Objective Through the comparative study of the acute toxic effects of PM2.5 in nickel-contaminated area in rats to explore the possible mechanism of acute toxicity of PM2.5.Methods A nickel-contaminated area and a control area were selected,the air quality of the two areas was monitored and the concentration of nickel in the collected PM2.5 was determined. Forty two male Wistar rats(SPF Grade)were randomly divided into three groups,including one saline control group and two experimental groups,the nickel-polluted group and the non-polluted group,in each.There were three subgroups.PM2.5 were administered to rats by intratraeheal instillation at doses of 1.6 mg/kg,8.0 mg/kg and 40.0 mg/kg respectively.The rats were sacrificed 24 hours after treatment and the brochoalveolar tavage fluid(BALF)were collected,the phagocytic function of alveola macrophages of rats were tested.Results There was no significant difference between the level of environmental quality in the two areas,the concentration of Ni in PM2.5 in the nickel-polluted area was 48.75 times of that in the non-polluted control area.The phagocytic function of alveola macrophages of rats in the experimental groups decreased significantly(P

Objective To investigate the potential relationship between initial 131Ⅰ uptake by lung metastases from differentiated thyroid cancer (DTC) and treatment outcomes. Methods From 1997 to 2009, 41 patients with DTC lung metastases were treated in the authors' department. 131Ⅰ whole body scan (WBS), serum Tg levels and other imaging results were analyzed to evaluate the therapeutic effects. Complete response (CR) or partial response (PR) was considered to be effective. The x2 test and correlation analysis were performed using SPSS 11.5 software package. Results 131 Ⅰ treatment was effective in 63% (26/41) patients with DTC lung metastases, CR in 8 patients and PR in 18 patients. In other 37% ( 15/41 ) patients, 131Ⅰ treatment was ineffective, including one case died of distant metastases. Patients with initial presence of 131Ⅰ lung uptake had higher effective rate than those with 131Ⅰ lung uptake during the second or later 131Ⅰ treatment (76% (22/29)vs33% (4/12),x2 =4.911, P=0.027). Also, significantly higher effective rate was found in patients with lung metastases alone than those with extra-pulmonary metastases (75% (24/32) vs 22% (2/9), x2 = 6. 312, P =0.012). However, the effective rate in patients with diffuse metastases was not significantly different from that in patients with focal metastases (67% (12/18)vs 61% ( 14/23), x2 =0. 146, P=0.702). The positive rate of initial 131Ⅰ uptake by lung metastases was higher in patients with total thyroidectomy than those with partial thyroidectomy (83% (24/29) vs 42% (5/12) ). Those positive rates in patients with papilary DTC and patients with follicular DTC were 72% (23/32) and 6/9, respectively. The surgical mode was correlated with the initial 131Ⅰ uptake by lung metastases (r = 0.411, P ＜ 0.05), but no correlation was found between the histological type and the initial 131Ⅰ uptake by lung metastases ( r = 0. 047, P ＞ 0.05 ). Conclusion Initial uptake of 131 Ⅰ by lung metastases alone is a favorable prognostic factor for DTC patients treated by131Ⅰ, and total thyroidectomy may be beneficial for initial 131Ⅰ uptake by lung metastases.

Cold Temperature ; Dinoprost ; analogs & derivatives ; urine ; Dust ; Humans ; Interleukin-6 ; urine ; Thromboxane B2 ; analogs & derivatives ; urine ; Weather

Animals ; Cold Temperature ; adverse effects ; Heart ; physiopathology ; Inflammation ; physiopathology ; Myocardium ; metabolism ; Oxidative Stress ; Particulate Matter ; adverse effects ; Rats

Animals ; Blood Pressure ; Lymphatic Vessels ; physiopathology ; Male ; Norepinephrine ; metabolism ; Rats ; Rats, Wistar ; Shock, Hemorrhagic ; metabolism ; physiopathology

