Table of Content

Volume 17 Issue 3
26 March 2012

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Effect and mechanism of tetramethylpyrazine on antithrombotic

YANG Wen-hui, GONG Guo-qing, ZHOU Yi, ZHANG Zhi-xian, LI Jie

2012, 17(3):  241-244. 

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AIM: To investigate the effect and mechanism of tetramethylpyrazine on antithrombotic. METHODS: The effect of tetramethylpyrazine (20, 40, 80 mg/kg, i.g.) on thrombosis induced by inferior vena cava ligation and electrically mediated carotid arterial in rats were evaluated.And studies were also conducted in rate of platelet aggregation, non-occlusion thrombosis, thrombin inhibition and plasm pro-time prothrombin time(PT) and activated partial thromboplastin time (APTT) in rabbits of different does of tetramethylpyrazine (10, 20, 40 mg/kg, i.g.). RESULTS: Tetramethylpyrazine showed competent anti-thrombin activity and inhibited platelet aggregation induced by thrombin and ADP, but presented lower potency in platelet aggregation induced by collagen. In addition it markedly decreased venous and arterial thrombosis and extended PT. CONCLUSION: Tetramethylpyrazine has a significant effect on antithrombosis in vivo. The mechanism seems to be related to the inhibition of platelet aggregation and protection of endothelium.

Effects of Schisandrin A on pharmacokinetics of midazolam and its metabolite in rats

XIN Hua-wen, LI Wei-liang, WU Xiao-chun, LI Qing, YU Ai-rong

2012, 17(3):  245-250. 

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AIM: To evaluate whether Schisandrin A (SchA) can modify the pharmacokinetic profiles CYP3A substrates-midazolam in male rats. METHODS: The rats were intragastric administrated with varied dose SchA or 75 mg/kg ketoconazole for 3 consecutive days.Using of single-pass duodenum perfusion and inguinal artery -canulated rats (in vivo), midazolam metabolism was studied under chemical inhibition of CYP3A (ketoconazole) as positive control. Plasma concentrations of midazolam and related metabolites were analyzed by high performance liquid chromatography (HPLC). RESULTS: The pharmacokinetic parameters of midazolam after coadministration with SchA were as follows: AUC_(0-t) (mg·L^-1·h): (1.08±0.29) (negative control) and (1.58±0.58)(SchA 8 mg/kg) and (2.02±1.29) (SchA 16 mg/kg) and (2.22±1.25) (SchA 32 mg/kg) and 3.34±2.25 (ketoconazole 75 mg/kg);C_max (mg/L): (1.6±0.6) (negative control) and (1.8±0.8) (SchA 8 mg/kg) and (2.2±1.2) (SchA 16 mg/kg) and (2.2±0.7)(SchA 32 mg/kg) and (2.9±1.1) (ketoconazole 75 mg/kg).The pharmacokinetic parameters of 1′-hydroxy midazolam after coadministration with SchA were as follows: AUC_(0-t) (mg·L^-1·h): (0.61±0.17) (negative control) and (0.40±0.15) (SchA 8 mg/kg) and (0.39±0.20) (SchA 16 mg/kg) and (0.40±0.14) (SchA 32 mg/kg) and (0.35±0.09) (ketoconazole 75 mg/kg); C_max (mg/L): (0.54±0.13) (negative control) and (0.42±0.15)(SchA 8 mg/kg) and (0.39±0.20) (SchA 16 mg/kg) and (0.36±0.16) (SchA 32 mg/kg) and (0.35±0.12) (ketoconazole 75 mg/kg). CONCLUSION: The current results provide direct and explicit evidence that the metabolism of midazolam (a CYP3A substrate) is controlled by SchA in comparison with vehicle-treated rats.

Effect of Oct-4 on chemosensitivity of cisplatin against gastric cancer cells

CAI Ke, ZHOU Rui, SHI Bai-ling

2012, 17(3):  251-255. 

