Table of Content

Volume 11 Issue 3
26 March 2006

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Applications of antisense oligonucleotides in cardicvascular disease

2006, 11(3):  241-245. 

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Antisense oligonucleotides is applicated abroadly in cardiovascular disease.It aims at the target genes involved in molecule mechanisms of disease pathogenesis.This technology reveals good foreground as a kind of clinical drug because of its researchful and therapeutic function in hypertension 、coronary disease,complications of heart transplantation and failure.

Progress in study of methodology of spontaneous locomotor activity in rats,pigs and monkeys

2006, 11(3):  246-250. 

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Spontaneous locomotor activity is a widely used evaluation method in safety pharmacology of central nerve system and investigation of neuroscience.Spontaneous locomotor activity test is an important method that can investigate several animals' species and their associated indexes of spontaneous locomotor activity;it can also provide parameters for several pharmacological objectives including safety pharmacology of central nerve system.The new developed equipments and methods have many merits.This paper reviews the progress of methodology of spontaneous locomotor activity test in rats,pigs and monkeys.

Effects and mechanisms of U50488H on ventricular arrhythmias induced by myocardial ischemia and reperfusion in rats

2006, 11(3):  251-255. 

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AIM: To investigate the effects and mechanisms of U50488H (a selectiveк-opioid receptor agonist)on ventricular arrhythmias induced by myocardial ischemia and reperfusion in rats.METHODS: Rats were randomly divided into different groups respectively.Heart rate (HR),arterial blood pressure (ABP),left ventricular pressure (LVP),contractive function (+dp/dt_max) and diastolic function (-dp/dt_max) were examined in rats,the incidence of ventricular arrhythmias,arrhythmia score and mechanisms were studied.RESULTS: HR,ABP,LVPand±dp/dt_max in rats were decreased with the administration of U50488H;U50488H intravenously injected before I/R,the incidence of ventricular arrhythmias and arrhythmia score were lowered (P<0.05).The effect of U50488H was abolished in the presence of Nor-BNI,a selectiveк-opioid receptor antagonist.Compared with U50488H +I/R group,with the administration of pertussis toxin,glibenclamide and chelerythrine in advance to block the effects of Gi protein,nitrogen oxide synthase,KATPand PKC respectively,the anti-arrhythmic effects induced byκ-opioid receptor in the rats subjected to myocardial ischemia/reperfusion injures were attenuated (P<0.01).While with the disposal of genistein (5 mg·kg^-1,30 min before U50488H) in advance to block TK,no influence was observed on the anti-arrhythmic effects induced byκ-opioid receptor (P>0.05).CONCLUSIONS: κ-opioid receptor stimulation by U50488H elicits the effects of anti-arrhythmia induced by myocardial ischemia and reperfusion.With the administration of pertussis toxin,glibenclamide and chelerythrine to block Gi/o,PKC and KATPrespectively in advance,the anti-arrhythmic effects mediated byκ-opioid receptor are weakened or completely abolished (P<0.01) which indicates that Gi/o,PKC and K_ATP are signal transduction ways ofκ-opioid receptor activiation.

Pharmacokinetic study of ginsenoside 20(R)-Rh₂ in Beagle dogs by LCESI-MS

2006, 11(3):  256-260. 

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AIM: To establish an LC-ESI-MS method for determination of ginsenoside 20(R)-Rh₂ and investigate its application to pharmacokinetic and absolute bioavailability study in Beagle dogs.METHODS: According to a randomized two-period crossover design,beagle dogs were given 1 and 0.1mg·kg^-1 20(R)-Rh₂ via po and ivrespectively.Drug plasma concentration was determined by LC-ESI-MS.Pharmacokinetic parameters were evaluated and absolute bioavailability was also calculated.RESULTS: The method was linear over the range of 0.5-200ng·ml^-1 (R₂=0.9998);The recovery of 20(R)-Rh₂ in dog plasma was more than 70%;Intra- and interbatch precision,expressed as the relative standard (RSD) was less than 15%;After iv administration of 20 (R)-Rh₂,the main pharmacokinetic parameters T_1/2,CL,AUC_0-∞ were 8.0±2.8h,0.1±0.03L·kg^-1·h^-1,857.0±209.6ng·h·ml^-1 respectively;after po administration,the major pharmacokinetic parameters T_max,C_max,T_1/2,AUC_0-∞ were 2.6±1.3 h,371.0±199.6ng·ml^-1,5.8±2.6 h,1215.7±598.6ng·h·ml^-1 respectively.The absolute bioavailability was 16.1%±11.3% after the correction of dosage.CONCLUSION: The method described in this report was sensitive and specific,and suitable for pharmacokinetic studies of 20(R)-Rh₂ in dog.The absolute bioavailability of 20(R)-Rh₂ in dog was relative low.

