Table of Content

Volume 18 Issue 2
26 February 2013

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Effect of natural borneol on the activities of cytochrome p450 isoforms in rats

WU Chun, GAO Jing-wen, YAO Mei-cun, HOU Xue-ying, ZHOU Yu-ting, DENG Xue-jiao, LIAO Qiong-feng, XIE Zhi-yong

2013, 18(2):  121-127. 

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AIM: To study the effect of natural borneol on the activities of cytochrome P450 enzymes CYP1A2, CYP2C6/11, CYP2E1 and CYP3A by a cocktail approach in rats. METHODS: The rats were randomly divided into two groups.One group of rats were treated with natural borneol suspension containing 0.8% CMC-Na (90 mg/kg) by intragastric injection once a day for 7 days.At the same time, the rats in the other group received 0.8% CMC-Na solution serving as control group.On the 8th day, all rats in each group were intravenously injected with cocktail probe drugs (10 mg/kg theophylline, 2.5 mg/kg tolbutamide, 10 mg/kg chlorzoxazone, 5 mg/kg dapsone).Blood samples were drawn into heparinized tubes at different time points.The plasma concentration of probe drugs were determined by ultra performance liquid chromatography (UPLC) and the main pharmacokinetic parameters were calculated by WinNonlin 5.0.1. RESULTS: In natural borneol group, the t_1/2, AUC_0-t, AUC_0-∞ and MRT_0-∞ of tolbutamide were significantly lower than those in Control group (P<0.05). There were no significant differences in the pharmacokinetic parameters of theophylline, chlorzoxazone and dapsone between control group and natural borneol group.CONCLUSION: Natural borneol can induce the activity of CYP2C6/11, but has no influence on the activities of CYP1A2, CYP2E1 and CYP3A.

Evaluation on the function of MRP1 in pulmonary epithelial cells by the efflux level of phenolsulfonphthalein

TAO Xiu-hua, WANG Dian-lei, CAO Yin, WANG Chen-yin, CHEN Jin-pei, YANG Li-li

2013, 18(2):  127-131. 

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AIM: To evaluate the function of MRP1 in pulmonary epithelial cells by the efflux level of substrate using phenolsulfonphthalein as MRP1 substrate and probenecid as MRP1-specific inhibitor. METHODS: The mouse was divided into the control group and inhibitor inhaled groups. The bronchoalveolar lavage fluid (BALF) and plasma samples were collected at 30 min after phenolsulfonphthalein (250 mg/kg) was administered to the control group mouse by intravenous injection. The inhibitor inhaled groups mouse was administered phenolsulfonphthalein (250 mg/kg) at 10, 30 and 60 min after inhaled probenecid (150 mg/kg), and the BALF and plasma samples were collected at 30 min after phenolsulfonphthalein administration. The phenolsulfonphthalein concentration in BALF and plasma was determined and the concentration of in BALF/plasma ratio was calculated.RESULTS: There was no difference in the plasma concentration of phenolsulfonphthalein between the control group and inhibitor groups. Compared with control group, the phenolsulfonphthalein concentration in BALF and the phenolsulfonphthalein concentration of in BALF/plasma ratio of the 60 min after inhaled probenecid group had significant difference.CONCLUSION: The efflux level of phenolsulfonphthalein in BALF could reflect the function of mouse pulmonary epithelial cells MRP1.

Experimental study of Yunnan hongyao and like product on repair-mechanism of endometrium in dysfunctional uterine bleeding rats

LV Xiao-bo, ZHOU Min, HUANG Chun-qiu, LIU Yun-mei

2013, 18(2):  132-136. 

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AIM: To study the effect of Yunnan hongyao and other 5 like products on VEGF and MMP-1 levels of uterine tissue in dysfunctional uterine bleeding (DUB) rats. And explore the repair-mechanism of endometrium of these drugs. METHODS: The models of DUB were established by administering intragastrically with mifepristone and misoprostol to pregnant rats. After management, the clotting time were observed, and the VEGF and MMP-1 levels of uterine tissue were determined with ELISA method. RESULTS: Compared with the model group, the clotting time were significantly decreased (P<0.01) in Yunnan hongyao and 5 like products groups. In addition, the level of VEGF of uterine tissue was significantly decreased and the level of MMP-1 was significantly increased in model group. Compared with the model group, the levels of VEGF were significantly increased in Yunnan hongyao,Gong xuening and Wujia shenghua groups (P<0.01 or 0.05), and the level of MMP-1 was significantly decreased in Yunnan hongyao+estradiol valerate group (P<0.05).CONCLUSION: Yunnan hongyao and 5 like products have significant therapeutic effect on DUB rats. Yunnan hongyao,Gong xuening and Wujia shenghua can repair endometrium. The mechanism is relevant to increasing the levels of VEGF.