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AIM: To explore the mechanisms of multidrug resistance in human gastric cancer by establishing a cisplatin(DDP) resistance BGC-823 cell line. METHODS: The human cancer BGC-823 cells were exposed in a gradually increasing dose of DDP.MTT assay was used to detect the cytotoxic activity of DDP against BGC-823 and BGC-823/DDP cells. The mRNA expression of Oct-4 was detected by RT-PCR analysis.The small interfering RNA was used to specifically knockdown Oct-4 in BGC-823/DDP cells. The protein expression of Oct-4 was determined by Western blot analysis. RESULTS: DDP resistance cell line BGC-823/DDP was established by DDP 30-34 weeks contionuous inducing.The IC₅₀ values of DDP against BGC-823 and BGC-823/DDP cells were (2.33±0.12)and (21.46±0.97) μmol/L by MTT assay, respectively.Compared with the BGC-823 cells, the resistance to cisplatin of BGC-823/DDP cells was 9.21 times. Semi-quantitative RT-PCR analysis showed that the mRNA expression of Oct-4 was upregulated in BGC-823/DDP cells.Western blot showed that the expression of Oct-4 protein was down-regulated by the chemical synthesis siRNA;After interfered the Oct-4 gene expression of BGC-823/DDP cells by siRNA,the IC₅₀ values of cisplatin against BGC-823/DDP cells was decreased from (22.04±1.84) to (6.15±0.53) μmol/L;there was no significant difference (P<0.01). CONCLUSION: The results show that Oct-4 gene expression plays an important role in gastric cancer with cisplatin resistance.

Effects of ASIC1a gene silencing by siRNA on apoptosis of articular cartilage cells of adjuvant arthritis rats

JIANG Sheng, CHEN Fei-hu, CHEN Cun-zhi, RONG Chao, HU Wei, WU Fan-rong, GE Jing-fang, TANG Jie

2012, 17(3):  256-262. 

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AIM: To estimate the effects of ASIC1a gene silencing by siRNA on apoptosis in articular cartilage cells of adjuvant arthritis rats. METHODS: Lipofectamine 2000 transfection reagent was used to transfect the small interfering RNA(siRNA) with FAM in articular cartilage cells. The expression level of ASIC1a mRNA and protein were detected by fluorescence microscope,flow cytometry(FCM),real-time PCR and Western blotting, respectively. And the apoptotic cell dyed with Annexin-V and propidium iodide were measured with a flow cytometer. RESULTS: ASIC1a siRNA were transfected into articular cartilage cells successfully. The expression of ASIC1a mRNA and protein in transducted chondrocytes was lower than the control chondrocytes (P<0.01). The rate of apoptosis was lower in the ASIC1a-silenced cell than that in the model cell. CONCLUSION: The silence cells model of ASIC1a expression by siRNA in chondrocytes of adjuvant arthritis rats is the perfect model to observe the effect on metabolism of chondrocytes of the acid-sensing ion channels. Transfection siRNA-3 into articular cartilage cells protected from apoptosis by extracellular acid, which may be related with different expression levels of ASIC1a.

Construction of human CYP2C19 gene polymorphism eukaryotic expression vector and establishment of stably transfected HepG2 cell line expressing human CYP2C19

CHEN Wang, YU Jing, QU Qiang, ZHANG Wei, LI Zhi, WU Lan-xiang, WEN Chun-jie, ZHOU Hong-hao

2012, 17(3):  263-268. 

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AIM: To construct the eukaryotic expression vector of CYP2C19^*1,^*2,^*3, respectively, then stably transfect HepG2 cells with them. METHODS: The full-length CYP2C19 wild-type cDNA fragment was amplified by PCR from the human liver cDNA library and mutagenesis build ^*2, ^*3 (mutant) cDNA in vitro, then those cDNA were inserted into eukaryotic expression vector pcDNA3.l(-). After identification of restriction digestion and PCR,the recombinant plasmid was transfected into HepG2 cells by lipofectamine. After screening culture by G4l8, a stably-transfected cell line was established, and the transcription and expression of the CYP2C19 gene SNPs were identified by RT-PCR, Western Blot assay. RESULTS: The eukaryotic expression vector spcDNA3.l-CYP2C19^*1, ^*2, ^*3 were successfully constructed and transfected stably into HepG2 cells, respectively. Stably-transfected cell lines were established and the CYP2C19 gene SNPs was expressed successfully. CONCLUSION: The establishment of the stably-transfected cell line and the expression of the target gene provide a solid experimental foundation for screening and prediction the metabolic of new drugs on the function of the CYP2C19 gene.