Affinity and selectivity of darusentan for rat endothelin receptors and effects of once iv administration of darusentan on hypoxia-induced pulmonary hypertensive in rats

2006, 11(3):  261-265. 

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AIM: To investigate the affinity and selectivity of endothelin antagonist darusentan on the ET_A and ET_B receptor of rat left ventricle and its effect on the hemodynamic parameters in hypoxia-induced pulmonary hypertensive rat.METHODS: Radio receptor binding assay method was used to determine the competition binding of darusentan.Pulmonary hypertensive rats were induced by hypoxia.A multiple physiological recorder was used to record the hemodynamic parameters.RESULTS: The competition binding of¹²⁵ I-ET1 to ETR at darusentan 0.1μmol·L^-1 presence was 31.50%±7.7%.The IC₅₀ to suppress ETA and ETB of darusentan was 1.93±0.21and 147±20μmol·L^-1.It was 76.16 fold of selectivity for the ET_A receptor over the ET_B receptor.By 28 d of exposure to hypoxia,rats had already developed significant pulmonary hypertension as estimated by increased right ventricle systolic pressure (RVSP),right ventricle end diastolic pressure (RVEDP),right ventricle +dp/dtmax and-dp/dt min.Once treatment with darusentan by ivinjection,pulmonary hypertensive changes were significantly reducad in the right ventricle.CONCLUSION: Darusentan has significantly antagonistic effects on the left ventricle membrane and has high selectivity for ETAR.It effectively ameliorates the hemodynamic parameters in hypoxia-induced pulmonary hypertensive rats.

Changes of plasma vascular active substances in dog circulation failures induced by cholinesterase inhibitor sarin and therapeutic effects of antidotal treatment

2006, 11(3):  266-269. 

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AIM: To investigate the changes of plasma vascular active substances before and after treatment with neuronal nicotinic receptor antagonist mecamylamine or muscarinic receptor antagonist atropine against the circulation failures induced by the cholinesterase inhibitort sarin in dogs.METHODS: Twenty healthy adult male dogs,weighing 12-15 kg,were divided into four groups randomly:control;treatment with mecamylamine;treatment with atropine and treatment with mecamylamine and atropine at the dose ratio of 1∶10(n=5).Animals were given intramuscularly sarin,and when the mean blood pressure(MBP) was decreased to 40-45 mmHg,the drugs were intramuscularly injected and the changes of vascular active substances such as nitric oxide (NO),PGI₂,atrial natriuretic peptide (ANP),endothelin (ET),angiotensinⅡ(AngⅡ) and TXA₂ before and after treated 15,30 and 60 min were observed.RESULTS: In anesthetized dogs intoxicated with cholinesterase inhibitor sarin,the plasma vascular active substances NO,PGI₂,ANP,ET,AngⅡand TXA₂ were increased significantly.After treated with mecamylamine and atropine 15 min,all the six vascular active substances were decreased markedly.After treated 60 min,they were almost resumed to the normal levels.The therapeutic effects of combination of mecamylamine and atropine were much better than those of mecamylamine or atropine used separately.CONCLUSION: The levels of vascular active substances NO,PGI₂,ANP,ET,AngⅡand TXA₂ in plasma can reflect the severity of circulation failure.There were synergic effects between mecamylamine and atropine against circulation failures induced by sarin.

Study on pharmacokinetics and bioavailability of granisetron nasal spray in beagles

2006, 11(3):  270-272. 

