最新刊期
      卷 31 ， 期 2 ， 2020
      • YANG Shujie,WU Zhi ’ang
        Vol. 31, Issue 2, (2020)
        摘要：OBJECTIVE：To provide reference for optimizing resource allocation and precise investment of China ’s pharma- ceutical industry. METHODS ：The number of invention patent applications in China ’s pharmaceutical industry was searched from China Intellectual Property Netwerk ，and the status quo and structure of patent applications in China ’s pharmaceutical industry were analyzed. SPSS 23.0 software was used to analyze the input-output correlation of the number of invention patent applications with R&D investment and main business income of pharmaceutical enterprises in China. RESULTS ：The number of invention patent applications in China ’s pharmaceutical industry increased year by year. From 2000 to 2015，225 861 invention patents had been applied by domestic applicants and 43 149 invention patents had been applied by foreign applicants in China ；only 49.94％ domestic applicants applied for professional invention ，while 96.79％ of foreign applicants applied for professional invention. There was a positive correlation between the R&D expenditure of pharmaceutical enterprises and the number of invention patent applications，which indicated that the R&D investment of pharmaceutical industry in China was beneficial to the invention patent applications. The number of invention patent applications of pharmaceutical enterprises was also positively correlated with the main business income ，indicating that the increase of invention patent applications of pharmaceutical enterprises also effectively expanded the economic scale of pharmaceutical industry. CONCLUSIONS ：Compared with foreign countries ，the structure of patent applicants in domestic pharmaceutical industry needs to be adjusted urgently. Pharmaceutical enterprises have not yet become the main applicants. The continuous R&D investment of pharmaceutical enterprises effectively promotes the application of invention patent，expanded the economic scale of the pharmaceutical industry.  
        关键词：Invention patent;Patent application;Pharmaceutical enterprise;Input-output;R&D   
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        发布时间：2022-06-21
      • WANG Huiguo,LI Dan,SUN Yingchao,LI Yutong,HAN Xinlong,ZHANG Jingying,TANG Ling
        Vol. 31, Issue 2, (2020)
        摘要：OBJECTIVE：To investigate the effects of dihydroartemisinin （DHA）on the metabolism of amino acid metabolites in human hepatocellular carcinoma cells Huh 7 and BEL- 7402，and to provide theoretic basis for clarifying the mechanism of DHA regulating the metabolism of hepatocellular carcinoma cells. METHODS ：CCK-8 method was taken to detect the effect of different concentrations of DHA （12.5，25，50，100 µmol/L）treating for 24，48，72 h on the two kinds of cells. Two kinds of cells were divided into control group and administration group （DHA，25 µmol/L），and then cultured with drug-free or drug-containing medium for 24 h，operated in parallel for three times. After derivatization of cell samples in each group ，GC-MS method was used to detect the content of amino acid metabolites ，combined with SIMCA-P software analysis and compound library comparison ，the differential metabolites in two kinds of cells were screened out. The pathway enrichment analysis of differential metabolism was conducted with Metaboanalyst 4.0 software. RESULTS ：Compared with control group ，the contents of glutamine ，glutathione， phenylalanine，fumaric acid and taurine were trending down in Huh 7 or BEL- 7402 cells. There were 28 and 29 differential metabolites obtained from the above two kinds of cells ，and 10 of them were common differential metabolites ，including glutamine，glutathione，taurine，fumaric acid ，phenylalanine，etc. The differential metabolites were enriched in 8 and 6 pathways respectively. The common enrichment pathways were amino acid-tRNA biosynthesis ，aspartate-alanine-glutamate metabolism ， nitrogen metabolism ，phenylalanine metabolism and pentose phosphate pathway ，etc. CONCLUSIONS ：DHA can significantly reduce the activities of Huh 7 cells and BEL- 7402 cells，and the contents of glutamine ，glutamic acid ，glutathione and phenylalanine，etc. It may regulate the growth of the two kinds of cells by influencing the mechanism of aspartic acid- alanine-glutamate metabolic pathway ，etc.  
        关键词：Dihydroartemisinin;GC-MS;Liver carcinoma;Mechanism;Metabolic pathway;Amino acid   
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        发布时间：2022-06-21
      • LIU Xiaoyan,JIANG Yiping,ZHANG Jiabao,WANG Nani,XIN Hailiang
        Vol. 31, Issue 2, (2020)
