Loading...
Welcome to Chinese Journal of Clinical Pharmacology and Therapeutics,Today is Share:

Table of Content

    Volume 18 Issue 3
    26 March 2013
    Advances on biological characteristics of PXR and its effect on drug metabolism
    CHEN Qun, XU Zhe, SUN Hua, XIE Hai-tang
    2013, 18(3):  241-246. 
    Asbtract ( 237 )   PDF (351KB) ( 276 )  
    References | Related Articles | Metrics
    The nuclear pregnane X receptor(PXR) is a kind of hormones and environmental receptors and is widely distributed in organism.PXR not only involved in the metabolism of energy,cholesterol,bile acids and other substances as well as regulation of the inflammatory response,and also regulates phase Ⅰ,Ⅱ phase drug metabolizing enzymes and the related the expression of drug transporters. It is important for the body to maintain a variety of physiological functions such as cell proliferation and differentiation, growth and development, metabolism, homeostasis.This paper reviewed the PXR structure and function, biological effects and the regulation of drug-metabolizing enzymes and drug transporters.
    Effects of a new the retinoic acid derivatives ATPR on proliferation and differentiation of SKOV3 tumor cell
    WU Fan-rong, HONG Fan-qing, CHEN Fei-hu
    2013, 18(3):  247-251. 
    Asbtract ( 219 )   PDF (539KB) ( 250 )  
    References | Related Articles | Metrics
    AIM: To explore the effect of the 4-amino-2-trifluoromethyl-phenyl retinate(ATPR) on the proliferation and differentiation of SKOV3 tumor cell in vitro.METHODS: Cell proliferation was assessed by MTT assay and growth curve of cells; morphologic changes were observed after Giemsa staining using inverted phase contrast microscope; CA125 were measured by ELISA; the cell cycle were analyzed by Flow Cytometry (FCM).RESULTS: The growth of SKOV3 cells was inhibited in a does-dependent manner after the treatment with ATPR. The phanero depressant effect appeared at 48 h, but it was significant after 72 h. Cell morphous was observed to be mature in inverted microscope. The content of CA125 decreased. The proportion of cells in G0/G1 phase increased while the cells in S phase decreased. Cell cycle progression was blocked in the G0/G1 phase.CONCLUSION: ATPR could inhibit the proliferation and induce differentiation in some degree. The direction of differentiation is still need further study.
    Hippocampal nNOS-neuronal regeneration pathways mediates the effect of 5-serotonin antidepressive drugs
    WU Hai-yin, ZHANG Jing
    2013, 18(3):  252-257. 
    Asbtract ( 222 )   PDF (475KB) ( 248 )  
    References | Related Articles | Metrics
    AIM: To explore the antidepressive mechanism of serotonin reuptake inhabitor and selective 5-HT1A receptor agonist.METHODS: Fluoxetine, a serotonin reuptake inhibitor, and 8-OH-DPAT, a selective 5-HT1A receptor agonist, were infused into the dentate gyrus (DG) of bilateral hippocampus of nNOS knockout and wild-type mice by stereotactic surgery. Brdu immunohistochemisty was performed to detect neurogenesis as well as novelty suppressed feeding test, forced swimming test and tail suspending test were used to measure depression-related behavior.RESULTS: Both selective infusion of fluoxetine and 8-OH-DPAT into hippocampus up-regulated neurogenesis and generated antidepressant- like effect, which were dependent on the function of nNOS.CONCLUSION: nNOS-neurogenesis cascade in the hippocampus mediates the antidepressive effect of serotonin reuptake inhabitor and selective 5-HT1A receptor agonist.
    Effects of naloxone on the expressions of JNK3 protein in rats after ischemia-reperfusion
    TIAN He-ping, CHU Zheng-min, JIN Cheng-shen, SHEN Jian-guo
    2013, 18(3):  258-262. 
