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Welcome to Chinese Journal of Clinical Pharmacology and Therapeutics,Today is Chinese

Table of Content

    Volume 15 Issue 12
    26 December 2010
    Therapeutic effects of total glucosides of Tibetan Herb Myricaria paniculata auct non Linn. Desv on adjuvant arthritis in rats
    ZENG Yang, MA Ji-xiong, BAO Min, CHEN Hai-juan, ZHANG Guo-yan, ZHANG Hong-quan
    2010, 15(12):  1321-1325. 
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    AIM: To study the therapeutic effect of total glucosides of Tibetan Herb Myricaria paniculata auct non Linn. Desv on adjuvant arthritis (AA) in rats and its mechanisms.METHODS: Freund's complete adjuvant (FCA) was used to induce AA in rats. The secondary paw swelling of AA rats was measured with volume meter and the polyarthritis index was scored. The changes of the levels of SOD and NO were assessed in blood serum. The synovium mononuclear macrophage (AM) productions of IL-1, TNF-α and PGE2 were estimated by enzyme linked immuno sorbent assay (ELISA).RESULTS: The secondary inflammation of AA rats appeared on the 12th day after injection of FCA. At the same time, total glucosides of Tibetan Herb Myricaria paniculata auct non Linn. Desv and indomethacin were given to AA rats by intragastric administration for two weeks. Total glucosides of Tibetan Herb Myricaria paniculata auct non Linn. Desv(1.0, 1.5 g/kg) could significantly inhibit secondary inflammatory reaction (secondary inflammatory swelling, multiple arthritis)of AA rats from the 24th day. Total glucosides of Tibetan Herb Myricaria paniculata auct non Linn. Desv could reduce the levels of the NO in blood serum and increase the activity of the SOD in blood serum. Meanwhile, total glucosides of Tibetan Herb Myricaria paniculata auct non Linn. Desv(1.0,1.5 g/kg) could remarkably down-regulate IL-1,TNF-α and PEG2 productions of AM.CONCLUSION: The results suggest that total glucosides of Tibetan Herb Myricaria paniculata auct non Linn. Desv have therapeutical effects on AA rats. Its mechanisms may be related to keeping the balance of cytokine network in AA rats and improving the capability of anti-oxidation effect.
    Established a new rat model of metabolic syndrome
    LONG Hui-dong, LIN Yun-en, ZENG Zhao-hua, LIANG Li-ying, LAN Zhong, ZHANG Hai-jun
    2010, 15(12):  1326-1329. 
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    AIM: To establish and evaluate a rat model of metabolic syndrome induced by high fat and salt diet.METHODS: Wistar rats, aged 3 weeks, which were divided into three groups in randomized manner: control with normal salt diet (0.5% NaCl, NS),high salt diet(4% NaCl,HS),fat and salt-enriched diet(49%fat+4%NaCl,FS), 12 rats in each group for 18 weeks.Then the bodyweights were measured. The right carotid artery was cannulated for direct blood pressure measurement. Insulin was measured in plasma sample by enzyme linked immuno sorbent assay(ELISA). Other remaining plasma samples were obtained for total cholesterol concentra tion(TC),triglyceride (TG),low density lipoprotein cholesterol (LDL-C),high density lipoprotein cholesterol (HDL-C),blood glucose(GLU).RESULTS: Compared with the NS and HS group, the body weight, blood pressure, insulin resistence index and triglycerol levels were all significantly increased in the FS group. But there was no significant difference between the NS and HS group.CONCLUSION: The fat and salt-enriched diet given to the rats can induce a metabolic syndrome,which corresponds or is analogous to the clinical metabolic syndrome.
    Effects of Glycyrrhiza uralensis decoction on liver cytochrome P450 in rats
    LIU Lin-na, WANG Ru-tao, WANG Qing-wei, ZHANG Yan
    2010, 15(12):  1330-1333. 
