Table of Content

Volume 11 Issue 9
26 September 2006

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Cardiac arrhythmias, ion channelopathy and new drug discovery

DAI De-zai

2006, 11(9):  961-965. 

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Occurrence of severe life-threatening arrhythmias is based on ion channelopathies in the sarcolemma or sarcoplasmic reticulum of myocardium.It has not been successful in research and development of antiarrhythmic agents which failed to suppress life-threatening tachyarrhythmias in the two famous clinical trials (CAST&SWORD) , attributed to lack of understanding of the channelopathy in myocardium.Patients with the LQTS(Long QT syndrome) caused by mutations in the hERG,KvLQT1 and SCN5A or the SQTS (short QT syndrome) by gain-of-function mutations in hERG and KvLQT1 or CPVT caused by mutation of RyR2 gene in sarcoplasmic reticulum, are at risk to developlife-threatening arrhythmias.Cardiomyopathy induced by L-thyroxin medication shares some resemblance with the above gene mutations and manifests varied length of APD.It provides an ideal animal model to investigate the mechanism underlying cardiac arrhythmias and evaluate activity of antiarrhythmic agents.CPU86017, an agent to block multiple ion channels,and CPU0213, a novel endothelin receptor antagonist,are under investigated and possess a promising effect to suppress cardiac arrhythmias by correcting the channelopathy in myocardium.

Mechanism profile of drug intestinal absorption about transporters , enzyme and potential

GUO Yuan-yuan, WANG Hui<, CHEN Ken<

2006, 11(9):  966-971. 

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The intestinal absorption of orally drug is a complicate process , which is not only dependent on physicochemical properties of drugs but also dependent on factors of organism and absorption conditions.This article summarized mechanism of drug intestinal absorption such as transporters , enzyme and potential.

Advances in mechanism on insulin-like actions of vanadium

ZHANG Ling, LI Da-wei, XIA Zuo-li, LI Qing<

2006, 11(9):  972-977. 

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The insulin-mimetic effect of vanadium is the most remarkable and important function among its several biological actions.Basing on the lots of representative literatures, this review summarized the researching background, development and acting mechanisms on the insulin-mimetic effects of vanadium.The key mechanisms involved are inhibition of protein-phosphotyrosine phosphatases and activation of nonreceptor protein-tyrosine kinases,in an insulin-receptor tyrosine kinase independent fashion.

Correlation of lamotrigine concentrations between saliva and serum in children with epilepsy

ZHANG Shen, WANG Li, LIU Ying

2006, 11(9):  978-982. 

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AIM: To study the correlation of LTG concentrations between saliva and serum in children with epilepsy.METHODS: After informed consent was obtained from the parents or guardian of children, children with primary epilepsy were collected in Peking University First Hospital.When reaching the steady drug concentration,1.0 ml blood samples were obtained by phlebotomy,and 0.5 ml saliva sample were collected at the same time.Serum and salivary LTG concentrations were determined by reversed-phase high performance liquid chromatography(RP-HPLC).Statistics software SPSS11.5 was used for data analysis.RESULTS: Linear regression analysis was made by LTG concentration (C) and the peak area ratio (Y) of LTG vs.internal standard (flurazepam),and the regression equation of serum concentration and saliva concentration were Y =0.1824 C -0.0080, r =0.9998 and Y =0.1816 C -0.0119, r =0.9997, respectively.We collected 39 patients and 53 serum and saliva concentrations samples, of whom, 27 were male and 12 female, aged 1 to 15 years (the average was 7.86).The correlation between LTG serum concentration(x) and saliva concentration(y) was y =0.5607x-0.6074 (n =53, r =0.9501, p<0.001).Themean saliva/serum LTG concentration ratio was 0.42 ±0.11.CONCLUSION: A significant positive correlation was found between LTG serum and saliva concentrations.Saliva sample may be a useful alternative to serum for therapeutic monitoring of LTG treatment, because saliva collection is simpler, less painful and cheaper than blood drawing, thus children may particularly benefit from this method.

Reversal of antibiotic resistance in methicillin-resistant Staphylococcus aureus by antisense phosphothioate oligodeoxynucleotides liposome

HUAN Meng-lei, LUO Xiao-xing, MENG Jing-ru, HENG Liang

2006, 11(9):  983-986. 

