Objective To determine the efficacy and toxicity of docetaxel in patients with paclitaxel-resistant advanced non-small cell lung cancer (NSCLC). Methods The clinical data from 15 patients with NSCLC who were admitted in the Shanghai Chest Hospital from January 2005 to May 2008 were retrospectively analyzed. The effects and toxicities of the second-line treatment were assessed. The progression-free survival time(PFS) and overall survival time(OS) were analyzed. Results The disease control rate was 66.7 %, with a progression-free survival time of 6 months, and a overall survival time of 17.3 months. The 1-year survival rate was 63.3 %. The toxic effects were as expected. Conclusion The doeetaxel-based agent is active in patients with paelitaxel-resistant advanced NSCLC.

OBJECTIVEAn UPLC method was developed to evaluate the quality of Paeoniae Radix by simultaneously determining four components, paeoniflorin, albiflorin, benzoylpaeoniflorin and paeonol in Paeoniae Radix Alba decoction pieces.

METHODThe UPLC chromatographic column was ACQUITY UPLC® HSS T3. The mobile phase was acetonitrile-0.05% phosphoric acid water with gradient elution. The column temperature was 30 °C and detection wavelength was 230 nm with a flow rate of 0.4 mL · min(-1). A linear model was obtained through principal component analysis (PCA), and PCA scores were used to evaluate the quality of Radix Paeoniae Alba decoction pieces comprehensively.

RESULTPaeoniflorin, albiflorin, benzoylpaeoniflorin and paeonol could be well separated from other components, and the results of specificity, precision, repeatability, linearity, recovery rate and stability reached the standards, respectively. The content of paeoniflorin in 9 batches of Paeoniae Radix Alba decoction pieces was below the standard given by Chinese Pharmacopoeia (2010 edition). Using the comprehensive scoring method with principal component analysis, the results showed that the samples from Zhejiang province have better quality than those from Anhui and Shandong provinces.

CONCLUSIONThe method established in this study can effectively determine the content of paeoniflorin, albiflorin, benzoylpaeoniflorin and paeonol, which could be used for quality control of Paeoniae Radix Alba.

Drugs, Chinese Herbal ; analysis ; Paeonia ; chemistry ; Principal Component Analysis

After studying the discipline of chemical components distribution in peony root, it was found that the content distribution of albiflorin, paeoniflorin, benzoylpaeoniflorin and paeonol was inhomogeneous in different parts of peony root, as same as in different roots belonging to a same plant. Therefore, in order to minimize the effects of different qualities of materials on experimental result, the content changing percentages of four chemical components was chosen as indicators to study processing method of Paeoniae Radix Alba. The processing technique of Paeoniae Radix Alba was put peony roots in the boiled water for at most ten minutes, and cut them into 2-3 mm slices after peeling the root bark, finally dry them in a oven under 55 degrees C, which was similar to the traditional processing method used in Bozhou. And the peeling, boiling and drying methods would affect the contents of albiflorin, paeoniflorin, benzoylpaeoniflorin and paeonol on several levels.
Chemistry, Pharmaceutical ; methods ; Chromatography, High Pressure Liquid ; Drugs, Chinese Herbal ; chemistry ; isolation & purification ; Paeonia ; chemistry ; Plant Roots ; chemistry

To ensure the stability of chemistry components and the convenience of operation, ultrasound method was chosen to study in this investigation. As the total common peaks area in chromatograms was set to be evaluation index, the influence on the technology caused by extraction time, ethanol concentration and liquid-to-solid ratio was studied by using single factor methodology, and the extraction technology of Paeoniae Radix Alba was optimized by using response surface methodology. The results showed that the extracting results were most affected by ethanol concentration; liquid-to-solid ratio came the second and extraction time thirdly. The optimum ultrasonic-assisted extraction conditions were as follow: the ultrasonic extraction time was 20.06 min, the ethanol concentration in solvent was 72.04%, and the liquid-to-solid ratio was 53.38 mL · g(-1), the predicted value of total common peaks area was 2.1608 x 10(8). Under the extraction conditions after optimization, the total common peaks area was 2.1422 x 10(8), and the relative deviation between the measured and predicted value was 0.86%, so the optimized extraction technology for Paeoniae Radix Alba is suitable and feasible. Besides, for the purpose of extracting more sufficiently and completely, the optimized extraction technology had more advantages than the extraction method recorded in the monogragh of Paeoniae Radix Alba in Chinese Pharmacopoeia, which will come true the assessment and utilization comprehensively.
Paeonia ; chemistry ; Technology, Pharmaceutical ; methods

