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Table of Content

    Volume 9 Issue 6
    26 June 2004
    Advance of drug metabolism enzyme P450 2C9
    CHEN Kun, WANG Rui
    2004, 9(6):  601-606. 
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    P450 2C9 is the most important drug metabolizing enzymes in humans.Polymorphisms in P450 2C9 gene produce variants at amino acid including P450 2C9 *2 and P450 2C9 *3.Metabolic capacities for P450 2C9 substrates are diminished by individuals of homozygous.P450 2C9 substrates mainly include tolbutamide, phenytoin, S-warfarin, fluoxetine, and losartan.P450 2C9 can be induced by rifampin and inhibited by amiodarone and fluconazole.
    Apoptosis of tumor cells induced by artesunate is associated with suppressing survivin expression
    LI Zhe, YUAN Shou-Jun, NIE Li-Ping, TIAN Zeng-Yue, XU Lan-Ping, HAN Chang-Ming
    2004, 9(6):  607-611. 
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    AIM: To study the relations between apoptosis of tumor cells induced by artesunate (Art)and expression of survivin. METHODS: Tumor cells were exposured to different concentrations of Art, apoptosis was examined by fluorescent staining, flow cytometry, agarose gel electrophoresis (AGE)and Caspase-3 activity assay. The expressions of survivin mRNA and survivin protein were assayed with RT-PCR and Western blotting after cells treated with Art. RESULTS: With Art treatment, HL60 cells showed typical apoptotic features, including chromatin condensation and apoptotic bodies (fluorescent staining), and apoptosis rate of tumor cells increasing in concentration-dependent manners (flow cytometry), DNA ladder (AGE), activity of Caspase-3 enhancing.Analysis of RT-PCR indicated that expression of survivin mRNA was reduced in concentration-dependent manners after A549 cells were exposured to 10 and 50 mg·L-1 Art for 72 h.Intensity ratios between survivin strip and GAPDH strip in control, 10 and 50 mg·L-1 Art groups were 1.745, 0.390 and 0.023, respectively.Western blotting detection was also indicated that Art inhibited expression of survivin protein. CONCLUSION: Tumor cells apoptosis induced by Art might be associated with suppressing survivin expression.
    Protective effects of onychin on oxidative injured endothelial cells
    GUO Yu, YAN Peng-Ke, ZHU Bing-Yang
    2004, 9(6):  612-614. 
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    AIM: To investigate the protective effects of onychin on oxidative injured endothelial cells and its protective mechanism. METHODS: The injured model was established by endothelial cell treated with oxLDL. Protective effect of onychin on growth inhibition of endothelial cells injured by oxLDL was determined by MTT assay;NO concentrations in the medium were determined by nitrate reductase assay.The damage degree of endothelial cells was assessed by showing the TBARS and LDH levels in conditioned media. RESULTS: Onychin with various concentrations, given 24 hours, could decrease the growth inhibitory rates of endothelial cells injured by oxLDL, increase NO concentration and decrease the TBARS and LDH levels in the medium. CONCLUSION: Onychin can protect endothelial cells against oxidative damage.
    Inhibitory effect of hydrocortisol on regulatory volume decrease in Jurkat cells
    KANG Jin-Song, JIANG Pin, FENG Juan, ZHANG Hai-Long, LI Zhi-chang, TANG Fu-Lei, FANShao-Guang, ZHU Shi-Gong, SONG Demao
    2004, 9(6):  615-618. 
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    AIM: To study the effect of hydrocortisol on regulatory volume decrease (RVD)in Jurkat cells and its possible mechanism. METHODS: The measurement of Jurkat cell volume was performed under the microscope and the imaging analysis which was carried out by Motic Images Advanced 3.1 Software.The cell proliferation was measured with 3H-TdR incorporation. RESULTS: Hydrocortisol (10-4 and 10-3 mol·L-1)inhibited RVD in Jurkat cells with dose dependent manner.A potassium channel blocker (quinine)was also found to have an inhibition to Jurkat cell RVD.The Jurkat cell proliferation (including with and without Con A)was significantly suppressed by hydrocortisol (10-3 mol·L-1)and quinine (10-3 mol· L-1). CONCLUSION: The inhibition of Jurkat cell RVD induced by hydrocortisol might be from the inhibition of potassium channel.
    Studies on distribution in mice tissues of α-Glycyrrhizic acid and β-Glycyrrhizic acid
    FAN Yi, DING Jian-Hua, LIU Su-Yi, ZHANG Xu-Ning, LIU Qiang, ZHANG Jing, HU Gang
    2004, 9(6):  619-622. 