    Asbtract ( 179 )   PDF (402KB) ( 189 )  
    References | Related Articles | Metrics
    AIM: To investigate the effect of naloxone on the expression of JNK3 protein in Hippocampus during transient focal cerebral ischemia reperfusion, and to discuss the probable mechanism of its protective effect.METHODS: The model of focal cerebral ischemia-reperfusion injury was established in rats by suture-occluded method. Rats were randomly divided into several groups, including Sham-operation, ischemia-reperfusion, low dose naloxone treated ischemia-reperfusion, high dose naloxone treated schemia-reperfusion, SP600125 treated ischemia-reperfusion and respective Vehicle treated ischemia-reperfusion. The infarction volume was detected by TTC staining. Western Blot was operated to detect expression of p-JNK3 in Hippocampus.RESULTS: Both groups of high dose naloxone treated ischemia-reperfusion and SP600125 treated ischemia-reperfusion, not only ischemia-reperfusion infarction volume was reduced, but also expression of p-JNK3 was down-regulated, compared with ischemia-reperfusion only group. As the dose increase, the effect of naloxone on inhibiting expression of p-JNK3 was obviously improved.CONCLUSION: Naloxone inhibits the expression of p-JNK3 in a dose-dependent manner during focal ischemia reperfusion which may be one of the mechanisms of its neuroprotective function.
    Effects of crocetin on ulcerative colitis in rats and the mechanism
    TAO Yun, GONG Guo-qing, QIAN Zhi-yu, CHENG Wen-yuan, WANG Xin-hui
    2013, 18(3):  263-270. 
    Asbtract ( 199 )   PDF (608KB) ( 240 )  
    References | Related Articles | Metrics
    AIM: To determine the effect of crocetin on ulcerative colitis(UC)induced by tri-nitrobenzene sulfonic acid(TNBS)in rats, and to explore the possible mechanism.METHODS: UC was induced by TNBS and ethanol in rats. After crocetin was given orally, the colon mucosa damage idex and histopathological score were determined, and the levels of MPO,MDA and SOD were measured. Tumor necrosis factor-α(TNF-α) and Interleukin-1β(IL-1β) in colon were detected by enzyme-linked immunosorbent assay(ELISA). Toll-like receptor4(TLR4) mRNA and nuclear factor-κBp65(NF-κBp65) mRNA expression were examined by Q-PCR. Immunohistochemistry staining was used to observe the expression of TLR4 and NF-κBp65.RESULTS: Crocetin greatly attenuated the severity of colonic gross lesions and reduced the histopathological scores. MPO activity and MDA concentration in colon were significantly increased,SOD activity was reduced in UC rats.Crocetin ameliorated these changes. Crocetin reduced the levels of TNF-α and IL-1β in colon. The expression of TLR4 and NF-κBp65 in colon were attenuated by crocetin.CONCLUSION: Crocetin can effectively attenuate the inflammatory reaction in UC rats,which may be due to the antioxidation and the inhibition of TLR4/NF-κB signal pathway.
    Effects of Naringin on expression of COX-2 mRNA and protein in Human ovarian cancer cell line SKOV3
    SONG Shu-hui, HU Xin, XIONG Yu-qing, CAI Li-ping
    2013, 18(3):  271-275. 
    Asbtract ( 187 )   PDF (315KB) ( 162 )  
    References | Related Articles | Metrics
    AIM: To investigate effects of naringin on expression of COX-2 mRNA and protein of Human ovarian cancer cell line SKOV3.METHODS: SKOV3 cells were cultured in vitro and divided into five groups randomly, namely control group, naringin group (10 μmol/L), naringin group (20 μmol/L), naringin group (40 μmol/L) and celecoxib group (80 μmol/L). The inhibition effects of naringin on cell- proliferation were determined by MTT method. The expression of COX-2 mRNA and protein were evaluated by Western Blot and Real-time quantitative PCR after forty-eight hours.RESULTS: Naringin could inhibit the growth of SKOV3 cells, and with the increase of the dosage and time, the tumor growth inhibition rate increased significantly (P<0.01).Compared with control group,the expression of COX-2 mRNA was down-regulated significantly by every dosage of naringin and celecoxib (0.828±0.006, 0.753±0.011, 0.412±0.216, 0.321±0.017). Meanwhile, the expression of COX-2 protein was down-regulated significantly by every dosage of naringin and celecoxib (1.7925±0.088, 1.2225±0.0822, 1.2725±0.07632, 0.3075±0.0977).CONCLUSION: The appropriate dosage of naringin can inhibit SKOV3 cells growth in vitro, and can down-regulate the expression of COX-2 mRNA and protein.