Objective To study the correlation between the deformation and displacement trend of the lumbosacral vertebra (L1-S1) for two typical scoliosis spines under vertical loads,so as to provide the mechanical basis of treatment and prevention of scoliosis in clinic.Methods The X-ray computed tomography (CT) images of two typical scoliosis spines (Lenke-4AN type and Lenke-5CN type) were converted into 3D models,and their finite element models were then established and verified.The internal stress distribution and displacement variation of the models were calculated by the finite element software;the correlation between the lumbosacral vertebral structure and displacement of the spine was analyzed.Results Under the same boundary conditions and load cases,the stress and displacement for two kinds of lumbosacral vertebral models showed different trends.Due to its leftleaning and forward convex bending deformation as well as the relatively large lordosis angle (60°) and smaller left-leaning angle (17.37°),the Lenke-4AN type lumbosacral spine produced slightly small forward convex displacement (8.18 mm) and relatively large left-leaning displacement (0.97 mm).The Lenke-5CN type lumbosacral spine showed left-leaning and forward convex bending deformation as well,with relatively large lordosis angle(59°) and left-leaning angle (26.97°),so it produced more severe left-leaning displacement (20.65 mm) andforward convex displacement (9.22 mm).Conclusions The deformation trend of lumbosacral vertebra is closelyrelated to its structural characteristics,and different scoliosis lumbosacral vertebral structures will cause the corre-sponding deformation trend.The research findings are important for the prevention and treatment of scoliosis.

OBJECTIVETo investigate the effect of Helicobacter Pylori lipopolysaccharide (Hp-LPS) on expression of Gli and Ptch-1 proteins in sonic hedgehog (Shh) signaling pathway of gastric mucosa GES-1 cells.

METHODSThe LPS was extracted from Hp by hot phenol water method, and then the concentration of LPS was detected by the kinetic turbidimetric assay. GES-1 cells were stimulated by different concentrations of Hp-LPS (0, 1, 10, 20, 30 and 40 μg/ml). The inhibition rates of cell growth were measured by MTT assay after treated with Hp-LPS for 24 h. The expression of Gli and Ptch-1 proteins were determined by Western Blot.

RESULTSMTT assay showed that the inhibition rates of GES-1 cell growth after treatment by different concentrations of Hp-LPS (1, 10, 20, 30 and 40μg/ml) were 25.8% ± 2.7%, 34.2% ± 3.1 %, 46.3% 3.4%, 60.8% ± 2.1% and 82.9% ± 2.8% respectively (r=0.985, P<0.001). Western blot showed that the expressions of Gli and Ptch-1 proteins were decreased after Hp-LPS treatment (0, 1, 10, 20, 30 and 40 μg/ml): the relative expression values of Gli were 1.286 ± 0.180, 0.963 ± 0.067, 0.850 ± 0.085, 0.566 ± 0.058, 0.549 ± 0.056 and 0.377 ± 0.047, respectively (r=-0.945, P<0.001); those of Ptch-1 were 1.688 ± 0.088, 1.466 ± 0.061, 1.170 ± 0.065, 1.042 ± 0.064, 0.648 ± 0.057 and 0.482 ± 0.074, respectively (r=-0.985, P<0.001).

CONCLUSIONHp-LPS can decrease the related protein expression of Shh signaling pathway, which indicates that Hp may interfere with the function of Shh signaling pathway in gastric mucosa via the effect of its LPS.

