AIM　A series of 4-piperidinylthioether and sulfone derivatives of 4-［1-hydroxy-1-(2,3-dimethoxyphenyl) methyl］-N-2-(4-fluorophenylethyl) piperidine (MDL 100907) were synthesized in order to find new 5-HT2A selective ligands. METHODS　Title compounds 2a-2c were synthesized from 2,3-dimethoxythiophenol and tested for their affinities to 5-HT2A, 5-HT2C, 5-HT6 and 5-HT7 receptors and some other nervous transmitter receptors in vitro. RESULTS　Compounds 2a-2c are new compounds. The results of the binding assay demonstrated that they have relatively high selectivity for 5-HT2A receptor in vitro. CONCLUSION　Some sulfur containing analogues of MDL 100907 showed selective affinity to 5-HT2A receptor and are worth further study.

Objective To investigate the influencing factors of hemorrhagic transformation in non-thrombolysis patients after acute cerebral infarction. Methods According to Chengdu Stroke Registry Project,2598 consecutive patients with acute cerebral infarction admitted to the Department of Neurology,West China Hospital within 1 week of attack from January 2010 to December 2013 were enrolled prospectively. The patients were divided into a hemorrhagic transformation group and a non-hemorrhagic transformation group according to whether they had hemorrhagic transformation or not. As for patients with hemorrhagic transformation,they were divided into a symptomatic hemorrhagic transformation (SHT)group and an asymptomatic hemorrhagic transformation (ASHT)group according to whether they had aggravation of symptom and sign. The baseline data of all patients were collected and compared between the groups. The P<0. 1 variables of the univariate analysis result were enrolled in multivariate logistic regression analysis in order to identify the independent influencing factor of hemorrhagic transformation. Results In 2598 patients,249 (9. 6%)had hemorrhagic transformation,28 of them (1. 1%)were SHT and 221 (8. 5%)were ASHT. There were significant differences in male,hypertension,dyslipidemia,atrial fibrillation,drinking and smoking ratio,blood glucose,cholesterol,low density lipoprotein cholesterol, National Institutes of Health Stroke Scale (NHISS)scores,and the trial of Org 1072 in acute stroke treatment (TOAST)classification between the HT group and the non-HT group (all P<0. 05). There were no significant difference in the related influencing factors between the SHT group and the ASHT group (all P>0. 05). The results of multivariate logistic regression analysis showed that dyslipidemia (OR,0. 588, 95%CI 0. 374-0. 924,P=0. 021)was negatively correlated with hemorrhagic transformation. Atrial fibrillation (OR,3. 188,95%CI 2. 159-4. 707,P<0. 001),blood glucose (OR,1. 081,95%CI 1. 044-1. 119,P<0.001),and NHISS score (OR,1. 305,95%CI 1. 170-1. 455,P<0. 001)were positively correlated with hemorrhagic transformation. In TOAST classification,relative to the large atherosclerotic stroke,the small artery occlusive cerebral infarction was negatively correlated with hemorrhagic transformation (OR,0. 315, 95%CI 0. 167-0. 596,P<0. 001). After removing the influencing factor of atrial fibrillation,compared with the large artery atherosclerotic stroke,cardioembolism stroke was positively correlated with hemorrhagic transformation (OR,2. 823,95%CI 1. 946-4. 095,P<0. 001). Conclusion Dyslipidemia,atrial fibrillation,blood glucose,NHISS score and TOAST classification were independently associated with hemorrhagic transformation in non-thrombolysis patients after acute cerebral infarction.

· AIM: To study the effects of topical anesthesia on corneal thickness in myopic eyes with Orbscan topography system and to assess the application prospect of this device in determining the corneal thickness for refractive surgery.and 5 minutes after administration of one drop of Benoxil (Oxybuprocaine) 4g/L solution (Santen, Japan) to 98 eyes (98 patients). The numeric value of the corneal thinness (THN) and the mean central corneal thickness (CCT) of 2mm in diameter were obtained before and after the instillation. The changes in anterior chamber depth (ACD) were also studied.P＜0.001) and CCT by 3.10±7.13μm (t=-4.310, P＜0.001) were found following the instillation of the topical anesthetic. There were no statistically significant changes in ACD (t=1.288, P=0.201).immediate effects on the corneal thickness in myopic eyes and this have implications for corneal refractive surgery and even for the accuracy of applanation tonometry.

