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Welcome to Chinese Journal of Clinical Pharmacology and Therapeutics,Today is Chinese

Table of Content

    Volume 19 Issue 9
    26 September 2014
    Effects of siRNA silencing COX-2 gene on VEGF-C expression and cell migration in SGC-7901 cells
    LUO Hui-ying, YANG Lin, WANG Xiao-peng, SU He, LIU Ying, MA Yun-tao, WU Zi-yan
    2014, 19(9):  961-966. 
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    AIM: To investigate the effects of using RNA interference to silence the expression of COX-2 gene on the expression of VEGF-C and cell migration. METHODS: Using siRNA interference the COX-2 gene in gastric carcinoma cell line SGC-7901, and RT-PCR and immunofluorescence detect the expression of COX-2 and VEGF-C gene,comparison the effect COX-2 gene on cell migration by cell scratch test.RESULTS: COX-2 gene and VEGF-C gene were significantly reduced in mRNA and protein levels after the silence of COX-2 gene in gastric cancer cell line SGC-7901,with statistically significant difference between groups (P<0.05). The expression of COX-2 was closely correlated with the expression of VEGF-C(P<0.05); the migration ability of gastric cancer cells also decreased. CONCLUSION: In gastric carcinoma cell SGC-7901, siRNA can inhibit the COX-2 expression,and COX-2 gene could enhance the migration ability of gastric cancer cells.The silence of COX-2 gene could download the expression of VEGF-C,reduce the migration ability of gastric cancer cells, therefore reducing the metastasis of gastric cancer cell.
    Infusion receptor eDR4/iFas enhances TRAIL-induced apoptosis of HT-29 cells
    LI Zhao-fa, WANG Cong-yang, DENG Xiao-ying, HUI Er-jing
    2014, 19(9):  966-972. 
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    AIM: To investigate the effect of sTRAIL combined with infusion receptor eDR4/iFas on apoptosis of HT-29 cells. METHODS: In this study, eDR4 and iFas genes were amplified respectively by PCR and used to generate fusion gene named eDR4/iFas by splicing overlap extension PCR. eDR4/iFas was cloned into the expression vector with the tumor-specific survivin promoter, and expressed sTRAIL with constitutive promoter CAG. After treatment with eDR4/iFas and sTRAIL, the cell viability analysis of both colorectal cancer cells HT-29 and human embryonic kidney cells HEK293 was assayed by MTT. Both TRAIL mRNA and protein expressions were detected with RT-PCR and ELISA respectively. The apoptosis of HT-29 cells was analyzed by Hoechst staining. RESULTS: In HT-29 cells, cell survival rate in sTRAIL group was 40.9%±18.7%, while cell survival rate in eDR4/iFas+sTRAIL group was 21.6%±9.1%, there was significant difference between the two groups (P<0.05). CONCLUSION: The results have revealed that eDR4/iFas can improve TRAIL-induced apoptosis of HT-29 cells, has no toxicity for HEK293 cells.
    Mfn2 gene transfer inhibites neonatal rat cardiomyocytes apoptosis induced by ischemia/reperfusion via activation of the Ras-PI3K-Akt signaling pathway
    ZHOU Jie, YAN Ling, HUANG Duo-xin
    2014, 19(9):  973-978. 