    The united effects of photodynamic therapy and aoup yanghetang upon SIL-2R of the rats with diabetic foot
    HU Zhu-hong, ZHU Ya-nan, NI Hai-yang, WEI Jia-ping
    2013, 18(3):  276-281. 
    Asbtract ( 189 )   PDF (255KB) ( 183 )  
    References | Related Articles | Metrics
    AIM: To observe the united effects of photodynamic therapy and soup yanghetang upon soluble interleukin-2 receptor (SIL-2R) of the rats with diabetic foot.METHODS: On the basis of diabetes model by STZ, to establish diabetic foots model through swimming, ice-cubed reducing the heat and liquid nitrogen freezing, which took about 3 weeks divide experimental model of rat into six groups in which 2 groups were respectively treated by He-Ne laser and improved dressing, only He-Ne laser, only improved dressing and Mupirocin, while the model group and normal group had no treatment. Every group was 10 respectively.RESULTS: There were significant difference with changes in the body weight of rats, the amount of drinking water, the score of diabetic foot and the results of blood rheology prompted the group of photodynamic therapy and soup yanghetang with other treatment group. The united effects of photodynamic therapy and soup yanghetang to SIL-2R was distinguished from the normal group, the model and the other the treatment groups (P<0.01). However, it had no difference from the photodynamic therapy group (P>0.05).CONCLUSION: The method of the photodynamic therapy diabetic and improved dressing on diabetic foots treatment has the lowest sIL-2R and the most significant ulcer healing. It may provides experimental proof and theoretical basis to further clinic treatment, which has increased a medical treatment and technological method in order to treat diabetic foots.
    Experimental study on anti-tumor activity of extracellular polysaccharides from Trichoderma pseudokoningii
    LI Li-hua, CHEN Kao-shan, YU Li-zhen, BU Xiao-yang
    2013, 18(3):  282-285. 
    Asbtract ( 219 )   PDF (228KB) ( 216 )  
    References | Related Articles | Metrics
    AIM: To study antitumor effect of extracellular polysaccharides from Trichoderma pseudokoningii.METHODS: In vitro, we studied the antitumor activity of TPeps on human leukemia HL-60 cells with MTT, and in vivo, TPeps were intragastrically given to mice with S180 solid tumor at the dose of 50, 100 and 200 mg·kg-1·d-1. Normal sodium and cyclophosphamide were taken as blank control and positive control respectively. The tumor weight, spleen index, thymus index and the relative growth rate were measured.RESULTS: TPeps could significantly inhibit HL-60 cells proliferation in a time and concentration dependent manner. Meanwhile, compared with control TPeps three dose groups significantly decreased the weight of tumor, increased the spleen index and thymus index(P<0.05,P<0.01). However, TPeps had no discernible effect on the relative growth rate.CONCLUSION: TPeps have a certain amount of anti-tumor action.
    Explore on the effects of General Friedman's Urn Model on power in clinical trial through simulation experiments
    YU Li-li, BU Xiao-dong, GU Xin, DU Qian, XIA Jie-lai
    2013, 18(3):  286-289. 
    Asbtract ( 227 )   PDF (187KB) ( 241 )  
    References | Related Articles | Metrics
    Urn model is a most commonly used randomization method of adaptive design. In this article, with some true data from the clinical trial of a new drug treating oral ulcer, the generalized Friedman's urn model was used to calculate the allocation proportions between the two treatments groups, and simultaneously, the influence of the allocation proportions on the power of statistical test were explored trough computer simulation experiments. It was showed in the results that the effects of response adaptive randomization on power was not as serious as we assumed, because the allocation proportions between the two treatments groups is usually less than 3∶1 for most clinical trials. We hope this study can provide some references for the application of urn model in practical clinical trials.
    Pharmacokinetics of Alvimopan capsules in healthy Chinese volunteers
    LI Xiao, GUO Xin, LIU Zhi, YU Peng, MA Yue-hui, CHENG Ze-neng
    2013, 18(3):  290-296. 
