Based on ninety three acetylcholinesterase inhibitors (AChEIs) which have the same mechanism of action but are different in structural characteristics, the pharmacophore model for acetylcholinesterase inhibitor was constructed by the CATALYST system. The optimal pharmacophore model with three hydrophobic units, a ring aromatic unit and a hydrogen-bond acceptor unit were confirmed (Weight=3.29, RMS=0.53, total cost-null cost=62.75, Correl=0.93, Config=19.05). This pharmacophore model will act on the double active site of acetylcholinesterase and is able to predict the activity of known acetylcholinesterase inhibitors that are used for clinical treatment of Alzheimer's disease (AD), and can be further used to identify structurally diverse compounds that have higher activity treating with Alzheimer's disease (AD) by virtual screening.

OBJECTIVEDesign and make triple cannula dual-lumen vacuum extractor to improve effect of decompression in operation of intestinal obstruction.

METHODSTriple cannula dual-lumen vacuum extractor was applied in 32 patients who underwent operation of intestinal obstruction from 2012 to 2015 in our hospital. The effect of intestinal decompression and patient prognosis were observed.

RESULTS32 patients that used triple cannula dual-lumen vacuum extractor had good recovery except for one patient abdominal incision with fatty liquefaction. The other patients had one-stage healed without any complication such as intestinal fistula, abdominal infection etc.

CONCLUSIONApplication of triple cannula dual-lumen vacuum extractor in operation for intestinal decompression could avoid contamination of abdomen and injury of intestinal mucosa, which had satisfied effect of intestinal decompression and promoted the effect of operation for intestinal obstruction.

Catheters ; Decompression, Surgical ; Digestive System Surgical Procedures ; instrumentation ; Humans ; Intestinal Obstruction ; surgery ; Vacuum

ObjectiveTo investigate the feasibility of using the ratio of (Cho + Cr)/Cit derived by MRS to predict the differentiation grades of prostatic cancer and Gleason grading.Methods Five postoperative prostate specimens were spitted and layered according to the region of interest of MRS inspections.The correlation between the CC/C values of each region of interest in each layer and the Gleason scores of the corresponding pathological sections was analyzed.The optimum diagnostic cutoff value was determined by conducting the hypothesis test of the area below the ROC curve of the well and moderately differentiated groups and poorly differentiated ones on the basis of CC/C values with a Spearman test.Results A total of 90 regions with valid pathologic diagnosis were obtained,70 cancer-affected and 20 cancer-free.In MRS,a CC/C value above 0.86 was used as a criterion for defining a cancer-affected region As a result,65 cancer-affected regions and 25 cancer-free regions were identified,among which pathologic diagnosis confirmed 59 and 14,respectively.Spearman′s rank correlation analysis revealed that the CC/C values of the prostatic carcinoma had significant positive correlation with Gleason scores ( r =0.746,P =0.000).For the well and moderately differentiated groups,the hypothesis test about the cutoff value,which was obtained by calculating the area below the ROC curve,was of no statistical significance.For the poorly differentiated groups,the optimum cutoff value was defined as 0.948,and the sensitivity and specificity were 81.4％ and 75.0％,respectively.It was also observed that the Gleason scores of the poorly differentiated endemic regions had positive correlation with the CC/C values ( r =0.605,P =0.000 ),suggesting that CC/C value was associated with the differentiation grade of the poorly differentiated prostatic cancer.When CC/C value was above 0.948,the poorly differentiated prostatic cancer was typically detected and Gleason score was often above 7.Conclusions CC/C values has positive correlation with Gleason scores.MRS may be used to predict the differentiation of prostate cancer.

OBJECTIVETo explore the regulatory effect of Suifukang (SFK), a compound Chinese patent drug on the change of free radical in tissue of spinal cord and blood caused by experimental spinal injury.

