Combining the structural features of picotamide and linotroban, a series of N,N'-bis-(halogenophenyl)-4-methoxybenzene-1, 3-disulfonamides were designed and synthesized on the basic principles of drug design. The structures of target compounds were confirmed by IR, 1H NMR and HR-MS, and the in vitro antiplatelet aggregation activity was evaluated by Born turbidimetric method with adenosine diphosphate (ADP) as the platelet aggregation inducers. The assay results showed that twelve compounds (4b, 4f, 4l, 5b, 5d-5g, 5j, 5k, 5m and 5n) were found to have superior anti-platelet aggregation activities than the positive drug picotamide. The preliminary structure-activity relationship (SAR) has been explored.
Adenosine Diphosphate ; Drug Design ; Phthalic Acids ; Platelet Aggregation ; Platelet Aggregation Inhibitors ; chemical synthesis ; chemistry ; Structure-Activity Relationship ; Sulfonamides ; chemical synthesis ; chemistry

Antigens ; analysis ; Cervical Intraepithelial Neoplasia ; metabolism ; Citric Acid ; Cyclin-Dependent Kinase Inhibitor p21 ; analysis ; Edetic Acid ; Formaldehyde ; Hot Temperature ; Humans ; Hydrogen-Ion Concentration ; Immunohistochemistry ; Intestinal Mucosa ; immunology ; Ki-67 Antigen ; analysis ; Microwaves ; Palatine Tonsil ; metabolism ; Proto-Oncogene Proteins c-bcl-6 ; analysis

Objective:The aim of this study was to detect the P2X7 receptor (P2X7R) protein expression in pancreatic carcinoma and to analyze its association with clinicopathology features of pancreatic carcinoma.And furtherly to explore the effects and underlying mechanisms of P2X7R on invasion and migration of PANC-1 cell line.Methods:P2X7R expression was determined by immunohistochemistry in specimens of primary cancer and adjacent noncancerous tissues respectively,and analyzed the relationship between P2X7R expression and clinicopathology features of pancreatic carcinoma.The transwell assay and wound healing assay were used for investigating cell invasion and migration ability of PANC-1,and western blotting was performed to measure the expresions of MMP2 and MMP9.Results:P2X7R protein was highly expressed in both PANC-1 cell line and tumor tissue,and associated positively with the histological differentiation and lymph node staging.The active P2X7R could increase the cell migration and invasion ability of PANC-1 cell line through up-regulated MMP2 and MMP9.Conclusions:The overexpression of P2X7R plays crucial roles in the migration and invasion of pancreatic carcinoma,and may represent a novel molecular target in pancreatic carcinoma therapy.

Female ; Humans ; Infant, Newborn ; Maple Syrup Urine Disease ; diagnosis ; therapy

Objective: To learn the health literacy level and its influencing factors among junior high school students in Jiaxing, so as to provide basis for health promotion of adolescents. Methods: The junior high school students who had been studying and living in Jiaxing for more than six months were selected by multistage cluster random sampling method. A questionnaire survey was conducted to collect general information and health literacy level (including basic knowledge and concept, healthy lifestyle and behaviors, and basic skills) of these selected students. The multivariate logistic regression model was used to analyze the influencing factors for health literacy. Results : Of 1 773 questionnaires collected, 1 738 were valid, accounting for 98.03%. The level of health literacy in the junior high school students in Jiaxing was 22.84% ( 95%CI: 20.87%-24.82% ), The levels of basic knowledge and concept, healthy lifestyle and behaviors, and basic skills were 55.29% ( 95%CI: 52.95%-57.63% ), 21.75% ( 95%CI: 19.81%-23.69% ), 53.05% ( 95%CI: 50.70%-55.40%), respectively. Multivariate logistic regression analysis showed that the second grade and above ( OR: 1.609-1.835, 95%CI: 1.195-2.459 ), mother's educational level of technical secondary school/senior high school and above ( OR: 1.965-1.976, 95%CI: 1.276-3.357 ), and self-rated academic achievement of medium and above ( OR: 1.881-2.441, 95%CI: 1.359-3.335 ) were the promoting factors for health literacy level of junior high school students; self rated health status as unhealthy ( OR=0.254, 95%CI: 0.089-0.721 ) was an obstructive factor. Conclusions The health literacy level of the junior high school students in Jiaxing was 22.84%. The level of healthy lifestyle and behaviors was the lowest in three aspects. Grade, mother's educational level, self-rated academic performance and self-rated health status may have impacts on health literacy level of junior high school students.

