Objective: To synthesize novel tetrahydroisoquinolines with both anti-fungal and contraceptive activities, so as to provide precursor structures for contraceptives with anit-fungal activities. Methods: 3,4-dimethoxyphenylethylamine was taken as the template and the title compounds were synthesized through Pictet-Spengler reaction, neutralization reaction, substitution, hydrolysis, and acylation. The anti-fungal activity and sperm-killing activity of the target compounds were tested in vitro. Results: Fourteen title compounds were obtained and they were: 2-octyl-6, 7-dimethyl-1, 2, 3, 4-tetrahydro-isoquinoline hydrochloride(1), 2-nonyl-6, 7-dimethyl-1,2, 3,4-tetrahydro-isoquinoline hydrochloride(2), 2-decyl-6, 7-dimethy-1, 2, 3, 4-tetrahydro-isoquinoline hydrochloride(3), 2-dodecyl-6, 7-dimethyl-1,2,3,4-tetrahydro-isoquinoline hydrochloride(4), 2-dodecyl 6, 7-diacetoxy-1, 2,3,4-tetrahydro-isoquinoline hydrochloride(5), 2-pentyl-6,7-diacetoxy-1,2,3,4-tetrahydro-isoquinoline hydrobromide(6), 2-hexyl-6, 7-diacetoxy-1,2,3,4-tetrahydro-isoquinoline hydrobromide(7), 2-heptyl-6, 7-diacetoxy-1,2,3,4-tetrahydro isoquinoline hydrobromide (8), 2-octyl-6, 7-dimethyl-1, 2, 3, 4-tetrahydro-isoquinoline hydrobromide(9), 2-nonyl-6, 7-dimethyl-1, 2, 3, 4-tetrahydro-isoquinoline hydrobromide(10), 2-decyl-6, 7-dimethy-1, 2, 3, 4-tetrahydro-isoquinoline hydrobromide(11), 2-dodecyl-6, 7-dihydroxyl 1, 2, 3, 4-tetrahydro-isoquinoline hydrobromide(12), 2-tetradecyl-6, 7-dihydroxyl-1, 2, 3, 4-tetrahydro-isoquinoline hydrobromide(13), and 2-cetyl-6, 7-dihydroxyl-1,2,3,4-tetrahydro-isoquinoline hydrobromide(14). Compounds 5-14 were firstly reported. It was found that all the 14 compounds had anti-fungal activity and 6 compounds also showed sperm-killing activities, with compounds 11, 12 having the strongest activities. Conclusion: A group of novel compounds with both anti-fungal and contraceptive activities have been synthesized, which provide a precursor structure for developing new contraceptives with anti-fungal activities.

Objective To investigate the levels of transformation growth factor-β1 (TGF-β1),vascular endothelial growth factor (VEGF) and insulin growth factor-Ⅰ (IGF-Ⅰ) role in the pathogenesis of serum of patients with combined pulmonary fibrosis and emphysema (CPFE).Methods Recruited 20 patients with CPFE,40 cases with idiopathic pulmonary interstitial fibrosis (IPF) and 40 cases with emphysema who were admitted to our hospital during July 2011 to February 2012.Serum levels of TGF-β1,VEGF and IGF-Ⅰ were detected by ABC-ELISA.Results Serum levels of TGF-β1 and IGF-Ⅰ were significantly higher in patients with CPFE and IPF than these in patients with emphysema (TGF-β1:(160.73 ± 40.62) ng/L vs.(167.35 ± 42.82) ng/L vs.(128.75 ±35.77) ng/L; IGF-Ⅰ:(179.65 ±60.73) ng/L vs.(192.32 ±58.75) ng/L vs.(148.73 ±49.67) ng/L,P ＜ 0.05 or P ＜ 0.01).The IPF group had significantly higher serum level of VEGF than the emphysema group ((506.12 ±82.37) ng/L vs.(437.31 ±62.58) ng/L,P ＜0.01).Serum levels of TGF-β1 and IGF-Ⅰ in CPFE and emphysema groups were positively correlated (r =0.885,0.918 respectively,P ＜ 0.01).Smokers in the CPFE group had significandy lower level of serum VEGF than those who did no smoke ((406.19 ± 66.94) ng/L vs.(482.88 ± 79.91) ng/L,t =-2.287,P =0.035).Conclusion Serum level of VEGF increased significantly in the IPF group,suggesting the participation of VEGF in pulmonary interstitial fibrosis.IGF-Ⅰ involved in the pathogenesis of pulmonary interstitial fibrosis.TGF-β1 and IGF-Ⅰ have a positive linear regressive relationship,which indicates that they may work synergistically in the process of the fibrosis.

