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.

Pololike kinase 1(Plk1)contain an Nterminal Ser/Thr kinase catalytic domain and a Cterminal region that contains two poloboxes.As a key regulator of multiple steps during cell cycle across eukaryotic species,many proteins interact with Plk1.Plk1 is highly expressed in malignant cells and serves as a negative prognostic marker in specific human cancer types.Plk1 is a potential target for cancer therapy.Some novel smallmolecule inhibitors of pololike kinase 1 provide novel opportunities for cancerdrug discovery,such as BI 2536,ON01910.

OBJECTIVETo search all studies that had been published in the world with regarding to the effectiveness of the extent of intralesional curettage and wide excision for recurrence rate and complications and comparative functional outcomes in patients with giant cell tumours (GCT) of the distal radius and analyze them which were in high quality by means of Meta analysis, in order to give some evidences for the choice of method dealing with giant cell tumors GCT in surgery.

METHODSCochrane central register of controlled trials(Issue 8 2014), PubMed(1970-01-01/2013-01-01), Ovid (1970-01-01/2013- 01-01), Elsevier (1970-01-01/2013-01-01), CNKI (1970-01-01/2013-01-01) were searched. Including intralesional curettage and wide excision were performed to treat giant cell tumors (GCTs) of the distal radius in the literatures, selecting on meet eligibility in the standard literatures underwent strict quality assessment. The Meta-analysis was performed with software RevMan5.0 from the Cochrane collaboration. Additionally, the analysis checked the heterogeneity of data. The effectiveness of the extent of intralesional curettage and wide excision for recurrence rate and complication in patients with giant cell tumours of the distal radius were evaluated and Odds Ratio was calculated.

RESULTSSeven relevant articles were identified involving total 163 cases. Among them, 92 cases were intralesional curettage (PMMA, n = 54; bone graft, n = 33; no PMMA or bone grafts, n = 5) and 71 cases were wide excision. The patients in the intralesional curettage group had a higher recurrence rate [OR = 3.87, 95% CI (1.42, 10.53)],especially for Campanacci grade 3 GCTs [OR = 10.12, 95% CI (1.57, 65.27)], yet fewer major complications [OR = 0.13, 95% CI (0.04, 0.40)] than the wide excision group. The use of PMMA versus bone graft did not affect the recur- rence rate [OR = 0.96, 95% CI (0.26, 3.56)]. By selecting the system evaluation of MSTS, the VAS and dynamometer, the result showed that the intralesional curettage group was equivalent or preferable to wide excision in terms of function rehabilitation.

CONCLUSIONBased on data obtained from the limited number of studies available, intralesional curettage appears to be moreappropriate for the treatment of local lesions (Grade 1 and 2) than Grade 3 GCTs of the distal radius. Moreover, PMMA was not additionally effective as an adjuvant, the intralesional curettage group was found to be equivalent or preferable to wide excision in terms of function rehabilitation.

Bone Neoplasms ; surgery ; Curettage ; methods ; Giant Cell Tumor of Bone ; surgery ; Humans ; Radius ; surgery

Objective To investigate the clinical features of Guillain-Barre syndrome (GBS) and clarify the long-term prognosis of acute inflammatory demyelinating polyneuropathy (AIDP) and acute motor axonal neuropathy (AMAN). Methods We conducted an analysis of the clinical data of 50 patients with GBS treated in our hospital between 2003 and 2007. According to the eleetrophysiological criteria, the eases were classified into AIDP (n=24) and AMAN eases (n=22), with 4 eases of unknown classification. The patients unable to walk upon discharge were followed up for more than 6 months, and the clinical features and prognosis of the two groups were compared. Results The age, gender, cranial nerve involvement, Hughes grade at the initial neurological examination and at the time of symptom peak did not differ significantly between the patients with AIDP and AMAN (P>0.05), and most of the AMAN patients had a good recovery. The number of patients capable of walking at one month after the onset was comparable between the two groups (P>0.05). In AMAN group, the percentages of patients with slow recovery and those having rapid recovery were significantly higher than those in AIDP group (P<0.05). Conclusion The clinical recovery of AMAN patients can be either rapid or prolonged, and rigorous immunotherapy should be administered to achieve early recovery and ensure more favorable outcomes of the patients.