    Asbtract ( 256 )   PDF (628KB) ( 275 )  
    References | Related Articles | Metrics
    AIM: To study the pharmacokinetics of Alvimopan and its metabolite ADL 08-0011 in Chinese healthy volunteers after single and multiple oral administrations of Alvimopan capsules.METHODS: This study contains 24 healthy adult subjects totally. 12 healthy adult subjects (6 males, 6 females) were randomly grouped by 3×3 Latin square. Three single doses of Alvimopan capsules, 6 mg, 12 mg, 18 mg, were given to each group at each period to make each group take each dose once after three periods. After three periods, the 12 subjects were given multiple doses of Alvimopan capsules at 12 mg (bid) for 6 days.The resting 12 subjects were given single highest dose of 24 mg. The plasma concentrations of Alvimopan and ADL08-0011 were measured by a validated LC-MS/MS method and the pharmacokinetic parameters were calculated using WinNonlin 6.1.RESULTS: The linear range of Alvimopan was 0.192-75 μg/L(r=0.9986). Results of methodology validation-specificity, precision,accuracy and average recovery-fit the requirements of sample determination. The main pharmacokinetic parameters of Alvimopan after single dose administration (6, 12, 18 and 24 mg) were Cmax: (8.79±6.10), (18.30±9.92), (31.48±13.68) and (32.91±17.95) μg/L; Tmax: (1.4±0.6), (1.8±0.6), (1.8±0.6) and(2.1±0.6) h; AUClast:(33.2±23.0), (60.3±28.9), (94.1±42.2) and (112.0±57.5)μg·h·L-1; t1/2: (8.4±4.9), (8.4±5.3), (7.9±4.8) and (10.0±4.3) h; CL/F: (218.1±111.8), (234.7±135.7), (217.6±95.3) and (256.9±132.5) L/h. Multiple administration (12 mg bid)pharmacokinetic parameters were: Cmax: (16.57±10.15) μg/L, Tmax : (1.6±1.0) h, AUClast: (64.4±32.0) μg·h·L-1, t1/2 : (12.0±3.3) h and CL/F (258.4±109.4) L/h.CONCLUSION: Determination method is convenient, sensitive and suitable for the pharmacokinetics investigation. The pharmacokinetics of Alvimopan in Chinese healthy volunteers exhibits linear behavior in dose range of 6 - 18 mg. But pharmacokinetic nonlinearity was observed when dose up to 24 mg.
    Simultaneous determination of thiamphenicol and its prodrug thiamphenicol glycinate in human plasma and its pharmacokinetics study
    YAN He-feng, ZHOU Cheng-lin, HAN De-en
    2013, 18(3):  297-301. 
    Asbtract ( 189 )   PDF (438KB) ( 213 )  
    References | Related Articles | Metrics
    AIM: To develop a simple and sensitive HPLC method for simultaneous determination of thiamphenicol (TAP) and its prodrug thiamphenicol glycinate (TG) in human plasma.METHODS: A single (0.5, 1.0, and 1.5 g) intravenous drip doses of thiamphenicol glycinate was performed on 24 Chinese healthy volunteers randomly. The plasma was treated with ethyl acetate.The chromatographic condition was as follows:a column of Hypersil ODS2(5 μm, 4.6 mm×200 mm),a mobile phase consisting of acetonitrile-water containing 0.003 mol/L tetrabutyl ammonium bromide and 0.056 mol/L ammonium acetate (13∶87, pH=6.6) at a flow rate of 1 mL/min with UV detection at 224 nm.RESULTS: The calibration curves of TAP and TG were all linear ranging from 0.78 to 100 μg/mL in plasma and the intra-day and inter-day relative standard deviations were all less than 15%.TAP was stable in plasma samples after extraction or in two freeze-thaw cycles or in 4 h at ambient temperature or at -70 ℃.CONCLUSION: The method is sensitive, accurate, simple, fast and is suitable for the pharmacokinetics study of TAP and TG.
    PhaseⅠ clinical trail tolerance of pegylated recombinant human granulocyte colony-stimulating factor injection
    SUN Cheng-chun, WANG Bao-cheng, BI Jing-wang, LV Wei-wei, HU Jun-li, KANG Chang-qing, ZHANG Li-zhi
    2013, 18(3):  302-306. 
