It has been demonstrated by our previous research that 4-(2-acetoxybenzoylamino) butyramide derivatives exhibited good antiepileptic activities. In this paper, to explore the SAR and improve the antiepileptic activities of these derivatives, a series of novel 4-(2-acetoxybenzoylamino) butyramide heterocyclic compounds (5a-5n) were synthesized and biologically evaluated. Their structures were confirmed by 1H MNR, ESI-MS and elemental analysis. Pharmacological test in vivo showed that target compounds (5f, 5i-5n) displayed strong antiepileptic activities on 4-AP induced epilepsy in mice with ED50 values ranging from 0.3137 to 0.3604 mmol x kg(-1).

To explore new agents of gamma-aminobutyric acid (GABA) derivatives with more potent antiepileptic activity, a series of 4-(2-acetoxybenzoylamino) butyramide derivatives were designed and synthesized. All of the novel compounds (5a-51) were synthesized from GABA as starting material, and their structures were confirmed with IR, 1H NMR, EI-MS and elemental analysis. Preliminary pharmacological test in vitro showed that all target compounds displayed strong antiepileptic activities and were worth for further study. The structure-activity relationship of 4-(2-acetoxybenzoylamino) butyramide derivatives was also discussed preliminarily.

BACKGROUND: Stem cell factors are hypoxia-induced neural regeneration factors. They stimulate animals' neural regeneration.OBJECTIVE: To observe Nestin and stem cell factor mRNA expressions after ischemia/reperfusion injury in rat brain, and to analyze the time rule of the two.DESIGN: A randomized controlled animal experiment.SETTING: Department of Ultrasound Diagnosis, Affdiated Hospital of Qingdao University Medical College.MATERIALS: Thirty-six healthy female adult Sprague-Dawley (SD) rats were provided by the Shanghai Laboratory Animal Center, Chinese Academy of Science. Nestin and stem cell factor mRNA in situ hybridization kits and 3,3'-diaminobenzidine (DAB)kit were provided by Boster Bioengineering Co.,Ltd (Wuhan, China).METHODS: This study was performed at the Shangdong Key Laboratory for Prevention and Treatment of Encephalopathy from January to June 2005. Thirty-two rats were created into models of ischemia/reperfusion models by occluding left middle cerebral artery with suture. At ischemia 1.5 hours and reperfusion 2, 6, 12, 24 hours, 2, 3, 7, 14 days, 4 rats were separately used in order to observe the expressions of Nestin and stem cell factor mRNA. The other 4 rats were used for sham-operation,in which, suture insertion was omitted, and the other procedures were identical to experimental groups. The expressions of Nestin and stem cell factor mRNA were detected in the cortex, corpora striatum and paraventricular nucleus region in rat brain by in situ hybridization.MAIN OUTCOME MEASURES: Nestin and stem cell factor mRNA expressions in the cortex, corpora striatum and paraventricular nucleus region in rat brain.RESULTS: Thirty-six rats were included in the final analysis. Nestin mRNA and stem cell factor were weakly expressed in the cortex, corpora striatum and paraventricular nucleus region in rats of sham-operation group. After ischemia/reperfusion, Nestin mRNA expression at each time point was significandy higher in the experimental groups (except in the cortex at ischemia 1.5 hours and reperfusion 2 hours, in the corpora striatum at ischemia 1.5 hours and reperfusion 2 and 6 hours and in the paraventricular nucleus region at ischemia 1.5 hours and reperfusion 2, 6 hours and 14 days) than in the sham-operation group (P＜0.05). While stem cell factor mRNA expression at each time point was significandy higher in the experimental groups (except in the cortex at ischemia 1.5 hours and reperfusion 2,6 and 12 hours, in the corpora striatum at ischemia 1.5 hours and reperfusion 2 and 6 hours and in the paraventricular nucleus region at ischemia 1.5 hours and reperfusion 2 hours and 14 days) than in the sham-operation group (P＜0.05).CONCLUSION: The time rule of stem cell factor mRNA expression is basically the same as that of neural stem cell proliferation. It indicates that following cerebral ischemia/reperfusion, stem cell factor mRNA expression may promote the proliferation of neural stem cells.

