This study is to investigate the mechanism and action characteristics of 6-chloro-3-methyl-4-(2-methyoxycarbonylthiophene-3-sulfonyl)-3, 4-dihydroquinoxa-lin-2-(1 H)-one (XU07011) against HIV-1 replication. XU07011 anti-HIV activity was tested by using VSVG/HIV pseudotype viral system and confirmed by HIV-1 live viruses' infectious assay. Time of addition was used to test HIV-1 reverse transcription process. RNA-dependent DNA polymerase activity and RNase H activity were tested by using enzyme linked immunoabsorbent assay and fluorescence method. Wild type and nine NNRTIs-resistant reverse transcriptase enzymatic models and cell-based pharmacological models were used to evaluate XU07011 bio-characteristics. The results showed that XU07011 inhibited HIV-1 replication with IC50 of (0.057 +/- 0.01) micromol x L(-1) which was comparable to nevirapine [IC50: (0.046 +/- 0.01) micromol x L(-1)]. Mechanism study data indicated that XU07011 blocked HIV-1 reverse transcription process through acting on reverse transcriptase RNA-dependent DNA polymerase with IC 50 of (1.1 +/- 0.3) micromol x L(-1). The compound showed no effect on RNase H activity. XU07011 exhibited better activities comparing with nevirapine on K103N mutated NNRTIs-resistant HIV-1 strains. This study could provide a theoretical basis for novel anti-HIV reagents development.

Objective To explore the characteristics of defense mechanism in patients with obsessive-compulsive disorder(OCD).Methods Outpatients diagnosed as OCD were tested by Yale-Brown obsessive Compulsive Scale. Among them, 40 patients with score beyond or equal to 16 were selected as research group. 33 healthy individuals were selected as normal group. They were tested with Defense Style Questionnaire.Results ①The factor score of immature defense mechanisms in the OCD group is much higher than that in the normal group (P<0.01); the factor score of mature defense mechanisms in the OCD group is lower than that in the normal group (P<0.05); the factor score of middle defense mechanisms in the OCD group is much higher than that in the normal group (P<0.01). ②Passive aggression, acting out, splitting, regression, somatization in the immature defense mechanisms and relief, false altruism, isolation in the middle defense mechanisms are much more used by the OCD group than that in the normal group; but suppression and humor in the mature defense mechanisms are less used by the OCD group than that of the normal group(P<0.05 or P<0.01). ③Sublimation, suppression and consuming tendency are much more used in male patients than female ones in OCD group(P<0.05).Conclusion The patients with OCD tend to use the immature defense mechanisms and middle defense mechanisms, and there is some difference between male and female patients in using defense mechanisms.

Objective To determine the impact of smoking on the clinical outcomes in male patients with chronic schizophrenia and explore management strategies for the smoking behavior of inpatients with chronic schizophrenia. Methods Ninety-nine male inpatients with chronic schizophrenia including 53 smokers and 46 non-smokers were enrolled in the study. The patients' psychotic conditions were evaluated by using Positive and Negative Symptoms Scale (PANSS) and Nurses Observation Scale for In-patient Evaluation (NOSIE). Results Compared with non-smokers, the total score and negative sub-score of PANSS as well as psychotic, tardive, total passive factor scores of NOSIE in smokers were significantly lower (P<0.05) .while the social function, social interest, total positive factor scores of NOSIE in smokers were significantly higher (P<0.05). However, the cigarette smoking dose was not correlated with the scores of PANSS and NOSIE (P>0.05). Conclusions Smoking may be a self-treatment behavior for patients with chronic schizophrenia. Furthermore, "divert" may be beneficial for the recovery.

Objective·To establish a cell-based screening system for identification of compounds with activity in regulating retinoic acid receptor (RARα) stability. Methods·The modified pMSCV plasmid constructs, named as RARα-EGFP-IRES-DsRed, consists of enhanced green fluorescent protein (EGFP) fusing to RARα and red fluorescent protein (DsRed) as internal references incorporating the internal ribosome entry site (IRES) as interval sequence. The RARα-EGFP-IRES-DsRed plasmid was stably transfected into NB4 cells which were named as NB4-pMGIR-RARα. Fluorescence signals of EGFP and DsRed indirectly reflecting the expression of RARα, were detected by flow cytometry in cells that were treated with all-trans retinoic acid, sodium valproate, cytarabine, lenalidomide, etoposide, montelukast and gambogic acid, respectively. Effects of these compounds on the expression of RARα protein were further examined by Western blotting. Results·A double fluorescence reporter system for screening compounds that can increase the stability of RARα protein was successfully established, and sodium valproate was identified as a potent compound to promote the stability of RARα. Conclusion·The double fluorescence reporter system can be used to screen compounds regulating the stability of RARα protein, which can be further used to identify compounds regulating the stability of other proteins.

