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

Table of Content

    Volume 10 Issue 5
    26 May 2005
    Progress of local anesthetics in cardiac toxicity
    DONG Xi-chen, HUANG Yu-guang
    2005, 10(5):  481-484. 
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    After first report of local anesthetics on cardiac toxicity was published in 1979, A lot of research-es of local anesthetics on the mechanism of cardiac toxici-ty and its treatments were reported, and some advances were reviewed in this article during recent years.
    Oxidative stress and Alzheimer's disease
    HUANG Yan, DONG Zhi
    2005, 10(5):  485-488. 
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    Alzheimer's disease (AD)is a kind of neuro-degenerative disease mainly affecting both cognition and behavior, and pathologically characterized by deposi-tion of amyloid-beta peptides as senile plaques and by the occurrence of neurofibrillary tangles (NFT).AD is corre-lated with many factors, there are several hypotheses about AD, and one of them is oxidative stress and some anti-oxidative drugs demonstrated effective. This paper reviewed the relation between oxidative stress and AD, and the recent study on anti-oxidative drugs for AD.
    Effects of iptakalim hydrohloride on KATP genes expression in renal tissues of spontaneously hypertensive rats
    XUE Hao, GAO Min, LIU Guo-shu, WANG Hai
    2005, 10(5):  489-493. 
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    AIM: To investigate the effects of iptakalim hydrohloride on KATP mRNA expression in renal tissues of spontaneously hypertensive rats. METHODS: SHRs at the age of 12-week-old were treated with Ipt 1, 3, and 9 mg°kg-1°d-1, benazepril 3 mg°kg-1°d-1 once a day for 12 weeks, respectively. The same aged WKY ratswere used as normal control. The effects of Ipt on BP and renal K ATP mRNA expression were detected by RT-PCR.RESULTS: mRNA expression level of SUR2、 Kir6.1 and Kir1.1 increased in SHR.After administra-tion of 1, 3, and 9 mg°kg-1°d-1 Ipt, the levels of BP were decreased, and the mRNA expression of Kir6.1 and Kir1.1were decreased. But there was no change in mR-NA expression of SUR2.In addition, there was no signif-icantly difference of mRNA expression of Kir6.2 among the SHR groups and the WKY group. CONCLUSION: The renal protective effects of Ipt may be related to regu-lation of genes expression of Kir6.1 and Kir1.1.
    Effects of huperzine A on theta-rhythm and long-term potentiation in CA1 pyramidal neurons in adult rat hippocampal slices
    WU Xiao-wei, WANG Meng-ya
    2005, 10(5):  494-498. 
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    AIM: To study the effects of huperzine A on the theta-rhythm and long-term potentiation in CA1 py-ramidal neurons in adult rat hippocampal slices and to get insight into the cell electrophysiological mechanisms un-derlying the potentiation of learning and memory by Hu-perzine A.METHODS: The intracellular recordings from CA1 pyramidal neurons in hippocampal slices related to learning and memory were made to analyze the mecha-nisms of Hup-A action.RESULTS: Power of frequencies ranged from 4 to 10Hz wasnot significantly difference be-tween pre-membrane potential oscillations (MPOs) and post-MPOs in control group, but it was significantly (P<0.005, n =3) changed between pre-MPOs before ad-dition of Hup-A and post-MPOs after addition of Hup-A. During long-term potentiation (LTP), the increase of am-plitudes of EPSPs was observed at post-tetanus 30 min in control group and 15 min in Hup-A group.CONCLUSION: Hup-A can increase the power of 4 to 10 Hz MPOs and facilitate induction of LTP in CA1 pyramidal neurons of rat hippocampal slices, which may contribute to the potentiation of learning and memory by Huperzine A.
    Changes of three COX isoforms expression after formalin induced inflammatory pain in brain and analgesic effects of different COX inhibitors
    LU Zhi-hong, XIONG Xiao-yun, MENG Jing-ru, LIU Zhen-guo, WANG Zhi-peng, MEI Qi-bing
    2005, 10(5):  499-504. 