Evaluation of pharmacokinetics and pharmacodynamics of acetylcysteine nanospheres in mice

WANG Fu-gen, SHEN Yi-qin, ZHUANG Rang-xiao, XI Jian-jun, FANG Hong-ying, XI Jian-jun

2013, 18(2):  136-141. 

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AIM: To evaluate the pharmacokinetics and pharmacodynamics of acetylcysteine nanospheres. METHODS: Two groups of NAC nanoparticles and free drug groups were injected into mouse tail vein. NAC was detected in plasma and different organs at different time. Chronic liver injury model was established by subcutaneous injection of carbon tetrachloride in rats. Different doses of NAC nanoparticles were administrated.Treatment of NAC nanospheres efficacy was evaluated on serum markers and indicators of liver tissue.RESULTS: Acetylcysteine nanospheres changed the distribution of drugs in the body.The results showed that drug concentration significantly increased in the liver tissue,half-life increased obviously. Pharmacodynamics result showed that the nanospheres can reduce serum markers and improve hepatic antioxidant function.Liver biopsy showed that the nanosphere treatment groups ameliorated hepatic steatosis, inflammatory and necrosis.CONCLUSION: The acetylcysteine nanosphere had obvious liver targeting, improving therapy for liver injure. Nanospheres are an ideal new formulations for acetylcysteine.

The level of anti-endothelial cell antibody and anti-β₂GP-Ⅰantibody in serum with systemic lupus erythematosus and the variation of human umbilical veins endothelial cell cultured in serum with SLE

ZHANG Meng-ying, LI Zhi, LV Kun, ZHONG Min, SUO Qi-feng, ZHONG Zheng-ling

2013, 18(2):  142-146. 

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AIM: To investigate the level of anti-endothelial cell antibody (AECA) and anti-β₂GP-Ⅰantibody in serum with systemic lupus erythematosus (SLE) and observe the variation of human umbilical veins endothelial cell(HUVEC) cultured in serum with SLE. METHODS: The level of AECA and anti-β₂GP-Ⅰantibody were detected by enzyme linked immunosorbent assay(ELISA) in serum with SLE and 40 healthy persons. Besides, the systemic lupus erythematosus disease activity index(SLEDAI)were collected for analyzing the relationship of the level of AECA and anti-β₂GP-Ⅰantibody and it. The HUVEC were cultured with the serum in SLE, and the influence of it were observed by methyl thiazolyl tetrazolium(MTT). RESULTS: The level of AECA and anti-β₂GP-Ⅰantibody in serum with SLE were significantly higher than that of control. The anti-β₂GP-Ⅰantibody was positive in 33 cases among 90 patients with SLE. The level of AECA and anti-β₂GP-antibody and SLE active index (SLEDAI) of 33 patients were respectively significant higher than that of 57 patients (P<0.01, P<0.05, P<0.05). There was a significantly positive correlation between the level of AECA and anti-β₂GP-Ⅰantibody(r=0.984, P<0.01).There was a positive correlation between the level of AECA and anti-β₂GP-Ⅰantibody with SLEDAI (P<0.05). The level of anti-β₂GP-Ⅰantibody was significant correlation with the index of PT (r=0.349, P<0.05). The proliferation of endothelial cells was inhibited by the serum of SLE with high level of AECA. There was no difference among three groups: the blank control group and the healthy group and the group with low AECA. The OD of group with the serum high expression of AECA was significantly higher than that of other groups (P<0.05).CONCLUSION: The level of AECA and anti-β₂GP-Ⅰantibody was correlative with the active of SLE. AECA can inhibit the proliferation of endothelial cell in vitro.

Study on the morphology of spinal cord contusion injury rats by early treatment with erythropoietin

GU Bing, WANG Shuo-yu, LI Hua-nan, WANG Jun, ZHANG Shui-yin

2013, 18(2):  147-155. 

