Chinese Journal of Clinical Pharmacology and Therapeutics

Role of ABCA4 in the mechanism and treatment of retinal degenerative diseases

JIANG Bing, ZHOU Hong-hao

2009, 14(11): 1201-1207.

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ABCA4 is a member of the ABCA subfamily of ATP binding cassette (ABC)transporters that is expressed in rod and cone photoreceptors of the vertebrate retina.ABCA4, also known as the Rim protein and ABCR, is organized as two tandem halves, each containing one transmembrane domain, one glyosylated extracellular domain and nucleotide-binding domain. Over 500 mutations in the gene encoding ABCA4 are associated with a spectrum of related autosomal recessive retinal degenerative diseases including Stargardt macular degeneration, cone-rod dystrophy and a subset of retinitis pigmentosa.Biochemical studies on the purified ABCA4 together with analysis of ABCA4 knockout mice and patients with Stragardt disease have implicated ABCA4 as a retinylidene-phosphatidylethanolamine transporter that facilitates the removal of potentially reactive retinal derivatives from photoreceptors following photoexcitation.Knowledge of the genetic and molecular basis for ABCA4 related retinal degenerative diseases is being used to develop rational therapeutic treatments for this set of disorders.

Effect of propofol on pulmonary injury induced by early-stage severe acute pancreatitis in rats

ZHANG Yi-sheng, WANG Ming-hai, TAO Kun, CHEN Fang-zheng, ZHAO Guo-hai

2009, 14(11): 1208-1211.

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AIM: To investigate whether propofol can alter the pulmonary inflammation induced by severe acute pancreatitis(SAP) in rats during its early period. METHODS: Seventy-two adult male Sprague-Dawley (SD) rats were randomly divided into nine groups with 8 animals in each group:sham group, SAP 30, 60, 120, 360 min groups and propofol treatment 30, 60, 120, 360 min groups.The preparation of SAP were induced by retrograde injection of 5 % sodium taurocholate into the pancreatic duct of rats.And the treatment groups received propofol with doses of 150 μg·kg -1·min -1 injected continually immediately in vena caudalis after the preparation of ASP were made. Rats were sacrificed at different time points, and the level of AMY and LIP, the wet dry weight ratio(W D) of pulmonary and pancreatic tissue, the pathological change of pulmonary and pancreatic tissue were examined. RESULTS: Water content and pathological score of pulmonary tissue were decreased significantly within 360 minutes after reproduction of SAP were received propofol(both P <0.01).But no obvious change was observed in water content and pathological score of pancreatitis tissue(both P >0.05). CONCLUSION: propofol can alleviate pulmonary inflammation induced by severe acute pancreatitis in its early period.But propofol can not alleviate the injury of pancreatitis tissue.

Losartan inhibits renal sympathetic nerve activity in Paraventricular nucleus in chronic heart failure rat

GUI Le, ZHU Jian-hua, CHEN Qing-hui

2009, 14(11): 1212-1215.

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AIM: Left coronary artery ligation (LAD) was used to induce heart failure.Losartan was microinjected into paraventricular nucleus (PVN ), heart rate(HR), blood pressure(BP) and renal sympathetic nerve activity (RSNA) were measured.The mechanism of PVN in chronic heart failure was investigated. METHODS: Sprague-Dawley male rats were selected for LAD ligation for heart failure models, the variation of cardiac function was detected by echocardiography.Losartan was microinjected into PVN, the responses of HR, BP and RSNA were analyzed. RESULTS: Compared with sham group, the level of LV was increased (P <0.01), the levels of EF and FS were decreased in operation group (P <0.01, P < 0.05).The level of RSNA was decreased greater in operation group than that in sham group(P <0.05). CONCLUSION: Losartan microinjection into PVN can decrease the level of RSNA in chronic heart failure.

Study on protection and mechanism for adriamycin-induced cardiotoxicity with tiopronin in rats

YAO Rong-xin, FENG Liang-hua, XIA Yi-zi, ZHU Bao-ling

2009, 14(11): 1216-1220.

