Table of Content

Volume 13 Issue 3
26 March 2008

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Advances in predicting of drug-drug interaction in vivo by using cytochrome P450 mechanism-based inhibition data in vitro

CAO Shan, ZHOU Hong-hao

2008, 13(3):  241-248. 

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In the last decade, the approaches for the invitro inhibition assessment of the potentials of drug-drug interaction in vivo have received process. DDIs remain an important issue in clinical practice and the development of new drugs.Mechanism-based inactivation is gaining more attention among in vitro study. This review would describe methods in identifying mechanism-based inactivation, and introduce predictive models and parameters in the field.

Luteolin activates the cystic fibrosis transmembrane conductance regulator chloride channel

HOU Shu-guang, LIN Sen, YU Bo, JIN Ling-ling, YANG Hong

2008, 13(3):  249-253. 

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AIM: To investigate the activation effect of luteolin on cAMP-dependent cystic fibrosis transmembrane conductance regulator (CFTR) chloride channel. METHODS: A stable transfected epithelial cell line coexpression human CFTR and a green fluorescent protein mutant with ultra-high halide sensitivity (YFP-H148Q) were used to determine CFTR-mediated iodide influx rate. RESULTS: Luteolin increased dose-dependently CFTR-mediated iodide influx.The activity was rapid, reversible and Forskolin-dependent. Luteolin had additive effect with Forskolin mixture and did not elevate intracellular cAMP concentration wirhout Forskolin. CONCLUSION: The study identified luteolin could dose-dependently activate CFTR and provided that luteolin acted by combining with CFTR directly.

Construction of recombinant adenovirus carrying Kringle 5 gene and effects on the survival of pulmonary carcinoma bearing mice

LIU Yan, LIU Fang, YE Xun, DONG Ji-bin, LU Qin, ZHAO Yi, LI Qiu-hua, CHEN Hongzhuan

2008, 13(3):  254-258. 

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AIM: To construct the recombinant adenovirus containing human plasminogen Kringle 5 (K5)gene, then observe the secreted expression and effect of K5 protein on TC-1 tumors. METHODS: We cloned K5 gene into the genome of replication-defective adenovirus by virus recombination technology;the K5 RNA expression was evaluated by RT-PCR;the K5 protein secreted expression was determined by Immunoprecipitation andWestern blotting;the effect of K5 was observed in xenograft lung cancr mice model;and the tumor microvascular density (MVD)was counted. RESULTS: The recombined adenovirus Ad-EF1α-K5 was constructed successfully and was expressing in the levels of both mRNA and protein.In the mice lung cancer xenograft model, the recombinant adenovirus can delay the growth of established TC-1 tumors and decrease the MVD. CONCLUSION: Recombinant adenovirus vectors Ad-EF1α-K5 can efficiently express protein K5 and inhibit tumor growth in the mice lung cancer xenograft model.The effect may related to inhibitory effect on angiogenesis.

Thapsigargin induces endoplasmic reticulum stress in rat cortical neurons and intervention of Danhong injection

ZHANG Hong, LIU Xue-qiu, ZHANG Xiao-qiao, ZHENG Li-fang, XU Jiang-hua, MEI Yuan-wu

2008, 13(3):  259-265. 

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AIM: To study the apoptosis induced by thapsigargin on rat cortical neurons and the intervention of Danhong injection. METHODS: Primary cortial neurons were cultured in vitro, and NSE-positive cells were detected by immunohistological chemistry and immunofluorescence staining.Protein levels of GRP78, bcl-2, cytochrome c(cyt c), active caspase-12 were assessed by immunoblotting cell extracts with specific antibodies.The percentage of apoptotic(annexin V positive and propidium iodide negative)cells was determined by flow cytometric analysis.Protein expression of active caspase-3, caspase-9, caspase-8, caspase-7 was measured by flow cytometric(FCM)analysis cytometry;Intracellular calcium concentrations([ Ca2+] i) were measured by fluorescence spectrophotometer with calcium sensitive fluorescence indicator Fura-2/AM. RESULTS: As expected, GRP78 and caspase-12 protein levels elevated in cortical neurons in response to thapsigargin(2 μmol L, 24 h and 48 h)but not to vehicle.The rate of apoptosis induced by thapsigargin 24 h and 48 h was 17.88% and 21.38%, and was depressed to 6.30% and 6.11% after treated by Danhong injection (8 mL L) respectively.Activated caspase-3,-9,-8 was detected at 24 h and 48 h after thapsigargin contribution and was reduced by Danhong injection.The enhancement of [ Ca2 + ] i in neurons were induced by thapsigargin and were depressed by Danhong injection. CONCLUSION: Thapsigargin activates ER-initiated apoptosis which can be inhibited by Danhong injection in in rat cortical neurons.