        摘要：OBJECTIVE：To establish HPLC fingerprint of Humulus lupulus ，and to investigate its correlation with the antioxidant activity. METHODS ：The determination was performed on Diamonsil C 18 column with mobile phase consisted of 0.1％ phosphoric acid solution-acetonitrile （gradient elution ）at the flow rate of 1.0 mL/min. The column temperature was 30 ℃，and detection wavelength was set at 358 nm，with sample size of 2 μL. Using xanthohumol as reference，HPLC fingerprints of 11 batches of H. lupulus were determined. The similarity of 11 batches of samples was evaluated by TCM Chromatographic Fingerprint Similarity Evaluation System （2012 edition）to confirm common peaks. Using scavenging rate of DPPH and ABTS free radical as pharmacodynamic indicators of antioxidant effects ，SIMCA 14.1 analysis software was used for PLSR to establish the spectra-effect relationship ，and validation test of in vitro anti-oxidation was carried out. RESULTS ：There were 19 common peaks in HPLC fingerprints of 11 batches of sample ，the similarity of which was higher than 0.830. Seven components were identified as xanthohumol，cohumulone，humulone，adhumulone，colupulone，lupulus and adlupulus. Eleven batches of H. lupulus had the ability to scavenge DPPH and ABTS free radicals. The spectrum-effect relationship showed that xanthohumol ，humulone and colupulone peaks were positively associated with its anti-oxidant ability ，and variable projection value was greater than 1. In vitro antioxidant results showed that scavenging effect of 0.1 mg/mL xanthohumol to DPPH free radicals was similar to that of 0.01 mg/mL vitamine C ，but scavenging effect of 10.0 mg/mL xanthohumol to ABTS free radical was less than that of 0.1 mg/mL vitamin C. CONCLUSIONS：Established HPLC fingerprint can be used for the quality evaluation of H. lupulus ；xanthohumol，humulone and colupulone are the main material basis for the antioxidant effect of H. lupulus  
        关键词：Humulus lupulus;HPLC;Fingerprint;Antioxidant;Spectrum-effect relationship;PLSR   
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        发布时间：2022-06-21
      • WANG Shumei,HAN Jinmei,Wurihan,Sachula
        Vol. 31, Issue 2, (2020)
        摘要：OBJECTIVE：To establish a method for the content determination of apigenin and piperine in the water extract as well as eucalyptol and cumin aldehyde in the volatile oil of Mongolian medicine Sugmel- 3 decoction. METHODS ：HPLC method was adopted for the content determination of apigenin and piperine. GC method was used for the content determination of eucalyptol and cumin aldehyde. The determination of HPLC method was performed on Agilent Eclipse XDB-C 18 column with mobile phase consisted of methanol- 0.1％ phosphoric acid aqueous solution at flow rate of 1.0 mL/min；the detection wavelength was set at 225 nm（apigenin）and 342 nm（piperine）；the column temperature was set at 30 ℃ with sample size of 10 μL. The determination of GC method was performed on Dimensions SH-Rtx- 1 capillary column with high-purity hydrogen as carrier gas ； the injector temperature was set at 270 ℃，with flow rate of carrier gas 1 mL/min by temperature programmed ；the sample size was 1 μL，and split ratio was 1 ∶ 10. RESULTS：The linear ranges of apigenin ，piperine，eucalyptol and cumin aldehyde were 12.5-200 μg/g/mL（r＝0.999 6），87.3-139.7 μg/mL（r＝0.999 9），136-2 187 μg/mL（r＝0.999 9），39-635 μg/mL（r＝0.999 9）， respectively. The quantitation limits were 0.02，0.06，0.06，0.12 μg/mL，respectively. The detection limits were 0.01，0.02，0.03， 0.04 μg/mL. RSDs of precision，stability and reproducibility tests were all less than 4％. The recovery rates of the samples were 89.26％ -97.26％（RSD＝2.69％ ，n＝6），94.20％ -104.01％（RSD＝3.64％ ，n＝6），98.51％ -110.11％（RSD＝3.87％ ，n＝6）， 95.76％-107.82％（RSD＝4.12％，n＝6），respectively. The contents of above components were 0.769-0.828，7.741-7.981，5.284 7- 5.846 6，1.038 6-1.101 2 mg/g（n＝3）. CONCLUSIONS：The established method is simple and feasible ，and can be used for quality control of different parts of Mongolian medicine Sugmel- 3 decoction.  
          
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        发布时间：2022-06-21
      • QIAO Lijie,LI Bin,WANG Xinlu,XIE Shiyang,GAO Yuan,ZHU Mingjun,WANG Yongxia
        Vol. 31, Issue 2, (2020)
        摘要：OBJECTIVE：To investigate the effects of Shenfu yixin decoction on the utilization of fatty acid in primary hypoxic cardiomyocytes and its potential mechanism. METHODS ：The apical tissue of neonatal SD rats with 1-3 days old were collected ， and the primary cardiomyocytes were isolated ，cultured and identified. The cardiomyocytes were randomly divided into normal group，model group ，coenzyme Q 10 group（positive control ，1×10－4 mol/L），Shenfu yixin decoction low-dose and high-dose groups（0.25，0.5 mg/mL）. Except for normal group ，cells in other groups were cultured under 5％O2，5％CO2 and 90％N2 for 6 hours to induce hypoxic injury model. After 6 hours of hypoxia ，the content of ATP was detected by luciferase luminescence assay. Western blotting assay was adopted to detect the expression of FAT/CD 36，PPARα and PPARβ/δ. RESULTS：Compared with normal group ，the content of ATP and relative expression of FAT/CD 36 protein were decreased significantly in model group （P＜ 0.05）. Compared with model group ，the content of ATP was increased significantly in coenzyme Q 10 group and Shenfu yixin decoction high-dose group ，while the relative expression of FAT/CD 36 and PPARα protein in coenzyme Q10 group，the relative expression of FAT/CD 36 protein in Shenfu yixin decoction high-dose group as well as the relative expression of PPARα and PPARβ/δ protein in Shenfu yixin decoction groups were decreased significantly （P＜0.05）. CONCLUSIONS ：Shenfu yixin decoction can inhibit the utilization of fatty acid of primary hypoxic cardiomyocytes and improve their energy metabolism by inhibiting the expression of FAT/CD 36，PPARα and PPARβ/δ protein.  