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    AIM: To investigate the effect of Mfn2 gene transfer on inhibiting the apoptosis of cardiomyocytes induced by ischemia/reperfusion. METHODS: Treating neonatal rat cardiomyocytes by hypoxia/reoxygenation to simulating myocardial ischemia/reperfusion injury. And then the cardiomyocytes were infected by adenovirus-mediated Mfn2 (Adv-Mfn2). TUNEL staining, cell death ELISA and FACS analysis were used to investigate the role of Adv-Mfn2 gene transfer on neonatal rat cardiomyocytes apoptosis. Western blot was used to analyze the protein expression of Bcl-2, Bax, cleaved caspase-9 and p-Akt. RESULTS: TUNEL staining evidenced that there were less positive-apoptoic cardiomyocytes in Adv-Mfn2 group than in H/Re group and Adv-LacZ group (P<0.01). ELISA and FACS results showed that cardiomyocytes apoptosis in Adv-Mfn2 group was significantly reduced compared with H/Re group and Adv-LacZ group, and this effect was time-dependent (P<0.01). The protein expression of Bcl-2 and phosphorylated Akt were significantly upregulated in Adv-Mfn2 group (P<0.05), whereas Bax and cleaved caspase-9 protein expressions were significantly downregulated in Adv-Mfn2 group (P<0.05). CONCLUSION: Mfn2 gene promotes the protein expression of Bcl-2 and phosphorylated Akt, supppres the protein expression of Bax and cleaved caspase-9 via activation of the Ras-PI3K-Akt signaling pathway to inhibite neonatal rat cardiomyocytes apoptosis induced by ischemia/reperfusion.
    Anticancer effects of hyperoside on human gastric cancer cells and its mechanisms
    SUN Shi-hua, JIANG Rong-hua, ZHU Hai-yan, JIANG Jian-jun
    2014, 19(9):  979-983. 
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    AIM: To observe the effects of hyperoside on the cell proliferation, cycle and apoptosis of human gastric cancer cell line BGC-823 and to explore its possible mechanisms. METHODS: The effects of hyperoside on the proliferation of BGC-823 cells were evaluated by MTT assay. Flow cytometry was used to analyze the cell cycle and apoptosis of the cells exposed to hyperoside. The activities of caspase 3, caspase 8 and caspase 9 were examined by spectrophotometry. RESULTS: With the hyperoside incubation for 24 h or 48 h resulted in a significant inhibition of proliferation in BGC-823 cells as a IC50 of 32.14 μg/mL and 22.67 μg/mL. After treatment with hyperoside,the cell cycle was suppressed obviously at G0/G1 phase. The apoptotic rates were significantly higher in the cells treated with hyperoside than in the control. Comparing with the control, the activities of caspase 3, caspase 8 and caspase 9 were up-regulated in hyperoside group. CONCLUSION: Hyperoside have significant anti-gastric tumor effects by induce cell cycle arrest and apoptosis of BGC-823 cells, and intracelular caspase 3, caspase 8 and caspase 9 are closely associated with the apoptosis.
    Protection of losartan on cultured rats hippocampal neurons odels of hypoglycemia anoxia injury in vitro
    CHEN Jiang-ying, YAN Zhen-wen, ZHANG Su-ping, YIN Yi-chen
    2014, 19(9):  984-987. 
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    AIM: To study the effects and possible mechanisms of losartan on cultured rats hippocampal neurons models of hypoglycemia anoxia injury in vitro. METHODS: The hippocampal neurons were cultured in vitro,and then cells were randomly divided into the hypoxic ischemic injury group,losartan low-dose group,losartan high-dose group.The cell model of hypoxic ischemic was established by oxygen-glucose deprivation mimicking cerebral hypoxic ischemic injury.Neuron apoptosis in hippocampus tissue were determined with Tunel staining.The expression levels of active-caspase-3 protein were observed by Western blot analysis.RESULTS: 12 h deprivation of oxygen-glucose induced cell apoptosis of hippocampal neurons. Cell apoptosis and expression of active caspase-3 were significantly decreased in pre-treatment losartan group.CONCLUSION: Losartan had protective effects on cultured hypoxic ischemic hippocampal neurons of rats.The mechanisms may be related with resisting apoptosis and caspase related pathway.
    Effects of platelet inhibitor from Agkistrodon halys venom on artery thrombosis in rabbit
    JI Na, ZHANG Gen-bao, HUANG Lu, WANG Fei, ZHANG Ya, WU Juan
    2014, 19(9):  987-990. 