Objective To analyze the survival,brain metastases and health-related quality of life (HRQOL) for small cell lung cancer patients after prophylactic cranial irradiation(PCI).Methods From Aug 2007 to Apr 2011,42 small cell lung cancer patients were eligible for analysis.Overall survival rate was estimated by the Kaplan-Meier method.The HRQOL scores before and after PCI were compared by the nonparameter wilcoxon test.Results The median survival time from the start of PCI was 23 months(95％ CI,15.05-30.95),progression free survival time was 17 months (95％ CI,14.33-19.67),1-,2-and 3-year survival rates were 85.5％,45.8％ and 36.6％,respectively.The median time from PCI to brain metastases was 15 months(95％ CI,12.44-17.56),1-and 2-year brain metastases rates were 77.6％ and 54.1％.PCI had a little influence on HRQOL scales except for cognitive function.Conclusions For patients with limited stage small cell lung cancer who achieve complete or nearly complete remission after initial treatment as well as patients with extensive stage who respond to initial chemotherapy,PCI is effective in decreasing the rate of brain metastasis and improving survival,while the adverse effects is acceptable.There is no significant impact on HRQOL scales during short term.

Brain ; blood supply ; Fetus ; blood supply ; Heart Defects, Congenital ; diagnostic imaging ; Humans ; Infant, Newborn ; Middle Cerebral Artery ; diagnostic imaging ; Ultrasonography, Doppler, Color ; Ultrasonography, Prenatal

Aged ; Case-Control Studies ; Humans ; Male ; Malondialdehyde ; metabolism ; Middle Aged ; Oxidation-Reduction ; Serum ; metabolism ; Silicosis ; blood ; Superoxide Dismutase ; metabolism

Aristolochia ; chemistry ; poisoning ; Aristolochic Acids ; analysis ; isolation & purification ; poisoning ; Drugs, Chinese Herbal ; poisoning ; Poisoning ; prevention & control

Objective To explore the application value of 18F-fluorodeoxyglucose positron emission tomography/computed tomography (18 F-FDG PET/CT) and 99Tcm-methylene diphosphonate (99 Tcm-MDP) bone scintigraphy for detecting bone destruction in multiple myeloma (MM).Methods 18 F-FDG PET/CT and 99Tcm-MDP bone scintigraphy results of 27 MM patients were analyzed retrospectively.Inspection areas checked by magnetic resonance imaging (MRI) and X-ray were the limited scopes.The location and number of bone destruction were recorded,and the maximal standardized uptake value (SUVmax) was measured simultaneously.The results were comparatively analyzed.Diagnostic certainty regarding the presence or absence of bone destruction was evaluated according to the reference standard consisting of MRI and X-ray.Results A total of 235 lesions were found according to the reference standard.Of these,227 lesions (97％) were identified by 18F-FDG PET/CT,whereas 187 lesions (80％) were identified by bone scintigraphy,with a significant statistical difference (x2 =32.43,P ＜ 0.05).SUVmax was 8.3 ± 1.7 (4.3 to 18.9).The discovery rates of bone fracture of 18F-FDG PET/CT and bone scintigraphy were 100％ (97/97) and 90％ (87/97),and there was a significant statistical difference between them (x2 =78.09,P ＜ 0.05).Conclusion 18 F-FDG PET/CT is a possible method to detect bone lesions in patients with MM,and is better than 99Tcm-MDP bone scintigraphy.