        关键词：Hypoxia;Primary cardiomyocytes;Fatty acid;Metabolism;Shenfu yixin decoction   
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        发布时间：2022-06-21
      • WANG Xiaowei,WANG Yanwei,WANG Haibo,SONG Hanmin,LIU Ruixin,SHI Yan
        Vol. 31, Issue 2, (2020)
        摘要：OBJECTIVE：To improve the quality standard of Xiangsha hezhong pills. METHODS ：Based on previous quality standard of Xiangsha hezhong pills ，the items of property observation and microscopic identification were revised. TLC identification methods were established for ginger-processed Magnolia officinalis ，Pogostemon cablin and Atractylodes Lancea （stir-fried with earth ）. HPLC methods were adopted for contents determination of hesperidin ，magnolol and honokiol. RESULTS ： The description of the appearance of Xiangsha hezhong pills should be modified to “yellow brown or brown water pill ”. The description of microscopical identification was adjusted slightly. TLC chromatogram of ginger-processed M. officinalis ，P. cablin and Atractylodes Lancea （stir-fried with earth ）all showed the same color spots in the same position as the corresponding substance control or reference medicinal material ，and the negative samples had no interference. The contents determination were performed on Phenomenex Luna C 18 column with mobile phase consisted of methanol-water （40 ∶ 60，V/V，hesperidin）or acetonitrile- 1％ glacial acetic acid （52∶48，V/V，magnolol and honokiol ）at the flow rate of 1.0 mL/min. The column temperature was 30 ℃. The detection wavelengths were set at 284 nm（hesperidin）or 294 nm（magnolol and honokiol ）. The linear ranges of hesperidin ， magnolol and honokiol were 0.201 8-2.018 μg，0.035 7-0.357 4 μg and 0.028 2-0.282 4 μg（all r＝0.999 9）. The detection limits were 2.0，0.72，0.45 ng；the limits of quantitation were 7.0，2.45，1.61 ng. RSDs of precision ，reproducibility，stability and durability tests were all lower than 3％. The average recoveries were 99.92％，100.49％ and 102.08％（all RSD ＜3％）. CONCLUSIONS ：The study verifies the description of character observation and microscopical identification ，adds TLC identification methods for ginger-processed M. officinalis ，P. cablin and Atractylodes Lancea （stir-fried with earth ）based on previous quality standard of Xiangsha hezhong pills. HPLC methods were adopted to determine the contents of hesperidin ，magnolol and honokiol ，and can effectively improve the quality control standard of the preparation.  
        关键词：Xiangsha hezhong pills;Identification;Content determination;TLC;HPLC;Quality standard   
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        发布时间：2022-06-21
      • WANG Ying,HE Yanan,CHE Yihao,YUAN Shimeng,ZHAO Hairong,WU Xiumei,YANG Zhibin
        Vol. 31, Issue 2, (2020)
        摘要：OBJECTIVE：To preliminarily optimize the preparation technology of Ligustrazine pellicle ，and to study its in vitro percutaneous permeation characteristics. METHODS ：With the amounts of PVA- 124，ethyl alcohol ，glycerin，tween-80 and azone as factors ，single factor experiment was used to optimize the Ligustrazine pellicle matrix formulation ；modified scoring standard was used to evaluate the film formation time ，film formation ability ，ductility，uniformity and the presence of bubble. On the basis of the optimal matrix formulation ，the pellicle with different loading amount of ligustrazine （300，250，200，150，100，50 mg/mL） was prepared and its maximum loading amount was investigated. HPLC method was adopted to determine the content of ligustrazine，and methodology investigation was conducted. Isolated back skin of rats were collected ，the percutaneous permeation test was conducted for high ，medium and low loading amount （100，75，50 mg/mL）of Ligustrazine pellicle. At 15，30，45，60， 75，90，120，150，180 min，the sample was taken and the permeation rate of ligustrazine was calculated. RESULTS ：When the amounts of PVA- 124，ethyl alcohol，glycerin，tween-80 and azone were 2.5 g，7.0 mL，1.97 mL，0.07 mL，0.28 mL（in terms of 50 mL formulation amount ），the optimal matrix formulation of Ligustrazine pellicle was obtained. The maximum drug loading amount of ligustrazine was 100 mg/mL. The linear ranges of ligustrazine was 3.125-100 μg/mL. The specificity，precision， reproducibility，recovery and stability investigation of content determination method of ligustrazine were all in line with the requirements（RSD＜2％）. The permeation rate of high ，medium and low loading amount of Ligustrazine pellicle were 608.42， 384.19，158.20 μg（/ cm2·h）. CONCLUSIONS ：According to the optimized formulation ，the prepared Ligustrazine pellicle had a short film forming time ，stable and re liable quality ； the drug-loading amount was up to 100 mg/mL. The pellicle with drug-loading amount of 75 mg/mL had reached the penetration rate range of effective plasma concentration of ligustrazine treatment.  
          
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        发布时间：2022-06-21
      • Wenchengdangzhi,ZHANG Yunsen,Renzhenwangjia,Cairangnanjia,Gongbaodongzhi,QIENIXIANGMAO,Cairangji,Ganghuanchenlei,ZHANG Yi
        Vol. 31, Issue 2, (2020)
        摘要：OBJECTIVE：To investigate t he p otential mechanism of Tibetan medicine Wuwei shexiang pills in the treatment of “Grum bu ”disease（i.e. rheumatoid arthritis ）. METHODS ：Referring to Sibu Yidian ，Drug Standard of the Ministry of Public Health（Tibetan Medicine ），Jingzhubencao，the constituent ，dose and flavor of Wuwei shexiang pills were collected ；vector structure model was built. From the aspects of six tastes ，three tastes after digestion and seventeen effects ，the properties of the formulation were analyzed ；the“formulation-drug property-disease ”network for the treatment of “Grum bu ”disease was constructed by using Gephi 0.9.2 complex network software. The effective components of Wuwei shexiang pills were screened by using the pharmacology analysis platform of TCM system and the database of organic small molecule biological activity. The target proteins corresponding to the active components were predicted by using BATMAN-TCM network pharmacology research platform ； the target proteins of “Grum bu ”disease were searched by ETCM database. On the basis of screening the common targets of the two，David 6.8 bioinformatics resource database was adopted to conduct gene ontology （GO） analysis and KEGG pathway enrichment analysis ；the network of Wuwei shexiang pills- “Grum bu ”- target-pathway was constructed by using Cytoscape 