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AIM: This study was using man-made dipalmitoyl phosphatidylcholine and dimyristoyl phosphatidylglycerol to prepare antisense oligodeoxynucleotide (AsON)anionic liposomes and to investigate the inhibitory effect of an antisense phosphothioate oligodeoxynucleotides(AS-ODNs)liposome targeting BlaR1 mRNA in methicillin-resistant Staphylococcus aureus (MRSA).METHODS: Designed and synthesized AS-ODNs by software. Prepare liposome by thin film-dispersion ,lyophilized technique.The appearances of liposomes were observed by transmission electron microscope.The liposomes were purified by centrifuge.The encapsulation efficiencies and the leaking efficiencies were determined by UV methods.The release properties in vitro were determined by agitation in PBS.The total colony forming unit(CFU)was counted.The bacteria growth curve was drawn by microplate reader.RESULTS: The liposomes were in spherical shape with uniform size.The encapsulation efficiency was 77.38 %and the leaking efficiency was 0.18 % after 1 month in lyophilized condition.The liposomes released 60 % drug after 24h when incubated in PBS with mild agitation.The AS-ODNs liposome could significantly inhibit the growth of MRSA compared with control groupand those AS-ODNs didn't encapsulated in liposome.Liposome encapsulated different concentration AS-ODNs could significantly decrease the CFU of MRSA ,which showed a concentration dependent manner (p<0.05), while AS-ODNs without liposome didn't show this effect.CONCLUSION: The liposomes prepared by this method were stable with a high encapsulation efficiency.The AS-ODNs liposome could reverse the antibiotic resistant in MRSA.The effect was better than those ASODNs without liposomes.This liposome could be used as a delivery system for AS-ODNs entrapped to bacteria.

Experiment of advancing chemosensitization of Etoposide by insulin in vitro

TIAN Chun-tao, JIAO Shun-chang, WEI Xiu-fang

2006, 11(9):  987-990. 

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AIM: To investigate the effects of insulin on drug sensitivity of Etoposide (Vp-16) to MBA-MD-543(human breast cancer cell line) in vitro.METHODS: Insulin was applied directly to the MBA-MD-543 cultured in vitro.The effects of insulin and Vp-16 on the number of viable cell, the total number of cells were assayed by MTT method and cell count.RESULTS: Insulin could induce the cell growth and promote the cell metabolism at the concentration 4.0 -32.0 mU·ml^-1(8 -18 hours).At the condition of same density of cells, the administration of insulin (7.5 mU·ml^-1) before adding Vp-16 in 9-15 h, enhanced the chemocytotoxity of Vp-16 (70.09μg·ml^-1) on human breast cancer cells as indicated by MTT colorimetry.CONCLUSION: Proliferation of human breast cancer cell line can be induced by insulin,and insulin can sensitize MBA-MD-543 to the anticancer activity of Vp-16 in vitro.The key of improving the chemotherapeutic effect is the selection of revulsant occasion and concentration.It is possible to increase the growth and metabolism of cancer cells first so as to enhance the chemosensibility, and then administer chemotherapeutic agents, thus improving their therapeutic effects.

Therapeutic effects of Taizhi'an on hyperlipidemia in rabbits

LI Qing-yi, MAO Yi-qing, ZHANG Jin-shu<, WU Nan, GAO De-lu<, ZHANG Yue-fei<, TAN Huan-ran

2006, 11(9):  991-994. 

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AIM: To observe the effects of Taizih'an in reducing the hyperlipidemia in rabbit models and to explore the mechanisms.METHODS: Hypelipidemia animal models were set upby normal diet and high choleisterol diet in rabbits.The concentrations of lipoprotein lipase and transaminase were detected by full automatic biochemical instrument.The fomation of plaque in the aorta was observed by staining with oil red O.RESULTS: Taizih'an obviously reduced the concentration of serum triglyeride and increased the content of lipoprotein lipase and high density lipoprotein.Taizhi'an had no obvious influence in the hepatic function.CONCLUTION: Taizhian can decrease the hyperlipidemia.Its mechanism is related to regulation of lipid metabolism and improvement of the concentration of lipoprotein lipase.

Effects of rheum tanguticum polysaccharides on ulcerative colitis induced by TNBS in mice

ZHANG Rong, WANG Zhi-peng, LIU Li, MEI Qi-bing

2006, 11(9):  995-998. 

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AIM: To explore the effects of rheum tanguticum polysaccharides (RTP) on TNBS -induced colitis in mice and its probable mechanisms.METHODS: Mice colitis model was induced by 2, 4, 6-trinitrobenzene sulfonic acid (TNBS).The mice were randomly divided into 5 groups, normal group, model group,RTP-100, 200 and 400 group.The macroscopical and histological changes of the colon were evaluated and the cytokines IL-8, IL-10, TNF-αand IL-4 produced by splenocyts were analyzed with ELISA.RESULTS: Compared with the model group, both symptoms and the lesions of colonic mucosa of RTP-200 and 400 groupwere slighter on ulcerative colitis induced by TNBS in mice.Furthermore, the expressions of TNF-αand IL-8 in colon tissue of mice with TNBS-induced colitis were higher and the IL-10 and IL-4 were lower than that of normal control(p<0.05).In RTP-400 group, the positive expressions of TNF-αand IL-8 were lower and IL-10 and IL-4 were higher than that of model group(p<0.01).CONCLUSION: RTphas significant effects on TNBS-induced colitis in mice, the mechanism of which may relate to its regulation on cytokines.