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AIM: To study the morphological and behavior changes of spinal cord contusion rats by early treatment with erythropoietin(EPO). METHODS: Spinal cord contusion injury model in rats was duplicated with a Benchmark^TM stereotaxic cortical impactor. Posttraumatic 30 min, animals were administrated by 5000UI·kg^-1·BW recombinant human erythropoietin or equal volume of saline through intraperitoneal injection. The inclined plane test and BBB scale were used to assess the hindlimb motor function. Morphological changes were inspected by using the Harris HE staining method combining with Luxol fast blue staining and Nissl staining. Blood routine test and hemorheology were to monitor the effect of erythrocytic hyperplasia.RESULTS: With the increase in training days the angle sustaining on the inclined plane and BBB scores of EPO group were significantly higher than that of model group(P<0.05). Posttraumatic 7,14,28 days the cavity size of injured center and adjacent parts in EPO group were significantly reduced. The numbers of survival neuron in the bilateral anterior horn of gray matter at 3 mm, 5 mm rostral and candual to the injury site in EPO group were statistically more than those in model group (P<0.05). Posttraumatic 14 and 28 days the LFB-positive area at injured site and 3mm, 5mm rostral and candual to epicentre in EPO group were significantly higher than those in model group (P<0.05). After injury the red blood cell count, hemoglobin and hematocrit showed a clear gradual upward trend. From posttraumatic 14 days the whole blood low-shear viscosity, middle-shear viscosity significantly increased compared with the model group (P<0.05).CONCLUSION: Early treatment with EPO may promote neuronal survival and reduce the loss of myelin sheath to mitigate secondary damage, and ultimately improve the hindlimb motor function, but increased the risk of hematogenic adverse reactions.

Effects of portulaca total flavone on proliferation of vascular smoothmuscle stimulated by PDGF-BB

LU Xin-hua, HUANG Huang, TANG Bing, DENG Hua-fei, WANG Gui-xia, ZUO Ke-qiang, LI Jian, HE Jun-shan

2013, 18(2):  156-160. 

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AIM: To study the effects of portulaca total flavone (PTF) on proliferation induced by PDGF-BB of rabbit aortic smooth muscle cells(VSMCs)and explore its mechanisms. METHODS: The VSMCs of cultured organization-adherence was induced to proliferate by PDGF-BB, and effects of PTF on VSMCs was tested by cell counting method and 3H-thymidine (3H-TdR) incorporation test; The effect of PTF on cell proliferative cycle of VSMC was observed by flow cytomytry technique;The intra-cellular calcium concentration was investigated by fluorimetry.RESULTS: PTF inhibited the proliferation of VSMCs induced by PDGF-BB in a dose dependent manner,and DNA symthesis,the cells numbers of G₁/G₀ phase were increased and that of G₂/S phase were decreased markedly(P<0.01).CONCLUSION: Proliferation of VSMCs induced by PDGF-BB can be inhibited by PTF.The mechanisms may be related with diminished VSMCs [Ca²⁺]_i.

Oridonin induces MDA-MB-231 cells apoptosis through PI3K/Akt pathway in vitro

WANG Ming, ZHANG Yao, XIE Xiang-rong, QI Zhi-lin, BI Fu-yong

2013, 18(2):  161-165. 

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AIM: To research the proliferation inhibitory effect of oridonin on human breast cancer MDA-MB-231cells and explore the mechanism of the inhibitory effect. METHODS: MDA-MB-231 cells were incubated with oridonin in vitro. Morphological changes of MDA-MB-231 cells induced by oridonin for 24 h were observed by invert microscrope. The cell viability rate was evaluated by MTT assay. The cell apoptotic rate was evalutated by flow cytometry (FCM). The apoptosis associated protein level of procaspase-3, PARP,Akt, p-Akt, p-GSK 3β was examined by Western blotting. RESULTS: The apoptosis phenomenon of MDA-MB-231 cells induced by oridonin for 24 h could be observed. The apoptosis phenomenon of 24 μmol/L group was more obvious than other groups. The cell viability rate induced by 6,12,24 μmol/L oridonin was decreased and apoptotic rate was increased in a time- and dose-dependent manner (P<0.01). Oridonin cleaved PARP which is the substrate of caspase-3 in a dose-dependent manner(P<0.05). Oridonin also down- regulated the protein level of procaspase-3, phospho-Akt(p-Akt) and phospho-GSK3β(p- GSK3β) in a dose-dependent manner(P<0.05).CONCLUSION: Oridonin can inhibit the proliferation of human breast cancer MDA-MB-231 cells and induce cell apoptosis by inhibiting PI3K/Akt pathway.

