Abstract: Fifteen novel ligustrazine-tetrahydroisoquinoline derivatives were designed and synthesized according to the association principle of pharmaceutical chemistry. The structures were identified by IR, NMR and ESI-MS. The inhibitory activities of platelet aggregation induced by ADP and AA have been measured by Bron method. Preliminary pharmacological results showed that compounds 7g, 7h and 7n had potent inhibitory activity against platelet aggregation induced by AA, and the compound 7o showed significant inhibitory activity against platelet aggregation induced by ADP.
Drug Design ; Platelet Aggregation ; drug effects ; Platelet Aggregation Inhibitors ; chemical synthesis ; chemistry ; Pyrazines ; chemical synthesis ; chemistry ; Tetrahydroisoquinolines ; chemical synthesis ; chemistry

Objective To analyze clinical charaCteristics and diagnostic experience on thyrotropinoma (TSHoma).Methods Clinical characteristics,laboratory findings,diagnostic experience,and surgical outcome were summarized from 16 cases of TSHoma in our hospital from January 2006 to September 2011.Results ( 1 )Among 16 cases ( 9 male,7 female ) aged ( 51.63 ± 13.23 ) years,14 ( 87.5 ％ ) cases presented with hyperthyroidism and 2 were diagnosed by physical examination. None of them had exophthalmos, acropachy, or pre-tibial myxedema.( 2 ) Serum FT4 and FT3 levels were all above normal range with serum TSH ( 4.37 ± 2.77 ) μIU/ml.There were 25％ (4/16) cases with positive serum thyroglobulin antibody and/or thyroid peroxidase antibody,none with positive TSH receptor antibody.TRH stimulating test was performed in 9 cases,3 were with positive response ( peak TSH level increased by 5.45-9.20 μIU/ml compared with baseline),and 6 without response (peak TSH level increased by -0.01-3.15 μIU/ml compared with baseline).TSH was suppressed to 27.15％ (5.19％-99.15 ％ ) of the baseline in 11 cases in which somatostatin suppression test was carried out.Prolactin and insulin-like growth factor-Ⅰ levels were increased in 2 cases.MRI performed in 15 patients showed 10 cases of microadenomas and 5 cases of pituitary adenoma.A mass in nasal cavity was found in one case,where no mass was found in the pituitary.( 3 )Surgery was made in 11 cases ( 9 patients underwent transsphenoidal operation,one craniotomy,and one underwent operation via endoscopic nasal septum ). All patients (11/11) were proved to yield pituitary adenoma pathologically.Conclusion Thyrotropinoma should be considered in hyperthyroidism with unsuppressed TSH level,and dynamic tests facilitated early diagnosis.Ectopic thyrotropinoma shoull be considered when normal pituitary morphology was shown by MRI.

The equilibrium configuration of fluid-phase phospholipid vesicles in aqueous solutions are controlled by bending elasticity. We exploited a method for calculating explicitly the stability of arbitrary symmetric shapes. The morphology of lipid vesicles with topological genus g=2, i.e. with two holes or two handles, is studied. We provided some stable shapes with results explicitly.

A method for the determination of Fe, Co, Mn and Ni in synthetic diamonds by inductively coupled plasma atomic emission spectrometry ( ICP-AES) was proposed. The synthetic diamond sample was decomposed completely, while the sample was burned in air at 1000 ℃ for 10 h, and then a mixed acid of H2 SO4 , aqua regia and HClO4 was used for the dissolving the residue of the sample. In this method, the limits of detection of Fe, Co, Mn and Ni were 0. 0147, 0. 0018, 0. 0006 and 0. 0027 mg/L, respectively. Under the optimum condition, Fe, Co, Mn and Ni in synthetic diamond sample were determined. The values of RSDs (n=7) were less than 0. 5%. The recoveries of added standard were 94. 0%-105. 0%.

A method for the simultaneous determination of oxygen and nitrogen in synthetic diamonds by inert gas high temperature extraction-impulse heating method was proposed. The sample weight, the selection of analysis power and the calibration curves of oxygen and nitrogen were discussed. Oxygen and nitrogen in analytical samples are determined. Values of RSDs (n=7) for oxygen and nitrogen were less than 4. 5% and 4. 0% respectively. The analytical results of oxygen and nitrogen obtained by the proposed method were in good agreement with those by inert gas fusion-impulse heating method.

