Objective To investigate the correlation between obstructive sleep apnea syndrome(OSAS)with myocardial ischemia and arrhythmia.Methods To observe the occuring rate of premature beats and change of ST- segment,90 eases of OSAS patients were detected by the polysomnogram(PSG)and dynamic electrocardiogram at the same time.Results Total morbidity of myocardial ischemia was 32.2 % in OSAS patients,and it was 59.4 %, 15.8 %,20 % in serious,moderate and mild groups respectively.There was a statistically significant difference be- tween the three groups and the control group(P0.05).Conclusion As one of the risky factors of cardiovascular diseases,OSAS can induce myocardial ischemia and arrhythmia.

Twenty-five compounds of novel quinoxaline-based scaffold with antiplatelet activity were designed and synthesized on the basis of previous quinoxaline analogues, and the structures were confirmed by ¹H NMR, ¹³C NMR, and MS. The antiplatelet activity was evaluated, structure-activity relationship (SAR) study was summarized and the selectivity of PAR4 was confirmed by calcium mobilization assays. It was indicated that compound 14a, 14g, 13i, 13p showed moderate activity against PAR4, especially, the activity of compound 14g (IC₅₀ = 0.26 μmol·L^-1) was 6.7 times than the lead compound A (IC₅₀ = 1.73 μmol·L^-1). Therefore, 2,3-dihydro-[1,4]dioxino[2,3-g]quinoxaline and [1,3]dioxolo[4,5-g]quinoxaline derivatives are promising compounds for the discovery of novel antiplatelet agents. It is worthy of further research to develop highly effective and selective PAR4 antagonists.

To develop an analytic method for qualitative and quantitative analysis of dodecatetraenamides A, B in 42 samples of two official species of Asari Radix et Rhizoma( ARR) (37 samples of Asarum heterotropoides var. mandshuricum with different collection time and 5 samples of Asarum sieboldiivar. seoulense). The HPLC-IT-TOF-MS/MS methods for the qualitative and UPLC-PDA methods for the quantitative analysis were established. Dodecatetraenamides A, B were identified by comparing the retention time, UV absorption spectrum and quasi-molecular ion peak [ M + H]+ with the reference compound using HPLC-IT-TOF-MS/MS. The content of dodecatetraenamides A and B in ARR were determined by UPLC-PDA. The separation was successfully carried out on a ACQUITY UPLC BEH C18 (2.1 mm x 100 mm, 1.7 µm) column eluted with mobile phases of water (A) and acetonitrile (B) in gradient program (0-3 min, 35% B; 3-5 min, 35%-36% B; 5-6 min, 36%-43% B; 6 min-11 min 43% B; 11-12 min, 43%-100% B). The column temperature was 45 °C, and the detection wavelength was set at 254 nm. The flow rate was 0.6 mL · min(-1). On one level mass spectrometry scanning, the results showed that the quasi-molecular ion [M + H] + of both dodecatetraenamides A and B were m/z 248.20. The quantitative method with UPLC-PDA has made the baseline separation of the constituents, which were reported as mixtures in the most literatures. The average recovery of dodecatetraenamides A and B were 97.90% and 99.86%, the relative standard deviation were 0.4% and 1.1%, respectively. The contents of dodecatetraenamides A, B in all ARR samples was in the range of 0.11-3.89 and 0.24-6.65 mg · g(-1). Their contents reduced with the extension of storage time. Compared with the samples of 2013, the average content of the two constituents in the samples collected in year 2002-2003 reduced 34% and 36%, respectively (P < 0.05). Compared the A. sieboldii var. seoulense and A. heterotropoides var. mandshuricum with the same collective time and production area, the average contents of the two constituents in latter were up to (1.59 ± 0.75) mg · g(-1) and (2.90 ± 1.17) mg · g(-1), respectively, significantly higher than that in A. sieboldii var. seoulense (dodecatetraenamide A were (0.78 ± 0.52) mg · g(-1), dodecatetraenamide B were (1.69 ± 0.83) mg · g(-1)) (P < 0.05). The content of the dodecatetraenamide A in overground part was in the range of 0.11-0.33 mg · g(-1), dodecatetraenamide B was 0. 24-0.60 mg · g(-1), which were much lower than that of the underground part of ARR (dodecatetraenamide A was in the range of 0.73-3.89 mg · g(-1), dodecatetraenamide B was 2.11-6.24 mg · g(-1)). The method was certified to be simple, accurate and reliable and could be used for qualitative and quantitative analysis of dodecatetraenamide A and B in different species of ARR, also can be used for the comprehensive quality control of traditional Chinese medicine, Asari Radix et Rhizoma.
Amides ; chemistry ; Asarum ; chemistry ; Chromatography, High Pressure Liquid ; Drugs, Chinese Herbal ; chemistry ; isolation & purification ; Mass Spectrometry ; Molecular Structure ; Rhizome ; chemistry