3.7.0 software，and the network topology analysis was carried out to screen the core targets. Using Glide score as evaluation index ， Maestro Version 11.1.011 software was used for molecular docking of above core targets with effective components of Wuwei shexiang pills. RESULTS & CONCLUSIONS ：Wuwei shexiang pills contains myrobalan ，Aconitum pendulum ，Aucklandia lappa ， Acorus calamus and artificial moschus ，and the highest dosage was myrobalan. The six tastes of this formulation were mainly bitter and sweet ；the three tastes after digestion were mainly bitter ；the seventeen effects were mainly blunt ，cool and heavy ，which were mainly used to treat twenty characteristics such as acute ，hot and light. In “formulation-property-disease”network，higher values of edge weight between seventeen effects and twenty characteristics were cooling effect-heat ， blunt effect-sharpness ， heavy effect-light，dilute effect-odor （edge weight values ≥430），etc. A total of 2 306 potential targets of effective components of Wuwei shexiang pills ，211 targets related to “Grum bu ”disease，32 common targets and 29 corresponding effective components were obtained. The results of GO analysis showed that 52 relative results were predicted ，the common targets mainly located in the extracellular area ，nucleus and other parts ，mainly including biological processes and molecular functions such as immune response，inflammatory response ，cytokine activity. The results of KEGG enrichment were significant in 31 pathways（P＜0.05）， involving TNF signaling pathway ，cancer pathway and other signaling pathways. There were 94 active components ，targets and pathway nodes in the network of Wuwei shexiang pills- “Grum bu ”-target-pathway，and 460 edges；TNF，FAS，IL6，IL10， FASLG，PTGS2 and IL 1B were the core targets of the network ， connected with effective components such as quinic acid ， thymol，dehydroepiandrosterone，norcaxone by Van Der Waals force ，hydrogen bond and hydrophobic interaction ，Pi-cation bond and other bonds ，so as to play a role in the treatment of “Grum bu ”disease.  
          
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        发布时间：2022-06-21
      • CHEN Jingjing,ZHANG Zhenling,CAO Miaomiao,ZHANG Ying,YANG Jianing
        Vol. 31, Issue 2, (2020)
        摘要：OBJECTIVE：To establis h HPLC fingerprint of Chinese gall leaven ，simultaneous determination of 5 components and optimization of distillers ’grains. METHODS ：HPLC method was adopted. The determination was carried out on Waters Symmetry Shield TM RP18 column with mobile phase consisted of acetonitrile- 0.1％ trifluoroacetic acid aqueous （gradient elution ）at the flow rate of 0.8 mL/min. The column temperature was 30 ℃，and detection wavelength was set at 280 nm. The sample size was 5 µL. Using gallic acid as reference ，HPLC fingerprints of 14 batches of sample were drawn. The similarity evaluation was performed by using Similarity Evaluation System of Chromatogram Fingerprint of TCM （2012 edition）to determine common peaks；SPSS 20.0 software was used for cluster analysis. RESULTS ：There were 11 common peaks in 14 batches of samples ，and the similarity range of 14 batches of samples was 0.424-0.998，A1-A5 was less than 0.850；5 components were identified in B 1-B9 sample，i.e. gallic acid ，（－）-epigallocatechin，methyl gallate ，2，4，6-tri-O-galloyl-α-D-glucose and 2，4，6-tri-O-galloyl- β-D-glucose. The results of cluster analysis showed that 14 batches of samples could be grouped into 3 categories，i.e. A1-A5 into one category，B1 and B 6 into one category ，B2-B5 and B 7-B9 into one category. The linear ranges of above 5 components were 29.96-599.2 μg/mL（r＝0.999 6），0.832-416 μg/mL（r＝0.999 6），0.102-51 μg/mL（r＝0.999 8），0.286 4-143.2 μg/mL（r＝0.999 8）， 0.286 4- 143.2 μg/mL（r＝0.999 8），respectively. The limits of quantitation were 0.060，0.104，0.017，0.029，0.057 μg/mL；the limits of detection were 0.018，0.031，0.005，0.009，0.017 μg/mL，respectively. RSDs of precision ，stability，reproducibility and durability tests were all lower than 3％. The recoveries were 97.16％-101.88％（RSD＝1.60％，n＝6），96.98％-99.24％（RSD＝ 0.85％，n＝6），97.7％-101.64％（RSD＝1.54％，n＝6），97.77％-103.08％（RSD＝1.82％，n＝6），98.16％-101.88％（RSD＝1.24％， n＝6），respectively. CONCLUSIONS：The established HPLC fingerprint and cluster analysis can be used to evaluate the quality of Chinese gall leaven. The established method is simple to Δ 基金项目：国家重点研发计划项目（No.2018YFC1707200）；公 operate and can be used to determine the contents of 5 益性行业科研专项项目（No.201507004-03）；河南中医药大学研究生 components simultaneously ；rice husk distillers ’grains were 科研创新基金项目（No.YJS2018B14） ＊硕士研究生 。研究方向 ：中药饮片及新药研究 。E-mail： not suitable for fermented Chinese gall leaven . 401327039@qq.com  
          
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        发布时间：2022-06-21
      • FENG Zhenyu,MENG Shuang,CHANG Jianmin,ZHOU Xiaorong,SHI Min,ZHAO Jianping
        Vol. 31, Issue 2, (2020)
        摘要：OBJECTIVE：To investigate the effects and its mechanism of pseudostrychnine on the apoptosis of human colon can - cer HT- 29 cells. METHODS ：Human colon cancer HT- 29 cells were randomly divided into blank group ，pseudostrychnine low-dose，medium-dose and high-dose groups （125，250，500 μmol/L）. They were cultured with culture medium without medicine or relevant concentration of pseudostrychnine for 48 h. The cell apoptosis and mitochondrial transmembrane potential were detected by flow cytometry. Western blotting assay was employed to detect the protein expression of P 53，Caspase-3，Caspase-9，DNA re - pair enzyme from rabbit （c-PARP）and Bcl- 2. RESULTS ：Compared with blank group ，apoptotic rate of cells was increased signifi - cantly in pseudostrychnine low-dose ，medium-dose and high-dose groups ，while mitochondrial transmembrane potential was de - creased significantly （P＜0.01），in concentration-dependent manner. The protein expression levels of P 53，Caspase-3，Caspase-9 and c-PARP were increased in pseudostrychnine medium-dose and high-dose groups ，compared with blank group ；while those of Bcl-2 were decreased significantly in pseudostrychnine low-dose ，medium-dose and high-dose groups （P＜0.05 or P＜0.01）. CON - CLUSIONS：Pseudostrychnine may change mitochondrial membrane potential by up-regulating the protein expression of P 53 and down-regulating the protein expression of Bcl- 2，and activate the expression of Caspase- 3，c-PARP and Caspase- 9，so as to acti - vate endogenous mitochondrial pathway and promote the apoptosis of HT- 29 cells.  