Effects of HSYA injection on platelet aggregation, ultrastructure and the content of PAF induced GMP-140 in PRP in rabbits

XU Lu, DONG Zhi

2012, 17(3):  269-273. 

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AIM: To observe the effects of HSYA injection on platelet aggregation and ultra structure in rabbits. METHODS: In vivo experiments, when platelet activating factor (PAF) induced respectively, we observed the impacts of HSYA injection (10 mg/kg, 5 mg/kg and 2.5 mg/kg) on platelet aggregation, ultra structural changes of platelets and PAF-induced content of GMP-140. RESULTS: HSYA injection inhibited AA and PAF-induced platelet aggregation(P<0.05,P<0.01). Scanning electron microscope showed: HSYA injection could reduce the number of aggregation type plateles which were induced by AA and PAF; and make fewer and shorter processes of dendritic platelets(P<0.05,P<0.01). HSYA injection can reduce the content of GMP-140 in PRP(P<0.01). CONCLUSION: HSYA injection can antagonism PAF-induced platelet aggregation, inhibit the activation of platelets and reduce the content of GMP-140. Thus for, there will be more choices for clinical using of anti-platelet aggregation drugs.

Expression and its significance of GABA signal in gestational trophoblastic cell pathological tissues

LUO Wen-ping, LIU Zhen-zhen, PENG Hong-ying, TAN Dong-mei, ZHAO Hai, TAN Yi

2012, 17(3):  274-279. 

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AIM: To explore the effects of GABA_R agonist or antagonist on JAR cells invasion by identifying the expression of GABA,π subunit of GABA_RA, B1 subunit of GABA_RB(GABAB1R) in JAR cells and taking Transwell chamber with GABA or receptor agonist or antagonists. METHODS: The protein expression of GABA, GABRP, GABAB1R were measured by immunocytochemistry and western bolt in JAR cells. The mRNA GABRP, GABAB1R was measured by RT-PCR. The effects of GABA and its receptors agonists and antagonists on JAR cells invasion were assay by Transwell chamber. RESULTS: GABA, GABRP, GABAB1R were expressed in JAR cells. GABA_A receptor agonist muscimol significantly promoted the invasion of JAR cells, while GABA_BR agonist baclofen significantly inhibited JAR cell migration. CONCLUSION: GABA signal may be associated with the pathogenesis of trophoblast-associated diseases of pregnancy.

Effects of crocetin on the proliferation and collagen synthesis of cardiac fibroblasts

HU Hui, QIAN Zhi-yu, CHENG Wen-yuan, YANG Li-na, ZHU Yan-hong, TAO yun

2012, 17(3):  282-288. 

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AIM: To investigate the effects of crocetin on proliferation and collagen synthesis in cultured neonatal rat cardiac fibroblasts (CFB) stimulated by angiotensinⅡ(AngⅡ), and to explore the action mechanism of crocetin. METHODS: We used cultured cardiac fibroblasts from neonatal 1-3 days rat and treating with AngⅡ to induce fibrosis model. The effects of crocetin on proliferation of CFB were observed by MTT assay, synthesis of collagen was observed by the hydroxyproline concentration measured. Cell cyclin distribution was determined with flow cytometre. CollagenⅠ, collagen Ⅲ, matrix metalloproteinase (MMP-2), the tissue inhibitor metalloproteinase (TIMP-1) and TGF-β₁ mRNA expression were examined by Q-PCR. The expression of P27 was tested by Western blotting. RESULTS: Within a concentration coverage, crocetin inhibited CFB proliferation and collagen synthesis induced by AngⅡ in a dose-dependent manner. The percentage of cells in G₀/G₁ phase in crocetin groups increased with concentration, the percentage of cells in S and G₂/M phases and the proliferation index in crocetin groups decreased with concentration, which compared with AngⅡ group difference was statistically significant (P<0.05, P<0.01, respectively). Crocetin decreased the levels of CollagenⅠmRNA, Collagen Ⅲ mRNA, TIMP1 mRNA and TGF-β₁ mRNA expression, but increased MMP-2 mRNA expression. ④Crocetin decreased the protein expression of P27 stimulated by AngⅡ. CONCLUSION: Crocetin inhibited CFB proliferation and collagen synthesis stimulated by AngⅡ, which related to the cytokines excreting and the regulation of extracellular matrix.