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    AIM: To compare the expression of three cyclooxygenase (COX) isoforms in the process of inflam-matory pain and evaluate the analgesic effects of different protocols about usage of COX inhibitors on inflammatory pain. METHODS: Formalinwas injected subplantarly to mice to induce inflammatory pain.The expression of COX-1, COX-2 and COX-3was evaluated by radioimmu-noassay and RT-PCR, respectively. For the analgesic ef-fect assay, animals were divided into 5 groups including control, SC, NS, IN and NS +SC group.The former 4 groups received saline, SC-560 (300μg°kg-1), NS-398 (150 μg°kg-1), and indomethacin (300μg°kg-1), re-spectively. In the NS +SC group, animals received NS-398 during the first 1 month and SC-560 during the sec-ond month in the NS +SC group.RESULTS: The ex-pression of COX-1was higher at the late phase while that of COX-2 was higher at the early phase of inflammatory pain.The expression of COX-3 did not significantly change in the process of inflammatory pain.Additionally, behavioral assessment showed that using COX-2 inhibitors at the early phase followed by COX-1inhibitors at the late phase could get better analgesic effect on inflammatory pain compared with single using COX-1 selective or COX-2 selective inhibitors. CONCLUSION: In brain, the ex-pression of COX-2 increases rapidly in the inflammatory pain processwhile COX-1 expression does not increase till the late phase. Brain COX-3 is poorly involved in the in-flammatory process.Combined use of COX-1 and COX-2 selective inhibitors may be a better protocol in inflamma-tory pain treatment.
    Kappa-selenocarrageenan-induced apoptosis of multidrug-resistant human leukemia cell and its mechanism
    ZHANG Zhe-wen, WEI Hu-lai, SU Hai-xiang, LIU Jian-min, HAO Chun-yan
    2005, 10(5):  505-508. 
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    AIM: To observe the apoptosis of K562 ADM cells induced by kappa-selenocarrageenan(KCS) and to explore its possible molecular mechanism. METHODS: MTT assay, Wright-Giemsa staining, DNA agarose gel electrophoresis and cell-cycle analysis were used for examining apoptosis in K562/ADM cells.Ex-pression of Fas, Bcl-2 and P53 proteins was measured with Flow cytometr(FCM). RP-PCR assay was employed to detect the expression of caspase-3 mRNA. RESULTS: KCS inhibited proliferation of K562/ADM cells.Morpho-logical typical changes of apoptosis were observed through light microscopy. DNA electrophoresis showed evident DNA fragmentation. Cell-cycle analysis indicated in-creased apoptotic cell population (Sub-G1 proportion) as well as apparent S phase arrest. The expression of Fas an-tigens and caspase-3 mRNA significantly increased, and that of Bcl-2 antigens decreased sharply after application of KSC.There was no distinct change of the expression of P53 protein inK562/ADM cells treatedwith KSC.CONCLUSION: KSC induces apoptosis of K562/ADM cells via Fas-caspase-3 pathway.
    Research of metabolism of antidepressant mirtazapine on mice liver micro-some in vitro
    CHEN Lei, XIAO Hong, LIU Wen-ying
    2005, 10(5):  509-513. 
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    AIM: To identify the isoforms of cyto-chrome P450 (CYP) involved in the metabolism of mir-tazapine and the influence of mirtazapine on the me-tabolism of mirtazapine. METHODS: Mirtazapine was incubated with rats liver microsomes induced by different inducers, and the reaction was terminated by acetonitrile. The sample was added 25%ammonia water and extracted with cyclohexane, and the determination was performed by RP-HPLC with the mobile phase of methanol-water (including 10 mmol°L-1 NH 4 AC, 5 mmol°L-1 SDS, pH 3.5) 62 :38(V/V). RESULTS: The assay was linear from 75.3 to 565 μmol°L-1 for mirtazapine in rat hepatic microsomal incubates.The livers induced by phenobarbi-tal were catalyzed and livers induced by rifampicin also showed more active performance, while the livers induced by rats had no significant difference between two groups. CONCLUSION: P450 3A4 induced by phenobarbital as well as rifampicin is crucial in the metabolism of mirtaza-pine. And P450 2C9/2C19 induced by rifampicin may al-so interfere the metabolism of mirtazapine. Mirtazapine has no obvious effect on the isoforms responsible for its metabolism of mirtazapine.
    Study of Salvia miltiorrhiza on bleomycin-induced pulmonary fibrosis in mice
    LU Si-jing, LIU You-ning, WANG Hua-zhou
    2005, 10(5):  514-517. 