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    AIM: To investigate the effects of Glycyrrhiza uralensis decoction on liver cytochrome P450 in rats.METHODS: SD rats were randomly divided into four groups (control, enzyme inducer, enzyme inhibitor and Glycyrrhiza uralensis decoction groups) and drugs were administrated through intragastric route for 14 days. Control group were treated with saline, enzyme inducer group were treated with 3.0 mg/kg phenobarbital, enzyme inhibitor group were treated with 40 mg/kg cimetidine and Glycyrrhiza uralensis decoction group were treated with 1.0 g/kg decoction, respectively. Phenacetin, which used as a probe drug, was given to all rats by intra-peritoneal injection on the 15th day. The blood samples were collected at different time points. A developed HPLC method was introduced to determine the concentration of the probe drug in rat plasma and Das software was used to estimate the pharmacokinetic parameters.RESULTS: The t1/2 value of probe drug in groups of control, enzyme inducer, enzyme inhibitor and Glycyrrhiza uralensis decoction were (104±10),(178±15),(86±9) and(90±9) min, respectively.CONCLUSION: Glycyrrhiza uralensis decoction has inductive effects on rat liver CYP450.
    Pioglitazone improves the hepatic insulin resistance condition induced by high-fat diet
    LI Lan-fang, CHEN Lin-xi, GUO Yu, TANG Guo-tao, YU Cui-yun
    2010, 15(12):  1334-1338. 
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    AIM: To observe the effect of pioglitazone on oxidative stress and insulin resistance in rats with high-fat diet.METHODS: Four-week male SD rats were chosen and divided into four groups: Control group, High-fat diet group, Pioglitazone group, Pioglitazon and high fat diet group. After 12 weeks feeding, the plasma glucose and insulin levels were detected, the insulin sensitivity index was counted. The liver intracellular glycogen content was measured using a glycogen assay kit. ROS generation in liver tissues was assessed by DHE fluorescence.RESULTS: The insulin sensitivity index of control group was -3.47±0.39 after feeding with high-fat diet for 12 weeks, the blood glucose content was increased,the insulin sensitivity index was decreased to -6.29±0.54, and pioglitazone increased the insulin sensitivity index to -4.54±0.33. The hepatic glycogen content in rats fed with high-fat diet was significantly decreased to (13.6±2.7) mg/g, confirming insulin resistance. But pioglitazone promoted hepatic glycogen content [(19.6±2.9) mg/g]. The DHE dyeing in hepatic tissue slices showed the ROS level was increased in rats with a high-fat diet. However, pioglitazone could decrease the ROS level of liver.CONCLUSION: Pioglitazone improves the hepatic insulin resistance condition by degrading oxidative stress level.
    Effects of paroxetine on cortisol and behavior of rats with psychological stress
    HUANG Huan-jie, SHAO Bei, ZHENG Rong-yuan, LI Jian-min
    2010, 15(12):  1339-1342. 
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    AIM: To study the effects of paroxetine on the level of cortisol and behavior of rats with psychological stress.METHODS: The rat psychological stress model was made by restraint stress. Expression of c-fos positive cells was detected by SP immunohistochemical assay in the rat PVN. The cortisol was analysed by radioimmnoassay and the behaviors of rats were tested in open-field conditions.RESULTS: The expression of c-fos positive cells, the crossing scores ,the rearing scores and the level of cortisol increased more significantly in the other groups than those in the control group , but decreased in the paroxetine group(P<0.05). The paroxetine inhibited the expression of c-fos positive cells in the PVN and the behaviors,reduced the level of cortisol of rats after psychological stress.CONCLUSION: The effects of paroxetine on the anxiety disorders in rats may be related to inhibit the expression of c-fos positive downregulation of the activation of HPA pathway.
    Effect of histamine on fat synthesis and regulation in the white adipocytes: a mechanism research
    ZENG Hui, LIU Zhao-qian
    2010, 15(12):  1343-1347. 
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    AIM: To study the effect of histamine on fat synthesis in the differentiated 3T3L1 cell in vitro and its mechanisms.METHODS: The 3T3L1 cells cultured and induced it to white fat cells.The levels of aP2 mRNA in the adipocytes under the treatment of histamine and diphenhydramine were detected by RT-PCR techniques.RESULTS: Histamine increased the expression of aP2 mRNA in the adipocytes, the concentration-dependent effect curve discovered the highest expression of aP2 mRNA was at 20 μmol/L, the time-dependent effect curve discovered the highest expression of aP2 mRNA was at 6 h.Compare with the same concentration of histamine, diphenhydramine decreased the expression of aP2 mRNA(P<0.05).CONCLUSION: Histamine increased the expression of aP2 mRNA in the differentiated 3T3L1 cell.Diphenhydramine inhibited the expression of aP2 mRNA. Histamine can increase the fat synthesis and maintain the balance of energy metabolism in the white adipocytes.
