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Healthy Beagle dogs were administrated with batroxobin by intravenous infusion at high, medium and low doses. The study of pharmacodynamics and pharmacokinetics was intended to clarify the relevance of them and provided strong evidence for clinical use of batroxobin. The blood samples were collected after injection based on the time schedule and samples were tested by ELISA method to get the concentration of batroxobin. At the same time, changes of prothrombin time (PT), thrombin time (TT), activated partial thromboplastin time (APTT), fibrinogen (Fib) and D-dimmer were tested. The results showed that the concentration of D-D increased significantly after administration compared with that of before administration. The main pharmacokinetic parameters were as follows: t1/2 were (2.27 +/- 0.42) h, (10.65 +/- 2.19) h and (11.01 +/- 3.51) h; C(max) were (11.9 +/- 1.72) ng x mL(-1), (154.53 +/- 12.38) ng x mL(-1) and (172.14 +/- 47.33) ng x mL(-1); AUC(last) were (29.38 +/- 3.69) ng xh x mL(-1), (148.43 +/- 72.85) ng x h x mL(-1) and (599.22 +/- 359.61) ng x h x mL(-1). The elimination of batroxobin was found to be in accord with linear kinetics characteristics. The results of pharmacodynamics showed that D-dimmer level increased significantly after the administration of batroxobin, which was similar with the changes of batroxobin plasma concentration. Simultaneously, Fib concentrations in Beagle dog blood decreased significantly after the iv administration of batroxobin, while recovered to base level after 48 hours. PT, TT and APTT significantly became longer after administration, which returned to normal level after 48 hours. Especially, the D-dimmer levels and the batroxobin concentration in plasma after intravenous infusion of the drug were synchronized in Beagle dogs. Changes between PD/PK results had obvious correlation, and the D-dimmer levels in plasma can be one of the important monitoring indicators of batroxobin in thrombolytic medication.

This paper is to report the study of the metabolism of forscolin in plasma and liver microsomes for guiding clinical therapy. Forscolin was quantified by HPLC-MS/MS. The metabolic stability of forscolin in rat, Beagle dog, monkey and human plasma and liver microsomes, mediated enzymes of forscolin and its inhibition on cytochrome P450 isoforms in human liver microsomes were studied. Results showed that forscolin was not metabolized in plasma of the four species but metabolized in liver microsomes of the four species. The t1/2 of forscolin in rat, Beagle dog, monkey and human liver microsomes were (52.0 +/- 15.0), (51.2 +/- 5.9), (6.0 +/- 0.2) and (11.9 +/- 1.8) min; CL(int) were (75.6 +/- 18.7), (60.9 +/- 6.8), (513.8 +/- 14.3) and (176.2 +/- 25.6) mL x min(-1) x kg(-1); CL were (34.8 +/- 4.5), (23.3 +/- 1.0), (40.3 +/- 0.5) and (17.9 +/- 0.3) mL x min(-1) x kg(-1), respectively. Forscolin was metabolized by CYP3A4 in human liver microsomes. There was definite inhibition on CYP3A4 at the concentrations of forscolin between 0.1 ng x mL(-1) and 5 microg x mL(-1). Therefore, forscolin is rapidly excreted from liver microsomes. Attention should be paid to the drug interaction when forscolin was used along with other drugs metabolized by CYP3A4 in clinics.