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    AIM: To explore the effects and possible mechanism of platelet inhibitor from Agkistrodon halys venom (AHV-PI) on artery thrombosis in rabbit. METHODS: Thirty rabbits were divided into control group, artery thrombosis model group and AHV-PI (0.2 mg/kg) group (n=10) randomly. The model of rabbits carotid artery thrombosis was induced by infiltering 70%FeCl3.The blood was taken from another carotid artery after 1 hour.Automatic coagulation analyzer was used to determined the APTT,PT,TT and the content of fibrinogen(FIB).The plasma content of plasmin was determined by Enzyme-Linked Immunosorbnent Assay (ELISA). RESULTS: Compared with control group, significantly shortened APTT, PT, TT and reduced plasmin level were observed in artery thrombosis model group (P<0.05), while the level of FIB in plasma was increased (P<0.05). Obviously prolonged APTT and TT, reduced FIB (P>0.05) and plasmin level were discovered in AHV-PI group as compared with model group, while PT had no difference (P<0.05).CONCLUSION: AHV-PI can prevent the artery thrombosis.The mechanism may be related to plasminogen activation.
    Protection and mechanism of extract of Phyllanthus emblica L. on focal cerebral ischemia-reperfusion injury in rats
    CHEN Chuang
    2014, 19(9):  991-994. 
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    AIM: To study the protection and mechanisms of extract of Phyllanthus emblica L.(EPE) on focal cerebral ischemia-reperfusion injury in rats. METHODS: The cerebral ischemia-reperfusion rats' models were created by the middle cerebral artery occlusion by modified suture method. The neurological function scores were observed, the infarct size was measured by TTC staining, and the contents of SOD, MDA, NO, IL-1β, IL-6, iNOS and NF-κB in brain tissue were measured. RESULTS: Compared with the model group, EPE could significantly reduce the neurological function scores, decrease the cerebral infarct size, increase the activity of SOD, and reduce the contents of MDA, NO, IL-1β, IL-6, iNOS and NF-κB in brain tissue. CONCLUSION: EPE has significant protection on cerebral ischemia-reperfusion injury in rats due to increases the antioxidant activity and inhibit inflammatory reaction.
    Correlation effect change of internal environmental in prostate antigen protein induced SD rat prostatitis
    ZHOU Li, WANG Yong, LUO Yong-wei, WANG Rong, MENG Xiang, JIA Yu-ling, LIU Xiang-yun, SUN Zu-yue
    2014, 19(9):  995-1000. 
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    AIM: To explore the internal environment correlation prostate antigen protein induced SD male rats with chronic prostatitis. METHODS: 30 male rats were randomly divided into 3 groups, each one contained 10 ones. One was negative control group; the other two groups were the experimental group. 20, 40 mg/mL of rat prostate protein purification liquid combined with complete freund's adjuvant (1∶1 mixed suspension) were injected respectively in SD rats by multipoint intradermal injection at 0, 7 days and 0.5 mL of DPT vaccine was injected by intraperitoneal injection. At 21 days, 0.5 mL 20, 40 mg/mL of rat prostate protein purification liquid combined with complete freund's adjuvant were injected respectively in SD rats by intradermal injection. The negative control group was injected by equal dose of normal saline at the same time and place. RESULTS: Histopathological analyses indicated that there was inflammatory infiltrates in the experimental groups prostate stromal, which showed obvious chronic inflammation. Immune factors of chronic nonbacterial prostatitis can lead to IgG concentration increased significantly (P<0.05), CRP and PSA levels increased significantly (P<0.05). CONCLUSION: According to the experimental results, chronic non-bacterial prostatitis induced by prostate antigen protein lead to IgG concentration, CRP and PSA levels increased significantly.
    Protective effect of hydroxy safflower yellow A on myocardial ischemia
    DONG Wen-bin, YE Xiao-di, CHENG Min, WANG Jun-qing, ZHENG Gao-li
    2014, 19(9):  1001-1005. 