Objective To evaluate the efficacy and safety of dezocine injection for analgesia.Methods A multicenter , randomized , double blind, parallel group controlled study was performed with dezocine as the test drug , and pethidine injection and morphine injection as positive con-trol for the single treatment and 7 days treatment of moderate and severe pain , respectively.The test drug was dezocine injection.One hundred of forty patients with postoperative moderate and severe pain received single treatment with dezocine ( single injection of dezocine , n=70 ) or pethi-dine ( single injection of pethidine and placebo , n =70 ).Fifty -six cancer pain patients received 7 days treatment with dezocine or morphine as follows:the test group was intramuscularly injected two dezocines each time ( n=31 ) , and the control group was injected morphine and moe-phine simulation respectively ( n=25 , four times a day ) .Pain intensity difference ( PID) was evaluated as the primary analgesic effect criteria.Results There was no significant difference in PID between the test group and the control one both in the controlled trail of postoperative pain and that of chronic cancer pain.The most common adverse reactions of dezocine were nausea , vomiting and dizziness , et al.Conclusion The analgesic effect and adverse effects of dezocine were similar to those of morphine , which indicats dezocine is an effective and safe analgesic for postoperative pain and chronic cancer pain that are moderate and severe.

OBJECTIVETo study the effects of desmopressin (DDAVP) on coagulation factor Ⅷ (FⅧ) and activated partial thromboplastin time (APTT) in children with mild hemophilia A.

METHODSEighteen children with mild hemophilia A were enrolled. DDAVP (0.3 μg/kg•d) was injected intravenously for 5 days. Plasma FⅧ levels and APTT were measured before and after DDAVP treatment.

RESULTSIn 16 of 18 children with mild hemophilia A, the bleeding symptoms, including the articular or musclar hematoma, were significantly alleviated as a result of DDAVP treatment. The plasma FⅧ levels increased significantly to (27±4)% and APTT was shortened to (66±10)s 60 minutes after the first dose of DDAVP treatment. The plasma FⅧ remained at the levels of 25%-30% during 3-4 days of DDAVP treatment. Five days after DDAVP treatment, the plasma FⅧ levels decreased [(21±3)%], and APTT was prolonged when compared with 1-4 days of DDAVP treatment.

CONCLUSIONSDDAVP treatment can increase plasma FⅧ levels and shorten APTT in children with mild hemophilia A. DDAVP is effective in the treatment of mild hemophilia A. The duration of DDAVP therapy for mild hemophilia A is recommended as 3 to 4 days.

Child ; Child, Preschool ; Deamino Arginine Vasopressin ; therapeutic use ; Factor VIII ; analysis ; Hemophilia A ; blood ; drug therapy ; Humans ; Infant ; Male ; Partial Thromboplastin Time

OBJECTIVESTo investigate the transmission process of severe acute respiratory syndrome (SARS) and to evaluate the infectiveness of SARS patients in different periods of disease epidemics.

METHODSStandardized questionnaire was used to conduct case investigation and contact tracing by combining the field investigation and telephone interview. Transmission process, infectivity, transmission chain and contact history of SARS were studied through data analyses.

RESULTSOn 25th March 2003, a 91 year old man was admitted to Hospital J in Beijing with stroke and fever. He died on 30th March. From 31st March, there was an outbreak of SARS among his contacts in the family and in the hospital he was admitted to. Contacts would include his relatives, other co-patients and health care workers in the Hospital J. Chinese Field Epidemiology Training Program trainees conducted an investigation of the outbreak. Among the 207 contacts of the index cases through different generations, there were 36 cases of SARS (attack rate 17%) patients with one death. There were 12 cases having directly contact with the index case and 13 cases with one secondary case. The transmission chains of this outbreak could clearly be depicted. All the cases had close contacts during the symptomatic period of their index patients. Among the relatives, 85% of the cases had 3 - 5-day contact with their index patients after the onset of the illnesses. There was no significant difference between the two attack rates-70% for whose who had contact with the patient before and after illness onset) and 67% for those who only had contact after the onset of the illness. Out of the 44 social acquaintances and 38 of the family members who had contacts with the index patients during the incubation period, no one was found ill. Among the close contacts at the hospital who had no protection when providing care to the patient, the attack rate was found over 80%.