Effects of ozone-stress on E-cadherin expression in human bronchial epithelial cells

BAI Hong-bo<, GUAN Cha-xiang<, LIU Yong-ping<, ZHANG Min<, ZHENG Shi-ping<, CUI Yan-ru<, LIU Hui-jun

2006, 11(9):  999-1002. 

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AIM: To explore the expression of Ecadherin(E-cd)in the human bronchial epithelial cells(HBECs)and their role in the damage and injury of the airway.METHODS: The E-cd protein expression and the E-cd mRNA of HBECs were determined by immunocytochemistry analysisand RT-PTR analysis , respectively.RESULTS: Ozone-stress caused a decrease in the HBECs membrane E-cd expression and an increase the cytoplasmic E-cd expression (p<0.05).These changes returned to normal 32 h after the ozone-stress was withdrawn.O₃-stress had little effect on the expression of HBECs E-cd mRNA (p>0.05).CONCLUSION: Ecd is distributed on HBECs.O₃-stress decreases the membrane E-cd expression but increases the cytoplasmic E-cd expression.The change of E-cd expression may mediate HBECs injuries induced by O₃-stress.

Determination of dopamine and its metabolites in rat cerebral microdialysates by HPLC-ECD

JING Fu-chun<, LIU Xiao-li<, CHEN Hong<

2006, 11(9):  1003-1005. 

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AIM: To developa sensitive and rapid determination method of dopamine (DA)and its metabolites 3 , 4-dihydroxyphenylacetic acid (DOPAC)and homovanillic acid (HVA)in rat cerebral microdialysates.METHODS: Microdialysis probes were placed into the right stratums of Wistar rat brains and perfused with Ringer's solution at a rate of 1.5 μl·min^-1.A reverse phase HPLC with electrochemical detection (ECD)were used to assay DA , DOPAC and HVA after the cerebral microdialysates were collected every 20 minutes from awake , freely moving rats.In order to know the reliability of this method , selectivity , linear range , precision and accuracy were tested and the contents of DA , DOPAC and HVA in rat microdialysates were determined.RESULTS: The standard curve were in good linear at the range of 12.5 to 250 μg·L^-1.The recovery rates of DOPAC , DA and HVA at the concentration of 0.05 , 0.13 , 0.25μg·L^-1 were 98.33 %, 102.67 %, 92.33 % respectively.Their with-in day RSD were 3.3 %, 3.4 %, 2.5 % and between-day RSD 4.2 %, 2.3 %, 5.6 % respectively.The contents of DOPAC , DA and HVA in rat microdialysates were 1.79 ±0.07 , 0.45 ±0.02 , 1.67 ±0.05μg·ml^-1 (n =6), respectively.CONCLUSION: The simple , accurate and stable method can be applied to the study of the basic researches of diseases related to DA by cerebral microdialysis in rat.

Effects of N, N'-di-(m-methylphenyi)-3, 6-dimethyl-1, 4-dihydro-1, 2, 4, 5-tetrazine-1, 4-dicarboamide on HL-60 leukemia cells in vitro

ZHOU Yong-lie, LV Ya-ping<, HU Wei-xiao<, QIU Lian-Nu, WANG Wen-Song, YANG Zhong-yu<, LIU Jian-dong

2006, 11(9):  1006-1012. 