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    AIM: To investigate the protective effects of hydroxy safflower yellow A (HSYA) on myocardial ischemia. METHODS: Myocardial ischemia and blood stasis models were used to observe the effects of HSYA on myocardial ischemia, hemoreology changes and blood coagulatory function in rats. RESULTS: Myocardial ischemia experiment showed that HSYA could reduce the area of myocardial infarction, the level of serum CK-MB and LDH, and the blood viscosity and platelet aggregation had been reduced, while the values of PT and APTT had been prolonged. Blood stasis experiment showed that HSYA could reduce blood viscosity, inhibit platelet aggregation, and the values of PT and APTT had been prolonged. CONCLUSION: HSYA has protective effect on myocardial ischemia, the effect is related to improve hemorheology and blood coagulatory function.
    The efficacy of Fructus Tribuli extract JL201 on type 2 diabetes and its potential mechanisms
    ZHAO Bao-sheng, LI Peng-shou, ZHANG Shu-yuan, LI Chun-na, LIU Yang-yang, SHI Xiao-juan, XU Tun-hai, LIU Tong-hua
    2014, 19(9):  1006-1010. 
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    AIM: To observe the effect of Fructus Tribuli extract (NO. JL201) on the concentration of fasting plasma glucose, blood insulin, TNF-α, IFN-β and that of TLR3, TLR4 mRNA in islet cell on spontaneous type 2 diabetes KKAy mice, and explore its potential hypoglycemic mechanisms. METHODS: Mice were randomly allocated into 5 groups: control group, JL201 high -dosage group (20 mg/kg BW), JL201 middle -dosage group (10 mg/kg BW), JL201 low-dosage group (5 mg/kg BW), and positive drug metformin group (400 mg/kg BW). Body weights, food and water intake and fasting plasma glucose (FPG) were measured weekly. Mice were sacrificed after 4 weeks administration to obtain the blood sample and measured the concentration of FPG and insulin (Ins), and calculated the sensitivity of Ins in mice. The concentrations of TLR2, TLR4 mRNA in Islet cell were measured using realtime-PCR method.RESULTS: Different concentration of JL201 reduced the intake of food and water respectively. In addition, the concentration of FPG decreased significantly (P<0.05 or P<0.01) and the concentration of serum Ins also lowed (P<0.05 or P<0.01). However, the sensitivity of Ins increased significantly (P<0.05) and the secretion of TNF-α, IFN-β reduced. At the same time, JL201 could decrease the concentration of TLR2, TLR4 mRNA spontaneously. CONCLUSION: JL201 has beneficial effects on hypoglycemic and strengthening the sensitivity of Ins. Besides, it also can improve polydipsia and polyphagia clinical symptoms. The potential beneficial effects may be associated with decreasing islet cell TLR2, TLR4 mRNA levels and inhibiting inflammation.
    Experimental study of a metabolic syndrome mouse model induced by high sucrose-containing drinking water
    SHEN Ji-zhong, LIU Hang
    2014, 19(9):  1011-1015. 
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    AIM: To establish a mouse model with metabolic disorders similar to human metabolic syndrome (MetS) by induced with long-term 32% high sucrose-containing drinking water. METHODS: All male/female mice (3 weeks of age) were divided into two different groups randomly (n=10):control group and sucrose water (SW) group. Control group was received chow diet plus plain water, while SW group were received chow diet plus 32% sucrose water. At 24 weeks of age, oral glucose tolerance test (OGTT) were conducted to assess glucose handling ability of mice. Then, body weight, body length and waist circumference was measured in live mice, blood samples were collected from the orbital vein of experimental animals for measuring blood biochemical index. Then, mice were sacrificed and different parts of the adipose tissue were weighted and recorded. RESULTS: Compared with control mice, SW mice emerged a profound central obesity body characteristics. Based on the SW mice blood biochemical index examination, we found that SW mice have emerged glucose and lipid metabolism disorder. OGTT results suggest that: glucose processing capabilities of SW mice has shown a significant decline.For insulin metabolism, SW mice had significant hyperinsulinemia and insulin resistance.CONCLUSION: High sucrose water-induced MetS mice model well mimic the pathophysiological characteristics of MetS in humans. It is a readily available and low-cost animal model of MetS, and will provide a platform for the new therapeutic drugs of MetS.