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    AIM: To examine the characters of distribution of two epimers of glycyrrhizic acid (GL) including α-GL and β-GL in mice. METHODS: After iv administration of a single 53.0 mg·kg-1 α-GL or β-GL in mice at 5, 15, 30, 60, and 180min, the concentrations of α-GL or β-GL in some tissues were determined by HPLCUV method, and the features of distribution of α-GL and β-GL were evaluated and compared. RESULTS: α-GL and β-GL were all quickly distributed.Except the plasma, the concentrations of α-GL and β-GL were higher in the liver than that in other tissues.The second peak of enterohepatic circulation could be observed at 30 min after iv administration.The concentration of α-GL in the liver was significantly higher than that of β-GL, but it was lower than or similar to that of β-GL in the plasma and other tissues after iv.Then the levels declined rapidly in all tissues but the intestine at 180min after iv administration, meanwhile, β-GL maintained rather high concentrations in various tissues, which were all 30 %-70 % of the peaks. CONCLUSION: After iv administration, α-GL is target to the liver, and can be efficiently converted to more α-GA than β-GL, and it nearly has no accumulation in the tissues.The tissue distribution of β-GL inmice appears to be wild throughout the body, and the metabolism is slower than that of α-GL to accumulate in some tissues.
    Pharmacokinetics and relative bioavailability of compound metformin hydrochloride and glibenclamide capsule in healthy Chinese volunteers
    YIN Xiao-Xing, ZHANG Yi-Di, DING Li, SHEN Jian-Ping, LI Li-Min, QIU Jun
    2004, 9(6):  623-627. 
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    AIM: To compare pharmacokinetics and relative bioavailability of metformin and glibenclamide in compound metformin hydrochloride and glibenclamide capsule (CMGC) with the reference preparations metformin tablet (MT) and glibenclamide tabet (GT). METHODS: Twenty male healthy volunteers were enrolled in a randomized two-way crossover design with a single-oral dose study.The plasma metformin and glibenclamide concentrations were determined by high performance liquid chromatography (HPLC) and liquid chromatography-mass spectrography (LC-MS), respectively.Pharmacokinetics parameters were calculated and bioequivalability was analyzed by two one-side t-test. RESULTS: The pharmacokinetics parameters of metformin in CMGC and co-administration of metformin glinbenclamide were as following, respectively:Cmax (1.87 ± 0.36 and 1.77 ±0.35) mg·L -1;Tmax (1.7 ±0.6 and 1.8 ±0.5) h;AUC0-∞ (8.13 ±1.32 and 8.62 ±1.47) mg·L -1·h -1, while those of glinbenclamide were as following, respectively: Cmax (129.2 ±51.4 and 123.9 ±50.7) μg·L -1;Tmax(2.3 ±0.7 and 2.6 ±0.9) h;AUC0-∞ (0.690 ±0.228 and 0.632 ±0.211) mg·L -1·h -1.Relative bioavailability of metformin and glibenclamide in CGMC were 95.0 % ±11.5 % and 109.6 %±8.8 %, respectively. CONCLUSION: The main components of CMGC, metformin and glibenclamide, are bioequivalent to the reference tablets, MT and GT.
    Antitumor effects of recombinant L-asparaginase modified by polyethylene glycol for mice leukemia cell P388
    CAO Rong-Yue, QIAN Zhi-Yu, JING Yong-Hua, SHEN Ke-Yu, LIU Jing-Jing
    2004, 9(6):  628-632. 
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    AIM: To study the antitumor effects of chemical modification enzyme which recombinant L-asparaginase (rL-ASP)modified by monomethoxy-polyethylene glycol (mPEG). METHODS: PEG modification of rLASP formed rL-ASP-PEG and compared molecular weight of rL-ASP and rL-ASP-PEG with sodium dodecyl sulfaete polyacrylamide gel electrophoresis (SDS-PAGE).Anti-tumor activity was tested by (3-(4, 4-dimcthylthioazol-2-yl)-2, 5-diphenyl tetrazolium bromide analysis(MTT)and apoptosis was valued by flow cytometry (FCM)in vivo.The effect of Anti-tumor activity was evaluated by weights of solid tumor of P338 on DBA/2 mice in vitro.Transmission electron microscopy (TEM)observed the effects of rLASP-PEG inhibiting P388 solid tumor on DBA/2 mice. RESULTS: rL-ASP-PEG had significant antitumor effects on P388 cells, and the inhibitory concentration 50 %(IC50)of rL-ASP-PEG was 2.056 IU·ml-1 .FCM data showed that the ultramicro pathological picture of transplant tumor in TEM that L-ASP-PEG reacting showed the tumor cells necrosis. CONCLUSION: rL-ASP-PEG shows a significant effect of antitumor.
    Establishment of RT-PCR for detecting clock genes in cultured rattus cardiac myocytes
    WEI Li, LI Xiao-Lin, HUANG Xin-Yan, LI Qing-Ping
    2004, 9(6):  633-636. 