In vitro inhibitory effect of papain on blood coagulation function and the related mechanism

XU Wei-hong, LV Yuan-dong, TAO Ping-hua, WU Guo-you, YU Wei, HU Xi-lia

2013, 18(2):  166-170. 

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AIM: To observe the in vitro effect of papain on blood coagulation function, and to explore the possible mechanism. METHODS: Human platelet poor plasma (PPP) and platelet rich plasma(PRP) were mixed with different dose of papain which were assigned into three groups (group 0 U/L, group 10 U/L and group 20 U/L). PPP and PRP were measured for prothrombin time(PT) and actvated partial thromboplastin time (APTT) with blood coagulation analyzer, the PPP was also measured for Ca²⁺ and activity of coagulable factor V, VII, VIII, IX, X and XI(FV:C、FVII:C、FVIII:C、FIX:C、FX:C and FXI:C) with blood-gas analyzer and blood coagulation analyzer, respectively. Fresh blood from volunteers was mixed with the three dose of papain, the clotting time(CT) was detected with silicified tube method. The PPP with 0, 20, 40,60 and 80 U/L of papain also was measured for PT and APTT.RESULTS: At group 10 U/L papain and group 20 U/L papain, PT and APTT of PPP and PRP as well as CT of whole blood was significantly higher, but FV:C and FVIII:C activity was remarkably lower than that at group physiological saline solution and group 10U/L papain, respectively. There was no statistical difference for PT and APTT between PPP and PRP at the three groups, for Ca²⁺ concentration and other four coagulable factors activity between the three groups one another. Either PT or APTT level at group 0,20, 40,60and 80U/L of papain showed positive correlation with papain dose. CONCLUSION: Papain has dose-dependent inhibitory effect on blood coagulation mainly through inhibition of coagulable facor V and VIII activity. Papain has the efficacy of anticoagulation

Study on pharmacodynamic effects of Xing di ke chuan ning capsule

PAN Mei, LI Meng-lin, LIANG Bin, ZHANG Yong-ping, TANG Jing-wen, XIE yu, ZHONG Zheng-ling, ZHANG Li-li

2013, 18(2):  170-174. 

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AIM: To evaluate relieving cough and phlegm, antiasthmatic and anti-inflammatory effects for Xing di ke chuan ning capsule. METHODS: Pharmacological effects of relieving cough and phlegm, antiasthmatic and anti-inflammation were evaluated by animal model which involed ammonia induced cough, tracheal phenol red method, capillary glass tube expectoration of apricot, xylene induced ear swelling method, carrageenan-induced rat paw edema and so on.RESULTS: Xing di ke chuan ning capsule could relieve cough and phlegm, increase apparently expectoration action, and relieve airway spasm,it would also inhibit inflammation induced xylene and carrageenan acetic acid. CONCLUSION: Xing di ke chuan ning capsule showed better effects of relieving cough and phlegm, antiasthmatic and anti-inflammation.

Statistical considerations of group sequential design in oncology clinical trials

GUO Yang, JIANG Zhi-wei, XIA Jie-lai, WANG Yu-kun

2013, 18(2):  175-180. 

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The group sequential design is a good choice of oncology trial design because of the smaller sample size and the probability of early stopping for efficacy/futility. To design and apply the group sequential trials scientifically, we illustrate how to choose the number, timing of interim analysis, alpha spending function and optimal trial parameters by employing Monte Carlo simulation. The simulation results show that the three-stage design of 2∶1∶1 time point, whose expected sample size is 420.53, is the best choice in the group sequential design. And the expect sample size is only 420.53. Among the five α spending functions proposed by Lan and DeMets, the 1.5th power and quadratic α spending function, which have the smallest expect sample size of 393 cases, are better than O'Brien-Fleming and Pocock design.

Bioequivalence study of endogenous drugs by iodine preparations

WANG Xin-gang, HUANG Yu-rong, LI Quan-sheng, SI Duan-yun

2013, 18(2):  181-185. 