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AIM: To study the bioavailability of granisetron nasal spray in beagles.METHODS: A single 2 mg dose of granisetron tablet or nasal spray was given to beagles in a randomized crossover design.The drug plasma concentrations were determined by HPLC fluorescence method using bisoprolol fumarate as internal standard.RESULTS: The pharmacokinetic parameters of granisetron tablet and nasal spray were as follow:tmax were 1.50±0.41 and 0.31±0.13 h,C_max were 6.45±1.15 and 11.93±1.33ng·ml^-1,AUC_0-12 were 25.14±3.75 and 27.76±3.46ng·h·ml^-1,AUC_0-∞ were 28.46±4.17and 31.46±3.43ng·h·ml^-1,respectively.The mean relative bioavailability of nasal spray vs tablet was(111.88±18.94)%.CONCLUSION: Granisetron nasal spray is readily absorbed and owns better bioavailability than the tablet.

Effects of breviscapin on isoproterenol-induced myocardial hypertrophy in mice

2006, 11(3):  273-276. 

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AIM: To investigate effects of Breviscapin on isoproterenol- inducedmyocardial hypertrophy in mice.METHODS: Isoproterenol was given subcutaneously (3mg·kg^-1,5 days) to induce myocardial hypertrophy in mice.Therapy grouPwere given Breviscapin 30 minutes before ISO treatment.We investigated the cardiac weight index and the malonyldialdehyde (MDA) content,the activity of superoxide dismutase(SOD),Ca²⁺-Mg²⁺-ATPase in myocardium and aspartate aminotransferase (AST) in serum,Myocardiac morphological alteration was observed by micrography.RESULTS: In cardiac hypertrophy model group,HW/BW,LVW/BW (the ratio of whole heart weight to body weight and left ventricle weight to body weight),and cardiac MDA,serum AST content were increased,the activity of SOD and Ca^{2 +}-Mg²⁺-ATPase were decreased compared with control.Breviscapin improved all the above parameters significantly and improved the left ventricular tissue morphological alteration.CONCLUSION: Breviscapine possess protective effects against Isoproterenol induced myocardial hypertrophy in mice.This may be related to reducing the oxidative stress and improving energy metabolism.

Expression and significance of TNFSF13B in experimental autoimmune myocarditis

2006, 11(3):  277-281. 

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AIM: To investigate the expression and significance of TNFSF13B in the experimental autoimmune myocarditis.METHODS: Immunize genetically predisposed BABL/c mice were with peptide containing myocarditogenic epitope covered by complete freund' s adjuvant(CFA) on 1st and 8th day,to establish the model of experimental autoimmune myocarditis.Hearts and serum of experimental and control mice were harvested on the 14th and 21st day after the first immunization.Histopathological changes of myocardium were detected by HE pigmentation.Expression of TNFSF13B in myocardium was measured by immunohistochemistry,and the computer aided video system was used to analysis and compare the positive expression rates of TNFSF13B in different groups.Titer of myosin-specific autoantibody was measured by ELISA.RESULT: Inflammation was emerged in the myocardium of fifteen experimental mice on 14th day after the first immunization.On 21st day after the first immunization,inflammation was detected in the myocardium of seventeen experimental mice,and the inflammation was more serious than on 14th day after the first immunization,but no inflammation was emerged in the myocardium of control mice.Expression of TNFSF13B was detected in myocardium of experimental autoimmune myocarditis remarkably,but was not detected in normal myocardium.High titer of myosin-specific autoantibody was detected in serum of mice with myocarditis.CONCLUSION: TNFSF13B play a role in the occurrence and development of autoimmune myocarditis.

Effect of safflower on renal interstitial fibrosis and renal function in rats

2006, 11(3):  282-285. 

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AIM: To research the effect of safflower in renal intertistial fibrosis by GFR and renal biopsypathology with Sprague-Dnwley(SD) rat model.METHODS: All rats were distributed into 6 groups.GrouPA was normal control,grouPB received sham operation,grouPC was vehicle control,grouPD received vehicle,grouPE received safflower(10 g·kg^-1 body wt·d^-1),and grouPFreceived enalapril (12.5 mg·kg^-1 body wt·d^-1).Rats underwent reversible left renal vein obstruction for 6 d,after which the obstruction was relieved.Renal function was determined by measuring GFR with inulin clearances.Both renal tubular epithelial cells(RTECs) and fibronection deposition for renal interstitial fibrosis were identified by immunohistochemistry.The positive and negative areas of per slice was determined by a motic medical 6.0 graphical analytical system.Atrophic tubules were determined by measuring the tubule diameter.10 fields per slice were analyzed at×400 magnification.RESULTS:Return of glomerular filtration rate(GFR) was seen in grouPE and gouPF,which was significantly better than grouPD(P<0.05).Atrophic tubules and fibronection deposition were found except in grouPA and groupB,but grouPD was worse significantly than grouPE and grouPF(P<0.05).The proportionalit of positive areas of RTECs recovered more significantly in grouPE and grouPF than grouPD(P<0.05).CONCLUSION: Safflowei can return renal function and postpone the development of chronic kidney disease by preventing renal interstitial fibrosis.

