TMP. The results suggested that 12D-TMP and 6D-TMP possessed remarkable isotope effects, and that the pyrazine ring of TMP may be responsible for its pharmacodynamics, while the substituted groups might primarily govern its pharma-cokinetics and toxicity. The results also indicated that to study the structure activity relationship of TMP and to modify its chemical structure are very fruitful for the development of TMP analogues of high potency.

A rapid and sensitive liquid chromatography-mass spectrometry/mass spectrometry (LC-MS/MS) method for quantification of sitagliptin in human plasma and urine had been developed. This method was applied to the pharmacokinetics study of sitagliptin tablet after single- and multiple-dosing in Chinese population. Plasma samples were prepared by a liquid-liquid extracted method, and urine samples were diluted. Compounds were analyzed by multiple reaction monitoring (MRM) mode with a electrospray ionization (ESI) interface. Mobile phase consisted of methanol and water (85 : 15, v/v). The linear concentration range of calibration curve was 0.5-1 000 ng.mL-1. and 0.2-100 µg.mL , intra-run/between-run accuracy was 98.98%-103.69% and 97.63%-102.29%, intra-run/between-run precision was <5.51% and 4.26% for plasma and urine sample, respectively. The stability of sitagliptin stock solution was tested for 55 days at -30 °C. Sitagliptin was stable when stored under the following conditions: 24 hours in the autosampler after sample preparation; 24 hours at room temperature, after 3 freeze and thaw cycles (from -30 °C to room temperature), 40 days at -30 °C for plasma and urine samples. The absolute recovery in plasma was 71.1%, and no matrix effect was founded. This method was proved simple, specific, sensitive, rapid and suitable for pharmacokinetics study of sitagliptin in human being.
Calibration ; Chromatography, Liquid ; Humans ; Liquid-Liquid Extraction ; Sitagliptin Phosphate ; blood ; pharmacokinetics ; urine ; Tandem Mass Spectrometry

This study was aimed to use the method of modulation transfer function (MTF) to compare image quality among three different Olympus medical rigid cystoscopes in an in vitro model. During the experimental processes, we firstly used three different types of cystoscopes (i. e. OLYMPUS cystourethroscopy with FOV of 12 degrees, OLYMPUS Germany A22003A and OLYMPUS A2013A) to collect raster images at different brightness with industrial camera and computer from the resolution target which is with different spatial frequency, and then we processed the collected images using MALAB software with the optical transfer function MTF to obtain the values of MTF at different brightness and different spatial frequency. We then did data mathematical statistics and compared imaging quality. The statistical data showed that all three MTF values were smaller than 1. MTF values with the spatial frequency gradually increasing would decrease approaching 0 at the same brightness. When the brightness enhanced in the same process at the same spatial frequency, MTF values showed a slowly increasing trend. The three endoscopes' MTF values were completely different. In some cases the MTF values had a large difference, and the maximum difference could reach 0.7. Conclusion can be derived from analysis of experimental data that three Olympus medical rigid cystoscopes have completely different imaging quality abilities. The No. 3 endoscope OLYMPUS A2013A has low resolution but high contrast. The No. 1 endoscope OLYMPUS cystourethroscopy with FOV of 12 degrees, on the contrary, had high resolution and lower contrast. The No. 2 endoscope OLYMPUS Germany A22003A had high contrast and high resolution, and its image quality was the best.
Diagnostic Imaging ; instrumentation ; Endoscopes ; Endoscopy ; instrumentation ; Software

OBJECTIVETo construct microRNA-223 overexpression and suppression lentivirus vectors and determine their effects after infecting oral squamous cell carcinoma (OSCC) cell line.

METHODSLentivirus vectors GV229 and GV232 were cut by the restriction sites of Age I and EcoR I and connected to the target gene, which contained mature microRNA-223 and microRNA-223 oligonucleotide. Real-time polymerase chain reaction (PCR) method was used to detect the microRNA-223 expression level after infecting the recombinant lentivirus vector into the OSCC cell line.

RESULTSThe successful construction of microRNA-223 recombinant lentivirus vectors was confirmed by the PCR method and DNA sequencing. HN-30 cell infected with microRNA-223 overexpression vector showed a significant increased in microRNA-223 expression, whereas HN-30 cell infected with microRNA-223 inhibitor vector suppressed microRNA-223 expression.

