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Table of Content

    Volume 11 Issue 7
    26 July 2006
    Progress and research in epigenetic therapy of tumor
    WANG Qiu-cheng, ZHOU Xiang-jun, WANG Yong-xiang
    2006, 11(7):  721-724. 
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    Epigenetic modification includes DNA methylation and histone modifications.Aberrant epigenetic modifications result in generation and development of tumor.The relationship between epigenetic modifications and tumor development as well as epigenetic therapy is reviewed.
    Effect of metallothionein on Doxorubicin-induced superoxide production in mice heart
    GUO Jia-bin, CHEN Li-juan, YAN Chang-hui, YANG Hai-ying, WANG Guo-qiang, PENG Shuang-qing
    2006, 11(7):  725-738. 
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    AIM: To investigate the effect of metallothionein(MT)on Doxorubicin (DOX)-induced superoxide generation.METHODS: Male wild type (MT+/+)and metallothionein-null (MT-/-)mice were divided into 4 groups respectively and were pretreated with either saline or ZnSO4(20 mg·kg-1 , s.c.)at 24 h and 48 h before a single administration of DOX (15 mg·kg-1 , i.p.)or equal volume of saline.Mice were sacrificed on the 4th day after treatment and their hearts were collected for analysis.RESULTS: Doxorubicin treatment significantly enhanced superoxide generation and depleted glutathione in MT+/+mice heart and these effects were even more severe in MT-/-mice.These toxic changes were greatly inhibited by zinc pretreatment in MT+/+ mice heart but not in MT--mice.Furthermore , zinc pretreatment significantly inhibited DOX-induced promotion of eNOS inMT+/+mice while similar effect did not occur in MT-/-mice.CONCLUSION: Metallothionein can inhibit DOX-induced enhancement of superoxide generation and protect the antioxidant defense system in mice heart , this effect is possibly associated with changes of eNOS expression.
    Effects of budesonide on expression of basic fibroblast growth factor and mRNA in asthmatic rats
    YE Hui, LI Chang-chong, CHEN Li-zhong, YING Xiao-ming
    2006, 11(7):  739-742. 
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    AIM: To investigate the effects of budesonide on expression of basic fibroblast growth factor and mRNA in asthmatic rats.METHODS: Thirty six male Sprague-Dawley rats were randomly divided into three equal groups, including asthma group, control group and budesonide treatment group.In this experiment, the rat model of asthma was established by the ovalbumin challenge methods.The concentration of basic fibroblast growth factor in bronchoalveolar lavage fluid(BALF) was measured by ELISA, the expression of the protein of basic fibroblast growth factor and mRNA were detected with immunohistochemistry methods and in situ hybridization methods.RESULTS: The concentration of basic fibroblast growth factor in bronchoalveolar lavage fluid, the protein and mRNA expression of basic fibroblast growth factor in lung tissue were significantly higher in the asthma group than those of control group (P<0.01) , it was much lower in the treatment group than that in the asthma group, but it was still higher than the control group.The epithelial cell is the chief expression cell.CONCLUSION: The basic fibroblast growth factor participates in the pathogenesis of asthma, inhaled budesonide can significantly inhabit the expression of the protein and mRNA of basic fibroblast growth factor in the acute stage of asthma,and prevent the airway remodeling.
    Differentiation-inducing activity of tubeimoside I in human erythroleukemicK562 cells
    LIU Ji-yan, GAO Ying, YU Li-jian, MA Run-di
    2006, 11(7):  743-747. 
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    AIM: To examine the differentiation-inducing effect of tubeimoside I on human erythroleukemic K562 cells.METHODS: The growth inhibitory activity of tubeimoside I was evaluated with K562 cells.Trypan blue exclusion , morphological observation , cytochemistry were used to observe the features of erythroid , granulocytic,and megakaryocytic lineages differentiated from K562 cells.Using Western blot analysis , we studied alterations in c-myc and c-fos expression accompanying tubeimoside I-induced differentiation of K562 cells.RESULTS: Tubeimoside I inhibited the proliferation K562 cells and induced the differentiation of K562 cells into the erythrocyts.It could down-regulate c-myc and up-regulate c-fos ,and the steps were found to be the early events of K562 cell differentiation mediated by tubeimoside I.CONCLUSION: Tubeimoside I can induce the differentiation of K562 cells into the erythrocytes , and down-regulation of c-myc and up-regulation of c-fos which are the early responses of K562 cells to the induction of differentiation mediated by tubeimoside I.
