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    药物研究
  • 药物研究
    LV Xiao-dong;CAI Xu;ZHANG Ying
    Objective To compare the concentration of triclosan and fasting plasma glucose after injection of different emulsions of four triclosan hydrogels. Methods Thirty rabbits of the same brood were divided into 5 groups randomly, with 6 rabbits in each group.The triclosan(control), triclosanhydrogel acid(TriHA), triclosanchitosan(TriCH) and triclosanpolymer hydrogel were injected intraarticularly into the injured knees of rabbits, respectively. 2 mL blood was collected at 6,12,24,48,72,96 hours after instillation,and analyzed with high pressure liquid chromatogram(HPLC)to calculate the blood concentration of triclosan. Results Triclosan was detected out in each group,which remained shorter in the control and polymer hydrogel groups compared with those in the TriHA and TriCH groups.The average concentration in polymer hydrogel group was significantly higher than that of other groups(P<0.05).Triclosan showed the lowest level in the TriHA group(P<0.05)and highest one (P<0.05)in the polymer hydrogel group. The variation of fasting blood glucose in the control and polymer hydrogel groups was more obvious than that of the other two groups (P<0.05). Conclusion ①Triclosanhydrogel acid and triclosanchitosan emulsions achieve lower triclosan level in the blood, and there is no significance abnormal change of fasting plasma glucose.②The lower blood triclosan level is occurred in the triclosanhydrogel acid emulsion compared with that in the triclosanchitosan emulsion, and no significance abnormal fasting plasma glucose is found out.Therefore, triclosanhydrogel acid is more suitable for clinic use.

  • 药物研究
    LI Jin;DENG Yu;LI Zhao-ming;CAO Xiao-nian;LI Xiao-lan;TAO De-ding;HU Jun-bo;WANG jing
    Objective To investigate the effects of mesalazine retarder on the expression of tumor necrosis factorα(TNF-α),interleukin1β(IL-1β) and interleukin6(IL-6)in trinitrobenzene sulfonic acid(TNBS)induced ulcerative colitis(UC) in rats and explore its antiinflammatory mechanism. Methods UC was induced in rats with TNBS and ethanol. The rats were randomly divided into three groups: normal control(group C), model control(group T), mesalazine retarder treatment group(100 mg&#8226;kg-1&#8226;d-1)(group M) and 5-ASA treatment group(100 mg&#8226;kg-1&#8226;d-1)(group A).One day after UC was induced, the rats in the treatment group were intragastric administered mesalazine retarder or 5-ASA every 12 hours for seven days, while the other three groups were taken an intragastric treatment of distilled water. The disease index(DAI),body weight and scores of pathological changes (HS)of rats were calculated.The activity of myeloperoxidase(MPO) was measured by biochemical method, and expressions of TNF-α、IL-1β and IL-6 mRNA were measured by Real-time PCR, respectively. Results Compared with the normal group,the model rats showed significantly increased DAI,HS score and MPO activity in the colon tissues(P<0.05),and upregulated expression of TNF-α、IL-1β and IL-6 mRNA in the colon mucosa (P<0.05) as well.Compared with the model and 5ASA treatment group,mesalazine retarder resulted in a significant reduction in DAI,HS score and MPO activity(P<0.05),and lower expression of TNF-α、IL-1β and IL-6 mRNA (P<0.05) in the colon mucosa. Compared with the model group,5-ASA treatment group led to a reduction in DAI,HS score and MPO activity,and decreased expression of TNF-α、IL-1β and IL-6 mRNA in the colon mucosa, but no statistic significance was found. Conclusion Mesalazine retarder has protective effect against rat ulcerative colitis, the mechanism of which probably links to reduction of TNF-α,IL-1β and IL-6 expression and neutrophil infiltration.

