(0.05)) during dobutamine 5 ?g?kg~(-1)?min~(-1) stage. Blood pressure had significant increase both in dobutamine 10 ?g?kg~(-1)?min~(-1) stage and post-coronary revascularization. The sensitivity,specificity,accuracy of dobutamine 5 and 10 ?g?kg~(-1)?min~(-1) were (73.0)% and (89.6)%, (81.7)% and (82.8)%,(76.9)% and (86.5)%, respectively. Conclusions LDDSE is a simple,safe and no injury means to identify survival myocardium in myocardial infarction.

In this article, the projects in drug metabolism and pharmacokinetics funded by NSFC during "10th Five Year Plan" (2001~2005) in China were reviewed. The major research fields of these projects in drug metabolism and pharmacokinetics funded by NSFC during the financial years were overviewed and analyzed. Finally, current problems in these research fields in China were also briefly analyzed.

Identification and validation of a new target is one of the most important steps for new antituberculosis (TB) drug discovery. Researches have shown that Mycobacterium tuberculosis (Mtb) encodes 20 CYP450 enzymes which play important roles in the synthesis and metabolism of lipid, cholesterol utilization, and the electron transport of respiratory chain in Mtb. With the critical roles within the organism as well as the protein structures of six Mtb CYP450 enzymes being clarified, some of them have been highlighted as potential anti-tuberculosis targets. In this paper, the phylogenetic analysis, the structural features, and the enzymatic functions of Mtb CYPs, as well as the mechanism of interactions with selective inhibitors such as azole antifungal agents for the CYPs have been reviewed and summarized. The druggability of the CYPs has also been analyzed for their further utility as targets in high throughput screening and rational design of more selective inhibitors.

Objective To study the life quality and influencing factors for empty nester elderly in rural area in Hunan,and to provide the scientific basis for the effective interventions.Methods The two villages of Yiyang and Huaihua were randomly selected by cluster sampling from June 2011 to December 2011 in Hunan.Data of the world health organizations quality of life instrument-short version (WHOQOL-BREF) was collected by face to face interview with the empty nesters.The risk factors for the quality of life in empty nester elderly in rural area were analyzed by the multiple linear regression analysis.Results A total of 785 valid questionnaires were acquired,among which 472 cases were from empty nester elderly (60.1％,472/785),the average age of them was (69.3±7.3) years,and the male:female ratio was 1.1:1 (250:222).The literacy of 81.8％ of empty nester elderly were under junior middle school,69.7％ of them married with consorts who were still living,74.4％ of them were farmer,75.2％ of them had monthly income under 500 Yuan,56.4％ of them got the income from their own labor,69.9％ of them considered that their relationship with children were harmony.64.2 ％ of empty nester elderly in village suffered from chronic diseases and 16.7 ％ of them suffered from accidental injury within the last one year.The scores in physiological health,psychological health and quality of life were lower in empty nester elderly than in the non-empty nester elderly [(60.8±15.7) vs.(63.1±13.5),(59.0±12.1) w (64.6±17.4),(59.5±9.8) vs.(63.0 ± 10.1),t=3.18,4.43,4.91,all P＜0.05].The multiple linear regression analysis showed that the influencing factors for quality of life in empty nester elderly were education background,marital status,source of finance,relationship with children,chronic disease and accidental injury within the last one year (β=1.693,2.426,0.779,1.060,-7.007,-3.784,all P＜0.05).Conclusions The empty-nest elderly accounts for more than half of the elderly in rural area,who have the lower levels in physio-psychological health and quality of life.We should improve their awareness and knowledge of health,build their harmonious relationship with spouse and children,improve the social security and medical insurance system,actively promote the knowledge of chronic disease and accidental injury,in order to improve the quality of life in empty nester elderly and achieve the healthy aging.

Objective To determine the solubility and apparent oil/ water partition coefficient of sitafloxacin in different solvents. Methods High performance liquid chromatography (HPLC) was used. The column was Dikma Diamonsil C18 (2) (4. 6 mmí250 mm,5 μm). The mobile phase was 0. 05 mol·L-1 KH2 PO4 solution (pH was adjusted with H3 PO4 to 2. 4)-acetonitrile (7030). The column temperature was set at room temperature. The flow rate was 1. 0 mL·min-1 . The detection wavelength was 295 nm and the injection volume was 10 μL. The solubility of sitafloxacin and the apparent oil/ water partition coefficient at pH 2. 0,4. 3,5. 8,6. 6,7. 4,8. 0,10. 0 and 11. 2 were determined. Results The equilibrium solubility of sitafloxacin in water was 0. 44 mg·mL-1 and the apparent oil/ water partition coefficient was 0. 23 (lgP= -0. 64) at (37±2) ℃ . Sitafloxacin has the lowest equilibrium solubility (0. 13 mg·mL-1 ) and the highest apparent oil/ water partition coefficient in pH7. 4 buffer solution system. At pH>10 and pH<5. 8,the solubility of sitafloxacin increased obviously and apparent oil/ water partition coefficient decreased. Conclusion Sitafloxacin is insoluble in water and also poorly soluble in oil,but its solubility could be improved significantly in acidic or alkaline solution.