Effects of resveratrol on the expression of osteoprotegerin and receptor activator for NF-κB ligand in femurs of ovariectomized rats

WANG Yan, TANG Xu-lei

2008, 13(3):  266-270. 

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AIM: To study effects of resveratrol on osteoprotegerin(OPG) and receptor activator of NF-κB ligand(RANKL) expression in femur of ovariectomized rats. METHODS: 48 female SD rats(3 months old) were assigned into 6 groups randomly:sham-operated group(SHAM);ovariectomized group(OVX);17β-estradiol replacement therapy group (ERT, 0.1 mg·kg^-1 ·d^-1, sc);high-dose resveratrol-treate group (RH, 40 mg·kg^-1·d^-1, i.p.);middle-dose resveratrol-treated group (RM, 20 mg·kg^-1 ·d^-1, i.p.); low-dose resveratrol-treated group (RL, 10 mg·kg^-1 ·d^-1, i.p.).Except for SHAM group, rats in other groups were operated by bilateral ovariectomy. Administration started at the 8th day after operation and lasted 8 weeks.At the end of the 9th week after operation, all rats were sacrificed.The bone mineral density (BMD) and vitodynamics properties(including ELASTIC, M-STRESS, M-LORD and STIFFNESS) of femurs were measured.The expression of OPG and RANKL in femurs of rats were observed by immunohistochemical staining methods. RESULTS: Compared with OVX group, resveratrol treatment (40 mg·kg^-1 ·d^-1 and 20 mg·kg^-1 ·d^-1) increased expression of OPG in femurs while decreased expression of RANKL in ovariectmized rats.In RH, RM, and ERT group, BMD, ELASTIC, M-STRESS of femurs were higher than those of OVX group. CONCLUSION: Resveratrol increased expression of OPG in femur while decreased expression of RANKL in ovariectmized rats, which was probably one of mechanism that resveratrol improve osteoporosis.

Anti-cardiac hypertrophic effect of ginsenoside Rg₁

DENG Jiang, HUANG Xie-nan

2008, 13(3):  271-275. 

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AIM: To investigate the inhibitory effect of ginsenoside Rg1 on left ventricular hypertrophy induced by abdominal aorta coarctation in rats. METHODS: SD rats were randomly divided into five groups, four groups of them were accepted an operation of abdominal aorta coarctation to elicit left ventricular hypertrophy (LVH), the other one was sham operation group.Rg1 (3.75, 15 mg/kg) or L-arginine (L-arg, 200 mg/kg) were administered to rats in three of those four groups respectively except model group.Three weeks after operation, Rg1 or L-arg was administered for 4 weeks.At the end of administration, the hemodynamics of the rats was detected by BL-420E system, and the LVH index (left ventricular weight body weight) and left ventricular weight/right ventricular weight (LVW/RVW) were used as hypertrophic parameters; the expressions of atrial natriuretic factors (ANF) and calcineurin (CaN) mRNA were determined by iCycler iQ Real-Time Polymerase Chain Reaction (Real-Time PCR). RESULTS: Compared with those in sham operation group, the blood pressure, the left ventricular systolic pressure, left ventricular end-diastolic pressure, LVH index and LVW/RVW were significantly increased, but the ±dp/dtmax was significantly decreased, and the ANF and CaN mRNA expressions were remarkably up-regulated in model group.Rg1 (3.75, 15 mg/kg) and L-arg (200 mg/kg) had no influence on the blood pressure and the left ventricular systolic pressure, but could significantly decrease the left ventricular end-diastolic pressure and increase the ±dp/dt max, LVH index and LVW RVW, reduce the ANF and CaN mRNA expressions. CONCLUSION: Rg1 has an inhibitory effect on the left ventricular hypertrophy induced by overload pressure in rats, which may be, in partly, mediated by its inhibitory effect on CaN signaling pathway.