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    AIM: To study protective effects of Salvia miltiorrhiza on bleomycin (BLM)-induced pulmo-nary fibrosis in mice. METHODS: Animal model with pulmonary fibrosis in SD mice was replicated by intratra-cheal injections of bleomycin and Salvia miltiorrhiza in-jection were given after replicated 7th day. Ratswere exe-cuted in 7th and 28th day, MDA, GSH andHYP in lung tissue bomogenate and the lung histopathological change were detected to investigate the effects of Salvia miltior-rhiza injection on lung fibrisis form in different stages. RESULTS: Salviae miltiorrhizae injection given after replicated first day restrained the increase of MDA and HYP, and decreased the GSH of lung tissue bomogenate, and lighten pathological lesion.Salvia miltiorrhiza injec-tion given after replicated the 7th day had no statistical difference between Salvia miltiorrhiza therapy groups and model group.CONCLUSION: Salvia miltiorrhiza injec-tion can prevent mice pulmonary fibrosis from and has no side effects on formative rat pulmonary fibrosis.
    Effects of seal oil on liver lipid metabolism and thromboxane A 2 and MDA of experimental fatty liver in rats
    LI Zhan-jun, LIU Jian-wen, XU Kang-sen
    2005, 10(5):  518-521. 
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    AIM: To study the inhibition effects of seal oil on fatty liver in rats.METHODS: A low dose of carbon tetrachloride and high fat diet chronically feed was given to five groups (n =10 in each) of male Wistar rats for 7 weeks to induce the model of fatty liver. Then the five groupswere orally administered olive oil, simvastatin 4 mg°kg-1°d-1, seal oil 0.5, 1.6 or 4.8 g°kg-1°d-1 for other 8 weeks, respectively. The untreated control group received only normal feed.The liver lipid, produc-tion of prostacyclin and thromboxane A2, lipid superoxi-dation parameters were measured to compare with the changes.The pathology was evaluated. RESULTS: The ratio of 6-keto-PGF/TXB2 were significantly increased in seal oil group due to decrease TXB2 and increase 6-keto-PGF in liverwhen compared with those in olive oil group (model group) (P<0.01). Liver TC, TG, FFA and MDA concentrations were significantly decreased in the seal oil groupswhen compared with those in model group (P<0.01), but SOD concentration increased (P< 0.01). Pathology showed that seal oil markedly improved fatty liver and the reduction of index analyzed from CYP2E1 express (P<0.01). CONCLUSION: Seal oil inhibits fatty changes of the liver by both direct effects of inhibition the synthesis of liver lipid and modulating lipid metabolism and indirect effects of increase the hepatic blood flow due to decrease the TXA2 concentration and blood viscosity. In addition, seal oil shows anti-lipid su-peroxidation by decreasing MDA concentration.
    Neuroprotective effects and mechanisms of propofol on neuronal damage induced by ketamine in rat posterior cingulate cortex
    GUO Jian-rong, DU Jin-man, XIE Dao-fen, REN Li-yuan, YU Lei-ting, LI Song
    2005, 10(5):  522-526. 
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    AIM: To investigate the effects of propo-fol on ketamine-induced c-fos mRNA and protein expres-sion in the rat posterior cingulate cortex, and to explore the possible mechanisms of using propofol to prevent or treat ketamine-induced psychotomimetic effects and neuro-nal damage.METHODS: Thirty male Wistar rats weigh-ing 250 -300 g were randomly divided into five groups with six animals in each :saline group which received nor-mal saline 5 ml intraperitoneally ip (NS), ketamine 100 group which received ketamine 100 mg°kg-1 ip (K); propofol 100 group which received propofol 100 mg°kg-1 ip (P);propofol 50 +ketmaine 100 group which received propofol 50 mg°kg-1 +ketmaine 100 mg°kg-1 ip (P 1 K) and propofol 100 +Ketamine 100 group which received propofol 100 mg°kg-1+Ketamine 100 mg°kg-1 ip (P 2 K). In group P 1 K and P 2 K, the interval between propofol and ketamine administration was 15 min.Two hours later, the animals were decapitated and brain was removed.c-fos mRNA expression in the posterion cingu-late cortex was detected by semi-quantitative RT-PCR technique, c-fos protein expression in posterior cingulated cortex was determined by immuno-histochemical method. RESULTS: The levels of c-fos mRNA and c-fos protein expression were significantly different among 5 groups. Ketamine induced marked c-fos mRNA and c-fos protein expression in the posterior cingulate cortex.Propofol did not induce c-fos gene expression in this brain region. Propofol significantly inhibited ketamine-induced c-fos mRNA and c-fos protein expression in the posterior cingu-lated cortex in a dose-dependent manner.CONCLUSION: Propofol pretreatment can significantly inhibit ket-amine-induced c-fos mRNA and protein expression in the posterior cingulate cortex. It may be one of mechanisms of inhibition of ketamine-induced psychotomimetic effect and neuronal damage by propofol.