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AIM: To study the bioequivalence of endogenous drug of iodized lecithin. METHODS: The endogenous and other sources (diet) iodine need to be controled. By a two-period cross-over tria1, a total of 24 healthy volunteers were randomized to two groups to receive 9 iodized lecithin tablets (test or reference formulation). The concentrations of iodized lecithin in serum or urine were determined by arsenic-cerium catalytic spectrophotometric method. The pharmacokinetic parameters were measured by DAS2.1.1 software.RESULTS: The value added of the average net concentration of blood iodine are 16.8% (test formulation) and 19.0% (reference formulation), and the recovery rate of urinary iodine are 84.5% and 83.3%.The net excretion of urinary iodine were subtracted from the amount obtained on the drug dosing day, and the bioequivalence analysis was done according to the baseline-adjusted parameters (Ae_{0-24 h}: cumulative urinary excretion from 0 to 48 hours,R_max: maximal rate of urinary excretion). The test and reference preparations of iodized lecithin were bioequivalent.CONCLUSION: It is a complicated design for the study of the bioequivalence of endogenous drug. Various kinds of in vivo and in vitro factors have a great influence on the result, and background need to be deducted.

Laryngeal mask insertion conditions at different target plasma concentrations of propofol combined with dexmedetomidine

ZHONG Jun-feng, HU Shuang-yan, LI Yu-hong, CHEN Nian-ping

2013, 18(2):  186-189. 

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AIM: To compare the laryngeal mask insertion conditions at different plasma target concentrations (Cp) during the induction of anesthesia with target-controlled infusion (TCI) of propofol combined with dexmedetomidine. METHODS: Seventy-five ASA I-II patients of both sexes aged 20-60 years, weighing 50-80 kg, in which the use of laryngeal mask was indicated were randomly divided into 3 groups (n=25) according to Cp of propofol set during induction of anesthesia: 2.0, 2.5 and 3.0 μg/mL.Dexmedetomidine 0.6 μg/kg was infused over 10 minitues. Then,TCI propofol was given by Diprifusor (Graseby 3500 infusion pump).Laryngeal mask was inserted when the effect-site concentration (Ce) of propofol reached the settled Cp. Laryngeal mask insertion conditions (jaw mobility,coughing,head and limb movement,laryngeal spasm) were assessed. SBP, MAP, HR and BIS value were recorded at four time points:baseline before induction (T₀), instant before laryngeal mask inserted (T₁), 1 min (T₂) and 3 min (T₃) after insertion of laryngeal mask. Changes of SBP, MAP and HR between T₁ and T₀ were calculated. The number of patients with apnea and apnea times were recorded. The administration of atropine and ephedrine was also recorded. RESULTS: The levels of SBP, MAP and HR were decreased with increasing depth of anesthesia in the 3 groups.The decline rates of SBP, MAP and HR after induction had significantly differences in group III than those in group I and II (P<0.05). BIS value was similar in all groups. The insertion conditions were significantly better in group II and III than that in group I. More patients developed apnoea and their apnoea times were longer in group III than the other two groups (P<0.05). More patients were administrated with atropine and ephedrine in group III compared with the other two groups (P<0.05).CONCLUSION: Induction of anesthesia with dexmedetomidine 0.6 μg/kg combined with TCI of propofol with Cp set at 2.5 μg/mL is satisfactory for laryngeal mask insertion in terms of cardiovascular stability and insertion conditions.

Serum IL-21 levels in patients with chronic hepatitis C and clinical significance of IL-21

PAN Qing-chun, YU Yong-sheng, TANG Zheng-hao, XI Min, ZANG Guo-qing

2013, 18(2):  190-194. 

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AIM: To determine serum interleukin-21 (IL-21) level and evaluate the roles of IL-21 in chronic hepatitis C (CHC). METHODS: Serum IL-21 levels of 27 CHC patients and 10 control subjects were determined by enzymelinked immunosorbent assay (ELISA) and the relationship between serum IL-21 levels and HCV-RNA, the live biochemical parameters were studied. RESULTS: Serum IL-21 levels in CHC patients were significantly higher than those in control subjects (P<0.01). Especially, CHC patients with elevated alanine aminotransferase (ALT) have higher IL-21 than patients with normal ALT. There were highly significant positive associations between serum IL-21 and ALT (r=0.647, P<0.01) as well as aspartate aminotransferase (AST) (r=0.591, P<0.01). But no association was observed between IL-21 and HCV-RNA. CONCLUSION: IL-21 is a cytokine involved in HCV-associated liver pathological damage and may be an available marker to evaluate hepatic inflammation for CHC.