          
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        发布时间：2022-06-21
      • CHENG Xuanxuan,CHEN Liangyuan,ZHENG Shijia,TANG Xiaomin,YANG Quan
        Vol. 31, Issue 2, (2020)
        摘要：OBJECTIVE：To estab lish the fingerprint ，analyze the monosaccharide composition and content ，investigate the inhibitory effects of the polysaccharide from Desmodium styracifolium on α-glucosidase in vitro . METHODS ：Polysaccharide from D. styracifolium was prepared by water extraction and ethanol precipitation. After hydrolyzed by TFA and derived by PMP ，HPLC method was adopted to establish the fingerprint （using glucose peak as reference ），and analyze the constituent and content of monosaccharide. The content determination was performed on Phenomenex Luna C 18 column with mobile phase consisted of acetonitrile-0.05 mol/L potassium phosphate （pH adjusted to 6.8 with sodium hydroxide ）in gradient elution at the flow rate of 0.8 mL/min. The detection wavelength was set at 250 nm，and column temperature was set at 30 ℃. The sample size was 10 μL. Using acarbose as control ，PNPG assay was used to investigate the α-glucosidase inhibitory activity of polysaccharide from D. styracifolium. RESULTS ：There were 9 common peaks in HPLC fingerprints of 18 batches of samples ，and the similarity of 15 batches of samples was higher than 0.90. Totally 7 peaks were identified as mannose ，rhamnose，galacturonic acid ，glucose， galactose，xylose and arabinose. The contents of rhamnose ，galacturonic acid ，glucose，galactose and arabinose were 0.471-2.092， 1.379-8.919，2.560-35.679，1.194-6.905，0.566-4.158 mg/g，respectively. Based on rhamnose ，the molar ratios of the other four monosaccharides were 1.58-4.07，2.26-19.95，2.20-4.21 and 1.31-2.86，respectively. The inhibitory activity of polysaccharide from D. styracifolium on α-glucosidase increased with the increase of dose ，and the half inhibitory concentrations of it was 0.70 mg/mL， lower than 7.76 mg/mL of acarbose （positive control ）. CONCLUSIONS ：Glucose is the main component of D. styracifolium polysaccharide in different batches ，and the contents of monosaccharides are different. The polysaccharide from D. styracifolium have significant inhibitory activity on α-glucosidase，which is better than that of acarbose.  
          
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        发布时间：2022-06-21
      • TANG Aicun,WEI Yanfei,LIU Xihua,WANG Minggang,LU Qiuyu
        Vol. 31, Issue 2, (2020)
        摘要：OBJECTIVE：To study the protective effect of tadehaginoside（TA）on liver fibrosis model mice induced by carbon tetrachloride（CCl4），and to investigate its mechanism. METHODS ：Kunming mice were randomly divided into normal group ， model group ，colchicines group （positive control ，0.2 mg/kg），TA low-dose ，medium-dose and high-dose groups （3，6，12 mg/kg），with 10 mice in each group. Those groups were intraperitoneally injected with 10％ CCl4-olive oil solution （5 mL/kg）to induce liver fibrosis model twice a week ，for consecutive 8 weeks；except that ，the normal group was intraperitoneally injected with olive oil. From 3rd week ，the mice in each administration groups were given relevant medicine intragastrically ，normal group and model group were given constant volume 2％ sodium carboxymethylcellulose solution intragastrically ，once a day ，for consecutive 6 weeks. The contents of ALT ，AST，HA and IL- 6 in serum of mice were test ed by ELISA. The contents of Hyp ， SOD，MDA and GSH-Px in liver tissues were detected by spectrophotometry. mRNA expression of Col- Ⅰ，TIMP-1 and TIMP-2 in liver tissue was detected by RT-PCR. The protein expression of MMP- 2 and TGF-β1 in liver tissue was detected by Western blotting. RESULTS ： Compared with normal group，the contents of ALT，AST，HA，IL-6，MDA and Hyp，the mRNA expression of Col- Ⅰ，TIMP-1 and TIMP- 2，as well as the protein exp ression of MMP- 2 and TGF-β1 were increased significantly ，while the contents of SOD and GSH-Px were decreased significantly （P＜0.01）. Compared with model group，the contents of ALT ，AST，HA，IL-6，MDA and Hyp ，the mRNA expression of Col- Ⅰ，TIMP-1 and TIMP- 2，as well as the protein expression of MMP- 2 and TGF-β1were decreased significantly ，while the contents of SOD and GSH-Px were increased significantly（P＜0.05 or P＜0.01）. CONCLUSIONS ：TA has a significant protective effect on liver tissue and anti-fibrosis effects in liver fibrosis model mice ，the mechanism of which may be associated with inhibiting lipid peroxidation and collagen synthesis ， down-regulating the mRNA expression of Col- Ⅰ，TIMP-1 and TIMP- 2 as well as the protein expression of MMP- 2 and TGF-β1.  