    Mechanisms of polyvinylpyrrolidone combined with adriamycin against bladder cancer and its clinical use for preventing tumor recurrence
    HAN Zi-hua, WENG Zhi-liang, WU Xiu-ling, YU Zhi-xian, WANG Tian-ji, LI Cheng-di
    2006, 11(7):  748-751. 
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    AIM: To investigate the clinical effects of polyvinylpyrrolidone and adriamycin in preventing postoperative recurrence of superficial bladder cell cancer and its mechanism.METHODS: 231 postoperative cases received intravesical instillation with adriamycin combined with polyvinylpyrrolidone (experiencial group) or isotonic Na chloride combined with adriamycin (control group).Bcl-2 and Bax protein expression was examined by immu-· 750 · Chin J Clin Pharmacol Ther 2006 Jul;11(7)nohistochemistry after 50 cases received intravesical instillation in such way before operation.Concentration and callback rate of adriamycin combined with polyvinylpyrrolidone were examined by ultraviolet analysis.RESULTS: 194 cases were followed.In experimental group, recurrence was found in 24 cases (18.6 %) , hematuria in 2 cases and bladder irritation in 3 cases.In control group,recurrence was found in 39 cases (60.0 %).Compared with control group, Bcl-2 expression in experimenta group has no difference (P>0.05) , Bax expression was up-regulated significantly (P<0.01) and Bcl-2 Bax expression was down-regulated (P<0.05).Polyvinylpyrrolidone and adriamycin could prolong evacuation time 2-4 times as long as NS and adriamycin in bladder.CONCLUSION: Intravesical instillation of polyvinylpyrrolidone and adriamycin are effective for prevention of postoperative recurrence of superficial bladder cell cancerwith fewer side effects Polyvinylpyrrolidone combined with Adriamycin can induce bladder cancer cell apoptosis and prolong medication time in bladder.
    Effect of dexamethasone Angelica sinensis polysaccharide prodrug on trinitrobenzene sulfonic acid induced ulcerative colitis in rats
    LIU Xin-you, ZHOU Si-yuan, CHENG Jian-feng1, TENG Zeng-hui, RAN Yu-hua, YANG Run-tao,YANG Xi, MEI Qi-bing
    2006, 11(7):  752-755. 
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    AIM: To explore the therapeutic effect of dexamethasone Angelica sinensis polysaccharide prodrug(DEX-AP) on trinitrobenzene sulfonic acid (TNBS) induced ulcerative colitis (UC) in rats and its side effects.METHODS: The experimental UC rats were induced by clusis of the solution of TNBS in 45 % alcoho1 (50 mg·ml-1 ).The UC rats were orally administrated with0.25μmol·kg-1·d-1 DEX and 0.05, 0.25, 1.25μmol·kg-1 ·d-1 DEX-AP (calculated by carried DEX in DEX-AP) for 7 days, respectively.The rats were killed after the amount of peripheral blood lymphocyte was counted,then the spleen, thymus and colon were separated and weighted.After the ulcerative area of colon was calculated,the colonic myeloperoxidase (MPO) activity was determined and parts of colon were paraffin sectioned and examined under light microscope by HE stain.RESULTS: After the UC rats were administrated with different doses of DEX-AP for 7 days, the ulcerative area, the weight and the MPO activity of colon reduced significantly.The reduction of MPO activity was correlated to the dose of DEX-AP and the MPO activity with DEX-AP at the doses of 0.25, 1.25μmol·kg-1 ·d-1 reduced more significantly than that with DEX at the the dose of 0.25μmol·kg-1·d-1.The number of peripheral blood lymphocyte,spleen weight and thymus weight of UC rats reduced significantly at the dose of 0.25μmol·kg-1 ·d-1DEX (P<0.01, compared with control group).DEXAP showed no significant effect on the number of peripheral blood lymphocyte, spleen weight and thymus weight of UC rats at the doses of 0.05, 0.25 μmol·kg-1 ·d-1.With the administration of 1.25 μmol·kg-1·d-1 DEX-AP to UC rats, the structure of the colonic mucosal tissue almost recovered.CONCLUSION: DEX-AP has significant therapeutic effect on TNBS induced UC rats and it has no obvious side effects, thus it indicates a great potential in treating UC.
    Effect of budesonide on eosinophils and histamine in nasal mucosa of guinea pig with allergic rhinitis
    DENG Qiu, ZHOU Yun, YANG Jun, LI Ying, ZHU Xiao-nong
    2006, 11(7):  756-759. 