    Study on proportion of pinellisa decoction for purging stomach-fire, gin-ger rind and licorice root with BP artificial neural network
    SONG Xiao-li, NIU Xin, SI Yin-chu
    2005, 10(5):  527-531. 
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    AIM: To observe the difference in the application of proportion of pinellisa decoction for purging stomach-fire, ginger rind and licorice root with different BP (back propagation, BP) method of artificial neural network.METHODS: The influence of gastric mucuqas content in normal rats was measured, and the groups of different flavor of a drug and dosage were divided accord-ing to homogeneous design.This research was pro-grammed with MATLAB6.5, conformed the experimental data with BP artificial neural network, and the research compared the different structural topology of 8-3-1、8-8-1、 8-12-1, and compared the different influence with the dif-ferent BP method to network.And then, the expected mode of gastric mucus content was formed, which based on the BP neural network. RESULTS: The artificial neural network model that had 8-10-1 structural topology and improved BP method was formed, and it was a kind of good method to uniform the studied samples and to forecast the unstudied samples, Moreover, the expected effect of variable learning rate back propagationwas best. CONCLUSION: Using the studying of pinellisa decoc-tion for purging stomach-fire, ginger rind and licorice as an example, and give birth to the new model in studying proportioning of compound prescription.This model will found its position in studying proportioning of compound prescription.
    Effects of 3,4,5, 6-tetrahydroxyxanthone on myocardial ischemia-reperfu-sion injury in isolated rat hearts
    DAI Zhong, HU Chang-ping, WU Tie, DAI Bin, LIN Xi
    2005, 10(5):  532-536. 
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    AIM: To study the protective effects and mechanisms of 3, 4, 5, 6-tetrahydroxyxanthone on myocar-dial ischemia-reperfusion injury in isolated rat hearts. METHODS: Ischemia-reperfusion injury was induced by 30 min of global ischemia and 30 min of reperfusion in isolated rat hearts.Heart rate, coronary flow (CF), left ventricular pressure (LVP), and the first derivative (+ dp/dtmax) were recorded.The activity of creatine kinase in coronary effluent and tumor necrosis factor-alpha (TNF-α) content in myocardial tissues were measured. RESULTS: 3, 4, 5, 6-tetrahydroxyxanthone (30, 100 or 300 μmol°L-1) caused a significant improvement of car-diac function and a decrease in the release of creatine ki-nase in coronary effluent as well as the level of TNF-αin myocardial tissues.CONCLUSION: 3, 4, 5, 6-tetra-hydroxyxanthone possesses a protective effect onmyocardi-al ischemia-reperfusion injury, and the effects may be re-lated to inhibition of TNF-αproduction.
    Inhibition effects of U50, 488H on hypertrophic myocardial cells induced by isoproterenol
    SHAN Dan, WANG Hong-xin, SU Yu-hong, YANG Yu-hong, WANG Hao
    2005, 10(5):  537-541. 
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    AIM: To observe the inhibition effects of cross-talk between kappa opioid receptor (κ-OR)and β1 -adrenoceptor (β1 -AR)on hypertrophic myocardial cells induced by isoproterenol (ISO)in neonatal rats.METHODS: The total protein content was assayed by the meth-od of Lowry's.The cardiomyocytes' volume was mea-sured by computer photograph analysis system and the protein synthesis was assayed with [3H] leucine intake method. RESULTS: ISO enhanced the total protein con-tent, the cardiomyocytes' volume and the protein synthe-sis in myocardial cells.U50, 488H (U50)showed the function inhibited by nor-BNI on reducing the previous mentioned indices induced by ISO.U50 also attenuated the hypertrophy induced by ISO combined with ICI118, 551(β2 -AR inhibitor).CONCLUSION: κ-OR has a cross-talkwith β1 -adrenoceptor in ISO-induced myocardial hypertrophy.
    Determinants of efficacy of famciclovir in treatment of patients with herpes zoster
    HU Hai-tang, CHEN Qi-guang, CHEN Bin-wei
    2005, 10(5):  542-546. 
