Table of Content

Volume 5 Issue 3
26 September 2000

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Activation of NF-κB in airway epithelial cell and modulation mechanism of NAC

MO Hong-Ying, ZHONG Nan-Shan, ZHENG Jing-Ping, LONG Qi-Cai

2000, 5(3):  193-196. 

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Aim The expression of NF-κB activation and the effect of antioxidant (N-acetylcys-teine, NAC)on NF-κB activity in human airway epithelial cell was assessed.Methods Using the TNF-α, the airway epithelial cell strains of normal subject(16HBE)and tumor patient (H292)was activated and using Western-Blot and ELISA the expression of NF-κB and IL-8 were detected.Results It was found that the activity of NF-κB could be stimulated by the TNF-α and increase with the amount of TNF-α with the peak occurring at 2 to 4 hours after stimulation and then decreasing at six hours.At the same time, the level of IL-8 was elevated, but decreased with inhibition of NF-κB activity by NAC, that means the action of NAC has a dose-dependent effect.Conclusion NAC not only blocks the signal transmission activated by NF-κB, but also anticipates the transcription modulation of expression of many cell factors and inflammatory mediums.It suggests that NAC may play a role in the anti-inflammatory treatment of respiratory diseases.

Experimental studies on the protective effect of defibrase against reperfusion injury after cerebral ischemia

HUANG Ru-Xun, XIAO Xiao-Hua, YIN Mei, LI Ling, LI Hua, SU Zheng-Pei

2000, 5(3):  197-200. 

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Aim To ascertain whether defibrase has the protective effect against reperfusion injury after cerebral i schemia.Methods 70 renovascular hypertensive rats(RHR) were randomly divided into defibrase group, control grouPand sham-operated group.Reversible middle cerebral artery occlusion(MCAO)models were produced by the modified.Long as method ,and reperfusion was begun 2 hours after occlusion.Rats in the defibrase grouPwere given defibrase 10 U·kg^-1body weight via femonal intraveneous injection, and in the control grouPwith the same amount of saline.The brain pieces were processed by TTC and HE staining and the infarct size, brain micro vessels damage and secondary bleeding were compared between the two groups.Results The volume of infarction in the defibrase grouPwas obviously smaller than in the control group, the damage of brain micro vessels was less severe ,and the bleeding lesions under optical microscope were less than in the control group.Conclusion Defibrase has protective effect against reperfusion injury post cerebral ischemia.

Estradiol in inhibition of proliferation of vascular smooth muscle cells after balloon injury

ZHAO Zhi-Sheng, HUANG Cong-Xin, JIANG Hong, WANG Teng, WANG Jing, LI Geng-Shan

2000, 5(3):  201-203. 

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Aim To investigate estradiol inhibition of neointimal prolife ration after rat carotid artery balloon injury.Methods Eight to ten-week old SD rats (male, n=21, female, n=21) were divided into intact control(n=7), gonadecto my control(n=7)and estradiol (n=7, gonadectomy) groups in each sex.Left carotid artery was not injured with 2.0 F PTCA balloon until estradiol was injected fo r three day s.Rats were killed 2 w k after injury. Neointimal areas and media area, ratio s of intimal areas/media areas were measured with computer.Results M ale neointimal areas and ratios of intimal areas /media areas in estradiol grouPwere less than those in intact control g rouPsignificantly(all P<0.01) and than those in gonadectomy control grouP(all P<0.05).T ho se in female, in estrdiol g rouPwere less than those in gonadectomy control grouPevidently (all P<0.01), and similar to those in intact control grouP(all P>0.05).Conclusion sEstrdiol inhibits neointimal proliferation after the gonadectomy in rats undergoing carotid artery balloon injury.

Study tetrandrine defer extraceller matrix mechanism

DONG Xing-Gang, LU Ming, YANG Hai-Chun, CAO He-Xing, ZHU Dong-Sheng, YE Chuan-Ji, XU Ming-Hua

2000, 5(3):  204-206. 

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Aim The effect of tetrandrine on TGF-β₁ mRNA expression in glomerulosclero sisrat was observed.Methods The rats were randomly divided into four groups, such as the normal control grouP(sham operative rat), glomerulosclerosis model group, tetrandrine grouPand amlodipine grouP.The expression of TGF-β₁ mRNA was analyzed by Northern blot hybridization.Results The expressions of TGF-β₁ mRNA in two treating groups were much lower than untreated model grouP.There were no difference between these two treating groups.Conclusion Tetrandrine can decrease the expression of TGF-β₁ mRNA in glomerulo sclerosis rat induced by unilateral renctomy plus adriamycin.

Effect of L-dicentrine on contractility of the sprips of porcine coronary artery

LI Hui-Lan, SU Yan-Hong, LI Zhong-Min, ZHANG Rong-Ping

2000, 5(3):  207-209. 