Mitochondrial dysfunction and decrease of antioxidase activities are involved in oxaliplation chemotherapy-induced peripheral neuropathy

LIU Guo-kai, BENNETT Gary

2012, 17(3):  289-293. 

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AIM: To measure and evaluate the function on mitochondrial respiration and antioxidase activities of sciatic nerves in rats of oxaliplation-induced peripheral neuropathy. METHODS: 36 adult male Sprague-Dawley rats (150-200 g) were housed on sawdust bedding in plastic cages. A stock solution of oxaliplatin was diluted to 2 mg/mL with 5% dextrose in distilled water and injected IP at 2 mg/kg on five consecutive days (d 0-d 4) in a volume of 1.0 mL/kg. Control animals were received vehicle(5% dextrose) injections. All respirometrical studies described below use animals with confirmed oxaliplatin-evoked neuropathic pain.Mechano-allodynia and mechano-hyperalgesia were assessed on d 8, d 22, d 27, d 35, and d41 postoperatively. The sciatic nerves of 9 model and 9 vehicle rats were excised on d 27-35 postoperatively. The nerves were minced into segments about 1mm long. Each segment was then teased apart into microfilaments (the mince & tease (M&T) preparation).We assessed mitochondrial activity consists of the sequential addition of substrates and inhibitors for the several complexes of the electron transport system (ETS; a more accurate term than “electron transport chain”). The sciatic nerves of 9 model rats on d7 and d35 and 9 vehicle rats were used to assay GPx and TrR activity. RESULTS: We found that peripheral nerve mitochondria from oxaliplatin-treated rats had significantly lower respiratory control ratios. The vehicle-treated vs.oxaliplatin-treated differences in these two ratios were about 16%. We also found that the addition of cytochrome C had no effect on respiration in the control animals (the normal result) but significantly increased respiration in the oxaliplatin-treated animals. The data also suggested that oxaliplatin treatment caused a significant decrease (15.4%) in the activity of a key anti-oxidant enzyme, glutathione peroxidase (GPx). Moreover, we had found a significant decrease (23%) in the activity of another key anti-oxidant enzyme, thioredoxin reductase. CONCLUSION: The Respiratory Control Rate (the State3/State2 ratio) shows the stimulatory effects of the addition of a non-limiting ADP concentration on Complex I activity (in the presence of an excess of its substrates) and is a measure of the efficiency of coupling between oxidation and phosphorylation.A deficit in this ratio suggests impaired energy production due to Complex I deficiency. The “Suc pre-post” ratio shows the capacity for respiration when Complex II is activated by an excess of its substrate (succinate) in the presence of ADP. A decrease in this ratio suggests impaired energy production due to Complex II deficiency. Decreases in mitochondrial GPx and TrR activity suggest a likely mechanism for decreased mitochondrial respiration.

Pharmacokinetic and pharmacodynamic interaction between irbesartan and hydrochlorothiazide in renal hypertensive rats

HUANG Xiao-hui, HUANG Ji-han, CHEN Yun, QIU Fu-rong, LI Jun, SUN Rui-yuan

2012, 17(3):  294-301. 

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AIM: Pharmacokinetic-pharmacodynamic (PK/PD) modeling was applied to investigate the pharmacokinetic and pharmacodynamic interaction between irbesartan and HCTZ in renal hypertensive rats at non-steady-state and steady-state. METHODS: The renal hypertensive rats were treated with oral irbesartan alone, or HCTZ alone, or the combination of irbesartan and HCTZ for 8 days. Systolic and diastolic blood pressure and plasma concentrations were measured after single- and multi- dosing and PK/PD parameters were analyzed. RESULTS: Irbesartan showed a two-compartment model pharmacokinetic profile. The concentration-time course of irbesartan was not changed by HCTZ, but irbesartan increased the peak plasma concentration and area under the curve of HCTZ at steady-state. Irbesartan plus HCTZ had greater blood pressure lowering action than irbesartan alone. HCTZ increased actions of irbesartan. Hysteresis phenomenon was found between effect and plasma concentrations of irbesartan after a single dose. However, hysteresis phenomenon disappeared at steady state with more rapid realization of maximum concentration and effects. The relationship between effects and effect-compartment concentrations of the drugs was represented by a sigmoid Emax model. CONCLUSION: The results suggest synergistic pharmacodynamic interaction between irbesartan and HCTZ in renal hypertensive rats and some differences of PK/PD properties between irbesartan and irbesartan/HCTZ combinations at non-steady state and steady state. These comparisons are likely to be clinically significant.