    Experimental study on astragalus polysaccharides promoting the human dendritic cells maturation in vitro
    WANG Qiong, ZHU Xue-jun
    2010, 15(12):  1348-1352. 
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    AIM: To study the effects of astragalus polysaccharides (APS) on maturation and survival time of human dendritic cells (DCs) in vitro.METHODS: Peripheral blood mononuclear cells from healthy volunteers were cultured for 2 hours to acquire adherent monocytes. The monocytes were cultured with rhGM-CSF (1000 U/mL) and rhIL-4 (500 U/mL) in serum-free medium. The experimental groups were added three concentrations of APS (1 μg/mL, 10 μg/mL, 100 μg/mL), the control group were added equal volume of saline. One group of cells were cultured for 7 days and the cell suspension were collected to get normal DCs (Mo-DCs) or APS -induced DCs (APS-DCs) . The immunophenotyping was detected by flow cytometry, T cells stimulating activity of DCs were detected by allogeneic mixed lymphocyte reaction. Another group of cells were continuously cultured for 14 days and the cell morphology and survival time were observed under light microscope.RESULTS: APS could significantly promote the DCs surface HLA-DR, CD83, CD80, CD86, CD40, CD54 expression. APS-DCs compared with Mo-DCs had a stronger T-cell activation activity. APS significantly extended the DCs survival time up to 2-3 days in vitro.CONCLUSION: APS could promote DCs maturation and extend the survival time of DCs, which may enhance the immunity.
    Screening of tumor mark for the lung cancer by using peptide ZS-1
    WANG Su-jun, PAN Xue-diao, ZANG Lin-quan, WANG Gui-xiang, SHI Lei, XIE Hai-tang
    2010, 15(12):  1353-1357. 
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    AIM: To select a potential biomarker for early lung cancer diagnosis and targeted therapy by using the cancer specific bounded peptide ZS-1 which had already been obtained from the laboratory.METHODS: The peptide ZS-1 marked by biotin was used as a probe to pan out the human lung cancer cDNA phage display library,after 3 rounds of subtraction panning,the specific binding clones of ZS-1 were identified.After amplification and purification,then those DNA sequences were identified and analyzed with bioinformatics. Tissue microarray technology was used to detect biomelecule in tissues.RESULTS: The lung cancer membrane receptor protein KIAA1199 binding ZS-1 was first found by bioinformatics analysis. Subsequently, a specific human lung cancer tissue microarray was detected and analysed by KIAA199 antibody.The results displayed KIAA1199 positive detection rate was 32.8%.CONCLUSION: A tumor biomarker KIAA1199 selected from human lung cancer cDNA library provides a potential tool for early lung cancer diagnosis and therapy.
    Protective effect of glycosides of Cistanches on CCl4 damaged mice
    LUO Hui-ying, YANG Huan, ZHU Li-juan, GAO Zhong-qing, YANG Hai-lin
    2010, 15(12):  1358-1361. 
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    AIM: To investigate the protective effect of glycosides of Cistanches (GCs) on CCl4 damaged mice.METHODS: 40 mice were randomly divided into 4 groups, control group,CCl4 model group,Cistanches groups (62.5,125 mg·kg-1·d-1). The acute liver damage mode was established by CCl4 peanut oil in mice. The mice were received intragastric administration twice a day. After 14 d,the effect of GCs on ALT, AST, ALP and pathological changes were detected.RESULTS: GCs could obviously reduce the levels of ALT, AST and ALP in CCl4 damaged mice, as well as moderating hepatocyte cytoclasis.CONCLUSION: GCs has protective effect on CCl4 damaged mice.
    Establishment of traumatic brain injury model in rats
    GU Bing, JIN Jian-bo, MENG Wei, LI Hua-nan
    2010, 15(12):  1362-1367. 
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    AIM: To establish a rat model for controlled cortical impact brain injury.METHODS: Traumatic brain injury(TBI) model in rats was duplicated by controlled cortical impact brain injury method with a BenchmarkTM stereotaxic impactor.Cognitive function was evaluated at 1, 3, 5, 7, 28 day after TBI with Morris water maze. And then morphological changes was carefully inspected in the injured part and adjacent area.RESULTS: Compared with the sham-operated rats, the time for brain injured rats to find hidden platform were significantly prolonged. Neuronal cells were swollen or loss, and glia cells remarkably increased in the injured sites and hippocampus areas.Neuron and its axon degeneration was observed by using curpric-silver straining technique.CONCLUSION: The rat model for controlled cortical impact brain injury is reproducible and suitable for the pharmacodynamic screening of brain protective drugs.