Objective: To explore the iodine level in the environment and the iodine status among the general population as well as the prevalence of thyroid nodules in Hangzhou city. Relationship between the prevalence of thyroid nodules and the policy of universal salt iodization in Hangzhou was also analyzed., Methods: Questionnaire, a 3-day weighed dietary record method, and 3 days' 24-hour dietary recall method were used to understand the iodine nutrition status and dietary intake of iodine among the general population in the city. Drinking water, edible salt and morning urine were collected to determine iodine content. All objects under survey underwent the thyroid B ultrasonic examination. Statistical analysis was done by SPSS 13.0 and SAS 9.1., Results: (1) In total, 12 620 effective questionnaires were available, with 221 water samples, 12 730 urine samples, and 3593 salt samples collected. 12 515 objects underwent B ultrasonic examination, and 1848 received dietary investigation. (2) Water iodine level of Hangzhou was in the range of 0.20 - 5.99 µg/L, with the median level as 2.58 µg/L. (3) Average daily dietary intake of iodine for adult males in Hangzhou was 289.2 µg/d. The contribution of iodine intake from iodized salt was 74.4%. (4) The median of Hangzhou residents' urinary iodine was 178.80 µg/L, with the urinary iodine levels at 100 µg/L-, 200 µg/L-, < 100 µg/L, and ≥ 300 µg/L groups were 37.14%, 23.11%, 21.05%, and 18.69% respectively. Urinary iodine of pregnant women was 141.0 µg/L. (5) Incidence of thyroid nodules in females (28.6%) was higher than that of males (20.1%). The detection rate increased with age (6.4% at group 6-, 10.9% at 12-, 12.0% at 18-, 24.4% at 40-, and 38.8% at 65-); with the highest in urban area (29.8%), followed by suburbs (23.3%) and in rural area it showed the least (20.3%). Urinary iodine level was found lower among the population who had been detected with thyroid nodules (160.36 µg/L) than those among the undetected population (182.00 µg/L)., Conclusion: Hangzhou appeared to be an area where the environmental was iodine deficient. Iodized salt was the major source of iodine intake. The iodine status among the general population seemed to be safe and suitable, but the iodine level for pregnant women was not sufficient. There was still no evidence indicating that the universal salt iodization policy in Hangzhou was associated with the prevalence of thyroid nodules.

This paper is to report the study of the metabolism of lidamycin in vitro including in plasma and microsomes to guide clinical therapy. Lidamycin was quantified by detecting its active ingredient using HPLC-MS/MS. The metabolic stability of lidamycin in rat, Beagle dog, monkey and human plasma and liver microsomes, and its inhibition to cytochrome P450 isoforms in human liver microsomes were studied. Results showed that lidamycin was metabolized in the four species of plasma, and the sequence of metabolic rates in plasma were in rat > in dog > in human > in monkey. But among the four species of liver microsomes, lidamycin was metabolized only in monkey liver microsomes. There was almost no inhibition to cytochrome P450 isoforms at the concentrations of between 0.0005 and 10 ng x mL(-1). Therefore, the property of lidamycin metabolism in human is similar with that in dog, and metabolism of other drugs would not be decreased by cytochrome P450 as used along with lidamycin in clinic.

Objective: to study the correlation of polymorphisms of CYP1A1 MspI, GSTM1 null genotype, cooking oil fumes independently and in combination with the risk of non-smoking lung cancer in females., Methods: one hundred and sixty female non-smoking patients with primary lung cancer and 160 controls were enrolled from Xiangya Hospital of Central South University. PCR-RELP and PCR were used to detect the distribution of CYP1A1 MspI and GSTM1 genotypes respectively. The correlation of these genes and cooking oil fumes with the susceptibility to lung cancer was analyzed., Results: There was a significant difference in the frequencies of cooking oil fumes exposure between cancer cases and controls (χ(2) = 10.734, P < 0.01);but there was no statistical difference in CYP1A1 MspI polymorphisms between the 2 groups (χ(2) = 3.731, P > 0.05). The combination of CYP1A1 polymorphisms and cooking oil fumes significantly increased the risk of lung cancer. The frequencies of GSTM1 null genotype was significantly different between cancer cases and controls (χ(2) = 0.518, P < 0.05). The risk of lung cancer was higher in those with the GSTM1 null genotype and the OR was 1.697 (95%CI 1.090 - 2.640). Individuals with both GSTM1 null genotype and exposure to cooking fumes had a higher risk of cancer than those with only one of them, the OR being 3.617 (95%CI 1.899 - 6.891). The combination of the two genes significantly increased the risk of lung cancer., Conclusions: cooking oil fumes exposure was a risk factor for non-smoking lung cancer in females. The combination of CYP1A1 with cooking oil fume increased the risk of female lung cancer. GSTM1 null genotype was associated with risk of lung cancer in non-smoking females. The combination of GSTM1 null genotype and cooking oil fumes significantly increased the risk of female lung cancer. The combination of CYP1A1 and GSTM1 significantly increased the risk of lung cancer.

