ column was studied, while the effects of proportion of organic additives, alcohol displacer and temperature on the separation were studied. And the mechanism of some of racemates was discussed. The results indicated that thirteen chiral drugs could be separated onchiral stationary phase of cellulose ramification in normal phase chromatographic system. The chromatographic retention and resolution of enantiomers could be adjusted by factors including column temperature and the concentration of alcohol displacer and organic alkaline modifier in mobile phase. It was shown that the resolution was improved with reducing concentration of alcohol displacer. When concentration of organic alkaline modifier was 0.2% (v/v), the resolution and the peak shape were fairly good. Most racemates mentioned above had better resolution at column temperature of 25 1C. When racemates were separated, the temperature should be kept so as to obtain stable separation results.

关键词： HPLC Chiral stationary phase Optical enantiomers Cellulose ramification

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