    Asbtract ( 375 )   PDF (278KB) ( 311 )  
    References | Related Articles | Metrics
    AIM: To evaluate the safety and tolerance of PEG-rhG-CSF in tumor patients, and to explore its efficacy of enhancing absolute neutrphil count(ANC).METHODS: This study was open-labeled, dose-escalation trial. All patients received 1 day chemotherapy. Patients received a single injection of PEG-rhG-CSF(30,60,100,150, or 200 μg/kg) 48 h after administration of chemotherapy drug. Each dose group had 3 patients.RESULTS: All the 15 patients enrolled were evaluable for safety and efficacy of PEG-rhG-CSF. Main adverse events related to PEG-rhG-CSF were fatigue(4/15), musculoskeletal pain(1/15). All adverse events were mild, and they were reversible without treatment. PEG-rhG-CSF enhanced ANC in a dose-dependent manner to some extent.CONCLUSION: PEG-rhG-CSF is well tolerated, with no serious adverse event in this trial.
    Effect of β3-adrenergic receptor gene Trp64Arg polymorphism on uric acid levels in a Chinese male type 2 diabetes mellitus population
    HUANG Qiong, ZHANG Liu-fu, CHENG Yan, SI Li, WEI Wei
    2013, 18(3):  307-311. 
    Asbtract ( 196 )   PDF (278KB) ( 274 )  
    References | Related Articles | Metrics
    AIM: To investigate the association of β3-adrenergic receptor gene Trp64Arg polymorphism with hyperuricemia in a Chinese male type 2 diabetes mellitus patients population.METHODS: 196 hyperuricemic and 196 normouricemic male subjects were genotyped in this study. Body mass index (BMI), waist to hip ratio (WHR), systolic blood pressure (SBP), diastolic blood pressure (DBP), serum uric acid, urea nitrogen, creatinine, triglyceride, total cholesterol, low-density lipoprotein-cholesterol (LDL-C), high-density lipoprotein-cholesterol (HDL-C), fasting plasma glucose (FPG), postprandial plasma glucose (PPG) were detected.RESULTS: We found patients with different Trp64Arg genotype showed significant differences in average uric acid concentrations (599.53±113.70 vs 529.78±81.10 vs 507.33±74.27, P<0.01) among CC, CT and TT genotype and there were significantly higher average uric acid concentrations in Trp64Arg TC+CC genotype individuals (557.95±99.91 vs 503.47±69.40 μmol/L, P<0.01) than those TT genotype subjects in the hyperuricemic group.CONCLUSION: Trp64Arg polymorphism was associated with hyperuricemia in a Chinese male population with type 2 diabetes mellitus.
    Correlation between serum concentration of platelet derived growth factor and intracerebral hemorrhage
    SUN Zhu-liang
    2013, 18(3):  312-316. 
    Asbtract ( 216 )   PDF (416KB) ( 259 )  
    References | Related Articles | Metrics
    AIM: To observe the dynamic changes of serum levels of platelet derived growth factor (PDGF) in the patients with intracerebral hemorrhage.METHODS: A total of 78 patients with intracerebral haemorrhagia (internal capsule) were enrolled in this study. The serum PDGF was determined by enzyme-iineked immunosorbent assay (ELISA). The degree of neural function defect was analysed by NIHSS appraise. The perihematomal edema volumes was evalulated by CT. The expression of PDGF in platelets was detected by flow cytometric analysis.RESULTS: The serum concentration of PDGF was significantly higher than that in control group (P<0.01). The PDGF level of intracerebral haemorrhagia group was increased remarkebly within 4 days. The expression of PDGF in platelets was also increased remarkebly as that in serum. The PDGF level was decreased remarkebly in the 8th day in intracerebral haemorrhagia group (P<0.05), and which was positively correlated with NIHSS appraise (r=0.62,P<0.01). The serum level of PDGF protein was positive associated with the value of hematoma (P<0.05).CONCLUSION: Increased PDGF level was found in the patients with intracerebral hemorrhage. The serum PDGF levels of patients with cerebral hemorrage may be used as a biomarker to reflect the degree of pathogenetic.
    Randomized study of thalidomide in combination with TP chemotherapy for the treatment of advanced non-small-cell lung cancer
    PENG Ye, WANG Mei-qin, XIE Na, LI Yan, LU Hai-yan, LI Bing-mao
    2013, 18(3):  317-321. 