Inhibition on liver carcinoma cells HepG₂ by Se-methylselenocysteine

2006, 11(3):  286-291. 

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AIM: To study the effects of Se-methylselenocysteine(MSC) on the growth and apoptosis of human liver carcinoma cell line,HepG₂ cells and the molecular mechanism of effects.METHODS: After HepG₂ cells treated with various concentrations of MSC,survival and apoptosis were determined by MTT assay and light microscope,apoptosis and cell cycle were determined by flow cytometry.Malignant phenotype was determined by soft agarose growth assay.Cyclin D1 mRNA expression was determined by RT-PCR and Caspase-3 activity was measured by Caspase-3 activity assay kit.RESULTS: After being treated with 25 μmol·L^-1 MSC for 24 h,the survival of HepG₂ cells was decreased,a marked apoptosis and S phase arrest characteristic was observed in timeand dose- dependent manner.Soft agatose growth assay showed MSC inhibited HepG₂ cells growth in soft agarose.RT-PCR and Caspase-3 assay showed that HepG₂ cells treated with 25 μmol·L^-1 MSC for 24 and 48 hours,the expression of Cyclin D1 mRNA was down-regulated by 38% and 47%,while Caspase-3 activity was up-regulat-ed by (39.61±6.65)%and (118.73±6.48)%.Hep-G2 cells treated with 50 μmol·L^-1 MSC for 24 and 48 h,the expression of Cyclin D1 mRNA was down-regulated by 53% and 82%,whereas Caspase-3 activity was up-regulated by (80.66±9.31)% and (152.67±7.95)%.CONCLUSION: MSC can inhibit the growth of HepG₂ cells,and induce apoptosis and S phase arrest of HepG₂ cells.The phenotype alterations of HepG₂ cells might relate with inhibition of Cyclin D1 expression and Caspase-3activity by MSC in the cells.

Study on metabolites of scutellarin in gastrointestinal tract by UPLC-MS/MS method

2006, 11(3):  292-295. 

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AIM: The metabolites of scutellarin were studied in gastrointestinal tract.METHODS: Scutellarin was hydrolyzed with hydrochloric acid andβ-glucuronidase.Human intestinal flora and scutellarin were incubated in vitro.The metabolites were identified by UPLC-MS/MS method.RESULTS: Scutellarin could be hydrolyzed with hydrochloric acid andβ-glucuronidase,and could be metabolized by human intestinal bacteria.A main metabolite,scutellarein,also was found in the plasma of healthy volunteers after oral administration.CONCLUSION: There were scutellarin and scutellarein in intestinal before absorption.It was suitable for scutellarin pharmacokinetic studies to determine scutellarein or total aglycone.

Effect of pantoprazole on Cytochrome P4501A2, N-acetyltransferase2,and xanthine oxidase activity in human

2006, 11(3):  296-299. 

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AIM: To investigate the effect of pantoprazole on Cytochrome P4501A2 (CYP1A2),N-acetyltransferase2(NAT2),and xanthine oxidase(XO) activity in human and to forecast the drug-drug interaction with it,so as to instruct clinician to prescribe rationally.METHODS: In thirty volunteers,use two-way cross design,caffeine was used as a metabolic probe for CYP1A2 、NAT2,and XO,before and after pantoprazole administration,urine samples were collected.The contents of five major metabolites of caffeine in the urine were determined by RP-HPLC method and then evaluated the activity change of CYP1A2 、NAT2,and XO by the ratio of metabolites of caffeine.RESULTS: It was found that the average activity of CYP1A2 、NAT2,and XO were 3.37±1.22,0.50±0.09,0.49±0.09 with before treatment,and 7 days after treatment,the average activity of CYP1A2 、NAT2,and XO were 3.50±1.23,0.48±0.12,0.48±0.13.There were no statistical significance between before treatment and after treatmen(P>0.05).CONCLUSIONS: Pantoprazole have no influence on CYP1A2 、NAT2,and XO,so pantoprazole do not modify the efficacy of drugs which metabolized by CYP1A2 、NAT2,and XO taken simultaneously.