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    AIM: To build an allergic rhinitis model to evaluate the effect of budesonide on the eosinophils and histamine in nasal mucosa in allergic rhinitis guinea pig.METHODS: 33 guinea pigs were randomly divided into three groups:natural controlled group , allergic rhinitis (AR)group and budesonide treatment group.Allergic rhinitis model in guinea pigs were built by using toluene-2 , 4-disocyanate (TDI) nasal immunization and challenge.The indexes of clinical symptoms , pathomorphological diagnosis and content of histamine in mucosa were used to evaluate the potency of budesonide when used to treat allergic rhinitis.RESULTS: The expression of eosinophils and the content of histamine in nasal mucosa in AR group both were significantly higher than that of in natural controlled group (respectively ,P<0.01 and P<0.05).After the treatment , the expression of eosinophils and content of histamine in guinea pigs nasal mucosa were significantly decreased (bothP<0.01)compared with the AR group.The point rating of clinical symptoms of guinea pig nasal in both AR group and treatment group were higher than that of in natural group (P<0.01).However , there was no difference between AR group and treatment group (P>0.05).CONCLUSION: Budesonide could effectively reduce the expression of eosinophils and content of histamine in nasal mucosa ,but it is invalid in releasing the symptoms of AR in guinea pig.The reason of this phenomenon may be concerned with the method of model building.
    Effect of recombinant human endostatin on expression of vascular endothelial cell growth factor in adjuvant arthritis synovium tissue
    XIA Li-juan, CHEN Fei-hu, HUANG Xue-ying, LIU Yong-jing, LI Jun
    2006, 11(7):  760-763. 
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    AIM: To investigate the effect of recombinant human endostatin on the expression of vascular endothelial cell growth factor (VEGF) in adjuvant arthritis synovium tissue.METHODS: Adjuvant arthritis rat model was induced by a single intradermal injection of 100 μl of Freund' s complete adjuvant(CFA) on d 0.The volume of rat hind paw was measured by means of Volume Meter.The expression of VEGF and microvessel density of the synovial tissue were measured by immunohistochemical method.RESULTS: The secondary inflammation of Adjuvant-induced arthritis(AA) rats appeared on the d 10 after the injection of CFA.The therapeutic administration of recombinant human endostatin(1.25, 2.5, 5.0 mg·kg-1 )were given for 7 days consecutively.Methotrexate (MTX)(1.0 mg·kg-1 )was given only once on d 10 as the control.It was found that recombinant human endostatin significantly inhibited the secondary paw swelling.Recombinant human endostatin significantly decreased the expression of VEGF and microvessel density of the synovial tissue on AA rats.CONCLUSION: Recombinant human endostatin had an inhibitory effect on the expression of VEGF and microvessel density of the synovial tissue on AA rats, which was related to its anti-angiogenesis and an inhibition of VEGF on synoviocytes.
    Inhibitory effects of tubeimoside 1, a cyclic bisdesmoside isolated from Bolbostemma paniculatum, on metastases of mouse B16 melanoma and lewis lung carcinoma
    WANG Chang-xiu, MA Run-di, YU Li-jian
    2006, 11(7):  764-770. 
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    AIM: To investigate the effects of tubeimoside 1 on the metastases of mouse B16 melanoma and lewis lung carcinoma.METHODS: The effects of tubeimoside 1 on metastasis were studied by using an experimental metastasis model of mouse B16 melanoma cell line and a spontaneous metastasis model of mouse lewis lung carcinoma.The effects of tubeimoside 1 on the expressions of CD44v6, ErbB-2, and nm23-H1 were studied by using streptavidin-peroxidase two step immunohistochemical method.RESULTS: In mice that received i.v.injec-tion of mouse B16 melanoma cells, daily i.p.administration of tubeimoside 1-without reaching systemic toxicic levels-remakably reduced lung weight, and number of lung metastases, with preservation of apparently healthy and active behaviors.Lung metastasis inhibition rates of B16 melanoma cells by tubeimoside 1 (2, 3 mg·kg-1·d-1×14 d) and cyclophosphamide (50 mg·kg-1 ·wk-1 ×2d) were 68.8 %, 82.8 %, and 49.1 %, respectively.The weight of primary tumors of mouse lewis lung carcinomain the tubeimoside 1-administered mice was significantly less than that of the control (P<0.05).The liver metastasis inhibition rates of lewis lung carcinoma by tubeimoside1 (2, 3 mg·kg-1·d-1 ×14 d) and cyclophosphamide(50 mg·kg-1 ·w-1 × 2 d ) were 46.3 %,52.0 %, and 54.7, respectively.Treatment of tubeimoside1 apparently resulted in down-regulation of expressions of CD44v6 and ErbB-2, and up-regulation of expression of nm23-H1 in mouse lewis lung carcinoma cells.CONCLUSION: These observations qualify tubeimoside 1 as an interesting lead compound to prevent cancer spread and metastatic growth.