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    AIM: To establish a PCR method for investigating the expression of clock genes in cultured rattus cardiac myocytes. METHODS: PCR was carried out using 3 primer pairs based on the published sequences of dbp, bmal1 and per2 genes of rattus.The conditions of PCR were optimized and the specificity of amplication was tested. RESULTS: In a volume of 20 μl, the optimal PCR mixture of bmal1 gene contains 0.5 U Taq polymerase, 0.006 μmol dNTP and 0.035 μmol Mg2+;the annealing temperature being 57 ℃;and circle times being 30.In a same volume, the optimal PCR mixture of dbp gene contains 0.5 U Taq polymerase, 0.006 μmol dNTP and 0.03 μmol Mg2+;the annealing temperature being 58 ℃;and circle times being 32.The optimal PCR mixture of per2 gene contains 0.5 U Taq polymerase, 0.006 μmol dNTP and 0.05 μmol Mg2+;the annealing temperature being 57 ℃;circle times being 30.The specificity of amplication was very high. CONCLUSION: The PCR method can successfully detect mRNA expression of clock genes in cultured rattus cardiac myocytes.
    Protective effects of pivanampeta on myocardial ischemia induced by isoproterenol in mice
    YU Bao-Rui, LONG Chao-Liang, XIA Yun-Feng, LIU Tong-Ku, WANG Hai
    2004, 9(6):  637-640. 
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    AIM: To evaluate the protective effects of pivanampeta onmyocardial ischemia induced by isoproterenol (ISO) in mice. METHODS: Forty-nine Kunming mice were divided into five groups randomly, each group including 8-11 mice and administered for 7 days.NS in control and ISO groups were given NS 10 ml·kg-1 twice a day.The three doses of pivanampeta (1.0, 5.0, and 25.0 mg·kg-1) in treatment groups were given by ig twice a day respectively.In the last two days, ISO was used at 20 mg·kg-1 sc half an hour after NS or pivanampeta were administered once a day in ISO and treatment groups, while NS was injected subcutaneously in control group continuously.Two hours after last subcutaneous administration of ISO or NS, the blood and hearts of mice were obtained to measure the serum levels of LDH and CK and to investigate the morphological changes of myocardium, respectively. RESULTS: Compared with the control group, the levels of LDH and CK in ISO groups were increased significantly (P <0.01), and morphologically severe injury was found in myocardial tissue and cells. And in each treatment group, the levels of LDH and CK were reversed (P <0.05), and myocardial injury reduced in comparison with that of ISO group. CONCLUSION: Pivanampeta has exact protective effect on myocardial ischemia mice induced by ISO in a dose-dependent manner.
    DNAzymes inhibit the expression of Methecillin-resistant staphlococcus aureus drug-resistant genes
    LIU Jie, LUO Xiao-Xing, MENG Jing-Ru, HU Ben-Quan, WANG Hai-Fang, MENG Jia
    2004, 9(6):  641-645. 
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    AIM: To evaluate the inhibition effects of DNAzymes specific to Methecillin-resistant staphylococcus aureus (MRSA)drug-resistant gene blaR1 on the expressions of drug-resistance. METHODS: mRNA of blaR1 was chosen as a target gene and DNAzyme DrzB specific to it was designed and synthesized.After DrzB was introduced into the MRSA, drug-resistant characters of MRSA were evaluated by cloning efficiency.The inhibition effects of DrzB on the expressions of drug-resistant gene blaR1 were observed by RT-PCR in MRSA. RESULTS: Colony forming units (CFU)of MRSA incubated with DrzB on the M-H agar added oxa (6 mg·L-1)were less than those of control group (P <0.01).Levels of blaR 1 mRNA of the DrzB group were lower than those of the control group (P <0.01). CONCLUSION: Antibiotic sensitivity on MRSA can be partially restored by exogenously delivered DrzB targeted to mRNA of blaR1 in blocking drug-resistant genes expression.DNAzyme DrzB is proved a specific and effective gene therapeutic means.
    Determination of trans-resveratrol in rat plasma after oral administration of Polygonum cuspidatum extract at a single dose by RP-HPLC
    WANG Dong-Geng, LIU Wen-Ying
    2004, 9(6):  646-649. 
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    AIM: To develop a method for the determination of trans-resveratrol in rat plasma. METHODS: Plasma samples were performed on a reversed-phase column by gradient elution after liquid-liquid extraction. RESULTS: Good linearity (r=0.9998) was obtained in the range of 0.0035-1.400 mg·L-1 for trans-resveratrol, and the limit of quantitation (LOQ) was 0.035 mg·L-1.The average recovery was 103.0 %and the RSD of intra-day and inter-day was less than 10 %.This method was applied to the determination of resveratrol in rat plasma and the pharmacokinetical parameters were calculated as follows:t1 2=11.5 min, tmax=10.0 min, and Cmax=1.93 mg·L-1. CONCLUSION: A reliable RPHPLC method for resveratol determination is developed, and appropriate for the determination of resveratrol in rat plasma.