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.
4-Aminopyridine ; Amides ; chemical synthesis ; chemistry ; therapeutic use ; Animals ; Anticonvulsants ; chemical synthesis ; chemistry ; therapeutic use ; Epilepsy ; chemically induced ; drug therapy ; Female ; Male ; Mice ; Molecular Structure ; Random Allocation ; Structure-Activity Relationship ; gamma-Aminobutyric Acid ; chemistry

OBJECTIVETo explore the relationship between body mass index, waist circumference and blood pressure among residents in Chongqing area.

METHODSA total of 5246 residents aged 15 and over in Chongqing area were enrolled in this study by use of stratified sampling and cluster sampling methods. Data on blood pressure (SBP, DBP), pulse, height, body weight, waist and hip circumferences as well as questionnaire survey were analyzed.

RESULTSThe level of SBP and DBP and hypertension prevalence rate were significantly positively correlated with BMI (all P < 0.01). SBP, DBP levels and hypertension prevalence rate were significantly higher in people with abdomen obesity than people with normal waist circumference (all P < 0.01). BMI, waist circumference in hypertensive residents were significantly higher than non-hypertensive residents (all P < 0.01).

CONCLUSIONBlood pressure level and hypertension prevalence rate were closely related with BMI and waist circumference among residents in Chongqing area.

Adolescent ; Adult ; Aged ; Blood Pressure ; Body Mass Index ; China ; epidemiology ; Female ; Heart Rate ; Humans ; Hypertension ; epidemiology ; physiopathology ; Male ; Middle Aged ; Prevalence ; Risk Factors ; Rural Population ; Urban Population ; Waist Circumference ; Waist-Hip Ratio ; Young Adult

OBJECTIVETo establish and evaluate a new method for measurement of dental plaque by using cellular neural network-based image segmentation.

METHODSA total of 195 subjects were selected from community population. After dental plaque staining, oral digital picture of anterior teeth area was taken by an Olympus digital camera (C-7070 Wide Zoom). At the same time, the Turesky dental plaque indices of anterior teeth were evaluated. The image analysis was conducted by cellular neural network-based image segmentation.

RESULTSThe image cutting errors between two operators were very small. The Kappa value is 0.935. Pearson's correlation coefficient is 0.988 (P < 0.001). There was high correlative consistency between traditional dental plaque index and plaque percentage obtained by using image analysis. Pearson's correlation coefficient was 0.853 (P < 0.001).

CONCLUSIONSCellular neural network-based image segmentation is a new method feasible for evaluating dental plaque.

Dental Plaque ; diagnosis ; Dental Plaque Index ; Female ; Humans ; Image Processing, Computer-Assisted ; Male ; Neural Networks (Computer) ; Photography, Dental

OBJECTIVETo study the effect of N-glycosylation on the modification of microvilli on the surface of rat liver epithelial cell WB-F344 and the growth of the cells in culture.

METHODSRecombinant adeno-associated virus (rAAV) expression vector pAGX (+) containing an antisense or a sense fragment of 6A8 cDNA encoding a human alpha-mannosidase was constructed. The recombinant vectors or the mock were transfected into WB-F344 cells by means of lipofectAmine. The transfected cells were selected in G418 medium and cloned by means of limiting dilution. Integration of the transfected DNA into host DNA was detected by neo PCR. Rat liver ER alpha-mannosidase activity in cell supernatant was measured by using P-nitrophenyl-alpha-D-mannopyranoside as a substrate. Microvilli on cell surface were observed upon a scan electron microscope. The growth curves of the cells in culture were drawn.

RESULTSThe cell clones transfected with antisense 6A8 showed reduction of ER alpha-mannosidase activity with various degrees. Clone AS1 and AS2 cell showed a pronounced reduction of the enzymatic activity. In the study on AS1 cells, Con A binding to the cells was found to be enhanced, cell growth in culture became slow from day 5. The microvilli on the cells were reduced and blunted.

CONCLUSIONSTransfection with antisense 6A8 resulted in reduction and blunting of microvilli on the surface of growing WB-F344 cells, which might be related to N-glycosylation modification.