Objective The purpose of this study was to investigate the knowledge，attitude and behaviors (KAB) of rural residents. Methods A correlative-descriptive design was used for the study. A cluster sampling of 1952 rural residents aged 18-60 years old in 8 villages of Lantian county was selected. Results The results showed as follows. The total correct rate of knowledge was 50.9%; 43.5% believed that the prevalence of HIV/AIDS in China indicated decline of the moral value; 71.3% never use condom when having sex in the past;There were positive relationships between knowledge and attitude,using condoms during sex and using condoms during first sex respectively (P<0.01). Conclusion The attitude and behavior on HIV/AIDS of the rural residents are largely determined by their knowledge.

BACKGROUND:Tracheal injury suture and the development of a new tracheal prosthesis all need to understand the tensile mechanical properties of tracheal cartilage.so as to repair and rebuild tracheal function.Previous researches on the biomechanics of artificial trachea are many reported.while the biomechanics of human tracheal cartilage is reported less.OBJECTIVE:To investigate the mechanical properties of tracheal cartilage using one-dimensional tensile test method.METHODS:Two fresh cadaver specimens of normal human trachea.with the informed consents of their families.were involved.The specimens were thaw at room temperature,and then tracheal cartilage specimens were cut using scalpel into 20 samples at the length of 25 mm,width 5 mm,thickness 1.8-2.2 mm.The 20 tracheal cartilage samples were subjected to one-dimensional tensile test with Shimadzu electronic universal testing machine Japan,at the tensile test speed of 5 mm/min.The tensile maximum load,maximum displacement,maximum stress,maximum strain,elastic modulus and stress-strain curve of the specimens were observed.RESULTS AND CONCLUSION:The maximum load of human cadaver tracheal cartilage was(60 946±10.377)N,maximumdisplacementwas(1.973±0.159)mm,maximum stresswas(6.229±1.125)Mpa,maximum strainwas(32.825±2.776)%.Tracheal cartilage stress-strain curves was changed along with the index,the initial low slope of the curye was due to the direction of imposed tension was similar with the arrangement of collagen structure,the steep slope represented the tensile strength of collagen.To describe the tracheal cartilage stress-strain relationship in a one-dimensional tension,15 stress-strain data of the tracheal cartilage experimental data adopted polynomial by the least square fitting method,to obtain stress(δ)-strain(ε)relationship forrnula:σ(ε)=-0.111 3e~5+1.602 1e~4-7.821 6e~3+17.995 1e~2+3.624e.It is indicated that tracheal cartilage has a strong capacity to bear Joad and resist deformation,reflecting their viscoelastic mechanical properties of both flexibility and viscosity,supporting that the mechanical properties of cartilage is positively related to cartilage collagen content.

A Review: A concept of tissue adaptation to hypoxia (i. e. hypoxic preconditioning) was developed and its corresponding animal models were reproduced in 1966s. The methods of model reproduction in rat, rabbit, and mouse in particular and the main results are briefly introduced in this review. The tolerance to hypoxia of preconditioned animals is significantly increased. Regular changes in animals' behavior, neurophysiology, respiratory and circulatory physiology, neuron morphology in vivo and function of brain and spinal cord in vitro are briefly demonstrated. The protective effects in vivo and in vitro of homogenate extract taken from the brain of preconditioned animals, neurochemicals and molecular neurobiological alterations are briefly presented. The essence and significance of tissue adaptation to hypoxia/hypoxic preconditioning are discussed in the review in terms of evolution and practical implication.
Animals ; Brain ; metabolism ; physiology ; Disease Models, Animal ; Hypoxia ; metabolism ; Mice ; Rabbits ; Rats