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Aim ＆ methods The antagonism of L-dicentrine to contraction of isolated porcine coronary artery strips induced by 5-HT KCl and Ca²⁺was observed with U-135 electrophsiological recorder.Results The contract ions induced by 5-HT KCl and Ca²⁺after high K⁺depolarization in the strips of porcine coronary artery were markediy inhibited by L-dicentrine. L-dicentrine significantly depressed maximal response and caused rightward displacement of the dose-response curve.Showing a non-competitive antagonism.In Ca²⁺free solution, L-dicentrine inhibited 5-HT-induced contraction of porcine coronary artery ,which is dependent on Ca²⁺relesed from intracellular store.After Ca²⁺concentration in bath solution was restored, L-dicentrine did not influence the contraction of porcine coronary artery depending on extracellular Ca²⁺.Conclusion L-D have significant relaxation on porcine coronary artery ,which possibly has 5-HT receptor and histamine receptor.

Immune modulation of anti-HBV iRNA from different sources in patients with chronic hepatitis B

YU Yong-Sheng, CHEN You-Hua

2000, 5(3):  210-212. 

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Aim To explore the function of immune modulation of anti-HBV iRNA in patient s with chronic hepatitis B(CHB).Methods Peripheral blood lymphocyte iRNA was prepared from anti-HBs positive human body with HBV complete clearance after HBV infection(h-iRNA). The effect of h-iRNA on HBV specific lymphocyte proliferative response of peripheral lymphocyte from patient s with CHB was observed by using MT T method and was compared with that by HBV specific iRNA from animal immunized only by HBsAg (a-iRNA).Results Both h-iRNA and a-iRNA increased the level of peripheral lymphocyte proliferative response to HBsAg in patient s with CHB to some degree.In grouPof HBcAg,only h-iRNA showed its enhancement of HBcAg specific lymphocyte proliferative response.Conclusion sh-iRNA can increase HBV specific lymphocyte proliferative response in patients with CHB and the function of increasing HBcAg specific lymphocyte proliterative response contributes to HBV clearance.

Pharmacokinetics of dauricine in dogs

CHEN Shu-Juan, ZHANG Bin, YANG Yi-Mei, DAI Zong-Shun, ZENG Fan-Dian

2000, 5(3):  213-217. 

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Aim To study the pharmacokinetic characters of Dauricine in dogs.Methods Dauricine was applied in 5 dosages of two administration ways 5 dogs according to Latin Square plan. The drug plasma concentration was determined by RP-HPLC.Results Dauricine spread quickly from central compartment to spherical compartment after intravenous administration of 6 mg·kg^-1.The t_{1/2 (α)} was 6~12min, K₁₂>K₂₁.The mean t_{1/2 (β)} was (2.7±0.4) h,V_d was about 11.18 L·kg^-1.The C-T profile conformed to two compartment open model.The plasma Dau concentration-time curves showed a double-peak phenomenon in all dosages of all dogswhen dauricine was given by intragastric was.The t_peak(1)was (0.8±0.6)~(1.2±0.5)h, t_peak(2) was (5.2±3.2)~(6.5±1.9) h, C_max(2)< C_max(1). Dauricine was eliminated linearly in the do sages of 12.5 and 25 mg·kg^-1,there was no obvious difference of parameters t_1/2(el),CL,AUC/X₀ between them (P>0.05)and the AUC was increased in pro portion.The drug is eliminated non-linearly when the dosage is above 50 mg·kg_-1,the parameters t_1/2(el), CL,A UC/X₀ shows great difference (P<0.01)comparing with dosage 12.5 mg·kg_-1,AUC was increased out of pro portion.Conclusion The plasma drug co ncentration-time curve of Dau afterig administration in dogs shows a double-peak phenomenon.A saturated character in Dauricine’s elimination is observed when the dosage is over or equal to 50mg·kg^-1.

Artihypertersive and regressive effect of valsartan and benazepril on left ventricular hypertrophy of spontaneously hypertensive rats

CAO Heng, HU Zuo-Yin, YANG Ting, YANG Shang-Yin, YU Guo-Hua

2000, 5(3):  218-220. 

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Aim To explore the effects of valsartan and benazepril on left ventricular hypertrophy (LVH)in spontaneously hypertensive rats (SHR).Methods 24 SHR were divided randomizedly into 4 groups of 6 rats each, among which three groups were fed with valsartan of 8 mg·kg^-1、of 24 mg·kg^-1and benazepril of 1 mg·kg^-1in NS per day for 4 weeks respectively, while the remained grouPand the other 6 Wistar Kyoto rats (WKY)were only given NS for equal time.Results The BPwas decreased markedly (P<0.05)in SHR fed with valsartan and benazepril.The decrease of BPwas more significant in SHR fed with 24 mg·kg^-1than in those fed with benazepril and the difference was statistically remarkable (P<0.01).The traverse diameter of myocyte (TDM) of the SHR treated with benazepril was lower than that in the controled groups.The TDM and heart weight/body w eight (HW/BW)of SHR treated with valsartan 24 mg·kg^-1was much lower than those in the benazepril and control groups.Conclusion Both benazepril and valsartan have effects of reversing LVH and decreasing BP.The effect of valsartan depends to some extent on the doses given, and the strength of the effect of decreasing BPand reversing LVH is not congruent.