    Preliminary study of the CYP2C19 genotype in the application of Chinese herbal medicine metabolism screening
    CHEN Wang, WEN Chun-jie, FU Li-juan
    2014, 19(9):  1016-1020. 
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    AIM: To determine the constants of enzyme kinetics and drug inhibition of the three CYP2C19 genotype(CYP2C19*1, CYP2C19*2, CYP2C19*3),and study the impact of CYP2C19 genetic polymorphism in drug metabolism in vitro. METHODS: In the study the CEC (3-cynao-7-ethoxycoumarin) as a CYP2C19-specific fluorescent substrate used for enzymatic reaction and detected CYP2C19 genotype activity, in addition, the nonlinear regression method to calculate the enzymatic kinetic parameters(Km value, Vmax of the value and intrinsicclear rate Clint value).Then, enzyme inhibition reaction analysis the inhibitory effect of 19 kinds of Chinese herbal medicine on the CYP2C19 genotypes, which by combined of fluorescent substrate CEC and herbal material, as well as other experimental conditions in vitro, and calculate the IC50 values.RESULTS: The screening experiment results showed that: CYP2C19 involved in the metabolism of substrates and known inhibitors all were its inhibitor, majority of Chinese medicine monomer weak or no inhibitory effect on CYP2C19; chemical structure or similar drugs with similar therapeutic effects on inhibition of CYP2C19 different;the same drug inhibitied different genotypes were not the same result,evern a larger difference.CONCLUSION: Establish an efficient, stable, and easy fluorescent high-throughput drug screening platform, it bulited a basement applied before the metabolic nature of innovative drugs or new drug lead compounds for clinical screening and predictive for late-stage study,providing experimental basis for the clinical potential drug interactions.
    Evaluation of warfarin anticoagulant management by clinic pharmacists on patients with cardiac valve surgery
    LIU Jun, XU Hang
    2014, 19(9):  1021-1024. 
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    AIM: To explore the effect of anticoagulant management by clinic pharmacists on increasing the efficacy of anticoagulant therapy with warfarin used in patients with cardiac valve surgery. METHODS: 203 patients undergone cardiac valve surgery who received anticoagulant therapy with warfarin in Nanjing Drum Tower Hospital from June 2012 to December 2012 were enrolled in the study group. As well,212 patients with cardiac valve surgery from January 2010 to December 2010 were in the control group. In the study group,all the patients were received anticoagulant management and health education by clinic pharmacists,the differences between the total international normalized ratio (INR) target rate of warfarin,the INR target rate before discharge,the time to first INR in the target,the occurrence rate of hemorrhage and thrombosis in the two groups were compared. The patients in the study group were received questionnaire survey and compared the differences in the scores of admission and before discharge. RESULTS: The total INR target rate in the study group were significantly higher than those in the control group(P=0.010),and the time to first INR in target was shorter than that in the control group(P=0.043). In the study group,the scores of patients before discharge were significantly higher than those of admission(P<0.001).CONCLUSION: Clinic pharmacists to participate in the anticoagulant management and systemically anticoagulant health education on patients can obviously enhance the efficacy of warfarin therapy and the patients' anticoagulant knowledge,which contributes to improving the patients' compliance.
    Effects and safety of Xinmaining for cerebral infarction treatment:a systematic review
    LI Lin, HUANG Ji-han, ZHANG Guang-min, LIU Chuan-gui, ZHANG Ping, XIE Xue-feng, HUANG Xiao-hui
    2014, 19(9):  1025-1032. 