    Effects of puerarin on AD animal model in mice induced by β-amyloid peptide
    YANG Dong-Xu, TANG Yu, HU Xiao-Min, LIU Jin-Xue, CHEN Yi, JIN You-Yu
    2004, 9(6):  650-652. 
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    AIM: To observe the effects of puerarin on leaning and memorizing in mice induced by β-amyloid peptide. METHODS: β-amyloid peptide (25-35, 3 μl, 1.0mmol·L-1) icv to mice was used as an AD animal model.Learning and memorizing ability inmice were inspected through Morris water maze test.In the meantime, the content of SOD and MDA in the mice of cerebral tissue and blood were also inspected. RESULTS: Puerarin 25 and 50mg·kg-1 improved learning andmemorizing ability in model mice (P <0.05 or P <0.01). And puerarin increased the content of SOD and reduce the content of MDA in cerebral tissue and blood of model mice. CONCLUSION: Puerarin can resist nerve poison of β-amyloid peptide, and the mechanism may be relevant to purge brain free radicals and to increase the activities of antioxidase.
    Clinical study on efficiency and reliability of the shukemian capsule in treatment of patients with asomnia (liver-spirit blocked)
    GAO Rui, ZHENG Qing-Shan1, HUANG Ji-Han1, LI Tao, SUN Rui-Ruan1
    2004, 9(6):  653-657. 
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    AIM: To evaluate the efficiency and safety of the shukemian capsule (SC) in treatment of patients with asomnia (liver-spirit blocked). METHODS: The double-dummy and randomized controlled method was adapted to assess 440 patients (liver-spirit blocked) who were divided into the treatment group (n=330, treated with SC 4 capsules, twice a day after supper and before sleeping) and the control group (n=110, treated with shumian capsule 3 capsules, twice a day after supper and before sleeping).The duration of treatment for both groups was 2 weeks. RESULTS: After 2 weeks, the rate of recover and effectiveness in control group was 40.0 % (n=110), and that in treatment group was 58.0 %(n=329) which was higher than that in treatment group (P < 0.01).No side effect was found in this clinical study. CONCLUSION: Shukemian capsule is a safe and effective agent in treating asomnia (liver-spirit blocked).
    Effects of pioglitazone on expression of myocardial proinflammatory cytokine in left ventricular hypertrophic rats
    ZHANG Cheng, YE Ping, ZHANG Jie
    2004, 9(6):  658-661. 
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    AIM: To examine the effects of pioglitazone, an agonist of peroxisome proliferator-activated receptor γon the expression of proinflammatory cytokine in cardiac hypertrophic rats, and to examine the anti-inflammatory activities of this drug. METHODS: Hypertrophic cells were produced by abdominal aortic banding.Pioglitazone(20 mg·kg-1·d-1) was given orally 1 week before operation and continued till 4 weeks after operation, then the rats were killed, the heart was excised and weighed, and the mRNA expression of interleukin-1β and cardiotropin-1 were examined by RT-PCR.The protein of the two cytokines was examined by immunohistochemical analysis. RESULTS: Pioglitazone reduced the mRNA and protein expression of the two proinflammatory cytokines and inhibited the pressure overload-induced increase in the heart weight-to-body weight ratio. CONCLUSION: Pioglitazone may regulate cardiac hypertrophy through inhibiting the expression of proinflammatory cytokines.
    Apoptosis induced by thermochemotherapy of adriamycin (ADM) and the change of mitochondial transmembrance potential in A549 cells
    ZHANG Ji-Xian, ZHANG Qi-Kun, WAN Yi-Xin
    2004, 9(6):  662-665. 
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    AIM: To investigate the effect of apoptosis and the change of mitochondial tansmembrane potential in A549 cells induced by thermochemotherapy of ADM. METHODS: ADM of different concentrations was directly applied to A549 cells cultivated in vitro.Cells maintained at 42.5 ℃for 30min. RESULTS: The inhibition of A549 cells was increased by thermochemotherapy of ADM significantly, and the cytoplasmic concentration of thermochemotherapy of ADM was significantly higher than that of chemotherapy (P <0.01).When it was 1.0 and 2.0 mg·L-1, apoptosis rate was increased and mitochondrial transmembrane potential was decreased by thermochemotherapy of ADM (P <0.01). CONCLUSION: The change of motochondial transmembrane potential was the key of apoptosis induced by thermochemotherapy of ADM in A549 cells.
