Objective To assess the clinical value of dobutamine 201Tl stress-redistribution/nitroglycerin augmented ~(99m)Tc-metho~(99m)Tc-xyisobutylisonitrile (MIBI) gated myocardial perfusion imaging (MPI) in patients with coronary artery disease (CAD). Methods A total of 132 patients with suspected CAD underwent dobutamine 201Tl stress-redistribution/nitroglycerin augmented MIBI gated MPI and coronary arteriography (CAG) within two weeks after MPI. Percutaneous coronary interventions (PCI) were performed in 23 patients with myocardial infraction. The regional wall movement was assessed with echocardiography before and within three months after PCI. Results Taking stenosis ≥50% as standard of CAD, the sensitivity, specificity and accuracy of dual-isotopic SPECT imaging in diagnosing CAD was 93.41%, 87.80% and 91.67%, respectively. The sensitivity, specificity and accuracy in diagnosing left anterior descending artery (LAD) stenosis was 93.85%, 91.04% and 92.42%, for left circumflex artery (LCX) was 86.79%, 89.87% and 88.64%, while for right coronary artery (RCA) was 81.25%, 82.14% and 81.82%, respectively. Of all 207 myocardium segments in 23 patients with myocardial infarction, radioactivity defect was found in 113 segments on the redistributed ~(201)Tl images, and radiofilling was found in 52 (52/113) segments on the nitroglycerin augmented ~(99m)Tc-MIBI images, whereas 61 segments had no radiofilling. Taking regional wall movement improvement as the criterion of viable myocardium, the sensitivity, specificity and accuracy of identifying viable myocardium with nitroglycerin augmented ~(99m)Tc-MIBI imaging was 87.23%, 83.33% and 84.96%. Conclusion Dobutamine ~(201)Tl stress-redistribution/nitroglycerin augmented ~(99m)Tc-MIBI gated MPI is able to effectively detect CAD and viable myocardium and helpful in diagnosis and treatment of CAD.

Objective The comparison of the clinical role of stress-redistribution/reinjection with dual isotopes of 99Tcm-methoxyisobutylisonitrile (MIBI) and 201TI in the detection of myocardial viability.Methods One hundred and sixty patients with clinically suspicious coronary artery disease (CAD) were included.All had intravenous injection with 740 MBq of 99Tcm-MIBI.Pharmacological challenge with dobu-macological challenge with dobutamin,111 MBq of 201Tl Was injected to all.Myocardial SPECT images were performed in all at 10-min (stress) and 3-h (redistribution/rest) after injection.The 201Tl(37 MBq)would be given to those patients with myocardial perfusion defect at stress images by 201Tl and were demon-strated by both 201Tl(redistribution) and 99Tcm-MIBI (rest).Coronary angiography (CAG) Was performed within two weeks.X2-test was used with SAS 6.12.Results Coronary artery abnormalities were found in all with 76 patients had one vessel disease,51 had two and 33 had three.Of the 152 patients who had myo- cardial perfusion defect during stress images,63 had redistribution by both 201TI and 99Tcm-MIBI.5 had re-distribution by 201Tl only.9 had redistribution by 99Tcm-MIBI only,and 75 had no redistribution in 201Tl or 99Tcm-MIBI images.The sensitivity of detection myocardial viability with myocardial SPECT images between 201Tl at redistribution (66.0%,68/103) and 99Tcm-MIBI at rest (69.9%,72/103) were insignificant (x2=O.36.P>0.05).Of the 75 patients who did not have redistribution in 201Tl or 99Tcm-MIBI images.34.7% (26/75)had myocardial perfusion when reinjection of 201Tl.In all,there were eight false negative myocardial perfusion SEPCT images.Three were triple vessel disease,one Was two, three were one, and the other was patent collateral circulation.Conclusions Stress.redistributed/reinjection 201TI myocardial perfusion SPECT imaging is superior to stress 201Tl/rest 99Tcm-MIBI simultaneous dual-isotopic myocardial imaging in the detec-tion of myocanrdial viability.