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AIM: To investigate the protection effect and mechanism of tiopronin on the cardiotoxicity induced by adriamycin in rats. METHODS: Rats were given intraperitoneal injection of adriamycin to induce the cardiotoxicity model.After continuous oral administration of tiopronin in adriamycin + tiopronin group for fourteen days, all the rats were killed.The content of cardiac troponin I (cTn Ⅰ), MB isoenzyme of creatine kinase (CK-MB) and brain natriuretic peptide (BNP) in serum were monitored.The activities of superoxide dismutase(SOD), the contents of malondialdehyde (MDA) and nitric oxide(NO), the activities of nitric oxide synthase (NOS) in myocardial tissue were determined.Myocardial pathology changes of rat myocardium were detected. RESULTS: Comapared with adriamycin group, the content of cTn Ⅰ, CK-MB and BNP in serum were significantly decreased(P < 0.05 or P <0.01), the activity of SOD in myocardial tissue was significantly increased, the contents of MDA and NO in myocardial tissue were significantly decreased, the activities of NOS and iNOS in myocardial tissue were significantly decreased(P <0.01), the pathology integral was significantly decreased in adriamycin +tiopronin group(P <0.05). CONCLUSION: Tiopronin has a protective effect on adriamycin-induced cardiotoxicity in rats.Tiopronin could relieve the oxidative injury of myocardial tissue induced by adriamycin in rats by increasing the activity of SOD, inhibiting the activity of iNOS which decreases the contents of NO.

Effect of ischemia injury on microcirculation of bile ducts relating to liver transplantation and protective effect of recombinant human growth hormone

WANG Zheng, ZHOU Jie, LIN Yi-xiong, CUI Zhong-lin, ZHANG Qi-fan

2009, 14(11): 1221-1224.

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AIM: To investigate the changes of microcirculation of bile ducts relating to liver transplantation in rats with ischemia injury and protective effect of recombinant human growth hormone (rhGH) on ischemia injury. METHODS: The rat orthotopic autologous liver transplantation was performed firstly. Wistar rats were randomly divided into three groups each with 6 rats including control group (CON), ischemia injury group (HLA) and rhGH group.Specimen of liver tissue was collected after 7 days post-operation. The blood vessels were tagged with rabbit anti-CD34 polyclonal antibody.The blood vessels and bile ducts of portal area were observed and enumerated. RESULTS: In HAL group, the array of intrahepatic cholangiocytes was significantly absent.There was no obvious soakage of inflammatory cells in portal area. The number of blood vessels and bile ducts in portal area was significantly decreased.The number of bile ducts not accompanying with blood vessels was significantly increased (P <0.05);In rhGH group, the changes of chronic hyperplastic inflammation were oberserved in intrahepatic cholangiocytes.The number of blood vessels and bile ducts in portal area was significantly increased.The number of bile ducts accompanying with blood vessels was significantly increased (P <0.05). CONCLUSION: Ischemia injury of bile ducts relating to rat orthotopic autologous liver transplantation damnifies the microcirculation of intrahepatic bile ducts.However, administration of exogenous rhGH promotes recovery of intrahepatic microcirculation consequently protecting bile ducts from ischemia injury.

Protective effect of Cistanchis glycosides on ethanol-induced liver damage in mice

LUO Hui-ying, LIU Yuan, XI Guo-zhu, DU Jian-de

2009, 14(11): 1225-1228.

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AIM: To research the protection of Cistanchis glycosides on ethanol-induced liver damage in mice. METHODS: 40 mice were divided into 4 groups in random, and administered by gavage for 4 weeks.Cistanchis glycosides were twice a day, ethanol were once a day.When time limit arrived, mice were weighted, the serum was afforded to detect the liver function index, liver homogenate were prepared for biochemical detections, liver remained were fixed for pathological investigation. RESULTS: When mice were damaged by ethanol, liver index, liver function index, contents of TG, TC, MDA and LPO were increased distinctly(P <0.05), The activities of SOD, GSH-Px and CAT were decreased at the same time(P <0.05).Imflammatory infiltration and flat vacuoles were observed.Cistanchis glycosides ameliorated these changes evidently(P <0.05);the effects were dosedependence. CONCLUSION: Protective effect of Cistanchis glycosides on ethanol-induced liver damage in mice is associated with antioxidation, enhancement of clearance for free radicals and metabolites, and inhibition of lipid overoxidation reactions.