To improve the sensitivity of molecularly imprinted electrochemical sensors, a Pd nanoparticles-modified molecularly imprinted polymer (MIP) film for the determination of trimethoprim (TMP) was developed by thermal polymerization with N, N′-methylene diacrylamide as a functional monomer, Pd nanoparticle as a dopant and ethylene glycol maleic rosinate acrylate as a crosslinking agent.The morphologies and chemical structures of the Pd nano-materials and the imprinted films were characterized using Fourier transform infrared spectroscopy and scanning electron microscopy, respectively.The electrochemical properties of the nano-doped and undoped MIP sensors were investigated by cyclic voltammetry and electrochemical impedance spectroscopy.Results showed that the morphologies and chemical structures and the electrochemical properties of the doped molecularly imprinted sensor were remarkably different from those of the undoped imprinted sensor.Linear responses of the imprinted sensor to TMP were observed for concentrations ranging from 5.0×10-7 mol/L to 4.0×10-3 mol/L (R=0.9995), with a detection limit of 3.2×10-8 mol/L (S/N=3).The Pd nanoparticle doped MIP sensors exhibited high selectivity.The chronoamperometry showed that no interference from potential interfering species such as sulfamethoxazole, sulfadiazine, glucose, and urea were noted.The proposed electrochemical sensor was used to determine TMP in actual samples, with average recoveries of 96.8%-102.0%.

Objective:To predict Th/B cell epitopes in HA of influenza virus(H1N1)and analyze antigenicity of the candidate epitopes in order to develop epitope-bacterin by the way of bioinformatics.Methods:The HA amino acid sequences of infiuenza virus(H1N1),which the viral infection was prevalent recently,were downloaded from Genbank.The Th/B cell epitopes were predicted and analyzed by bioinformatics methods.Then,specificity and conservation of the candidate epitopes were estimated.Finally,antigenicity of the candidate epitopes was identified by influenza virus(H1N1)positiVe serum samples of mice.Results:Three Th/B cell epitopes containing HA_(73-87),HA_(125-139),HA_(188-205) were acquired Two of the candidate epitopes were in a relatively conserved domain of HA1,and a deal of 2006-2009 influenza virus(H1N1)isolates contained the sequences.Moreover,the candidate epitopes were showedin a distinct antibody combining reactivity with the influenza virus (H1N1)positive serum of mice,which inferred the predicted epitopes to be functional ones.Conclusion:The selected epitopes are able to be functional HA Th/B cell epitopes of influenza virus(H1N1).Our study also establish the foundations for the further research of influenza virus infectlon and immunity mechanism,the recognition of influenza virus(H1N1)functional epitope and the development of epitope vaccines.

Objective:To predict Th/B cell epitopes in HA of influenza virus(H1N1) and analyze antigenicity of the candidate epitopes in order to develop epitope-bacterin by the way of bioinformatics.Methods:The HA amino acid sequences of influenza virus (H1N1),which the viral infection was prevalent recently,were downloaded from Genbank.The Th/B cell epitopes were predicted and analyzed by bioinformatics methods.Then,specificity and conservation of the candidate epitopes were estimated.Finally,antigenicity of the candidate epitopes was identified by influenza virus (H1N1) positive serum samples of mice.Results:Three Th/B cell epitopes containing HA73-87,HA125-139,HA188-205 were acquired.Two of the candidate epitopes were in a relatively conserved domain of HA1,and a deal of 2006-2009 influenza virus (H1N1) isolates contained the sequences.Moreover,the candidate epitopes were showedin a distinct antibody combining reactivity with the influenza virus (H1N1) positive serum of mice,which inferred the predicted epitopes to be functional ones.Conclusion:The selected epitopes are able to be functional HA Th/B cell epitopes of influenza virus (H1N1).Our study also establish the foundations for the further research of influenza virus infection and immunity mechanism,the recognition of influenza virus (H1N1) functional epitope and the development of epitope vaccines.

Objective To investigate the trend and related determinants of cigarette smoking on experimental smokers among undergraduate students in Changsha.Methods Stratified sampling method was adopted and 3600 undergraduate students from grade 1 to 3 in Changsha city were investigated through a self-administered questionnaire.All the experimental smokers during the last month were selected and divided into two groups based on the present smoking status.x2 test and logistic regression analysis were used to compare the differences of cigarette smoking among subpopulations and to explore the determinants.Results Among the 1550 experimental smokers of undergraduate students,the prevalence of cigarette smoking was 30.8％(95％CI:28.5-33.1).Students from the second-class(OR=2.367)or the third-class universities(OR=2.562)were more likely to adopt smoking behavior than those from top universities.Students majored in sports or arts(OR=2.456)were significantly more inclined to smoke than the liberal arts students.Students whose father were cadres(OR=1.602)were more likely to become smokers than those whose fathers were workers.Students being males(OR=7.386),having high monthly expenses(OR=1.139),with positive attitude to smoking benefits(OR=1.140)were risk factors for smoking.Number of smoking members in the family(OR=1.801)was significantly associated with the prevalence of cigarette smoking.Knowledge on diseases caused by smoking(OR=0.806)was protecting factor to smoking among the experimental smokers.Conclusion Those experimental smokers among undergraduate students might become smokers and the determinants of cigarette smoking behavior would include:ranking of universities,students' major,gender,father' s occupation,amount of pocket money,number of smoking members in the family,knowledge about smoking,the attitude to the benefit of smoking.

