Table of Content

Volume 13 Issue 7
26 July 2008

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Progress and research in pharmacogenetics of OATP1B1

ZHANG Wei, HE Yi-jing, ZHOU Hong-hao

2008, 13(7):  721-729. 

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Many types of drug transporters are expressed in different organs.The transporters play important roles in drug absorption, distribution and excretion, and lead to consequences for interindividual differences in disposition kinetics, interaction profiles of clinical drugs, susceptibility to side effects and treatment efficacy.The genetic polymorphisms have been shown to alter both the expression and function of their gene products.The identification of allelic variations and their functional confirmations is a necessary step towards the use of genetic information for personalized medicine.This review focuses on the role of organic anion transporting polypeptide 1B1 (OATP1B1) gene polymorphisms in pharmacokinetic and pharmacodynamic consequences in pharmacotherapy.

Mistletoe induces apoptosis by down-regulating the constitutive activation of nuclear factor-κB in HCT116 cells

LIN Lei, YE Meng, WANG Shao-ming, NI Shu-min, WU Xiao

2008, 13(7):  730-734. 

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AIM: To investigate the role of NF-κB in apoptosis induced by mistletoe in human colon cancer HCT116 cells.METHODS: The cell growth inhibiting was measured by MTT assay, the cell apoptosis was observed by the agarose gel electrophoresis.The protein expression was detected by Western Blotting. DIG-EMSA was conducted to detemine the DNA-binding activation of NF-κB.RESULTS: Mistletoe had a remarkable growth inhibitory action on HCT116 cells. After exposed to mistletoe, HCT116 cells presented some morphologic features of apoptosis including cell shrinkage, nuclear condensation and DNA fragmentation.NF-κB was inhibited in cancer cells treated with mistletoe.Mistletoe may potentiate the cytotoxic effects of chemotherapeutic agents such as HCPT.CONCLUSION: Mistletoe may induce apoptosis in HCT116 cell line.Inhibitory action of NF-κB may play a significant role in apoptosis induced by mistletoe.

Synergistic anti-tumor activity of cetuximab combining with cisplatin in human nasopharyngeal carcinoma cells

LI Jing-jing, FENG Gong-li, ZHU Xiao-feng, ZHANG Xiao-shi

2008, 13(7):  735-739. 

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AIM: To detect the effect of cetuximab combining with cisplatin on growth effect of nasopharyngeal carcinoma xenografts in nude mice and its possible mechanism.METHODS: HONE1 cancer cells were suspended and injected into nude mice subcutaneouly.Then the mice were randomly assigned to four groups: normal saline group, cetuximab group, cisplatin group and combination group.The largest and smallest diameters of athymic mouse tumor were measured regularly, and the tumor volume was calculated.After treatment, all animals were sacrificed, the tumor xenografts were weighed and the inhibitory rates were calculated. The expression of phospho-protein kinase β (p-AKT) and phospho-extracellular signal regulated kinase (p-ERK) were detected with immunohistochemistry.RESULTS: The tumor volume and average weight of cetuximab group after treatment had no significant differentce, there was obvious inhibitory effect in cisplatin group and the combination with cetuximab group, but the later was more significant.The immunohistochemistry assay showed that the expression levels of p-AKT and p-ERK were higher in the samples from the group treated with cisplatin alone compared with saline group, but reduced when treated with cetuximab combined with cisplatin or not.CONCLUSION: The growth of transplantation tumor on HONE1 nasopharyngeal carcinoma bearing cancer in nude mice had no significant effect, it could enhance the antitumor effect of cisplatin on nasopharyngeal carcinoma xenografts.

Apoptosis of the neurocytes after cerebral ischemia-reperfusion injury and effects of melatonin

YU Juan, ZHOU Yu, ZHENG Xiang, CHEN Chong-hong

2008, 13(7):  740-743. 