Effect of specific immunotherapy on TGF-β₁/ Smads in asthmatic rats

LI Shao-bo, JIN Xiao-hong, WANG Xin-xin, LAI Xiao-ying, TONG Xia-sheng

2009, 14(11): 1229-1233.

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AIM: To approach the effect of specific immunotherapy on transforming growth factor (TGF-β₁) Smads in asthmatic rats. METHODS: Forty Wistar rats were randomly divided into 4 groups:control group, asthma group, control of specific immunotherapy group and specific immunotherapy group, with 10 rats in each group.The model of asthma was established by the ovalbumin (OVA) challenge methods and the specific immunotherapy group received specific immunotherapy by repeated inhaling different doses of OVA. The concentrations of TGF-β₁ in BALF and serum were detected by ELISA.The expressions of TGF-β₁, phosphorylated Smad2/3(P-Smad2/3) and Smad7 proteins in lung tissue were detected by immunocytochemical method. RESULTS: In BALF or serum, the concentration of TGF-β₁ in control group was lower than that in asthma group or specific immunotherapy group respectively.The concentrations of TGF-β₁ in BALF or serum in specific immunotherapy group was lower than that in asthma group.The expressions of TGF-β₁ and PSmad2/3 in lung in asthma group were higher, but the expressions of Smad7 was lower than that in control group or in specific immunotherapy group respectively. CONCLUSION: Specific immunotherapy could decrease the expressions of TGF-β₁ and P-Smad2/3, while increase the expression of Smad7 in asthmatic rat, and relieve the airway inflammation in some extent and inhibit the occurrence and development of airway remodeling.

Antitumoral effect of the immunoconjugate composed of ricin A-chain and EGFR mab

SHEN Su-jian, WU Jin-ming, JIN Si-si, HUANG Zhi-ming, WU Jian-sheng

2009, 14(11): 1234-1238.

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AIM: To research the antitumoral effect in vitro of the immunotoxin composed by RTA and EGFR mab. METHODS: Taking SPDP as the coupling agent, RTA, which was purified from castor bean, was linked with EGFR mab.After further purification, the purification of RTA and the construction of the immunotoxin were detected by SDS-PAGE.The combining capacity to HepG2 cells was detected by DAB chromogenic method.The immunoreactivity was detected by indirect ELISA.The cytotoxicity in vitro was detected by CCK-8 method. RESULTS: The immunotoxin was constructed successfully.Immunotoxin retained the combining capacity of EGFR mab to HepG2 cells and a major part of the immunoreactivity.The immunotoxin displayed a different cytotoxicity between HepG2 cells and LO2 cells. CONCLUSION: Immunotoxin plays a specific role in suppressing the multiplication of the hepatoma carcinoma cell and has a good prospect in liver cancer treatment.

Effect of SB203580 on cell apoptosis during lung ischemic/reperfusion injury in rats

ZHENG Yan-rong, SHI Lu, HONG Jia-lin, JIA Xu-guang, WANG Wan-tie

2009, 14(11): 1242-1246.

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AIM: To explore the effect of SB203580, P38 mitogen activated protein kinase specific inhibitor(p38MAPK), on apoptosis during lung ischemic/reperfusion injury in rats. METHODS: 30 rats were randomly divided into three groups, group control (Group C ), group lung ischemia/reperfusion injury (Group I/R) and group SB203580 (Group S).The changes of arteriae pulmonalis apoptosis were detected with TdT-mediated dUTP nick end labeling (TUNEL). The content of Bcl-2 and Bax in cytoplasm were determined with immunohistochemistry and meanwhile the ultrastruction changes of lung were observed under electron microscope. RESULTS: Compared with Group C, the expressions of Bcl-2, Bax protein were increased and the ratio of Bcl-2/Bax were decreased in Group I/R (all P <0.01), and the apoptosis index(AI) was increased, the abnormal changes of the lung tissue in morphologically were significant in Group I/R.After using SB203580, the expression of Bcl-2 protein was increased and the expression of Bax protein was decreased, the ratio of Bcl-2/Bax was increased(all P < 0.01), the values of AI was decreased in Group I/R, and the abnormal changes of the lung tissue in morphologically were lessen at different degree (all P < 0.01). CONCLUSION: SB203580 produces notable protective effects on lung ischemic/reperfusion injury in rats by up-regulating Bcl-2 protein expression, downregulating Bax protein expression in lung tissue and regulating the balance of Bcl-2 protein and Bax protein, decreasing apoptosis.