Effects of extracts of ginkgo biloba leaves on platelet adhesion and thrombosis

MING Liang, ZHANG Yan, ZHANG San-Jun, JIANG Qin

2000, 5(3):  221-223. 

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Aim To observe the effect of extracts of ginkgo biloba leaves(GbE)on platelet adhesion and thrombosis.Methods The platelet adhesion was assayed by rotating glass-globe method.The thrombogenesis method in artery-vein by pass was applied to observe thrombosis in vivo.The Chandler method was applied to induce thrombosis in vitro.The tail bleeding time was recorded by shearing tail method.Results GbE significantly decreased platelet adherence rate in rabbits,decreased the weight of thrombus produced in artery-vein bypass in rabbits,shortened the length and reduced dry weight of thrombus of rats in vitro,prolonged the tail bleeding time in mice.Conclusion GbE inhibits the platelet adhesion and thrombosis.

Antioxidative effect of total axtract of astragalosides

YAO Yu-You, WANG Bin, LI Chang-Yu, LI Qiang-Jing, CHEN Min-Zhu, CAO Zheng-Zhong

2000, 5(3):  224-228. 

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Aim The relationshiPbetween the therapeutic effect of TEA (total extract of astragalosides) on adjuvant arthritic (AA)rat s and its antioxidative effects were studied.Methods The volume of non-injected hind paw of AA rat s and malondialdehyde (MAD) content of arthritic synoviocytes from AA rats were measured and the proliferative responses of fibroblast,the level of superoxide anion(O₂^-)and the hydroxyl radical (-OH)generated in vitro were detected. Results The anti-inflammatory effect of TEA might be related to its antioxidative activity.In vitro low-level oxidative stress promo ted the proliferative responses of fibro blast in rats synovium,which was marked by inhibited by TEA in a concent rat ion-dependant manner.Further study showed that TEA could inhibit NBT reduction induced by both xanthine-xanthine oxidase and no n-enzyme generated O₂^-,but the inhibitory effect of this compound on activity of xanthine oxidase was obtained only at high concent ration (more than 80μg·ml^-1).It was also found that TEA could dose-dependantly inhibit the hydroxylation of benzoic acid induced by Fenton react ion gene rated ·OH.Conclusion TEA has significant therapeutic effects on AA rats,which might be related to its antioxidative effects

Effect of ganquan 6 on mesenteric microcirculat ion in rats

XING Guo-Qing, SHI Yi-Ju, NIE Zhao-Wei, QIU Yu-Fang, NIE Heng-Huan

2000, 5(3):  229-230. 

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Aim To observe the effect of Ganquan 6 on mesenteric micro circulation in rat s.Methods 21 Wistar rats were randomly divided into 3 groups (n=7).The first grouPserved as the controled, the other two groups were o rally given ganquan 6 at doses of 1.5 g·kg^-1and 3.0 g·kg^-1for 10 days.30 minutes after the last administration, all the rats were injected 2ml·kg^-1sterile amniotic fluid via lingualis vena.Results In the control group, amniotic fluid injection caused significant decreases in instant blood flow rate and blood flow (P<0.05).In the ganquan 6 treated groups, although amniotic fluid injection failed to cause significant changes in microcirculation, the blood flow rate and blood flow had significant differences from those in the control group(P<0.05,P<0.01).Conclusion Ganquan 6 can improve the microcirculation in rats with microcirculatory disturbance caused by decreasing blood flow rate and blood flow and strengthen anoxia-tolerance of cells.

Variation of asthma patient’s qual ity of life after anti-inflammation treatment

ZHANG Jing-Bo, JI Yan-Yan

2000, 5(3):  231-234. 

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Aim To evaluate the influence of asthma and the effect of anti-inflammation therapy on the quality of life (QOL)in allergic asthma patients.Methods The QOL of 45 patients with asthma were investigated by collecting questionnaire before and after three months anti-inflammation treatment, at the same time the serum eosinophil cationic protein(ECP) level was detected in 20 patients.The QOL questionnaire included 4 domains, they were respiratory symptoms, physical activity limitation, emotional function and environmental stimuli.Results The factors which influenced the QOL in asthma patients ranging from high to low were environmental stimuli, respiratory symptom and emotion function and physical activity limitation.After anti-inflammation treatment, the QOL was significantly improved and the serum ECP was decreased (P<0.001 and P<0.01).Al though the male patient, those the aging more than 50 and those with advanced education had relatively higher score, there was no significant difference amongsex, age and education before and after anti-inflammation treatment.Conclusion Asthma not only severe impacts patient shealth, but also affects patient diary, social activity and emotional function.Anti-inflammation treatment would significant improve the QOL for asthma patients.