          
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      • ZHAO Yu,WAN Zhiqiang,ZHANG Rongrong,MA Xintong,WANG Miao,SHAO Shuai,YAN Mingming,QI Bin
        Vol. 31, Issue 2, (2020)
        摘要：OBJECTIVE：To optimi ze the optimal composition proportion of 4 ingredients （Panax ginseng ，Astragalus membranaceus，Polygonatum sibiricum ，Lycium chinensis ）in Compound ginseng immune-enhancing formula （CGIF），and to study immune activity and acute toxicity of the extracts with the optimal ratio. METHODS ：The cell activity test was used to screen the crude drug concentration range of 4 ingredients. After treated with different crude drug concentrations of each medicinal material，using the contents of NO ，IL-6 and TNF-α as indexes，uniform design was used to determine the optimal ratio of each ingredient in CGIF. Totally 240 mice were taken and randomly divided into 4 batches，with 60 mice in each batch. Each batch of mice was randomly divided into blank group （normal saline ），model group （normal saline ），positive drug group [levamisole ，4 mg/（kg·d）]，and optimal proportion extract of CGIF low-dose ，medium-dose and high-dose groups [ 0.952 8，1.905 6，3.811 2 g/（kg·d）]，with 10 mice in each group ；they were given medicine intragastrically ，qd，for consecutive 30 d. Except for blank group，mice in the other groups were intraperitoneally injected with cyclophosphamide [ 40 mg/（kg·d）] on the 24th day after first administration，qd，for consecutive 3 d to induce immunocompromised model. The immune activity of the optimal proportion extract was evaluated by determining visceral coefficients ，spleen lymphocyte transformation capacity ，serum contents of hemolysin，IL-2，IgM，IgG and IgA ，phagocytosis function of peritoneal macrophages. Another 20 mice were collected and given the optimal proportion extract 20 mL/kg intragastrically ，twice；acute toxicity of the formula was investigated with oral maximum tolerated dose （MTD）. RESULTS ：The optimal ratio of CGIF was that crude drug mass ratio of P. ginseng ， membranaceus，P. sibiricum ，L. chinensis was 1 ∶ 2 ∶ 2 ∶ 4. The immunological activity experiment showed that theoptimal proportion extract can significantly improve visceral indexes of mice ， spleen lymphocyte proliferation ability serum contents of hemolysin ，IL-2，IgM，IgG and IgA as well as macrophage phagocy tosis ability （P＜0.05 or P＜ 0.01）. The acute toxicity test indicated that oral MTD was over 15 g/kg，which was non-toxic. CONCLUSIONS ：The optimal proportion extract of CGIF can significantly enhance the immune function of mice and are non-toxic.  
        关键词：Ginseng immune-enhancing formula;Couplet medicine;Uniform design method;Mice;Immune function;Acute   
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      • HUANG Zhiquan,WANG Zhenwen,ZHU Liang
        Vol. 31, Issue 2, (2020)
        摘要：OBJECTIVE：To investigate the effects of metformin on malignant phenotype of pancreatic cancer BxPC- 3 cells. METHODS：Using human pancreatic cancer BxPC- 3 cells with natural deletion of Smad4 gene as reaserch objects ，CCK-8 assay and flow cytometry were used to detect the proliferation and apoptosis of BxPC- 3 cells after treated with different doses of metformin（5，10，20 mmol/L）for 24 h. The cell survival rate and apoptosis rate were calculated. Transwell assay was used to test the migration of cells after treated with different doses of metformin （10，20 mmol/L）for 24 h. The number of migrating cells was recorded. qRT-PCR and Western blotting assay were performed to determine mRNA and protein expression of E-cadherin ，Vimentin and RGC- 32 in cells. RESULTS ：Compared with control group and 5 mmol/L metformin group ，survival rate of cells were decreased significantly in 10，20 mmol/L metformin groups ，while apoptosis rate was increased significantly ；the apoptosis rate in 20 mmol/L metformin group was significantly higher than 10 mmol/L metformin group （P＜0.05）. Compared with control group ， the number of migrating cells was decreased significantly in 10，20 mmol/L metformin groups ，and the 20 mmol/L metformin group was significantly lower than 10 mmol/L metformin group （P＜0.05）. Relative mRNA and protein expression of E-cadherin were increased significantly in 10，20 mmol/L metformin groups ，and relative mRNA expression of E-cadherin in 20 mmol/L metformin group was significantly higher than 10 mmol/L metformin group. Relative mRNA expression of Vimentin in 10 mmol/L metformin group ，relative mRNA and protein expression of Vimentin in 20 mmol/L metformin group ，relative mRNA and protein expression of RGC- 32 in 10，20 mmol/L metformin groups were decreased significantly ；relative mRNA and protein expression of Vimentin as well as mRNA expression of RGC- 32 in 20 mmol/L metformin group were significantly lower than 10 mmol/L metformin group （P＜0.05 or P＜0.01）. CONCLUSIONS ：Metformin can inhibit the proliferation and migration of pancreatic cancer cells through smael-independent pathways in a dose- dependent manner ，and promote their apoptosis ，which is associated with the inhibition epithelial- mesenchymal transition and the expression of RGC- 32 of pancreatic cancer.  