Stress induced early renal injury by upregulating NADPH oxidase, hyperphosphorylation of PKCε is mitigated by endothelin receptor antagonist CPU0213

XU Jin, DAI De-zai, PENG Hong-jun, DAI Yin

2009, 14(11): 1247-1252.

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AIM: Stress likely contributes to oxidative stress initiating early renal insufficiency, that may relate to abnormal endothelin-1 (ET-1) -PKC(protein kinase C) εpathway.It is aimed to test if the endothelin receptor antagonist CPU0213 could reverse stress induced renal early lesion by suppressing abnormal ET and pPKCε. METHODS: Sprague-Dawley rats were subdivided into 3 groups:(1) normal, (2) isoproterenol (ISO) 1 mg/kg, s.c.for 10 days and (3) the ISO injected rats were intervened with CPU0213 20mg/kg, s.c., at day 6 -10.Biochemical measurements and expressions of ETAR (endothelin receptor A), NADPH oxidase p67^phox and PKCεwere conducted. RESULTS: Serum creatinine and 24 h urinary albumin were increased significantly (P < 0.01), compared with normal.The activities of GSHPx and SOD were decreased and the content of MDA was increased in the renal cortex associating with upregulated mRNA and protein of ETAR, PKC (, and NADPH oxidase p67^phox in ISO treated rats.CPU0213 was effective to reverse the renal function by suppressing the abnormalities. CONCLUSION: Activated ETAR, NADPH oxidase and pPKCεare assocaited with renal dysfunction in response to ISO.Endothelin receptor antagonist of CPU0213 is effective in reversing these changes.

Antitumor effect of combination of carboxymethyl-chitosan and Adriamycin in vitro

YANG Jing-ya, WANG Xiao-ji, ZHANG Jian

2009, 14(11): 1253-1257.

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AIM: To investigate the effects of carboxymethyl chitosan (CM-CTS) and adriamycin (ADM)on the proliferation of human cervical carcinoma cell line Hela and human colon cancer cells LS174- T in vitro. METHODS: The anti-proliferation activities of two drugs on tumor cells were evaluated by MTT assay.The jin's formula was used to analyze the experimental data. RESULTS: Both CM-CTS and ADM could inhibit tumor cell proliferation and an additional synergistic inhibitory effect could be improved when two drugs were combined.In sequential test, administration of ADM first followed by CM-CTS had a synergistic effect;but administration of CM-CTS first followed by ADM produced an antagonistic effect. CONCLUSION: Combined treatment with CM-CTS and ADM produces synergistic effects.Sequential administration of CM-CTS and ADM produces a unidirectional synergistic effect.

Comparison of inhibitory effect of five natural medicines on proliferation induced by rhbFGF in lens epithelial cell

QI Ming-xin, ZHANG Qing-lin, HUANG Xiu-rong, YANG Xin

2009, 14(11): 1258-1262.