Genetic Polymorphism of human CYP3A4 gene in population of Han nationality in China

2006, 11(3):  300-304. 

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AIM: To investigate the distribution of cytochrome P450 3A4 (CYP3A4) genetic polymorphism in population of Han nationality of mainland in China.METHODS: Genomic DNA was extracted from 140 mainland Chinese peripheral blood,then polymerase chain reaction-single strand conformation polymorphism (PCRSSCP)combined with silver staining and DNA sequencing were used to detect mutations in CYP3A4 gene.RESULTS: In the population,a novel mutation in intron 2 of CYP3A4 gene was detected in 31 out of 140 persons.The frequency of intronic mutation in CYP3A4 gene was 22.1%.No mutation was found either in 5′proximal regulating region or in 13 exons of CYP3A4 gene.CONCLUSION: There is a novel mutant allele in CYP3A4 gene in population of Han nationality of mainland in China.It is different from those in other ethnic groups.

Effects of Raphanus sativus roots on gastrointestinal stimulatory activity

2006, 11(3):  305-308. 

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AIM: To explore the effects of the extract of Raphanus sativus roots (Er)on gastrointestinal stimulatory activity and its possible mechanism.METHODS: After Er were administrated orally,the remaining rate of substance in stomach,the distance of charcoal meal in intestines was measured.The samples of isolated ileum segment from guinea pigs were prepared,then the contraction intensity and frequency of the smooth muscle were measured pre-and post treatment of Er.RESULTS: The crude extract(Ecr),the petroleum spirit(Ept),chloroform(Ecl)and aqueous(Eaq)fractions of Raphanus sativus roots all showed dose-dependent spasmogenicity in guineapig ileum,and could abolished by pyrilamin,the crude extract being more potent.The Er could significantly improve gastric emptying,and it also could enhance the transit of charcoal meal in mice at 30-100 mg·kg^-1.CONCLUSION: The extract of Raphanus sativus roots demonstrated spasmogenic effect on gastrointestinal tract,and this effect may through activating histaminergic (H₁)receptor.

Discussion about effect of high glucose environ on vascular endothelial cells in earlier period

2006, 11(3):  309-313. 

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AIM: To discuss the influence of high glucose on the proliferation and ICAM-1 expression of human umbilical vein endothelial cells(HUVEC) within 48h and to observe the altered effect of high glucose when high glucose and inflammatory stimulator exist at the same time.METHODS: HUVEC were cultured with different concentrations of glucose.The proliferation of HUVEC induced by high glucose was detected by MTT assay.The ICAM-1expression of HUVEC induced by high glucose was assayed by flow cytometry and cell ELISA.The difference of ICAM-1 expression between induced by LPS and by LPS together with high glucose was compared.RESULTS: 25 、45 mmol·L^-1 glucose did not inhibit the proliferation of HUVEC within 48 h,and they also had no effect on the expression of ICAM-1.However,when stimulated HUVEC with LPS,the proliferation of HUVEC was extremely inhibited in high glucose groups,and the expression of ICAM-1 increased significantly in those groups.CONCLUSION: In short time,high glucose has no effect on the proliferation and ICAM-1 expression of HUVEC,but when inflammatory stimulation exists,high glucose can inhibit the proliferation and increase the expression of adhesion molecules.

Effect of Pinaverium Bromide on different layers and segments of colonic smooth muscle strips in wrap restraint stress rats

2006, 11(3):  314-318. 

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AIM: To evaluate effects of Pinaverium Bromide on different segments and layers of colonic smooth muscle in wraPrestraint stress (WRS) rats and explore its possible therapeutic mechanism on different types of irritable bowel syndrome (IBS).METHODS: Adult SD rats were randomly divided into model group(wraPrestraint stress group) and control group.Colonic smooth muscle strips were made from different segments and layers in two groups.The spontaneous contraction activities of colonic longitudinal/circular muscle (LM/CM)strips of rats were observed with organ bath system before and after addition of series concentrations of pinaverium.RESULTS: Pinaverium Bromide caused concentrationdependent inhibition of colonic smooth muscle,the inhibitory effect of pinaverium in model grouPwas significantly stronger than that in control group(proximal colon:28.54±4.82 vs 7.48±1.65,21.75±1.00 vs 12.56±3.15;distal colon:15.71±5.27 vs 3.89±1.16,20.16±3.16 vs 7.56±1.96) (P<0.05).Compared with that of distal colon,inhibitory effect of pinaverium was significantly higher of proximal colon (P<0.05).For the inhibition of pinaverium,there was no significant difference between LM and CM strips in the same intestinal segments (P>0.05).CONCLUSION: Effects of Pinaverium Bromide on different colonic muscle layers and segments in WRS rats is probably related with its therapeutic mechanism on different types of IBS.