    Effects of metformin on the proliferation of vascular smooth muscle cells induced by advanced glycation end products
    FANG Li-juan, LIU Nai-feng
    2010, 15(12):  1368-1372. 
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    AIM: To observe the effects of advanced glycation end products on the proliferation of vascular smooth muscle cells(VSMCs) and how the course are interfered with metformin.METHODS: Well-conditioned VSMCs were dealed with different concentrations of advanced glycation end products (50,100,200,400 mg/L) in different times (12,24,48,72 h). On the basis of above treatments, different concentrations of metformin (10-3,10-4,5×10-5,10-5,10-6 mol/L) were given to interfere VSMCs, combined with the 200 mg/L AGEs on different times (12,24,48,72 h). The proliferation of VSMCs was measured by MTT.RESULTS: 50 mg/L AGEs could promote the proliferation of VSMCs at the time point of 72 h; 200 mg/L AGEs began to play the role of promotion at the time point of 12 h, furthermore, 24 h were the strongest. The effects of 400 mg/L AGEs was similar to those of 200 mg/L AGEs at all the time points. 10-3 mol/L and 10-4 mol/L metformin had the strongest effects of inhibition at the time point of 12 h, and this effect continued to 72 h. 10-6 mol/L metformin had lower inhibition on proliferation and its effective time was from 24 h to 72 h.CONCLUSION: AGEs can promote the proliferation of vascular smooth muscle cells in a concentration- and time- dependent manner; metformin can inhibit the proliferation of vascular smooth muscle cells induced by AGEs.
    Effects of cornel iridoid glycoside on platelet aggregation and bleeding time in rabbits and rats
    BAI Ying, WANG Shi-quan, ZHANG Lan, ZHANG Ru-yi, YIN Lin-lin, ZHANG Li, LI Ya-li, LI Lin
    2010, 15(12):  1373-1376. 
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    AIM: To investigate the effects of cornel iridoid glycoside (CIG) on platelet aggregation and bleeding time.METHODS: Born's turbidimetry was used to measure platelet aggregation rate in rabbits (in vitro) and blood stasis model rats (in vivo). The tail-cutting method was applied to determine the bleeding time in rats. The blood stasis rat model was established by adrenalin and ice water stimulus method.RESULTS: In vitro study showed that CIG (0.75~3 mg/mL)significantly inhibited platelet aggregation induced by ADP or AA (P<0.05, P<0.01), and CIG (6~12 mg/mL)obviously inhibited platelet aggregation induced by PAF (P<0.01) in rabbits. In vivo study demonstrated that intragastric administration of CIG (180 mg/kg) markedly inhibited platelet aggregation induced by ADP in blood stasis model rats (P<0.01), and prolonged the bleeding time in normal rats (P<0.05).CONCLUSION: CIG has the effect of anti-platelet aggregation, and its high dose can prolong the bleeding time.
    Study on the therapeutic effects of ferulic acid sodium in cerebral hemorrhage model rats induced by collagenase and its mechanism
    SUN Yu-ming, LOU Jian-Tao, HUANG Guang-xiang, SUN Jun
    2010, 15(12):  1377-1382. 