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AIM: To compare the inhibitory effect of five natural medicines on proliferation induced by recombinant human basic fibroblast growth factor (rhbFGF) in lens epithelial cell (LEC). METHODS: The proliferations of cultured LEC were induced by rhbFGF, which were incubated with five natural medicines, [curcumine (Cur), elemene(Ele), arsenite trioxide (As₂O₃ ), triptolide (Tri) and rhizoma curcumae (Rc) ], respectively.The LEC activities were detected via methyl thiazolyl tetrazolium (MTT).The proliferating cell nuclear antigen (PCNA) of LEC were detected via flow cytometer(FCM). RESULTS: The activity of LEC and the expression of PCNA in proliferation group were higher than those in control group (P <0.01). Compared with the proliferation group, the activity of LEC and the expression of PCNA were significantly decreased in group Cur, Ele, As₂O₃, Tri and Rc (P < 0.01).The inhibitory effects of Cur and Ele are the strongest.As₂O₃, in the middle.Tri and Rc are the weakest(P <0.01), the effects of Cur and Ele are similar. CONCLUSION: The five natural medicines can inhibit the proliferation of LEC induced by rhbFGF.Cur and Ele may become effective medicines of preventing and treating after-cataract.

Effects of Ping Yang Jiang Ya Fang on blood pressure and insulin resistance in Gan Yang Shang Kang Syndrome model of spontaneous hypertensive rats

WU Hao, NING Yang-gen, XIAO Chang-jiang, LIU Zhao-qian, LI Sha

2009, 14(11): 1263-1268.

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AIM: To observe the effect of Ping Yang Jiang Ya Fang on blood pressure and insulin resistance (IR)in Gan Yang Shang Kang Syndrome model of spontaneous hypertensive rats(SHR), and to explore its hypotensive effect and possible underlying mechanisms. METHODS: Twenty-four SHR were randomly divided into four groups with 6 rats in each group, all of the SHR were drenched with Aconiti Praeparatae Decoction for four weeks to make Gan Yang Shang Kang Syndrome model.Another six healthy Wistar rats were taken as normal control group.From the fifth week, each SHR group was drenched with low or high dose of Ping Yang Jiang Ya Fang Decoction (8 g/kg, 16 g/kg), the suspension of nitrendipine (1.6 mg/kg)or distilled water for thirty consective days, once a day.After the first intragastric administration, the tail artery systolic pressure of all rats was measured at every two hours for twenty-four hours in order to observe the acute hypotensive effect of drugs.And it was also measured at every three days during drenching drugs in order to observe its chronic hypotensive effect. The changes of the fasting plasma glucose (FPG), fasting insulin (FINS), insulin sensitivity index (ISI)and resistin of all rats were also determined before and after therapy. RESULTS: (1)In the acute hypotensive experiment, low or high dose of Ping Yang Jiang Ya Fang Decoction and nitrendipine could reduce the tail artery systolic pressure of SHR(P <0.05), but therewas no significant difference in twenty-four hours among them (P >0.05).The changes of systolic pressure of SHR in the groups with low dose or high dose of Ping Yang Jiang Ya Fang Decoction were smaller than those with nitrendipine during twenty-four hours (P <0.05).In the chronic hypotensive experiment, they could also decrease the tail artery systolic pressure of SHR (P < 0.05).The hypotensive effect of high dose of Ping Yang Jiang Ya Fang Decoction was better than that of low dose (P <0.05).(2)The plasma FINS and resistin of SHR in the groups of low or high dose of Ping Yang Jiang Ya Fang Decoction, or nitrendipine were significantly decreased (P <0.05), while the ISI was significantly increased (P <0.05) after treatment. And the effect of either low or high dose of Ping Yang Jiang Ya Fang Decoction was better than that of nitrendipine (P <0.05). CONCLUSION: (1)Ping Yang Jiang Ya Fang has obvious acute and chronic hypotensive effects to Gan Yang Shang Kang Syndrome model of SHR.(2)Ping Yang Jiang Ya Fang can improve the IR of Gan Yang Shang Kang Syndrome model of SHR.

Construction of determination of cefditoren and the investigation of mechanism of biliary excretion

ZHANG Qing-hao, MENG Qiang, LIU Qi, WANG Chang-yuan, MEI Lin, SUN Hui-jun, LIU Kexin

2009, 14(11): 1269-1274.