Effects of azithromycin on lung function and serum CTGF of asthma patients

ZHENG Mei-mei, WANG Fang-jian, YUE Tie-gang, DONG Li-yan, DUAN Cheng-cheng

2013, 18(2):  194-197. 

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AIM: To observe the clinical efficacy of azithromycin on bronchial asthma, and the effects on lung function, serum connective tissue growth factor (CTGF). METHODS: 48 cases of asthma were randomly divided into conventional treatment group (group A), azithromycin in treatment group (group B). Two groups were inhaled budesonide, group B was given azithromycin additional, 18 healthy people were distributed to control group (group C).The level of serum CTGF was detected by enzyme-linked immunosorbent assay (ELISA).The changes of asthma control test(ACT) scores,lung function, serum CTGF were evaluated in each group patients before and after treatment.RESULTS: After 8 weeks treatment, the levels of ACT scores, lung function were significantly improved than before treatment, but the serum CTGF concentrations were decreased in group A and B(all P<0.05). After 8 weeks treatment,compared with group A,the levels of ACT scores,lung function were significantly increased in group B, but the CTGF serum concentration was decreased(all P<0.05). CONCLUSION: Azithromycin can inhibit airway remodeling, improve lung function and control asthma,the reason may be related to inhibiting the expression of CTGF.

Effects of pioglitazone combined with atorvastatin on lipids and endothelial function in patients of type 2 diabetes mellitus

HE Chun-ling, XING Wen, LU Ke-bing, XIA Li-bin, WANG An-cai

2013, 18(2):  198-201. 

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AIM: To observe the effects of pioglitazone combined with atorvastatin on lipids and endothelial function in patients of type 2 diabetes mellitus. METHODS: 65 cases of type 2 diabetes patients were randomly divided into two groups, 30 cases were divided into control group (Group A), receiving routine hypoglycemic therapy with atorvastatin 10 mg/d; the experimental group (Group B), 35 cases on the basis of the control group with pioglitazone 15 mg/d.The levels of blood glucose, Glycated hemoglobin, lipids, nitric oxide (NO) , endothelin -1 (ET-1) and the change rate of brachial artery flow mediated dilatation(FMD)were assessed before and after 12 weeks of the treatment. RESULTS: Compared with pre-treatment,the levels of blood glucose after treatment were significantly decreased in two groups (P<0.01). there was no significant difference between two groups (P>0.05). The ET-1 levels in two groups were decreased (P<0.05), and the levels of nitric oxide (NO) and FMD were increased in two groups,compared with pre-treatment,there was significant difference(P<0.01).However, the levels of nitric oxide (NO) and the change rate of brachial artery flow mediated dilatation(FMD) in Group B were higher than those in Group A, there was significant difference in two groups(P<0.05).After treatment,the BMI was improved in patients of two groups (P<0.05, P<0.01).CONCLUSION: Pioglitazone combined with atorvastatin can adjust blood lipids and improve the function of vascular endothelium in type 2 diabetes mellitus

Effects of intramuscularly injected methoxamine on tourniquet deflation induced hemodynamic changes in patients with lower limb surgery

SHAN Li-xin

2013, 18(2):  202-204. 

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AIM: To study the effect of intramuscularly injected methoxamine on blood pressure, pulse and cardiac output fluctuation induced by turiquet deflation in orthopaedic patients. METHODS: 60 patients scheduled for lower limb surgery with toumiquet were selected and randomly divided into two groups, each group with 30 patients. Patients in methoxamine group received intramuscular injection methoxamine 3 mg before the surgical skin saturation. Patients in control group received the same volume of nomal saline. In the following time points baseline level (T₀),before the surgical skin suturation (T₁), and 1 min(T₂), 3 min(T₃) and 5 min (T₄) after the toumiquet deflation ,the hemodynamic parameters systolic blood pressure(SBP),diastolic blood pressure(DBP) ,heart rate(HR) and cardiac output (CO) were measured. RESULTS: There was stable HR, blood pressure and cardiac output after the toumiquet deflation in methoxamine group. Whearas, a decreased BP and CO and faster HR were observed in control group. There were statistical significance on BP and HR between two groups.CONCLUSION: Intramuscularly injected methoxamine could effectively prevent cyclic changes induced by tourniquet deflation in patients with lower limb surgery, keep relatively stable haemodynamics.

Research progress on the PK evaluation of anti-cancer nano-preparation

LUO Dan, ZHANG Jing-wei, ZHOU Fang, WU Xiao-lan, WANG Guang-ji

2013, 18(2):  205-211. 