    Determination of cilostazol in human plasma and its pharmacokinetics by HPLC
    HU Yu-Rong, ZHAO Yong-Xing, A You-Mei, JIA Xin, YIN Zhi-Feng, LIU Shi-Long, QIAO Hai-Ling
    2004, 9(6):  666-668. 
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    AIM: To establish a reversed phase highperformance liquid chromatographic method to determine cilostazol in human plasma and to study the pharmacokinetics of cilostazol in 10 healthy volunteers. METHODS: Using diazepam as the internal standard, cilostazol was extracted from human plasma with a mixture of 2mol ·L-1 NaOH-diethyl ether anhydrous (1:4).The mobile phase was acetonitrile-water (45:55), flow rate 1 ml· min-1, and the UV absorbance wavelength 254 nm.The pharmacokinetic analysis of cilostazol in 10 healthy volunteers after oral administration of 100mg was studied. RESULTS: Linear range of the standard curve was from 20 to 2 000 μg·L-1 (r=0.9999).The quantitative limit for cilostazol was 10 μg·L-1.The mean extraction recovery was 80.2 %±3.6 %.The mean analytical recovery was 97.0 % ±3.8 %.The relative standard deviation of intra-day and inter-day did not exceed 5.8 % and 10.1 %, respectively.It was found to be fitted to a twocompartment open model and its pharmacokinetic parameters were as follow:tmax 3.58 ±1.08 h, Cmax 920 ±230 μg ·L-1 AUC0-48 11.0 ±3.3 mg·h-1 ·L-1, respectively. CONCLUSION: The method is suitable for drug monitoring of cilostazol and the pharmacokinetics of cilostazol in human provides a useful index for clinical trial.
    Determination of levofloxacin in dog plasma using RP-HPLC and its pharmacokinetics
    JIANG Xi-Ling, SUN Jian-Guo, WANG Guang-Ji, LI Hao, LI Peng, HE Hui
    2004, 9(6):  669-672. 
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    AIM: To establish a HPLC method for the determination of levofloxacin in dog plasma and its pharmacokinetics in dogs. METHODS: The plasma protein was precipitated by the addition of 10 % perchloric acid.The resulting supernatant liquid was directly injected after centrifuge and dilution.The chromatography conditions were:DIKMA column (DiamonsilTM C18 5 μm, 150 mm ×4.6 mm), methanol-PBS-triethylamine-isopropanol (33 ∶67 ∶0, 14 ∶0.4, adjusted pH to 3.0 with H3PO4) as mobile phase with a flow rate of 1.2 ml·min-1.It was detected by fluorescence detector, and the detection wavelength was λex=295 nm and λem=440 nm.Ciprofloxacin was the internal standard. RESULTS: The linear range of calibration curve was within drug plasma concentrations of 0.25-50 mg·L-1 (r=0.9998), the detection limit was 0.02 mg·L-1 (S N > 3), the extraction recovery was 83.0 %-85.6 % (n=5), the method recovery was 92.10 %-106.77 %(n=5), the within-day RSD and between-day RSD were 1.3 %-4.0 % and 1.8 %-8.2 % (n=5), respectively. CONCLUSION: The method possesses merits of simplicity, sensitivity, good accuracy, high precision, and fine reproducibility, which is suitable for pharmacokinetic and bioavailability studies of levofloxacin in dogs.
    Pharmacokinetic study of the nano red elemental selenium in Beagle dogs
    WANG Xue-Wen, ZHENG Qing-Shan, ZHANG Jin-Song, GUI Chang-Qing, HUO Jian-Bei, SUN Rui-Yuan
    2004, 9(6):  673-675. 
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    AIM: To study the pharmacokinetics of the nano red elemental selenium (Nse) in Beagle dogs. METHODS: Blood levels of selenium were determined before and different times after administration.The observed values and increased values (observed value plus baseline) of blood levels of selenium were used to calculate pharmacokinetic parameters. RESULTS: Nse conformed to one-compartment model with fast absorption and slow elimination.T1 2 was 34.2 h by observed values in calculation and 20 h by increased values. CONCLUSION: Nse leads to toxicity easily in the administration with long term and large dose.For the material with baseline in body, the pharmacokinetic analysis should use the increased values to calculate parameters.
    Effects of Capsule Yi-Zhi on delayed neuronal death in hippocampal CA1 region and memory function after global cerebral ischemia in rats
    SUN Li-Sha, OU Yang-Shi, LI Lin, XU Jiang-Ping
    2004, 9(6):  676-679. 