CONCLUSIONThe microRNA-223 overexpression and suppression lentivirus vectors are successfully constructed. These vectors could alter the expression level of microRNA-223 in OSCC cell line significantly, and provide a stable cell line for functional studies in the future.

Objective To investigate the mechanism of an antifibrotic drug, pirfenidone, in preventing radiation-induced pulmonary fibrosis. Methods Male BALB/C mice were randomized into 4 groups:control group (C), radiation alone group (R), pirfenidone alone group (P), and pirfenidone plus radiation group (P + R). Irradiation was administrated to the whole pulmonary with a single fraction of 12 Gy. The pirfenidone was given 0. 3 ml/kg/d from 3 days prior to irradiation to 12 weeks after.Bronchoalveolar lavage fluid (BALF) from right lung was collected for macrophages counting every monthmonthly until 6 months after irradiation, and left lungs were collected and fixed for. The pulmonary fibrosis was assessed by Masson trichrome staining. The plasma transforming growth factor β(TGF-β) was measured by ELISA. The lung hydroxyproline was evaluated by alkaline solution. Results Compared to group R, the counts of macrophages in BALF in group P + R were reduced by 76% and 62%, and hydroxyproline levels were reduced by 21% and 24% at the 4th and 5th months, respectively. The plasma TGF-β decreased from the 3rd month to 5th month. Pirfenidone markedly ameliorated the severity of lung fibrosis at the 4 - 6th month after radiation. Conclusions Pirfenidone can prevent radiation-induced pulmonary fibrosis, the mechanism of which may be the reduced of inflammation and collagen deposition by decreasing macrophages and hydroxyproline.

0.05). Conclusion: Although the mechanism of the correlation between upper and lower airway inflammatory diseases is not yet clear,chronic sinusitis and nasal polyposis may share some characteristics in involving the lower airway.

OBJECTIVE: To observe the household environment dust mites allergens content distribution characteristics and influence factors of children with allergic rhinitis to dust mites in Wuhu. METHOD: Collect the surface dust in bedroom and living room floor, mattresses, pillows, sofa of 102 children with allergic rhinitis families. Dust mite allergen components 1 (Der f1) and house dust mites allergens 1 components (Der p1) of the dust samples were determined by enzyme-linked immunosorbent assay (ELISA). RESULT: One hundred and twenty samples were collected . In a domestic dust mites samples, with a median of M (Min and Max) said dust mite allergen levels, Der f1 and Der p1 content was 2.66 (0.03, 26.63), 3.48 (0, 03, 33.68), respectively. Der f1 was significantly less than Der p1, and the difference was statistically significant (P < 0.05). According to the classification of urban and township, there were 68 cases and 34 cases. Der f1 content in the samples was 2.91 (0.31, 26.63), 2.40 (0.08, 16.02), respectively. Der p1 content was 4.28 (0.03, 20.77), 3.88 (0.14, 33.68), respectively. The dust mites content of urban was significantly more than that of villages and towns, the difference was statistically significant (P < 0.05). Samples were also classified by gender. The dust mites allergens content in either boy's or girl's family were similar, there was no statistically significant difference (P > 0.05). CONCLUSION The household dust mites of children allergic rhinitisin Wuhu area is given priority to with Der p1, and urban dust mites are significantly more than village's and town's. Enhancing health education, controlling dust mites allergens contamination inside the bedroom, especially urban areas, are positive differences for the prevention and treatment of allergic diseases such as allergic rhinitis in children.
Allergens ; analysis ; Animals ; Antigens, Dermatophagoides ; analysis ; Arthropod Proteins ; analysis ; Bedding and Linens ; Child ; Cysteine Endopeptidases ; analysis ; Dermatophagoides farinae ; Dust ; analysis ; Enzyme-Linked Immunosorbent Assay ; Female ; Humans ; Male ; Rhinitis, Allergic ; epidemiology