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    AIM: To investigate the determinants of the efficacy of famciclovir in treatment of patients with herpes zoster.METHODS: The patients were adminis-tered famciclovir 250 mg, three times a day for 7 days. Logistic regression was used for investigate the factors. RESULTS: The correlations of cure rate and effective rate with some factors were negative. Those factors in-cluded age, number of lesions (papules/vesicles), time to stop new vesicles, time to loss of acute phase pain, time to appear crusting, time to full crusting, inducer, total score before treatment. But some factors such as gender, location of lesions, ulcers, erythema, score of pain were not effect on the efficacy. CONCLUSION: Some factors such as age, number of lesions (papules vesicles), time to stop new vesicles, time to loss of acute phase pain, time to appear crusting, time to full crusting, inducer, total score before treatment show important influ-ences on the efficacy of famciclovir in treatment of patients with herpes zoster.
    Roles of adhesion molecules in adhesion of polymophonuclear leukocytes-human umbilical vein endothelial cells
    ZHANG Xue-ping, REN Yong-gong, LIU Xin-bo, SHI Bi-ming, ZHENG Bang-xiong
    2005, 10(5):  547-550. 
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    AIM: To investigate the interaction of CD11b and its ligand ICAM-1 on PMN-HUVEC adhesion and their action mechanism. METHODS: Human neu-trophils were isolated from fresh heparinized blood of healthy volunteers by dextran sedimentation followed by Ficoll-Hypaque gradient centrifugation.The polymopho-nuclear leukocytes-human umbilical vein endothelial cells (HUVECs) were isolated from human umbilical veins by 0.25%trypsin and then cultured in RPMI1640.There were five groups in this experiment for the adhesion as-say :control group, LPS treated group (PMNs and HU-VECs were stimulated with 100 μg°L-1 LPS in different time), CD11bMoAb pretreated group, ICAM-1 MoAb pretreated group, combined CD11b and ICAM-1 MoAb pretreated group.The rate of PMN-HUVEC adhesion was calculated as formula after radiolabelling PMNs with 99mTc-HM-PAO.adherence(%) =cpm lysate/cpm added ×100.RESULTS: PMN-HUVEC adhesiveness in-creased after stimulated for 15 min compared with that in the control group (37.45%±3.92% vs 11.03% ± 4.15% P<0.05), and it reached the peak after 4 hours (73.50%±6.39%). MoAb to CD11b and ICAM-1 sig-nificantly inhibited this adhesiveness (P<0.05). More-over, an additive effect was observed when two MoAbs were used together (P< 0.05). CONCLUSION: CD11b and ICAM-1 play a crucial role in the course of PMN-HUVEC adhesion, and the adhesiveness between cells is significantly attenuated after MoAb blocked the action of adhesion molecules.
    Pharmacokinetics of different felodipine sustained-release tablets in healthy volunteers
    LIANG Zhu, WANG Bao-de, YU Yan-li, XIE Ji-qing, LU Huai-ping, YUAN Cheng
    2005, 10(5):  551-554. 
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    AIM: To compare pharmacokinetics and bioavailability of different felodipine sustained-release tablets in healthy volunteers.METHODS: Drug concen-trations were determined in plasma following a single oral dose of 5 mg felodipine sustained-release tablets by high performance liquid chromatography method. Referenced with the general felodipine tablets, pharmacokinetics and bioavailability were calculated and compared. RESULTS: Good linear relationship between felodipine con-centration was obtained at ranges of 0.5 -10μg°L-1 in plasma and the peak-high.Pharmacokintic parameters were different clearly for different felodipine sustained-re-lease tablets in healthy volunteers, and bioavailability ref-erenced with the general felodipine tablets were 168%, 177%and 125%, respectively. CONCLUSION: There are difference at pharmacokintics and bioavailability among those three felodipine sustained-release tablets.
    Changes of p38 mitogen-activated protein kinase in lung tissue and effects of dexamethasone in asthmatic rats
    HUANG Cui-ping, YANG He-ping, ZHANG Zhen-xiang, XU Yong-jian
    2005, 10(5):  555-558. 
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    AIM: To identify the changes of p38 mi-togen-activated protein kinase (p38MAPK) in lung tissue of asthmatic rats and the effects of dexamethasone on it. METHODS: Ovalbumin (OVA) was injected intraper-itoneally and inhaled to produce the asthmatic model. Twenty ratswere randomly divided into three groups:con-trol group, asthma group and DEX group. The concentra-tion of IL-5 in BALF and the expression of phospho-p38 MAPK in lung tissue were measured by ELISA and West-ern blot, respectively. RESULTS: The expression of phospho-p38 MAPK was up-regulated in the lung of asth-matic rats.The injection of DEX intraperitoneally de-creased the expression of phospho-p38 MAPK and abol-ished the increases of airway resistance, the concentration of IL-5 and the number of eosinophil in BALF. His-topathologic damage of lung tissue was alleviated.There were positive correlations between the expression of phos-pho-p38 MAPK and airway resistance, the concentration of IL-5 and the number of eosinophil in BALF. CONCLUSION: p38 MAPK may play a role in pathological process of asthma. DEX can effectively treat asthma by inhibiting the expression of p38 MAPK.