Cells, Cultured ; Epithelial Cells ; drug effects ; Gastric Mucosa ; cytology ; Hedgehog Proteins ; metabolism ; Humans ; Lipopolysaccharides ; administration & dosage ; pharmacology ; Patched Receptors ; Patched-1 Receptor ; Receptors, Cell Surface ; metabolism ; Signal Transduction ; Transcription Factors ; metabolism ; Zinc Finger Protein GLI1

OBJECTIVETo explore toxicokinetics of tetramethylene disulphotetramine (TETS) in rabbit and the effects on toxicokinetics of TETS after activated charcoal by gavage.

METHODSEight rabbits were exposed through gavage and vein respectively, the blood samples were collected from the center artery in ear of rabbit at an arranged time. Four rabbits were exposed after being intubated into urethra and common bile duct. The samples of bile and urine were collected at arranged times. After being exposed by gavage, activated charcoal (1 g/kg) was administrated in the activated charcoal group and the distilled water (1 g/kg) administrated to the controls. The samples of blood were collected from the center artery in ear of rabbit at arranged times. The contents of TETS in samples were determined by GC/NPD method. Analysed by the 3p87 soft, toxicokinetics parameters of TETS were acquired.

RESULTSTETS was eliminated very slowly in rabbit. The plasma half time in elimination phase (Tke1/2) of TETS was 56.9 hours in vein exposure group and 262.5 hours in oral exposure group respectively. The plasma clearance (CL) of it was only 15.4 ml.kg(-1).h(-1) in oral exposure group and 24.1 ml.kg(-1).h(-1) in vein exposure group. TETS was eliminated from urine in rabbit. The eliminated amount of it from urine was more 5 times than from bile. All parameters of toxicokinetics of TETS were significantly different between the activated charcoal group and the control. Compared to the control, Tke1/2 of TETS in the activated charcoal group was equal to 55%, CL was increased over 3-fold, area under the curve was equal to 30%.

CONCLUSIONTETS was a poison eliminated very slowly in body. The eliminated amount of it from urine was more than from bile. The excretion of TETS could be quickened after activated charcoal by gavage.

Animals ; Antidotes ; administration & dosage ; Bile ; metabolism ; Bridged-Ring Compounds ; blood ; pharmacokinetics ; urine ; Charcoal ; administration & dosage ; Female ; Male ; Metabolic Clearance Rate ; drug effects ; Rabbits

To investigate the relationship between the structures of methylhesperetin-7-alkyl ether analogues and their anti-inflammatory activities, nine new compounds, methyl-hesperetin (2), methylhesperetin-7-ethyl ether (3), 7-n-butyl ether (4), 7-n-hexyl ether (5), 7-n-octyl ether (6), 7-n-decyl ether (7), 7-n-dodecyl ether (8), 7-n-tetradecyl ether (9) and 7-n-hexadecyl ether (10), were synthesized with the lead compound of methylhesperidin (1). Their structures were confirmed by UV, 1H NMR, MS and HR-MS spectral data. The in vivo antiinflammatory activities of these compounds were tested on mouse paw edema induced by Freund's complete adjuvant (FCA) and mouse capillary permeability induced by acetic acid with po dose of 300 mg x kg(-1) x d(-1). The result indicated that the anti-inflammatory activities of the synthetic compounds increased firstly and then decreased with the elongating of the length of alkyl chain. After 25-day oral administration of compounds 6, 7 and 8, the inhibitory rates on mouse paw edema of adjuvant arthritis (AA) were 31.9%, 38.5%, 39.1%, respectively. They showed the concentrations of COX-2 in serum of AA mice respectively were 79.3, 75.4, 73.9 ng x L(-1) and the concentrations of PGE2 were in correspondence with 275.4, 258.9, 242.6 ng x L(-1). The inhibitory rates of compounds 6 and 7 on mouse capillary permeability induced by acetic acid were, respectively, 42.4% and 41.5% after 5-day oral administration. Compared with the lead compound of methylhesperidin, the anti-inflammatory activities of compounds 6, 7 and 8 were increased and showed an effective inhibition on the symptom of adjuvant arthritis and capillary permeability in mice.
Acetic Acid ; Animals ; Anti-Inflammatory Agents ; chemical synthesis ; chemistry ; pharmacology ; Arthritis, Experimental ; blood ; chemically induced ; drug therapy ; metabolism ; Capillary Permeability ; drug effects ; Cyclooxygenase 2 ; blood ; Dinoprostone ; metabolism ; Edema ; chemically induced ; drug therapy ; Female ; Freund's Adjuvant ; Hesperidin ; analogs & derivatives ; chemical synthesis ; chemistry ; pharmacology ; Male ; Mice ; Molecular Structure ; Random Allocation