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AIM: To observe apoptosis of the neurocytes after focal cerebral ischemia-reperfusion injury (CIRI) in the brain tissue of rats and the effects and mechanism of melatonin (MT).METHODS: The models with cerebral ischemicre-reperfusion were induced by intraluminal middle cerebral artery occlusion (MCAO) with a nylon monofilament suture, 2 h occlusion followed by 24 h reperfusion.MT was intraperitonealed after reperfusion for 0, 1, 2, 6 h.The volume of cerbral infarction was observed using 2, 3, 4-triphenyl tetrazolium chloride (TTC) dyeing, apoptosis of the neurocytes was detected with TUNEL technique, the expression levels of Bcl-2 and Bax proteinum in brain tissue were detected by immunohistochemistry technique, the calcineurin activation in brain tissue was determined by inorganic phosphate method, ATP contents in brain tissue were measured with capillary zone electrophoresis(CZE) method.RESULTS: Compared with the vehicle model, the volume of cerbral infarction was reduced significantly by 10, 20 mg/kg MT, apoptosis of the neurocytes of ischemia penumbra (IP) area in the brain tissue was depressed by 20 mg/kg MT, the ratio of Bcl-2/Bax proteinum expression was increased, and the calcineurin activation of brain tissue in injured side was inhibited significantly, ATP contents in brain tissue were advanced.CONCLUSION: MT can antagonize apoptosis of the neurocytes in brain tissue after CIRI, reduce the volume of cerbral infarction.The mechanism may be related with the ratio of up-regulation Bcl-2/Bax, advancing of calcineurin activation inhibition, increasing of the ATP capacity.

Effects of acanthopanacis senticosi on inflammatory mediators in rats with acute pancreatitis

ZHU Jian-ping, LI Mei-fang, CHEN Bo, DENG Xiu-jian

2008, 13(7):  744-746. 

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AIM: To investigate the effect of acanthopanacis senticosi on the inflammatory mediators in acute pancreatitis(AP) rat models.METHODS: The rat models of AP were induced by intraductal administration of 5% sodium taurocholate, which were killed on time after model induction.The levels of TNF-α, IL-1, IL-6, amylase, lipase and phospholipase A₂ in the blood samples were determined.RESULTS: In the acanthopanax senticosus group, the levels of TNF-α, IL-1 and IL-6 were decreased significantly, the activation of serum amylase, lipase, phospholipase A₂ were attenuated significantly.CONCLUSION: Acanthopanacis senticosi has protective effect on AP model through cytokine pathways, within which the inhibitory effects on TNF-α, IL-1, IL-6 and phospholipase A₂ were the most important mechanism.

Involvement of ADMA NO pathway in antiatherosclerotic properties of the extract of shi-liang cha in hypercholesterolemic diet-fed rabbits

DU Wan-hong, LIU Zhong-hua, SHI Ling, ZHOU Zhong-wang, PENG Shi-xi, ZHANG Yong, SHI Zhao-peng, JIANG De-jian

2008, 13(7):  747-752. 

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AIM: To investigate the effects of the extract of shi-liang cha on atherogenesis in hypercholesterolemic diet-fed rabbits.METHODS: Male rabbits were fed with food containing cholesterol for 8 weeks to induce atherosclerosis.For drug treatment, the animals were orally treated with different doses of the extract of shi-liang cha (25, 50 or 100 mg/kg per day) during the last four-week period of the experiment.At the end of the experiment, blood samples were collected to measure the plasma levels of nitric oxide (NO), asymmetric dimethylarginine (ADMA) and malondialdohyde (MDA), and the aortas were isolated to determine endothelium-dependent vasodilator response and lesion area.RESULTS: The extract of shiliang cha could dose-dependently decrease plasma levels of total cholesterol, low-density lipoprotein and lesion area in atherosclerotic rabbits.Moreover, such treatment could improve endothelium-dependent vasodilator response and erythrocyte deformability, decrease the plasma levels of ADMA and MDA and increase NO content.CONCLUSION: The extract of shi-liang cha lowers blood lipids and inhibits atherogenesis, which may be related to improving endothelial function and erythrocyte deformability via inhibiting lipid peroxidation and modulating ADMA/NO system.

Effects of antidigoxin antiserum on expression of NOSs in ischemiareperfusion myocardium of rats

WANG Xing, WANG De-guo, KE Yong-sheng, TANG Zheng-guo, YANG Yu-wen, WANG An-cai

2008, 13(7):  753-757. 