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AIM: To develop a high-performance liquid chromatography internal standard method for determining of cefditoren in the rat plasma, bile and urine, and to clarify the relation between multidrug resistance- associated protein 2 (Mrp2) and biliary excretion of cefditoren using perfused rat livers. METHODS: 4-dimethylaminoantipyrine was used as the internal standard.Chromatographic separation was performed on a C₁₈UG 120 column (4.6 mm ×250 mm, 5 μm) and mobile phase was composed of 0.1 % ammonium acetate and methyl alcohol (67:33, V/V). The flow rate was 0.8 mL/min and 25 μL of mixture was injected.Perfused rat livers were performed to investigate whether cefditoren was transported via Mrp2. We established the control (cefditoren 1 μmol/L) and experimental group (cefditoren 1 μmol/L added the inhibitor of Mrp2-probenecid, 20 μmol/L).Perfusate samples and bile were collected at setting times.Cefditoren was determined by HPLC.We compared the hepatic extraction ratio and cumulative biliary excretion rates in control and experimental groups. RESULTS: The concentration range of cefditoren was 0.1 -4 μg/mL in plasma, 0.1 -5 μg/mL in bile and in urine, with good linearity.The relative recovery was 85 %- 110 %.The intra- and inter-day RSD were <13.5 %. The hepatic extraction ratio showed no statistically significant differences, whereas cumulative biliary excretion rates were significantly reduced to 40.0 % compared to control over 25 min in experimental group. CONCLUSION: It can be used for the determination of cefditoren concentration in plasma, bilary and urinary samples and for pharmacokinetic study since it is economic, simple, sensitive and fast method.Cefditoren is the substrate of Mrp2, which is related with biliary excretion of cefditoren.

Effects of schizandrin A on the activity of CYP3A in rat liver microsomes

SU Ming-wei, LI Wei-liang, LIU Hui-ming, XIN Hua-wen, WANG Nai-ping

2009, 14(11): 1275-1280.

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AIM: To study the effects of schizandrin A on CYP3A by in vitro drug metabolism experiments. METHODS: Midazolam (MDZ)was adopted as a drug “probe” and a detection method of high-performance liquid chromatography (HPLC)was established, the rat liver microsome was as a carrier.The IC₅₀ value of schizandrin A by in vitro administration and related enzyme kinetic parameters on CYP3A were detected. RESULTS: The endogenous substances did not interfere with the determination in the incubation system. The method was fast, stable and had high sensitivity. The IC₅₀ of schizandrin A on MDZ metabolism in liver microsomes was 6.26 μmol/mL, and the enzyme kinetic parameters were as follows:K_m =15.77 μmol/L, K_i=5.5 μmol/mL. CONCLUSION: Schizandrin A is able to inhibit CYP3A activity in rat liver microsomes. The inhibition is mixed type, non-competitive and anticompetitive inhibition.

Establishment and application of ligase-based method detecting polymorphism of TPMT

LIANG Xin, ZHANG Ya-tong, CHENG Gang, HU Xin, SUN Ying-qi, YANG Chen, LI Kexin, SUN Chun-hua

2009, 14(11): 1281-1285.

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AIM: To establish one ligase-based method to detect the gene polymorphism of TPMT. METHODS: The multiplex PCR ligase detection reaction(LDR) was established, and 50 blood samples of healthy postulants were investigated with this method. RESULTS: This method was reliable, rapid, high-degree automatic.The genotype of ^＊2, ^＊3A, ^＊3B and ^＊4, which depressed the activity of TPMT were not found, only 2 samples of TPMT ^＊3C heterozygote were detected.CONCLUSION: This method can be applied for TPMT polymorphisms detection.

Tolerance of Tuodushu capsule in normal drug addicts:A phase Ⅰclinical trial

HE Jian-chang, XU Gui-li, ZHANG Qing, ZHANG Dian-min, HAO Jiang, SHEN Liang, FENG En-fu, LIU Miao

2009, 14(11): 1286-1291.

