Chronic Disease ; therapy ; Constipation ; diagnosis ; therapy ; Gastrointestinal Transit ; Humans

To explore a new strategy for further optimization to the C-3 bioisteric heterocyclic ring of fluoroquinolones,twelve novel fluoroquinolone C-3 s-triazole Schiff-base carboxylic acid derivatives(7a-71) were designed and synthesized with both functionalized sulfanylacetic acid and Schiff-base moieties as the modified side-chain for the C-3 bioisosteric s-triazole ring of pefloxacin(1).The structures were characterized by elemental analysis and spectral data,and the in vitro anti-tumor activity of the title compounds against SMMC-7721,L1210 and HL60 cell lines was evaluated.The preliminary pharmacological results demonstrated that the title compounds possessed more significantly anti-proliferative activity than either the parent 1 or the corresponding amine intermediates(6).In particular,the title compound bearing a fluorine atom (7j) and compound bearing a nitro group attached to benzene ring (71) were comparable to the control doxorubicin against SMMC-7721 cells with an IC50 value of micro-molar concentration,respectively.It suggests that s-triazole ring modified with functional side-chain moieties instead of the C-3 carboxylic group is favorable to the improvement of antitumor activity.

Objective To study the effects of Liang-Xue-Yu-Chang decoction on intestinal epithelium of rats with radiation enteritis.Methods Sixty male SD rats were divided into three groups randomly:normal rats as control,abdominal radiation control group given distilled water after 10 Gy radiation,and abdominal radiation plus drug group given Liang-Xue-Yu-Chang decoction after 10 Gy radiation.Drugs or distilled water were chronically administered to animals for 7 days.After that,5-bromodexyridine (BrdU) was injected into abdominal cavity,SP immunohistochemistry was used to evaluate intestinal epithelium proliferating cell nuclear antigen (PCNA) and the positive cells labeled with Ki67 and BrdU.Results The number of intestinal epithelium cells with PCNA expression,positive Ki67 and BrdU were 22.0 + 2.7,71.2 + 5.7,and 26.2 + 5.9 respectively in the drug treatment group,significantly higher than those in the abdominal radiation control group (11.2 + 1.9,61.6 ± 5.5,and 11.3 ± 2.2) (t =14.629,5.420,11.582,P ＜ 0.05),but lower than those in the normal control group (30.4±5.7,86.6 ±5.1,and 32.3 ±3.2)(t =14.291,9.004,4.731,P＜0.05).Conclusion Liang-Xue-Yu-Chang decoction could improve the proliferation of intestinal epithelium in the rats with radiation enteritis.

DNA, Circular ; isolation & purification ; DNA, Viral ; isolation & purification ; Hepatitis B ; diagnosis ; Hepatitis B virus ; genetics ; Humans

Objective To study the possible mechanisms by which repetitive transcranial magnetic stimulation (rTMS) pretreatment antagonizes seizures induced by lithium chloride-pilocarpine and any correlation with antiapoptosis in hippocampal CA1 neurons.Methods Thirty rats were randomly divided into a control group, a sham stimulation group and an rTMS pretreatment group. The rTMS pretreatment group was pretreated on 7 consecutive days with low-frequency rTMS (0.5 Hz, 75％ of threshold intensity, 20 times/bundle, and 5 bundles/d), while the sham-stimulation group was sham-stimulated with a similar sound. Lithium chloride-pilocarpine ( LPC ) was used to induce a model epileptic state.Epileptic stroke latency and severity were recorded ; neuronal morphology was observed using hematoxylin and eosin (HE) staining; mean positive-reactive cell number and mean optical density and absorbance of B cell lymphoma/leukemia gene-2 (Bcl-2) were recorded, and Fas and Caspase-3 protein in the hippocampal CA1 region were observed with immunohistochemistry.Results Compared with the sham stimulation group, epileptic latency in the rTMS pretreatment group was significantly longer. Seizures in the rTMS pretreatment group were less severe, and a number of degenerated neurons were observed to be apoptotic. Bcl-2 protein expression increased at each time point, but Fas and Caspase-3 protein expression decreased.Conclusions rTMS pretreatment has an anti-epilepsy effect. The possible neuronal protection might be produced by regulating the expression of Bcl-2, Fas and Caspase-3 protein in the hippocampus.