Objective:To explore the influence of different cell culture methods in the genome-wide DNA methylation status of breast cancer MDA-MB-231 cells,and to clarify the relationship between genome-wide DNA methylation status and cell growth environment and the role of genome-wide DNA methylation status in the occurrence and development of tumor.Methods:The MDA-MB-231 cells were cultured with 2D and 3D cell culture models and mouse orthotopic transplantation model (Ti model)and collected, then DNA was extracted by DNA extraction kit and the genome-wide DNA methylation status of MDA-MB-231 cells after cultured with three different culture methods was detected by DNA methylation chip,then the value of beta,DiffScore and Delta_Beta of the CpG loci of each gene were calculated by applying Genomestudio software, and the differential methylation genes were screened by Genomestudio software and GO and Pathway analysis of these genes were performed in DAVID on-line analysis tool.Results:All 480 genes of the MDA-MB-231 cells showed significant differences in the degree of methylation in 3D and 2D models (P<0.05);86 448 genes in 3D and Ti models (P<0.05);90 005 genes in Ti and 2D models (P<0.05).The differential methylation genes in 3D and 2D,3D and Ti,and Ti and 2D models were enriched on the multicellular organismal development term and cell differentiation term (P<0.05);also on MAPK signaling pathway,cell adhesion molecules (CAMs),and regulation of actin cytoskeleton (P<0.05). Conclusion:There are differences in genome-wide DNA methylation status of MDA-MB-231 cells cultured in 2D, 3D cell culture and Ti models.

Objective To investigate the ultrasonographic characteristics of angiofollicular lymph node hyperplasia (AFH). Methods The ultrasonographic and pathological characteristics in nine patients with pathologically confirmed AFH were retrospectively analyzed. Results All the 9 patients were hyaline vascular type of AFH. Ultrasonic manifestations included complete capsule, regular shape and clear boundary, internal solide low echo, mild posterior echo enhancement and without cystic degeneration, which was relative to the less incidence of necrosis and hemorrhage on pathologic findings. Calcification in the lesions were found in two patients. Color Doppler flow signals were observed in the periphery of lesions in 9 patients, and rich flow signals were observed in the center of lesions in 2 of them. Conclusion The ultrasonic manifestations of AFH has its own characteristics. The ultrasonic manifestations combined with clinical features are helpful to the differential diagnosis. The final diagnosis depends on pathologic examination.

To explore novel coumarin derivatives with more potent anti-proliferative activity, a series of novel compounds were designed and synthesized by linking Schiff base and N, N-bis (2-chloroethyl) amine pharmacophore of nitrogen mustards to the coumarin's framework. Their structures were confirmed by 1H NMR, MS and element analysis techniques. In vitro anti-proliferative activities were evaluated against HepG2, DU145 and MCF7 cell lines by the standard MTT assay. The results showed that some of the target compounds exhibited strong anti-proliferative activities against selected tumor cells, and compounds 7c, 7f, 7g, 7h and 7q were better than or equal to the activities of positive control, they deserved further development.

Objective To explore the value of virtual touch tissue quantification (VTQ) elastography and its influencing factors in identifying benign and malignant thyroid nodules.Methods A retrospective analysis was conducted in 210 cases of 240 thyroid nodules.Their images,including 2D ultrasound,color Doppler flow imaging (CDFI) and VTQ elastography,were reviewed,and the scanning view,the maximum diameter of the nodule,inside blood flow,calcifications and its depth beneath the skin were recorded.The value of shear wave velocity(SWV) in identifying benign and malignant thyroid nodules was calculated using receiver operating characteristic (ROC) curve.The influences of the maximum diameter of the nodules,calcifications,internal blood flow,the depth beneath skin and scanning views as well as type of pathology on the value of SWV were analyzed using multiple linear regressions (MLR).Results The sensitivity and specificity of VTQ in differential diagnosis of benign and malignant thyroid nodules was 74.8％ and 73.4％,respectively,and the area under ROC curve was 0.799.MLR indicated that the maximum diameter of the nodule,the type of pathology and internal blood flow were correlated with the SWV value (P ＜0.05),of which,the type of pathology was the important factor (standardized coefficient was-0.312).Microcalcifications,the depth of the nodules located and the scanning surface were not significantly related to SWV value (P ＞0.05).Conclusions VTQ can quantitatively provide the information on the hardness of thyroid tissue,which is of a definite value in the differential diagnosis of the nodules.The pathology of the nodule,its internal blood flow and maximum diameter are the factors that affect the value of SWV,and not its depth,scanning views and microcalcifications.