    Asbtract ( 201 )   PDF (300KB) ( 208 )  
    References | Related Articles | Metrics
    AIM: To evaluate the efficacy and safety in the patients with advanced non-small cell lung cancer (NSCLC), treated with thalidomide combined with paclitaxel plus cis-platinum (TP) chemotherapy.METHODS: 110 patients with stages ⅢB and Ⅳ NSCLC were divided randomly into two groups, the trial and the control groups. The trial group were treated with thalidomide and TP chemotherapy, in which thalidomide was given 100 mg per night for the first week and then added to 200 mg per night for 3 months if tolerable. The control group were treated with TP chemotherapy only. All patients were treated primarily and received treatments for at least two periods, 21 days for one period.RESULTS: Of 110 assessable patients, the overall response rate was 41.18% in the trial group and 37.74% in the control group (P>0.05). The clinical benefit rate was 86.27% in the trial group and 69.81% in the control group (P<0.05). Besides, the trial group indicated considerable improvement as compared with the control group in the increased appetite rate, weight gain rate and the KPS score improvement rate. The median PFS was 7.45 (5-26) months for the trial group, and 5.77 (4-20) months for the control group (P<0.05); The median OS was 12.88 (6-26) months for the trial group, and 11.32 (5-21) months for the control group (P<0.05).The Ⅲ -Ⅳ grade untoward effects were rare in both groups.Nausea,vomiting of Ⅲ-Ⅳ grade incidence in the treatment group was significantly lower than the control group (P=0.03). But there were no significant differences in the remaining toxicities between the two groups (P>0.05). The most common untoward effects of thalidomide, somnolence and constipation, were rare (incidence rate 10%-30%).CONCLUSION: Though without considerable improvement in short term efficacy, TP regimen combined with thalidomide with high safety significantly improve clinical benefit rate, quality of life and free survival in patients with advanced NSCLC. Therefore the treatment of TP regimen combined with thalidomide deserves clinical popularization.
    Clinical observation of CO2 laser combined with ALA photodynamic therapy for recurrent perianal Condyloma Acuminatum
    WANG Jun, LIU Wei-bei, CI Chao, CHANG Xiao-li, HE Cai-feng, QIANG Di, HANG Shou-yun, JI Bi-hua
    2013, 18(3):  322-324. 
    Asbtract ( 294 )   PDF (219KB) ( 636 )  
    References | Related Articles | Metrics
    AIM: To investigate the efficacy of CO2 laser combined with ALA photodynamic therapy for recurrent perianal Condyloma Acuminatum.METHODS: Forty-six patients with perianal Condyloma Acuminatum were randomly divided into two groups, experimental group for the CO2 laser combined with ALA photodynamic therapy (ALA-PDT), first with CO2 laser dispel wart body, exposing out photodynamic laser treatment, once a week for three consecutive times; control group for the CO2 laser treatment group, visually the wart was completely cleared.One week after the treatment for efficacy evaluation,all patients were followed up to evaluate the recurrence rate within 3 months after treatment.RESULTS: After treatment, the warts were completely disappear, the recurrence rate of experimental group and control group was 19%,65%,respectively.CONCLUSION: CO2 laser combined with ALA photodynamic therapy for recurrent perianal Condyloma Acuminatum is safely and effectively, can reduce the relapse rate.
    Histone demethylase JMJD1A and its biological functions
    ZHAN Min, ZHOU Hong-hao
    2013, 18(3):  325-330. 
    Asbtract ( 230 )   PDF (296KB) ( 237 )  
    References | Related Articles | Metrics
    Histone demethylase JMJD1A (Jumonji domaincontaining protein 1A) regulates gene transcription by hydroxylation pathway, which demethylases mono- and di-methy H3K9 (H3K9me1/2). JMJD1A play roles in spermatogenesis, energy metabolism, regulation of stem cell as well as the initiation and progress of cancer. Here, we review the structure, catalytic mechanism, substrate specificity, biological function and inhibitor of JMJD1A.
    Translation initiation factors and abnormalities of translation control in tumors
    SHEN Jie, XIE Hai-tang, LIU Zhao-qian
    2013, 18(3):  331-338. 
