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Acta Pharmacologica Sinica 2004年第7期25卷 91-96页

作者： Yong-hong ZHANG2, Hai-yan PENG3, Guo-hao XIA3, Ming-yan WANG3, Ying HAN4 First Clinical College 3Basic Medicine College, nanjing University of TraditionalChinese Medicine, nanjing 210029 4jiangsu institute of Materia Medica, nanjing 210009, china First Clinical College Basic Medicine College Nanjing University of Traditional Chinese Medicine jiangsu institute of Materia Medica

AIM: To study the inhibitory effect of two diterpenoid compounds isolated from Annona glabra Linn (Cunabic acid and ent-kauran-19-al-17-oic acid) on the proliferation of Human Liver Cancer (HLC) cell line SMMC-7721 and its mechanism. METHODS: Inhibition of cell proliferation was measured by MTT assay. The morphological changes of SMMC-7721 cells were observed under inverted phase-contrast microscope, fluorescent microscope, transmission electron microscope (TEM), and scanning electron microscope (SEM). Flow cytometer (FCM) was used to calculate the cell apoptotic rate, and immunohistochemical staining was used to observe the regulation of gene expression. RESULTS: The proliferation of SMMC-7721 cells was obviously inhibited after being treated with Cunabic acid at the concentration >5 μmol/L and ent-kauran-19-al-17-oic acid >10 μmol/L. The biggest inhibitory effect was 81.05 % when treated with Cunabic acid at the concentration of 25 μmol/L. The effect had a linear relationship with concentration. The result indicated that drug-treated cells exhibit typical morphological changes of apoptosis, including condensed chromatin and a reduction in volume. Sub-G0/G1 peak was found by FCM analysis and the cell cycle was arrested at G0/G1 stage. The apoptotic rates of the cells treated by Cunabic acid and ent-kauran-19-al-17-oic acid were 43.31 % and 24.95 %, respectively. It was visualized by immunohis- tochemical staining that the drugs down-regulated the gene expression of bcl-2 gene and up-regulated that of bax gene. CONCLUSION: The two diterpenoid compounds isolated from Annona glabra Linn, Cunabic acid and ent- kauran-19-al-17-oic acid can obviously inhibit the proliferation of HLC cell line SMMC-7721. The mechanism is correlated with the induction of cell apoptosis by down-regulating the gene expression of bcl-2 gene and up- regulating that of bax gene.

关键词： Annona glabra Linn diterpenes hepatocellular carcinoma apoptosis gene expression

Fingerprint analysis of placenta polypeptide injection by high performance liquid chromatography

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Journal of Pharmaceutical Analysis 2012年第1期2卷 71-75页

作者： Li Huanga, Xiao-Man Wub, Yu Jib, Yu Wanga,bachina Pharmaceutical University, nanjing 210009, china bjiangsu institute for Food and drug control, nanjing 210008, china china Pharmaceutical University Nanjing 210009 China. jiangsu institute for Food and drug control Nanjing 210008 China.

Objective: To develop the representative fingerprint for the quality control of placenta polypeptide injection. Methods: The chromatographic separation was performed using a Phenomenex Gemini C18 column (250 mm 4.6 mm, 5 mm) maintained at 30 1C. 0.1% aqueous trifiuoroacetic acid (Solvent A) and acetonitrile contained 0.1% TFA (Solvent B) were used as mobile phase with a gradient elution. Detection wavelength was 280 nm with the sample injection volume of 50 mL; the fiow rate was 1.0 mL/min. The fingerprints of different samples were investigated by similarity analysis. Results: Nine peaks were identified as the characteristic common peaks. The similarities of the fingerprints of the 10 batches of samples were above 0.992. Conclusion: This method showed high precision and good repeatability, and provided the basis for the improvement of the quality control of placenta polypeptide injection.