  • 药物研究
    DENG Yu;WANG Gui-hua;ZUO Xue-liang;DONG Shuo;JIN Yuan;LI Wei-na;GONG Jian-ping;HU Jun-bo
    Objective To investigate the anti-proliferation effects of cell-permeable TAT-N24 fusion peptide on prostate cancer cells.Methods The human prostate cancer cell line PC3 was treated with TAT-N24, cell cycle distribution was analyzed by flow cytometry,DNA synthesis of which was measured by BrdU incorporation assay.and the expression of phosphorylated AKT was examined by Western blot analysis. Results ① G0/G1 phase arrest induced by TAT-N24 was observed. The cell cycle distribution was that: in the blank group G0/G1 phase as (56.9±6.1)%, S phase (27.0±2.3)%, G2/M phase (16.1±1.3)%; G0/G1 phase (57.9±4.8)%, S phase (24.2±3.1)%, G2/M phase (27.8±1.4)% in the control peptide group; G0/G1 phase (68.6±5.4)%(P<0.05), S phase (19.4±1.5)%(P<0.05) , G2/M phase (12.3±1.4)% in TAT-N24 group, respectively. ②The BrdU positive cells in the blank, control peptide and TAT-N24 groups was(37.9±3.2)%,(36.2±4.1)%,(21.5±2.4)% (P<0.05) , respectively;③It was revealed that TAT-N24 had no significant effects on AKT phosphorylation Conclusion The cellpermeable TAT-N24 fusion peptide effectively blocks cells processing into G0/G1 phase and inhibiting DNA synthesis of PC3 cell line. TAT-N24 may become an effective molecular targeted gene medicine for cancer therapy.

  • 药物研究
    TAN An-xiong;ZHU Yao-bin;WANG Yu-yin
    Objective To investigate the protective effect and mechanism of crocetin on focal cerebral ischemiareperfusion injury. Methods 120 SD rats were divided into six groups, named as sham operation (sham group), model control of cerebral ischemiareperfusion injury (model group), nimodipine positive control(Nim group), high dose of crocetin group(40 mg&#8226;kg-1), moderate dose of crocetin group(20 mg&#8226;kg-1), low dose of crocetin group(10 mg&#8226;kg-1). The sham group and model group were given with the same dose of normal saline. The rats were treated once in each group in the morning by reperfusion for a week. The model of neurological deficits was made by 2 h of middle cerebral artery occlusion followed with 22 h reperfusion. To observe the nerve functional defect score, cerebral infarction, and check the content of malondialdehyde (MDA), nitrogen monoxidum oxide (NO) and activity of superoxide dismutase(SOD) in ischemic brain tissues. Results The nerve functional defect scores of high, moderate and low dose of crocetin group, Nim group, sham group and model group were (0.35±0.31), (1.21±0.54), (2.04±0.32), (1.29±0.42), (0.00±0.00), (2.12±0.64), respectively; volume ratio of cerebral infarction were (13.2±4.3)%, (21.6±3.5)%, (34.2±2.7)%, (20.6±4.2)%, (0.0±0.0)%, (44.8±3.2)%, respectively; the content of MDA were (2.0±0.5), (2.9±0.4), (3.8±0.7), (2.5±0.8), (2.1±0.6), (4.2±0.7) μmol&#8226;g-1, respectively; the content of NO were (5.8±1.5), (8.8±1.3), (10.8±2.3), (8.8±2.1), (6.3±1.1), (12.8±1.3) μmol&#8226;g-1, respectively; the activity of SOD were (198.3±13.1), (159.8±10.9), (132.4±12.1), (164.3±10.7), (202.6±12.5), (121.1±11.6) kU&#8226;g-1, respectively.Crocetin improved cerebral infarction and nerve function, enhanced SOD activity, reduced MDA and NO content in a dosedependent manner. Conclusion Crocetin can protect focal cerebral ischemiareperfusion injury, the mechanism of which may be related to SOD activity enhancement and reduction of MDA and NO levels.