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    AIM: To conduct a meta-analysis to evaluate the efficacy and safety of Xinmaining for cerebral infarction. METHODS: CBM, CNKI,WanFang Data, Cochrane Library, MEDLINE, EMbase were electronically searched for randomized controlled trials (RCTs) involving Xinmaining in the treatment for cerebral infarction. Meanwhile, all relevant Chinese and English literatures were retrieved by hand search. Stata 11.0 was used for Meta analysis.RESULTS: A total of twenty three randomized controlled trails involving 2737 patients were included . Clinical assessment measures were total response rates, neurological deficit scores, changes of hemorheology and blood lipids. The result of meta-analysis (twenty two trials) showed that there was significant difference on total response rates[RR=1.14,95%CI(1.11,1.18)]; Xinmaining group was superior to the control group in lowering WBLSV,WBHSV,plasma viscosity, HCT ,fibrinogen and WBRV; Xinmaining group showed better results in decreasing TC and TG and increasing HDL-C; Mild adverse effects were reported in only three patients of one trial.CONCLUSION: Current evidences showed that xinmaining could increase the total response rates, reduce the neurological deficit scores, decrease the hemodynamic indexes and improve the blood lipid parameters with a low incidence of adverse effects,which provides a good application prospect in clinical practice. However,the quality of current clinical trials was not high, more high-quality RCTs were needed to provide clear evidences for the efficacy and safety of Xinmaining for cerebral infarction.
    Effects of different end-tidal sevoflurane concentration on cisatracurium produced neuromuscular blockade in elderly patients
    XIANG Xiao-bing, LIAN Yan-hong, WU Ying-li, YUAN Xiao-hong, LIU Zhao-fang
    2014, 19(9):  1033-1036. 
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    AIM: To discuss the effects of different end-tidal sevoflurane concentration on cisatracurium-produced neuromuscular blockade in the elderly. METHODS: Forty-five patients of ASAⅡ-Ⅲ undergoing abdominal surgery were randomly divided into three groups with 15 cases each,all patients were received general anesthesia. Anesthesia with propofol infusion (group P),0.5MAC sevoflurane (group S1) or 1.0 MAC sevoflurane inhalation (group S2) respectively. Group P,routine intravenous anesthesia induction,injectioned cisatracurium 0.15 mg/kg after anesthesia induction,and intubation was performed as soon as the T1 fell below 5%; group S1,inhalated 8% sevoflurane firstly,and regulated inhalation concentration to make the end-tidal sevoflurane concentration 0.5MAC,others same with group P; group S2,the end-tidal sevoflurane concentration 1.0MAC,others same with group S1. After performed tracheal intubation,groups to receive propofol TIVA(group P)or inhalation sevoflurane(group S1,group S2),the end-tidal sevoflurane concentration of group S1 was 0.5MAC,the end-tidal sevoflurane concentration of group S2 was 1.0MAC. The intubation time,the onset time,no-response time,the time of T1 5% recovery,the time of T1 25% recovery,the time of T1 75% recovery,recovery index,the 0.70 recovery time of TOF(T4/T1) and hemodynamic effects were recorded. RESULTS: There were no significant differences in the intubation time,the onset time and hemodynamics among three groups (P>0.05). Compared with group P,the time of T1 25% recovery was significant longer in group S1 (P<0.05). No-response time,the time of T15% recovery and the time of T1 25% recovery were significant longer in group S2 (P<0.05). Compared with group S1,the time of T1 25% recovery was significant longer in group S2 (P<0.05). Compared with group P,the time of T1 75% recovery,the 0.70 recovery time of TOF and recovery index were significant longer in group S1,S2 (P<0.05). Compared with group S1,the time of T1 75% recovery and the 0.70 recovery time of TOF in group S2 were longer(P<0.05). CONCLUSION: Sevoflurane inhalation can significantly enhance the neuromuscular block effect of cisatracurium in dose-dependent manner for the elderly, but the onset time is similar.
    Effect and safety of bevacizumab with chemotherapy as first-line and second-line therapy for metastatic colorectal cancer patients
    ZHU Li-ming, ZHOU Chen-xi, ZHAO Ya-zhen, LIU Lu-ying, XU Qi, YING Jie-er, ZHONG Hai-jun
    2014, 19(9):  1037-1041. 