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    AIM: To observe the effects of Capsule Yi-Zhi on the delayed neuronal death in hippocampal CA1 region and memory function after global cerebral ischemia. METHODS: The model of acute reperfusion injury after cerebral ischemia in rats was made by vertebral and carotid arteries occlusion;after the models were made 1, 2, 4, 8 and 40 d, the neurons in hippocampal CA1 region were immunohistochemically stained and calculated.The Morris water maze test was carried out to observe the learning and memory capacities in the 40th day. RESULTS: The number of normal neurons was significantly higher in the Capsule Yi-Zhi (100 mg·kg-1) group than that of the control group.Compared with the control group, the rats in the Capsule Yi-Zhi (100 mg·kg-1) group decreased time in finding the platform under the water surface in Morris water maze test. CONCLUSION: CYZ has protective effects on neurons in hippocampal CA1 region, and shows promising effects on learning and memory dysfunction after global ischemia / reperfusion injury.
    Study on learning and memorising of Yizhifang in ovariectomized mice by uniform design of experiments with mixtures
    YU Ri-Yue, YU Zhou, HU Jun, CHEN Qi
    2004, 9(6):  680-682. 
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    AIM: To observe the effect of the Yizhifang and its analytic prescription on learning and memory in the ovariectomized mice. METHODS: Five pieces of different analytic prescriptions were composed of three groups of herbal medicines, applying the uniform design of experiments with mixtures (UDM).The mice were fed with these prescriptions and then the ability of learning and memory of these mice were measured in the test of special searching and location. RESULTS: One optimal prescription, mainly consisted of the medicine tonifying the kidney, can improve the ability of special learning and memory in ovariectomized mice. CONCLUSION: It is feasible and convenient to analyze the prescription of a larger formula with UDM.
    Effect of fraction F of Naja naja atra venom on proliferation of vascular smooth muscle cells
    YU Qing-sheng, ZHANG Mei, QIU Yuan, HANG Shao
    2004, 9(6):  683-686. 
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    AIM: To study the effect of fraction F of Naja naja atra venom on proliferation of vascular smooth muscle cells (VSMC). METHODS: The rate of incorporation of [ 3H] thymidine (3H-TdR) into VSMC was observed by cultured VSMC in vitro, and expression of oncogene C-myc and proliferation cell nuclear antigen (PCNA) in VSMC stimulated by 20 % serum was assayed by protein immunoblotting (western blotting). RESULTS: Fration F significantly inhibited the incorporation of3HTdR into VSMCs and the expression of oncogene C-myc and PCNA in VSMC which was stimulated by 20 %serum in a dose-dependent manner.Groups of 30 and 100 mg·L-1 had obvious difference (P <0.05) when compared with control group. CONCLUSION: Fraction F of Naja naja atra venom inhibits the proliferation of VSMC by affecting expression of oncogene C-myc and PCNA.
    Experimental evaluation of the antihistamine effect of domestic azelastine hydrochloride
    ZHANG Xiao-Hong, WU Jin-Xiang, HU Chang-Ping
    2004, 9(6):  687-690. 
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    AIM: To evaluate the antihistamine effects of domestic azelastine hydrochloride. METHODS: Histamine increased skin vascular permeability and induced shock model in guinea pigs.In isolated guinea pig ileal rings, the contraction of smooth muscle induced by histamine was determined. RESULTS: Pretreament with azelastine hydrochloride(0.05, 0.15, and 0.45 mg·kg-1,ig) significantly inhibited the increase in skin vascular permeability induced by histamine in a dose-dependent manner in guinea pigs.Pretreament with azelastine hydrochloride(0.05, 0.1, and 0.2 mg·kg-1, ig) produced a significant improvement of shock, as shown by a decrease in reactivity degree, mortality and a prolongation of latency.In isolated guinea pig ileal rings, azelastine hydrochloride (10-8, 3 ×10-8, 10-7, 3 ×10-7mol·L-1) significantly inhibited contraction of smooth muscle induced by histamine in a concentration-dependent manner and caused a parallel right shift of the dose-effect curve of histamine (pA2=8.55). CONCLUSION: Domestic azelastine hydrochloride shows significant the antihistamine effects.
    Study on the model of diaphragmatic fatigue in vitro induced by hypoxic, hypercapnic acidosis and effects of salmeterol and caffeine
    XU Xuan-Li, YANG Qiu-Huo, FAN Li-Ben, XIE Qiang-Min, Qiang-Min, SHEN Yue-Liang
    2004, 9(6):  691-694. 