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AIM: To investigate the changes of myocardial NO levels and the expression of NOS isoforms in rats with myocardial ischemia reperfusion (MIR) and the protective effect of anti-digoxin antiserum, an digoxin specific antagonist, on MIR induced NO system injury.METHODS: Myocardial ischemia reperfusion injury models were made by ligating the left anterior descending coronary artery for 30 min and followed by 45min reperfusion.Sprauge-Dawley rats were randomly divided into seven groups each with 10 rats including sham group, MIR group, normal saline group, verapamil group, low dose, middle dose and high dose anti-digoxin antiserum groups.The NO levels of myocardial and serum, activities of eNOS and iNOS were measured.The expression of myocardial eNOS and iNOS were determined by immunohistochemisry. The myocardial morphology was observed under optical microscope.RESULTS: The myocardial NO levels were significantly increased;The serum NO levels did not changed significantly;The eNOS expression were significantly decreased;The iNOS expression were significantly increased.Meanwhile, myocardial morphology injury was remarkable.With the intervention of middle and high dose anti-digoxin antiserum, the expression of myocardial iNOS were significantly depressed, the eNOS expression were reverted, the serum and myocardium NO levels were significantly increased.The myocardial histological morphology was significantly improved.CONCLUSION: The anti-digoxin antiserum can protect the function of myocardial NO system against MIR.The mechanism maybe antagonize endoxin and regulate the expression of NOS isoforms in myocardium.

Protective effect of Caspase-1 inhibitor on liver injury in experimental severe acute pancreatitis

ZHANG Xiao-hua, ZHU Ren-min, JI Hong-zan, YANG Miao-fang, SUN Quan, WU Xiao-wei, XU Xiao-bin

2008, 13(7):  758-763. 

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AIM: To assess the protective effect of Caspase-1 inhibitor on liver injury in experimental severe acute pancreatitis (SAP).METHODS: Fortytwo SD rats were randomly divided into 3 groups: healthy controls (HC, n=6);SAP-S group (n=18);SAP-ICE-I group (n=18).SAP was induced by retrograde infusion of 5% sodium taurocholate into the bili-pancreatic duct of SD rats.HC rats underwent same surgical procedures and duct cannulation without sodium taurocholate.In SAP-S group, rats received the first intraperitoneal injection of isotonic saline 2 h after induction of acute pancreatitis and repeated after 12 h. In SAP-ICE-I group, rats were firstly given ICE inhibitor intraperitoneally 2 h after induction of pancreatitis. As in SAP-S group, this was repeated at 12 h.Surviving rats were killed at certain time points, and all samples were obtained for subsequent analysis.RESULTS: The serum levels of ALT, AST and IL-1β in SAP-S group were (215±58), (372±38) U/L, (277±45) pg/mL at 6 h, (397±70), (548±75) U/L, (309±35) pg/mL at 12 h, (425±86), (666±84) U/L, (312±46) pg/mL at 18 h, respectively, which were increased significantly (P<0.01 vs HC).In SAP-ICE-I group, their levels were decreased significantly (P<0.01 vs SAP-S).Intrahepatic expressions of Caspase-1, IL-1β and IL-18 mRNA could be observed in HC, which were increased significantly in SAP-S group (P<0.01 vs HC).The expressions of IL-1β and IL-18 mRNA were decreased significantly in SAP-ICE-I group (P<0.01 vs SAP-S), whereas Caspase-1 mRNA expression had no significant differences (P>0.05).CONCLUSION: Caspase-1 activation, and the over production of IL-1β and IL-18may play pivotal roles in the pathogenesis of liver injury and Caspase-1 inhibitor improves liver functions effectively in experimental SAP.

Tissue distribution of triptolide in rats

HUANG Xiu-wang, XU Jian-hua, CHEN Yuan-zhong

2008, 13(7):  764-767. 

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AIM: To establish an HPLC method for the analysis of tissue distribution of triptolide in rats.METHODS: The concentrations of triptolide in biological samples were determined by an HPLC method with UV detection.RESULTS: The results of tissue distribution showed that triptolide was distributed widely in rats.The highest levels were found in lung, liver and kidney after i.v.administration (200 μg/kg) of triptolide.The peak levels appeared at 5 min and decreased significantly in 60 min in most tissues. CONCLUSION: Triptolide is widely distributed and rapidly eliminated in main tissues, and it can permeate blood brain barrier and blood testicle barrier.

Protective effect of semen plantaginis on oxidative damage of lens epithelial cell and its mechanism of signal transduction

HUANG Xiu-rong, QI Ming-xin, YAN-Jing, WU Zheng-zheng, HU Yan-hong

2008, 13(7):  768-771. 