    Bioequivalence study of ranitidine caps in healthy volunteers
    CHEN Lei, YANG Jing, ZHOUMei, YU Feng, WANG Guang-ji
    2006, 11(7):  771-775. 
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    AIM: To study the pharmacokinetic activities and bioequivalence of ranitidine capsule after oral administration in healthy volunteers.METHODS: A single administration of 300 mg test and reference ranitidine were given to 20 healthy male volunteers in randomized crossover study respectively.The HPLC was developed to determine the concentration of ranitidine in human plasma.RESULTS: The pharmacokinetics parameters after a single oral dministration of 300 mg test and reference products were as follows:Cmax were 1.62±0.56 and 1.78±0.69 μg·ml-1, t max were 2.8±1.1 and 2.6±0.8 h, AUC0-τ were 6.69±1.46 and 6.67±1.86μg·h·ml-1 , AUC0-∞ were 7.06±1.56 and 7.06±1.86 μg·h·ml-1 , respectively.The relative bioavailability of single oral administration group was 103.8 %±19.1 %.CONCLUSION: The test and reference products were bioequivalent.
    Analysis of biologically active compounds in Erzhi Pills and its compositions by immobilized liposome chromatagraphy
    CHEN Bing-luan, SHENG Liang-hong, LI Ping, ZOU Han-fa, ZHANG Lu-yong
    2006, 11(7):  776-779. 
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    AIM: To analyse the intestinal absorbable compounds in Erzhi Pills and its compositions by immobilized liposome chromatagraphy (ILC ).METHODS: The ILC column separation and retention of the extracts of Erzhi Pills, Fructus Ligustri Lucidi and Herba Ecliptae extracted with different solvents were observed.Also analysed were the contents of quercetin and apigenin in 75 % ethanol extract of Erzhi Pills, Fructus Ligustri Lucidi and Herba Ecliptae.RESULTS: It was found that the 75 % ethanol extract was better than the water extract based on the number and peak areas of retention peaks.In the 75 % ethanol extract of Erzhi Pills, the content of quercetin was 9.6 μg·g-1 , and the content of the apigenin was 2.7 μg·g-1.The content of quercetin and apigenin in the 75 % ethanol extract of Herba Ecliptae corresponded to 2.8 and 3.8 μg·g-1 respectivelly.In the 75 % ethanol extract of Fructus Ligustri Lucidi, the content of quercetin was 9.1 μg·g-1 , but apigenin was not detected.CONCLUSION: Quercetin and apigenin are two main retained components of Erzhi Pills on ILC, the former is contributed by both Fructus Ligustri Lucidi and Herba Ecliptae, the latter only by Herba Ecliptae.Quercetin and apigenin were predicted to be intestinal absorbable components of Erzhi Pills with ILC.Immobilized liposome chromatagraphy can be used as a tool in screening possible bioactive ingredients and in quality control of traditional Chinese medicine (TCM).
    Study on absorption of ginsenoside Rg1 using rat ansa intestinal model
    LV Tian, SUN Jian-guo, LV Hua, XU Mei-juan, XIE Hai-tang, LI Hao, WANG Guang-ji
    2006, 11(7):  780-783. 
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    AIM: To develop an accurate, sensitive and reliable HPLC-MS method for the determination of ginsenoside Rg1 in rat plasma, and to study the absorption characteristics of Rg1 at different intestinal sections (duodenum, ileumand, jejunum and colon ) of rats.METHODS: Ginsenoside Rg1 or total ginsenoside which containing equal amount of Rg1 was injected into different intestinal sections (duodenum, ileum, jejunum and colon) of each rat.At the same time, Ginsenoside Rg1 or total ginsenoside was administrated to rats by intragastric gavage.Blood samples were collected according to preset timetable and Rg1 concentrations were determined.RESULTS: The bioavailability of Rg1 in rats was increased significantly when total ginsenoside was administrated compared with that of Rg1 given alone.The absorption profile of Rg1 was different in duodenum and ileum but similar in jejunum and colon.CONCLUSION: There might be some specific substance in total ginsenoside,which could improve the absorption of Rg1 in duodenum and ileum.
    Inhibitory effect of receptor of advanced glycation endproducts, nuclear factor-κB double gene antisense RNA on productions of inflammatory factor treated by advanced glycation endproducts
    YOU Jie, ZHAO Rong, LIU Li-bin, LIN Jian-yin
    2006, 11(7):  784-788. 