Effect of ginsenoside-Rg2 on learning and memory of vascular dementiarats

ZHANG Li, PAN Zhi-yuan, JIN Yi, LONG Chao-liang, WANG Hai

2008, 13(3):  276-282. 

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AIM: To investigate the effect of ginsenoside-Rg2 on learning and memory of vascular dementia rats and its underlying mechanisms, especially the expression of NMDA AMPA receptors. METHODS: Vascular dementia(VD)of rat was induced by permanent occlusion of bilateral common carotid arteries(2OV).The rats were given different doses of ginsenoside-Rg2(2.5, 5.0, 10.0 mg kg)as while as operation. The spontaneous movement and the delayed non-matching-to-position task(DNMPT)in the water maze were used to examine the behavior changes on learning and memory;the mRNA of four different subtypes of NMDA AMPA receptors, including NR1 、 NR2A 、NR2B and GluR2 in hippocampus were determined by the RT-PCR method. RESULTS: The spontaneous movement and spatial learning and memory of VD rats were all decreased.After ginsenoside-Rg2 administration, the spontaneous movement and the spatial learning andmemory were improved;the latency of information swim(IS)and choice swim(CS)decreased, and choice accuration in choice swim increased.The expression of NR1 mRNA was enhanced while NR2A, NR2B and GluR2 were attenuated in hippocampus of VD rats.These pathological changes could be reversed by treatment with ginsenoside-Rg2. CONCLUSION: Ginsenoside-Rg2 can patently improve the spatial learning andmemory of VD rats.The mechanism may be related to the regulation of ginsenoside-Rg2 on the expression of NMDA AMPA receptors in hippocampus.

Scutellarin attenuates hydrogen peroxide-induced apoptosis in PC12 cells

LIU Ping, HONG Hao

2008, 13(3):  283-287. 

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AIM: To investigate the mechanisms of inhibition of hydrogen peroxide (H2O2)-induced cell apoptosis in PC12 cells by scutellarin. METHODS: Exposure of cells to hydrogen peroxide (H2O2), a inducer of oxidative stress, triggered a typical apoptosis determined by PI singel staining, Annexin V-PI double staining and DNA agarose gel electrophoresis.Bcl-2 mRNA expression was determined by RT-PCR and caspase-3 was detected by fluoremetry. RESULTS: Scutellarin significantly inhibited H2O2-induced the DNA fragmentation and the externalization of phosphatidylserine(PS), and decreased the percentage of cell apoptosis induced by H2O2 in PC12 cells.Also, down-regulation of Bcl-2 expression and up-regulation of caspase-3 activity resulting from H2O2 exposure were significantly reduced by scutellarin in PC12 cells. CONCLUSION: Scutellarin could significantly protect cell against H2O2-induced apoptosis, which might be associated with the increase of Bcl-2 expression and the inhibition of caspase-3 activity.

Anti-tumor and antioxidation effects of 4-p-amino-benzoinc acid-4’-demethylepipodophyllotoxin ester

CHEN Xiao, WANG Zhe-yuan, ZHANG You-cheng, LI Wen-guang

2008, 13(3):  288-292. 

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AIM: To investigate the antitumor and antioxidation effects of 4-p-amino-benzoinc acid-4'-demethylepipodophyllotoxin ester (PDE). METHODS: The in vitro antitumor effects was measured by MTT method, and in vivo antitumor effects was studied by transplanting tumor model of S180 and H22 in mice.The malondialdehyde (MDA) generation in tissues of rats was measured with the thiobarbituric acid (TBA) reaction.H2O2-induced RBC hemolysis was determined with spectrophotometry. RESULTS: PDE strongly inhibited SGC-7901 cell proliferation for 48 h in a concentration-dependent manner with IC50 of 84.7 (51.7-138.9) mg L.In vivo experiments showed that10, 20 mg kg PDE obviously inhibited the growth of S180 and H22 with inhibition rate 25.2%, 46.5%and 22.9%,39.3%, respectively.PDE also significantly inhibited MDA generation spontaneously [IC50 22.7 (16.9-30.4) mg L] or induced by Fe2 +-AA in homogenate of heart, liver and kidneys of rats with IC50 30.3(13.9-66.1), 29.9(20.9-42.7) and 13.3 (1.8-96.9) mg L, respectively.PDE 40, 80 mg L significantly inhibited haemolysis induced by H2O2 with inhibition rate 26.8% and 100.2%, respectively. CONCLUSION: PDE exhibits antitumor and antioxidation effects and there is relationship between the effects.