A Meta-analysis for hemorrheologic parameters in patients with cerebral infarction or high risk population treated by Shuxuetong or Danshen

YAN Tao, ZHOU Qi-xin, FEI Hui-zhi, HU Xiao-ya, YANG Qiu-jun

2012, 17(3):  302-307. 

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AIM: To compare effects of Shuxuetong on hemorrheologic parameters to that of Danshen in patients with cerebral infarction or high risk population, so that evidences in Evidence-based Medicine can be provided for clinical pharmacotherapy. METHODS: Thirteen articles corresponding to our researching condition were searched out by retrieving and screening domestic articles from 2000 to 2011 according to the criterion for including or excluding articles. The data were processed by the method of meta-analysis. RESULTS: A comparison between Shuxuetong versus Danshen: HS [WMD=-0.53, 95%CI (-0.76, -0.31), P<0.05]; LS [WMD=-1.40, 95%CI (-2.05, -0.74), P<0.05]; PV [WMD=-0.27, 95%CI (-0.39, -0.15), P<0.05]; FIB [WMD=-0.75, 95%CI (-0.97, -0.52), P<0.05]; HCT [WMD=-0.05, 95%CI (-0.08, -0.01), P<0.05]. CONCLUSION: The improvement effects of Shuxuetong on hemorrheologic parameters are better than that of Danshen, even though serious heterogeneity exists among the selected articles.

Determination of Pidotimod in Human Serum by HPLC-MS/MS

YANG Jing-jing, SUN Hua, ZHAO Jun, DAI Min, LI Xiang-hong, ZHAO Ya-nan, LU Jian-ping, XIE Hai-tang

2012, 17(3):  308-312. 

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AIM: To develop and validate an HPLC-MS/MS for the determination of pidotimod in human serum. METHODS: Glipizide was added as internal standard.The sample preparation included a simple deproteinization step with methanol.Chromatographic separation was achieved on a Lichrospher C₁₈ column(4.6 mm×150 mm,5 μm)at 30 ℃ with the mobile phase consisted of methanol-2.5 mmol/L NH₄Ac (90∶10, V/V). The mobile phase was eluted at a flow rate of 0.5 mL/min.Tandem mass spectrometer equipped with electrospray ionization source was applied and operated in the negative ion mode. Multiple reaction monitoring using the precursor to product ion combinations of m/z 242.9/153.0 and m/z 444.0/169.9 was performed to quantify pidotimod and glipizide, respectively. RESULTS: The calibration curves were linear over the range of 0.1-10 mg/L(r=0.9995). RSD of intra-batch and inter-batch were less than 15%, extraction recovery of three level concentrations were 85.52%-98.30%. CONCLUSION: The method is shown to be convenient, accurate, sensitive, and suitable for clinical pharmacokinetic study of pidotimod.

Effect of risperidone on S100B levels and relationship with treatment response in first-episode schizophrenic patients

LIU Lin-jing, XIU Mei-hong, ZHANG Xiang-yang, CHEN Da-chun

2012, 17(3):  313-317. 

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AIM: To study if S100B levels is abnormity, to study the effect of risperidone on S100B levels and relationship between S100B levels and treatment response in first-episode schizophrenic patients. METHODS: Fifty-three first-episode schizophrenia inpatients according to DSM-IV were treated only with risperidone for 12 weeks, the Positive and Negative Syndrome Scale (PANSS), Clinical General Impression (CGI) and Hamiton Depression Rating Scale (HAMD) were estimated at the baseline and the endpoint to evaluate the clinical efficacy. The serum S100B levels of the patients at the baseline and the endpoint and the 58 healthy controls were assayed using Enzyme Linked Immunosorbent Assay (ELISA). RESULTS: The serum S100B levels of the patients groups were significantly higher than the controls (P<0.01) at the baseline, were significantly decreased after 12 weeks treatment with risperidone but remained significantly higher than controls (P<0.05). The serum S100B levels was negative correlated with the age of onset and score of HAMD(r= -0.28, -0.31, P all <0.05)at baseline, The serum S100B levels were significantly lower in the treatment responders comparing no-responders, were negative correlated with reduction of PANSS total score and negative subscore from baseline to 12 weeks (r=-0.28, -0.31, P all <0.05). CONCLUSION: The serum S100B levels of the schizophrenic patients are significantly higher than the healthy controls, Risperidone treatment reduced the S-100B levels that were associated with treatment response, indicating that patients with schizophrenia may suffer structural damage in central nervous system.