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AIM: To assess the safety and tolerance of Tuodushu capsule in normal drug addictive volunteers. METHODS: 43 subjects were enrolled in the non-controlled single-dose trial or multiple-dose trial. Thirty-one subjects were randomized into 7 dose groups (1, 2, 3, 4, 5, 6 and 7 capsules group) for singledose trial.Twelve subjects, six males and six females, equally divided into two treatment groups (3 capsules or 4 capsules group), were orally given 3 or 4 capsules per times, b.i.d.in the first 3 days and 2 capsules per times, b.i.d.in the last 3 days for multiple-dose trial.The physical examination, vital signs, electrocardiogram, routine blood tests, routine urine tests, and blood biochemical tests were conducted on schedule and statistically evaluated. RESULTS: There were no significant clinical changes in physical examination and vital signs after administration.In single-dose trial, statistically significance (P <0.05) in BUN in 4 groups (3, 4, 5, 6 capsules group) and Cr in 2 groups (3, 7 capsules group) were found.In multiple-dose trial, statistically significances (P <0.05) in BUN and Cr between two groups were observed.There were significant clinical changes in CK in a small number of cases, but no differences between cases.All adverse events were mild to moderate and transient and no serious adverse events were found in the trial. CONCLUSION: Tuodushu capsule is safe and well tolerated in normal drug addictive volunteers at dose of 1-7 capsules once daily.In addition, the multiple-dose level of 4 capsules per times, b.i.d.in the first 3 days and 2 capsules per times, b.i.d.in the last 3 days is assessed as safe and well tolerated.The recommended oral dosage regimen for phase II clinical trial is 3 or 4 capsules per times, b.i.d.in the first 3 days and 1 or 2 capsules per times, b.i.d.in the last 3 days for multiple-dose trial.Attention should be paid to the changes in sleep, diet, Cr and defecation.

Retrospective analysis of antibacterial agents utilization in acute pancreatitis patients

ZHAO Pei-xi, GUO Ying-hua, LIU Yu, CHANG Ying, WANG Jing-wen, ZHU Yan-rong, WANG Zhi-rui, WEN Ai-dong

2009, 14(11): 1292-1295.

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AIM: To examine the rational use of antibiotics in acute pancreatitis of Xi-Jing hospital. METHODS: Retrospective analysis 93 patients who were provided with antibiotics drugs of acute pancreatitis patients from January to December of 2008. RESULTS: There are 93 AP cases in the DegestionMedical Department.78 MAP cases account for 83.67 %, 15 SAP cases account for 16.13 %.Excessus-medication were found in prophylaxis utilization in antibacterials drug, for the bulk of antibacterials drug combination was unreasonable, the reasonable course of treatment only account for 30 %.The rates of bacterial culture were too low in infection cases, which caused severity experience medication. CONCLUSION: Generally, the choices of antibiotic are rational, but there are still substandard usage of antibiotics in hospital, and it's necessary to improve the management of rational usage of antibiotics.

Study on IL-12, IL-10 expression of infants with none or low response to recombinant hepatitis B vaccine stimulated by bacillus Calmette-Guerin

DI Jun-bo, CHEN Yi-ping, XU Zhi-wei

2009, 14(11): 1296-1299.

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AIM: To investigate the efficacy of Bacillus Calmette-Guerin (BCG) on IL-12, IL-10 expressions of infants with none or low response to recombinant hepatitis B vaccine. METHODS: The geometric mean titer (GMT) of anti-HBs was tested by radioimmunity assay after hepatitis B vaccine stimulation, selected 60 cases with non-or low-response(GMT <100 UL), who were divided into two groups, one group was injected by BCG, the concentrations of IL-10, IL-12 were detected by ELISA. RESULTS: BCG could significantly stimulate infants with none or low response to recombinant hepatitis B vaccine to product IL-12 and IL-10 associated cytokines, the enhancement was course-dependent.Compared with the control group, the GMT of anti-HBs was significantly higher than that in the Bacillus Calmette-Guerin injection group. CONCLUSION: BCG might be an effective adjuvant to induce cellular immune response via the enhancement of IL-12 and IL-10 of infants with none or low response to recombinant hepatitis B vaccine.

Effect ofWuling capsule in the treatment of patients with gastroesophageal reflux disease accompanied with anxiety

CHEN Xiao-yan, YAN Jun, CAI Zhen-zhai, XIA Xuan-ping, ZHENG Jun-jie, XUE Zhan-xiong

2009, 14(11): 1300-1303.