OBJECTIVETo examine the influence of vascular endothelial growth factors (VEGF) in controlling the growth of an experimental osteosarcoma in mice by performing retrovirus-mediated sFlt-1 gene modification.

METHODSFrom March to October 2010 human osteosarcoma G-292 cells were in vitro infected with retroviral vectors encoding soluble Flt-1 or LacZ gene before transplanted into proximal tibiae of immune deficient SCID mice to establish experimental orthotopic osteosarcoma. Daily observation and biweekly microCT were performed to monitor tumor development and progression till sacrifice at 8 weeks after tumor cell inoculation for histological and molecular analyses.

RESULTSSuccessful transgene expression was confirmed in the culture media of sFlt-1 transduced G-292 cells using ELISA, and with positive X-gal staining of the LacZ transduced cells. Noteworthy tumors were grown in all mice on the tibiae receiving G-292 cell inoculation, with clear detection on microCT images starting 2 weeks after inoculation. Over the time period, tumors derived from sFlt-1 transduced G-292 cells were distinctively smaller in size compared to the ones from wide-type G-292 and G-292-LacZ cells. Histology showed typical osteosarcoma characteristics including severe cellular pleomorphism, bone erosions, and neo-vascularization. Real-time polymerase chain reaction indicated significantly higher sFlt-1 expression in sFlt-1 transduced groups than the wild-type G-292 or LacZ treated groups. Strong expression of oncogenes c-myc and c-fos were also obvious, along with the expression of VEGF in the primary tumor tissue.

CONCLUSIONRetrovirus-mediated sFLT-1 gene modification decelerates the osteosarcoma tumor growth in this murine model.

Animals ; Bone Neoplasms ; genetics ; metabolism ; pathology ; Cell Line, Tumor ; Female ; Genetic Vectors ; Humans ; Lac Operon ; Mice ; Mice, SCID ; Neovascularization, Pathologic ; metabolism ; pathology ; Osteosarcoma ; genetics ; metabolism ; pathology ; Retroviridae ; genetics ; Transgenes ; Vascular Endothelial Growth Factor A ; metabolism ; Vascular Endothelial Growth Factor Receptor-1 ; metabolism

OBJECTIVETo investigate the impact of intrauterine infection induced by LPS injection on long-term brain development of premature rats.

METHODSEighteen day-gestation pregnant rats were randomly assigned to a control group receiving an intraperitoneal injection of normal saline, and two infection groups that were intraperitoneally injected with 0.3 mg/kg or 0.6 mg/kg LPS. Twenty-four hours after injection, 7 pregnant rats of each group were sacrificed. The pathological changes of the placenta after hematoxylin and eosin staining were observed under a light microscope. The neural cell apoptosis of fetal brains was examined by the TUNEL assay. The remained pregnant rats were induced to labour before 21 gestation days. The long-term brain development of premature rats was tested with the Y type electric maze on postnatal day 42.

RESULTSObvious pathological changes were observed in the placenta in the infection groups. The apoptotic neural cells in the fetal brain increased in the infection groups compared with that in the control group (32.41+/-5.36 in the 0.3 mg/kg infection group and 66.41+/-7.61 in the 0.6 mg/kg infection group vs 8.00+/-0.36 in the control group; P<0.01). The number of trials to criterion in the Y type maze test in the infection groups was much more than that in the control group [117.8+/-8.7 (0.3 mg/kg infection group) and 194.4+/-13.7 (0.6 mg/kg infection group) vs 56.8+/-3.7 (control group); P<0.01]. The number of correct reactions in memory retaining in the infection groups was lower than that in the control group (0.62+/-0.09 in the 0.3 mg/kg infection group and 0.37+/-0.09 in the 0.6 mg/kg infection group vs 0.92+/-0.06 in the control group; P<0.05).

CONCLUSIONSIntrauterine infection can cause fetal rats' neural cell apoptosis and affect adversely long-term brain development of neonatal rats.