Lu Dangshen, a traditional authentic medicinal material of Codonopsis Radix is mainly produced in Shangdang (Changzhi) area of Shanxi Province. Baitiao Dangshen is mainly produced in Gansu Province. Codonopsis Radix contains many kinds of components such as phenylpropanoids, polyalkynes, alkaloids, terpenes, fatty acids, flavonoids, and so on. At present, the effect of producing areas on its chemical compositions has not been systematically studied. This study analyzed the differences of metabolites among Codonopsis pilosula from different producing areas by UPLC-HRMS. PCA, OPLS-DA coupled with Thermo mzcloud online and local databases were used to compare the overall differences of metabolites among Codonopsis pilosula from different producing areas, and the chemical constituents were identified to further screen and find out the different metabolites and analyze the metabolic pathways by information retrieval in HMDB, PubChem, Chemspider and KEGG databases. The results showed that 72 differential metabolites were identified in this study. There were 15 kinds of up-regulated and 57 kinds of down-regulated metabolites of Lu Dangshen compared with Baitiao Dangshen. The top 30 metabolic pathways were analyzed by KEGG enrichment, and the most important metabolic pathways were phenylpropanoid biosynthesis, which was demonstrated that phenylpropanoid biosynthesis pathway and related intermediate metabolites could be used as the characteristics of distinguishing Lu Dangshen from different habitats of Codonopsis pilosula. The present study provided a basis for analyzing the influence of producing areas on the chemical components of Codonopsis pilosula and reasonably evaluating the quality of Codonopsis Radix, and also provided a new idea for expounding the authenticity of Lu Dangshen.

OBJECTIVETo explore the effect of polycyclic aromatic hydrocarbons on the neurobehavioral function of coke oven workers.

METHODS200 healthy adult male coke oven workers were selected from a coke plant of a state-owned steel enterprise in Taiyuan City. 88 controls occupationally unexposed to polycyclic aromatic hydrocarbons (PAHs) were selected from the same enterprise. All the subjects participated in this investigation voluntarily in their consent. Concentration of B(a)P in the working environment was monitored by High Performance Liquid Chromatography (HPLC). Urine samples were sampled immediately after working shifts. The level of urinary 1-hydroxypyrene was determined by HPLC. General information of workers correlated with the investigation was collected in a questionnaire according to the same criteria by well-trained investigators. Neurobehavioral core test battery (NCTB) recommended WHO was performed on coke oven workers and controls to test the neurobehavioral changes and the mood state.

RESULTSthe concentration of B(a)P at oven bottom,oven side and oven top were 0.0195 microg/m3, 0.186 microg/m3 and 1.624 microg/m3 respectively, that at oven side and oven top being higher than the one stipulated by the occupational hygiene criterion. Urinary 1-hydroxypyrene was significantly different between the exposure group (3.42 +/- 0.98 micromol/mol creatinine) and control group (2.75 +/- 1.09 micromol/mol creatinine). No significant differences were found between exposure group and control group of age, working years, smoking, drinking and unhealthy food consumption; however, compared to the controls, the scores of total digital span, the forward digital span, and right dotting in the coke oven workers were lower, but that of total dotting was higher, with a statistical significance. According to urinary 1-hydroxypyrene concentration, all the subjects were divided into three groups. (<3.10 micromol/mol creatinine, 3.10 micromol/mol creatinine, >3.87 micromol/mol creatinine). Significant differences of the total digital span, the forward digital span, backward digital span, digit symbol and Benton visual retentions existed in different urinary 1-hydroxypyrene concentration groups and showed a dose-response tendency. Results of multiple stepwise regression analysis and correlation analysis showed that the level of urinary 1-hydroxypyrene affected memory and perception of coke oven workers and negative correlations between the level of urinary 1-hydroxypyrene and changes in neurobehavioral function were found.

CONCLUSIONPAHs mainly causes decrease of memory and perception in coke oven workers.

Adult ; Air Pollutants, Occupational ; analysis ; Coke ; Humans ; Male ; Memory ; Neuropsychological Tests ; Occupational Exposure ; Polycyclic Aromatic Hydrocarbons ; urine

AIMTo observe the effect of mesenteric lymph duct ligation on free radical and inflammatory mediator of myocardium with severe hemorrhagic shock in rats at different period, and explore the effect of intestinal lymphatic pathway on myocardium injury pathogenesis in shock rats.

METHODS78 male Wistar rats were divided into the sham group, shock group and ligation group. The model of serious hemorrhagic shock was established in shock group, ligation group, and mesenteric lymph was blocked by ligating mesenteric lymph duct in ligation group after resuscitate. All rats were executed and taken out heart making for homogenate of 10 percent to determine the MDA, SOD, tumor necrosis factor-alpha (TNFalpha), interleukin-6 (IL-6), myeloperoxidase (MPO), NO and NOS at after shock 90 min, after transfusion and resuscitate 0 h, 1 h, 3 h, 6 h, 12 h and 24 h etc. different times, and the expression of inducible nitric oxide synthase (iNOS) mRNA in myocardium was detected by RT-PCR.

