OBJECTIVE To analyze impulsive-like behaviors of SD rats induced by pramipexole in Y-maze avoidance tasks. METHODS Behaviors of SD rats in Y-maze avoidance tasks were recorded with a camera and analyzed by Noldus Etho Vision XT8 software after acute subcutaneous injection of pramipexole(0.1,1 and 10 mg · kg-1),including right reaction numbers of 20 consecutive avoidance tasks,shuttle number of times between the three arms of Y-maze, distance covered in Y-maze and time spent in safe arms during 20 consecutive avoidance tasks. Then,the prepulse inhibition(PPI)of the startle reflex test was used to assess the effect of pramipexole on sensorimotor gating (SG). Effects of pramipexole on the dialyzed content of monoamine neurotransmitter and its metabolites in the striatum and amygdala of SD rats were measured by microdialysis in vivo. RESULTS Compared with normal control group,the rats of pramipexole group showed a significant increase in the shuttle number of times and distance covered in Y-maze between Y-maze avoidance tasks(P<0.01),but a statistically significant decrease in the time spent in safe arms(P<0.01),while the number of right reactions in Y-maze avoidance tasks was not changed. Such premature responses were quite similar to certain impulsive-compulsive behaviors in rodent models,such as five-choice serial reaction time tasks. In the PPI test,pramipexole displayed an impairing effect on SG(P<0.01). The microdialysis results showed that there was an increase of dopamine and 5-hydroxytryptamine in the striatum of pramipexole group, but not statistically significant. Monoamine neurotransmitters and their metabolites were not significantly changed in the amygdala. CONCLUSION Pramipexole can induce impulsive-compulsive behaviors in Y-maze avoidance tasks,which might be attributed to impaired SG.

Objective To optimize purification technology of total flavonoids in Callicarpa nudiflora Hook. et Arm. by macroporous adsorption resin. Methods Macroporous resin models including AB-8, D-101, HP-20, HP2MG, were optimized by static adsorption and desorption experiments regarding to adsorption rate and desorption rate of total flavonoids. Purification technology parameters of total flavonoids were optimized by single factor test. Results HP-20 macroporous resin presented the best purification efficiency,the optimum purification conditions were that taking 4. 46 mg·mL-1 of total flavonoidsat pH 3. 0, loading at 3 BV·h-1, washed with 3BV of water at 3 BV·h-1,then eluted with 4 BV 75% ethanol at 2 BV·h-1, finally obtaining the total flavonoids from the dry extract of Callicarpa nudiflora Hook. et Arn. with the purity of 47. 4%. Conclusion HP-20 macroporous resin is suitable for preliminary purification of total flavonoids in Callicarpa nudiflora Hook. et Arn.

Objective To compare the efficacy of endovascular interventional treatment and surgical clipping in posterior communicating artery aneurysm (PCoAA) patients with fetal-type posterior cerebral artery (fPCA).Methods The PCoAA patients with fPCA were enrolled.Their baseline clinical data were collected.The modified Rankin Scale (mRS) was used to assess the clinical outcomes at six months after procedure.The mRS score 0-2 was defined as good outcome.Results A total of 35 PCoAA patients with fPCA were enrolled into the study,23 were treated with interventional embolization therapy and 12 were treated with craniotomy clipping.There were no significant differences in age,gender,preoperative Fisher grade,Hunt-Hess grade,baseline GCS scores,and aneurysm typing between the 2 groups.The good outcome rate of the interventional embolization group at 6 months was higher than that of the surgical clipping group,but there was no significant difference (65.22％ vs.41.67％;P =0.282).Results The efficacy of PCoAA using interventional embolization therapy combined fPCA is almost the same as craniotomy clipping.

