AIM: To study the effects of insulin and glucose on tissue-type plamingen activator (tPA) and its inhibitor-1 (PAI-1) secretion in cultured human endothelial cells. METHODS: Human endothelial cell line ECV-304 was cultured with glucose and/or insulin at different concentrations with or without hypoxic exposure. RESULTS: The tPA, PAI-1 secretion and ratio of tPA/PAI-1 increased in endothelial cells during hypoxia. Insulin and glucose increased the tPA and PAI-1 secretion in endothelial cells exposed to hypoxia, and increase in tPA/PAI-1 ratio was also observed at 4 h and 8 h. CONCLUSION: Hypoxia stimulates the release of tPA and PAI-1. Insulin and glucose also stimulate the tPA and PAI-1 secretion during hypoxia.

Objective To investigate the effect of low-dose hydrocortisone(HC)on hippocampus nuclear factor kappa B((NF-?B)),I?B expression in lipopolysaccharide(LPS)induced septic rats and the role of NF-?B signal transcription pathway in pathogenesis.Methods Fifty-four rats were randomly divided into 3 groups: control group(A group,n=6),model group(B group,n=24),low-dose HC treatment group(C group,n=24).The septic rat model was established by intraperitoneal injection LPS(1 mg/kg),as the intervention by caudal vein injection low-dose HC(6 mg/kg),each of B and C group was subdivied into 2,8,16,24 hours respectively after LPS injection(n=6).At serial time points,the animals in each group were sacrificed,brain tissue samples were harvested to determine NF-?B,I?B expression by immunhistochemistry in hippocampus.Results In B group: NF-?B expression was up regulated compared with A group(P

Objective To compare three kinds of irradiation treatment plans for cervical and upper thoracic esophageal cancer,in order to arrived at proper decision for the patient.Methods From February 2001 to June 2004,43 such patients were studied with three different simulated treatment plans made including conformal plan,conventional four-field plan and conventional two-field plan for every one.All plans were evaluated with iso- dose curve and dose-volume histogram.Results GTV on 95% isodose curve was 99.5%,98.2% and 87.4% in conforaml plan,conventional four-field plan and conventional two-field plan,respectively;PTV_1 and PTV_2 on 95% isodose with 97.8%,97.2%,94.8% and 95.8%,86.6%,73.7%.The volume of＞20 Gy dose of left lung accepted was 18.6%,17.2% and 32.3%,in conformal plan,conventional four-field plan and conventional two-field plan,respectively;the right lung received 20.5%,19.9% and 35.5%.Conclusions Conformal plan is the best in radiotherapy,as it can provide ideal dose distribution of irradiated target with adequate protection of the normal tissues.Conventional four-field plan,being easy to carry out,can replace the conformal plan in most situations.Conventional two-field has the most uneven dose distribution and largest lung volume irradiated.

Six bacterial strains were isolated from lead-zinc mine tailings with the age of about 100 years, and their phylogenetic position was determined by the analysis of partial 16S rRNA gene sequence. Three strains belonged to genus Arthrobacter, and were close to A. nicotinovorans and A. histidinolovorans. Other three strains belonged to genus Agromyces, and were close to Ag. mediolanus. All of them were resistant to Pb(NO_(3))_(2), CdCl_(2), ZnSO_(4), CuSO_(4) and CoCl_2. Relatively, minimal inhibitory concentration(MIC)of Zn~(2+) and Co~(2+) of three Arthrobacter strains was significantly higher than that of three Agromyces strains. Additionally, these strains displayed strong adsorption of Pb(NO_(3))_(2), CdCl_(2), ZnSO_(4). Averagely three Arthrobacter strains could adsorb about 400mg of Pb~(2+), 177mg of Cd~(2+) or 80mg of Zn~(2+) per gram of dried cells. Therefore, these strains were important candidates for application in bioremediation of heavy metal-contaminated environment.

OBJECTIVETo explore the efficacy and safety of Jieyu Anshen Decoction (JAD) combined with aripiprazole in treating chronic schizophrenia.