METHODSSeventy male adult SD rats were randomly divided into 4 groups, the SFK group (n = 20), the hormone group (n = 20), the control group (n = 20) and the normal group (n = 10). Rats in the former three groups were made into the right hemitransected spinal cord (T12) injury. SFK were given to the rats in the SFK group 3 days before and 2 hrs after modeling via gastrogavage, saline was given to rats in the control group at the same time. As for the rats in the hormone group, methyl-prednisolone 30 mg/kg was given once immediately by peritoneal injection. The rats were sacrificed in two batches (10 of each group in each batch) at 8 hrs and 24 hrs after modeling to obtain the serum and injured spinal cord tissue for determining superoxide dismutase (SOD) activity and malondialdehyde (MDA) content.

RESULTS(1) As compared with the normal group, SOD activity in serum and spinal tissue of the control group was lower significantly both at 8 hrs and 24 hrs after modeling, but the changes of SOD activity in the SFK and the hormone group were insignificant; (2) Content of MDA in serum and spinal tissue of rats elevated after modeling, which in the control group at 8 hrs after modeling were higher than that in the normal group, also higher than that in the SFK group and the hormone group; but at 24 hrs after modeling, it lowered significantly in both treated groups. The changes of MDA content in serum were similar to those in the spinal tissue.

CONCLUSIONSFK could effectively eliminate the excessive free radical in serum and injured spinal tissue, and raise the capability of antioxidation of organism.

Animals ; Drugs, Chinese Herbal ; pharmacology ; therapeutic use ; Free Radical Scavengers ; pharmacology ; therapeutic use ; Male ; Malondialdehyde ; metabolism ; Neuroprotective Agents ; pharmacology ; therapeutic use ; Random Allocation ; Rats ; Rats, Sprague-Dawley ; Spinal Cord Injuries ; drug therapy ; metabolism ; Superoxide Dismutase ; metabolism

Exercise fatigue is a physiological phenomenon not only for athletes, but also for astronauts. It is vital for athletes with hard training and astronauts with the heavy exercises for the mission in manned space flight to know how to solve the exercise fatigue. This article reviewed current commonly used TCM protective measures against fatigue.

Objective To investigate the effect of low frequency electric deep brain stimulation on amygdale kindling in rats.Methods The amygdale kinkling model of rats was established by operation on the brain.The effects of low frequency deep brain electric stimulation used alone or in combination with anti-epilepsy drugs were ob- served in terms of severity of seizure attack reflected by Racine's scale and afterdischarge duration recorded in electro- encephalogram.Results Fifteen minutes of low frequency electric stimulation at 1 Hz and 100 to 350?A effective- ly inhibited amygdale kindling as demonstrated by a significant decrease of afterdischarge duration,and decreased the severity of seizure attack (P

The potential of Rhizobium sp. N613 to produce the exopolysaccharide (REPS) was studied in this paper. Using an orthogonal design in a flask-shaker culture system, the fermentation medium and conditions of synthesizing REPS were optimized. Based on these results, the fermentation kinetic parameters were obtained in the batch fermentation with a 10L fermentor. The REPS yield of 11.31g/L was achieved by metabolic regulation during 40 h fed-batch fermentation. Transplanted tumor models of sarcoma 180 in mice were used to evaluate the anti-tumor effect. The result of anti-tumor activities showed that inhibition rate was 53.40%, when dose of REPS was 5mg/kg. These results indicate that REPS has the following properties: the short duration of fermentation, the high yield, the low cost, the effective immunocompetence and thickening. Thus, REPS has the value of development and application.