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AIM: To investigate the effect of semen plantaginis(SP)on [Ca²⁺]_i, cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP)of lens epithelial cell (LEC)damaged by H₂O₂ and the mechanism of calcium signal transduction.METHODS: Sub-cultured bovine LECs were incubated with H₂O₂ and deferent concentrations of SP(8, 4, 2mg/mL)for 12, 24 and 36 h respectively.The LEC activities were observed by methyl thiazolyl tetrazolium assay (MTT).LEC [Ca²⁺]_i were detected by spectrofluorophotometer.Intracellular cAMP and cGMP of LEC were determined by radioimmunoassay.And the effects of different concentrations of SP and incubation for different times of 12, 24, 36 h were studied.RESULTS: The activities of LEC increased in deferent concentrations of SP groups compared with those in H₂O₂ group(P<0.01), which showed dosedependent and time-dependent manner.The [Ca²⁺]_i of LEC decreased in SP groups compared with those in H₂O₂ group(P<0.01), which showed time-dependent manner.The cAMP concentration of LEC decreased and the cGMP concentration of LEC increased in SP groups compared with those in H₂O₂ group (P< 0.01), which showed time-dependent manner.CONCLUSION: SP can protect LEC against oxidative damages and increase activities of LEC.The [Ca²⁺]_i, cAMP and cGMP signal transduction system and the cross-talk may be the mechanisms of SP preventing and delaying the cataract formation.

Effect of Huoxuetongqiao patch in transdermal delivery on hemorheology indics and SOD and LPO in experimental cerebral hemorrhage rabbits

ZHAO Qing-chao, HU Jiu-lue

2008, 13(7):  772-775. 

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AIM: To study the mechanism of Huoxuetongqiao patch in transdermal delivery andmagnetic field on experimental cerebral hemorrhage rabbits.METHODS: The cerebral hemorhage model rabbits were randomly divided into four groups: normal control group, model group, herbs group and herbs in magnetic field group.The normal control group and the model group were not treated.The herbs group were given Huoxuetongqiao herbs.Herbs in magnetic field group were given Huoxuetongqiao patch in the magnetic field.Hemorheology indices and SOD and MDA were detected respectively.RESULTS: Most of the hemorheology indices significantly decreased compared with those in normal control group.And one hour later, the main indices of hemorheology indices decreased below the normal level.In addition, the content of SOD obviously decreased and the content of MDA inmodel croup increased compared with those of normal control group (P<0.01).Compared with model group, the content of SOD increased and the content of MDA was obviously decreased in herbs group and herbs in magnetic field group (P<0.01 or P<0.05).Otherwise, those of herbs in magnetic field group were more significant compared with herbs group.CONCLUSION: Huoxuetongqiao patch can obviously improve the hemorheology of rabbits with cerebral hemorrhage, increase the content of SOD and induce the content of MDA.These may be the partial mechanisms of patch on experiment cerebral hemorrhage rabbits.

Pharmacokinetics and excretion of phenolic acids from mailuoning injection in rats

WANG Wei, WANG Guang-ji, HAO Hai-ping, CUI Nan, SUN Xuan-rong

2008, 13(7):  776-781. 

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AIM: To study the pharmacokinetics of phenolic acids from Mailuoning injection in rats. METHODS: SD rats were given a single i.v.administration dose of Mailuoning injection 10 mL/kg, plasma and urine were collected before and after injection. Phenolic acid components in plasma and urine were measured by LC MS.Pharmacokinetic parameters were determined from the plasma concentration-time data and urinary excretion-time data with the DAS software package.RESULTS: After i.v.of Mailuoning injection, chlorogenic acid (CGA), 1, 5-dicaffeylquinic acid (1, 5-DCQA), 3, 4-dicaffeylquinic acid (3, 4-DCQA), 3, 5-dicaffeylquinic acid (3, 5-DCQA)and caffeic acid (CA)were quickly excrectioned.The t_1/2 of CGA, 1, 5-DCQA, 3, 4-DCQA, 3, 5-DCQA and CA were 0.649, 0.334, 0.479, 0.486 and 0.330 h, respectively.AUC_0-∞ were (22.522±2.716), (0.353±0.062), (3.620±1.246), (5.287±1.627)and (2.257±0.360)mg·L^-1 ·h, respectively.After i.v. of Mailuoning injection, CGA, 1, 5-DCQA, 3, 4-DCQA, 3, 5-DCQA and CA can all be detected in the urine.The amounts of CGA, 1, 5-DCQA, 3, 4-DCQA, 3, 5-DCQA and CA excreted from urine during 0-24 h were (122.22±26.49)%, (3.30±1.26)%, (0.24±0.11)%, (1.93± 0.77)% and (18.61± 4.99)% of dose given in rats, respectively.CONCLUSION: After i.v.of Mailuoning injection, phenolic acids can be excreted quickly.Only a small quantity of 1, 5-DCQA, 3, 4-DCQA, 3, 5-DCQA and CA were excreted from urine.3, 4-DCQA and 3, 5-DCQA may be metabolized into CGA in the rat plasma.