Objective:To study the antisense oligonucleotide mediated inhibition on telomerase activity and cell proliferation of GBC-SD cell.Methods:We design the antisense,sense,and random oligonucleotide with phosphoric acid modification for the hTR(Human Telomerase RNA)template sequence.MTT and PCR methods were used to observe the inhibition on telomerase activity and cell proliferation of GBC-SD cell ,and fibroblast cells were used as control group.Results:PS-ODN can lead to the reduction of cell survival rate of GBC-SD cell,wich dosage dependence.Tne experimental group cell detected by scanning electron appeared apoptotic feature.Conclusion:PS-ODN can inhibit telomerase activity of GBC-SD cell effectively and induce the cell apoptosis.

Objective To investigate histopathological changes and expression of integrin ?1 of sternomastoid muscle,and probe the mechanism and significance during disease process in congenital muscular torticollis(CMT).Methods Histopathological changes of sternomastoid muscle section stained with HE and Gomori silver staining were observed and the expression of integrein ?1 with immunohistochemistry was detected,and the expressive quantity and distribution with image analysis system was quantitive analyzed.Results 1.With light microscopy observation,the results showed that the fibrous degeneration of sternomastoid muscle could be summed up 2 kinds: A category displayed the myocytes atrophyed,and there were lots of connective tissue hyperplasy around myocytes,and the direction of fibrous arrangement was disordered,meanwhile there were lots of vessels and nervers hyperplasy,and eventually the myocytes shrank back and disappeared.B category displayed that the structure of cross striation or sarcomere disappeared or changed,and myocytes could maintained the outline and the sarcolemma were integrated,and then fibrous pathological changes of myocyte took place,and there were lots of fibroblast-like that had much more enations between fiber bundles.With Gomori silver staining,the major changes of fibrotic sternomastoid muscle showed that there were lots of collagenous fibers hyperplasy.The arrangements of collagenous fibers were disordered in A category and were well-arranged in B ca-tegory.2.With immunohistochemistry,the results showed the expression of integrin ?1 was weak positive in normal control group(125.7?5.167).In diseased groups,the results showed 3 different extents:the expression of integrin ?1 displayed stronger positive in A category myocytes(30.15?6.543),and the level of expression was significantly different from normal controls(P0.05).Conclusions The fibrous pathological changes of sternomastoid muscle are a complicated and gradually process,which may has different mode,and ingetrin ?1 may participated the process of pathological changes.

Objective To study the changes in the percentage of CD+4 CD+25 regulatory T (Tr) cells in peripheral blood and deciduas in unexplained recurrent spontaneous abortion (URSA) patients, normal non-pregnant and pregnant women respectively. Methods The percentage of CD+4 CD+25 Tr cells in deciduas and peripheral blood from 25 URSA patients, 22 normal non-pregnant (NNP) women, and 34 normal early pregnant (NP) women were measured by double-staining followed by flow cytometric analysis. Results (1) The percentage of CD+4 CDbright25 T cells in peripheral blood in both URSA and NP [ ( 1.55±0.77 ) %, (2. 65±1.10)%, respectively] women were increased significantly than that in NNP women [ (0. 39± 0.14)% P<0.05]. The percentage of CD+4 CDbright25 T cells in peripheral blood in URSA women was significantly lower than that in NP women (P<0.05 ). (2) The percentage of CD+4 CDbright25 T cells in decidua in URSA women was significantly lower than that in NP women [ ( 0. 59±0. 23 ) %, ( 1.24 ± 0. 55)%, respectively, P <0. 01 ]. There was no significant difference in the percentage of CD+4 CDdim25 T cells in decidua between URSA women and NP women [ (4. 23±1.52)%, (3.75±1.88)%, respectively, P>0.05]. (3) The proportion of CD+4 CDbright25/CD+4 cells in deeiduas was significantly higher than that in peripheral blood in NP women [(13. 10±10. 25 ) %, ( 5.59±2.62 ) %, respectively, P < 0. 05 ] . However, a significant difference in the proportion of CD+4 CDbright25/CD+4 between decidua and peripheral blood was not found in URSA patients [ (5. 16±2. 83 ) %, ( 4. 64±2. 07 ) %, respectively, P>0.05)].Conclusions The number of CD+4 CD+25 Tr cells is increased in normal pregnancy and decreased in URSA. Therefore, CD+4 CD+25 Tr cells may play an important role in maintaining maternal-fetal tolerance and may be involved in the pathogenesis of URSA.