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    AIM: After approval of bevacizumab in Chinese, postmarketing surveillance studies reported on efficacy and safety was rare. We evaluated the efficacy and safety of bevacizumab for metastatic colorectal cancer patients in daily practice. METHODS: All unresectable metastatic colorectal cancer patients who began receiving bevacizumab in participating facilities from October 2010 to April 2013 were retrospectively analyzed for efficacy and safety. Response Evaluation in Solid Tumors criteria,version 1.1, was used for the tumor response rate. The Kaplan-Meier method was used to determine PFS and OS. Adverse events were assessed by the National Cancer Institute Common Terminology Criteria for Adverse Events. RESULTS: A totalof 74 patients were assessed. Response rates were 62.8%, 28.6% overall among patients re-ceiving bevacizumab as first-,second-line therapy. Median progression-free survival was 8,7,4.4 months,and median overall survival was 25.3, 14.6 months, respectively. All grade adverse events related to bevacizumab included hypertendion in 9.5%, proteinuria in 8.1%, thrombosis in 2.7%,gastrointestinal perforation in 2.7%,poor wound healing in 4.1% and bleeding in 17.6%. CONCLUSION: Although the sample size was small and there were several study limitations, these results suggest that colorectal cancer patients in our center benefit from bevacizumab in combination with chemotherapy and might safely in daily practice.
    Tacrolimus pathways:pharmacokinetics,pharmacodynamics and pharmacogenomics
    ZHANG Yue-li, MING Ying-zi, ZHOU Hong-hao, ZHANG Wei
    2014, 19(9):  1042-1049. 
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    The calcineurin inhibitors tacrolimus is immunosuppressant drug used for the prevention of organ rejection following transplantation. Pharmacogenomics research studying the effects of genetic polymorphisms on drug absorption, metabolism, disposition and response may eventually provide information that can be used in the clinical setting for individualizing immunosuppressant therapy. Understanding the influence of genetic factors on the pharmacokinetics and pharmacodynamics of calcineurin inhibitors could allow identification of the optimal immunosuppressant drug combination for a particular individual, assist in early prediction of the optimal starting dose and maintenance regimen, and help identify patients with an increased risk of drug inefficacy or side effects.
    Advances in relationship of genetic polymorphism with the toxicity caused by platinum-based therapy
    ZHENG Yi, YIN Ji-ye, ZHOU Hong-hao, LIU Zhao-qian
    2014, 19(9):  1051-1056. 
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    Platinum-based therapy are widely used in treating lots of cancers such as lung cancer, colorectal cancer, ovarian cancer and breast cancer. Although the efficacy of platinum drugs are quite notable in clinical practice, serious toxicity are inevitable. Clinical research have revealed that a wide inter-individual variability in the toxicity caused by Platinum-based therapy exists and this variability may partly due to individual genetic variations. This review summarizes the relationship between the polymorphisms of genes encoding platinum-based drug transporters, platinum-based drug-metabolizing enzymes and DNA repair enzymes and toxicity of platinum-based drugs.
    Research progress for glucose transporter 1 at the blood brain barrier
    WANG Yu-Zhu, LIU Gao-Lin, LI Xiao-Yu
    2014, 19(9):  1057-0. 
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    lucose is the main energy source in the central neuronal system. The family of facilitative glucose transporter proteins (GLUTs) is responsible for entry of glucose into brain. 13 members of the GLUTs family have been described thus far. Based on sequence similarities, the GLUTs family is divided into three classes, the first class (GLUT1-GLUT4) mostly transporting glucose; the second class (GLUT5, GLUT7, GLUT9 and GLUT11) mainly delivering fructose; the third class(GLUT6, GLUT8, GLUT10, GLUT12 and HMIT), however its function is still unclear. GLUT1 isomers are expressed in many kinds of cells, however,45kDa GLUT1 is the major transport protein mediating glucose across the blood brain barriers. The change of GLUT1 expression and function in some central nervous system diseases results in glucose transport process disturbed or glucose metabolism dysfunction. Recent researches show that GLUT1 can transport prodrugs by glycosylation modification across blood brain barrier. Therefore, method of glucose transport depending on GLUT1 may be a selective drug-delivery system. By utilizing such highly specific transport mechanism, it will widely attract the attention of researchers.