Cytoprotective effect and its mechanisms of isoliquiritigenin on acetaminophen induced acute injury of hepatocytes

ZHANG Dao-hua, YE Lan-lan, CHENG Hao, YU Wei, YANG Jing, GUO Peng

2008, 13(3):  293-298. 

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AIM: To study the cytoprotective action and mechanisms of isoliquiritigenin(ISL)on acute injury of hepatocytes induced by acetaminophen. METHODS: Rat hepatocytes in sandwich cultures were randomly divided into control group, model group, ISL group and ISL plus L-NAME groups.The acute injury of hepatocytes was induced by being exposed into acetaminophen (20 mmol L)for 12 h.In the pretreatment groups, L-NAME and or ISL were given before administration of acetaminophen.The activities of ALT and AST in medium were measured by using enzyme assays.The CYP2E1 expression in hepatocytes was determined by using enzyme assays and semiquantitative RT-PCR.The contents of cGMP and cAMP in hepatocytes were measured by radioimmunoassay.The activites of nuclear transcription regulation factors such as NF-κB were determined by sandwich ELISA. RESULTS: ISL (5-20 μmol L)reduced the increase of the ALT and AST levels dose-dependently. And the cytochrome P450(CYP)2E1(aniline hydroxylase, ANH)activity was decreased by 75.7% maximumly and the mRNA expression was inhibited in a dose (50-200 μg mL)dependent manner, the maximum inhibitory rate was 78.7%.In addition, ISL remarkably increased the glutathione content decreased by acetaminophen of hepatocytes. L-NAME (2 mmol L)could reverse the protective effect of ISL (20 μmol L).ISL could not reverse the decrease of the level of cAMP induced by acetaminophen of hepatocytes but ISL could dose-dependently enhance the intracellular cGMP content (to 4.75 times maximumly)and suppress the NF-κB activation, the inhibitory rates were 24.8%,37.3% and 64.1%. CONCLUSION: ISL can protect the injury of hepatocytes induced by acetaminophen.It may be relate to the inhibition of NF-κB activation and down regulation of CYP2E1 expression via NO-cGMP pathways.

Sample size estimation and hypothesis testing of assessing equivalence/noninferiority for paired binary data

LIU Yu-xiu, XU Xiao-li, ZHENG Jun

2008, 13(3):  299-302. 

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Sometimes assessment of equivalence / noninferiority between two new drugs and medical devices involves comparisons of the response rates between paired binary endpoints in clinical trials.Statistical procedures have been developed for inferring equivalence / noninferiority often concentrated on comparing the rates of two independent binary responses in the past few years.Procedures for assessing equivalence/ noninferiority between the paired binary endpoints have not been well studied.In this paper, we introduce the determination of sample size and hypothesis testing of equivalence / noninferiority for paired binary data based on restricted maximum likelihood estimation.An equivalence / noninferiority clinical trial of ultrasound diagnostic device is used to illustrate the proposed methods.Discussions on some important issues are provided to help understand and conduct these trials.

Pharmacokinetics and bioequivalence of citric acid tamoxifen dispersible tablet in healthy volunteers

ZHANG Qian, ZHU Yu-bing, YU Cui-xia, ZOU Jian-jun, LU Tao, XIAO Da-wei, ZHUDong-ya

2008, 13(3):  303-308. 

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AIM: To study the pharmacokinetics and relative bioavailability of citric acid tamoxifen dispersible tablet in Chinese healthy volunteers. METHODS: In a randomized two period crossover study, 20 healthy volunteers received tested and reference tablets 20 mg.The plasma concentrations of tamoxifen were determined by HPLC.The pharmacokinetics of tamoxifen was estimated by the non-compartment model. RESULTS: The main pharmacokinetics parameters of tested and reference tablets were as the following:tmax (6.3±2.2), (6.7±2.4)h;Cmax (72±14), (68± 16) μg/L;AUC(0-492)(4.6±2.0), (4.6 ±2.0) mg·L-1 h;t12(143±24), (153±33)h, respectively.The relative bioavailability was (101±13)%. CONCLUSION: The two formulations are bioequivalent in human.