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    AIM: To observe the effects of receptor of advanced glycation endproducts(RAGE) , NF-κB double gene antisense RNA on the productions of TNF-αand IL-6 treated by advanced glycation endproducts (AGEs ).METHODS: The levels of TNF-αand IL-6 in the supernatants were measured by enzyme linked immunosorbent assay (ELISA) in ECV304 cells treated by AGEs.The RAGE, NF-κB single double gene antisense RNA were transfected into ECV304 cell.The expressions of RAGE and NF-κB were detected by flow cytometry and RT-PCR.In different clone cells, the effects of antisense RNA on the productions of TNF-α、IL-6 were determined by ELISA.RESULTS: AGEs, instead of human serum albumin (HSA) , stimulated ECV304 cell to produce TNF-α and IL-6 with a time-and dose-dependent manner.The RAGE, NF-κB single double gene antisense RNA were transfected into ECV304 cell.Induced by AGEs, the expressions of RAGE and NF-κB in double gene cotransfected cell were inhibited by (62.2 ±8.7) % and (37.2 ±7.1) %, respectively.Induced by AGEs, the amount of TNF-α、IL-6 in the medium were lower in single gene transfected cells ECV-asRAGE, ECV-asP65 than ECVVector(P <0.05).The amount of TNF-α、IL-6 in the double gene transfected cells ECV-asRAGE-asP65 were lower than ECV-Vector and ECV-asRAGE, ECV-asP65(P<0.05).CONCLUSION: The production of TNF-α and IL-6 is increased in ECV304 cell treated by AGEs.RAGE, NF-κB double gene antisense RNA can inhibited the production of inflammatory factor treated by AGEs.
    Calcium caused calcium release causes a vascular smooth muscle cell line A10 cells apoptosis
    WU Yu-lin, MA Bing-liang , DAI Xiao-ming, CHEN Lin-lin
    2006, 11(7):  789-796. 
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    AIM: To investigate the apoptosis of a vascular smooth muscle cell line A10 caused by mild K+depolarization.METHODS: Apoptosis was evaluated by nuclear staining, DNA fragmentation gel electrophoresis and propidium iodide-stained flow cytometry.Mitochondrial transmembrane potential (Δψm) was measured by flow cytometry.RESULTS: K+depolarization caused dose correlated A10 cells apoptosis; nifedipine, BAPTA AM, ryanodine inhibited the cytotoxic effect of K+completely.The combination use of nifedipine and cyclosporin A made it clear that mitochondria was involved in the apoptosis of A10 cells, and Δψm measurement further confirmed this speculation; A10 apoptosis caused by K+depolarization was not influenced by heparin or Zn2+, a effectivecapacitative calcium entry(CCE) blocker.CONCLUSION: Ca2+entry through voltage-dependent ca channels increases intracytoplasm Ca2+, then triggers furtherCa2+release from endoplasmic reticulum via ryanodine receptor, and the microdomains of elevated intracytoplasmCa2+are sensed by adjacent mitochondria, which ultimately lead to cell apoptosis.
    Protective effect of Hydroxyethyl Starch on hemorrhagic-shocked rat brain
    LIAO Shi-hong, CUI Rui, YUAN Cong-shun
    2006, 11(7):  797-800. 
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    AIM: To investigate the protective effect of 6 %Hydroxyethyl Starch (HES, 200 0.5) on the brain of hemorrhagic-shocked rats.METHODS: Sprague-Dawley rats were randomly divided into sham operation group (group A) , hemorrhagic shocked group(group B) , whole blood return group(group C) , HES at 2x shed blood volume(SBV) group(group D) , HES at 1x SBV plus 1/2 SBV group(group E).Hemorrhagic Shock was induced by intermittently withdrawing blood from an iliac catheter.Except group A and B, the other groups were resuscitated with different liquids and lasted 30 min after 1h for shock.The extent of brain edema and inflammatory cells infiltrating was observed by Hematoxylin-Eosin staining,and the expression of nuclear factor kappa-B (NF-κB) in the rat brain and translocation of nucleus were detected using immunohistochemistry and Western blot method. RESULTS: Except the sham group, there were brain edema and inflammatory cells infiltrating in the other groups, which was more obvious in group C and D.The expression of NF-κB in the rat brain was significantly increased in group B and other groups as compared with those in group A (P<0.01);but their increase were markedly decreased in group E as compared with those in C and D groups(P<0.05 orP<0.01).The increase of translocation of NF-κB was nearly accordant with the expression of NF-κB in the rat brain in every group.CONCLUSION: Our results suggest that the expression and the translocation of nucleus of NF-κB in brain tissue were significantly increased in the rat during early hemorrhagic shock (acute blood loss was 35 % of the estimated total blood).6 %HES in the normal doses resuscitation can decrease the expression and the translocation of nucleus of NF-κB, and alleviate the cerebral ischemia-reperfusion injury , and there is the protective effect on the rat brain during hemorrhagic shock.