    Development of microRNA-dependment control of drug transporter
    LIU Li, GUO Chen-xian, PENG Jin-fu, HUANG Jie, YANG Guo-ping
    2014, 19(9):  1064-1068. 
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    MicroRNA is a class of small non-coding single-stranded molecule RNA, regulating the expression of target genes though complementary binding with the target gene mRNA 3 'untranslated region (3'-untranslated region, 3'-UTR) and plays an important role in biology developmental, cell differentiation, proliferation and apoptosis. And it closely related to the occurrence and development with many human diseases such as cancer, diabetes and so on. Drug-metabolizing enzymes and transporters expression can be affected by the changes of MicroRNA expression, thereby affecting drug effect. Current researches on drug metabolizing enzymes are more in-depth, while the transporters are relatively small. This paper summarizes research at home and abroad in recent years, the mechanism of action about MicroRNA and its regulation about drug transporter were reviewed. So as to provide a theoretical basis to guide the clinical individualized medicine.
    Research progress for glucose transporter 1 at the blood brain barrier
    WANG Yu-zhu, LIU Gao-lin, LI Xiao-yu
    2014, 19(9):  1067-1063. 
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    Glucose is the main energy source in the central neuronal system. The family of facilitative glucose transporter proteins (GLUTs) is responsible for entry of glucose into brain. 13 members of the GLUTs family have been described thus far. Based on sequence similarities, the GLUTs family is divided into three classes, the first class (GLUT1-GLUT4) mostly transporting glucose; the second class (GLUT5, GLUT7, GLUT9 and GLUT11) mainly delivering fructose; the third class(GLUT6, GLUT8, GLUT10, GLUT12 and HMIT), however its function is still unclear. GLUT1 isomers are expressed in many kinds of cells, however,45kDa GLUT1 is the major transport protein mediating glucose across the blood brain barriers. The change of GLUT1 expression and function in some central nervous system diseases results in glucose transport process disturbed or glucose metabolism dysfunction. Recent researches show that GLUT1 can transport prodrugs by glycosylation modification across blood brain barrier. Therefore, method of glucose transport depending on GLUT1 may be a selective drug-delivery system. By utilizing such highly specific transport mechanism, it will widely attract the attention of researchers.
    Advances in research of filament middle cerebral artery occlusion model and neuroprotective agents
    LIANG Zheng-yu, TANG Song-shan, ZHOU Dong
    2014, 19(9):  1069-1074. 
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    Ischemic stroke is the pathological process caused by reduced cerebral blood flow due to cerebrovascular thrombosis or embolism. Middle cerebral artery occlusion model serves as an indispensable tool to investigate mechanisms of ischemic cerebral injury and develop novel anti-ischemic regimens. This paper reviews the strengths and weaknesses of filament middle cerebral artery occlusion model and promising neuroprotective agents.
    Recent progresses on antibody-targeted conjugates of antitumor antibiotics
    SHANG Li-na, HONG Ming-yue
    2014, 19(9):  1075-1080. 
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    Recent studies have reported that some antibiotics such as calicheamicin and lidamycin display potent cytotoxicity respectively to variousmolecular targets, so they can be used as potent “warhead” agent to constitute antibody-targeted conjugates including immunoconjugates and fusion proteins. Antibody-targeted drugs exert a powerful antitumor potency because of its specific distribution and function in vivo. This paper mainly reviews on the construction and effect characteristics of antibody-targeted conjugates of antitumor antibiotics and provide a preliminary outlook for its future research direction.