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

[Objective]To discuss the microsurgical approaches of 30 patients with tentorial meningiomas and conclude their treatment experiences.[Methods]A retrospective analysis of clinical data was performed on 30 patients underwent microsurgical approaches from July 2004 to September 201 1.The pathology of these patients was confirmed after operation.The outcome and follow-up were evaluated.[Results] The meningiomas were totally removed in 19 patients subtotally in 6,and partially in 5.All the patients received 8 months to 5 years of follow-up:no mortality or death were found;no surgical related complications were noted.[Conclusion] Appropriate approaches according to the size and site of the tumors,intraoperative protection of venous sinus,facial and acoustic nerves and brain stem are the key points to improve the therapeutical outcomes and the post-operative quality of patients with infra and supra tentorial menmingiomas.

OBJECTIVETo compare the efficacy difference between acupotomology and operation in the treatment of lumbar disc herniation (LDH).

METHODSOne hundred and eighty-four cases were randomized into an acupotomology group (109 cases) and an operation group (75 cases). In acupotomology group, acupotomology was applied to relevant local soft tissues in LDH and the reactive points in the distribution of superior gluteal nerves, at the outlet of sciatic nerve and in the nerve innervate area of the lower extremities separately. In operation group, the small-windowed discectomy through small incision was adopted. The clinical efficacies were assessed between two groups.

RESULTSIn acupotomology group, the clinical cured rate was 82.6% (90/109) and the effective rate was 96.3% (105/109). In operation group, they were 86.7% (65/75) and 97.3% (73/75) respectively. There were no significant differences in statistics between two groups (both P > 0.05).

CONCLUSIONAcupotomology is definitely effective in the treatment of lumbar disc herniation and its efficacy is similar to that of operation.

Acupuncture Therapy ; Adolescent ; Adult ; Aged ; Diskectomy ; Female ; Humans ; Intervertebral Disc Displacement ; surgery ; therapy ; Lumbar Vertebrae ; surgery ; Male ; Middle Aged ; Treatment Outcome ; Young Adult

Objective To investigate the efficacy and safety of Bushen Huoxue Decoction in the treatment of carotid atherosclerotic plaque. Methods Totally 50 patients of carotid atherosclerotic plaque were collected to conduct health education. At the same time, they were given Bushen Huoxue Decoction, one dosage a day, twice a day, decoction, for 12 weeks. The correlation indexes of carotid artery before and after treatment were observed, and TCM syndrome integrals were evaluated before and after 4, 8 and 12 weeks treatment. FBG, TC, LDL-C, CRP HCY, IL-6, IGF-1, and OPG were detected before and after treatment. Hematuria routine, liver and renal function were monitored. Results After treatment, the Crouse score and the plaque grade score of carotid atherosclerotic plaque showed a tendency to decrease, without statistical significance (P=0.060, P=0.336). Carotid maximal plaque area and modified total score of carotid atherosclerotic plaque were significantly reduced compared with that before treatment (P<0.05). TCM syndrome integrals were significantly reduced compared with that before treatment (P<0.05), and the scores decreased significantly with the prolongation of treatment time. TCM syndrome integrals after 4, 8, and 12 weeks were significantly reduced compared with that before treatment (F=160.352, P<0.001). Total effective rate of treatment in the efficacy of TCM syndrome was 85.11％ (40/47). Serum levels of FBG and TC decreased significantly after the treatment compared with that before the treatment, with statistical significance (P<0.05). Serum levels of LDL-C, HCY, CRP, IL-6, IGF-1, and OPG all showed a tendency to decrease, without statistical significance (P>0.05). No abnormality in hematuria routine, liver and renal function examinations were found during the research. Conclusion Bushen Huoxue Decoction has obvious clinical efficacy for carotid atherosclerotic plaque, which can improve clinical symptoms of patients, it also could stabilize and reduce plaque with high safety.

OBJECTIVETo investigate the effects of valsartan on expression of angiotensin II receptors in different regions of heart after myocardial infarction (MI).