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AIM: To study the effect of N, N'-di-(m-methylphenyi) -3, 6-dimethyl-1, 4-dihydro-1, 2, 4, 5-tetrazine-1, 4-dicarboamide (ZGDHu-1) on proliferation inhibition, differentiation and apoptosis in HL-60 human leukemia cell line and explore its possible mechanism.METHODS: Different concentration of ZGDHu-1 and the different time of cultivate were used to treat HL-60 cell.The proliferation inhibition was analyzed by cell counting,alive cell count and MTT assay.Cell apoptosis was analyzed by cell morphology, DNA agarose gel electrophoresis,DNA content and Annexin-V/PI.The TdT-mediated dUTpnick end labeling (TUNEL) assay was used to quantitate the in situ cell apoptosis.The cell morphological analysis, expression of CD_11b, CD₁₃, CD₁₄, CD₆₄ and NBT reduction were performed to evaluate differentiation of HL-60 cells.The expressions of bcl-2, bax, Fas, P53 and mitochondrial membrane protein were analyzed by flow cytometry.While the mitochondrial transmembrance potential (ΔΧm) was labeled by dihydrorhodamin 123.RESULTS: ZGDHu-1 could inhibit HL-60 cell proliferation viability within a certain range of treating time and doses, with a 48 h IC50 of 180 ng·ml^-1 and 72 h of 180 ng·ml^-1.A majority of HL-60 cells were arrested in G2/M phase and a progressive decline in G0/1.The HL-60 cells apoposis was confirmed by type cell morphology,DNA fragment, sub-G1 phase, TUNEL and Annexin-Ⅴ/PI Labeling method with a time and dose related manner.The morphology of HL-60 cells cultured in the presence of 10 -100 ng·ml^-1 ZGDHu-1 for three days was more mature with higher positive rate of NBT and up-regulated expressions of CD_11b, CD₁₃, CD₁₄ and CD₆₄ than those of control.The expression of bax and Fas was increased,and bcl-2 was unchanged by the treatment of ZGDHu-1.ZGDHu-1 could increase the expression of mitochondrial membrane protein in a dose-dependent manner while the ΔΧm was reduced.CONCLUSION: ZGDHu-1 can inhibit proliferation, induce differentiation and apoptosis of HL-60 cells.The mechanism may associate with its upregulation of bax, open the mitochondrial permeability transition pore and reduce ΔΧm.Furthermore, the Fas is activated during the apoptosis process.

Targeting multiple signaling pathways in LNCaP prostate cancer cell line by trichostatin A

SUN Sheng-kun<, LIU Bing<, LI Xiu-shen<, HOU Chun-mei<, HONG Bao-fa2, YU Xiao-dan<

2006, 11(9):  1013-1016. 

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AIM: To investigate the molecular mechanisms underlying the antitumor effect of trichostatin A (TSA) on LNCaP prostate cancer cells.METHODS: Colony formation analysis was performed to assay the effect of TSA on LNCaP colony forming ability.Western blotting was used to analyze protein acetylation standard as well as the expression of a panel of signaling molecules after TSA exposure.RESULTS: TSA inhibited the colony forming ability of LNCaP cells at a very low concentration.TSA exposure caused elevated acetylation of total cellular proteins as well as accumulation of acetylated-H3.In addition, signaling molecules which play key roles in prostate cancer such as AR, ErbB2, Raf-1,CDK4, and Akt were depleted by TSA in a dose and time-dependent manner.CONCLUSION: TSA exhibits significant antitumor activity against LNCaP cells by simultaneously interfering with multiple signaling pathways such as HER2/MAPK, AR, and PI-3K-AKT pathways.

Study of animal trial and clinical use on fully soluble hemostatic fibre

WANG Hui-min, PAN Ji-yong<, YANG Bing<, LIU Ke-xin<

2006, 11(9):  1017-1020. 

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AIM: To investigate the hemostatic effect of fully hemostatic fibre (FHF).METHODS: In the animal experiment, 30 rabbits were treated to produce different models of trauma surface and artery and vein trauma.Different materials were used to stopbleeding, in order to compare the hemostasis time and the bleeding volume and observe the difference of hemostatic effect for different materials between before and after the treatment with heparin.A prospective study was designed.Two hundred and fourteen patients admitted in our department due to surgery were divided randomly into test groupand control group.FHF was used in test groupand Glutin Spong and vaseline oil gauze in the control groups for hemostasis with a view to comparing their hemostasis time and effect.RESULTS: It was suggested that the hemostatic effect of FHF had no significant difference with the Surgicel group.FHF and Surgicel groups appeared significant difference with the Glutin Sponge (p<0.05).No significant difference by using FHF was observed between before and after the treatment with heparin, but significant difference (p<0.05) was found in the Glutin Sponge.The results of clinical test suggested that the hemostatic time of FHF was shorter than that of control group.CONCLUSION: The results of animal experiment and clinical test demonstrated that the hemostatic effects of FHF were not only believable, but also safety and convenience.

Effects of centalla asiatica apozem compound on expression of α-SMA and vimentin in mice kedney with unilateral ureteral obstruction

YANG Ru-chun, WANG Yong-jun, ZHOU Da-wei, LIN Jing-lian, WANG jun, ZHU Xiao-ling

2006, 11(9):  1021-1025. 