    Pravastatin improves level of antithrombin Ⅲ in rats combined nephrotic syndrome with hypercoagulability
    GAO Xu-xia, ZHANG Dao-you, SONG Jian-guo, ZHANG Hui
    2006, 11(7):  801-805. 
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    AIM: To investigate the anticoagulant effect of pravastatin and low molecularweight heparin (LMWH), as well as their combination, over time, in a rat model of experimental nephrotic syndrome.METHODS: Healthy SD male rats were chosen randomly to perform nephrotic syndrome models by single injection of Adriamycin via tail vein, the matched normal control rats received single injection of equivalent 0.9 % sodium chloride instead.After 14 days, the models were set up and randomized into model control group, pravastatin group (pravastatin 2mg·kg-1·d-1gavage once a day) , LMWH group(LMWH 200 U·kg-1 ·d-1 intraperitoneal injection once a day) and combined treatment group(pravastatin 2mg·kg-1 ·d-1gavage+ LMWH 200 μ·kg-1 ·d-1intraperitoneal injection) , then all rats underwent measuring proteinuria every two weeks and fibrinogen, antithrombin Ⅲ(AT Ⅲ) , D-dimer, platelet count, serum total protein and serum albumin after 4 weeks of treatment.RESULTS: The concentration of fibrinogen and D-dimer in model group was higher significantly than that in control group, and the level of AT Ⅲ was lower remarkably than that in control group, but platelet count had no obvious change; Compared with model group, pravastatin could increase the level of AT Ⅲ and decrease the concentration of D-dimer, but the concentration of fibrinogen and platelet count did not change obviously; LMWH and combined treatment could also decrease level of D-dimer, but had no great effects on AT Ⅲ, fibrinogen and platelet count; all treatment group had no obvious change of serum total protein and serum albumin.CONCLUSION: Adriamycin-induced nephrotic syndrome rat models have hypercoagulability and pravastatin can increase the level of ATⅢ.;
    Protective effects of mitoKATP opener on cardiac myocytes damages induced
    ZENG Yuan, LONG Chao-liang, LI Yan-fang, WANG Hai
    2006, 11(7):  806-809. 
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    AIM: To investigate the protective effects of Diazoxide, a selective mitoKATP opener, on the cardiac myocytes damages induced by oxidative stress and to discuss its mechanism.METHODS: Oxidative damage cell model was induced by hydrogen peroxide (H2O2 500 μmol·L-1).Lactate dehydrogenase (LDH) activities in the medium and mitochondrial membrane potential assessed in flow cytometry by dual labelling with rhodamine-123 (Rh-123) and propidium were measured in the diazoxide(100 μmol·L-1 ) pretreated and un-pretreated groups.RESULTS: The level of LDH and the percentage of injured cells in H2O2 exposure group after 2 h injury were significantly higher than those in the control group(P<0.01).On the contrary, after exposure to H2O2 ,the Rh-123 fluorescence intensity was significantly decreased.Compared with simple injury group, pre-treatmentwith diazoxide (100 μmol·L-1 ) could obviously attenuateH2O2 induced cytotoxicity, which could be abrogated by the mitoKATP channel blocker 5-hydroxydecanoate(500 μmol·L-1).CONCLUSION: Diazoxide exerts significant protective effects against the damages induced by H2O2 in the cultured neonatal rat cardiomyocytes,which may be mediated by activation of mitoKATP channels.
    Effect of Heparin on heparanase mRNA expression and invasion of human hepatoma carcinoma cells in vitro
    CHEN Xiao-peng, LIU Ying-bin, SHI Liang-hui, PAN Yi-long, RUI Jing
    2006, 11(7):  810-813. 