          
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      • LI Chao,JIANG Wenliang,YANG Zixian,LI Kexin,NI Qian,PEI Yifang,LI Ting,TAN Ling
        Vol. 31, Issue 2, (2020)
        摘要：OBJECTIVE：To rapidly evaluate the effectiveness，safety and economics of rosuvastatin （RSV）in the treatment of dyslipidemia，so as to provide evidence-based support for clinical drug use. METHODS ：Retrieved from PubMed ，Embase， Cochrane Library ，CNKI，Wanfang database and CBM ，etc.，health technology assessment （HTA）related website and database were searched systematically to select HTA report ，Meta-analysis/systemic evaluation and pharmacoeconomics study about RSV versus placebo or other positive drugs in the treatment of dyslipidemia. According to the inclusion and exclusion criteria ，two researchers independently screened the literatures ，extracted and summarized the data ，then performed qualitative description of results. RESULTS ：Totally 11 Meta-analysis and 11 pharmacoeconomic studies were included ，and no relevant HTA report was retrieved. Results of the study showed that compared with the control group ，RSV could regulate dyslipidemia ，and reduce the levels of LDL-C ，TG，TC，C-reactive protein and sdLDL ；RSV could also reverse atherosclerotic plaque ，reduce all-cause mortality with good safety. In terms of economy ，compared with other statins or placebo ，RSV could prolong quality-adjusted life year，its incremental cost-effectiveness ratio is lower than the desired payment threshold ，which had more economic advantages. CONCLUSIONS：RSV is effective ，safe and economical in the treatment of hyperlipidemia.  
        关键词：Rosuvastatin;Dyslipidemia;Hyperlipidemia;Effectiveness;Safety;Economics;Rapid health technology   
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      • XI Xiaoyu,XIE Wenwen,LIU Yan,HUANG Rong,CHEN Lei
        Vol. 31, Issue 2, (2020)
        摘要：OBJECTIVE：To provid e reference for safe ，effective and economical medication scheme for type 2 diabetes mellitus（T2DM）. METHODS ：Markov model was established for rosiglitazone sodium and metformin in the treatment of T 2DM. According to the development characteristics of T 2DM，the development of T 2DM was simulated by the dynamic changes of event-free，complications and deaths of T 2DM. The long-term cost and effect of rosiglitazone sodium and metformin in the treatment of T 2DM were obtained by regression analysis and queue simulation analysis. QALYs was used as a health output indicator，and t he superiority and inferiority of different schemes were judged by the ICER value ，and in our study ICER value was WTP（12 000 yuan per year ）of diabetics. The sensitivity of cost ，utility and discount was analyzed to check the stability of the analysis results. RESULTS ：Cost-effectiveness analysis of Markov model showed that the cumulative cost and health effectiveness of rosiglitazone sodium therapy were 25 164.00 yuan and 7.50 QALYs，while 17 773.36 yuan and 7.36 QALYs for metformin ； ICER of rosiglitazone sodium relative to metformin was 50 983.08 yuan/QALYs，which was greater than WTP ，so the metformin treatment was an advantageous scheme. Sensitivity analysis showed that health utility value and discount rate of diabetes mellitus greatly influenced analysis results of the model ，but advantage plan had not changed within the sensiitivity analysis range seted in this study. CONCLUSIONS ：For T 2DM，metformin is more cost-effective than rosiglitazone sodium.  
        关键词：Type 2 diabetes mellit us;Rosiglitazone sodium;Metformin;Cost-effectiveness;Markov model;Pharmacoeconomic   
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      • ZHANG Lei,LI Qingsong,HUANG Yu
        Vol. 31, Issue 2, (2020)
        摘要：OBJECTIVE：To provide reference for safe and rational use of Sodium tanshinone ⅡA sulfonate（STS）injection in the clinic. METHODS ：The information of the patients who received STS injection from Jan. 2016 to Dec. 2017 were collected from a Grade 3 hospital. According to relevant suggestions in drug package inserts ，drug utilization rationality was evaluated ，and single-factor and multi-factor analysis on the risk and influential factors for ADR/ADE were performed by group design and individual matching to examine their correlation. RESULTS ：Totally 3 283 patients were included in the study. The drug use frequency were less than 1.5，and the drug utilization indexes were less than 1.0，suggesting that the hospital using STS injection was basically reasonable. Irrational use of drugs mainly included that inappropriate indications （46.48％），unreasonable solvent selection（15.84％），and excessive concentration （2.71％）. Patients with renal insufficiency received STS injection ，and then the risk of ADR/ADE increased by correlation analysis （P＜0.05）. CONCLUSIONS ：Irrational use of STS injection in clinics existed ， mainly like off-label drug use ，excessive concentration ，irrational solvent selection. Drug use evaluation and monitoring should be strengthened. For patients with renal insufficiency ，it is necessary to prevent the occurrence of ADR/ADE ．  
          
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      • ZHONG Yizheng,HUANG Jiahua,PAN Meijun,JIANG Huaqing,ZHENG Hao,LI Wei,CHEN Sijian,CAO Yingying,HUANG Fan,DENG Fasen,SUN Weipeng,GUO Kaimin
        Vol. 31, Issue 2, (2020)
        摘要：OBJECTIVE：To systematically evaluate therapeutic efficacy of Gongliuqing capsules combined with mifepristone in the treatment of uterine leiomyoma ，in order to provide evidence-based reference for clinical medication. METHODS ：Retrieved from Cochrane Library ，PubMed，Embase，CJFD，VIP，CBM and Wanfang database ，randomized controlled trials （RCTs）about Gongliuqing capsules combined with mifepristone （trial group ）versus mifepristone alone （control group ）in the treatment of uterine leiomyoma were collected. After literature screening and data extraction ，the quality of included literatures was evaluated with modified Jadad scale. Meta-analysis was conducted by using Stata 14.0 software，and trial sequential analysis （TSA）was performed by using TSA 0.9 software. RESULTS ：A total of 12 RCTs were included ，involving 1 210 patients. The results of Meta- analysis showed that the total response rate of trial group [RR ＝1.12，95％CI（1.00，1.26），P＜0.05] was significantly higher than that of control group ；maximum uterine leiomyoma volume after treatment [SMD ＝－1.08，95％CI（－1.21，－0.95），P＜0.05]，uterine volume after treatment [SMD ＝－0.80，95％CI（－1.14，－0.45）， P＜0.05]，follicle stimulating hormone （FSH）level [SMD ＝ － 0.28，95％ CI（－ 0.45，－ 0.19），P＜0.05]，luteinizing hormone（LH）level [SMD ＝－0.44，95％CI（－0.52，－0.12）， 020-38076311。E-mail：867203217@qq.com P＜0.05]，E2 level [SMD ＝－2.69，95％CI（－3.08，－1.49）， P＜0.05] and progesterone （P）level [SMD ＝－1.27，95％CI（－1.69，－0.71），P＜0.05] of trial group were significantly lower or better than those of control group. Results of subgroup analysis showed that except for the level of FSH in 5 and 10 mg mifepristone groups （P＞0.05），maximum uterine leiomyoma volume after treatment ，uterine volume after treatment ，the levels of FSH，LH，E2 and P in trial group were significantly lower than control group. The results of TSA showed that there were definite evidences for total response rate of Gongliuqing capsules combined with mifepristone being better in the treatment of hysteromyoma. CONCLUSIONS ：Total response rate of Gongliuqing capsules combined with mifepristone in the treatment of hysteromyoma is better than mifepristone alone ，which can effectively decrease the volume of maximum uterine leiomyoma volume and uterine vilume ，and reduce the level of serum hormone.  
