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

To investigate the effect of Tanreqing injection on immune activity of peripheral blood lymphocytes of patients with lung cancer. The peripheral blood lymphocytes of patients with lung cancer and healthy persons were separated by the density gradient centrifugation method for subsequent experiments, with those from healthy persons as the positive control. The effect of Tanreqing injection on stimulating the proliferation of lymphocytes with phytohemagglutinin (PHA) was determined by MTT method. The effect of Tanreqing injection on the lymphocyte secretions of IFN-γ and TNF-α and the subset ratio of lymphocytes cultured separately or with Tanreqing injection of different concentrations were examined by ELISA and flow cytometry (FCM) respectively. In addition, the LDH release assay was used to detect the cytotoxicity of cytotoxic T cells (CTL) and natural killer cells (NK). According to the findings, all of immunological indexes of lymphocytes from patients with lung cancer were weaker than that of healthy persons, but with the obvious increases in proliferation activity and IFN-γ and TNF-α secretions of lymphocytes co-cultured with Tanreqing Injection (P < 0.05). Among lymphocyte subsets co-cultured with Tanreqing Injection, CD3+, CD3+ CD4+ and CD3- CD16 + 56+ cell ratios notably increased, whereas CD4+ CD25+ Treg cell ratio obviously decreased (P < 0.05). In the meantime, Tanreqing injection can markedly promote the cytotoxicities of CTL and NK (P < 0.05). In conclusion, Tanreqing injection shows a significant effect in promoting the immune activity of lymphocytes from patients with lung cancer and their anti-tumor immunity.
Cell Proliferation ; drug effects ; Cells, Cultured ; Drugs, Chinese Herbal ; administration & dosage ; Humans ; Interferon-gamma ; genetics ; immunology ; Killer Cells, Natural ; drug effects ; immunology ; Lung Neoplasms ; drug therapy ; genetics ; immunology ; physiopathology ; T-Lymphocytes, Cytotoxic ; drug effects ; immunology ; Tumor Necrosis Factor-alpha ; genetics ; immunology

Objective To study the macrophage colony-stimulating factor(M-CSF)expression levels of serum and synovial fluids from patients with spondyloarthropathy(SPA)and its contribution to the pathogen- esis of SpA.Methods Eleven SpA synovial tissue samples were compared to those from peripheral blood mononuclear cells(PBMC)of 10 normal subjects using a 1176 gene array.M-CSF was detected in both serum samples and synovial fluids by enzyme linked immunosorbent assay(ELISA).Two groups of AS subjects were tested.The first group consisted of 41 ankylosing spondylitis(AS)patients who had not been treated with bio- logics.The second group consisted of 13 subjects whose serum samples were collected before and 14 weeks af- ter initiation of infliximab.These were compared to serum samples from 28 normal subjects,and synovial fluid samples from 15 SpA patients.Results Expression of M-CSF could be detected in both serum samples and synovial fluids.The concentration of M-CSF in the group of 41 AS patients not treated with biologics correlated with the Bath Ankylosing Spondylitis Disease Activity Index(BASDAI)values(r=0.41,P=0.004).Treatment of infliximab in AS patients led to a significant decrease in the values of BASDAI(P=0.000 07),but no signif- icant change in the serum M-CSF values.Conclusion M-CSF is a promising candidate for research on the mechanisms of SpA and its signaling on pathway in SpA is different from tumor necrosis factor(TNF)-?,and it may provide new basis for developing new anti-biologics for SpA.

Objective To evaluate the expression quantity of T lymphoma invasion and metastasis inducing factor 1(Tiara 1)in gastric cancer tissues,tissues around the cancer over 3 cm and tissues of gastric benign lesions,and to analyze the correlation between amount of Tiaml and gastric cancer biological behaviours.Methods Real-time fluorescence quantitive RT-PCR(FQ-RT-PCR)was used to detect the expression level of Tiaml mRNA in 66 cases of gastric cancer tissues,tissues around the cancer over 3 cm and the gastric tissues of 11 cases with benign lesion.Results Positive rate of Tiam1 mRNA expression in gastric cancer tissues,tissues around the cancer was 92.4%,19.7%,respectively,and only one case express Tiaml mRNA in 11 cases gastric benign lesion tissues.There was significant difference(P0.05),on the other hand,the expression quantity of Tiaml mRNA in gastric cancer was significantly correlated with metastasis into lymph node,the extent of invasion,differentiated degree of histologic type,and the stages of TNM(P

Objective To evaluate the functional outcome,predicting response and toxicity of CT- guided permanent implanted ~(125)I seed branchytherapy for metastatic cancers in vertebrae.Methods Forty three vertebrae with metastatic cancer were treated by CT-guided percutaneous permanent implanted ~(125)I seed branchytherapy in 15 patients.There were 8 male and 7 female patients with average age of 54.6 years and 2 to 5 vertebrae involved in this group.According to the size of tumor,the optimal activity and quantity of seeds were calculated by TPS and correlative formula.~(125)I seeds were implanted percutaneous puncture under CT- guidance with coaxial needles to pass the normal osseous tissue for approaching the lesions including 3 routes of pedicnlar lateral and anterior ways.The distance between seeds and posterior border of vertebral body was over 3 nun(3-10mm).Permanent ~(125)I seed implantation brachytherapy for paraspinal metastatic lesions were also taken place.Results Mean follow-up time was 12.3 months(range 3-30 months)and outcome was evaluated clinically and radiographieally in 10 of 15 procedures,with 5 only on clinical data.No new pain occurred at 11 sites with no previous complaint.The pain was completely controlled at 18/32 sites,partial control at 14/32 sites.No complications correlated to the radiotherapy damage of nerve and spinal cord were found.Conclusion The procedure of CT-guided permanent implanted ~(125)I seeds brachytherapy for vertebral metastatic cancers is a safe effective and minimal invasive method with few complications.It is beneficial not only for pretherapeutic metastasis but also for recurrent tumors after radiotherapy;bearing rather high tolerance and safety.(J Intervent Radiol,2007,16:834-837)