Objective To observe the preventive effects of puerarinon development of deep vein thrombosis (DVT) in elderly women with osteoporosis after hip replacement. Methods 100 elderly women with osteoporosis who scheduled for femoral head arthrolastybetween January 2012 and January 2014 in Cangzhou Central Hospital were selected and then randomly divided into a study group (n=50) and a control group (n=50). The control group received routine anti?inflammatory and anticoagulant therapy ,while the study group received intravenous drip of puerarinof 400 mg mixed with 5%glucose liquid 500 ml daily for 15 days as a treatment course. After the treatment, DVT incidence rate ,change of early diagnostic indexes and hemorheology were compared with their baselines. Results DVT incidence rate was significantly lowerin the study group than in the control group (8.0%vs. 24.0%, P<0.05). Ascompare with the control group,thromboxane A2/prostacyclin,plasma homocysteine and hemorheology?were significantly reduced (P < 0.05). Conclusions Puerarin has a preventive effect for deep vein thrombosis in elderly women with osteoporosis after hip replacement.

Objective To investigate the association between 5-hydroxytryptamine 2A receptor (HTR2A)gene T102C locus polymorphism and schizophrenia,and to provide basis for evidence-based medicine for the genetic background of schizophrenia.Methods PubMed,EMbase,CNKI,WanFang and Vip information databases were used to search full text of all the relevant studies about the association between HTR2A gene T102C locus polymorphism and schizophrenia,which were published during 2003 to 2012.Based on reviewing full text,the data were selected, evaluated and accessed. RevMan 5.1 and Stata 1 2.0 were used to perform the statistical analysis of those studies that were in accordance with the inclusive criteria. According to the different ethnicities, the obj ects were divided into two subgroups as European and Asian to analyze respectively. Also, depending on different inheritances, the obj ects were divided into five patterns including C/T allele, CC/TT, CC/CT+TT, CC+CT/TT and CC+ TT/CT genotypes to analyze respectively, including heterogeneity inspection, effect consoliating and publication bias assessment. Results A total of 11 studies were available for this analysis, including 2 443 schizophrenia patients and 2 469 controls.The Meta-analysis results showed that the allele of all people were OR=1.12,95%CI=0.96-1.31,P>0.05;CC/TT of all people were OR=1.11,95%CI=0.80-1.53,P>0.05;CC/CT+TT of all people were OR=1.13,95%CI=0.99-1.30,P>0.05;CC+CT/TT of all people were OR=1.18, 95%CI=0.93-1.50,P>0.05;CC+TT/CT of all people were OR=0.95, 95%CI=0.84-1.06,P>0.05.Conclusion Current evidence is insufficient to show that HTR2A gene T102C locus polymorphism may be associated with schizophrenia, suggesting that the gene polymorphism has no significantly genetic association with schizophrenia.

Aim To study the effects of HiHi and HiLo on the lipid metabolism in rats through blood lipids and fatty acid oxidation in gastrocnemius of rats. Methods Thirty male SD rats were selected by means of adaptive training, and then divided into 3 groups randomly: living low-training low group (LoLo), living high-training high group (HiHi), and living high-training low group (HiLo). The rats ran on a treadmill 60 min a day at the speed of 35 m/min under normoxic condition or 30 m/min under hypoxic condition (13.6% of ambient FIO_2), 6 days a week for 4 weeks. The samples from blood and gastrocnemius were removed 24 hours after the last training by the end of 4-week experiment. TC, TG, HDL and LDL were tested with a full-automatic biochemical analyzer. LPL, leptin and AD were measured using ELISA. Real-time quantitative PCR was adopted to test the expression of PPARa and CPT-1 mRNA in rats' gastrocnemius. Results Compared to the LoLo, TC and TG decreased significantly (P0.05) and LPL and AD increased significantly (P<0.01) in HiHi.' PPARa mRNA and CPT-1 mRNA expressions in gastrocnemius were significantly higher in HiHi(P<0.05) than in LoLo, and significant descent of HDL(P<0.05) and CPT-1 mRNA expression(P<0.01) revealed in HiLo, as compared to the LoLo. Compared to the HiLo, HDL(P<0.05), and LPL, AD and CPT-1 mRNA expression(P<0.01) enhanced in HiHi. Conclusion (l) HiHi was more superior in regulation of blood lipids than LoLo due to increasing of LPL, and could facilitate fatty acid oxidation because of enhancement of CPT-1 mRNA, AD and PPARa mRNA. (2) Comparing to the normoxic training, HiLo had no beneficial effect on the blood lipid metabolism and decreased the fatty acid oxidation in gastrocnemius.(3 )HiHi was more superior in the effeet of HDL thah HiLo due to increasing of LPL, and could facilitate fatty acid oxidation because of enhancement of AD and CPT-1 mRNA.