    Efficacy of freeze-dried M.vaccae vaccine in treatment of patients with multi-drug resistant pulmonary tuberculosis
    DING Wei-min, YANG Jun-xing, WANG Guang-hui
    2005, 10(5):  559-561. 
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    AIM: To explore the immunotheraptical drugs for multi-drug resistant pulmonary tuberculosis (MDR-TB). METHODS: 79 patients with MDR-TB were randomly assigned to two groups.46 cases in M. vaccae group were treated with “3AkPaThLevl/15Pa-ThLevL” and M. vaccae, and 33 cases in control group were treated only with“3AkPaThLevl/15PaThLevL”. The clinical effect and T-lymphocyte subsets in patients were observed after being treated for 1, 2 and 3 months, re-spectively. RESULTS: The sputum negative rates (41.3%, 63.0%, and 80.4%) and the X-ray resolu-tion rates (30.4%, 50.0%, and 67.4%) of the M. vaccae group were superior to those (12.1%, 27.3%, and 39.4%, P<0.001) and those (6.1%, 21.2%, and 27.3%, P<0.05) of the control group after being treated for 1, 2 and 3 months.The percent of ${CD_{3}}^{+}$,${CD_{4}}^{+}$and the ratio of ${CD_{4}}^{+}$ ${CD_{8}}^{+}$ of the M. vaccae group were significantly higher than that of the control group (P<0.001), while the percent of ${CD_{8}}^{+}$ of the M. vaccae groupwas significantly lower than that of the control group (P<0.05). CONCLUSION: The M. vaccae can en-hance the cellular immune function of the patients with MDR-TB.
    Study on serum concentration and effects of sotalol in treatment of patients with arrhythmia
    ZHANG Hui-jie, PENG Xiao-lin, WANG Qian-zhou, GONG Shang-chu
    2005, 10(5):  562-566. 
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    AIM: To observe the relationship among the effects, side-effects and serum concentration of sotalol in treatment of patients with arrhythmia. METHODS: 100 cases (male 53, female 47) of out patient department (OPD) with atrial or ventricular arrhythmia were select-ed. Every different doses of sotalol (80, 160, 240 mg°d-1) were administrated two weeks in order.Samples of 3 ml peripheral venous blood were collected during the last day of the period of every different dose. The time of blood collecting was in the morning before administration and three hours after administration (i. e.peak and bot-tom serum concentration). RP-HPLC method was adopt-ed. ECG (including QT, QTc episodes and QTd) and Holter examination were performed.RESULTS: Total ef-ficiency of sotalol on arrhythmia :ventricular premature beats (VPB) was 85.7%, couple VPB and paroxysmal ventricular tachycardia was 73.3%, and atrial arrhythmia was 70%.The following resultswere still observed:bet-ter effects on the prevention to paroxysmal atrial fiberal-lation, ventricular rates being better controlled in atrial flutter and fiberallation.The average bottom value (ABV) of the effective serum concentration of the effective cases was 0.67±0. 21 mg°L-1 and the peak value was 1.33± 0.51 mg°L-1, but the ABV of the serum concentration was 0.69 ±0.22 mg°L-1 and peak value was 1.36 ± 0.53 mg°L-1 in ineffective cases.CONCLUSION: The most rational doses of sotalol ranges between 160 -240 mg°d-1 with some advantages, such as lower side ef-fects, and effective to both atrial and ventricular arrhyth-mia.
    Effects of berberine on left atria and trachea in guinea pigs
    DAI Chang-rong, LUO Lai-yuan
    2005, 10(5):  567-569. 
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    AIM: To observe the effects of berberine (Ber) on left atria and trachea in guinea pigs. METHODS: The experiment was carried out with isolated left atria and trachea in guinea pigs, and the effects and in-teractions were compared between Ber and pinacidil (Pin). RESULTS: Ber concentration-dependent in-creased the force of contractile, while Pin decreased the force. Ber leaded a parallel rightward shift in accumulated response curve of depression contraction of left atria by Car, and it hardly changed the maximum response (E max), while Pin leaded a parallel leftward shift in the same curve.In the combination of Ber and Pin, the dose-response curve hardly changed as the control one. In iso-lated guinea pig trachea, Ber caused a leftward shift in the dose-response curve of ACh, whereas Pin produced a rightward shift in the same curve without changing E max. When both Ber and Pin existed in the same container, there was no modification in the response to ACh.CONCLUSION: Ber shows the effect of blocking potassium channel.