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    AIM: To explore the effect of Heparin on heparanase (HPA) mRNA expression and invasion of human hepatoma carcinoma cells(HCC) in vitro.METHODS: Human liver carcinoma cells, BEL-7404, were transfected with a full-length human HPA cDNA using a pcDNA3 expression plasmid, and different dose of Heparin was added when the cells were cultured.The invasiveness of transfected BEL-7404 was measured by the Matrigel invasion assays, and the HPA mRNA expression was observed by using RT-PCR.RESULTS: The HPA mRNA expression could not be detected in BEL-7404 cells(HCC group) and HCC transfected with a control pcDNA3 plasmid lacking the HPA cDNA insert (pcDNA3 group) while the HPA expression was positive in HPAtransfected HCC (pcDNA3-HPA group).The number of membrane-permeating cells in pcDNA3-HPA group(27.00±4.30) was significantly more than that in the other groups (11.67±2.52 for HCC group and 9.67±2.89 for pcDNA3 group ) (P<0.01).No obvious changes inHPA expression and cell invasiveness were observed in both HCC group and pcDNA3 group after Heparin was added.The membrane-permeating cells in pcDNA3-HPA group gradually decreased along with the increase in the dose of Heparin, and the further decrease was no longer found when added Heparin exceeded a certain quantity.The HPA expression was positive all the time in pcDNA3-HPA group.CONCLUSION: Within a certain dose range, Heparin can inhabit the invasive ability of HPA gene-transfected HCC, but does not influence the HPA mRNA expression.
    Determination of dihydroartemisinin in human plasma by LC/MS/MS
    LIU Yi-ming, ZENG Xing, FENG Yi, ZHOU Dan, TANG Bo, WANG Hai-lan
    2006, 11(7):  814-817. 
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    AIM: To develop a HPLC MS MS method for the determination of dihydroartemisinin in healthy human plasma.METHODS: Artemisinin was used as the internal standard.Plasma samples were pretreated by liquid-liquid extraction.Dihydroartemisinin was detected by the positive electrospray ionization-MS method under multiple reaction monitoring mode.RESULTS: The calibration curve of dihydroartemisinin in plasma was linear over the range of 1.01-2 020 ng·ml-1 , the low limit of quantitation was 1.001±0.072 ng·ml-1.The relative recovery was 93.0 %-98.2 %.The within-day and between-day RSDs were both less than 10 %.CONCLUSION: This assay method is accurate, sensitive, and specific, and it is suitable for the measurement of plasma concentration.
    Effect of Danhong Zhiganching capsules in rats with experimental fatty liver
    LIU Yuan, CHEN Zhen, QIAN Zhi-yu
    2006, 11(7):  818-821. 
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    AIM: To study the effect of Danhong Zhiganching capsules on the experimental fatty liver in rats.METHODS: Male SD rats were treated by high fat diet for 6-week after being treated by a low dose of CCl4 to induce fatty liver model.Then, drugs were given by oral to the rats, the contents of triglyeride, total cholesterol in serum and liver tissue, the contents of superoxide dismutase and malondialdehyde in serum and the contents of free fatty acids in liver tissue acted as indexes to determine the effect of Danhong Zhiganching capsules.RESULTS: The contents of triglyeride and total cholesterol in serum and liver tissue of rats were significantly reduced by Danhong Zhiganching capsules, and so it is with the contents of free fatty acids in liver tissue (P<0.01,P<0.05).The contents of superoxide dismutase in serum was increased markedly by Danhong Zhiganching capsules and the contents of malondialdehyde was decreased (P<0.01,P<0.05).CONCLUSION: Danhong Zhiganching capsules show great effects on the experimental fatty liver induced by a low dose of CCl4 and high fat diet.
    Effects of total ginkgolides counteract platelet aggregation and experimental thrombosis
    GONG Xiao-jian, LI Yun-man, BIAN Hui-min, FANG Wei-rong, LIU Guo-qing
    2006, 11(7):  822-825. 
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    AIM: To study the effect of total ginkgolides on platelet aggregation and experimental thrombosis.METHODS: The model of artery-vein bypass thrombosis and Chandler' s method were established to observe the effect of total ginkgolides.Platelet activating factor,arachidonic acid and adenosine diphosphate were used to induce platelet aggregation in rabbits and the ratio of platelet aggregation was detected.RESULTS: It was found that total ginkgolides inhibited the artery-vein bypass and Chandler' s s thrombus in different degrees, reduced the thrombus weight significantly (either wet or dry,P<0.01);Total ginkgolides inhibited platelet aggregation with different revulsant at different time, and reduced the maximum aggregation rate.CONCLUSION: Total ginkgolides exerted remarkable effect against thrombosis and possessed strong effect against platelet aggregation induced by ADP and PAF.
    Best formulation and clinical effects of marzulene-S grranuls membrane for oral ulcer
    CHEN Hong, ZHOU Li-xia, LIN Zhong
    2006, 11(7):  826-828. 
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    AIM: To choose the best formulation of marzulene-S grranuls oral membrane and to evaluate the clinical effects.METHODS: Orthogonal method was used for studying.Take the appearance, viscidity and dissolubility of the oral membrane as the indexes of scoring 108 cases of patients were chosen and divided into two groups randomly.58 case were treated with marzulene-S grranuls oral membrane and 50 cases were treated with gargarisma chlorhexidine as the control group.RESULTS: The best prescription is sodium carboxymethyl cellulose 4 %, polyvinyl alcohol1750 1 %and polyvinyl alcohol17-88 3 %.CONCLUSION: The design of the formulation is reasonable and the clinical effect was satisfactory.