Cognitive impairment is a common complication of diabetes. Hippocampus plays an important role in cognitive function. In hyperglycemia, synaptophysin, a crucial synaptic vesicle membrane protein in hippocampus neuron is found to be down-regulated. Recent evidences have shown that angiotensin IV can facilitate memory acquisition and recovery. However, whether it can also improve cognitive functions of diabetic rats with cognitive disorder, and the possible mechanisms are uncertain. Hence, the objectives of this study. Forty fi ve Sprague Dawley male rats were randomly divided into three groups: Control, diabetic group and diabetes with angiotensin IV treatment group. The cognitive functions, mainly learning and memory of the rats were evaluated using Morris water maze task. The synapses ultrastructure, relative mRNA concentrations and protein expression levels of synaptophysin in hippocampus CA1 area were estimated using transmission electron microscope, RT-PCR, immunohistochemistry and western blotting, respectively. Our study showed that in the diabetic rats with angiotensin IV treatment, the cognitive impairment as measured by Morris water maze task improved, the ultrastructure of synapses in hippocampus reversed, the relative mRNA concentrations and protein levels of synaptophysin in hippocampus signifi cantly increased, when compared with diabetic rats. We conclude that angiotensin IV plays an important role in improving cognitive function of diabetic rats. The possible mechanisms are up-regulating the expression of synaptophysin and normalizing the ultrastructure of synapses in hippocampus.

Objective To analyze the ophthalmologic characteristics and examinations which caused by vertebral-basilar insuffi- ciency.Design Retrospective case series.Participants 469 eases of vertebral-basilar insufficiency.Methods Retrospective analysis of 469 cases of vertebral-basilar insufficiency patients with ophthalmologic signs' features,incidence,the main cause,color Doppler flow imaging and(or)digital subtraction angiography clearly stenosis location,the degree of stenosis from July 1st 2005 to July ist 2007 in PLA General Hospital.Main Outcome Measures Ophthalmologic signs' related reasons and supplementary examination.Results 96 cases were with the corresponding eye symptoms(20.4%).Vision decreased in 83 cases,diplopia was in 56 cases,ipsilateral hemiopia quadrant blind in 12 cases and depending on deformation in 10 cases,fundus arteriosclerosis in 72 cases,nystagmus in 39 cases,the eye movement disorder in 16 cases.Among 96 patients with associated ocular symptoms,75 patients with color Doppler flow imaging (CDFI)showed unilateral vertebral artery abnormal in 66 cases(88%),among those blood flow velocity decreased in 26 cases,17 cases with vascular plaque stenosis,thinning in 20 cases,3 cases with complete occlusion;different bilateral vertebral artery abnormal in 9 cases(12%),among those velocity dropped in 4 cases,two cases with vascular plaque stenosis and thinning in 3 cases.Forty-five cases with the digital subtraction angiography(DSA),left vertebral artery was abnormal in 24 cases,18 cases with stenosis,occlusion in 5 cas- es,abnormal bending in 1 case.Right vertebral artery was abnormal in 16 cases,13 cases with stenosis,occlusion in 3 cases.Bilateral vertebral artery stenosis was found in 2 cases;vertebral artery stenosis was in 3 patients.Conclusion Vertebral-basilar insufficiency may cause eye-related symptoms,therefore,vision acuity decrease,fundus 'arteriosclerosis,diplopia and nystagmus symptoms are more likely for patients with vertebral-patients with basilar artery insufficiency performance of the eye.(Ophthalmol CHN,2002,16:406-410)