Objective For bioequivalence test of the consistency evaluation of generic drug products,providing a reference of varieties of biowaiver.Methods Based on Human bioequivalence test waiver guidelines (draft),on condition that first drug of the consistency evaluation,to introduce and conclude briefly the standards of biowaiver and varieties of biowaiver in FDA,WHO and EMA.Results Contrast to FDA,there are 59 varieties applied for the waiver and 19 varieties not applied for the waiver in the 289 varietie;compared to WHO,10 drugs are exempted and 1 grug is exempted in EMA.Conclusion At present,the specific list of drugs are not published of biowaiver in our country,the pharmaceutical companies should compare and consult revelant standards and specific drugs in China and abroad,to speed up the progress of the consistency evaluation.

Objective To study the tortuosity coefficient (TC) values of basilar arteries in the adult,and its change in cerebral basilar artery infarction.Methods TC values of basilar arteries was prospectively analyzed using the magnetic resonance angiography images of 135 controls(19-80 years of age,male 90,female 45)and 42 patients with cerebral infarction(5l-70 years of age,male 28,female 14).The relationship between TC values and posterior circulation infarction was statistically evaluated.Results Differences of TC between age groups were statistically significant except group B (31-50 years)and C(51-70 years)(F=10.31,P<0.01).The infarction group had greater TC value(2.497±1.200)than the control group(1.939±0.850,t=2.39,P=0.0195).Conclusions (1)Basilar artery tortuosity is positively related to age,reflecting the degree of arteriosclerosis;(2)Basilar artery tortuosity increases in patients with posterior circulation infarction.

Objective To build a RNA interference vector for PQ-loop repeat protein (LRP) gene,and to evaluate the effect of the vector on the expression of PQ-LRP gene in Microsporum canis.Methods The PUC-PLULT and PCB309-PLULT vectors were constructed sequentially by using Agrobacterium tumefaciens-mediated T-DNA insertional mutagenesis,adding multiple cloning sites,and introducing the hygromycin-resistance gene.Microsporum canis was transformed with the PCB309-PLULT vector followed by a series of passages and hygromycin selection.Real-time quantitative PCR was performed to measure the expression of PQ-LRP gene in Microsporum canis before and after transformation.Results The intermediate vectors PUC-PLUT and PUC-PLULT were constructed and identified by PCR and gene sequencing.The 8 825-bp interference vector PCB309-PLULT was successfully built and confirmed by enzyme digestion.The optimum concentration of hygromycin for screening for Microsporum canis transformants was determined as 300 mg/L.The mRNA expression level of PQ-LRP was decreased by 61％ in the transformants as compared with untransformed Microsporum canis (0.39 vs.1.00).Conclusion The constructed PCB309-PLULT interference vector can effectively inhibit the expression of PQ-LRP gene in Microsporum canis.

Objective To investigate the impact of glucose metabolism-related protein 1 (GMRP1) on the regulation of c-Myc gene transcription, to establish GMRP1 gene knockout mouse model, and to study the influence of GMRP1 on glucose metabolism. Methods Chromatin immunoprecipitation-PCR (ChIP-PCR) was utilized to screen out the genes transcriptionally regulated by GMRP1. Luciferase reporter system was applied to assay the regulation of c-Myc promoter activity by GMRP1. GMRP1 knockout mice were constructed and validated by PCR and western blotting. Body weight and random blood glucose were measured in both knockout and wild type mice fed with either chow diet or high-fat diet. The levels of glucose metabolism in mice of 20 or 28 weeks old were evaluated by intraperitoneal glucose tolerance test. Results GMRP1 was capable of binding to the promoter of c-Myc gene and activating the expression of c-Myc gene. There were no significant differences in body weight, random blood glucose or glucose tolerance between GMRP1-deficient and wild type mice fed with either chow diet or high-fat diet (all P > 0.05). Conclusion GMRP1 may activate the transcription of c-Myc gene. GMRP1 deficiency exerted no significant effects on mouse glucose metabolism.

Objective To investigate the efficacy and tolerability of estradiol (E2) gel with postoperative patients of moderately severe ovarian endometriosis cyst,who suffer from the side effect of GnRH agonist.Methods Sixty samples were selected with stage Ⅲ ～ Ⅳ ovarian endometriosis after conservative operation by the same operator at the Department of Gynecology,Xiangya Hospital,Central South University,between February 2013 and August 2014.All of the patients after surgeries were randomly divided into three groups:control group (n =20) with only goserelin injection after conservative surgery,treatment group A (n =20) who received estradiol gel,and treatment group B (n =20) who received tibolone as an add-back therapy.The serum E2,follicle stimulating hormone (FSH),luteinizing hormone (LH),hypoestrogenic symptoms,the incidence of uterine bleeding,and the recurrence after conservative operation were compared among three groups.Results Three months later aster treatment with goserelin,the serum level of E2 of three groups showed statistically significant difference (P ＜ 0.05).Serum E2 level of treatment group A was not significantly higher than treatment group B (P ＞ 0.05).The kupperman sore,the incidence of hot flashes sweating,tiring,and agrypnia of treatment groups A and B were significantly lower than the control group (P ＜ 0.05).The incidence of uterine bleeding and recurrence dont differ sharply among three groups (P ＞ 0.05).Conclusions GnRHa combined with estradiol gel can improve symptoms of postoperative patients,reduce side effects effectively,and avoid increase of the risk of vagina bleeding and relapse.