Experimental study on chronopharmacology of Chinese medicinal formulae Ji-Ming-San

HAN Jun, SONG Jian-guo

2008, 13(7):  782-785. 

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AIM: To study the sedation, diuresis and anticoagulation effects of Ji-Ming-San (JMS)in animal models for exploring the circadian variations of the dosing action and verifying the rationality of administering JMS on special time.METHODS: The sedation effect and circadian difference were determined by observing the time session of ambulation, raising double-forefoot test and autonomic activity of model mice. The diuretic effect and the circadian variation in rats were examined by metabolic cage test while the anticoagulation and the circadian change were observed by glass test.RESULTS: JMS produced significant sedation effect by reducing time session of ambulation, raising upper limbs frequencies time and autonomic activity and the built-in rhythm with autonomic activity disappeared after JMS administration.JMS had satisfactory diuretic effect and total urinary output in water-loaded rats was increased after dosing.The diuretic effect of dosing showed a circadian rhythm with more significant output during the night than that during the daytime. Also, JMS prolonged the clotting time significantly and the action exhibited circadian difference.As compared with administration at the night, the clotting time was more prolonged at the daytime.CONCLUSION: JMS can produce obvious sedation, diuresis and anticoagulation effects with varied circadian rhythm.The findings suggest that the effect of administering JMS is better at the end of rest phase than other time session.

Study of the symptoms scale for evaluating changes in patients with coronary angina pectoris and Qi-deficiency combined with stagnation of blood in traditional Chinese medicine

LV Ying-hua, HE Ying-chun, YANG Juan, XU Ling, LIU Hong-xia, ZHENG Qing-shan

2008, 13(7):  786-791. 

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AIM: To develope a symptom scale for evaluating efficacy of coronary angina pectoris and Qideficiency combined with stagnation of blood.METHODS: The symptom score is always related with its incidence rate (frequency), its importance (evaluated by experts)and its serious degree (light, moderate and serious) in a measuring scale, and a mathematical model was used to calculate the weight factor and its score for each symptom in the scale.In an example of coronary angina pectoris and Qi-deficiency combined with stagnation of blood trial was analyzed based on the scale, and the scale was evaluated with the reliability, the validity, and the responsibility to change.RESULTS: Six symptoms (chest pain, chest distress, palmus, short breath, debilitation, and cyanosis)were selected as indices, and their weight factors and grades were calculated in a score scale.Some evaluations demonstrated that the approach showed a better feasibility, uniformity, and responsibility to change.CONCLUSION: This scale can be used to evaluating the efficacy of coronary angina pectoris and Qi-deficiency combined with stagnation of blood in traditional Chinese medicine.

Implement of timing function when incoming data with EpiData

GUO Jun-hao, LIU Yu-xiu, CAI Hui

2008, 13(7):  792-795. 

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AIM: To perform the function of timing during incoming data with EpiData, which can provide an effective method to monitor data.METHODS: The data were input with EpiData, then the function of timing was come true through two methods of compiling control sequence code.The first way was variable chronometry, which sets up variance in database and installed the order of quality control.The second way was document chronometry.Timing results were wrote-in document drawing assistance from the function of writenote with EpiData.The above two methods can count time during incoming data.The system would automatically make time write-in variance or document. RESULTS: The numeric type timing variance would be obtained in database with the way of variable chronometry.The timing would be kept as a document of textual form with the way of document chronometry.All the operations would be counted time with the above ways.CONCLUSION: EpiData has the function of counting time.On these grounds, the data would be research-on-research and the inputting plan would be instituted reasonably.The method of timing can make data-in more effective, which can check operators recording ability as an index.