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    AIM: To set up a fatigued diaphragm model in vitro duo to hypoxic, hypercapnic acidosis, and to observe the effects of salmeterol and caffeine on this model. METHODS: The fatigued diaphragm model was set up with mixed gas including 21 %O2, 12 %CO2 and 67 % N2, and the effects of salmeterol (10-9-10-6mol·L-1) and caffeine (10-5-10-3 mol·L-1) on fatigued diaphragmatic contractility were surveyed. RESULTS: The value of force decreased by gas mixture at each frequency (5-120Hz).PTT, maintaining tension, and tension by muscle-stimulation decreased significantly; diaphragmatic contractile force of diaphargma increased by salmeterol with the concentration of 10-9-10-6mol·L-1at the frquencies 40-120 Hz(P <0.05);contractile force of diaphragma and PTT, maintaining tension and tension by muscle-stimulation significantly increased by caffeine with the concentration of 10-4 or 10-3mol·L-1 atall stimulus frequencies (5-120 Hz) (P <0.01). CONCLUSION: The model of rat diaphragmatic fatigue in vitro induced by hypoxic and hypercapnic acidosis can be set up by aerating with 3 kind of gas mixed with 21 % O2, 12 %CO2 and 67 %N2, and contractility of fatigued diaphragm of rat enhanced by salmeterol and caffeine to some extent.
    Relation between recombinant human leukemia inhibitory factor(rh-LIF) induced apoptosis of HL-60 cells in vitro and expression of bcl-2 and p53
    DU Bing, ZHU Dao-Yin, TANG En-Jie
    2004, 9(6):  695-697. 
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    AIM: To investigate the effect of recombinant human leukemia inhibitory factor (rh-LIF) on human myeloid leukemia cell line HL-60. METHODS: HL-60 cells were treated with various concentrations of rh-LIF (10-4 000 U·ml-1) for a few days, cell cycle and cell apoptosis rate were analysed by flow cytometry.Cell apoptosis was also observed under microscope with TUNEL.Expression of P53 protein after addition of rh-LIF (800 U ·ml-1) was observed by immunohistochemistry, and p53 mRNA and bcl-2 mRNA were assayed by in situ hybridization. RESULTS: Cell apoptosis rates (CAR) in rh-LIF groups by flow cytometry were higher than those in control group, and 1 000 U·ml-1 rh-LIF had the most potent effect on induction of apoptosis. There was also a marked increase of positive-cells by TUNEL method in a concentration-dependent pattern on the 3rd day after addition of rh-LIF (10-1 000 U · ml-1).Following addition of rh-LIF (800 U·ml-1) and incubation for 2 to 6 days, the expression of P53 protein and p53 mRNA of HL-60 cells increased obviously, and bcl-2mRNA expression decreased in a time-dependent pattern(vs control, P <0.01). CONCLUSION: rh-LIF can induce apoptosis, and the effects may be related to the increase of P53 protein and decrease of bcl-2 mRNA expression.
    Plaque morphological characteristics of acute myocardial infarction observed by intravascular ultrasound
    ZHANG Hang, CHEN Shao-Liang, SHAN Shou-Jie, YE Fei, DUAN Bao-Xiang, ZHANG Jun-Jie
    2004, 9(6):  698-700. 
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    AIM: To study the plaque morphological characteristics of acute myocardial infarction by intravascular ultrasound(IVUS), comparing plaque morphology in acute myocardial infarction and stable angina pectoris. METHODS: 59 patients with acute myocardial infarction (male 43, mean age 60 ±9 years) and 50 patients with stable angina pectoris (male 38, mean age 62 ±10 years) underwent coronary artery angiography (CAG) and IVUS examinations.The plaque morphology, including incidence of eccentric plaque, subtle dissections, low echoic thrombus, calcification, echolucent areas, and bright speckled echo material, were assessed by IVUS. RESULTS: There were no significant differences in plaque eccentricity or plaque calcification between the two groups, except low echoic thrombus(acute myocardial infarction 15 % vs stable angina pectoris 0 %), subtle dissection (37 % vs 4 %), echolucent areas (31 % vs 0 %), and bright speckled echo material (90 % vs 0 %) (P < 0.001 for all). CONCLUSION: Low echoic thrombus, subtle dissection, echolucent areas, and bright speckled echo material are morphological characteristics associated with plaque at the time of acute myocardial infarction.It is confirmed that the rupture of plaque is related to the occurrence of acute myocardial infarction.
    Culture and drug susceptibility of mycoplasma in patients with nongonococcal urogenital infection
    JI Bi-Hua, SONG Jun, LIU Wen-Bei, WANG Jun, WANG Wei-Liang
    2004, 9(6):  701-704. 
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    AIM: To determine the mycoplasma infection and the drug resistance in outpatients with NGU. METHODS: Mycoplasma culture, identification and drug sensitivity assay were carried out with samples of 472 NGU patients by using one complex mycoplasma kit. RESULTS: 153 in 472 cases showed mycoplasma positive. The total positive rate was 32.4 %.The positive cases of Uu, Mh andmixed both infection were 112(23.7 %), 11 (2.3 %), and 30 (6.4 %), respectively.The female positive rate was found significantly higher than that of male (χ2=4.157, P <0.05).The highest susceptibility rare of mycoplasma to 12 kinds of antimicrobial agents were doxycycline (96.1 %) and mynocyclin (94.8 %). The highest resistant rate of mycoplasma were acetylspiramycin (69.3 %) and erythromycin (60.1 %). CONCLUSION: Mycoplasma shows prevalent drug-resistant to many antimicrobials in virvo.Doxycycline, mynocyclin or josamycin may be selected as the first drugs to treat mycoplasma infection.