METHODSAll 100 patients with chronic schizophrenia diagnosed according to CCMD-3 criteria were equally randomly assigned to the study group (treated with JAD combined with aripiprazole) and the control group (treated with aripiprazole alone) for 12 weeks. The efficacy and safety were evaluated by Positive and Negative Syndrome Scale (PANSS) and Treatment Emergent Side Effect Scale (TESS).

RESULTSAfter 12 weeks of treatment, the clinical efficacy in the study group was significantly higher than that in the control group, the PANSS score in the study group was significantly decreased with a higher speed and range of decreasing, becoming lower than that in the control group at the same period. But the difference between the two groups in scores of TESS at corresponding times showed no significance.

CONCLUSIONJAD combined with aripiprazole has definite effect in treating chronic schizophrenia, shows advantages of quickly initiating effect, high safety and with no harm for increasing adverse reactions, so it is better than using aripiprazole alone.

Adult ; Antipsychotic Agents ; therapeutic use ; Aripiprazole ; Drug Therapy, Combination ; Drugs, Chinese Herbal ; therapeutic use ; Female ; Humans ; Male ; Middle Aged ; Phytotherapy ; Piperazines ; therapeutic use ; Quinolones ; therapeutic use ; Schizophrenia ; drug therapy ; Treatment Outcome

AIMTo study the effects of sodium magnesium fructose diphosphate (SMFD) on free calcium concentration and nitric oxide synthase activity of ischemic synaptosome, so as to explore the protective mechanisms of SMFD on cerebral ischemia.

METHODSThe synaptosomes from normal rat brain were prepared by phase partition and cultured with oxygen-glucose deprivation to establish ischemic synaptosome model. The intrasynaptosomal free calcium concentration and nitric oxide synthase activity were detected separately after the synaptosomes were co-incubated with SMFD (1.3 mmol.L-1) or fructose-1, 6-diphosphate (FDP, 4.0 mmol.L-1) for 60 min.

RESULTSSMFD decreased the free calcium concentration and reduced the activity of nitric oxide synthase (NOS) of ischemic synaptosomes. Its effects were more powerful than those of FDP.

CONCLUSIONSMFD may protect neurons from ischemic injury by preventing intracellular Ca2+ overload and inhibiting the activity of nitric oxide synthase.

Animals ; Brain Ischemia ; enzymology ; metabolism ; Calcium ; metabolism ; Chelating Agents ; pharmacology ; Fructosediphosphates ; pharmacology ; Magnesium ; chemistry ; Male ; Nitric Oxide Synthase ; drug effects ; metabolism ; Rats ; Rats, Wistar ; Sodium ; chemistry ; Synaptosomes ; metabolism

Objective　To explore the risk factors and causes affecting the operative mortality in esophagectomy patients with esophageal can cer. Methods　1400 cases with a curative esophagectomy for neopl asm of esophagus hospitalized from Mar,1973 to June, 2000 were reviewed. There w ere 31 died within 30 d or during hospitalization after esophagectomy as a group , and 1 369 survival cases, after operation, as another group. Sixteen factors t hat may influence the operational mortality were selected. A multi-variate anal ysis of these individual variables was performed by the computer′s logistic reg ression model. Results　The operative mortality was 2.2%(31/1400 ). The causes of death included respiratory complication 17 cases (including res piratory failure caused by pneumonia or atelectasis), 15 cases, and adult respir atory distress syndrome (ARDS) 2 cases, the mortality was 54.8% in the death gro up), anastomotic leak 11 cases (34.5%), Chylothorax 2 cases (6.5%) and postopera tive digestive tract hemorrhage 1 case (3.2%). The results showed that the major risk factors that affected operative mortality in cases with esophageal cancer were history of long-herm heavy smoking, duration of operation and the year of operational (P<0.05). Conclusion　To minimize operative mort ality of esophagectomy, some means must be noticed, including the reinforcemen t of the perioperative care, the improvement of anastomotic methods and surgical skill, reduing operative time as p ossible, disposing pulmonary complications in time and using respirator if neces sary.