    Clinical evaluation on marine capsules combined with the composite Salvia miltiorrhiza dropping pill in treatment of patients with cirrhosis related to chronic hepatitis B
    WANG Chang-sheng, XU Hui-yang, KUAI Hui-fen
    2005, 10(5):  570-573. 
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    AIM: To investigate the therapeutic ef-fects of the marine capsules combined with composite Salvia miltiorrhiza dropping pill in treatment with patients with hepatic fibrosis related to chronic hepatitis B. METHODS: 54 patients were enrolled and randomly di-vided into control group and treatment group.The liver function, the marker of hepatic fibrosis and hepatitis B virus were determined before and after therapy. RESULTS: The markers in this study were significantly im-proved than those before treatment and those in control group (P<0.05 or P<0.01). CONCLUSION: The marine capsules combined with composite Salvia miltior-rhiza dropping pill can effectively control the activity of liver inflammation in the patients with chronic hepatitis B and markedly heighten the effects in treatment of patients with hepatic fibrosis and inhibit the replication of HBV without severe side effect.
    Effects of aspirin-niacinamide-zinc complex (WUY) on platelet aggrega-tion and experimental thrombosis
    PU Qi-song, LEI Jun, HANG Xiang
    2005, 10(5):  574-578. 
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    AIM: To study the effects of aspirin-ni-acinamide-zinc complex (WUY) on platelet aggregation and experimental thrombosis.METHODS: With ade-nosine diphosphatethe (ADP), arachidonic acid (AA) and collagen, the effectsof aspirin-niacinamide-zinc com-plex (WUY) on platelet aggregation in vitro or in vivo were investigated by Born'smethod.The mouse mortality caused by intravenous injection of AA and experimental thrombus formation in rats were observed.Radioimmuno-assay was used for measuring thromboxane B2 (TXB2) and 6-keto-PGFin plasma of rabbits.RESULTS: In high, middle and low dose groups, drugs, in vitro, inhibited ADP-, AA-and collagen-induced platelet aggregation and the effect of WUY was stronger than that of ASP in high dose groups.In vivo, WUY showed more potent inhibito-ry effects on AA-induced aggregation in 1 h and 3 h. WUY had a powerful inhibitory effect on mouse death as a result of pulmonary thrombi induced by AA injection into the tail vein and ED50 was lower than that of ASP. In ad-dition, WUY exhibited strong inhibitory effect on throm-bus formation in rat arteri-venous shunt and significantly reduced plasma level of TXB2 while it markedly increasing 6-keto-PGFin high dose groups and ASP significantly reduced plasma level of both TXB2 and 6-keto-PGF. CONCLUSION: The effect of WUY on platelet aggrega-tion and experimental thrombosis is stronger than that of ASP and can increase plasma level of 6-keto-PGF.
    Experimental study of protective effects of compound oral liquid xinkang on myocardium
    WU Hong-ling, FU Ying-jun, WANG Fang, PANG Hong, SU Zhuo-wa, HE Ming
    2005, 10(5):  579-585. 