Influence of dezocine injection to the side effects during tracheal extubation period in laparoscopic cholecystectomy

GENG Wu-jun, TANG Hong-li, ZHANG Xue-zheng, HUANG Lu-ping, GAO Xiao-yan

2012, 17(3):  318-321. 

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AIM: To explore the effect of dezocine injection to the side effects during tracheal extubation period in laparoscopic cholecystectomyMETHODS: 90 patients treated with laparoscopic cholecystectomy were divided into three groups randomly, the dezocine group,including 16 men and 14 women, were injected with dezocine 0.1 mg/kg,and the fentany group(15 men and 15 women) were injected with fentanyl 0.002 mg/kg,and the tramadol group,including 17 men and 13 women, were injected with tramadol 2 mg/kg when the surgery was over. After venous induction with midazolam,propofol and cisatracurium to endotracheal intubation,the patients inhalated sevoflurane and injected propofol continuously during operation.The VAS analgesic score,Ramsay sedative score and the side reaction between the three groups were observed and recorded within 24 h after operation. RESULTS: The VAS scores of the dezocine group and the fentany group were much lower than those of the tramadol group at 0.5,1,4 h after operation,there was statistical significance(P<0.05). The VAS scores at 12,24 h in three groups had no statistical significance.The Ramsay sedative scores of the dezocine group were much higher than those of the fentany group and the tramadol group at 0.5,1 h after operation(P<0.05),The Ramsay sedative scores at 4,12,24 h in three groups had no statistical significance(P<0.05). There were no nausea and vomiting in dezocine group, 4 nausea and 0 vomiting in fentany group,and 14 nausea and 7 vomiting in tramadol group. CONCLUSION: Injecting the dezocine 0.1 mg/kg in vein is effective and safe when using in laparoscopic cholecystectomy.

Analgesic effects of dezocine combining with flurbiprofen after posterior spinal approach

ZHOU Bin-fu, QU Qing, CHEN Chun-li

2012, 17(3):  322-325. 

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AIM: To observe the analgesic effects of dezocine combining with flurbiprofen in patient controlled intravenous analgesia (PCIA) after posterior spinal approach. METHODS: Sixty patients undergoing posterior spinal internal fixation surgery were equally randomized into two groups : dezocine combining with flurbiprofen group (Group DF, n=30 ) , and sufentanil group (Group S, n=30) . Visual analogue scale (VAS) in the quiet time and movement in the stand, and Ramsay sedation scale were evaluated at 1,4, 8, 12, 24,36 and 48 h after surgery ; the number of effective compression ratio and the actual number of pressing within 48 h PCA,patient satisfaction with pain,overall assessment of pain patients and the incidence of adverse reactions were also recorded. RESULTS: The two groups were able to provide good postoperative analgesia, the number of effective compression ratio and the actual number of pressing were similar (P>0.05). DF group's VAS scores movement in the stand,patient satisfaction with pain and overall assessment of pain patients were significantly better than those in the S group(P<0.05), and had lower incidence of adverse reactions(P<0.05). CONCLUSION: Dezocine combining with flurbiprofen can provide satisfactory postoperative analgesia after posterior spinal approach,and has lower incidence of adverse reactions.

Clinical application of carboprost tromethamine on prevention and treatment of postpartum hemorrhage in cesarean section

LUO Yong-hong, HE Lian-zhi, SUN Yun-xia

2012, 17(3):  326-330. 