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The poor water-solubility and pharmacokinetics of anticancer drugs will cause significant problems during clinical application.Developing nano-preparations is a reliable and safe way to improve the water solubility and pharmacokinetics of anticancer drugs, which possesses a promising prospect in both research and application in recent years. On the basis of recent studies, the pharmacokinetics of nano-preparation in vivo and in vitro and the mechanisms underlying the advantages of nano-preparations are reviewed in this paper.

The role of the endoplasmic reticulum chaperone tapasin in mediating specific CTL responses

TANG Yu-yan, CHEN Xiao-hua, YU Yong-sheng

2013, 18(2):  212-216. 

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The clearing of virus and tumor cell a large degree relied on Specific CD8+ cytotoxic T lymphocytes (cytotoxic T cell, CTL). CTL recognised virus peptide paragraph through T cell receptor (TCR) and caused infection cell melting through MHC-I class molecular presenting. The assembly of classic MHC-I molecular composition in endoplasmic reticulum (ER) required antigen peptide ligand and beta 2m,and this process need chaperones such as tapasin. Tapasin was offspring of transporters associated with antigen processing (TAP) and a member of the immunoglobulin superfamily as well as MHC-I. Tapasin as molecular bridges between TAP and MHC-I, have an important role in mediated specific CTL reactions. This review resumes its biological characteristics, the role in mediated specific CTL reactions and contacting with diseases.

Effect of electronic data capture system in new drug clinical trials

LENG Wen-yu, JIANG Zhi-wei, YU Li-li, LI Chan-juan

2013, 18(2):  217-221. 

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With the developments of computer and net technology, the superiorities of Electronic Data Capture(EDC) system are increasing in clinical trials and it is getting popularity in trial participants. With the help of the excellent technologies, EDC simplifies the trial process of traditional paper CRFs and overcomes the lags of data entry and data cleaning. The roles and responsibilities of sponsors, monitors and data managers change. Meanwhile, EDC makes it feasible to apply new trial designs and statistical methods, such as, adaptive design.

Research progress on relationship between eNOS and ACE gene polymorphisms and coronary heart disease

FANG Chao, ZENG Hui, ZHOU Hong-Hao, LIU Zhao-Qian

2013, 18(2):  222-228. 

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Coronary heart disease (CHD) is one of the most serious disease that affects human health and life. It is also a public health problem concerned worldwide. The nitric oxide synthase (eNOS) and angiotensin-converting enzyme (ACE) have an important influence on the cardiovascular system in vivo. The genomics study found that the eNOS and ACE gene polymorphism correlate with the occurrence of CHD. This article covers the progress between eNOS and ACE gene polymorphism and coronary heart disease susceptibility.

Research progress of glucagon-like peptide-1 and analogues on blood pressure

CHEN Yong-fei, SHAO Hua, YU Feng

2013, 18(2):  228-233. 

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Glucagon-like peptide-1 (GLP-1) is an incretine, which lowers blood glucose dependently on ambient glucose concentration, and its analogues have been used for treatment of type 2 diabetes mellitus. Recent findings including preclinical and clinical studies have demonstrated that GLP-1 and its analogues may have blood-pressure-lowering effect by inhibiting the proximal tubular sodium reabsorption and thereby increasing urinary excretion of sodium, or via an endothelium-independent mechanism.This review summarizes the recent findings regarding the antihypertensive effects of GLP-1 and its analogues.

Pharmacogenetic progress of rosuvastatin in atherosclerosis

BAO Mei-hua, ZHANG Yi-wen, CHENG Lin, ZHOU Hong-hao

2013, 18(2):  234-240. 

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Hypercholesterolemia plays a key role in the initiation and progression of atherosclerosis. Rosuvastatin is widely used to prevent cholesterol synthesis. There are great individual differences in pharmacokinetics and pharmacodynamics characters in clinical use of rosuvastatin.Pharmacogenetics indicates that genetic polymorphisms of drug transporters, metabolizing enzymes, and receptors play very important roles in the metabolism and therapeutical efficacy of rosuvastatin. In this review, we summarized the effects of genetic polymorphisms of certain drug transporters, CYP450 enzymes or other related genes on the pharmacokinetics and pharmacodynamics of rosuvastatin.It will provide part of the basis for personalized medicine of rosuvastatin.