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    AIM: To investigate the therapeutic effects of ferulic acid sodium in cerebral hemorrhage model rats induced by collagenase and its mechanism.METHODS: 108 male SD rats were randomly divided into 3 groups,including sham operation group, acute cerebral hemorrhage group(ICH model group), ferulic acid sodium intervention group(treatment group).Each group including 6 subgroups:2,6,24,48,72 h,1 week group.Treatment group intraperitoneal injection ferulic acid sodium 100 mg·kg-1·d-1 which was diluted by 3 mL NS. ICH model group intraperitoneal injection NS.After 7 days, the changes of neuroethology in each group were observed, the brain water content was detected,the expression of AQP4 mRNA was detected by RT-PCR, and the level of plasma endothelin was determined.RESULTS: Compared with the sham operation group,the the Longa evaluation was obviously increased in the ICH model group and the treatment group before treatment. Compared with the ICH model group,the Longa evaluation was obviously decreased in treatment group (P<0.05) during 6 to 48 h;and the limbs symmetry score was significantly decreased in treatment group during 6 h to 1 week (P<0.05);the balance beam score was significantly decreased in treatment group during 24 hours to 1 week(P<0.05).At the 48 and 72 h,the levels of brain edema in treatment group were significantly inhibited(P<0.05).Compared with the ICH model group,the mRNA expression in treatment group was decreased after making model 72 h,there was no significant difference (P>0.05) .During 6 to 72 h,the level of plasma endothelin was significantly decreased (P<0.05)in treatment group.CONCLUSION: Treating cerebral hemorrhage by ferulic acid sodium can improve neuroethology and anti brain edema,its mechanism is related to reducing the generation of endothelin.
    Inhibitory effect of botulinum toxin type A on acetylcholine induced contractile response in rat pyloric smooth muscle in vitro
    XU Gui-zhong, LIU Xiang-wen, HOU Yi-ping
    2010, 15(12):  1383-1387. 
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    AIM: To investigate the effect of botulinum toxin type A (BTX-A) on endogenous and exogenous acetylcholine (ACh) induced contractile response in rat pyloric smooth muscle in vitro.METHODS: The effects of BTX-A and atropine on pyloric contractility-induced respectively by electrical field stimulation (EFS), which is used to promote endogenous ACh release, and by ACh addition were comparatively evaluated.RESULTS: BTX-A inhibited the pyloric smooth muscle contractility-induced by EFS (P<0.001). Both of atropine and BTX-A significantly abolished pyloric contractility-induced by ACh (P<0.001), but BTX-A incompletely did it.CONCLUSION: The evidence of the inhibitory effect of BTX-A on pyloric contractility-induced by EFS suggests that BTX-A inhibits endogenous ACh release through cleaving SNAP-25 protein within presynaptic membrane. The result of the inhibition of BTX-A on ACh induced pyloric contractile response is similar to atropine, suggests that BTX-A probably acts on postsynaptic receptor or pyloric muscle directly.
    In vitro activities of levofloxacin in combination with fosfomycin against staphylococcus aureus
    SONG Xiu-jie, JU Hong-mei, YU Xu-hong, LIN De-feng, WANG Rui, LIU You-ning
    2010, 15(12):  1388-1394. 
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    AIM: To investigate the in vitro bactericidal activity of levofloxacin alone and combined with fosfomycin against 3 strains MSSA and 1 stain MRSA.METHODS: Three MSSA strains and 1 MRSA from clinical specimens were used in this study. Time-kill curve method was carried out with different concentration of the two drugs both alone and in combination.RESULTS: Levoloxacin alone showed a concentration-dependent time-kill curve against three strains of MSSA, fosfomycin showed a nonconcentration-dependent time-kill curve. Neither levofloxacin nor fosfomycin alone inhibited bacterial growth at 1/4 MIC; but the combination of this two drugs at 1/4 the respective MIC showed a synergistic bactericidal effect, a 2-3 log10 decrease with respect to the most active antibiotic alone.CONCLUSION: The combination of subinhibitory concentrations of levofloxacin and fosfomycin presented synergism,exerting a bactericidal effect. The combination also has a bactericidal effect against MRSA.
    Ligase-based method to detect the polymorphism of warfarin related genes: VKORC1,CYP2C9
    ZHANG Ya-tong, LIANG Xin, HU Xin, LI Ke-xin, YANG Li-ping
    2010, 15(12):  1395-1401. 
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    AIM: To establish one ligase-based method to detect the polymorphism of warfarin related genes.METHODS: The multiplex PCR/ ligase detection reaction(LDR) was established to detect warfarin related genes(VKORC1,CYP2C9) polymorphisms and 207 Han Chinese was detected using this method.RESULTS: No CYP2C9*2(rs1799853)was detected and the frequency of CYP2C9*3,VKORC1:1173C>T,VKORC1:3730G>A,VKORC1:-1639G>A were 4.35%, 5.8%, 5.31%, 6.76%,respectively . The mutation frequency of rs4086116 which located in the 3rd intron of CYP2C9 was 10.14%.CONCLUSION: This method is accurate, time-saving and labor-saving. And the detection results of the blood sample consistent with previous results.