关键词： Placenta polypeptide injection Fingerprint Similarity analysis High performance liquid chromatography

Metabonomic phenotype and identification of “heart blood stasis obstruction pattern” and “qi and yin deficiency pattern” of myocardial ischemia rat models

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Science china(Life Sciences) 2009年第11期52卷 1081-1090页

作者： YAN Bei1, A JiYe1, HAO HaiPing1, WANG GuangJi1, ZHU XuanXuan2, 3, ZHA WeiBin1, LIU LinSheng1, GUAN EnZe3, ZHANG Ying1, GU ShengHua1, HUANG Qing1 & ZHENG YuanTing1 1Key Laboratory of drug Metabolism and Pharmacokinetics, china Pharmaceutical University, nanjing 210009, china 2Pharmacological Laboratory of Clinical Research institute, jiangsu Provincial Hospital of Traditional Chinese Medicine, nanjing 210029, china 3College of Pharmacy, nanjing University of Traditional Chinese Medicine, nanjing 210029, china 1. Key Laboratory of drug Metabolism and Pharmacokinetics China Pharmaceutical University Nanjing 210009 China 2. Pharmacological Laboratory of Clinical Research institute Jiangsu Provincial Hospital of Traditional Chinese Medicine Nanjing 210029 China 3. College of Pharmacy Nanjing University of Traditional Chinese Medicine Nanjing 210029 China

The traditional Chinese medicine concepts of "Xinxueyuzuzheng (heart blood stasis obstruction pattern)" and "Qiyinliangxuzheng (qi and yin deficiency pattern)" for myocardial ischemia rat models were constructed in the present study. Endogenous metabolites in rat plasma were analyzed using the GC/TOF-MS-based metabonomic method. Significant metabolic differences were observed between the control and two model groups, and the three groups were distinguished clearly by pattern recognition. Compared with those of the control, the levels of hydroxyproline, threonic acid, glutamine and citric acid were strikingly up or down-regulated in model rats. The metabolites contributing most to the classification between the two "pattern" rats were identified, such as valine, serine, threonine, ornithine, hydroxyproline, lysine, 2-hydroxybutanoic acid, 3-hydroxybutanoic acid, galactofuranose and inositol. These compounds were indicated as the potential biomarkers. The results suggested that the two "patterns" are involved in dysfunction in oxidative stress, energy metabolism and amino acid metabolism. These findings also provided the substantial foundation for exploring the scientific connotation of these two "Zhengxing (pattern types)" of myocardial ischemia, and "Bianzheng (pattern identification)".

关键词： Metabonomics GC/TOF-MS heart blood stasis obstruction pattern qi and yin deficiency pattern myocardial ischemia rat model

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非理想状态下的塔板理论模型

色谱 2002年第1期20卷 30-33页

作者：王少坤夏芸汪圣利江苏省药品检验所江苏南京210008 江苏省疾病控制中心江苏南京210009 南京大学数学系江苏南京210008

在色谱过程中 ,将流动相看成是由许多连续的塔板组成 ,每一塔板的高度与固定相塔板的高度相同。初始浓度的溶质被认为全部集中在流动相的第一塔板中 ;溶质在流动相和固定相之间动态分布。由于色谱动力学因素的影响 ,当流动相流过一个塔... 详细信息

在色谱过程中 ,将流动相看成是由许多连续的塔板组成 ,每一塔板的高度与固定相塔板的高度相同。初始浓度的溶质被认为全部集中在流动相的第一塔板中 ;溶质在流动相和固定相之间动态分布。由于色谱动力学因素的影响 ,当流动相流过一个塔板距离时 ,溶质不能够迅速地从固定相释放到流动相中 ,因此溶质在流动相和固定相中的分布浓度受到两个因素即反映色谱系统热力学性质的分配系数P和反映色谱系统动力学性质的释放概率因子α的影响。这一过程被认为是非理想状态下的色谱过程。采用统计学的观点 ,综合分析了非理想状态下P和α对色谱分布的影响 ;利用计算机技术模拟了色谱分布曲线 ,最终建立了一种非理想状态下的塔板理论分布模型 ,推导出了非理想状态下色谱分布方程 ,提出了释放概率因子和分配系数对色谱结果共同作用的模式。结果表明色谱释放概率因子可以作为衡量色谱系统优劣的一个指数。