Objective: To explore the preparation methods of nanomete r powder of ZrO 2 for dental application. Methods:Zirconia gel wa s dehydrated by heterogeneous azeotropic distillation process and n-butanol was used as azeotropic solvent. The properties of ultrafine powder obtained via dec ompression (process b), atmosphere pressure (process c) and direct ethanol-wash ing (process a) were studied. Results: After drying and calcini ng the gel, the ultrafine powder obtained from process a,b and c was about 25 n m,22 nm and 17 nm respectively. 3Y-TZP ceramic prepared with the three kinds of nanometer powder had bending strength of 660 MPa,710 MPa and 640 MPa; fracture toughness of 4.34 MPa?m 1/2 ,4.77 MPa?m 1/2 and 4.24 MPa?m 1/2 , respectively. Conclusion: By the heterogeneous azeotropic dis tillation process, zirconia ultrafine powder without hard agglomeration (d BE T=17 nm) can be obtained.

OBJECTIVETo provide a theoretical basis for designing of lumbar intervertebral disc prosthesis by collecting the data of the lumbar endplate morphology.

METHODSA total of 100 healthy adults were measured about the following parameters: lumbar lordosis, the Cobb angle of each segment, the concavity depth (ECD) of the endplate, the location of concavity apex (ECA) of the endplate. And a correlation analysis on lumbar lordosis and ECD, ECA was made, respectively.

RESULTSIn total, 100 volunteers were measured. The mean age of the volunteer was 40 years (range 20 - 50 years); the average depth of ECD was (2. 37 ± 1. 42) mm, the average location of ECA was (52. 21 ± 9. 70) %; the average depth of ECD of inferior endplate (IEP) was (2. 81 ± 1. 52) mm (0. 54 - 7. 60 mm), and the parameter of the superior endplate (SEP) was (1. 94 ± 1. 16)mm(0. 39 - 6. 10 mm). The average depth of ECD of the IEP was bigger than of the SEP for each lumbar vertebral body. Most of the location of ECA was at the back of the intervertebral body, the average location of ECA of IEP was (49. 60 ± 8. 78) % (22. 57% - 75. 58%), and the parameter of the SEP was (55. 03 ± 9. 90) % (16. 03% -75. 58%); the mean angle of lumbar lordosis was 39. 760 11. 25°(13. 8° - 72. 00°). There was no obvious correlation between the lumbar lordosis and the ECD (r -0. 193, P =0. 195), neither was the location of ECA(r =0. 080, P =0. 592).

CONCLUSIONMost of the location of ECA is at the back of the intervertebral body, the average depth of ECD is 2. 37 mm, the average location of ECA is 52. 21%.

Adult ; Humans ; Intervertebral Disc ; Lumbar Vertebrae ; anatomy & histology ; Lumbosacral Region ; anatomy & histology ; Middle Aged ; Prostheses and Implants ; Reference Standards ; Spine ; anatomy & histology ; Young Adult

Objective To investigate the traumatic characters, the causative factors and the outcomes of surgical treatments of cervical spinal cord injuries without radiographic abnormality(SCIWORA).Methods From March 2000 to July 2004, 81 patients of cervical SCIWORA undergone surgery were evaluated retrospectively. There were 55 males and 26 females, with a mean age of 57.3 years. According to the mechanisms of injuries and pathological changes of the cervical spine, the causative factors were divided into 3 groups: hyper-flexion type of injury (1 or 2 segments) with protrusion or prolapse of the cervical intervertebral discs (19 cases), hyper-extension type injury with multiple (≥3 segments) cervical spinal stenosis (41cases), and whiplash injury with multiple cervical spinal stenosis and segmental intervertebral instability or anterior protrusion of the cervical intervertebral discs (21 cases). A variety of surgeries as anterior discectomy with interbody fusion, multiple posterior decompressions with cervical laminoplasty, and multiple posterior decompressions with internal fixation at the facet joints were performed based the classification. Results The average follow-up period was 78.5 month (54-118 months). During the follow-up of 1 month, 3 months,1 year and last visit post-operatively, the rate of JOA improvement were 25.1%, 41.3%, 63.6% and 60.9%respectively. In the long-term follow-up, the good ratio of neurological function was obtained with 80.2%.Conclusion SCIWORA is considered as a course of acute, dynamic and limited injury. In spite of common clinical manifestation, its traumatic characters and causative factors are different indeed. The distinct improvement of neurological function can also be achieved with proper classification and surgery.