METHODSCanines were divided into sham-operated control group (n=7), infarction group (n=7) and Valsartan group (10 mg x kg(-1) x day(-1) for 4 weeks after MI operation, n=7). Four weeks after operation, Doppler tissue imaging (DTI) was used to evaluate regional ventricular function in the noninfarcted myocardium (apical and basal near to the infarction region). The mRNA and protein expressions of angiotensin II type 1 receptor (AT1-R) and angiotensin II type 2 receptor (AT2-R) on the corresponding regions were detected by competitive reverse-transcriptase polymerase chain reaction technique and immunohistochemical technique respectively. Results The protein and mRNA expressions of AT1-R were significantly increased in both apical and basal regions near to the infarction in dogs with MI compared with those in control group (P < 0.05) which could be downregulated by valsartan (P < 0.05). AT2-R expressions were significantly upregulated in infarction group in both apical and basal regions compared with those in control group and valsartan further increased AT2-R expressions in both areas (P < 0.05). Myocardial peak systolic velocity (Sm), myocardial peak early diastolic velocity (Em) and myocardial peak late diastolic velocity (Am) at both apical and basal regions near to the infarction regions were significantly lower in MI group than those in the control group which could be significantly improved by valsartan.

CONCLUSIONBoth mRNA and protein expressions of AT1-R and AT2-R are upregulated in noninfarcted regions near MI, valsartan improved myocardial function via inhibiting AT1-R upregulation and enhancing AT2-R upregulation.

Angiotensin II Type 1 Receptor Blockers ; pharmacology ; therapeutic use ; Animals ; Dogs ; Female ; Male ; Myocardial Infarction ; drug therapy ; metabolism ; physiopathology ; Myocardium ; metabolism ; RNA, Messenger ; metabolism ; Receptor, Angiotensin, Type 1 ; metabolism ; Receptor, Angiotensin, Type 2 ; metabolism ; Tetrazoles ; pharmacology ; therapeutic use ; Valine ; analogs & derivatives ; pharmacology ; therapeutic use ; Valsartan

OBJECTIVETo investigate the specific antitumor immune response induced by idiotype protein (Id)-pulsed dendritic cells (DC) in vitro.

METHODSDC was generated from peripheral blood monocytes of the multiple myeloma (MM) patients using GM-CSF, IL-4, and TNF-alpha. The DCs were pulsed with idiotypic fragment, the F(ab')2 fragment of M protein from MM patient at the immature stage. The morphologic characteristics of the cells were observed with light and electron microscopes. The phenotypic features were analyzed with FACS, MTT assay was employed to evaluate the proliferation of autologous T cells and the inhibition rate of MM cells.

RESULTSDC precursors in peripheral blood could be induced to typical mature DC in medium containing GM-CSF, IL-4 and TNF-alpha. Mature DC with Id could increase the proliferation of the autologous T cells and activate naive T cells to become tumor specialized cytotoxic T lymphocytes (CTL). The CTL at different doses showed significant inhibition on or killing ability to autologous MM cells in vitro.

CONCLUSIONSIn a suitable cytokine environment, the DC precursors from peripheral blood of MM patients could be induced to functional DC, and vaccination of Id-pulsed DC could induce active antitumor immune response.

Adult ; Aged ; Antibodies, Anti-Idiotypic ; immunology ; Cancer Vaccines ; immunology ; Cells, Cultured ; Dendritic Cells ; immunology ; Female ; Humans ; Immunotherapy, Active ; Male ; Middle Aged ; Multiple Myeloma ; immunology ; therapy ; T-Lymphocytes, Cytotoxic ; immunology