Animals ; Apoptosis ; Bacterial Infections ; physiopathology ; Blood-Brain Barrier ; Brain ; growth & development ; pathology ; Female ; Maze Learning ; Neurons ; pathology ; Pregnancy ; Pregnancy Complications, Infectious ; physiopathology ; Rats ; Rats, Wistar ; Uterus ; microbiology

BACKGROUNDMultiple epiphysis dysplasia (MED) is a common skeletal dysplasia with a significant locus heterogeneity. In the majority of clinically defined cases, mutations have been identified in the gene encoding cartilage algometric matrix protein (COMP).

METHODSFive patients were included in the study. Linkage analysis and mutation analysis of the COMP gene were conducted in the patients and their family members.

RESULTSWe have identified a novel mutation in axon 14 of COMP gene in the family.

CONCLUSIONSThis mutation produced a severe MED phenotype with marked short stature, early onset osteoarthritis, and remarkable radiographic changes. Our results extended the range of disease-causing mutations in COMP gene and contributed more information about relationship between mutations and phenotype.

Adolescent ; Asian Continental Ancestry Group ; Cartilage Oligomeric Matrix Protein ; genetics ; Female ; Humans ; Male ; Osteochondrodysplasias ; genetics ; Pedigree ; Point Mutation ; genetics

OBJECTIVETo evaluate the association between vasectomy and prostate cancer.

METHODSWe searched comprehensively the databases, CBMDisc, CMCC, CMAC, CNKI (from 1978 to January 6, 2009), and PubMed (from 1965 to January 6, 2009) using the key words "vasectomy" and "prostate cancer", screened the retrieved literature according to the inclusion and exclusion criteria, performed a Meta-analysis with the software RevMan 4.2 after identification of the relevant data, and calculated the overall pooled OR (95% CI) as well as that of the association of prostate cancer with <20 and > or =20 yr vasectomy.

RESULTSA total of 20 088 cases and 232 506 controls in 27 reports (7 cohort and 20 case-control studies) were included in this investigation. The overall pooled OR (95% CI) was 1.10 (0.97-1.24), and those of <20 and > or =20 yr vasectomy were 0.94 (0.83-1.06) and 1.05 (0.90-1.23), respectively.

CONCLUSIONNo existing literature show any positive association between vasectomy and prostate cancer.

Humans ; Male ; Prostatic Neoplasms ; epidemiology ; etiology ; Risk Factors ; Vasectomy ; adverse effects

OBJECTIVETo investigate the relationship of seminal plasma levocarnitine with sperm concentration, vitality and motility.

METHODSEnrolled in this study were 64 infertile men, who were divided according to the results of routine sperm tests into a normozoospermia (n = 12), an oligozoospermia (n = 16), an asthenozoospermia (n = 20) and an oligoasthenozoospermia group (n = 16). The level of seminal plasma levocarnitine was detected by LC-MS-MS, the concentration of seminal plasma testosterone measured by chemiluminescence immunoassay, the correlation of seminal plasma levocarnitine with sperm concentration, motility and vitality determined by bivariate correlation analysis with SPSS15.0, and so was the correlation between the carnitine and sperm concentration by partial correlation analysis with seminal plasma testosterone as a control variable to exclude the influence of testosterone.

RESULTSThe concentrations of total seminal plasma levocarnitine, free seminal plasma levocarnitine and seminal plasma acetolevocarnitine were (91.33 +/- 40.49) mg/L, (40.89 +/- 24.13) mg/L and (50.44 +/- 21.90) mg/L; the Pearson coefficients of correlation of the levocarnitine level with sperm motility, vitality and concentration were 0.161 (P = 0.235), 0.114 (P = 0.370) and 0.637 (P < 0.001), those of free seminal carnitine with sperm motility and vitality were 0.325 (P = 0.024) and 0.316 (P = 0.029), respectively, with the oligozoospermia group excluded, and that of partial correlation between the concentrations of seminal levocarnitine and sperm was 0.641 (P < 0.001).

CONCLUSIONThe level of seminal plasma levocarnitine is positively correlated with sperm motility and vitality, and more significantly with sperm concentration.

Adult ; Carnitine ; analysis ; Humans ; Infertility, Male ; physiopathology ; Male ; Semen ; chemistry ; cytology ; Sperm Count ; Sperm Motility ; physiology ; Spermatozoa ; cytology ; physiology ; Young Adult

OBJECTIVETo evaluate the efficacy and safety of Capsule metadoxine in the treatment of alcoholic liver disease.