Objective To evaluate 99Tcm-Arg-Glu-Ser (99Tcm-RES) as a potential tumor imaging agent. Methods RES was synthesized using solid phase peptide synthesis. The optimal labeling conditions of RES were determined under different reagents and reacting temperatures using SnC12 as reducing agent.The biodistribution of 99Tcm-RES was studied in nude mice bearing human lung cancer A549. Results The radiochemical purity of 99Tcm-RES was up to 85% and the radiochemical purity was 75% ever after 6 h at room temperature. The tumor uptake of 99Tcm-RES was obvious and the radioactivity ratios of tumor/blood,tumor/heart, tumor/liver, tumor/lung, tumor/spleen and tumor/muscle were 5.31, 1.88, 1.57, 3.58,4. 16 and 5.92, respectively at 6 h after 99Tcm-RES injection. Gamma camera imaging showed that tumor uptake of 99Tcm-RES was negative in rabbits with inflammatory mass but positive in those bearing tumor.The radioactivity ratio of tumor/inflammation was 3.12 at 6 h after injection. Conclusion 99Tcm-RES might possibly become a potential tumor imaging agent.

Adult ; Heroin Dependence ; drug therapy ; prevention & control ; Humans ; Male ; Methadone ; therapeutic use ; Patient Compliance ; Treatment Outcome

OBJECTIVETo assess the predictive value of hemoglobin (HGB) levels for non-alcoholic fatty liver disease (NAFLD) by performing a prospective cohort study of NAFLD incidence in a healthy population.

METHODSA total of 2840 individuals in the Xinjiang province were enrolled in the study from 2008 to 2011, based on liver ultrasound showing no evidence of fatty liver disease and the discovery of no major risk factors upon interview. All participants completed an epidemiological questionnaire survey, a physical examination, an abdominal ultrasonography, and gave blood for biochemistry testing. The hazard ratios of NAFLD were compared when the participants were grouped according to HGB level (g/L in quintiles): Q1, less than or equal to 145 for males and less than or equal to 123 for females; Q2, > 145 to less than or equal to 151 for males and > 123 to less than or equal to 129 for females; Q3, > 151 to less than or equal to 155 for males and >129 to less than or equal to 134 for females; Q4, > 155 to less than or equal to 161 for males and > 134 to less than or equal to 139 for females; Q5, > 161 for males and > 139 for females. Between-group comparison of measurement data was carried out by t-test and of percentage or count data by chi-square test. Between group comparison of the HGB level was carried out by one-way ANOVA. The prospective association between HGB levels and NAFLD was assessed by conditioned logistic regression analysis.

RESULTSThe values of body mass index, blood pressure, and triglyceride level were significantly higher in the participants with elevated serum uric acid quartiles. Within the 3-year study period, NAFLD was newly diagnosed in 19.6% of the male participants and 10.1% of the female participants; the difference between males and females reached the threshold of statistical significance (X2 = 51.043, P less than 0.01). The incidence of NAFLD in the quintile groups was 6.10% in Q1, 10.50% in Q2, 13.13% in Q3, 16.95% in Q4, and 22.03% in Q5 (X2 = 70.495, P less than 0.01), and the increasing trend with elevated HGB quartiles was significant (P less than 0.01). In multivariate logistic regression analysis, with adjustment for sex, age, race, metabolic syndrome and its components, the hazard ratios for incidence of fatty liver comparing Q2 to Q5 of HGB concentration to Q1 were 1.125, 1.325, 1.516 and 1.982.

CONCLUSIONElevated HGB concentration is predictive of NAFLD in otherwise healthy subjects and may be used for screening during a routine health check-up.