    Asbtract ( 270 )   PDF (537KB) ( 317 )  
    References | Related Articles | Metrics
    Maintenance of cell homeostasis and regulation of cell proliferation depend importantly on regulating the process of protein synthesis. Most translational controls occur during the initiation phase of protein synthesis recruiting several translation initiation factors (eIFs), with the initiation factors being the major target of regulation through their phosphorylation. When the process of protein synthesis is hyper-activated, abnormalities in the phosphorylation, expression and degradation were frequently observed, leading to an imbalance of cellular proteins that promotes cell proliferation and malignant transformation. This occurs, for example, when the cap-binding protein, eIF4E, is overexpressed, or when the methionyl-tRNAi-binding factor, eIF2, is too active, and when eIF3 hyper-activated. The importance of eIFs as regulators of protein synthesis and cell proliferation makes them potential therapeutic targets for the treatment of cancer. This review focuses on eIFs and mechanisms of translational control and how disregulation results in cell malignancy.
    Inhibitor of thrombin, bivalirudin
    HE Yan, WANG Liang-you
    2013, 18(3):  339-343. 
    Asbtract ( 220 )   PDF (227KB) ( 336 )  
    References | Related Articles | Metrics
    Bivalirudin was approved by US Food and Drug Administration as a new direct inhibitor of thrombin in 2000, the drug was currently approved the application to PCI / PTCA, HIT / HITTS, ACS etc. Existing research shows bivalirudin have a better security and can be used for the classic treatment regimens ( heparin and glycoprotein IIb/IIIa inhibitors ) alternative treatment, Moreover, it can reduce the risk of bleeding and mortality. This paper analysis the mechanism of action, pharmacokinetics, pharmacodynamics, clinical application, safety and cost-effectiveness of bivalirudin. But it limited in application in the domestic market, thus strengthening the clinical trails research is promising.
    The relationship between main transporter pharmacogenetics and statin efficacy
    WANG Li-ping, SONG Jin-chun
    2013, 18(3):  344-350. 
    Asbtract ( 247 )   PDF (673KB) ( 278 )  
    References | Related Articles | Metrics
    Organic anion-transporting polypeptide 1B1 and breast cancer-resistance protein are the important transporters in human, participating in absorption, distribution and excretion of many substances including statins. However, researchers had paid more attention on the metabolic enzymes in the pharmacokinetics and pharmacodynamics, the studies on transporters is lagged behind of metabolic enzymes. With the development of science, we got to focus on the role of transporters on the statin toxicity recently. This paper is to review the relationship between the main transporter pharmacogenetics and statin efficacy.
    Apparent pharmacogenetics in antihypertensive therapy
    KUANG Ze-min, HUANG Zhi-jun, YANG Guo-ping, YUAN Hong
    2013, 18(3):  351-355. 
    Asbtract ( 257 )   PDF (256KB) ( 249 )  
    References | Related Articles | Metrics
    With the development of pharmacogenetics,people gradually realize that gene polymorphism cannot fully explain the antihypertensive drugs curative effect of individual differences. At the molecular level,many antihypertensive drugs related metabolic enzyme,receptors,transporter are subject to the influence of the regulation of gene expression,and play an important role in differences of antihypertensive treatment. Therefore, from the perspective of epigenetics genetic factors and the relationship between the antihypertensive drugs,will help to better explain the clinical drug reaction from the individual differences. This review summarizes the DNA methylation,histone modification and microRNAs,apparent genetic control way for antihypertensive related drugs coding genetic effects.
    Study on the relationship between thyroid hormones and hepatic insulin resistance
    JIANG Li, HE Bi-xia, DING Qi-long
    2013, 18(3):  356-360. 
    Asbtract ( 174 )   PDF (224KB) ( 478 )  
    References | Related Articles | Metrics
    Insulin resistance means the peripheral target tissue and cells of insulin have a decreased effect on endogenous or exogenous insulin sensitivity and reactivity, leading to physiological dose of insulin producing physiological effects below normal and appearing clinical manifestations of hyperinsulinemia, high blood sugar, high blood pressure, high cholesterol and other metabolic disorders. The normal thyroid function status is an important factor to maintain the normal glucolipid metabolism and insulin sensitivity and thyroid hormone levels are important in the formation of hepatic insulin resistance. This article summarizes the present study of the relationship between thyroid hormones and hepatic insulin resistance, aiming to provide a systematic and fundamental document for the follow-up research.