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AIM: To investigate the effect of centalla asiatica compound on the expression of α-smooth muscle actin (α-SMA) and vimentin in mice kedney with the unilateral ureteral obstruction (UUO).METHODS: Mice were randomly assigned to sham operation group(sham group) , UUO model group, centella asiatica compound treatment groupand ACEI treatment group.The protein expression of α-SMA and vimentin was assessed by immunohistochemistry andWestern-blotting;The mRNA was detected by using reverse transcription-polymerase chain reaction analyses (RT-PCR);And the change of renal pathology was observed at the same time.RESULTS: In comparison with the sham group, the mRNA expression and protein levels of α-SMA and vimentin in the UUO model groupand treatments groups increased significantly,in addition, compared with UUO model group, centella asiatica compound and ACEI treatments could significantly ameliorate renal interstitial fibrosis and reduce the expression of α-SMA and vimentin protein.The effects of centella asiatica compound on vimentin were more significant than ACEI.CONCLUSION: Centella asiatica compound could reduce the transdifferentiation of renal tubular epithelial cells or renal interstitial cells and prevent renal interstitial fibrosis.

Protective effects of Chishaogancaochongji on chemical liver injury induced by D-galactosamine in mice

WANG Di-sheng, GAO Ji-jun, ZHANG Cheng-guang, XIANG Lei, YANG Qing-yang, XIN Ya-qun, CEN De-yi<, DONG Liu-yi<, CHEN Zhi-wu<

2006, 11(9):  1026-1029. 

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AIM: To investigate the effects of Chishaoganaochongji D-galactosamine-induced liver injury in mice.METHODS: The chemical-associated liver injury in mouse was induced made by administration of DGalN.The serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) level, and malondiadehyde(MDA) and nitric oxide (NO) level in liver homogenate were assayed by chemochromometry.RESULTS: Chishaogancaochongji (200, 400, 800 mg·kg^-1)was able to decrease levels of serum transaminases (ALT,AST) , liver index and thymus index significantly.Furthermore,Chishaogancaochongji also decreased MDA content and NO level in liver homogenate.CONCLUSION: Chishaogancaochongji has protective effect on chemicalassociatedliver injury in mice.

Effect of Bacille Calmette Guerin inoculation with or without IFN-γ/Vit A on immunologic status of infant with bronchiolitis

LIU Ya-li, YANG Xi-qiang<

2006, 11(9):  1030-1034. 

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AIM: To discuss the effects of Bacille Calmette Guerin (BCG) inoculation with or without supplement of vitamin A/IFN-γon tubercle bacillus protein purified derivative (PPD) skin test, wheezing episode and in vitro the cytokine levels of peripheral blood mononuclear cells (PBMC) in infants with acute bronchiolitis.METHODS: 44 acute bronchiolitis infants (ABI) were treated with BCG alone or BCG combined with Vitamin A/IFN-γ.19 ABI treated without BCG as control.PPD skin test, in vitro production of IL-10 、IL-12 、IL-18 、IL-4 and IFN-γby supernatant of PBMC of bronchiolitis measured by ELISA, and expression of lymphocyte activation gene-3 (LAG-3) mRNA from PBMC of bronchiolitis measured by semi-quantitative RT-PCR were observed before and 3 months after BCG inoculation.Follow upfor average 12 months was to observe thewheezing episodes.RESULTS: The diameters of PPD skin test in ABI after BCG inoculation combined with IFN-γ/VitA were larger than those of ABI before inoculation and control group.The frequencies and persistence of wheezing were lower in interfered infants with acute bronchiolitis either by BCG alone or BCG combined with IFN-γ/VitA than those of control groupby 1 year.IL-12 、IL-18 and IFN-γactivities in ABI treated with BCG or BCG combined with IFN-γ/Vitamin A in vitro were higher than those of pre-treatment bronchiolitis infants;the level of IL-4 was lower;the level of IL-10 was a little bit lower, and expression of LAG-3 mRNA was stronger.Frequency of wheezing episode in 1 year in acute bronchiolitis infants with BCG or BCG combined with IFN-γ/Vitamin A was lower than that of control group.There were no difference between ABIwith BCG or BCG combined with IFN-γ/Vitamin A.Clinical manifestation and the level of cytokines do not show superiority in BCG with IFN-γ/Vitamin A.CONCLUSION: BCG inoculation is able to enhance PPD skin test response,promote Th1 reactivity, and prevent from recurrent wheezing after acute bronchiolitis.The level of IL-10 was degraded lightly after BCG intervention, presumably concerning with regular T cells(CD4 +CD25 +Tr) induced by BCG inoculation.

Anti-apoptotic effects of carvedilol enantiomers in cardiac myocytes

LIU Xiao-ying, YANG Min, LIN Qiu-xiong, YU Xi-yong, SHAN Zhi-xin, ZHENG Meng, LIN Shuguang

2006, 11(9):  1035-1038. 