    Study on safety and efficiency of oral anticoagulation in patients with transient ischemic attack
    LUO Wei-Liang, XU Jian-Bin, HUANG Lin-Hui, XU Nan-Yan, QU Jing-Hua, LIU Wu
    2004, 9(6):  705-708. 
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    AIM: To evaluate the safety and efficiency of oral anticoagulation in patients with transient ischemic attack (TIA). METHODS: The hospitalized patients with TIA were treated by oral anticoagulation according to Roberts'age adjustedWarfarin loading protocol from February of 2003 for 12 months.The cases in control group were those with TIA except those having been used heparin from February of 2002 till January of 2003. RESULTS: Compare the two groups with average age, rate of gender, rate of cases complicated cardiac disease, hypertension and diabetes, blood pressure, cholestein, and triglyceride.There was no significant difference in all general conditions between two groups (P >0.05).However, there was no patient with the anticoagulation to develop stroke and hemorrhage in following days, but there were 6 cases had acute ischemic stroke in control group after that (P <0.05). CONCLUSION: Oral anticoagulation by using Roberts'Warfarin dosing guidelines is safe and more effective in patients with TIA.
    Expression of vascular endothelial growth factor in chronic hypoxia and hypercapnia rats and effects of SHENYI Capsule
    CHEN Yan-fan, CHEN Shao-Xian, FAN Xiao-Fang, WANG Liang-Xing
    2004, 9(6):  709-712. 
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    AIM: To explore the roles of vascular endothelial growth factor (VEGF) in hypoxia pulmonary hypertension and effects of SHENYI Capsule. METHODS: Thirty SD rats were randomly divided into normal control group (N), hypoxia hypercapnia group (F), and hypoxia hypercapnia +SHENYI Capsule group (S).The levels of VEGF in serum and lung tissue are measured by ELISA, the ultrastructure of pulmonary arterioles was observed by electron microscopy, and the expression of VEGFmRNA was observed by in situ hybirdization. RESULTS: Mean pulmonary arterial pressure (mPAP), weight ratio of RV to LV +S, the levels of VEGF in serum, and lung tissue of group F were significantly higher than those of group N and group S (P <0.01 or <0.05).Electron microscopy showed proliferation of smooth muscle cells and collagenous fibers of pulmonary arterioles in rats of group F, and SHENYI Capsule could reverse the changes mentioned above.VEGF mRNA in pulmonary arterioles was significantly higher in rats of group F than that of group N(P < 0.01), and it was significantly decreased in rats of group S than that of group F. CONCLUSION: VEGF plays an important role in the process of hypoxia pulmonary hypertension, and SHENYI Capsule can prevent hypoxia pulmonary hypertension by inhibiting the role of VEGF.
    Protective effect of Acanthopanecis senticosus injection in rats with acute myocardial hypoxia
    XU Shan-Chu, TAO Ming-Fei
    2004, 9(6):  713-716. 
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    AIM: To observe the protective effect of Acanthopanecis senticosus injection in rats with acute myocardial hypoxia. METHODS: The mean survival time and capacity for myocardial oxygen consumption were detected in rats with acute hypoxia under ordinary or low pressure. RESULTS: Various dosages of Acanthopanecis senticosus injection could prolong the mean survival time and reduce capacity for myocardial oxygen consumption in rats with acute hypoxia under ordinary or low pressure. CONCLUSION: The Acanthopanecis senticosus injection can evidently reduce capacity for myocardial oxygen consumption and increase ability to anti-stress and plays a protective role in rats with hypoxic myocardium.
    Measuring data quality of clinical trials
    WANG Yi-Bing, XIONG Ning-Ning, BO Qing-Yan, ZOU Jian-Dong, JIANG Meng, LIU Fang, FU Wei-Min
    2004, 9(6):  717-720. 
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    Each step about data which are collected, reported and manipulated has an error rate associated with it.Therefore, measuring data quality is a key element of quality control for clinical trial data.The techniques of measuring data quality includes:evaluating data precision, establishing inter-rater reliability, aggregating statistics and statistical process control charts, cross checking between referential data, checking the format of lab reports, checking among relevant documents and data, comparing between source data and CRF, and between CRF and database, data validating, calculating error rate in the processes of data processing, laboratory normalizing and data cleaning.