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AIM: To investigate the clinical efficacy of carboprost tromethamine on the prevention and treatment for hemorrhage during cesarean section (CS) and postoperative hemorrhage. METHODS: From Feb. to Oct. 2011, 120 cases undergone CS with high risk of PPH were divided randomly into two groups. After delivery 250 μg carboprost tromethamine was injected on the uterine body in study group, while methyl-carboprost suppository 1.0 mg by sublingual was given immediately in control group,both on the basis of oxytocin intravenous drip. The intraoperative blood loss, postpartum bleeding in 2 h and 2-24 h and the rate of postpartum hemorrhage were compared between two groups. The changes of vital signs before and after the treatment in two groups were observed. RESULTS: There were statistically significant differences between two groups on intraoperative blood loss, postpartum hemorrhage in 2 h and 2-24 h (P<0.05); And the incidence rate of postpartum hemorrhage in study group was less than that in control group(P<0.05). There were no significant differences on the change of vital signs before and after treatment (P>0.05)CONCLUSION: It was effective, rapid and convenient to use carboprost tromethamine for the prevention and treatment in high hemorrhagic risk fators of PPH during CS with less adverse reaction.

Effects of hypertonic sodium chloride hydroxyethyl starch 40 injection on cytokines of patients with septic shock

LV An-qing, CHEN Zhong-hua

2012, 17(3):  331-333. 

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AIM: To investigate the effect of intravenous infusion with hypertonic sodium chloride hydroxyethyl starch 40 injection(HSH40) on cytokines of patients with septic shock. METHODS: 60 operated patients with intestinal obstruction and septic shock were randomly divided into two groups (30 in each group). Therapy group (Group Ⅰ)was administrated with HSH40 at a dose of 10 mL/kg for 30 min after anesthesia induction. Control group (Group Ⅱ) was received the same amount of lactated Ringer's solution(LRS). Blood samples were taken at the following time point, immediately enter the operation room(T₀), at 30 min after infusion(T₁) and at the end of surgery(T₂), the levels of TNF-α, IL-1β, IL-6 and IL-10 in plasma were measured by ELISA. RESULTS: Compared with T₀, the levels of plasma TNF-α, IL-1β and IL-6 were decreased at T₁ and T₂ in groupⅠ (P＜0.05), while the level of plasma IL-10 was increased (P＜0.05). Compared with group Ⅱat T₁ and T₂, the levels of plasma TNF-α, IL-1β and IL-6 were decreased in groupⅠ (P＜0.05), while the level of plasma IL-10 was increased (P＜0.05). Compared with T₀, the levels of plasma TNF-α, IL-1β, IL-6 and IL-10 at each time point had no significant difference in GroupⅡ(P＞0.05). CONCLUSION: HSH40 may modulate the inflammation response during septic shock.

Clinical observation of fudosteine in the acute exacerbation of chronic obstructive pulmonary disease

ZHOU Ying, JING Qian, CHAI Xiu-juan

2012, 17(3):  334-337. 

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AIM: To evaluate the efficacy and safety of fudosteine in the acute exacerbation of chronic obstructive pulmonary disease( AECOPD). METHODS: 100 patients diagnosed as AECOPD were randomly divided into either therapy group and control group. Antibiotics, oxygen, bronchodilators, etc were used in two groups. At the same time the therapy group was given oral fudosteine 400mg three times daily, and the control group was given oral mucosolvan 60mg three times daily. Then the clinical efficacy and safety in two groups of patients were observed and analyzed. RESULTS: The response rate (RR) of clinical composite efficacy in the therapy group was significantly higher than that in the control group (86% vs 68%, P<0.05), and there was no significantly difference between the two groups of the safety (P>0.05). CONCLUSION: Fudosteine tablet is effective and slight side-effect used in AECOPD and should be used as a routine.

The safety and feasibility of dezocing in gynecological laparoscopy under epidural anesthesia

ZHANG Yan, LIU Ling-ling, YE Xiu-qing

2012, 17(3):  338-341. 