    Effects of Rosa roxburghii Tratt extract-CL1 on gastric carcinoma SGC-7901 cells growth and human umbilical cord CD34+cells proliferation and differentiation
    LIU Hong-lin, CHEN Dai-xiong, FANG Ning, YU Li-mei, LIU Jin-wei, LIU Zu-lin, WEN Guo-rong, YANG Xiao-sheng, XIAO Yu, QI Ying, XIAO Jian-hui, WAN Wei-hong, HU Xi-jie
    2006, 11(7):  829-832. 
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    AIM: To investigate the effects of Rosa roxburghii Tratt extract-CL1 on proliferation of gastric carcinoma SGC-7901 cells, and on proliferation and differentiation of human umbilical cord (UCB) CD34+cells.METHODS: The OD value of living cells was measured by MTT test.UCB CD34+cells were isolated by magnetic-activated cell sorting, and surface marker of cells was determined using f low cytometry.Cells were counted by trypan blue dye exclusion test.RESULTS: The inhibitory percentages of CL1 (0.01-10 μmol·L-1) on growth of SGC-7901 cells were concentration-dependent and time-dependent from 12 to 96 h.After culturing for 14 d,compared with control group, there was a downtrend of the numbers of CL1 10 and 1 μmol·L-1 but there was no significance(P>0.05) , and there were no difference in the cell number percentage of both expressing CD15 and expressing CD11b.But compared with d 0, the cell number percentage of expressing CD15 were remarkably increased;the cell number percentage of expressing CD11b had an increasing tendency, but it was not significant (P>0.05).CONCLUSION: CL1 has inhibitory effect on growth of SGC-7901 cells in vitro, but does not affect proliferation of CD34+and differentiation of CD34+haematopoietic stem progenitor cells to granulocyte and monocytes.This demonstrates that CL1 has anticancer effect,but does not affect the proliferation and differentiation of haematopoietic stem progenitor cell to granulocytes and monocytes.It may not cause obvious haematopoietic depression.
    Pharmacokinetic and bioequivalence studies of simvastatin tablet in healthy volunteers by LC-MS/MS
    LIU Shi-jia, CHU Ji-hong, JU Wen-zheng, TAN Heng-shan, XIONG Ning-ning
    2006, 11(7):  833-836. 
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    AIM: To establish a LC-MS MS method for determination of simvastatin in human plasma, and investigate the pharmacokinetics and bioequivalence of simvastatin tablet in Chinese healthy volunteers.METHODS: 20 male healthy volunteers were randomized to receive a single crossover oral dose of simvastatin reference tablet or domestic tablet.The concentration of simvastatin in plasma was determined by LC-MS/MS.RESULTS: The main pharmacokinetic parameters of test and reference simvastatin tablets were as following:Tmax:1.8 ±1.3,2.10 ±1.00 h, Cmax:7.12 ±1.61, 7.38 ± 1.54μg·L-1 , AUC(0-24):30.50 ±11.25, 30.17 ±10.21μg·h·L-1 , t1/2 :3.90 ±0.78, 3.76 ±0.85 h, respectively.F (0-24) was (101.2 ±7.8) %.CONCLUSION: The assay method is shown to be sensitive and accurate giving reliable results.The test tablet was bioequivalent to the reference tablet.
    Ethic review in clinical research:persons who are serving a sentence or receiving reeducation through labour
    WANG Xiu-qin, XIONG Ning-ning, LIU Shen-lin, LI Qi-yi, JIANG Meng, LIU Fang, ZOU Jian-dong, GAO Wei-min, XUE Xue-kun
    2006, 11(7):  837-840. 
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    Persons who are serving a sentence refer to those who are serving a sentence in a prison, Persons who are receiving reeducation through labour refer to those who are receiving reeducation through labour in an institution,for short, both are called persons who are serving a sentence or receiving reeducation through labour.Ethical justification for research involving this special group are as follow:specific IRB should include someone who has appropriate background and experience to serve in that capacity;the research might not equally well be carried out with subjects other than persons who are serving a sentence or receiving reeducation through labour;definition of minimal risk shouldn' t be compared with the risks normally encountered by this special group, but rather that of healthy persons;free choice in informed consent should be ensured;arrange treatment for research subjects after research terminated;fairly distribute research burdens;maintain confidentiality of research data and privacy;reasonable payment need to be considered, etc.