The paper is to report the pharmacokinetic character of a series of chemical compounds in vitro and in vivo. Metabolism stability of a series of chemical compounds was screened by using rat liver microsomes. The samples of different chemical compounds were combined and then simultaneously detected by LC-MS/MS. Compounds y13, y12 and y11 were screened out by microstability assay in vitro. The pharmacokinetics of compounds y11, y12 and y13 was evaluated by using SD rat. The plasma samples were pooled at the same time. The plasma concentrations were determined by LC-MS/MS. The pharmacokinetic character of two compounds y13, y11 was good by screening in vivo, so they were developed for further research. High-throughput screening of drug candidates in vitro and in vivo was effective, to provide information for the chemical structure information and lower the drug development risk.

Objective: To explore the risk factors of injuries among school aged children from migrant workers' families, in Hangzhou., Methods: A cross-sectional survey on 3582 students from eight separate schools in which, four were set for migrant workers' families and the other four were for families of permanent residents. Stratified cluster random sampling method was used. Data was analyzed by unconditional univariate and multivariate logistic regression methods under SPSS 13.0., Results: The incidence rate of injury did not show statistical difference between children of migrant workers or from the permanent residents. The incidence rate of multiple injuries was higher in children from the migrant workers' families. The incidence rates on electric shock occurred at the primary school, drowning among boys at the secondary school and scald/crash/cutting by knives in girls at secondary schools were seen higher among children from the of migrant workers. Results from multivariate analysis showed that factors as gender (OR = 1.20), age (6 - 9 years: OR = 0.70, 10 - 12 years: OR = 1.45), fond of playing Pingpong (OR = 1.35), history of injuries by pets (OR = 1.41), skills on swimming (OR = 1.22), no history of being threatened (OR = 0.68), having harmonious family relations (OR = 0.69) and owning a house by family (OR = 0.76) appeared to be the major one that related to the occurrence of injury., Conclusion: Personal behavior as well as family and social environment seemed to be factors affecting the occurrence of injuries among children from the migrant workers' families.

Objective: To explore the correlation of the expressions of metastatic tumor antigen 1 (MTA1) and hypoxia-inducible-factor l alpha (HIF-1alpha) to the clinical features of lung cancer., Methods: The expressions of MTA1 and HIF-1alpha proteins in 59 lung cancer patients were detected by immunohistochemistry., Results: Positive staining of MTA1 and HIF-1alpha was found in 54.24% and 50.85% of the patients, respectively. MTA1 expression was not found to correlated to any of the clinical parameters. HIF-1alpha expression was significantly lower in poorly differentiated than in moderately and well differentiated lung cancer (P<0.05), and a positive association between the expressions of MTA1 and HIF-17alpha were noted (P<0.05)., Conclusion: MTA1 and HIF-1alpha overexpression occurs in lung cancer possibly as an important factor of lung carcinogenesis. MTA1 may promote lung carcinogenesis by enhancing HIF-1alpha protein activity.