Adult ; Early Diagnosis ; Female ; Hemoglobins ; analysis ; Humans ; Logistic Models ; Male ; Middle Aged ; Non-alcoholic Fatty Liver Disease ; blood ; diagnosis ; Predictive Value of Tests ; Prospective Studies ; Surveys and Questionnaires

Ibuprofen/ethyl-cellulose (EC)-polyvinylpyrrolidone (PVP) sustained-release composite particles were prepared by using supercritical CO2 anti-solvent technology. With drug loading as the main evaluation index, orthogonal experimental design was used to optimize the preparation process of EC-PVP/ibuprofen composite particles. The experiments such as encapsulation efficiency, particle size distribution, electron microscope analysis, infrared spectrum (IR), differential scanning calorimetry (DSC) and in vitro dissolution were used to analyze the optimal process combination. The orthogonal experimental optimization process conditions were set as follows: crystallization temperature 40 degrees C, crystallization pressure 12 MPa, PVP concentration 4 mgmL(-1), and CO2 velocity 3.5 Lmin(-1). Under the optimal conditions, the drug loading and encapsulation efficiency of ibuprofen/EC-PVP composite particles were 12.14% and 52.21%, and the average particle size of the particles was 27.621 microm. IR and DSC analysis showed that PVP might complex with EC. The experiments of in vitro dissolution showed that ibuprofen/EC-PVP composite particles had good sustained-release effect. Experiment results showed that, ibuprofen/EC-PVP sustained-release composite particles can be prepared by supercritical CO2 anti-solvent technology.
Calorimetry, Differential Scanning ; Carbon Dioxide ; chemistry ; Cellulose ; administration & dosage ; analogs & derivatives ; chemistry ; Crystallization ; Delayed-Action Preparations ; Drug Carriers ; Drug Compounding ; Ibuprofen ; administration & dosage ; chemistry ; Microscopy, Confocal ; Particle Size ; Povidone ; administration & dosage ; chemistry ; Solubility ; Spectrophotometry, Infrared ; Technology, Pharmaceutical ; methods

OBJECTIVETo construct the eukaryotic expression vector of rat GPR17 (rGPR17) cDNA,and to identify its function in HEK293 cells.

METHODSTotal RNA was extracted from rat brain tissue; full-length GPR17 cDNA was prepared by RT-PCR, and cloned into pcDNA3.1(+) plasmid. The recombinant plasmid was converted into E.coli DH5alpha and confirmed by PCR, double enzyme digestion analysis and DNA sequencing. The recombinant plasmid pcDNA3.1(+)-rGPR17 was transiently transfected into HEK293 cells using Lipofectamin 2000. Expression of rGPR17 gene was confirmed by RT-PCR and immunofluorescence staining. The exogenous LTD(4) enhanced intracellular calcium was measured using Fluo-4.

RESULTRT-PCR, double enzyme digestion analysis and sequencing showed that the rGPR17 gene was cloned into recombinant vector, and the recombinant rGPR17 was expressed after transfection in HKE293 cells. LTD(4) increased intracellular calcium release in the transfected HEK293 cells.

CONCLUSIONThe eukaryotic expression vector of rGPR17 cDNA has been constructed; it is functionally expressed in HEK293 cells. This work provides a basis for further research of the GPR17 receptor and its antagonists.

Animals ; Base Sequence ; DNA, Complementary ; genetics ; Escherichia coli ; genetics ; metabolism ; Female ; Genetic Vectors ; genetics ; HEK293 Cells ; Humans ; Male ; Molecular Sequence Data ; Rats ; Rats, Sprague-Dawley ; Receptors, G-Protein-Coupled ; biosynthesis ; genetics ; Recombinant Proteins ; biosynthesis ; genetics ; Transfection

OBJECTIVETo investigate the role of cysteinyl leukotriene (CysLT) receptors in the differentiation of rat glioma C6 cells.

METHODSRat glioma C6 cells were treated with the agonist LTD(4), the CysLT(1) receptor antagonist montelukast and the differentiation inducer forskolin. Cell morphology and GFAP protein expression were determined after treatments.

RESULTForskolin (10 μmol/L) induced morphological changes and GFAP protein expression (cell differentiation) in C6 cells, but LTD(4) (0.1-100 nmol/L) did not induce these changes. Montelukast (1 μmol/L) alone did not affect C6 cell differentiation, while it induced the differentiation when combined with the LTD(4) (100 nmol/L).