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    AIM: To explore the protective effects of compound oral liquid xinkang on the acute myocardial in-jury. METHODS: The rats were divided into four groups:control group, sport group, Tau group and Ts group.9 groups of rats were taking compound oral liquid xinkang of different ingredient, and the swimming time was observed.Exosomatic heart model of Wistar ratswere divided into three groups:control group, A/R group and xinkang group. Heart function index, CPK activity, MDA, GSH-PX, SOD and myocardial microscopic struc-ture were observed.The ventricular myocardial cells of 1 -3 days old SD rats were divided into three groups.In control group, the cells were cultivated with reperfusion liquid.In A/R group, the cells were cultivated with an-oxia/reperfusion liquid.In xinkang group, the cells were first cultivated with xinkang oral liquid and second with anoxia/reperfusion liquid. Myocardial survival ratio, LDH activity in cultivating liquid and myocardial microscopic structure were observed. RESULTS: Swimming time in Tau and Ts groupwere longer than that in sport group (P<0.05). Serum CPK in Tau and Ts group were lower than that in sport group (P<0.05). Taurine influenced the swimming time much more than salvia miltiorrhiza. Taurine of high concentration and salvia miltiorrhiza of middle concentration were better. LVSP, dp/dt max and HR in control group were steady during perfusion, but those in A Rgroupwere decreased during perfusionfor 5, 10, 20 and 30 min (P<0.01), and those in xinkang group were higher than those in control group during per-fusion for 5, 10, 20 and 30 min (P<0.01). In A/R group, myocardial enzyme activity was lower, and MDA and CPK were higher than those in control group (P< 0.01). The results were inverse contrast xinkang group with A R group.Myocardial microscopic structure in con-trol groupwas normal, and that in A R group was serious-ly destroyed. The structure in xinkang group was im-proved. Myocardial survival ratio in A/R group was lower than that in control group (P<0.01). The ratio in xin-kang group was higher than that in A/R group (P< 0.01). LDH activity in A/R group was higher than that in control group (P<0.01). The activity in xinkang group was lower than that in A/R group (P<0.01). Myocardial microscopic structure in control groupwas nor-mal, and that in A/R group was seriously destroyed.The structure in xinkang group was improved.CONCLUSION: Oral liquid xinkang compounded of taurine and salvia miltiorrhiza can protect the myocardium experienced anoxia/reperfusion.
    Inhibitive and protective effects of guanxinning tablets on platelet aggrega-tion and vascular endothelium in qi stagnation and blood stasis rats
    CHEN Ming-li, SHOU Qi-yang, PAN Yong-ming, ZHANG Jian-bing, SANG Rui, GUAN Min-wen, WU Bi-yuan
    2005, 10(5):  586-589. 
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    AIM: To observe the effects of the guanxinning tablets on platelet aggregation, blood coagu-lation and vascular endothelial secretion function in qi stagnation and blood stasis rats.METHODS: Rats were treated with high (1.2 g°kg-1), middle (0.6 g°kg-1) and low (0.3 g°kg-1) doses of guanxinning for fifteen days, and then qi stagnation and blood stasis rat model was established by adrenalin subcutaneous injection and ice water immersion.Spontaneous platelet aggregation and adhesion rate, prothrombin time (PT), thromboplastin time (TT), activated partial thromboplastin time (APTT), level of plasma thromboxane B2 (TXB2), 6-Ke-to-PGF, nitric oxide (NO), endothelin (ET), content of MDA and activity of serum superoxide dismutase (SOD) were determined. RESULTS: Spontaneous platelet aggregation and adhesion rate in guanxinning rats was remarkably descended.PT, TT, APTT content of NO and TXB2 in plasma were elevated significantly, the content of MDA in serum was increased and activity of SOD was re-duced obviously. And the content of ET in plasma was decreased obviously, and the rate of (TXB2) to 6-Keto-PGF in plasma was digressive. CONCLUSION: Guanxinning contributes to inhibit platelet aggregation and blood coagulation in rat models, to boost elimination for free radical, and to improve secretion function of vascular ehdothelial cells.
    Design of clinical trials of Chinese Herbs Medicine in treatment of patients with headache
    LI Tao
    2005, 10(5):  590-593. 
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    The clinical trials of Chinese Herbs Medi-cine should meet the guidelines of International Headache Societion (IHS)in treatment of patients with tension-type headache and migraine, including the choice of subjects and control, and different criteria.
    Design of clinical trials of TCM new drugs in treatment of patients with chronic idiopathic constipation
    JIANG Meng, XIONG Ning-ning, ZHOU Xian-hong, SHEN Hong
    2005, 10(5):  594-597. 
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    In treatment of patients with chronic func-tional constipation, the clinical trials of TCM new drugs should include cases in accordance with the principle of shunting diagnosis and treatment. If the cases do not ob-tain effect, they are converted to secondary diagnosis and treatment, and the results will be feedback to re-evaluate the curative effect of the new drug. The design of protocol will take into account the drug formulae and the charac-teristics of the effects.This design may guarantee the ac-curacy of the results of trials and safety of subject.
    Problems and countermeasures of choice of control drug in clinical trials of the traditional Chinese new drug
    XIANG Nan, DENG A-li, DENG Lan-qiong, ZHAI Hua-qiang, LI Xiao-dong
    2005, 10(5):  598-600. 
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    The choice of control drug is an important factor in the clinical trial of the traditional Chinese drug, and it directly relates to the quality of clinical trial. This paper lists several problems about the choice of control drug and puts forward some proposal and countermea-sures.