    Clinical observation on compound matrine injection plus interleukin-2 in the treatment of malignant pleural effusion induced by lung cancer in elder
    ZHOU Ying, XU Xian-rong, ZHOU Ping
    2010, 15(12):  1402-1405. 
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    AIM: To evaluate the efficacy and toxicity of pleural perfusion with compound matrine injection plus interleukin-2 in the treatment of elderly patients diagnosed as malignant pleural effusion induced by lung cancer.METHODS: 60 elderly patients diagnosed as malignant pleural effusion induced by lung cancer were randomized to either therapy group or control group: the patients' pleural cavity in the therapy group were infused with compound matrine injection 30 mL plus interleukin-2 2 milion IU, while the pleural cavity of the control group were infused with interleukin-2 2million IU. The treatment of two group were repeated after a week for a total of four times. After four weeks, the efficacy, quality of life and side effect were recorded.RESULTS: The response rate (RR) in the therapy group were significantly higher than these in the control group (86.7% vs 63.3%, P<0.05) ; The KPS scores(>70)in the therapy group was significantly higher than that in the control group after treatment (P<0.05). The adverse effects of chest pain, nausea and disgorging in the therapy group wese significantly lower than these in the control group (P>0.05), except fever.CONCLUSION: Compound matrine injection plus interleukin-2 shows proved efficacy and slight side-effect for elderly patients diagnosed as malignant pleural effusion induced by lung cancer efficacy in that the quality of life of the elderly has been improved, thus it serves as an effective regimen for elderly malignant plural effusion patients.
    Effects of recombinant human brain natriuretic peptide in Non-ST-segment elevation acute myocardial infarction patients with heart failure
    QIAO Hua, HE Sheng-hu, JI Jun, CHEN Shu, LIU Xiao-dong, XU Ri-xing, XIE Yong
    2010, 15(12):  1406-1409. 
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    AIM: To evaluate the effect and adverse reactions of recombinant human brain natriuretic peptide(rhBNP) in Non-ST-segment elevation acute myocardial infarction patients with heart failure.METHODS: Treatment group:26 cases of conventional drug therapy based on rhBNP to the treatment; Control group: 27 patients received routine treatment. Vital signs, respiratory difficulty, BNP and related changes in hemodynamics were observed before and after treatment.RESULTS: The two groups in clinical performance(including symptoms and signs),functional class,left ventricular ejection fraction,urine volume(average urine volume per hour)and so,the difference was significant (P<0.05).CONCLUSION: rhBNP for Non-ST-segment elevation acute myocardial infarction (NSTEMI) with heart failure have a significant effect, but a low incidence of adverse reactions.
    Effects of hemopoietic stem cell mobilized by Hyper-CVAD/MA+G-CSF on lymphoma patients
    CHEN Jun-fa, ZHENG Zhi-yin, SHEN Jian-ping, ZHOU Yu-hong
    2010, 15(12):  1410-1413. 
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    AIM: To investigate the clinical effects of hemopoietic stem cell mobilized by Hyper-CVAD/MA (methopterin+cytarabine)+granulocyte colony-stimulating factor (G-CSF) regimen on lymphoma patients.METHODS: 25 patients with aggressive non-Hodgkin lymphoma (NHL) were randomly divided into two groups, which were separately applied with cyclophosphamide+G-CSF regimen (Control group) and Hyper-CVAD/MA+G-CSF regimen (Study group) to mobilize hemopoietic stem cells. And then mobilization and safety were detected.RESULTS: The data in the study group was successfully collected on the first try, the times of collection in the study group was significant reduced compared to that of the control group (P<0.01); The total number of CD34+ cells in the study group and control group were separately (5.45±4.63)×106/kg and (3.04±0.74)×106/kg, which had no significant difference(P>0.05); There was a similar incidence rate of infection between the two groups (P>0.05); In addition, there was no significant difference in the incidence rate of thrombocytopenia between the two groups(P>0.05).CONCLUSION: Hemopoietic stem cells mobilized by Hyper-CVAD/MA+G-CSF on lymphoma patients was not only safe and effective but also easy to operate. Addionally, it played the role of in vivo purging prior to transplantation. Therefore, it gained two advantages by this regimen.
    Effects of intensive insulin therapy on the prognosis and serum vWF,ET-1 and NO levels in patients with sepsis
    MAO Yao-sheng, CAO miao-ying, ZHOU Xin
    2010, 15(12):  1414-1417. 