Objective To construct the prostate-specific double gene expression vector pIRESPSMAe/p-TK-Cx43 and establish the foundation for experimental prostate cancer gene therapy research. Methods Cx43 gene was amplified and cloned into pMD19-T Simple vector. HSV-TK gene was then synthesized and cloned into multiple clone site (MCS) A of the eukaryotie vector plRES. The new plasmid was named plRES-TK: PSMAe/p was obtained and cloned into plRES-TK by replacing CMV promoter. The new plasmid was named plRES-PSMAe/p-TK; Fourth, Cx43 gene was cloned into the MCS B of pIRES-PSMAe/p-TK and the new plasmid was named pIRES-PSMAe/p-TK-Cx43.This plasmid was identified by double digestion with Sal Ⅰ/Not Ⅰ and sequenced; Finally, LNCaP cells were transfected by the plasmid plRES-PSMAe/p-TK-Cx43 and the mRNAs expression of HSV-TK gene and Cx43 gene was tested by RT-PCR. Results The plasmids synthesized in this experiment were double digested respectively and the specific bands of the inserted genes were confirmed by RTPCR. plRES-PSMAe/p-TK-Cx43 was in line with the expected design by DNA sequencing. The mRNAs of TK gene and Cx43 gene were expressed and successfully confirmed by RT-PCR after LNCaP cells transfected with pIRES-PSMAe/p-TK-Cx43. Conclusion Double gene expression vector pIRES-PSMAe/p-TK-Cx43 containing HSV-TK gene and Cx43 gene is constructed successfully.

Continuously cropping obstacle restricts ginseng production and rational use of land resource severely, and autotoxicity is one of the most important factors. In our previous work, ginseng autotoxin degrading bacteria were isolated, in the present re- search, plate culturing method and traditional physiological and biochemical method were used to analyze biological indices and protective enzyme activities, in order to elucidate the mitigative effect of autotoxin degrading bacteria on autotoxicity of P. ginseng. Results indicated that, except for palmitic acid, autotoxicity of benzonic acid, diisobutyl phthalate, diisobutyl succinate, and 2,2-bis (4- hydroxyphenyl) propane on the growth of ginseng seeds was significantly alleviated after autotoxins degrading bacteria was inoculated, and which have no evident difference with control. Except for benzoic acid, enzyme activity of SOD, POD and CAT in other autotoxin degrading treatments decreased significantly. The present research showed that, microbial degradation could alleviate the autotoxicity of autotoxins on ginseng seeds effectively, and which will be helpful for the resolution of ginseng continuously cropping obstacle problem.
Bacteria ; metabolism ; Panax ; enzymology ; growth & development ; metabolism ; microbiology ; Toxins, Biological ; metabolism

Objective To study the effect and mechanisms of berberine (BBR) on the proliferation of papillary thyroid cancer K1 cells induced by high glucose.Methods K1 cells were cultured under 5.5 mmol/L or 25 mmol/L glucose condition with or without different concentration of BBR (0,10,40 and 80 μmol/L) for 24 hours.The proliferations of K1 cells in each condition were detected by MTT.Western blot was used to measure the expression of nuclear factor erythroid 2-related factor 2 (Nrt2),phosphoinositide 3-kinase (PI3K),protein kinase B (Akt) and phosphorylated-Akt (p-Akt).The distribution pattern of Nrf2 in K1 cells was determined using immunofluorescent staining.Results Compared with 5.5 mmol/L condition,the proliferation rate [(126.64 ± 5.41) ％ vs (87.31 ± 3.67) ％],expression levels of PI3K (0.425 ±0.019 vs 0.272 ±0.039),p-Akt/Akt (0.446 ±0.021 vs 0.168 ±0.035) and Nrf2 (0.597 ± 0.014 vs 0.308 ± 0.026),and Nrf2 distribution (93.0％ vs 23.1％) in nuclear of K 1 cells under 25 mmol/L condition were significantly elevated,respectively (all P ＜0.01).Addition of BBR in 25 mmol/L condition dose dependently (10,40,80 μmol/L) lowered the proliferation rate of K1 cells [(111.76 ± 4.10)％,(70.03 ±2.18)％,(32.41 ±3.76)％ vs (126.64 ±5.41)％,all P＜0.05],and suppressed the expression of PI3K,p-Akt/Akt,Nrf2,and Nrf2 nuclear distribution (P ＜ 0.05).Conclusions BBR dose dependently inhibited the proliferation of high glucose-induced K1 cells.This effect was associated with the suppression on of PI3K/Akt signaling activation,Nrf2 expression and its nuclear translocation.