Influence of CYP2D6 genetic polymorphism on pharmacokinetics of metoprolol in Chinese population

LI Qin, WANG Rui, GUO Ya, PEI Fei

2008, 13(7):  796-802. 

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AIM: To investigate the influence of CYP2D6 genetic polymorphism on pharmacokinetics of metoprolol in Chinese volunteers. METHODS: CYP2D6 genotypes were determined by genechips. Forty adult healthy Chinese volunteers were divided into the following four groups (n=10 in each group); Group 1: CYP2D6 *2W *10W, Group 2: CYP2D6 * 2H *10W or CYP2D6 *2M *10W, Group 3: CYP2D6 *2M *10H, Group 4: CYP2D6 *2M * 10M.After oral administration of 100 mg metoprolol, plasma and urine samples were collected from each subject over a 24-h period.The plasma and urine concentrations of metoprolol and its metabolite α-hydroxy metoprolol (HM) were determined by HPLC with fluorescence detection.RESULTS: The main pharmacokinetic parameters of metoprolol andHM in Group 2 were not significantly different from those in Group 1.In Group 3, t_1/2, AUC and C_max of metoprolol were significantly higher than those in Group 1, while t_1/2 of HM was 47.3% longer than that in Group 1 and AUC was 56.0% lower than that in Group 1.In Group 4, t_1/2, AUC and C_max of metoprolol were significantly higher than those in Group 1 and Group 3, respectively. While for HM, there was a significant difference compared with those in Group 1 and Group 3.The oral clearance and renal clearance in Group 3 and Group 4 were significantly lower than those in Group 1.The metabolic ratio (MR_0-24) in Group 3 and Group 4 were 1.82 and 3.96 times than that in Group 1, respectively.CONCLUSION: The present results show that CYP2D6 *2 has no influence on the pharmacokinetics of metoprolol, but CYP2D6 *10 reduces CYP2D6 activity which leads to the change of phenotype, and the homozygotes has more significant influence on the pharmacokinetics of metoprolol than the heterozygotes in Chinese population.

Study on genistein clinical adverse reaction and gene polymorphism of CYP1A2、UGT1A7

YANG Ming, TANG Bo, CHEN Jing-bao, ZHANG Xian, ZHU Shou-lun, DING Chun-yan, LU Yun-tian, ZENG Xing

2008, 13(7):  803-808. 

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AIM: In order to discuss the relation between clinical adverse reaction and gene polymorphism of CYP1A2、UGT1A7 when using genistein. METHODS: 114 cases of healthy volunteers were randomly divided into 2 groups: model group, and normal group.the model group take genistein 50, 100, 200 mg by oral, and each dose of genistein was observed 3 days for the occurrence of adverse reaction.Gene fragment was amplified by restriction fragment length polymorphism polymerase chain reaction(RFLR-PCR), and polymorphism of CYP1A2G2964A, C734A and UGT1A7Trp208Argwas analysised by enzyme electrophoresis.RESULTS: There had no significant difference of gene distribution between model and normal groups(P>0.05).Model group was divided into 2 groups of genotypes according to adverse reaction occurrence, CYP1A2G2964A gene: the 10 cases genotype among 14 cases in adverse reaction group was G/A(account 71.43%), but 22 cases genotype among 41 cases in no adverse reaction was G/G (account 53.66%); CYP1A2C734A gene: 7 cases genotype among 13 cases in adverse reaction was C/A(account 53.85%), but 16 cases genotype among 32 cases in no adverse reaction was A/A(account 50.00%).UGT1A7Trp 208Arg Gene: 12 cases genotype among 15 cases in adverse reaction was Trp/Trp (account 80.00%), and 32 cases genotype among 53 cases in no adverse reaction was Trp/Trp (account 60.38%).CONCLUSION: The relation gene in adverse reaction by using genistein is CYP1A2G2964A, CYP1A2C734A and UGT1A7, especially higher in G/A, C/A and Trp/Trp for each gene.

Pharmacokinetics of ropivacaine during epidural block combined with general anesthesia

ZHU Yong-ming, XIAO Wang-pin, AN Er-dan, ZHOU Qing-he, TU Li-biao, LOU Honggang

2008, 13(7):  809-812. 