关键词：非理想状态塔板理论模型色谱释放概率因子

Synthesis of Two Nucleotide Derivatives with Phosphate Replaced by Vanadate

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Chinese Chemical Letters 1997年第5期8卷 401-402页

作者： De Ping XUE Ji Mei MIN Li He ZHANG Kui WANG(Coordination Chedstry institute,nanjing University,nanjing 210008)(National Laboratory of Natural and Biomboic drug,Beijing Medical University,Beijing 100083) nanjing UNIV INST COORDINAT CHEMNANJING 210008PEOPLES R CHINA BEIJING MED UNIV NATL LAB NAT & BIOMIM DRUGSBEIJING 100083PEOPLES R CHINA

Two kinds of vanadyl nucleotide were synthesized from vanadyl trichloride with adenosine derivatives.

关键词： DMSO 亚砜 MHz

Investigation of integrons/cassettes in antimicrobial-resistant Escherichia coli isolated from food animals in china

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Science china(Life Sciences) 2010年第5期53卷 613-619页

作者： SONG Li1,NING YiBao1,SHEN JianZhong2,FAN XueZheng,ZHANG ChunPing1,YANG ChengHuai1 & HAN JianFeng3 1 china institute of Veterinary drug control,Beijing 100081,china 2 china Agricultural University,Beijing 100094,china 3 china Center for Disease control and Prevention,Beijing 100050,china 1. china institute of Veterinary drug control Beijing 100081 China2. China Agricultural University Beijing 100094 China3. China Center for Disease Control and Prevention Beijing 100050 China

In this study,326 Escherichia coli isolates from food animals collected during the last four decades in china were characterized using antimicrobial susceptibility testing and screening for integrons/*** inhibitory concentration(MIC) testing indicated that the antimicrobial resistance of *** has increased since the *** findings of this study present a warning to veterinary practitioners about the excessive use of antimicrobials,and suggest the necessity for surveillance and control of antimicrobial resistance in veterinary clinical medicine in china.

关键词： E.coli Antimicrobial resistance integron/cassette last four decades

STUDY ON THE IMMOBILIZATION OF PAPAIN WITH A MACROPOROUS BEAD CARRIER OF COPOLYMER CONTAINING MONOMER UNITS OF NAMINOETHYL ACRYLAMIDE AND VINYL ALCOHOI

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Chinese Journal of Polymer Science 2000年第1期18卷 25-31页

作者： Yan-feng Li Jun-rong Li Lian-di Fu Yao-zeng Li Department of Chemistry, Lanzhou University, Lanzhou 730000, china Gansu Natural Energy Research institute, Lanzhou 730000, china Gansu Provincial institute of drug control, Lanzhou 730000, china 兰州大学甘肃兰州甘肃自然能源所甘肃兰州 730000 甘肃省药检所甘肃兰州 730000

A kind of macroporous bead carrier of copolymer containing monomer units of N-aminoethyl acrylamide and vinylalcohol was synthesized, i.e. the MR-AA carrier. Papain was immobilized on the carrier using glutaraldehyde as the couplingagent. The enzymatic activity of the immobilized papain was compared with free papain using casein as a substrate, and theeffects of glutaraldehyde concentration, pH, temperature, time and papain amount added on the activity recovery were alsoinvestigated. The results show that the MR-AA carrier contains reactive primary amine groups, hydrophilic amido links andhydroxyl groups, as well as macroporous structures based on its matrix (MR-AV matrix), furthermore, the activity recoveryof papain in the immobilization could reach 48%/～58%. In comparison with free papain, the resulting immobilized papainexhibits a remarkable thermostability and better reusability.