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AIM: To investigate the anti-apoptotic effects of R (+) and S (-) enantiomers of carvedilol in cardiac myocytes.METHODS: H9C2-1 cardiac myocytes were induced to apoptosis by isopropylarterenol(ISO) for 12 h, R (+) carvedilol or S (-) carvedilol was added as the treatment with 2 μmol·L^-1 or 10μmol·L^-1 dose.Apoptotic cells were identified by Hoechst 33258, and for the determination of apoptosis ratio,Annexin Ⅴ-FITC/ PI double-staining assay was applied with the flow cytometer.The apoptotic effect of 10 μmol R (+) (carvedilol) or S (-) carvedilol alone on cell was also measured.RESULTS: 2 mmol·L^-1 ISO induced a apoptosis in a great quantity of H9C2-1 cells (p<0.01) , and R (+) (carvedilol) or S (-) carvedilol could decreased the apoptotic ratio markedly(p<0.01).The late stage and total apoptotic ratios of 2 μmol·L^-1 R(+) carvedilol +ISO were lower than those of 2 μmol S (-) carvedilol +ISO group(p<0.05) ,but there is no significant difference between 10 μmol·L^-1 group.The apoptotic ratio of 10 μmol·L^-1 S(-) carvedilol itself was a little higher than that of control but was much lower than that of ISO groups (p<0.05).CONCLUSION: Both R (+) (carvedilol) and S (-) carvedilol can effectively inhibit the apoptosis of H9C2-1 cardiac myoctytes induced by ISO, and there is stereoselective difference in it's anti-apoptotic activity on cardiac myocytes between these two enantiomers.R(+) carvedilol is more potential to antagonize the cell apoptosis.

Effects of compound salvia miltiorrhiza injection on lung injury after cardiopulmonary bypass in rats

ZHANG Pi-xing, LIN Li-li

2006, 11(9):  1039-1042. 

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AIM: To investigate the effects of compound salvia miltiorrhiza (SM) injection on lung injury after cardiopulmonary bypass (CPB).METHODS: Twenty-four rats were randomly divided into control group, CPB groupand SM group.Cardiopulmonary bypass was made in rats of CPB groupand SM group.Lung tissues of all rats were taken 60 min after the weaning of CPB for the assay of malondialdehyde (MDA) , myeloperoxidase(MPO) , water content of tissue, the observation of pathological changes were made under optical microscope.RESULTS: Remarkable pathohistological and biochemical changes were detected 1 h after CPB.Compared with control group, MDA in lung tissue were increased in CPB groupand SM group(p<0.05) , but MDA in SM groupwas lower than that in CPB group(P<0.05).Similarly, the level of MPO and water content were increased markedly compared with control groupand SM group(p<0.05).Accordingly , swelling and infiltration of leucocyte were found in lung tissue of CPB groupunder an optical microscope.These pathohistological damages caused by CPB were greatly attenuated in SM group.CONCLUSION: CPB-related lung injury can be reduced by compound salvia miltiorrhiza injection which has free radical scavenging and neutrophil infiltration relieving activities.

Bioequivalence of Metoprolol Tartrate Tablets in healthy volunteers

WANG Jing, FU Liang-qing, GUAN Yong-biao<, FANG Yi<, LIU Ze-yuan

2006, 11(9):  1043-1047. 

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AIM: To study the bioequivalence of domestic and imported Metoprolol Tartrate Tablets in Chinese healthy volunteers.METHODS: According to the rule published by SFDA , the serum concentration of 20 selected volunteers among 18 to 40 years old was determined by HPLC-fluorescence detection after giving domestic and imported Metoprolol Tartrate Tablets 0.1g , and the pharmacokinetic parameters were calculated by DAS software.RESULTS: The method of HPLC-fluorescence detection to study the pharmakokinetics of Metoprolol Tartrate was sensitive , reliable , accurate and reasonable.The main pharmakokinetics parameters of domestic and imported Metoprolol Tartrate Tablets were Tmax:1.11 ±0.36 h and 1.39 ±0.65 h respectively;Cmax:269.20±87.15 μg·L-1 and 262.03 ±75.52 μg·L-1 respectively;AUC0 -12h:1088.91 ±510.52 μg·L-1·h and1098.29 ±5 55.14 μg·L-1·h respectively.The relative bioavailability of domestic Metoprolol Tartrate Tablets was 100.09 %.CONCLUSION: The domestic and imported Metoprolol Tartrate Tablets was bioequivalents.

Inhibitory effects of elemene on proliferation of lens epithelial cell in vitro

HUANG Xiu-rong, QI Ming-xin<, HU Yan-hong<, YAN Jing, WU Zheng-zheng, MA Lan<

2006, 11(9):  1048-1051. 