        关键词：Uterine leiomyoma;Mifepristone;Gongliuqing capsules;Therapeutic efficacy;Meta-analysis;Trial sequential   
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      • WU Yanzi,YE Shan,LIU Fang
        Vol. 31, Issue 2, (2020)
        摘要：OBJECTIVE：To sy stematically evaluate the efficacy and safety of a spirin combined with clopidogrel in the treatment of progressing stroke. METHODS ：Retrieved from the Cochrane library ，PubMed，Embase，Clinical trials.gov ，CBM， VIP，Wanfang database and CNKI databases ，randomized controlled trials （RCTs）about aspirin combined with clopidogrel （trial group）versus aspirin or clopidogrel alone （control group ）in the treatment of progressing stroke were collected. After literature screening and data extraction ，the quality of literatures were evaluated with bias risk assessment tool recommended by Cochrane system evaluator manual 5.2. Meta-analysis was performed by using Rev Man 5.3 software. RESULTS ：A total of 27 RCTs involving 2 854 patients were enrolled. The results of Meta-analysis showed that response rate of trial group was significantly higher than aspirin group [RR ＝1.31，95％CI（1.26，1.37），P＜0.000 01]；Neurological deficit score （NDS）of trial group was significantly lower than control group [MD ＝－3.80，95％CI（－5.30，－2.30），P＜0.000 01]；National Institutes of Health Stroke Scale Score in trial group was significantly lower than aspirin group [MD ＝－3.72，95％CI（－5.25，－2.20），P＜0.000 01] and clopidogrel group [MD ＝－2.44，95％CI（－4.14，－0.73），P＝0.005]. Results of subgroup analysis showed that NDS score of trial group was significantly lower than control group after 14 d of treatment [MD ＝－2.19，95％CI（－3.11，－1.27），P＜0.000 01]，15 d of treatment [MD ＝－5.73，95％CI（－10.65，－0.81），P＝0.02] and 28 d of treatment [MD ＝－3.45，95％CI（－4.24，－2.67），P＜ 0.000 01]. Compared with trial group ，there was no statistical significance in response rate with clopidogrel group ，the incidence of ADR with clopidogrel group ，the incidence of bleeding event with clopidogrel group ，and mortality with control group （P＞0.05）. CONCLUSIONS：Aspirin combined with clopidogrel in the ； treatment of progressive stroke ，can improve the efficacy and improve neurological deficit symptoms in the short term ，but can not reduce the incidence of ADR or the mortality during E-mail：wuyanzi89@126.com the treatment.  
          
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      • XUE Ying,SI Fangying,LIU Shuaibing
        Vol. 31, Issue 2, (2020)
        摘要：OBJECTIVE：To provide reference for individualized treatment of patients with Neuroleptics-induced malignant syndrome（NMS）. METHODS ：A patient with NMS related to antipsychotics was admitted to our hospital in Sept. 19th 2018. Clinical pharmacists provided pharmaceutical care throughout the whole process ，and put forward suggestions for medication. Through literature review ，clinical pharmacists summarized the clinical manifestations ，risk factors ，pathogenesis，diagnosis and therapeutic drugs of NMS. RESULTS & CONCLUSIONS ：Based on the history of antipsychotic drug use ，the characteristic clinical manifestations of NMS and laboratory examination ，the clinical pharmacist proposed that the patient suffered from antipsychotic drug-related NMS ，and the doctor adopted the suggestions. In the course of treatment ，the clinical pharmacist suggested that the subhibernating mixture should be stopped ；Bromocriptine mesylate tablets should be used in combination with continuous hypothermia instrument for physical cooling ，and the treatment course should be at least 10 days according to drug use before admission and medication plan after admission. The doctor adopted the suggestion. The symptoms began to relieve on the third day ，and the symptoms basically disappeared on the 10th day ，then the patient was discharged on the 13th day. The clinical manifestations of NMS were high fever ，myotonia，mental state change ，autonomic nervous disorder ，creatine phosphokinase and leukocyte increase etc. ；risk factors included drug factors ，demographic factors ，genetic and etc. ；the pathogenesis may be associated with dopaminergic receptor block and musculoskeletal fiber toxicity ；the identification diagnosis was based on clinical manifestation，including the onset time ，neuromuscalar reactivity ，remission time ，etc.；the commonly used drugs were bromocriptine mesylate and dantraline.  
          
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