CONCLUSIONSAll the secondary cases of this outbreak had a history of direct and close contacts to the index patients after the onset of the illness. There was no evidence indicating that SARS cases were infectious during their incubation period.

Aged ; Aged, 80 and over ; China ; epidemiology ; Humans ; Infectious Disease Transmission, Patient-to-Professional ; Male ; Severe Acute Respiratory Syndrome ; epidemiology ; prevention & control ; transmission

OBJECTIVEElderly patients with obstructive sleep apnea/hypopnea syndrome (OSAHS) has a higher risk of cardiovascular and cerebrovascular disease. However, changes of homocysteine (Hcy) as markers of cardiovascular and cerebrovascular disease associated with OSAHS and their mechanism have not been elucidated so far. This study aims to investigate the changes of both serum Hey and oxidative stress and their possible links with OSAHS in elderly patients.

METHODSBased on polysomnogram (PSG) and age, 83 patients with OSAHS were recruited and divided into elderly-OSAHS (n=32) and non-elderly OSAHS groups (n=51). Fifty two subjects without OSAHS were divided into elderly control (n=29) and non-elderly control groups (n=23). A total of 135 subjects were included in the present study. All subjects were recorded for PSG variables and the contents of homocysteine (Hcy), malonaldehyde (MDA), and glutathione (GSH) which were detected after sleep. Serum homocysteine was measured by cyclophorase. MDA and GSH were measured by spectrophotometer.

RESULTS(1) The serum levels of Hcy showed significant difference among the four groups (P < 0.05). The concentrations of Hey in elderly OSAHS patients were higher than in other groups, while those in the elderly control group were higher than in the non-elderly control; the concentrations in the non-elderly OSAHS group were higher than in the non-elderly control. (2) The concentrations of MDA and GSH changed at an equal pace with Hey in the four groups. (3) Multielement linearity regression analysis indicated a statistically significant relationship between Hcy concentration and age, MDA, GSH, and apnea hypopnea index (AHI).

CONCLUSIONS(1) The concentrations of Hey and oxidative stress have increased with advancing age. (2) The concentrations of Hey and oxidative stress have further increased in the elderly patients with OSAHS. (3) Oxidative stress might cause high-level serum Hey in the elderly patients with OSAHS.

Adult ; Aged ; Female ; Homocysteine ; blood ; Humans ; Male ; Middle Aged ; Oxidative Stress ; physiology ; Sleep Apnea Syndromes ; blood

To clone porcine bone marrow stromal antigen-2 (BST-2) gene, construct its recombinant eukaryotic expression plasmid and induce the expression of the fusion antiviral protein, we amplified BST-2 gene by RT-PCR from the total RNA extracted from PK15 cells. The recombinant expression plasmid pcDNA-BST-2 was constructed and then was transfected into HEK293T cells to expresse the BST-2 fusion protein. Western blot and indirect immunofluorescence assay (IFA) were performed, and the biological activity was detected. The results showed that the construction of recombinant plasmid pcDNA-BST-2 was confirmed by restriction enzyme digestion and sequencing. The expressed product had antiviral activity against Vesicular stomatitis virus (VSV), Avian influenza virus (AIV) and Porcine reproductive and respiratory syndrome virus (PRRSV). In conclusion, the research paves the way for further research on bioactivity assayand antiviral medication.
Animals ; Antigens, CD ; genetics ; immunology ; Cell Line ; Chickens ; Cloning, Molecular ; Gene Expression ; Humans ; Influenza in Birds ; immunology ; virology ; Orthomyxoviridae ; physiology ; Porcine Reproductive and Respiratory Syndrome ; immunology ; virology ; Porcine respiratory and reproductive syndrome virus ; physiology ; Swine ; Vesicular Stomatitis ; immunology ; virology ; Vesicular stomatitis Indiana virus ; physiology ; Virus Replication