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AIM: To investigate the inhibitory effects of elemene (Ele) on proliferation of lens epithelial cell (LEC) induced by recombinant human epidermal growth factor (rhEGF) and the relationshipbetween dose-effect and time-effect, in order to pursue effective method of prevention and treatment for after cataract.METHODS: The inhibitory effects of different concentrations of Ele on proliferation of bovine LEC induced by rhEGF were detected by cell activities via methyl thiazolyl tetrazolium(MTT) and expression of proliferating cell nuclear antigen(PCNA) via flow cytometer (FCM).Meanwhile, the relationshipbetween time and effect was observed.RESULTS: The inhibitory rates of LEC proliferation were increased in a dose-dependent manner (p<0.01) after LEC incubated with low, middle, high concentrations of Ele for 24 h;The inhibitory rates of LEC proliferation were increased in a time-dependent manner (p<0.01)after LEC incubated with middle concentrations of Ele for 6, 12, 24, 48 and 72 h.Ele can down-regulate expression of PCNA.Expression rates of PCNA were decreased in a dose-dependent manner (p<0.01) after LEC incubated with low, middle, high concentrations of Ele for 24 h;The expression rates of PCNA were decreased in a time-dependent manner (p<0.01) after LEC incubated with middle concentrations of Ele for 6, 12, 24, 48 and 72 h.CONCLUSION: Elemene can effectively inhibit LEC proliferation induced by rhEGF.There are broad prospects for prevention and treatment of after cataract.

Study of realgar induced apoptosis of eosinophils from bronchoalveolar lavage fluid in asthmatic guinea pigs

XU Ji-de, HUANG Zhi-xiang, YANG Shao-wei, WEN Zhong-hui, ZENG Rui-fang

2006, 11(9):  1052-1055. 

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AIM: To observe the realgar induced the apoptosis of eosinophils from bronchoalveolar lavage fluid in asthmatic guinea pigs and investigate the mechanism that realgar treated asthma.METHODS: The morphology of apoptosis of eosinophils was observed by Giemsa staining and electron microscope.The rate of apoptosis of eosinophils was assayed by the flow cytometry.RESULTS: The characteristic changes of the apoptosis in both light microscope and electron microscope were shown after 6 hours treatment of realgar.Flow cytometry showed that the rate of apoptosis of the eosinophils was increased with both increasing realgar concentration and prolonging realgar action time to the cells.CONCLUSION: Realgar promotes the apoptosis of eosinophils from bronchoalveolar lavage fluid in asthmatic guinea pig.Realgar induced the apoptosis of eosinophils is one of the causeses for asthmatic treatment.

Protective effect of omeprazole, Talcid and misoprostol on acute gastricmucosa lesion

LIU Jing, LI Zhao-shen, XU Guo-ming

2006, 11(9):  1056-1059. 

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AIM: To investigate the protective effect of antiulcer agents omeprazole, misoprostol and Talcid on the acute gastric mucosa lesion.METHODS: Water immersion-restraint stress model were performed with SD rats.Mucosa lesion was evaluated by ulcer index.Apoptosis cells in gastric mucosa were measured by terminal deoxynucleatidyl transferase mediared dUTpnick and labelling(TUNEL) techniques, while expression of inducible NO synthase (iNOS) was detected by immunohistochemical staining and CX43 by In situ hyberdization.RESULTS: Compared with control group, the groups of pretreatment with Omeprazole, Misoprostol and Talcid showed a significant reduction of damaged mucosa and epithelial cell apoptosis, the effects of Omeprazole and Misoprostol were better than Talcid.Three antiulcer agents decreased iNOS expression and increased CX43 expression,the effect of Misoprostol and Talcid was better than Omeprazole.CONCLUSION: Omeprazole, misoprostol and Talcid can exert the protective effect to counter the acute gastric mucosa lesion with different mechanism.

Determination of loratadine in human plasma by LC-MS and its pharmacokinetic studies

YUAN Gui-yan, GUO Rui-chen, WANG Ben-jie, LIU Hui

2006, 11(9):  1060-1064. 