Objective: To observe the clinical efficacy of spleen-invigorating and qi-benefiting pediatric massage (tuina) for treating recurrent respiratory tract infection in children with cerebral palsy due to qi deficiency of spleen and lung. Methods: A total of 70 children with cerebral palsy who suffered from recurrent respiratory tract infection due to qi deficiency of spleen and lung were randomized into an observation group and a control group by the random number table method, with 35 cases in each group. Both groups were treated with conventional rehabilitation training, while the observation group was given additional spleen-invigorating and qi-benefiting pediatric massage, and the control group additionally took oral Yu Ping Feng granule. The clinical efficacy was evaluated by the total effective rate, traditional Chinese medicine (TCM) symptom score, and serum levels of immunoglobulin (Ig) A, IgM and IgG. Results: The difference in total effective rate between the two groups after treatment was statistically significant (P<0.05). After treatment, the TCM symptom scores in both groups decreased to varying degrees than those before treatment, and the intra-group differences were statistically significant (all P<0.01); the differences in the scores of various TCM symptoms between the two groups were statistically significant (all P<0.05). After treatment, the levels of IgA, IgM and IgG of the children in both groups increased to varying degrees, and the intra-group differences were statistically significant (all P<0.05). The between-group differences in the IgA, IgM and IgG levels after treatment were statistically significant (all P<0.05). Conclusion: Spleen-invigorating and qi-benefiting pediatric massage can effectively treat recurrent respiratory tract infection due to qi deficiency of spleen and lung in children with cerebral palsy, relieve the clinical symptoms and improve immune function, and thus is worthy of clinical promotion and application.

Objective To summary the nursing cooperation experience during interventional radiology treatment for patients with haemorrhage after pancreatoduodenectomy in order to enhance the quality of care.Methods Eighteen patients with haemorrhage after pancreaticoduodenecomy treated with interventional radiology. The nursing cooperation during interventional radiology treatment for pancreatoduodenectomy haemorrhage was summarized. Results Eighteen patients performed 29 interventional procedures. Haemorrhage was ceased in 16 cases after the last time of interventional radiology treatment. In addition, haemorrhage did not occurred in other 2 cases after treated with surgery. Conclusions The patients' conditions of haemorrhage post pancreaticoduodenecomy were complicated, so the nurses in catheter lab should prepare carefully, strengthen the interventional knowledge and do the predictable nursing care.

OBJECTIVETo explore the protection of high intensity microwave radiation on hypothalamo-pituitary-adrenal axis (HPAA) activity and hippocampal CA1 structure in rats and the protectiveeffect of Qindan Granule (QG) on radiation injured rats.

METHODSTotally 48 Wistar rats were randomlydivided into 8 groups, i.e., the normal control group, post-radiation day 1, 7, and 10 groups, 7 and 10days prevention groups, day 7 and 10 treatment groups, 6 in each group. Rats in prevention groups wererespectively administered with QG liquid (1 mL/100 g, 4. 75 g crude drugs) for 7 days and 10 days bygastrogavage and then microwave radiation. Then preventive effect for radiation injury was statisticallycalculated with the normal control group and the post-radiation day 1 group. Rats in treatment groupswere firstly irradiated, and then administered with QG liquid (1 mL/100 g, 4.75 g crude drugs). Finally preventive effect for radiation injury was statistically calculated with the normal control group, post-radiation day 7 and 10 groups. Contents of corticotrophin releasing hormone (CRH), beta endorphin (beta-EP), adrenocorticotropic hormone (ACTH), and heat shock protein 70 (HSP70) were detected. Morphological changes and structure of hippocampal CA1 region were observed under light microscope.

RESULTSCompared with the normal control group, contents of CRH and beta-EP significantly decreased in each radiation group. Serum contents of ACTH and beta-EP significantly increased in post-radiation day 1 and 7 groups (P < 0.05). Compared with radiation groups, beta-EP content in serum and pituitary significantly increased, and serum ACTH content significantly decreased in prevention groups (P < 0.05). Pituitary contents of CRH and beta-EP significantly increased in prevention groups. Serum contents of ACTH, beta-EP, and HSP70 were significantly lower in day 7 treatment group than post-radiation day 7 group (P < 0.05). Morphological results showed that pyramidal neurons in the hippocampal CA1 region arranged in disorder, with swollen cells, shrunken and condensed nucleus, dark dyeing cytoplasm, unclear structure. Vessels in partial regions were dilated with static blood; tissues were swollen and sparse. In prevention and treatment groups pathological damage of hippocampal CA1 region was obviously attenuated; neurons were arranged more regularly; swollen, pycnotic, or deleted neuron number were decreased; vascular dilatation and congestion was lessened.

CONCLUSIONQG could affect HPAA function and activity of high intensity microwave radiated rats, showing certain preventive and therapeutic effects of microwave radiated rats by adjusting synthesis and release of partial bioactive peptides and hormones in HPAA, improving pathological injury in hippocampal CA1 region.