OBJECTIVETo study the pattern of polymorphism expression of heat-shock protein 70 (HSP70) family in A549 cell line treated with different concentrations of benzo(a)pyrene (BaP) and its probable biological effect.

METHODTwo-dimensional polyacrylamide gel electrophoresis (2D-PAGE) was used for the HSP70 expression analysis.

RESULTS2D-PAGE showed that when A549 cells were exposed to different concentrations of BaP (0.1, 1.0, 5.0, 10.0 micromol/L) for 24, 48 h respectively, the HSP72 in A549 gradually declined as BaP concentrations increased [the integral OD (IOD)] for 24 h were: 150.36 +/- 26.03, 98.57 +/- 13.34, 64.92 +/- 15.03, 34.65 +/- 19.10, 32.92 +/- 18.71 respectively, for 48 h: 126.85 +/- 17.41, 106.19 +/- 15.32, 73.64 +/- 21.02, 35.18 +/- 11.95, 16.27 +/- 9.35 respectively), while the IOD of HSP73 did not show any remarkable change (24 h: 102.29 +/- 21.24, 87.71 +/- 18.70, 71.19 +/- 14.08, 71.87 +/- 15.16, 72.78 +/- 17.31 respectively; 48 h: 86.66 +/- 16.86, 75.67 +/- 10.61, 66.83 +/- 12.63, 67.29 +/- 10.26, 91.37 +/- 13.68 respectively).

CONCLUSIONBaP can inhibit HSP72 expression and with certain dose-effect relationship, but cannot affect HSP73 expression.

Benzo(a)pyrene ; Cell Line, Tumor ; Dose-Response Relationship, Drug ; Electrophoresis, Polyacrylamide Gel ; HSP70 Heat-Shock Proteins ; genetics ; metabolism ; Humans ; Polymorphism, Genetic

Objective To observe the brain activation of interictal epiletiform discharges(IEDs) and to localize the epileptogenic foci of epilepsy.Methods The electroencephalogram(EEG)and functional MRI data of 12 focal epileptic patients were acquired using a combination of EEG and functional MRI simultaneously.The IEDs onset time detected with EEG were set as the time parameters in an event- related paradigm of functional MRI analysis.The spatial and temporal characters of IEDs activation were analyzed in detail.In order to confirm the consistency of this method,all patients were scanned repeatedly and the results were correlated with clinical evaluation.Results Of the 12 patients,valid data from EEG- fMRI were obtained from 10 patients in a total of 18 sessions..Compared with the structural foci,the epileptic foci localization results of eleven sessions were good,five sessions were fairly good,and two sessions were poor.The results obtained from six patients in two separate sessions were concordant.respectively.Moreover,thalamic activation was detected in ten sessions,cerebellar activation was detected in all sessions,and the deactivation was found in the default mode loci in nine sessions. Conclusion The method of performing EEG and fMRI simultaneously can potentially be a useful tool in epilepsy research.

OBJECTIVESTo study the efficacy of proximal embolic protection device in preventing intracranial artery embolization during carotid artery stenting (CAS) and to evaluate its security and maneuverability.

METHODSFrom October 2007 to July 2008, 23 patients with carotid artery stenosis who were suitable for surgical therapy according to the standards of NASCET or ACAS were enrolled in this clinical research. Among them 19 patients (82.6%) were symptomatic, 6 patients (26.1%) with 50%-70% stenosis and 17 cases (73.9%) with > 70% stenosis. All the patients received carotid angioplasty and stenting under the protection of MO. MA system (one kind of proximal embolic protection device). We recorded the cerebral ischemic time during the procedure and observed neurologic events within 30 days.

RESULTSAll the procedures were performed successfully, the mean carotid artery blocking time was (5.3 +/- 1.2) min. No death or stroke occurred during perioperative period. Two cases of patients developed transient loss of consciousness combined with contralateral limb convulsion, while the common carotid artery was occluded by balloon. Two cases of patients developed bradycardia, sustained 6 hours and 1 week. Plaque debris in the withdrawal blood from carotid artery were found in 9 cases. At 30-day follow-up after CAS, TIA occurred in 1 case, new contralateral stroke occurred in 1 case, the incidence of 30-day stroke and death rate was 4.3%.

CONCLUSIONThe application of proximal embolic protection device in CAS procedure for preventing neurologic complications is safe and effective, especially for severe stenosis and unstable plaque in carotid artery stenting.

Aged ; Aged, 80 and over ; Angioplasty, Balloon ; instrumentation ; methods ; Carotid Stenosis ; surgery ; Embolic Protection Devices ; Female ; Follow-Up Studies ; Humans ; Intracranial Embolism ; etiology ; prevention & control ; Male ; Postoperative Complications ; prevention & control ; Stents ; Treatment Outcome