Effects of resveratrol on isolated coronary artery rings of canine

2006, 11(3):  319-323. 

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AIM: To investigate the relaxative characteristicsof resveratrol (RES) and 17β-Estradiol (EST)on coronary arteries in dogs and its mechanism.METHODS: Rings of canine coronary arteries were suspended in organ baths containing Krebs-Henseleit solution,and then isometric tension was measured.RESULTS: Both RES and EST caused the does-response contractile curve of KCl in K-H solution and CaCl₂ in Ca²⁺-free K-H solution shift rightward,and their sensitivies and the values of maximum contractions had been decreased.In the Nω-Lnitro-arginine,Methylene Blue and Sodium Orthovanadate groups,the vasorelaxant effects of both estrogens were markedly attenuated (P<0.01),but there was no change in the grouPof Glibenclamide (P>0.05).CONCLUSION: Resveratrol and 17β-Estradiol relaxe vascular smooth muscle in an endothelium-dependent manner,and are not related to KATPchannel.

Effect of anti-huamn TLR9 antibody on CpG tumor necrosis factor induced tumor necrosis factor-αrelease from human peripheral blood mononuclear cells

2006, 11(3):  324-327. 

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AIM: To observe the role of cell-surface TLR9 during TLR9-mediated signal transduction pathways.METHODS: Using anti-huamn TLR9 antibody to blockade cell-surface TLR9,internalization of CpG oligodeoxynucleotide(ODN) and tumor necrosis factor-α(TNF-α) release in human peripheral blood mononuclear cells (hPBMCs) were investigated.RESULTS: Both of CpG ODN and GpC ODN were endocytosed by the cells,only CpG ODN could induce TNF-αrelease.Addition of chloroquine (CQ),an inhibitor of endosome mature,delayed degradation of both ODN molecules,with no obvious difference between them.Importantly,blockade of cell-surface TLR9 using an anti-hTLR9 antibody did not significantly affect CpG ODN internalization,CpG ODNinduced TNF-αrelease,or CQ-induced inhibition of TNF-αrelease in hPBMCs.CONCLUSION: Cell-surface TLR9 does not directly participate in internalization of CpG ODN or TNF-αrelease from hPBMCs.

Effect of different quantities of carboxymethyl chitosan modification to pharmacokinetic performance of paclitaxel liposome in rats

2006, 11(3):  328-331. 

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AIM: To study the effect of different quantities of carboxymethyl chitosan (CMCT)modification to the pharmacokinetic performance of PTX-LPin rats.METHODS: Plasma was extracted with tert-butyl methyl ether and Norethisterone was employed as internal standard after i.v.unmodified PTX-LP,0.1%CMCT modified PTX-LPand 0.2%CMCT modified PTX-LPin rats.Plasma samples were analyzed on a C18 column at 227 nm and the mobile phase was methanol and water (65∶35,v/v).RESULTS: The plasma concentration-time profile in rats after iv.unmodified PTX-LP,0.1%CMCT modified PTX-LPand 0.2% CMCT modified PTX-LPfollow bi-exponential disposition.T_1/2β are 11.20,15.55 and 30.6 h respectively,AUC were 2541.99,2748.78 and 3451.64 mg·L^-1·min for each of them.CONCLUSION: Significant changes of in vivo pharmacokinetic performance have been found after CMCT modification to PTX-LPin rats by comparison with unmodified LP.T_1/2βand circulation time in plasma have been lengthened and AUC has been improved in some extent.We found that this kind of long circulating action had some correlation with the quantities of CMCT employed.

Meta-analysis of effectiveness and safety of granisetron for preventing chemotherapy-induced nausea

2006, 11(3):  332-335. 