  • 药物研究
    HAN Ying;XU Wen-qing;YANG Fu-jun;SHEN Xiu;HONG Ge;HUANG Jie;ZHOU Ze-wei
    Objective To investigate the inhibition effect on H22 hepatoma by polysaccharides from Tremella fuciformis and explore the mechanism by applying gene expression array chip. Methods The H22 hepatoma model was set up in mice. The inhibition rate was used to evaluate antitumor effects of polysaccharide from Tremella fuciformis and tumor inhibitory mechanism was explored by using cDNA microarray. Results The best inhibition rate was showed as 72.3%(P<0.01) by Tremella fuciformis polysaccharides at the dose of 6 mg&#8226;kg-1. There was expression difference in 324 of the total 4 000 genes compared with negative control groups, 185 genes of which were upregulated and 139 genes were down regulated. By the prelinminary analysis, most of genes were those about signal conduction, DNA injury check/P53 and ATM path, antigen presentation and chemotherapy response. Conclusion The polysaccharide from Tremella fuciformis inhibits H22 hepatoma in mice markedly. The mechanism of action is multitargeted and multiple factors involved, which linking either to cancer associated gene or to immune regulation and signal conduction.
  • 药物研究
    ZHENG Ya-dong;XU Xi-qiang;PENG Fei;YU Ji-zhe;WU Hua
    Objective To investigate the anticancer effects of cisplatin cotreated with PARP-1 inhibitor 3-aminobenzamide (3-AB) on human osteosarcoma cells. Methods Cell count kit-8 was used to analyze cell proliferation. In CCK-8 assay, U2OS cells were divided into two groups, one group was treated with cisplatin, and the other was treated with cisplatin plus 3-AB. Cell apoptosis and cell cycle were assessed by flow cytometric detection. Results The IC50 of U2OS cells by cisplatin plus 3-AB was lower than that by cisplatin alone, and the sensitized ratio was 1.76. It was showed that the apoptosis rate was increased in cells treated with 3-AB and cisplatin compared with that treated with two agents alone. And the combination treatment induced a more sustained S phase arrest. Conclusion PARP-1 inhibitor 3-AB enhances the anti-proliferation and apoptosisinducing effects of cisplatin in human osteosarcoma cells.

  • 药物研究
    ZHANG Zhao-lin;ZHANG Shu-feng;WANG Shu-jun;HE Shu-fen
    Objective To prepare the complex of pefloxacin and zinc, and investigate its antimicrobial activity. Methods The complex was produced by chemical reaction between 0.136 3 g zinc chloride and 0.666 0 g pefloxacin. The elemental analysis and infrared spectroscopy were conducted for the complex detection, and the antibacterial activity was determined in vitro. Results The complex contained 13.16% Zn, 41.05% C,4.02% H,8.43% N,7.15% Cl and 12.50% H2O. The molecular formula of the complex was extrapolated to be Zn2(C17H20FN3O3)2Cl2(H2O)7 by the element analysis. The carboxyl C=O stretching vibration absorption peaks appeared in pefloxacin at 1 713 cm-1s, which disappeared in the complexes, and the corresponding asymmetric and symmetric carboxyl stretching vibration absorption peak appeared in pefloxacin at 1 572.1,1 343.7 cm-1. The naphthyridine ring carbonyl (C=O) stretching vibration occurred in pefloxacin at 1 634 cm-1 which in the complexes were redshifted 13 to 1 621.2 cm-1. The MIC of pefloxacin against Haemophilus influenzae and Streptococcus faecalis MIC were 1.25 and 2.5 mg&#8226;mL-1, respectively. While the MIC of the complexes against Haemophilus influenzae and Streptococcus faecalis were 0.62 and 1.25 mg&#8226;mL-1, respectively. Conclusion The method for preparation of the complex is simple. It indicates that in vitro antibacterial activity against Haemophilus influenzae and Streptococcus faecalis by the complex of pefloxacin and zinc is slightly higher than that of pefloxacin.