Objective To establish the normal parameters of psychometric measures such as the number connection tests A(NCT-A)and digit symbol tests(DST)in assessment of minimal hepatic en- cephalopathy(MHE).Methods One hundred and sixty healthy volunteers(aged 25 to 64 years;educa- tional level＞9 years)were divided into＜35 ys,35～44 ys,45～54 ys and 55～64 ys groups.All of the healthy volunteers were assessed with NCT-A and DST to establish the normal value of age-related parameters,which can be used for diagnosis of MHE in patients with liver cirrhosis.Two standard devi- ation of the normal mean was used as a diagnostic criterion for MHE.One hundred and six cirrhotic patients were assessed with these parameters.Results The parameters of NCT-A were(25.1?4.6) sec in＜35 ys group,(32.1?6.8) sec in 35～44 ys group,(38.6?7.1)sec in 45～54 ys group or (49.3?6.3)sec in 55～64 ys group.The scores of DST were 49.9?4.7 in＜35 ys group,44.6?4.8 in 35～44 ys group,38.5?5.0 in 45～54 ys group or 35.4?4.7 in 55～64 ys group.Thirty one out of 106 cirrhotic patients were diagnosed as MHE based on these parameters.Conclusion The NCT- A and DST are psychometric assessments for diagnosis of MHE.Age-based normal paramerters of NCT- A and DST are needed to be established.

OBJECTIVETo observe response characteristics of human brain to acupuncture of corresponding channel point selection and probe into the central nervous mechanism of acupuncture at the points selected along channel.

METHODSSix cases of chronic migraine were treated with acupuncture at Fengchi (GB 20), Waiguan (TE 5), Yang-lingquan (GB 34) on the Shaoyang Channel. Positron emission computerized tomography (PET-CT) was used for scanning and statistic parameter map (SPM 2) software was used to analyze the data and compare with healthy human brain function imaging and investigate the changes of metabolism of glucose in the brain of the patient of migraine before and after acupuncture.

RESULTSAfter acupuncture, excitation areas of the pain brain regions such as the brain stem, insula, etc. obviously reduced, and the brain function-reducing area turned from the right temporal lobe as main to bilateral temporal lobes with symmetry.

CONCLUSIONThe pons, insula, anterior frontal gyrus, etc. possibly are the target points of analgesic effect of acupuncture at the Shaoyang Channel on chronic migraine, and the change of metabolism reduction on bilateral temporal lobes induced by acupuncture possibly is one of the mechanisms for acu-puncture at points on the Shaoyang Channel for treatment of migraine. Acupuncture achieves whole and beneficial therapeutic effect possibly through coordination and redistribution of energy metabolism in the brain.

Acupuncture Points ; Acupuncture Therapy ; Adult ; Brain ; metabolism ; Cerebrum ; diagnostic imaging ; metabolism ; Chronic Disease ; therapy ; Female ; Glucose ; metabolism ; Humans ; Male ; Migraine Disorders ; diagnostic imaging ; therapy ; Positron-Emission Tomography ; Treatment Outcome

A growing body of evidence suggests that p300 histone acetyltransferase plays important roles in cancer cell differentiation and proliferation. Here, we employed structure-based hierarchical virtual screening method to identify novel lead compounds of p300 histone acetyltransferase. From a screening library containing approximate 100 000 diverse druglike compounds, 33 compounds were chosen for experimental testing and one compound, 4-acetyl-2-methyl-N-morpholino-3,4-dihydro-2H-benzo[b][1, 4]thiazine-7-sulfonamide (17), showed as micromolar inhibitor. Based on its predicted binding pose, we investigated its binding characteristics by designing two series of structural modifications. The obtained structure-activity relationship results are consistent with the predicted binding model. We expect that the identified novel p300 histone acetyltransferase inhibitors will serve as starting points for further development of more potent and specific histone acetyltransferase inhibitors.
Drug Design ; Enzyme Inhibitors ; chemical synthesis ; chemistry ; Molecular Structure ; Morpholines ; chemical synthesis ; chemistry ; Structure-Activity Relationship ; Sulfonamides ; chemical synthesis ; chemistry ; p300-CBP Transcription Factors ; antagonists & inhibitors ; chemistry