Adrenocorticotropic Hormone ; blood ; Animals ; CA1 Region, Hippocampal ; drug effects ; pathology ; radiation effects ; Corticotropin-Releasing Hormone ; metabolism ; Drugs, Chinese Herbal ; pharmacology ; HSP70 Heat-Shock Proteins ; blood ; Hypothalamo-Hypophyseal System ; drug effects ; radiation effects ; Microwaves ; adverse effects ; Pituitary-Adrenal System ; drug effects ; radiation effects ; Random Allocation ; Rats ; Rats, Wistar ; beta-Endorphin ; blood ; metabolism

Objective To study the national surveillance results and learn the current situation of iodized salt consumption at household level in 2008, and to find out the remaining problems and to provide scientific basis for developing control strategies against iedine deficiency disorders. Methods In 2008, in accordance with the requirements of the "National Iodine Deficiency Disorders Surveillance Program (Trial)", the surveillance was conducted at county level in 31 provinces and at division level in Xinjiang Production and Construction Corps. In each county 9 townships were randomly selected according to their sub-area positions of east, west, south, north and center;4 villages were randomly sampled in each chosen township;8 households were randomly selected in each chosen village. In every county with 9 or less townships, 1 township was randomly selected respectively in the east, west, south,north and center sub-areas;4 villages were randomly sampled in each chosen township;15 households were randomly selected in each chosen village. Edible salt from these households was collected. Iodized salt coverage rate, proportion of qualified iodized salt and consumption rate of the qualified iodized salt of the households in each province were counted and analyzed. Iodized salt was determined by direct titration;the salt samples from Sichuan and other enhanced salt were detected by arbitration. Results Totally 2817 counties (districts, cities, banners) and 14 divisions of the Xinjiang Production and Construction Corps reported the monitoring results, monitoring coverage reached 99.96%(2831/2832). Mean of iodine content was 31.51 mg/kg.Sixteen provinces had a variation coefficient of iodine content for more than 20%. A total of 826 968 households were tested of their edible salt, in which iodized salt 798 725 copies, non-iodized salt 28 243 copies, and unqualified iodized salt 20 270 copies. Weighted by population,at national level, the coverage rate of iodized salt was 97.48%, qualified rate of iodized salt 97.16%, and consumption rate of qualified iodized salt was 94.79%.Twenty seven provinces (autonomous regions and municipalities) and Xinjiang Production and Construction Corps had a qualified iodized salt coverage rate of above or equal 90.00%. Tibet, Hainan, Xinjiang and Tianjin provinces (regions) had a qualified iodized salt coverage rate lower than 90.00%. Further, 2487 counties had the rate high or equal 90.00% accounting for 87.82% (2487/2831) of complementing monitoring counties. One hundred and four counties and 1 division of the Xinjiang Production and Construction Corps had the coverage rate of iodized salt below 80.00%. Conclusions Sixteen provinces(autonomous regions and municipalities) have relatively a high degree of variation coefficient in salt iodine content. The quality of iodized salt needs to be improved. The coverage rate of iodized salt and the qualified iodized salt at national level are both above or equal 90.00%. However, the non-iodized salt problem is still serious and have a relatively lower coverage of iodized salt in Tibet, Hainan and Xinjiang.

Objective To understand the current level of iodized salt coverage in areas with intensified monitoring measure in China in 2008. Methods In accordance with the "National Iodine Deficiency Disorders Surveillance Program (Trial)" of Ministry of Health issued in 2007, the selected key counties (cities, districts and banner) were divided into 5 sub-areas, 1 non-iodine townships(towns, street offices) was sampled randomly in each sub-area, 4 administrative villages (neighborhood committees) were sampled from each selected township;15households salt samples in each selected village were randomly collected. All salt samples were detected by semiquantitative kit at first. The salt samples that can not be determined by the kit were tested by direct titration and the arbitration act (GB/T 13025.7-1999) detection. Iodized salt determination criteria: reagent color change in semiquantitative test kit or iodine content ≥ 5 mg/kg were identified as iodized salt. Otherwise, the salt samples were identified as non-iodized salt. Results All the provinces(autonomous regions, municipalities) except Tibet in China had conducted a specific survey on iodized salt coverage in non-iodized salt high-risk areas, which revealed that the national coverage rate of iodized salt was 93.01%(130 928/140 770). At the provincial level, twenty provinces and the Xinjiang Production and Construction Corp had a iodized salt coverage over 90%, while the other six provinces (Beijing, Xinjiang, Zhejiang, Fujian, Tianjin and Jiangxi) between 80% - ＜ 90% and the rest four provinces,such as Guangxi, Qinghai, Guangdong and Hainan, lower than 80%. At the county level, 64.57%(277/429) of all the surveillance counties had a iodized salt coverage over 95% while 10.02%(43/429) lower than 80%. Among all the six types of areas where specific survey were conducted, areas with incomplete iodized salt distribution network and areas with crude salt production had a iodized salt coverage lower than 90%, 81.74%(4978/6090) and 86.53%(17 098/19 759), respectively. In raw salt production area, there were 10 out of 21 provinces with iodized salt coverage rate below 90%, it consisted of 47.6%(10/21) of the total monitoring provinces in the same type areas.There were 8 out of 16 provinces with iodized salt coverage rate lower than 90% in the areas with faultiness iodized salt network, it consisted of 50.0%(8/16) of the sampling provinces in the same type area. Conclusions Most provinces(21) in China have a relatively high iodized salt coverage at household level during this specific survey.Areas with incomplete iodized salt distribution network and crude salt production are the most affected areas by noniodized salt. Aiming at the high-risk non-iodized salt areas discovered during this survey, corresponding intervention measures should be implemented with joint efforts from sectors concerned.