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AIM: To compare the differences in the effectiveness and safety between granisetron and other drugs for preventing chemotherapy-induced nausea.METHODS: The effectiveness and safety between granisetron and other drugs for preventing chemotherapy-induced nausea were analyzed by Meta-analysis in homogeneity test and combined test.RESULTS: Homogeneity test showed that the cited studies of efficacy and safety were homogeneous withχ²=28.57,χ²=26.19,P>0.05,respectively.In combined test,the combined OR=1.879,OR=0.760 and its 95% confidence interval was in 1.453-2.431,0.122-0.605,respectively.CONCLUSION: The effectiveness of granisetron in treating chemotherapy-induced nausea is significantly superior to those of the medications used at present and the rate of side effects was low.

Study on treatment of simple herpes encephalitis in mice with Salvia miltiorrhiza Bunge

2006, 11(3):  336-338. 

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AIM: To explore the curative effect and mechanism of Salvia miltiorrhiza Bunge (SMB) against mice' s viral encephalitis induced by simple herpes virus-1(HSV-1).METHODS: To establish damage model of viral encephalitis in order to observe the mortality rate of mouse,to test the level change of the factors of cells such as IL-1β,IFN-γ,NO and to observe the structural change in neural cells under the electron microscope.RESULTS: Cells swelled,nucleoli pyknosised and the structure of nucleus was damaged after been inoculated with HSV-1 under the electron microscope.There was hollow-like change in mitochondria and virus-like pellet in nucleus,spine was damaged,the levels of IL-1β,IFN-γ,NO and the death rate obviously increased in model group,and those indexes decreased after treating with SMB except IFN-γ.CONCLUSION: Early treated with SMB has certain clinical curative effect.It may result from regulating immune response in the body.

Determination of high molecular weight impurities in Cephradine Capsule by gel filtration chromatography

2006, 11(3):  339-341. 

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AIM: To develoPa method for the determination of high molecular weight impurities in Cephradine Capsule.METHODS: Gel filtration chromatography was adopted.The analytical column was Sephadex G-10 gel column.The mobile phase was consisted of A,0.2mol·L^-1 phosphate buffer (pH 8.0) and B,water.The flow rate was 1.0 ml·min^-1.The detection wavelength was at UV 254 nm.RESULTS: The content of high molecular weight impurities in Cephradine Capsule is less than 0.5%.CONCLUSION: The method is sensitive,accurate,simple and convenient enough to be used for the quality control of Cephradine Capsule.

Tissue distribution of brucine in mice

2006, 11(3):  342-344. 

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AIM: To study the tissue distribution of brucine in mice.METHODS: After ig and iv administration of brucine at doses of 60 and 10 mg·kg^-1 in mice,the plasma and tissue concentrations at different time points were determined by fluorescence spectrophotometry.RESULTS: After ig and iv administraction,The main tissue distribution of brucine in mice was similar,the brucine concentrations in the liver and kidney were the highest and those in the spleen,heart,lung,brain,stomach,fat and muscle decreased sequentially.CONCLUSION: There is an extensive distribution of brucine in mice and it has ability to permeate blood brain barrier.

Comparison of clinical therapeutic effects of mycophenolate mofetil and azathioprine in patients after renal transplantation

2006, 11(3):  345-347. 

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AIM: To compare the clinical therapeutic effects of mycophenolate mofetil(MMF) with those of azathioprine on kidney graft recipients after renal transplantation.METHODS: 56 patients were randomly divided into 2 groups:the grouPMMF and the grouPAza (n=28 in each group).In the grouPMMF,the patients were subjected to MMF,together with cyclosporin A (CsA) and prednisone(Pred).In the grouPAza,the patients received the triple drug treatment protocol:Aza,CsA and Pred.The whole blood concentration of CsA,function of the liver and the kidney as well as routine urine test were monitored at each monthly interval.RESULTS: The required administration of CsA and its blood concentration were remarkably lower in the groupMMF than those in the grouPAza(P<0.05).Compared with the grouPAza,the serum level of creatinine in the grouPMMF was also significantly lower (P<0.05).MMF had better therapeutic effects to resist acute rejections.The incidence of drug induced liver injury in the grouPMMF was lower as well.CONCLUSION: compared with Aza,MMF causes less adverse effects and induces less impairment on the liver and kidney.So MMF has better clinical therapeutic effects and can improve the survival rate of kidney grafts significantly.