Alcohol Drinking ; China ; epidemiology ; Exercise ; Fatty Liver ; epidemiology ; etiology ; prevention & control ; Humans ; Hyperlipidemias ; complications ; Obesity ; complications ; Prevalence

Objective　To study the mechanisms of Pericarpium Arecae. Methods　A total of Wistar rats were randomly divided into Pericarpium Arecae group and control group, Pericarpium Arecae decoction or distilled water were given respectively. Changes of gastrointestinal motility rats were assayed by Dextran blue-2000 after 1 and 6 hours. The distributions of SP and VIP in antrum and jejunum were investigated by immunohistochemistry assay. Results　The gastrointestinal motility of rats was markedly enhanced (P<0.01 or P<0.05). The expressions of SP increased significantly (P<0.01 or P<0.05) and the expressions of VIP decreased significantly (P<0.01 or P<0.05) in antrum and jejunum of rats at 1 and 6 h after Pericarpium Arecae decoction was given. The changes were more obvious at 1 h than at 6 h. Conclusion　The kinetogenic effect of Pericarpium Arecae is closely correlated to the increase of SP expression and the decrease of VIP expression in gastrointestinal tract.

The present study is to investigate the quality changes of ginseng stems and leaves before and after frost. The contents changes of ginsenoside, free amino acid, and total phenolic compounds, as well as DPPH radical scavenging effect before and after frost were measured. The content of 9 ginsenoside monomer in ginseng stems was decreased except for Rg, and Re after frost, but in ginseng leaves was all decreased. The total content of amino acids was decreased in ginseng stems after frost, while increased in ginseng leaves. The content of phenolic compounds in ginseng stems and leaves were both decreased after frost while the ability of DPPH radical scavenging was improved. The factor of frost has great impact on the quality of ginseng stems and leaves.
Drugs, Chinese Herbal ; chemistry ; Ecosystem ; Freezing ; Panax ; chemistry ; Plant Leaves ; chemistry ; Plant Stems ; chemistry ; Quality Control

Objective To investigate the effects of five elements music combined with acupoint massage on sleep quality in insomnia patients with coronary heart disease (CHD).Methods A total of 120 cases of insomnia patients with CHD were randomly divided into the experimental group and the control group with 60 cases,respectively.The control group was given routine medicine treatment for CHD.The experimental group was given five elements music combined with acupoint massage besides the routine treatment.The Pittsburgh Sleep Quality Index (PSQI) was used to compare before and 4 weeks after the intervention for sleep quality,hear rate and blood pressure between two groups.Results Four weeks after the intervention,total effective rate of sleep effect in the experimental group was 96.67％,and there was significant difference between two groups (P＜0.05).Four weeks after the intervention,heart rate,blood pressure,total score and scores for each dimension were decreased for both groups,but those in the experimental group declined more obviously,and the differences were significant (P＜0.05).Conclusion Five elements music combined with acupoint massage can significantly alleviate insomnia for patients with CHD.

OBJECTIVETo study the clonality of polygonal cells and surface cuboidal cells in the so-called pulmonary sclerosing hemangioma (PSH).

METHODS17 female surgically resected PSH were found. The polygonal cells and surface cuboidal cells of the 17 PSH cases were microdissected from routine hematoxylin and eosin-stained sections. Genomic DNA was extracted, pretreated through incubation with methylation-sensitive restrictive endonuclease HhaI or HpaII, and amplified by nested polymerase chain reaction for X chromosome-linked androgen receptor (AR) and phosphoglycerate kinase (PGK) genes. The length polymorphism of AR gene was demonstrated by denaturing polyacrylamide gel electrophoresis and silver staining. The PGK gene products were treated with Bst XI and resolved on agarose gel.

RESULTSAmongst the 17 female cases of PSH, 15 samples were successfully amplified for AR and PGK genes. The rates of polymorphism were 53% (8/15) and 27% (4/15) for AR and PGK genes respectively. Polygonal cells and surface cuboidal cells of 10 cases which were suitable for clonality study, showed the same loss of alleles (clonality ratio = 0) or unbalanced methylation pattern (clonality ratio < 0.25).

CONCLUSIONSThe polygonal cells and surface cuboidal cells in PSH demonstrate patterns of monoclonal proliferation, indicating that both represent true neoplastic cells.

Chromosomes, Human, X ; genetics ; DNA, Neoplasm ; genetics ; Female ; Humans ; Male ; Phosphoglycerate Kinase ; genetics ; Polymerase Chain Reaction ; Polymorphism, Genetic ; Pulmonary Sclerosing Hemangioma ; genetics ; pathology ; Receptors, Androgen ; genetics ; X Chromosome Inactivation