AIM To explore the curative effects,adverse events,effects on immunity function and cost-effectiveness of Aiyu Capsules (Cremastrae pseudobulbus,Solanum lyratum,Angelicae sinensis Radix,etc.) or Fufang Banmao Capsules (Mylabris,Ginseng Radix et Rhizoma,Astragali Radix,etc.) combined with icotinib hydrochloride in the treatment of advanced non-small cell lung carcinoma (NSCLC).METHODS One hundred and sixty patients with advanced NSCLC were randomly divided into three groups.The patients in icotinib hydrochloride group (n =80) took icotinib hydrochloride,125 mg each time,three times a day;the patients in Aiyu Capsules + icotinib hydrochloride group or Fufang Banmao Capsules + icotinib hydrochloride group were treated with Aiyu Capsules (40 cases,three pills each time,three times a day) or Fufang Banmao Capsules (40 cases,one pill each time,three times a day) combined with icotinib hydrochloride (125 mg each time,three times a day),respectively.Curative effects,adverse events,serum tumor markers,dendritic cell subsets and cost-effectiveness among the three groups were compared.RESULTS Eight weeks after the treatment,effective rates in the Aiyu Capsules + icotinib hydrochloride group (82.50％) and Fufang Banmao Capsules + icotinib hydrochloride group (97.5％) were significantly higher than that in the icotinib hydrochloride group (73.5％) (P ＜ 0.05).Six-month survival rates in the icotinib hydrochloride group,Aiyu Capsules + icotinib hydrochloride group and Fufang Banmao Capsules + icotinib hydrochloride group were 93.7％,97.5％ and 97.5％,respectively;one-year survival rates in the three groups were 53.7％,72.5％ and 75.0％,respectively;two-year survival rates in the three groups were 20.0％,37.5％ and 40.0％,respectively.One-year,two-year survival rates in the Aiyu Capsules + icotinib hydrochloride group and Fufang Banmao Capsules + icotinib hydrochloride group were significantly higher than those in the icotinib hydrochloride group (P ＜ 0.05).Myeloid dendritic cell (mDC) subsets' increases (d8week-d1) in the Aiyu Capsules + icotinib hydrochloride group and Fufang Banmao Capsules + icotinib hydrochloride group were significantly higher than that in the icotinib hydrochloride group (P ＜ 0.05).There was no statistical significance in plasmacytoid dendritic cell (pDC) subsets' change among the three groups (P ＞ 0.05).Changes of carcinoembryonic antigen (CEA),cytokeratin-19-fragment (CYFRA21-1),neuron-specific enolase (NSE) in the Aiyu Capsules + icotinib hydrochloride group and Fufang Banmao Capsules + icotinib hydrochloride group were higher than those in the icotinib hydrochloride group (P ＜ 0.05).Treatment costs in the Aiyu Capsules + icotinib hydrochloride group and Fufang Banmao Capsules + icotinib hydrochloride group were significantly lower than that in the icotinib hydrochloride group (P ＜ 0.05).No obvious statistical difference in adverse events was found among the three groups (P ＞ 0.05).CONCLUSION The curative effects and cost-effectiveness of Aiyu Capsules or Fufang Banmao Capsules combined with icotinib hydrochloride are better than those of icotinib hydrochloride alone in the treatment of advanced NSCLC.

A series of novel 4-substituted-3-nitrobenzamide derivatives were designed and synthesized. The structures of the target compounds were confirmed with 1H NMR, 13C NMR, MS and element analysis. Anti-tumor activities against HCT-116, MDA-MB435 and HL-60 cell lines in vitro were evaluated by SRB assay. The results indicated most of the target compounds exhibited potent anti-tumor activity. Compound 4a showed the most potent inhibitory activities against three cancer cell lines with the GI50 values of 1.904-2.111 micromol x L(-1). Compounds 4g, 41-4n exhibited more potent inhibitory activities against MDA-MB435 and HL-60 cell lines with the GI50 values of 1.008-3.586 micromol x L(-1) and 1.993-3.778 micromol x L(-1), respectively. The structure-activity relationship of these compounds is discussed preliminarily.
Antineoplastic Agents ; chemical synthesis ; pharmacology ; Benzamides ; chemical synthesis ; pharmacology ; Cell Line, Tumor ; Cell Proliferation ; Drug Design ; HL-60 Cells ; Humans ; Inhibitory Concentration 50 ; Structure-Activity Relationship

Objective To study Caveolin-1,EGFR expression in bladder transitional call carcinoma and their prognostic value. Methods Immunohistochemical method was used to detect Caveolin-1,EGFR in 89 cases.of bladder transitional call carcinoma.Results In 89 cases,the percentage of abnormal Caveolin-1 and EGFR expression were 37.1% and 50.6 % respectively.Significant change was observed in different grade case,P

OBJECTIVETo investigate a new method to construct tissue-engineering bone that will be applicable clinically.