Bridging studies in clinical trials for new drug application

XIN Wei-quan, XUN Peng-cheng, YU Hao, CHEN Feng

2008, 13(3):  309-314. 

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AIM: To introduce the concept of bridging study and its strategies in clinical trials for new drug application. METHODS: The concept of bridging study proposed in the ICH E5 guideline was introduced, with a case using bridging strategies in the new drug applications (NDAs) approved by the regulatory authority in Japan.The concrete mode and the development of bridging studies in Asia were summarized. RESULTS: With the application of the ICH E5, some countries and regions have successfully used the bridging strategy in the new drug applications.The bridging strategy is becoming a common and practical basis for the decision making of marketing approvals of new drugs in the Asia-pacific country. CONCLUSION: The currently bridging studies in Asia will play an important role in the extrapolation of foreign clinical data in new drug application.Using bridging study is very helpful in judging ethnic differences of drugs, reducing duplication of clinical trails, as well as shortening clinical development periods.

Bioavailability and bioequvilence of bezafibrate capsule in human

XIAO Feng, WU Cheng-yi, TAO Chun-lei, GAN Lei, WEI Wei

2008, 13(3):  315-319. 

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AIM: To study the bioavailability and bioequvilence of bezafibrate capsule and tablet in health human. METHODS: 20 health volunteers were given bezafibrate capsules and tablets 400mg once with the interval of one week.Plasma samples were obtained and determined with HPLC method.Pharmacokinetics parameters were calculated and compared with DAS software. RESULTS: The main pharmacokinetics parameters of bezafibrate capsules and tablets were as follow:t1 2 (1.9 ±0.5) 、(2.0 ±0.6) h;Cmax (12±4) 、 (11±3) μg mL;tmax (1.7±0.9) 、(1.9±0.7) h; AUC(0-12) (36±10)、(33±7)μg·mL-1·h;AUC(0-∞) (37±10) 、(34±7) μg·mL-1 h.The biovailability of bezafibrate capsule campared to tablet was 92.3%and 92.9%. CONCLUSION: The test bezafibrate capsule is bioequivalent to the reference talbet in health human.

Analysis of adverse effects of fosfomycin injection in 148 cases

YANG Li-jie, LI Xiao-meng, GUO Mei-hua

2008, 13(3):  320-322. 

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AIM: To provide a rationale of adverse effects in therapy of fosfomycin sodium for injection by characterizing the adverse drug reactions (ADRs) of fosfomycin sodium. METHODS: 148 ADRs repots were pooled and statistically analyzed from domestic literatures from 1997 to 2006 with regard of patients' gender, age, ADRs history, route of medication, clinical manifestation and treatment actions. RESULTS: The patients who had ARDs histories occupied by 75.44% except the patients whose ADRs histories were unknown.The patients experienced ADRs of 86.21% when they simultaneously administered fosfomycin sodium, of which 99.32% of those ADRs were recovered or improved after other medical interventions.One death report was submitted.Most of ADRs were categorized as allergic reaction. CONCLUSION: The clinic apperance of fosfomycin sodium injection was diversified.The main one was allergic reactions.

Effects of regular consumption of RRR-a-tocopherol on the metabolism of simvastatin

DUAN Juan, ZHANG Song-bo, ZHANG Sai-dan

2008, 13(3):  323-327. 

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AIM: RRR-a-tocopherol is an essential micronutrient which can activate the pregnane X receptor (PXR) and regulate the expression of its target gene CYP3A and P-glycoprotein.Simvastatin is metabolized and transported by CYP3A and P-glycoprotein.The aims of the study was to investigate the effect of RRR-a-tocopherol on the metabolism of Simvastatin in vivo. METHODS: In a two-stage doubly periodic cross-over study, 12 healthy volunteers, who were randomly divided into two groups, ingested RRR-a-tocopherol 600 mg or placebo(control) for 14 days.On the fifteenth day, a single 40 mg dose of Simvastatin was taken by all of them and 5 mL peripheral vein blood of each one was taken at 0, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5,3, 4, 6, 8, 12 and 24 h.The plasma concentrations of Simvastatin and Simvastatin-acid were determined by HPLC-MS-MS after centrifugation and blood plasma separation.The differences of pharmacokinetic parameters of every control groups were compared and analyzed. RESULTS: The plasma concentrations of Simvastatin and Simvastatin-acid of RRR-atocopherol group decreased obviously.Both the area under the curve of AUC(0 ~ 24h) of Simvastatin of RRR-a-tocopherol group and control group and Cmax of each showed significant difference (P <0.05);The area under the curve of AUC(0~24h) and Cmax of Simvastatinacid also showed an obvious difference between the two groups (P <0.05). CONCLUSION: RRR-a-tocopherol can significantly induce the clearance rate of Simvastatin.Great attention should be paid when the drug interaction occurs between RRR-a-tocopherol and Simvastatin, which can decrease lipid-lowering effect and lead to adverse drug reaction.