Effect of ipratropium bromide on ventilation weaning in COPD patients

2006, 11(3):  348-350. 

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AIM: To study the effect of increasing ipratropium bromide (IB) dosage in the morderated to severe degree COPD patients with difficultly ventilation weaning.METHODS: Observed the effects of high dosage(120μg one time) ipratropium bromide in 17 patients with morderated to severe degree COPD who were fail to ventilation weaning at giving the routine dose (80μg one time) ipratropium bromide.RESULTS: All 17 patients were weaned ventilator successfully.The patients' indexes of artery blood gas analysis with giving high dosage IB were higher than those with routine dosage IB,the patients'modify Borg scores and respiration rates,heart rates with high dosage IB were lower than those with routine dosage IB(P<0.01),no further side effect for increasing IB dosage was observed.CONCLUSION: When the expiratory resistance becomes the most important factor of delaying ventilation weaning,giving a high dosage IB during ventilation weaning period may helPmorderate to severe degree COPD patients weaning the ventilator.

Antidotal effect of N-acetylcysteine on acute poisoning with sodium cyanide

2006, 11(3):  351-353. 

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AIM: To study the antidotal effect of Nacetylcysteine(NAC) on acute poisoning with sodium cyanide(NaCN).METHODS: After intraperitoneal (ip)injected of four sulphydryl compounds respectively,the mice which were acutely poisoned by NaCN were observed of the behavioral change,convulsion number and mortality rate(within 72 h).The median lethal dose (LD₅₀) of acutely poisoned mice was detected in NaCN grouPand NAC protection group.1 min after mice were poisoned by NaCN,the mice were divided into three groups:the first was iPnormal saline (NS),the second was iPNAC in combination with sodium thiosulfate (Na₂S₂O₃),the third was iPsodium nitrite (NaNO₂) in combination with Na₂S₂O₃.Then the behavioral change,convulsion number andmortality rate(within 72 h)were observed,recorded,and compared the differences between the mice groups.RESULT: All of the four sulphydryl compounds had protecting effect on acutely NaCN poisoned mice,among them NAC had most prominent effect (P<0.01).LD₅₀ were raised significantly (P<0.01) in acutely NaCN poisonedmice pretreated with iPNAC.After NaCN poisoned for 1 min,in the grouPof treatment with iPNAC in combination with Na₂S₂O₃,convulsion number and mortality of mice (within 72 hours) were declined significantly(P<0.01).It was not significant different when compared with the grouPwhich were treated by iPNaNO₂ in combination with Na₂S₂O₃.CONCLUSION: Sulphydryl compounds antagonizing cyanide intoxication are related with Sulphydryl.All of the results indicate that NAC has the antidotal effects on acutely NaCN poisoned animals.

Comparative study of synergistic effect of eupolyphaga on chemotherapeutics of digestive canal cancer

2006, 11(3):  354-356. 

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AIM: To compare the synergistic effect of eupolyphaga on chemotherapeutics of digestive canal cancer.METHODS: Drug sensitivity of stomach cancer cell(BGC-823) was determined in vitro by MTT anti-tumor screening assay for eupolyphaga with HCPT,5-Fu,Oxa,docelaxel,by comparing cell inhibition,the synergistic effect of eupolyphaga was analysed to find the best synergistic drug.RESULTS: The synergistic effects of eupolyghaga were more significant in HCPT and Oxa than those of 5-Fu and docelaxel in vitro (P<0.05).CONCLUSION: Eupolyphaga has a higher sensitivity in clinical routine chemotherapeutic regimens for stomach neoplamas cells in vitro.

Key activities involved in conduct of clinical trials

2006, 11(3):  357-360. 

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Key trial activities include:development of the trial protocol;development of standard operating procedures;development of support systems and tools;generation and approval of trial information documents;selection of trial sites and the selection of properly qualified,trained,and experienced investigators and study personnel;ethics committee review and approval of the protocol;review and approval by applicable regulatory authorities;enrollment of subjects into the study:recruitment,eligibility,and informed consent;the investigational product (s):quality,handling,and accounting;trial data acquisition:conducting the trial;trial data acquisition:conducting the trial;safety management and reporting;monitoring the trial;managing trial data;quality assurance of the trial performance and data;reporting the trial.