OBJECTIVETo investigate the seasonal characteristics and the sources of elements and ions with different sizes in the aerosols in Beijing.

METHODSSamples of particulate matters (PM2.5), PM10, and total suspended particle (TSP) aerosols were collected simultaneously in Beijing from July 2001 to April 2003. The aerosol was chemically characterized by measuring 23 elements and 18 water-soluble ions by inductively coupled plasma-atomic emission spectroscopy (ICP-AES) and ion chromatography (IC), respectively.

RESULTSThe samples were divided into four categories: spring non-dust, spring dust, summer dust, and winter dust. TSP, PM10, and PM2.5 were most abundant in the spring dust, and the least in summer dust. The average mass ratios of PM > 10, PM2.5-10, and PM2.5 to TSP confirmed that in the spring dust both the large coarse (PM > 10) and fine particles (PM2.5) contributed significantly in summer PM2.5, PM2.5-10, and PM > 10 contributed similar fractions to TSP, and in winter much PM2.5. The seasonal variation characteristics of the elements and ions were used to divide them into four groups: crustal, pollutant, mixed, and secondary. The highest levels of crustal elements, such as Al, Fe, and Ca, were found in the dust season, the highest levels of pollutant elements and ions, such as As, F-, and Cl-, were observed in winter, and the highest levels of secondary ions (SO4(2-), NO3-, and NH4+) were seen both in summer and in winter. The mixed group (Eu, Ni, and Cu) showed the characteristics of both crustal and pollutant elements. The mineral aerosol from outside Beijing contributed more than that from the local part in all the reasons but summer, estimated using a newly developed element tracer technique.

Aerosols ; China ; Chromatography, Ion Exchange ; Environmental Monitoring ; Particle Size ; Particulate Matter ; analysis ; chemistry ; Seasons ; Spectrophotometry, Atomic

OBJECTIVETo investigate the predisposing role of HLA-DRB1, DQB1 genes in pemphigus vulgaris (PV).

METHODSPolymerase chain reaction-specific sequence primers method was used to type HLA-DRB1, DQB1 subregion in the patients with PV of Han nationality from Jiangsu and Anhui provinces and matched control subjects.

RESULTSDR4, DRB1*14(*1401,*1404,*1405) gene frequencies in PV patients were significantly higher than those in controls (Pc<0.05 and Pc<0.01 respectively). DQB1*0302, DQB1*0503 gene frequencies were significantly higher in PV patients (Pc<0.05). Further typing of DR4 positive subjects revealed that the gene frequencies of DRB1*0406, *0403 were significantly increased in PV patients as compared with controls (Pc<0.05). The haplotype frequencies of HLA-DRB1*04, DQB1*0302 and HLA-DRB1*14, DQB1*0503 in PV patients were significantly higher than those in controls (P<0.05).

CONCLUSIONThe results suggest that the combination of HLA-DRB1*4, DQB1*0302 and HLA-DRB1*14, DQB1*0503 forms putative susceptible haplotypes for PV patients in Chinese Hans.

Adult ; Aged ; Aged, 80 and over ; China ; DNA ; genetics ; Female ; Gene Frequency ; Genotype ; HLA-DQ Antigens ; genetics ; HLA-DQ beta-Chains ; HLA-DR Antigens ; genetics ; HLA-DRB1 Chains ; Humans ; Male ; Middle Aged ; Pemphigus ; genetics