RESULTSThe contents of MDA, TNFalpha, IL-6, MPO, NO, NOS and iNOS expression in myocardium of shock group were rising after transfusion and resuscitate, and that was higher level at 3 h to 12 h, and that was significantly higher than sham group, the activity of SOD was significantly lower than sham group. The contents of MDA, TNFalpha, IL-6, MPO, NO, NOS and iNOS expression in myocardium of ligation group were significantly lower than that of shock group at sameness points, and the SOD activity was higher.

CONCLUSIONThe mesenteric lymph duct ligation and blocking mesenteric lymph could reduce the PMN detaining, decrease the discharging of TNFa and IL-6, reduce the NO and expression of iNOS mRNA, and reduce the releasing of free radical and consuming of SOD.

Animals ; Free Radicals ; metabolism ; Inflammation Mediators ; metabolism ; Interleukin-6 ; metabolism ; Lymphatic Vessels ; metabolism ; Male ; Mesentery ; metabolism ; Myocardium ; metabolism ; pathology ; Neutrophils ; metabolism ; Nitric Oxide ; metabolism ; Nitric Oxide Synthase Type II ; metabolism ; Peroxidase ; metabolism ; Rats ; Rats, Wistar ; Shock, Hemorrhagic ; metabolism ; pathology ; Superoxide Dismutase ; metabolism ; Tumor Necrosis Factor-alpha ; metabolism

OBJECTIVETo discover BCR-ABL tyrosine kinase inhibitors through structure based virtual screening.

METHODSDocking screening against the distinctive inactive conformation of the catalytic domain of BCR-ABL tyrosine kinase was performed on 3D database. The MTT assay was performed to assess the viability of the tumor cells treated with selected compounds. The amount and kinase activity of BCR-ABL protein were detected in the presence of compounds by Western blot analysis and immunoprecipitation.

RESULTSFrom the top 1,000 compounds with the best DOCK energy score, 15 compounds were selected for biological assay. Eight out of 15 compounds showed notable inhibitory activity against Ph+ human K562 cells with IC50 values ranging from 10 to 200 micromol/L. In cell-based assays of ABL tyrosine phosphorylation, the ability of two kinds of novel, structurally diverse, lead compounds to inhibit ABL kinase activity was observed. However, no significant differences in the amount of BCR-ABL protein were noted on the ABL immunoblot in the presence of these lead compounds.

CONCLUSIONSTwo promising lead compounds were discovered to inhibit BCR-ABL tyrosine kinase activity. Virtual screening technique has been proven to narrow down the size of screening compound libraries to the most prospective drug candidates with high success rates.

Computer Simulation ; Drug Evaluation, Preclinical ; Enzyme Inhibitors ; chemical synthesis ; Fusion Proteins, bcr-abl ; Humans ; K562 Cells ; Models, Molecular ; Molecular Conformation ; Phosphorylation ; Protein-Tyrosine Kinases ; antagonists & inhibitors ; chemistry ; genetics

AIMTo synthesize novel derivatives of hydroxylbenzenedisulfonanilide with high insecticidal activity against the Fasciola hepatica.

METHODSo-(m-, p-) Chlorphenol were used to synthesize the title compounds by sulphonation and nucleiphilic-substitution reaction. The uncoupling activity (insecticidal activity) of these compounds were tested by determining the influence on mitochondrial respiration control ratio (RCR) and the variation of inorganic phosphate in oxidative phosphorylation (delta Pi).

RESULTSCompounds 1-14 are new compounds. The structures of the compounds were determined by IR, HNMR and elemental analysis. Most new compounds have relatively high uncoupling activities, especially compounds 3, 5, 6 and 9.

CONCLUSIONCompounds 3, 5, 6 and 9 will become novel fasciolicides and are worth further studying.

Anilides ; chemical synthesis ; chemistry ; pharmacology ; Animals ; Anthelmintics ; chemical synthesis ; chemistry ; pharmacology ; Fasciola hepatica ; drug effects ; Mitochondria, Liver ; physiology ; Molecular Structure ; Oxygen Consumption ; drug effects ; Sulfonamides ; chemical synthesis ; chemistry ; pharmacology