Objective:To observe the anti-carcinoma and immuno-regulatory effects of shikonin derivatives.Methods:A water-soluble preparation of shikonin derivatives was prepared (designated as LE)and given by lavage (2.5～10 mg/kg daily for 10 days) to the mice inoculated with either HepA22 or S180 sarcoma. Their survival duration and the in situ tumor mass were observed. Thymus and spleen indexes of the mice were measured. The parameters for immuno-functions were detected by the routine activity assays, which included NK cytotoxicity, ConA-induced lymphocyte transformation and IL-2 production by the splenocytes of the mice. Thymic and splenic morphology of the experimental animals were microscopically examined with HE staining.Results:Both thymic and splenic indexes in the tumor-bearing mice diminished extremely compared to those of the normal control, and the immunological functions analyzed were also found obviously lowered when loaded with the transplantable carcinomas. Under light microscopy, it was surprisingly exhibited that thymus cortex was almost disappeared in the organs of tumor-bearing mice, and the germinal centers of their spleens were visibly shrunk. LE inhibited propagation of the inoculated tumors and at the same time, it amended the immunosuppresive impacts by tumor-bearing, including both structures of immune organs and the bioactivities of spleen cells.Conclusion:LE can reverse the immune damages mediated by carcinomas.

Objective: To study the radioprotective effect of flavonoids from Ginkgo biloba leaves(GBF). Methods: Three water extracts of GBF were prepared (low dosage 10 mg/100 ml, medium dosage 20 mg/100 ml and high dosage 100 mg/100 ml) and orally administered to mice . After 10 d, the mice were exposed to 8.5Gy -rays. After another 10 d of oral administration, the survival rates were recorded in 30 d. In another experiment, six groups of mice (three GBF groups, radiation control, normal control and cyclophosphamide group) were arranged. The first three groups were orally administered with low, medium and high dosage of GBF respectively for 11d; the other three groups with distilled water. Then the three GBF groups and radiation group were exposed to 1.0Gy -rays. Then they were orally administered again in the following 7d . Micronucleated polychromatic erythrocytes in bone-marrow and sperms (AFS) in mice were observed on the 21st day after termination of oral administration. Proliferation rates of lymphocyte (PRL) were determined in the three GBF groups and normal control. Results: Low, medium and high dosage of GBF increased the survival rates by 31.7%, 25.3% and 26.5% respectively(P

Objective To construct an eukaryotic expression vector pcDNA-UCA1a(CUDR)and to observe its expression in bladder cancer UM-UC-2 cells, and to provide experimental basis for study on the relationship between UCA1a(CUDR)gene and bladder cancer.Methods Human total length of UCA1a(CUDR)gene was obtained from the 5′-RACE-Ready cDNA of bladder cancer BLZ-2 1 1 cells by PCR and was inserted into pcDNA3.1 (+)vector.pcDNA-UCA1a(CUDR)was identified by digestion with EcoRⅠ and BamHⅠ.The bladder cancer UM-UC-2 cells were transfected stably with the constructed eukaryotic expression vector pcDNA-UCA1a(CUDR). The expressions of UCA1a(CUDR)gene in the UM-UC-2 cells transfected with pcDNA-UCA1a(CUDR)and the UM-UC-2 cells transfected with pcDNA3.1(+)(control vector)were detected by RT-PCR.Results The inserted fragment with 2 200 bp was successfully amplified, which was in accordance with the expected results. The eukaryotic expression vector pcDNA-UCA1a(CUDR)was constructed successfully after identified by double enzyme digestion and sequencing.The RT-PCR results showed that the expression of UCA1a(CUDR)gene in the cells transfected with pcDNA-UCA1 a (CUDR ) was significantly increased compared with the cells transfected with pcDNA3.1 (+). Conclusion The eukaryotic expression vector pcDNA-UCA1a (CUDR ) is successfully constructed.The UCA1a(CUDR)gene highly expresses in the UM-UC-2 cells transfected with the expression vector.