A novel method concerning the coding technology of polystyrene beads with Si encapsulated quantum dot (QD) particles (Si@QDs particles) is studied in this paper. In the reverse microemulsion system containing tetraethoxysilane (TEOS), water-soluble QDs (emission peak at 600 nm) were enveloped within the silica shell, forming Si@QDs particles. The Si@QDs particles were characterized by TEM, showing good uniform size, with an average diameter of about 167.0 nm. In comparison with the pure water-soluble QDs, the encapsulation of water-soluble QDs in the silica shell led to an enhancement in anti-photobleaching by providing inert barriers for the QDs. Images presented by SEM and confocal laser scanning microscopy demonstrated that the Si@QDs particles were equably coated on the surface of carboxyl functionalized polystyrene (PS) beads. Then, with the assistance of ethyl-3-(dimethyl aminopropyl) carbodiimide/N-hydroxysuccinimide (EDC/NHS), human IgG could be successfully crosslinked to Si@QDs particle coated PS-COOH beads. Furthermore, the Si@QDs coated PS-COOH beads with human IgG were examined in immunoassay experiments, and the results indicated that these beads could be applied in the specific recognition of goat-anti-human IgG in solution. This investigation is expected to provide a new route to bead coding in the field of suspension microarrays, based on the use of QDs.

This study was purposed to verify the binding part of human complement C3 to complement receptor III (CRIII) in monocytes, the peptide rC3B, including the binding-site, was expressed, purified and identified. rC3B, the binding part of human complement C3 to CRIII, was selected by computer-aided modeling and summarizing researches published. Then, rC3B gene fragment was amplified by PCR, and cloned into prokaryotic vector pQE30a. The fusion protein rC3B was expressed in E.coli M15 and purified by Ni(2+)-chelating affinity chromatography. The activity of rC3B was identified by Western blot and adherence assay with monocytes. The results showed that rC3B fragment was obtained, and a prokaryotic expression vector pQE30-rC3B was constructed. rC3B was efficiently expressed and purified. In Western blot, the target protein showed the activity of binding with C3 antibody, while the purified protein showed the activity of adherence with monocytes. It is concluded that the recombinant C3B was obtained and identified, and this study lay the basis for the further functional analysis of C3.

Objective: To study the pathological basis of radiological reaction types of radiation-induced liver disease on multiphasic CT scans., Methods: Three pigs (tagged with A, B, and C) were subjected to single-dose radiation of 40, 40 and 30 Gy on the right or left lobe of the liver, respectively. At 42, 56, 133, and 168 days after irradiation, all pigs were examined with non-enhanced scan and contrast-enhanced scans at different time points after contrast injection. Hounsfield units (HU) were measured in each CT study to evaluate the density of irradiated and non-irradiated liver tissue to determine the reaction type. Liver tissues in the irradiation area obtained by needle biopsy with CT guidance were examined with electron microscopy, and specimens of the tissue corresponding to the region of interest on CT were obtained from necropsies for pathological examination., Results: Radiologically, the 3 pig models presented with 3 reaction types on the multiphasic CT scans on days 133, 56, and 168 after radiation, respectively. Type 1 presented constant low-density change in all phases, the pathological basis of which was radiation hepatitis; type 2 showed pre-contrast phase isodense, arterial phase hyperdense, portal phase isodense and later phase hyperdense changes; type 3 was characterized by pre-contrast phase isodense, arterial phase hyperdense, portal phase hypodense and later phase hyperdense changes. The pathological basis of the last two radiological reaction types was radiation cirrhosis (postnecrotic cirrhosis)., Conclusions: Different radiological reaction types of radiation liver injury on multiphase CT have different pathological basis, and multiphase contrast-enhanced CT may help distinguish the radiation reactions from tumor recurrence.

Objective: Grope for Optimization of Extraction Parameters and De-protein Process for Gastrodia elata Bl. Polysaccharides (GPS). Provide the theoretical basis for the industrialization production of GPS., Methods: The effects of extracting temperature, ration between Gastrodia elata Bl. and water, heating time on extraction rate of GPS were studied with orthogonal experimental design. Compared the application of the two de-protein process measures (Sevag and Enzyme-Sevag) in purification technics for Gastrodia elata Bl., Results: The optimum parameters were: extraction 3h at 120 degrees C with 1:40 ratio of Gastrodia elata Bl. to water. The de-protein efficiency of Enzyme-Sevag is better than Sevag.