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AIM: To study the pharmacokinetics characteristics of patients who used ropivacaine epidural block with general anesthesia.METHODS: Twelve patients scheduled for upper abdominal surgery were included in this study.0.5% ropivacaine was injected into epidural space before general anesthesia.Blood samples were taken from left radial artery at 1, 10, 20, 30, 45, 60, 75, 90, 120, 150 and 180 min after injecting ropivacaine.The plasma concentration of ropivacaine was determined by HPLC.The Compartment model was fitted by DAS statistics software, and the pharmacokinetic parameters were calculated.RESULTS: There were no adverse effects about ropivacaine during and after operation.The main pharmacokinetic parameters were as follow: t_max was 10 min;C_max was 0.713mg/L; t_1/2α was 122 min;t_1/2β was 190 min;AUC_0→180 was (72±10)μg·mL^-1·min^-1.CONCLUSION: The concentration-time curves were fitted to two-compartment open pharmacokinetic model.0.5% ropivacaine was proved to be safe, and it had good analgesia effect.

Therapeutic strategies for stroke: targeting the neurovascular unit

GAO Mei, LIU Rui, DU Guan-hua

2008, 13(7):  813-821. 

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Over the past two decades, researches have heavily emphasized on basic mechanisms of irreversible damage in brain cells after stroke.Many studies focused on what makes neurons die easily and what kind of strategies render neurons resistant to ischemic injury.In the past few years, clinical experience with clot-lysing drugs had confirmed expectations that early reperfusion improves clinical outcome.With recent research emphasizing methods to reduce tissue damage, both vascular and cell-based mechanisms, the spotlight is now shifting towards the study of how blood vessels and brain cells communicate with each other.The neurovascular unit (NVU) origins from an integrative blood vessel and neural system response in which all cellular and matrix elements involved in.The new research focus provides challenges and opportunities for research and therapy of stroke.

Advancement of research on the role and signal transduction pathway of gastrin in gastroenteric tumor

PAN Jun-tao, WU Pei

2008, 13(7):  822-827. 

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Studies have proved that gastrin plays key roles in the development and progression of gastroenteric tumor.After gastrin combined with the tumor cell surface receptors, some genetic transcription and expression were adjusted through certain signal transduction pathways, resulting in the development and growth of gastrointestinal carcinoma.Effective treatment method would been founded about gastroenteric tumor through the studies of mechanism of action and signal transduction pathways of gastrin in gastroenteric tumor.

Perplexities and considerations in clinical trials of the new traditional Chinese medicines

XUE Jie, HAN Rong, XIE Wei

2008, 13(7):  828-831. 

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In clinical trials, there are many perplexities and problems need to be resolved urgently, for example scientific scheme, authority of diagnostic standards, feasibility of physics and chemical indexes, characteristic of Chinese traditional medicine, rationality of control design etc.This article analyzes these problems and offers corresponding measures.

Beijing anti-AIDS drug clinical trial case and particular protection to vulnerable persons as subjects

ZHANG Jian-ping, LOU Xiao-jie, ZHOU Yu-sheng

2008, 13(7):  832-836. 

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Case of Beijing Anti-AIDS drug clinical trial has reveal problems about the protection to vulnerable persons as subjects in drug clinical trials.Vulnerable persons are those who are incapable of protecting their owninterests, including children, Pregnant women, mental disorders, prisoners, patients with incurable disease, illiteracies, etc.In ethical review of clinical trial, it should appraise their ability to understand the information, to protect own interests and their particular healthy situation.

Clinical progress of anti-epidermal growth factor receptor antibody, cetuximab, in the treatment of colorectal cancer

WU Liang, ZHENG Min-hua

2008, 13(7):  837-840. 

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Recent clinical trials suggested that epidermal growth factor receptor (EGFR) targeted agents could benefit many patients with colorectal cancer.This article reviews the clinical efficacy of cetuximab, which is an antibody directed at the EGFR, in the treatment of metastatic colorectal carcinoma.Several articles about EGFR-targeted therapies in metastatic colorectal carcinoma and other solid tumors were reviewed.Cetuximab showed the increase in progressionfree survival (3.98 months vs 2.56 months, P< 0.01).However, it did not show any advantage in mean survival time.For side effects, the severity of acne-like rash implied the response and the cetuximab therapy could be pursued by applying topical corticosteroids and emollients.Hypomagnesaemia, as a relatively special side effect, can be treated with intravenous magnesium sulfate.