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AIM: To investigate the safety and feasibility of dezozine in gynecological laparaoscopy under epidural anesthesia. METHODS: Sixty ASAⅠorⅡpatients, aged 18-55 yr, undergoing gynecological laparoscopy surgery, were randomly divided into 2 groups (n=30 each): Dezocing group (group D) and Fentanyl group (group F). P_ETCO₂ and Ramsay sedation scales were recorded at the time points followed: pre-anesthesia (T₀), 10 min after administration (T₁), instantly after pneumoperitoneum (T₂), 30 min (T₃) and 60 min (T₄) after pneumoperitoneum, 5 min after eliminating pneumoperitoneum (T₅). The incidences of side effects such as nausea, vomiting, algor and respiratory depression was observed. RESULTS: Ramsay sedation scales were not statistically different between the two groups. D group's P_ETCO₂ was lower than of F group at the time points of T₃ and T₄. The incidences of nausea, vomiting and respiratory depression were higher in F group (P<0.05). CONCLUSION: Dezocine has significant advantages over fentanyl to assist epidural anesthesia in gynecological laparoscopy with respect to reduce discomfort during pneumoperitoneum, better analgesia and sedation, less side effects.

Compare the clinical effects of obstetrics and gynecology intravenous injection for postoperative analgesia with Sufentanil and Dezocine

ZHANG Fan, ZHANG Hang, LI Feng

2012, 17(3):  342-345. 

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AIM: To observe and analyse the clinical effects of gynecology intravenous injection for postoperative analgesia with Sufentanil and Dezocine. METHODS: 150 cases of obstetrics and gynecology patients were randomly divided into groups of Dezocine,Sufentanil,Dezocine joint Sufentanil. 24,48 h after intravenous analgesia recorded the VAS, BCS, Ramsay score,vomiting score,recorded a variety of adverse reactions. RESULTS: Compared between 24 h and 48 h among Dezocine group,Sufentanil group and Sufentanil combined with Zuoxin Group ,Sufentanil combined with Zuoxin Group had higher VAS, BCS,vomiting score, and there were statistically significant among three groups (P<0.05). Adverse reactions in addition to stupor,respiratory rate and mean arterial pressure had no significantly different between three groups(P>0.05),the jiont group had better results than those of other two groups in other indicators (P<0.05). CONCLUSION: Postoperative analgesia with Sufentanil combined with Dezocine for gynecology intravenous injection has good clinical effects.

Progress in clinical herb-drug interactions mediated by drug metabolism- related genes

GAO Li-chen, ZHANG Wei, LIU Zhao-qian, FAN Lan, ZHOU Hong-hao

2012, 17(3):  346-351. 

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Herbal medicines can be used for both prescriptions or food supplements with a wide range of applications.Inductive or inhibitive effects of herbal medicines on cytochrome P450 enzymes and drug transporters is the main mechanism that mediates herb-drug interactions and produces clinical toxicity. Herbal medicines could alter plasma exposure of substrate drugs for drug metabolizing enzymes or transporters by influencing the expressions and functions of drug metabolizing enzymes or transporters, perhaps resulting in unexpected clinical toxicity or therapeutic failure and leading to herb-drug interactions with clinical importance.Moreover, herb-drug interactions are in accordance with the gene-dosage rule, and therefore have genetic interindividual differences. Research progress of the clinical herb-drug interactions and related pharmacogenomics studies mediated by drug metabolism-related genes are reviewed in this article.

The physiology and pharmacology research puogression of T-ceu potassium channel

QIU Hong-xia, ZHAO Yin-huan, ZHU Gui-qi, ZHAO Hai-hui

2012, 17(3):  352-356. 

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The voltage-gated Kv1.3 channel and the Ca²⁺-activated IKCa1 K⁺ channel are expressed in T cells in a distinct pattern that depends on the state of lymphocyte activation and differentiation. The channel phenotype changes during the progression from the resting to the activated cell state and from naïve to effector memory cells. Kv1.3 and IKCa1 channel are related to the activation of T lymphocyte, and the specific K⁺ channel blockers can be used in the therapy of many diseases such as autoimmune diseases. In this article, we review the functional roles of these channels in both naïve cells and memory cells, describe the development of selective inhibitors of Kv1.3 and IKCa1 channels, and provide a rationale for the potential therapeutic use of these inhibitors in immunological disorders.

Latest development of Melia toosendan

SHI Deng, LIU Yan-ru, YANG Jian-yun, XIAO Bing-kun, HUANG Rong-qing

2012, 17(3):  357-360. 

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In this paper, the progresses about the identification,processing,chemical constituents,pharmacological action and toxicity of Melia toosendan are summarized , which could provide some useful information for further study and application of Melia toosendan.