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AIM: To establish an LC-MS method for determining the concentrations of loratadine (LOR)in human plasma and to evaluate its pharmacokinetic characteristics.METHODS: A ZORBAX Eclipse XDB-C8 (5μm , 150 mm ×4.6 mm)column was used , atmospheric pressure electronic spray ionization (AP-ESI) and ion mass spectrum (m/z)of 388.2 (M+H)⁺were selected to quantify LOR , and 275.1 (M +H)⁺for ropivacaine(internal standard , IS).RESULTS: The linear range of LOR standard curve was 0.5 -50 ng·ml^-1 , and the determination limit was 0.5 ng·ml^-1.The pharmacokinetic parameters of LOR after a single dose of 20 mg tablet(T1), capsule (T2)and reference (R)were as follows ,the half life (t_1/2)13.52 ±1.35 , 13.14 ±0.98 and 14.00 ±1.25 h , the time to peak concentration (Tmax) 1.24 ±0.06 , 1.18 ±0.12 and 1.17 ±0.12 h , the peak concentration (Cmax)21.72 ±7.70 , 21.49 ±8.34 and 20.50 ±8.65 ng·ml^-1 , the area under time-concentration curve (AUC_{0 -48} and AUC_{0 -∞})137.24 ±47.84 and 146.61 ±51.03 ng·ml^-1·h , 139.65 ±45.69 and 148.04 ±48.10 ng·ml^-1·h , 134.19 ±49.03 and 143.70 ±52.08 ng·ml^-1·h , the relative bioavailability of LOR tablet and capsule were (105.49 ±8.08)% and(102.90 ±10.02)%, respectively.CONCLUSION: The LC-MS method for determining the concentration of LOR in human plasma is sensitive and accurate and can be used for LOR bioavailability and pharmacokinetic studies.LOR tests and reference are bioequivalent.

Effects of insulin treatment on content of intramyocellular triglyceride and expression of CPTI-βgene in skeletal muscle of diabetic mellitus rats

WU Qian, CHEN Lu-lu, WANG Bao-ping, WEI Cui-feng, ZHOU Min, LI Yan

2006, 11(9):  1065-1068. 

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AIM: To study the effect of insulin administration on the content of triglyceride and the expression of carnitine palmitoyl transferase I-β(CPTI-β) gene in skeletal muscle of diabetic mellitus (DM) rats. METHEDS: Wistar rats were randomly divided into normal control group(NC, n =10) , diabetes with high fat diet (DH, n =10) , and diabetes with high fat diet plus insulin therapy (DHI, n =10).The fasting plasma glucose(FPG) , insulin (FPI) , free fatty acids (FFAs) ,triglyceride (TG) and the TGm (intramyocellular triglyceride) and the expression of CPTI-βgene in skeletal muscle were measured.HOMA2-IR was computed on the basis of FPI and FPG.RESULTES: Compared with NC group, HOMA2-IR, TG and FFAs levels in the plasma and TGm contents of DH groupwere significantly higher (p<0.01) , and the expression of CPTI-βgene was decreased (p<0.01).Compared with DH group, insulin administration didn't normalize TG (p>0.05) , but FFAs were decreased (p<0.01) , and TGm were increased (p<0.01) , although it improved insulin sensitivity of DHI group(p<0.05) , and the expression of CPTI-βwere increased (p<0.01).CONCLUSION: TG is accumulated in the skeletal muscle of DM rats, and the expression of CPTI-βis decreased, too.Insulin administration is able to up-regulate CPTI-βtranscription, although it can increase the content of TGm as well.This phenomenon suggests insulin can ameliorate triglyceride metabolize in the DM rats.

Protective properties of colloidal bismuth subcitrate on gastric mucosa

GAO Li-zhong<, CHEN Ding-ding, CHAO Jie, DING Qiang-jun

2006, 11(9):  1069-1072. 

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AIM: Explore the relationshipbetween the protection of CBS on gastric mucosa and the effect of CBS on gastric mucosal NO content and NOS activity.METHODS: The mucosal injury was induced by ethanol n rat and then treated with CBS.NO content and NOS activity were determined by benzidine-fluorescence spectrophotometer.RESULTS: CBS was applied intragastricly, which significantly reduced the area of gastric ulcer and inhibit iNOS activity.As a result, the NO level was reduced to normal.When CBS was applied intraperitoneally,the NO level of gastric mucosa as well as iNOS activity was reduced, and cNOS activity was increased.In Vitro experiment showed that CBS inhibited NOS activity significantly.CONCLUSION: CBS inhibits the increased iNOS activity and NO level, which may be an underlying biochemical mechanism for its protective on gastric mucosa.

Analysis of multivariate of time-to-even in clinical trial

SU Xia<, QIAN Guo-hua<, XUN Peng-cheng<, YU Hao<, LANG Su-ping<, CHEN Feng<

2006, 11(9):  1073-1077. 

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This paper discussed the analysis of multivariate of time to even (TTE) or survival-time data.It introduces the principle of PWpmodel and the applied technique of PWpmodel in dealing with the actual multivariate survival-time data.The results show that this method is good at dealing with multivariate outcome event, and it can obtain the effect of concomitant variable to the different outcome events to limit the parametric value of the model.PWpmodel is an efficient analytical method for dealing with multivariate survival-time data.

Progress in abnormal toxicity safety test about the quality standard of drugs

ZHANG Rui, LI Zhan-jun

2006, 11(9):  1078-1080. 

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To discuss about the question and development of abnormal toxicity safety test in control of biochemical drugs.It would be referred to revise quality standard of drugs.