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AIM: To explore the efficacy of Wuling capsule in the treatment of gastroesophageal reflux disease (GERD) accompanied with anxiety. METHODS: 64 patients with gastroesophageal reflux disease accompanied with anxiety(the score of the SAS ≥50) were randomly divided into 2 groups.Study group(n = 32) was treated with Wuling capsule and esomeprazole magnesium tablets for 8 weeks and control group was treated with esomeprazole magnesium tablets.Clinical efficacy was assessed with gastroesophageal reflux symptoms and Zung self-rating anxiety scale (SAS). RESULTS: After 8 weeks treatment, the efficacy rate and total effective rate of study group were 58.6 %and 93.1 %, which were significantly higher than those in the control group(32.2 % and 67.9 %, respectively, P <0.05).Scores of the SAS of both groups were significantly reduced(P <0.01);and scores of the SAS were significantly different between the study group and the control group after 4, 8 weeks treatment(P <0.05, P <0.01). CONCLUSION: Wuling capsule has significant effectiveness and high safety in the treatment of GERD accompanied with anxiety.

Concentrations of tumor necrosis factor receptors at prostatic secretion in male patients with chronic pelvic pain syndrome

CHEN Rong-sheng, LUO Dong-jiao, CHEN Li, TONG Xia-sheng, CHEN Hao, WANG En-zhi

2009, 14(11): 1304-1307.

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AIM: To detect the concentrations of solube tumor necrosis factor receptors (sTNF-R1 and sTNF-R2) at prostatic secretion in male patients with chronic pelvic pain syndrome(CPPS).And to investi-gate the potential roles of sTNF-R1 and sTNF-R2 in the development of CPPS inflammation. METHODS: All the patients were obtained during March 2008 to January 2009 including 24 cases of CPPS ⅢA and 20 cases of CPPS ⅢB, and were compared to 24 cases of volunteers. Expressed prostatic secretion were obtained by rectum massage methods.Concentrations of sTNF-R1 and sTNF-R2 were measured by enzyme linked immunosorbent assay methods. RESULTS: The concentrations of sTNF-R1 and sTNF-R2 proteins were significantly higher from CPPS ⅢA group than those from CPPS ⅢB group [ (46 ±6 vs 41 ±6), P <0.05, (13.0 ±4.8 vs 7.9 ±4.1) ng/mL, P <0.01], and they were dramaticly higher from CPPS ⅢB group than those from compared group [(25 ±8), (2.5 ±1.9) ng/mL, all P <0.01]. CONCLUSION: Concentrations of sTNF-R1 and sTNF-R2 proteins are increased in male patients with CPPS.Both of them may be associated with the development of CPPS inflammation.

Progress in receptor protein &drug molecule docking approaches

ZHU Zhi-yuan, ZHANG Yan, LI Zheng, LI Jing-heng, RUI Jian-zhong, YUAN Jing

2009, 14(11): 1308-1312.

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The development of computer technology greatly facilitated the process of life science research.The study on the use of molecular docking receptor protein and drug interactions is the current hot spot.The molecular models of proteins and drugs are established and the interaction are studyed.In this way, the more ideal, safe and effective drugs are designed.The problem how to create the molecule model has been solved.Protein molecules and drug molecules docking in what manner, and this problem is worth exploring.This article describes the current research progress in molecular docking, emphasizing on its methods and tools.

Membrane proteins and membrane proteomics

LIANG Yan, KAN Hong-wei, YANG Shi-you

2009, 14(11): 1313-1320.

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A membrane protein is a protein molecule that is attached to, or integrated into the membrane of a cell or an organelle.As the membrane protein is a good target for drugs, more than 80 % of the drugs on the present market take the effect on the membrane protein.Therefore, it is significant to study the membrane proteins.However, the traditional study on membrane proteomics is obstructed by the difficulties in solubilizing, separating, and identifying membrane proteins.This review summarizes the structure of membrane proteins, the significant role of the membrane proteins on the cell physiology and the human diseases, the potential of the membrane proteins to be the target for drugs and the techniques of the research on the membrane proteomics.

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