Effects of Tongxinluo Ultramicro-pulverization on acute myocardial infarction in anaesthetic dogs

ZHU Hui-ming, TANG Si-wen, ZHANG Hui-xin, WANG Hong-tao, ZHAO Shao-hua, WU Yi-ling

2008, 13(3):  328-331. 

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AIM: To study the effects of Tongxinluo Ultramicro-pulverization(TXLU) on acute myocardial infarction in anaesthetic dogs. METHODS: The acute myocardial infarction model was made by ligation of left anterior descending (LAD) artery.The experiments adopted the epicardial electrogram to measure the scope and degree of myocardial ischemia, the quantitative histologic assay (triphenytetrazolium chloride, TTC stain) to determine the size of myocardial infarction. The blood oxygen pressure and oxygen saturation were measured by blood-gas analyzer.The utilization rate of myocardial oxygen was calculated. RESULTS: Compared with the controls and before dosing, the TXLU obviously alleviated the degree of myocardial ischemia (Σ-ST) and narrowed the ischemic area indicated by the epicardium electrograph data display and TTC staining.In addition, TXLU could decrease the utilization rate of myocardial oxygen. CONCLUSION: TXLU could attenuate the damage subjected to myocardial ischemia and infarction, restore the utilization ratio of myocardial oxygen.

Clinical investigation of the correlation between TNF-αand proteinuria in patients with chronic glomerulonephritis treated with angiotensin Ⅱ blockers

ZHANG Dao-you, YANG Yan-lang, YANG Li-cai, XU Hai-hong, WANG Yu-wei

2008, 13(3):  332-335. 

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AIM: To investigate the effects of angiotensin Ⅱ(Ang Ⅱ) blockers on TNF-αand the relationship between TNF-αand proteinuria in patients with chronic glomerulonephritis (CGN). METHODS: 32 patients examined by biopsy as primary CGN with proteinuria were treated by benazepril, valsartan or combination with benazepril and valsartan for 8 to 12 weeks respectively.The TNF-αlevels in serum and urine, 24 hours proteinuria quantity, and serum creatinine level were assayed and recorded respectively before and after 8 to 12 weeks therapy. RESULTS: The TNF-αlevels in serum and urine and 24 hours proteinuria quantity were reduced significantly after therapy [ (7.8 ±3.9) vs (5.0 ±1.6) fmol mL, (11.9 ±6.8) vs (8.3 ± 3.5) fmol /mL, (2.6 ±2.0) vs (1.0 ±0.5) g, respectively;P <0.01, P <0.05, P <0.01].There was a positive correlation between the 24 hours proteinuria quantity and TNF-αlevels in serum and urine before and after therapy (P <0.01, P <0.05;P < 0.05, P <0.05;respectively). CONCLUSION: The TNF-αlevels in serum and urine were significantly increased in CGN patients, and there was a positive relationship between the TNF-αlevel and 24 hours proteinuria quantity.The Ang Ⅱ blockers could decrease TNF-αlevels in serum and urine, reduce proteinuria, and protect renal function.

Clinical effects of combination therapy with sodium ozagrel and low molecular weight heparin on progressive cerebral infarction

GAO Li-li, TANG Yong-chun, LIU Qian, LI Bin

2008, 13(3):  336-339. 