  • 中药及天然药物专栏
  • 中药及天然药物专栏
    PENG Ying;HUO Shi-xia;KANG Yu-tong;YAN Ming
    Objective To study the curative effect of victoria medicine qubaibabuqi capsule on experimental vitiligo in guinea pigs. Methods The animal model of vitiligo was prepared by decolourization process of hydroquinone production, then the model animals were treated with different doses of qubaibabuqi capsule. After the medical treatment, dopamine and iron staining were used for observing the changes of melanocytes and black granules, and immunohistochemisty was used to test the content of tyrosine. Results Compared with the model group, the count of melanocytes and basal cells with black pigment particles and the tyrosine’s expression in the treatment groups were significantly higher by the end of experiment (P<0.01). Conclusion The victoria medicine qubaibabuqi capsule can increase epidermal melanocytes and production of black granules and enhance the expression of tyrosine.
  • 中药及天然药物专栏
    CHENG Li-juan;CHEN Xiao-nong;LIU Qing-chuan;XU Xue-yu;SU Cheng-hu;YU Shan;HUANG Zheng-ming
    Objective To study the prevention and therapeutic effect of lingwu (LW) granules on chronic liver injury induced by carbon tetrachloride in rats and explore its possible mechanism. Methods The Wistar rats were randomly divided into 6 groups, which were given with 350 mg &#8226;L-1 phenobarbital aqueous solution for 2 weeks to induce drugmetabolizing enzyme except for the normal control being treated with water. Since the third week, the rat models of chronic liver injury were set up with the CCl4[50% CCl4 olive oil solution, ig, 0.08 mL at first, then 0.08 mL&#8226;(100 g)-1, once a week for 5 weeks]. As soon as the models was established, the rats were ig LW qd for 5 weeks. After the last administration, rats were fasted for 16 h. Then blood, liver, spleen, thymus were taken out to detect the liver function (ALT,AST,ALP,ALB,TP), Hyp, MDA in liver and the activity of SOD; the histopathology of liver was examined and the organ index was calculated. Results The rats in the model group suffered obvious hepatic injury and chronic fibrosis. Liver function and hepatic fibrosis were improved in rats being treated(P<0.01 or P<0.05). The liver pathological test showed that LW alleviated the hepatic fibrosis obviously. Conclusion LW has a good effect on CCl4 induced chronic liver injury, especially the hepatoprotection and enzyme reduction, the mechanism of which may be related to the inhibition of increased Hyp, MDA declining and elevation of SOD antioxidant effects.
  • 中药及天然药物专栏
    WU Feng;ZENG Ying;LIANG Hua-min
    Objective To compare the baceriostasis in vitro between zhizhi capsules and huaijiao pills. Methods The MH agar dilution method was used to explore the in vitro bacteriostasis against 6 kinds of common bacterial growth by zhizhi capsules and huaijiao pills. Results The zhizhi capsules showed antibacterial activity against all of the 6 common bacteria, in which minimal inhibitory concentration (MIC) for Staphylococcus aureus, Bacillus proteus and Group B Streptococcus was 0.062 5 g&#8226;mL-1;MIC for Pseudomonas aeruginosa was 0.125 g&#8226;mL-1;MIC for E.coli was 0.25 g&#8226;mL-1 and for Enterococcus was 0.5 g&#8226;mL-1. But huaijiao pills only showed baceriostasis against staphylococcus aureus and proteus, MIC for both was 0.125 g&#8226;mL-1. Conclusion Zhizhi capsules have broader antibacterial spectrum and stronger bacteriostasis ability than huaijiao pills.