Objective: To review the appearance of radiation-induced liver injury on computer tomography for quantitative assessment of dosimetric changes in different radiological reactions and the influence of time-effect., Methods: The focal liver reactions of 35 patients treated with three-dimensional conformal radiation therapy (3-D CRT) for liver malignancies were evaluated, with the applied doses of 36-65 Gy in 4-28 fractions completed in 8-41 days. All patients received nonenhanced CT scan and arterial-dominant phase contrast-enhanced CT scan 1-6 months after therapy. The liver tissue density in irradiated and nonirradiated liver was compared, and the reaction type and the threshold dose determined radiologically., Results: On at least one follow-up examination, 51.4% of patients were found to have a focal radiation reaction in the liver. The radiation reaction was hypodense in 43.75% of the follow-up nonenhanced CT examinations and in 19.23% of arterial-dominant phase contrast-enhanced CT scans. It was hyperdense in 42.31% of arterial-dominant phase contrast-enhanced CT scans. The median threshold dose inducing a radiation reaction was 30.8 Gy (range 18-42.8 Gy). The detected threshold dose was positively correlated with the time of detection of the reaction (P=0.041), with a correlation coefficient of -0.473. On arterial-dominant phase contrast-enhanced CT scans, the threshold dose was significantly higher for hyperdense than for hypodense changes (P=0.017). In additional follow-up, the reaction volume decreased and the reaction types changed on arterial-dominant phase contrast-enhanced CT scans., Conclusions: The threshold dose can be different in different radiological reaction types on multiphase CT scans. The detected threshold dose is inversely correlated with the time of detection of the early reaction. Multiphase contrast-enhanced CT is helpful to distinguish radiation reactions from recurrent tumors.

The design, fabrication, and testing of micro-cannulae with integrated insertion stops is presented. The micro-cannulae were engineered through the use of a silicon micro-mold fabricated via bulk-silicon micro-machining techniques. The use of microelectronic fabrication techniques allows precise control of three critical parameters, insertion depth, interface contact area, and tubing out of round. Worst case variations were found to be 5microm for insertion depth, 502microm(2) for interface contact area, and 7% for tip out of round. Histological evaluation revealed the cannula to be located correctly within the basal portion of scala tympani.

Objective: To evaluate the role of integrated positron-emission tomography and computed tomography (PET/CT) in gross tumor volume (GTV) delineation for three-dimensional conformal radiotherapy for bone metastasis., Methods: Three patients with multiple bone metastases were enrolled in this study, whose primary tumors were pathologically identified as lung cancer, liver cancer and renal cell carcinoma. In each case, 6 sites of bone metastases were selected, labeled as BM1 to BM6 which located in the lumbar, thoracic vertebra, rib, ilium, scapula and thighbone respectively. The GTVs of the 6 bone metastases were delineated on the CT scans for treatment planning by 8 radiation oncologists, and the results were compared with the delineation obtained on the basis of integrated CT and PET/CT for analyzing the interobserver variability., Results: For BM1-5 with obvious bone cortex lesions by the carcinoma, the GTV delineated on the basis of CT was greater than that derived from PET/CT (P<0.05), whereas for BM6 with intact bone cortex, the contrary result was observed (P<0.05). For any of these bone metastasis, the interobserver variability in GTV delineation with PET/CT was less than that with CT., Conclusion: PET/CT is useful for improving the accuracy of GTV delineation for the protection of the normal tissues during radiotherapy.

Pharmaceutical tablets made of modified high-amylose starch have a hydrophilic polymer matrix into which water can penetrate with time to form a hydrogel. Nuclear magnetic resonance imaging was used to study the water penetration and the swelling of the matrix of these tablets. The tablets immersed in water were imaged at different time intervals on a 300 MHz NMR spectrometer. Radial images show clearly the swelling of the tablets and the water concentration profile. The rate constants for water diffusion and the tablet swelling were extracted from the experimental data. The water diffusion process was found to follow case II kinetics at 25 degrees C. NMR imaging also provided spin density profiles of the water penetrating inside the tablets.