A rapid and sensitive liquid chromatography-mass spectrometry/mass spectrometry (LC-MS/MS) method for quantification of sitagliptin in human plasma and urine had been developed. This method was applied to the pharmacokinetics study of sitagliptin tablet after single- and multiple-dosing in Chinese population. Plasma samples were prepared by a liquid-liquid extracted method, and urine samples were diluted. Compounds were analyzed by multiple reaction monitoring (MRM) mode with a electrospray ionization (ESI) interface. Mobile phase consisted of methanol and water (85 : 15, v/v). The linear concentration range of calibration curve was 0.5-1 000 ng.mL-1. and 0.2-100 µg.mL , intra-run/between-run accuracy was 98.98%-103.69% and 97.63%-102.29%, intra-run/between-run precision was <5.51% and 4.26% for plasma and urine sample, respectively. The stability of sitagliptin stock solution was tested for 55 days at -30 °C. Sitagliptin was stable when stored under the following conditions: 24 hours in the autosampler after sample preparation; 24 hours at room temperature, after 3 freeze and thaw cycles (from -30 °C to room temperature), 40 days at -30 °C for plasma and urine samples. The absolute recovery in plasma was 71.1%, and no matrix effect was founded. This method was proved simple, specific, sensitive, rapid and suitable for pharmacokinetics study of sitagliptin in human being.

Objective: To investigate the relationship between heart rate variability (HRV), blood pressure variability (BPV) and autonomic nerve function, blood vessel damage in patients with essential hypertension (EH) via synchronous monitoring. Methods: A total of 275 EH patients admitted to our hospital from 2011-04 to 2014-01 were enrolled. The vascular function was assessed by carotid-femoral pulse wave velocity (PWV). Based on PWV, the patients were divided into 2 groups: Normal PWV group (PWV<9m/s),n=185 and High PWV group (PWV≥9m/s),n=90. Synchronic 24h dynamic electrocardiogram (Holter) and 24h ambulatory blood pressure monitoring (ABPM) were performed in all patients. t-test, chi-square test, person liner correlation study and multi stepwise regression analysis were conducted to explore the relationship between HRV, PBV and PWV. Results: HRV and BPV in High PWV group had been changed unusually. Compared with Normal PWV group, High PWV group showed decreased standard deviation of the average of all normal-to-normal intervals in all 5-minute intervals (SDANN) (159.66±66.50) ms vs (194.36±119.29) ms and increased 24 h systolic blood pressure standard deviation (24h SSD) (14.40±3.65) mmHg vs (12.98±3.46) mmHg, all P<0.01; increased new index of night/day HR ratio (0.90±0.08) vs (0.87±0.06), P<0.01 and it had liner correlation to PWV (r=0.169, P=0.005). Multi stepwise liner regression analysis indicated that 24hSSD and HRV at low frequency (LF) portion had obvious and independent correlation to PWV (standard β value=0.352 and 0.212 respectively). Conclusion: ① EP patients were with decreased HRV (SDANN), increased BPV (24h SSD) and the higher incidence of arteriosclerosis; 24h SSD and HRV at LF portion were the most 2 important risk factors affecting PWV. ②Autonomic nerve dysfunction, vagus nerve over-excitatory were the independent risk factors for promoting the occurrence and development of arteriosclerosis in EH patients. ③Night/day HR ratio as a sensitive index for examining autonomic nerve function was independently related to hypertensive vessel damage. Synchronic monitoring of HRV and BPV is helpful to identify blood vessel damage in EH patients.

Objective To analyze the application and funding for projects in radiation oncology from National Natural Science Foundation of China ( NNSFC ) from 2006 to 2015. Methods To collect the funding information in radiation oncology from NNSFC from 2006 to 2015, a computerized search was performed in the ISIS system using a subject code of H1610 and a keyword of radiation oncology. Analyses were performed in distribution of research fields, the geographical distribution of applicants, and the properties of institutes/universities the applicants were affiliated with. Results In the last decade, a total of 435 projects in the field of radiation oncology were funded with 180 million yuan. Most projects were funded by general, youth, and regional foundation, which covered the highest proportion of NNSFC. For a single project, the amounts of funding from general, youth, and regional foundations were 530, 220, and 400 thousand yuan, respectively. The institutes/universities the NNSFC?funded projects were affiliated with were located quite close to each other. The top 10 institutes/universities in terms of the number of NNSFC?funded projects covered 53% of projects. In all projects, 88% studied basic science, which covered many hot topics in oncology including biological effects of radiotherapy, microenvironment, and stem cells. A small number ( 12%) of projects focused on physics. Top 3 cancers in terms of the number of projects and the amount of funding were lung cancer, nasopharyngeal carcinoma, and esophagus cancer. Conclusions In the last decade, the field of radiation oncology has stable increases in the number of NNSFC?funded projects and the amount of funding. The NNSFC?funded research teams are unevenly distributed, most of which are located in East China. The most popular topic in basic science studies is about biological effects of radiotherapy.