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    AIM: To investigate the effects of intensive insulin therapy on the prognosis and serum vWF,ET-1,NO levels in patients with sepsis.METHODS: Ninety patients were randomly assigned to intensive insulin therapy group and conventional insulin therapy group, serum von Willebrand factor (vWF), endothelin-1 (ET-1) and nitric oxide (NO) of the two groups of patients were determined by enzyme-linked immunoadsorbent assay double antibody sandwich principle (ELISA) before treatment and the next 3 d,7 d after treatment. At the same time we observed the two groups of patients with the days of hospitalized in ICU, number of days for using mechanical ventilation , the last day of APACHE II score in ICU and incidence rate of hypoglycemia and 28 d mortality.RESULTS: Compared with conventional insulin therapy group, vWF, TM and ET-1 levels in intensive insulin therapy group were significantly decreased (P<0.05),NO were significantly higher (P<0.05);and the days of hospitalized in ICU, number of day for using mechanical ventilation, the last day of APACHE II score in ICU, 28-d mortality were significantly decreased (P <0.05)in intensive insulin therapy group, and incidence rate of hypoglycemia of two group had no difference(P>0.05).CONCLUSION: Intensive insulin therapy in patients with sepsis can reduce serum vWF, ET-1 levels and elevate NO levels,at the same time can reduce the case-fatality rate of patients,improve the prognosis.
    Roles of drug metabolism enzymes in drug resistance of tumor
    ZHOU Ying, ZHOU Fang, WU Xiao-lan, WANG Guang-ji
    2010, 15(12):  1418-1427. 
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    Tumor chemotherapy is one of the most commonly used and effective treatment in antitumor therapy, but drug resistance usually leads to tumor chemotherapy failure. Drug resistance of tumor is often caused by varied mechanisms, of which the drug metabolism enzymes play very important role. In recent years, researchers found that there were many kinds of drug metabolism enzymes related to drug resistance of tumor. Such as Phase I enzymes (cytochrome P450 enzymes, COX-2), PhaseⅡ enzymes(GST, UGT, GCS, NQO1), and Phase Ⅲ enzymes drug transporter protein. In this article, we reviewed the correlation between drug metabolism enzymes and drug resistance of tumor, in order to provide a new way for anti-tumor therapy.
    Mechanism profile for arousal effects of modafinil
    CHEN Chang-rui, QU Wei-min, HUANG Zhi-li
    2010, 15(12):  1428-1433. 
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    Modafinil is a potent wake-promoting compound with low abuse potential used in the treatment of narcolepsy and day time sleepiness. The compound is reported to affect multiple neurotransmitter systems such as catecholamines, serotonin, glutamate, GABA, orexin, and histamine, however, the molecular mechanism by which modafinil increases wakefulness is debated. It was previously testified that arousal effects of modafinil were not exhibited in dopamine transporter KO mice; furthermore, treatment of dopamine (DA) D2 receptor (D2R)-deficient mice with D1R-specific antagonists completely abolished arousal effects of modafinil. These findings strongly indicate that dopamine and dopaminergic D1R and D2R are essential for the wakefulness caused by modafinil, and its influence on other neurotransmitter systems may result from enhanced dopaminergic activity and wakefulness.This review summarizes the progress on mechanism profile for arousal effects of modafinil.
    Progression of ADP receptor inhibitors antiplatelet drugs
    WU Ya-ning, ZHAO Di, LI Ning, CHEN Xi-jing
    2010, 15(12):  1434-1440. 
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    Antiplatelet therapy has a well established role as an antithrombotic agent in the settings of percutaneous coronary intervention and acute coronary sydromes, and it has been successful in reducing mortality and morbidity in the two diseases above-mentioned. Recently, the most commonly used drugs were aspirin and clopidogrel, but some clinical data indicate that the combination of these two drugs doesn't work well for all the patients, which may cause some cardiovascular adverse reactions. Therefore, it's extremely necessary to do some further research on a number of promising new anti-platelet drugs. This article reviews the metabolic and onset characteristic of ADP receptor inhibitors antiplatelet drugs (e.g. clopidogrel, prasugrel, ticagrelor, cangrelor) in the treatment of cardiovascular disease and provide a reference for clinical medicine.