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AIM: To observe the clinical effect of combination therapy with ozagrel and low molecular weight heparin on progressive cerebral infarction. METHODS: 96 cases with acute progressive cerebral infarction were randomly divided into treatment group (48 cases) and control group (48 cases).The control group was only administered with 80 mg sodium ozagrel, bid, for 14 days.And the treatment group was administered with 80 mg sodium ozagrel, bid, for 14 days and 0.4 mL low molecular weight heparin sodium injection, bid, for 14 days.The number of platelet, blood clotting routine and the severity of neuro-functional defect (NDS) of both groups were detected before and after 14 days treatmeat. RESULTS: After 14 days treatment, the NDS of treatment group was significantly lower than that of control group (P <0.05). The efficacy of treatment group was significantly better than that of control group (P <0.05).Both the number of platelet and the blood coagulation time were in normal range. CONCLUSION: Sodium ozagrel combined with low molecular weight heparin sodium are an effective and safe therapy for progressive cerebral infarction.

Effects of postoperative analgesia with lornoxicam and butorphano in patients undergoing laparoscopic cholecystectomy

YU Jun, GUO Jian-rong, JIN Xiao-ju

2008, 13(3):  340-343. 

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AIM: To investigate the effect of postoperative analgesia with Lornoxicam and butorphano after laparoscopic cholecystectomy (LC). METHODS: 90 ASA Ⅰ-Ⅱpatients scheduled for LC were randomly divided into three groups:group lornoxicam (n = 30) received lornoxicam 8 mg, group butorphano (n = 30) received butorphano 1mg, group NS (n =30) received 0.9%NS 2 mL at the time of the complaint of pain by the patients after extubate of tracheal catheter. Postoperative abdomen pain was assessed by visual analog scale (VAS), the patients were assessed by brungmann comfort scale (BCS) and Ramesay score (RS) within 1, 6, 12, 24 hours postoperatively.Side-effects were also assessed. RESULTS: The patients of group lornoxicam and butorphano had significantly higher BCS and RS scores than group NS (P <0.01), both of them also had significantly lower VAS than group NS (P <0.01).Group lornoxicam caused no more sideeffect, such as nausea, vomiting than group butorphano and NS(P <0.05). CONCLUSION: The study suggests that postoperative analgesia with lornoxicam 8 mg or butorphano 1 mg provide satisfactory postoperative pain relief with no more side-effects for patients undergoing LC.

Effects of natural drugs on CYP3A

YI Fei, ZHOU Hong-hao

2008, 13(3):  344-349. 

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Natural drugs are widely used in China and Southeast Asia, and they are more and more popular in Europe and America.Though complicated their component are, their monomer and active ingredients are metabolized by CYP450s as synthetic drugs. CYP3A is one of the most important cytochrome P450, and more than half of drugs are metabolized by this enzyme.Now many in vitro and in vivo researches indicate that many natural drugs and the ingredients effect CYP3A widely, and lead to drug-drug interactions in combined use.So researching on the regulation of natural drugs will not only benefit medication safety, but also make sense to the development of new drugs and revealing the mechanism of drug-drug interactions.

Advances in nonsteroidal antiinflammatory drugs and cardiovascular disease

ZHU Yu, WU Mei-hua

2008, 13(3):  350-354. 

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Nonsteroidal antiinflammatory drugs (NSAIDs) are widely used nowadays, Current evidence indicates significant adverse cardiovascular effects induced by selective COX-2 inhibitors that include increased risk for myocardial infarction, stroke, heart failure, and hypertension.The risk for these adverse effects is likely highest in patients with a prior history of cardiovascular disease, or with high risk of cardiovascular disease.In these patients, use of COX-2 inhibitors for pain relief should be limited to patients for whom there are no appropriate alternatives, and then, only in the lowest dose and for the shortest duration necessary.More long-term data are needed to fully evaluate the extent to which these adverse cardiovascular effects may be offset by the benefits of these medications.More data are also needed on the cardiovascular safety of conventional NSAIDs.It is recommended that both patients and physicians should balance the risks and benefits of NSAIDs.

GNB3 C825T and essential hypertension

HUANG Hai-ying, ZHOU Hong-hao

2008, 13(3):  355-360. 

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G protein plays an important role in the process of signal transduction.It mediates many intracellular effects of blood vessel competent and proliferation.So pharmacologists are very interested in the relation of its polymorphisms and cardiovascular diseases particular essential hypertension.GNB3 C825T polymorphism distributes differently in various populations. We focus on the relation of GNB3 C825T polymorphism with essential hypertension in different populations, and therapeutic effects on hypotensive drugs.