  • 中药及天然药物专栏
    SHI Qiang
    Objective To compare the effects of Smilax sieboldii Miq., Clematis chinensis Osbeck. and C. hexapetala Pall. on non-specific immunity, and further determine the feasibility of Smilax sieboldii Miq. to be used as drug. Methods The carbon granules clearance test in mice and chicken red blood cell phagocytosis test were carried out to compare the effects. Results All of Smilax sieboldii Miq., Clematis chinensis Osbeck. and C. hexapetala Pall. inhibited the phagocytic function of monocytemacrophage and abdominal cavity macrophage in mice, and reduced nonspecific immune function. Conclusion Smilax sieboldii Miq. can be used equivalently as Clematis chinensis Osbeck. for the treatment of rheumatism.
  • 中药及天然药物专栏
    ZHANG Qiu-yu;YU Yong-jun;HUI Jing-fang;YANG Gui-ran;WANG Mei
    Objective To investigate antidepression effect of baihe dihuang decoction with ganmai dazao decoction. Methods A total of 40 mice were randomly divided into model group, high dose group, low dose group and positive control group, with 4 mice in each group. Animals of positive control group were given 0.04 g.kg-1 of clomipramine hydrochloride by gastrogavage. Mice of high dose group and low dose group were treated orally with 30 and 15 g.kg-1 baihe dihuang decoction with ganmai dazao decoction, respectively. Model group received the same volume of saline.the treatment last 7 days.The mouse tail suspension test, forced swimming test and reserpine reversal test were used as models to study effects of baihe dihuang decoction with ganmai dazao decoction. Results The immobility time of high dose group, low dose group, positive control group and model group in tail suspension test was (49.80±39.52), (49.20±33.10), (24.90±28.71), (79.40±25.17) s, respectively; The immobility time of forced swimming test was (78.00±37.92), (81.70±34.59), (32.6±36.82), (113.9±19.81) s, respectively; The initial time of ptosis was (18.00±6.25), (10.30±2.87), (12.40±4.67), (6.20±3.00) s, respectively; The scores of ptosis were (2.30±1.34), ( 2.50±1.08), ( 2.50±1.65), ( 4.00±0.00), respectively.Baihe dihuang decoction with ganmai dazao decoction significantly decreased the duration of tailing suspension and forced swimming, at the same time reversed the ptosis by reserpine. Conclusion Baihe dihuang decoction plus with ganmai dazao decoction exhibits significantly antidepressant effect.
  • 中药及天然药物专栏
    ZHANG Quan-long;QIU Jian-guo;LI Mao-xing;WEI Li-li;HE Xi-rui;JIA Zheng-ping
    Objective To study the external hemostatic effect of the components from Herba Lamiophlomis Rotata. Methods The mouse taIL-cutting model, abdominal aorta incision, ears artery cutting in rabbits and the experimental model of superficial cut of liver in SD adult rats, were used to evaluate and compare the hemostatic effect by starch, yunnan baiyao powder, L.rotata aqueous extract (LRAE) and the iridoid glycosides extract of L.rotata (IGLR). Results In the tail cut mice model, the bleeding time for IGLR, LRAE, yunnan baiyao powder and starch groups were (64.8±25.0), (97.2±44.0), (105.1±65.0), (124.8±43.2) s, respectively. The average bleeding duration of superficial cut of liver for IGLR group was (93.8±39.5) s, (101.1±25.9) s for LRAE, (74.0±26.3) s for yunnan baiyao powder and (152.8±47.1) s for starch control. The IGIR group had significantly lower bleeding time than the placebo group in the abdominal aorta incision model and ears artery model (P<0.01), which was stronger than yunnan baiyao powder (P<0.05 or P<0.01). Likewise, the LRAE group showed significantly shorter bleeding time than the placebo group(P<0.01), but was longer than IGIR group. Conclusion Herba Lamiophlomis Rotata. provides hemostatic effects being applied externally, which is better than LRAE and yunnan baiyao powder.

  • 药物制剂与药品质量控制
  • 药物制剂与药品质量控制
    Hajinisa;Dilxat HEBIBULLA;Meriban ABDUREYIM;Haji Akber AISA
    Objective To extract and determine total flavonoids from Cydonia Oblonga Seeds and select the optimal extraction technology. Methods With rutin being taken as the standard indicator, the total flavonoids were determined by spectrophotometry at 506 nm to optimize the isolation technique. Results The total flavonoids in the samples were detected as 13.60 mg&#8226;g-1, and the best extraction process included using 75% ethanol, at a solid liquid ratio of 1:10, refluxing for 2.5 h at 60 ℃ and extracting for 3 times. Conclusion The content determination of total flavonoids from Cydonia Oblonga seeds by ultraviolet spectrophotometry with rutin as control is an accuracy, practical and simple method.