CONCLUSIONThe CysLT(2) receptor may modulate the differentiation of rat glioma C6 cells.

Acetates ; pharmacology ; Animals ; Cell Differentiation ; drug effects ; Cell Line, Tumor ; Colforsin ; pharmacology ; Cysteine ; Glioma ; metabolism ; pathology ; Leukotriene Antagonists ; pharmacology ; Leukotriene D4 ; pharmacology ; Leukotrienes ; Quinolines ; pharmacology ; Rats ; Receptors, Leukotriene ; agonists

OBJECTIVETo construct HEK293 cell lines stably expressing hCysLT(2) receptor, and to evaluate its application in screening of synthetic compounds with antagonist activity.

METHODSThe recombinant plasmid pcDNA3.1(+)-hCysLT(2) was transfected into HEK293 cells using Lipofectamin 2000. The transfected HEK293 cells were selected in 96 well plates by limiting dilution with 600 μg/ml C418 for 8 weeks. The expression of human CysLT(2) receptor was detected by RT-PCR and immunofluorescence staining. In HEK293 cells stably transfected with hCysLT(2), the agonist LTD(4)-induced elevation of intracellular calcium concentration ([Ca2(+)]i) was measured as the index for screening compounds with antagonist activity.

RESULTAfter selection in 96 well plates by limiting dilution, 12 monoclones were obtained and 11 of them highly expressed hCysLT(2) receptor. The positive control ATP at 50 μmol/L and LTD(4) at 100 nmol/L elevated [Ca2(+)]i in hCysLT(2)-HEK293 cells. AP-2100984 inhibited LTD(4)-induced [Ca2(+)]i elevation, but selective CysLT(1) receptor antagonists did not exert such an effect. The newly synthesized compounds DXW2, DXW3, DXW4, DXW5, DXW9, DXW25, DXW26, DXW29 and DXW35 at 1 μmol/L significantly inhibited LTD(4)-induced [Ca2(+)]i elevation. The IC(50) values of DXW4 and DXW5 were 0.25 μmol/L and 7.5 μmol/L.

CONCLUSIONHEK293 cell lines stably expressing hCysLT(2) receptor have been successfully constructed, and can be used to screen compounds with CysLT(2) receptor antagonist activity.

Drug Evaluation, Preclinical ; HEK293 Cells ; Humans ; Leukotriene Antagonists ; Receptors, Leukotriene ; genetics ; Transfection

OBJECTIVETo establish a method for screening cysteinyl leukotriene receptor 2 (CysLT(2)) antagonists and to preliminarily screen a series of synthetic compounds.

METHODSRat glioma cell line (C6 cells) highly expressing CysLT(2) receptor was used. Intracellular calcium concentration was measured after stimulation with the agonist LTD(4),which was used to screen compounds with antagonist activity for CysLT(2) receptor. Bay u9773, a CysLT1/CysLT(2) receptor non-selective antagonist, and AP-100984, a CysLT(2) receptor antagonist, were used as control.

RESULTPT-PCR showed a higher expression of CysLT(2) receptor in C6 cells. LTD(4) at 1 mumol/L significantly increased intracellular calcium in C6 cells; the maximal effect was about 37.5% of ATP, a positive stimulus.LTD(4)-induced increase of intracellular calcium was blocked by CysLT(2) receptor antagonists, but not by CysLT(1) receptor antagonists. Among the synthetic compounds, D(XW-)1,2,13,23,29 and 30 inhibited LTD(4)-induced increase of intracellular calcium.

CONCLUSIONLTD(4)-induced change in intracellular calcium in C6 cells can be used as a screening method for CysLT(2) receptor antagonists. The compounds, D(XW-)1,2,13,23,29 and 30, possess antagonist activity for CysLT(2) receptor.

Animals ; Brain Neoplasms ; pathology ; Cell Line, Tumor ; Drug Evaluation, Preclinical ; methods ; Glioma ; pathology ; Leukotriene Antagonists ; isolation & purification ; Leukotriene D4 ; metabolism ; pharmacology ; Rats ; Receptors, Leukotriene ; chemistry