Clinical study of low dose continuous infusion of ceftazidime (CAZ) for the treatment of low respiratory tract infections

LIU Zhen-Tong, GU Jun-Ming

2000, 5(3):  235-237. 

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Aim This experiment was designed to probe whether low dose (1 g·d^-1)continuous infusion of CAZ is safe, efficacious and low costing in the treatment of infections in low respiratory tract.Methods The patients were divided into control group and treatment group at random.The routine administration (1 g,bid)of CAI was adopted in the treatment group,while the low dose continuous infusion method (1 g·d^-1,and a loading dose 1 g)was used in the control group.Results In the control group and the treatment group, the clinical curative rates were 73.3 % and 73.9%, the efficacy rates were 90.0 % and 91.3 %, the bacterial clearance rates were 86.7 % and 82.7 % and the adverse effect rates were 6.7% and 8.7 % respectively.There was no significant difference between the two groups (P>0.05).Conclusions Low dose continuous infusion of CAZ to treat low respiratory infections is efficacious, safe and economical.

Effect of ciprofloxacin on pharmacokinetics and pharmacodynamics of glipizide

JIA Zhi-Fan, WANG Wei-Li, WONG Fu-Hai

2000, 5(3):  238-240. 

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Aim The effect of ciprofloxacin on the pharmaco-kinetics and the hypoglycemic effect of glipizide was studied.Methods Diabetic rats were given glipizide or glipizide combined with ciprofloxacin for nine days.Serum glipizide samples were assayed and pharmacokinetic parameters were analyzed.Results The concent ration-time curves in diabetic rats were fitted to one compartment model in both glipizide and glipizide combined with ciprofloxacin groups.The concentration of glipizide in glipizide combined with ciprofloxacin grouPwas elevated significantly.The clearance rate of the drug was declined by 50%(P<0.05), t_1/2(Ka)was prolonged by 63.7 % (P<0.05).After treatment of glipizide,or glipizide combined with ciprofloxacin,the blood glucose was 5.978 mmol·L^-1 or 5.301mmol·L^-1respectively. The difference of hypoglycemic effect between glipizide and glipizide combined with ciprofloxacin was significant. Conclusion The ciprofloxacin can affect the absorption of glipizide.The effect of lowering blood glucose of glipizide combined with ciprofloxacin is better than that of glipizide alone.

Pharmacokinetics of rebamipide in the patients with peptic ulcer

ZU Lu-Ning, LI Li YU Da-Hai

2000, 5(3):  242-244. 

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Aim The pharmacokinetics of rebamipide domestic and imported pro ducts in 27 patients with peptic ulcer was investigated.Methods The rebamipide concentrations in plasma were determined by high performance liquid chromatographic method following a single oral dose of 600 mg rebamipide made either in China or in Japan.The pharmaco kinetic parameters were computed with PKBP-N₁ program.Results Following a single oral dose of rebamipide, the concentration-time curves of the domestic and imported products fitted to two compartment open model.There was no significant difference in each pharmacokinetic parameters between the two product s(P>0.05). C_max of domestic and imported rebamipide tablet were (0.56±0.24) and (0.59±0.29)mg·L^-1,with that t_max were (1.75±0.92)and (1.98±1.05) h, t_1/2(β) were (1.86±1.38)and (1.93±1.45)h, AUC_0~∞ were (2.48±1.06) and (2.62±1.35)mg·h·L_-1. Conclusion The pharmacokinetics of the two products are similar.

Bioequivalence of domestic nimodipine capsules and toblets

ZHANG Hong, FU Jun, DAI Qun, LI Yan-Yan, XIONG Yu-Qing

2000, 5(3):  245-247. 

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Aim The bioequivalence of domestic nimodipine capsules and tablets in healthy volunteers was compared.Methods A single oral dose of capsule or tablet of 100 mg nimodipine was given to 18 healthy volunteers in a randomized crossover study.Plasma levels of the drue were determined with HPLC method.Results The plasma concentration-time curve fitted to the first order absorption,1-compartment open model.Their main pharmacoknietic parameters were C_max (56.4±16.9)μg·L^-1,t_1/2(ke) (2.08±0.42)h,t_peak (1.27±0.52) h ,AUC_0~9 (197.2±46.5)μg ·h^-1·L^-1.These was no statistically significant difference between the two products (P>0.05).The relative bioavailability of tested capsules to reference tablets was (99.3±13.1)%.Conclusion Both formulations are of bioequivalence.