METHODSA randomized double blind multicenter placebo-controlled clinical study was performed to evaluate the therapeutic effectiveness and safety of capsule metadoxine. Patients in metadoxine group received capsule metadoxine 500mg tid po. Patients in placebo group received placebo 2 pillows tid po. The treatment duration was 6 weeks. Patients were followed up 2 weeks after the treatment. Patients were visited once every 3 weeks during the treatment period. Clinical symptoms and liver function were evaluated in all the patients before treatment, at week 3, week 6 and 2 weeks after therapy. CT scan was done in some patients before treatment and at the end point of therapy.

RESULTS254 patients were recruited in the study, 126 in metadoxine group and 128 in placebo group. Median ALT, AST, GGT level in metadoxine group were decreased from 80.0 U/L, 59.2 U/L, 123.0 U/L (before treatment) to 41.1 U/L, 36.0 U/L, 57.0 U/L (after 6 weeks therapy). The improvement in liver function was more significant in metadoxine group than in placebo group (P less than 0.05). For the patients who stopped drinking during the study, the total effective rate of improvement in liver function was 82.8% in metadoxine group, much higher than that in placebo group (55.7% , P=0.0000). For the patients who did not stop drinking during the study, the total effective rate of improvement in liver function was 65.4% in metadoxine group, which is not significantly higher than that in placebo group (44.8%, P=0.1767). The CT value ratio of liver to spleen was significantly improved in metadoxine group (P=0.0023), and there was no significant difference between the two groups (P=0.6293). The rate of adverse was 1.6% in both of groups.

CONCLUSIONCapsule metadoxine is an effective and safe treatment for alcoholic liver disease.

Administration, Oral ; Adult ; Aged ; Alanine Transaminase ; blood ; Alcohol Deterrents ; administration & dosage ; therapeutic use ; Analysis of Variance ; Aspartate Aminotransferases ; blood ; Capsules ; Double-Blind Method ; Drug Combinations ; Fatty Liver, Alcoholic ; blood ; drug therapy ; pathology ; Female ; Follow-Up Studies ; Humans ; Liver ; diagnostic imaging ; pathology ; Liver Diseases, Alcoholic ; blood ; drug therapy ; pathology ; Liver Function Tests ; Male ; Middle Aged ; Pyridoxine ; administration & dosage ; therapeutic use ; Pyrrolidonecarboxylic Acid ; administration & dosage ; therapeutic use ; Treatment Outcome ; Ultrasonography ; Young Adult ; gamma-Glutamyltransferase ; blood

AIMTo investigate the pharmacokinetics of hylotelephin in Beagle dogs and obtain the main pharmacokinetic parameters.

METHODSAn HPLC method with UV detection was developed to study the pharmacokinetics of hylotelephin in dogs by joining an internal standard (anthracene). Benzoyl chloride was used to the pre-column derivatization of hylotelephin and methanol-water (64:36) was used as the mobile phase. According to the 3P97 pharmacokinetic program, the main parameters were calculated.

RESULTSThe hylotelephin pharmacokinetics conforms to a two-compartment open model after a single iv dose of hylotelephin 10.6 or 21.3 mg x kg(-1) in Beagle dogs. The parameters of two groups were as follows: T(1/2) alpha were 2.3 and 2.1 min, T(1/2) beta were 1.9 and 2.0 h, K12 were 0. 12 and 0.11 min, K21 were 0.17 and 0.21 min, K10 were 0.011 and 0.0094 min, Vc were 0.54 and 0.54 L x kg(-1), AUC were 1.8 and 4.1 g x min x L(-1), CL were 0.0048 and 0.0056 L x kg(-1) x min(-1), MRT were 2.10 and 2.4 h, respectively.

CONCLUSIONThe pharmacokinetics of hylotelephin after iv administration showed a rapid distribution and elimination process in Beagle dogs and was of first order kinetics.

Animals ; Antiviral Agents ; chemistry ; isolation & purification ; pharmacokinetics ; Area Under Curve ; Chromatography, High Pressure Liquid ; Crassulaceae ; chemistry ; Dogs ; Female ; Heterocyclic Compounds, 3-Ring ; chemistry ; isolation & purification ; pharmacokinetics ; Male ; Molecular Structure ; Plants, Medicinal ; chemistry ; Spectrophotometry, Ultraviolet