METHODSThe cultured 5th generation rabbit bone marrow stroma osteoblasts (MSO) was dissolved in 3% sodium alginate solution (the final concentration of sodium alginate in the solution being 1%, and MSO, 5x10(6)/L), and then inoculated into prepared true bone ceramic (TBC) and gelatinized the bone by dribbling with calcium gluconate. The standard bone defect models were made in 48 adult New Zealand rabbit's both radius. Among the 48 rabbits, 24 were in Groups A and B, in which the left radius was implanted with gelatinized MSO-TBC (Group A) and right radius implanted with autograft-bone (Group B); and the other 24 were in control group whose left radius was implanted with non-gelatinized MSO-TBC (Group C) and right radius implanted with gelatinized TBC (Group D). Outcomes of the implanted bones were assessed by radiology, pathological histology, osteogenetic quantitative analysis, and biomechanics at 2, 4, 8, 12 weeks postoperatively.

RESULTSIn Groups A and B, a satisfactory bone reparation and bony union was noted within 12 weeks. In Groups C and D, bone reparation was not satisfied compared with Group A in terms of ostogenetic quantity and biomechanics.

CONCLUSIONSGelatinized MSO-TBC is an ideal artificial active bone that overcomes TBC shortcomings of fragileness and smooth surface that is not eligible for seed cell's adhesion. It is promising to put into clinical use extensively.

Animals ; Biomass ; Bone Diseases ; diagnostic imaging ; pathology ; therapy ; Bone Marrow Cells ; cytology ; Bone Substitutes ; Ceramics ; Disease Models, Animal ; Female ; Gelatin ; Male ; Osteoblasts ; cytology ; transplantation ; Osteogenesis ; Rabbits ; Radiography ; Radius ; diagnostic imaging ; injuries ; pathology ; surgery ; Stromal Cells ; cytology ; transplantation ; Tissue Engineering ; methods ; Treatment Outcome

OBJECTIVETo observe the binding power of polymyxin B (PMB) and its simulation peptide to lipopolysaccharide (LPS) and lipoid A.

METHODSLPS and lipoid A were separately coated on biosensor. 5 microl of PMB (0.01 microg/L) 5 microl of its simulating peptide 1 (PMBSP1 0.01 microg/L) and 5 microl of its simulating peptide 2 (PMBSP2, 0.01 microg/L) were respectively added into the hydrophobic sample pool. The combining power of PMB and its simulating peptides PMBSP1 and PMBSP2 to LPS and lipoid A was compared. RESULTS (1) PMBSP1 almost did not bind LPS and lipoid A, while PMB and PMBSP2 possessed high affinity with LPS and lipoid A. (2) The peak value (98.41 +/- 7.31) rad/s of PMBSP2 binding LPS was much higher than that (83.58 +/- 5.42) rad/s of PMB in binding LPS (P < 0.05). While the peak value of PMB in binding lipoid A was similar to that of PMBSP2. (3) The peak value of PMB binding LPS was significantly lower than that of PMB in binding lipoid A (P < 0.05). But there was no difference between the peak value of PMBSP2 in binding LPS and that of PMBSP2 in binding lipoid A. (4) PMBSP2 could bind to LPS and lipoid A in a shorter time to reach peak levels.

CONCLUSIONCompared with PMB, the PMBSP2 could bind to LPS and lipoid A in a shorter time. In addition, PMBSP2 exhibited similar affinity to LPS and lipoid A. This indicated that PMBSP might possess better anti-LPS activity due to its lack of space steric hindrance when PMBSP binding the lipoid A of LPS.

Cell Wall ; chemistry ; Endotoxins ; Gram-Negative Bacteria ; Lipopolysaccharides ; chemistry ; toxicity ; Peptides ; chemistry ; pharmacology ; Polymyxin B ; chemistry ; pharmacology

OBJECTIVETo investigate the effect of bacillus Calmette-Guerin (BCG) on Toll-like receptors (TLRs) expression and cytokine production in human bladder cancer cell line T24.

METHODSHuman transitional carcinoma cell line T24 was cultured in RPMI1640 medium with 10% FBS, BCG was added into the cell culture with various doses in bacteria-cell ratio. After T24 cells were stimulated by BCG for 1 hour, total RNA of cells was extracted. RT-PCR procedure was conducted with the primer of TLR-2 and TLR-4, and the products were analyzed with agarose gels electrophoresis. Then the expression of TLR-2 and TLR-4 in T24 cells was assessed by the analyzing system of gel imaging. After the stimulation culture for 12 hours, the supernatant of cells was collected. The levels of IL-4 and IL-12 in each sample were assayed by ELISA method.