Edible bird's nest contains lots of glycoproteins. The glycosylation inhomogeneity for glycoprotein often results in wide range of molecular weight and the difficulty for protein separation and charaterization. In this paper, proteins in the edible bird's nest were extracted using multiple extractions, and then digested by PNgase F and trypsin. The digest mixture was separated with HPLC, and peptides were identified based on MS/MS data searching. The results indicated that the extracted proteins were amount to 79.7% of total protein in the edible bird's nest. More than 20 species of peptides in the digested mixture were identified. The sequences of these peptides showed similarity with some proteins from Swiss-prot. The research indicated that deglycosylation, tryptic digestion coupled with HPLC-MS/MS is a proper strategy for characterization of proteins in the edible bird's nest.
Amino Acid Sequence ; Animals ; Birds ; Chromatography, High Pressure Liquid ; Glycoproteins ; chemistry ; Mass Spectrometry ; Medicine, Chinese Traditional ; Peptide Fragments ; chemistry ; isolation & purification ; metabolism ; Proteolysis

OBJECTIVETo study the function of the hypothalamus-pituitary-adrenal (HPA) axis in children with attention deficit hyperactivity disorder (ADHD).

METHODSOne hundred and twenty-eight boys with ADHD at ages of 6 to 14 years were enrolled. The diagnosis and grouping of ADHD were based on the Diagnostic and Statistical Manual of Mental Disorders (DSM-IV): ADHD-predominantly inattention type (ADHD-I, n=44), ADHD-predominantly hyperactive impulsivetype (ADHD-HI, n=32) and ADHD-combined type (ADHD-C, n=52). Thirty healthy boys served as the control group. Plasma levels of cortisol and adrenocorticotropic hormone (ACTH) were measured by automatic particle enzyme immunoassay and electrochemiluminescence respectively at 8:00 am. The intelligence level was tested by Raven's standard progressive matrices.

RESULTSThe children with ADHD had lower IQ score (84.5 + or - 11.3) than the control group (94.6 + or - 12.4) (p<0.01). There were significant differences in the IQ score among the three ADHD subgroups (p<0.01). The IQ score in the ADHD-I and the ADHD-C groups was significantly lower than that in the control group. The mean plasma cortisol level in the ADHD group (226.5 + or - 129.1 nmol/L) was significantly lower than that in the control group (384.5 + or - 141.4 nmol/L) (p<0.01). The three ADHD subgroups showed significantly decreased plasma cortisol level compared with the control group (p<0.01). The plasma level of cortisol was the lowest in the ADHD-HI group (154.4 + or - 71.6 nmol/L), followed by the ADHD I group (219.4 + or - 117.7 nmol/L) and the ADHD-C group (258.3 + or - 136.4 nmol/L). There were no significant differences in plasma concentration of ACTH between ADHD and control children.

CONCLUSIONSIn the non-stress state, the HPA axis may be dysfunctional in children with ADHD, which may be attributed to the under reactivity of the HPA axis. Lower plasma cortisol has fewer impacts on the cognitive-behavior function, but it may closely be related to attention deficit, hyperactivity and impulsive behaviors.

Adolescent ; Adrenocorticotropic Hormone ; blood ; Attention Deficit Disorder with Hyperactivity ; physiopathology ; Child ; Electroencephalography ; Humans ; Hydrocortisone ; blood ; Hypothalamo-Hypophyseal System ; physiopathology ; Intelligence ; Male ; Pituitary-Adrenal System ; physiopathology

OBJECTIVETo investigate the phenotype, frequency and function of CD4+ T cell subsets and the relevant cytokines, as well as the relationship between these cells and appearance of pneumonia of novel (H1N1) influenza A patients.

METHODS68 healthy people, 53 confirmed novel A(H1N1) influenza patients without pneumonia and 16 confirmed severe novel A (H1N1) influenza patients with pneumonia were enrolled in this study. Viral load in nasopharyngeal swabs specimens was measured by real time PCR assay. The phenotype and percentage of CD4+ T cell subsets including Th1, Th2, Th17, and Treg cells were measured by Flow cytometry analysis. The relevant cytokines in plasma including TGF-beta, IL-6 and IFN-gamma were measured by ELISA. Data was analyzed by one way ANOVA.