Animals ; Cloning, Molecular ; Epithelial Cells ; cytology ; Glycosylation ; Liver ; cytology ; Microvilli ; Rats ; Transfection ; alpha-Mannosidase ; genetics ; metabolism

This study was purposed to investigate the serum levels of soluble intracellular adhesion molecule (sVCAM-1), interleukin 18 (IL-18) and vascular endothelial growth factor (VEGF) in patients with aplastic anemia (AA) and their clinical significance. Enzyme linked immunosorbent assay (ELISA) was used to detect sVCAM-1, IL-18 and VEGF in serums of 30 patients with AA and 25 normal controls. The results showed that the serum levels of sVCAM-1 and IL-18 in patients with AA [(839.08 +/- 173.97) ng/ml, (380.35 +/- 47.76) pg/ml] were significantly higher than those in normal controls [(538.16 +/- 91.21) ng/ml, (256.39 +/- 59.52) pg/ml] (p < 0.01; p < 0.01). The levels of sVCAM-1 and IL-18 in severe AA patients [(969.94 +/- 182.54) ng/ml, (388.96 +/- 46.06) pg/ml] were higher than those in chronic AA patients [(709.26 +/- 165.32) ng/ml, IL-18 (352.21 +/- 47.08) pg/ml] (p < 0.01; p < 0.05), but the level of VEGF in AA patients [(69.63 +/- 27.42) pg/ml] was lower than that in the normal controls [(125.62 +/- 32.15) pg/ml] (p < 0.01)]. The level of VEGF in severe AA patients [(51.30 +/- 29.86) pg/ml] was significantly lower than that in chronic AA patients [(80.02 +/- 25.14) pg/ml] (p < 0.01). The levels of sVCAM-1 and IL-18 in AA patients after treatment were lower than those before treatment (p < 0.01; p < 0.05), but the level of VEGF after treatment was significantly higher than that before treatment (p < 0.05). It is concluded that the high levels of sVCAM-1, IL-18 and low level of VEGF in serum may be involved in the pathogenesis and progress of AA.
Adolescent ; Adult ; Aged ; Anemia, Aplastic ; blood ; Case-Control Studies ; Female ; Humans ; Interleukin-18 ; blood ; Male ; Middle Aged ; Vascular Cell Adhesion Molecule-1 ; blood ; Vascular Endothelial Growth Factor A ; blood ; Young Adult

OBJECTIVETo investigate the inhibitory effect of 6A8 alpha-manosidase expression on the adhesiveness of CNE-2L2 cells to laminin and the lamellipodia on cell surface.

METHODS6A8 alpha-manosidase expression was detected by Western blotting. For assaying the adhesion of cells to laminin, cells were incubated in laminin-coated plate at 37 degrees C for 1 h, the adhered cells were stained with crystal purple dissolved in 0.1 mol/L Sodium Citrate/50% ethanol. Absorbance 540 nm was measured. Adhesion rate (R) was calculated according to formula R = AT/A100 x 100%. Here A100 represents 100% adhesion. lamellipodia on cell surface was observed upon a scanning electron microscopy.

RESULTSThe adhesion rate of two clones (AS1 and AS2) with inhibition of 6A8 alpha-manosidase expression to laminin was 0.447 +/- 0.096 and 0.533 +/- 0.065 respectively. The adhesion rate of three controls with normal expression of 6A8 alpha-manosidase to laminin was 0.78 +/- 0.035, 0.7 +/- 0.05 and 0.80 +/- 0.04 respectively. The difference was significant (P < 0.01). CNE-2L2 cells with normal expression of 6A8 alpha-manosidase was rich in lamellipodia on their surface. Lamellipodia nearly disappeared on the cells with inhibition of 6A8 alpha-manosidase expression.

CONCLUSIONSInhibition of 6A8 alpha-manosidase expression results in decrease of adhesion to laminin and reduction of lamellipodia of human nasopharyngeal carcinoma cell CNE-2L2.

Cell Adhesion ; drug effects ; Humans ; Laminin ; physiology ; Nasopharyngeal Neoplasms ; pathology ; Neoplasm Metastasis ; Neoplasm Proteins ; genetics ; physiology ; Pseudopodia ; physiology ; Tumor Cells, Cultured ; alpha-Mannosidase ; biosynthesis ; genetics