RESULTSThe expression level of either TLR-2 or TLR-4 was increased by the stimulation of BCG in a dose-dependent manner, the effects reached the maximal level at the dose of BCG as 10 bacilli per cell. The production of IL-12 in T24 cells was also increased gradually by the stimulation of BCG in a dose-dependent manner, and the dose of BCG obtained maximal effect was 10 bacilli per cell, which is coincident with the results observed in the expression of TLRs. There was no difference showed on the production of IL-4 between T24 cells stimulated with BCG and control.

CONCLUSIONSThe stimulation of BCG not only up-regulated the expression of TLR-2 and TLR-4, but also increased the production of IL-12 in bladder cancer T24 cell line. The expression of TLRs and the production of cytokine in bladder cancer cells may be related to the BCG-induced immunol response to human bladder cancer.

BCG Vaccine ; pharmacology ; Cell Line, Tumor ; Dose-Response Relationship, Drug ; Electrophoresis, Agar Gel ; Enzyme-Linked Immunosorbent Assay ; Gene Expression Regulation, Neoplastic ; drug effects ; Humans ; Interleukin-2 ; analysis ; Interleukin-4 ; analysis ; Membrane Glycoproteins ; genetics ; Receptors, Cell Surface ; genetics ; Reverse Transcriptase Polymerase Chain Reaction ; Toll-Like Receptor 2 ; Toll-Like Receptor 4 ; Toll-Like Receptors ; Urinary Bladder Neoplasms ; genetics ; metabolism ; pathology

OBJECTIVETo explore the effect of Shugan Jianpi Recipe (SJR) on LXRα/FAS signaling pathway mediated hepatocyte fatty deposits in nonalcoholic fatty liver disease (NAFLD) rats.

METHODSTotally 75 SPF grade male SD rats were randomly divided into 5 groups, i.e., the normal control group, the model group, the Shugan Recipe (SR) treatment groups, the Jianpi Recipe (JR) treatment group, and the SJR group. Except rats in the normal control group, the NAFLD rat model was duplicated using high fat diet (HFD). SR (Chaihu Shugan Powder) was administered to rats in the SR group. JR (Shenlin Baizhu Powder) was administered to rats in the JR group. SJR (Chaihu Shugan Powder plus Shenlin Baizhu Powder) was administered to rats in the SJR group. Changes of liver fat were analyzed using automatic biochemical analyzer. Liver cells were separated by low-speed centrifugation. Their activities and purities were identify using Typan blue and flow cytometry (FCM). Expression levels of LXRα and FAS mRNA in hepatocytes detected by Real-time quantitative PCR. Expression levels of LXRα and FAS protein were detected by Western blot.

RESULTS(1) Pathological results showed in the model group, hepatocytes were swollen with nucleus locating at the cell edge after oil red O staining; unequal sized small vacuoles could be seen inside cytoplasm. Some small vacuoles merged big vacuoles. All these indi- cated a NAFLD rat model was successfully established by high fat diet. Pathological structural changes could be impaired to some degree in all medicated groups, especially in the SR group. (2) Compared with the normal control group, expression levels of LXRα and FAS genes and proteins obviously increased in the model group (P < 0.01). Compared with the model group, their expression levels were obviously down-regulated in the JR group and the SR group (P < 0.01, P < 0.05).

CONCLUSIONSLXRα/FAS signaling pathway was an important signaling pathway for mediating lipid metabolism disorders of NAFLD rats. SJR could make hepatocyte fatty deposits tend to repair by adjusting the LXRα/FAS signaling pathway in NAFLD rats, which might be one of important mechanisms for SJR to prevent and cure NAFLD.

Animals ; Diet, High-Fat ; Down-Regulation ; Drugs, Chinese Herbal ; pharmacology ; therapeutic use ; Hepatocytes ; Male ; Nitric Oxide Synthase Type II ; metabolism ; Non-alcoholic Fatty Liver Disease ; metabolism ; Orphan Nuclear Receptors ; metabolism ; RNA, Messenger ; Rats ; Rats, Sprague-Dawley ; Signal Transduction ; fas Receptor ; metabolism