RESULTSIt was found that peak viral load and viral shedding period of severe patients with pneumonia was significantly increased compared with mild patients without pneumonia (P < 0.05). The percentage of Th17 cells of severe patients with pneumonia was significantly diminished compared to that of healthy subjects and mild patients without pneumonia (P < 0.05). However, Th1, Th2, Treg cells frequencies had no significant differences (P > 0.05) among these three groups. The level of TGF-beta in plasma for the severe patients with pneumonia was also significantly decreased compared to that of healthy subject and mild patients without pneumonia (P < 0.05). The viral shedding period inversely correlated with the frequency of Th17 cells (r = - 0.38, P < 0.05).

CONCLUSIONH1N1 influenza A virus can inhibit Th17 cells to differentiate, particularly more extent in patients with pneumonia. Impaired Th17 cells may correlate with viral clearance and pneumonia of novel H1N1 influenza A patients.

Adolescent ; Adult ; CD4-Positive T-Lymphocytes ; immunology ; Cytokines ; immunology ; Female ; Humans ; Immunity, Cellular ; immunology ; Influenza A Virus, H1N1 Subtype ; immunology ; Influenza, Human ; immunology ; Male ; Pneumonia, Viral ; immunology ; T-Lymphocyte Subsets ; immunology

OBJECTIVETo study the cognitive function, its correlation with and the impact on quality of life in epileptic children aged 6-13 years in regular school.

METHODCognitive function of 172 children with various types of epilepsy were measured using a computerized neuropsychological test battery including six items. Their scores across the neuropsychological measures were compared with 172 healthy control subjects from the general population strictly matched for age, sex and the region where education was accepted. The quality of life was measured in 105 cases by the Quality of Life in Epilepsy Inventory (QOLIE-31).

RESULT(1) After adjusting for age, gender, and education, children with epilepsy performed significantly worse than healthy control subjects on 5 of 6 cognitive tasks, including Raven's progressive matrices correct number (8.6 vs. 14.0), choice reaction time (620.4 ms vs. 489.5 ms), word-rhyming tasks (2796.9 ms vs. 2324.4 ms), simple substraction correct number (28.6 vs. 35.5)as well as number comparision (1002.4 ms vs. 803.1 ms), P < 0.01. When an impairment index was calculated, 44.2% patients had at least one abnormal score on the test battery, compared with 14.5% of healthy volunteers, there was statistically significant differences between the two groups, P < 0.001. (2) Children with new onset epilepsy before the treatment with anti-epilepstic drugs performed significantly worse than healthy controls on 5 of 6 cognitive tasks, including Raven's progressive matrices correct number (9.1 vs. 13.8), choice reaction time (625.8 ms vs.474.5 ms), word-rhyming tasks(3051.8 ms vs. 2575.4 ms), simple substraction correct number (28.9 vs. 35.3) as well as number comparison (942.4 ms vs. 775.8 ms), P < 0.01. (3) Cognitive performance was not related to the age of onset, type of epilepsy, therapy duration or comorbid emotional and behavior disorders, P > 0.05. (4) 105 cases filled in the QOLIE-31 questionaire, the total score of the quality of life in the group without cognitive impairment and psychical conditions was the highest (60.5 ± 0.9), and the lowest total score was found in group with cognitive impairment and psychical conditions (54.6 ± 1.5), there were highly significant differences between the groups, P < 0.001.

CONCLUSIONAlmost one-half of the children with epilepsy accepting regular education had at least one abnormal score in the battery tests. Newly diagnosed untreated patients with epilepsy are cognitively compromised before the start of antiepileptic drug medication. Cognitive impairment was not related to the epilepsy-related or psychiatric variables. Cognitive impairment and mental disorders require further attention and essential therapy, which is important to the improvement of the quality of life in epileptic children.

Adolescent ; Child ; Cognition ; physiology ; Cognition Disorders ; diagnosis ; epidemiology ; psychology ; Comorbidity ; Epilepsy ; complications ; psychology ; Female ; Humans ; Male ; Neuropsychological Tests ; Quality of Life ; Reaction Time ; Surveys and Questionnaires