  • 药物制剂与药品质量控制
    LI Wei;WU Feng;WANG Wen-qing;HE Guo-fang;FANG Jian-guo;JIANG Han-ying
    Objective To establish a content determination method for kalium(K),natrium (Na) and magnesium(Mg)in a self-made nutrient solution by atomic absorption spectrometry(AAS). Methods Sodium chloride(NaCl)and strontium chloride(SrCl2) were used as deionization agents, respectively and K,Na and Mg were determined by FAAS method. Results The average recovery of K,Na and Mg were 99.1%,98.5%,100.0%(n=9)and RSD were 0.77%,1.51% and 0.99%,respectively. Conclusion This method showed good linearity, precision and accuracy, which can be used for quality control of K,Na and Mg in the selfmade nutrient solution.

  • 用药指南
  • 用药指南
    MA Zu-fu;JIANG Yuan-yuan;LI Li;YAO Ying
    Objective To investigate the distribution, drug resistance and rational use of antibiotics in complicated bacterial urinary tract infection. Methods To retrospect the clinical data and Results of drug susceptibility from 188 patients in our hospital with complicated urinary tract infection from 2004 to 2009. Results The Gramnegative bacilli(40.4% Escherichia coli and 8.5% Klebsiella pneumoniae) accounted for 69.1%,Enterococcus faecalis 10.6%,Enterococci 7.4%,coagulasenegative staphylococci 3.7%,fungi 4.3% among the pathogens caused complicated urinary tract infection. ESBL positive rate in 76 cases of Escherichia coli was 48.2%. The drug resistance to amoxicillin/clavulanic acid, cefoperazone/sulbactam, piperacillin/tazobactam, cefoxitin, amikacin, carbapenem, nitrofurantoin was low; while the resistance to ampicillin, piperacillin, cephalosporins, quinolones was high. Conclusion Escherichia coli is still the main pathogen for current complicated urinary tract infection in hospitals, the drug resistance of which is high and multiple, and is the most common bacterial strain producing ESBLs. The antimicrobial therapy should be adjusted under the guidance of drug sensitivity test.

  • 药事管理
  • 药事管理
    CHEN Li;TAN Guang-ming;HUANG Rui;FENG Zhan-chun
    Objective To investigate the status of drug use in new rural cooperative medical institutions and promote the level of rational drug use. Methods Randomly selected the outpatient prescriptions in county and township new rural cooperative medical institutions in a county in Henan province, analyzed the average kinds of drugs prescribed in each prescription, the average cost, and the percentage of outpatients that received antibacterial drugs, injections. Results Maximum numbers of drugs per prescription were 5 for county hospital and 9 for township hospital, and the mean numbers were 1.97 and 2.68 ,respectively. There were 52 prescriptions including antibacterial drugs in county hospitals, and 67.3% contained one kind of antibacterial drugs, 28.8% with two kinds, 1.9% of them consisted of three or four kinds of antibacterial drugs. While in township hospital, the number of prescriptions including antibacterial drugs was 35, 91.4% with one, 5.7% and 2.9% contained two and three kinds of those drugs respectively. The number of prescriptions with injections was 5 for county hospital and 32 for township hospital, meanwhile, the utilization rates of injections were 3.4 and 23.5, respectively. The maximum of per prescription expense of county hospitals was 380.2 yuan, minimum of that was 0.2 yuan, and the mean was 84.86 yuan, while the numbers of the township hospitals were 434, 0.4 and 50.58 yuan, respectively.Conclusion The status of drug use in sample medical institutions is general good, reduce prescription costs and quantities of prescription drugs in township level medical institutions should be strengthened. Improve the level of rational drug use in rural areas needs many efforts, which including the followings, improve the internal management of medical institutions, enhance knowledge and skills training of the rural doctors, cultivate awareness of rational use of drugs of the farmers and so on.