关键词： Immobilization Papain Proteolytic enzyme Macroporous bead carrier

Antihypertensive effects of total ginsenosides and regulation of the perturbed metabolism of spontaneously hypertensive rats

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Antihypertensive effects of total ginsenosides and regulatio...

Synthesis of N^(11)-anchoring biotinylated artemisinin derivatives and their preliminary biological assessment

第九届全国药物和化学异物代谢学术会议

作者： A Ji-ye~1,WANG Guang-ji~(1*),HAO Hai-ping~1,HUANG Qing~2,LU Yi-hong~2,YAN Bei~1, ZHA Wei-bin~1,GU Sheng-hua~1,ZHANG Ying~1,LIU Lin-sheng~1,CAO Bei~1,SHI Jian~1,LI Meng-jie~1, WANG Xin-wen~1,ZHAO Chun-yan~1,ZHANG Mei~2,FAN Xia-lei~2 1 Key Laboratory of drug Metabolism and Pharmacokinetics,china Pharmaceutical University,nanjing 210009, jiangsu,china 2 jiangsu institute for Food and drug control,nanjing 210008,jiangsu,china

AIM:Essential hypertension is inherently associated with metabolic disorders,and its pathogenesis remains poorly *** of the metabolic perturbation of hypertension and the regulation of this perturbed metabolism using therapeutic agents can extend our insight into the pathogenesis of this ***:We used gas chromatography mass spectrometry and principal component analysis to profile the metabolic phenotype of hypertension in spontaneously hypertensive rats(SHR) and studied the regulatory effect of total ginsenosides(TG) and four typical antihypertensive agents on in vivo ***:The five agents yielded different hypotensive effects and distinct regulation patterns on the perturbed metabolism that occurs in ***,amlodipine,and terazosin efficiently depressed systolic blood pressure(SP) but had a negligible regulatory effect on the perturbed metabolism of SHR,even after the remission of hypertension for 8 *** finding suggests that hypertension may not be the cause of the metabolism perturbation observed in these *** contrast,TG gradually and markedly regulated the perturbed metabolism, and led to a mild but sustained depression of SP up to 2 weeks after the cessation of ***, TG downregulated free fatty acids(FFA) toward normal levels;the elevation of FFA correlates with blood pressure,in both animals and ***:These results suggest that TG may act as a special antihypertensive agent that regulates the perturbed metabolism of hypertension.

关键词： metabonomics hypertension total ginsenosides spontaneously hypertensive rats free fatty acids

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Science china Chemistry 2010年第1期53卷 119-124页

作者： PAN QiYu1,2,WANG ShaoZhong1,LU JinJian3,MENG LingHua3 & YAO ZhuJun1,2 1nanjing National Laboratory of Microstructures(NNLM),School of Chemistry and Chemical Engineering,nanjing University,nanjing 210093,china 2Joint Laboratory of Green Chemistry,Department of Chemistry,University of Science and Technology of china,Hefei 230026,china 3State Key Laboratory of drug Research,Shanghai institute of Materia Medica,Shanghai institutes for Biological Sciences,Chinese Academy of Sciences,Shanghai 201203,china. 1. nanjing National Laboratory of Microstructures (NNLM) School of Chemistry and Chemical Engineering Nanjing University Nanjing 210093 China2. Joint Laboratory of Green Chemistry Department of Chemistry University of Science and Technology of China Hefei 230026 China3. State Key Laboratory of Drug Research Shanghai Institute of Materia Medica Shanghai Institutes for Biological Sciences Chinese Academy of Sciences Shanghai 201203 China

Unique endoperoxide moiety of artemisinin and its derivatives has been considered the functionality exhibiting highly potent antimalarial and anticancer *** investigate the mechanisms of their biological actions,development of suitable molecular probes including biotinylated derivatives is of extreme *** synthesis and preliminary biological assessment of four new biotinylated artemisinin derivatives have been reported in this work.

关键词： artemisinin endoperoxide biotinylated derivative synthesis anticancer activity