Photoaffinity labeling is widely applied to demonstrate targets of small molecule ligands. In this paper, biotin photoaffinity labeled molecule with propargyl group 1 has been designed and synthesized, followed it's labeling of N2-acetyl-2'-O-propargyl guanosine 9 by "click chemistry". This technology presents delight development potential in labeling of second messenger cyclic nucleotide, antisense oligonucleotide or siRNA.
Biotin ; chemistry ; Click Chemistry ; Guanosine ; chemical synthesis ; chemistry ; Ligands ; Photoaffinity Labels

Antigens, Neoplasm ; analysis ; Carcinoma, Hepatocellular ; chemistry ; Humans ; Liver Neoplasms ; chemistry

OBJECTIVETo compare the features of brain injury in neonatal rats with different severities of hypoxia-ischemia (HI), and explore the role of microglial activation and cytokines.

METHODSOne hundred and twenty 7-day-old rats were randomized to three groups: sham control, mild HI, and severe HI. The rats in the HI groups were subjected to right carotid artery occlusion and 8% oxygen hypoxia exposure (40 minutes, 34.5 Celsius degree in the mild HI group; 65 minutes, 35.5 Celsius degree in the severe HI group). MRI, microtubule associated protein (MAP2) and TUNEL staining were used to confirm the severity of brain injury. Changes in expression of activated microglia (ED1) and signs of cytokine involvement or oxidative stress (TNF-alpha, nitrotyrosine) were assessed immunohistochemically.

RESULTSIn the mild HI group, MRI scans demonstrated increased T2 values in the ipsilateral subcortical white matter and a slight loss of T2 values in the cortex, corresponding to a medium loss of MAP2 in the ipsilateral cortex. There was an increase in the number of TUNEL positive cells compared to the control group within the subcortical white matter. In the severe HI group, the T2 value increased in the majority of the hemisphere, corresponding to a severe loss of staining for MAP2 in the ispilateral hemisphere. The number of TUNEL positive cells significantly increased in the ipsilateral cortex and white matter. In the mild HI group, ED1, TNF-alpha and nitrotyrosine expression increased only in the acute stage and was only observed in subcortical white matter. In contrast, after severe HI, the increase in ED1, TNF-alpha and nitrotyrosine expression was observed in the whole ipsilateral hemisphere and prolonged for weeks.

CONCLUSIONSFollowing a mild HI a relatively selective white matter injury compares to the pannecrosis in the cortex and white matter following a severe HI. Microglial activation and over-expression of cytokines might contribute to the development of hypoxic-ischemic brain damage.

Animals ; Animals, Newborn ; Apoptosis ; Hypoxia-Ischemia, Brain ; etiology ; metabolism ; pathology ; Magnetic Resonance Imaging ; Microglia ; pathology ; Microtubule-Associated Proteins ; analysis ; Rats ; Tumor Necrosis Factor-alpha ; analysis ; Tyrosine ; analogs & derivatives ; analysis

BACKGROUNDPhacoemulsification yields successful outcomes in eyes with standard cataract. Though techniques have been improved, it is still challenging to perform phacoemulsification in cases of hard cataracts for difficulty in nuclear management and much more complications. This study aimed at describing and evaluating the efficacy and safety of a peripheral radial chop technique to remove hard cataracts.

METHODSIn this prospective study conducted between January 2003 and January 2004, 107 consecutive eyes with hard cataract underwent modified phacoemulsification surgery with peripheral radial chop technique by the Bausch & Lomb Millennium phacoemulsifier with preset parameters of power less than 30%; vaccum, 150 mmHg; and bottle height, 85 cm when a DP8145 phaco tip was used, and vaccum, 380 mmHg; bottle height, 95 cm when a DP8245 phaco tip was used.

RESULTSThe mean ultrasonic power was 14.7% (range 9% to 19%), ultrasonic time was 1.98 minutes (range 1.55 to 3.18 minutes). At 1, 7 and 30 days postoperatively, the eyes with uncorrected visual acuity 0.5 or better accounted for 76.42%, 87.16% and 90.67% respectively. At 1 month, the endothelial cell loss rate was 9.74% (range 8% to 17%). There were 6 cases of posterior capsule rupture in an early period of study. No serious intraoperative or postoperative complications were noted.

CONCLUSIONSThe peripheral radial chop technique was effective without serious complications in hands of an experienced surgeon.

Aged ; Female ; Humans ; Male ; Middle Aged ; Phacoemulsification ; adverse effects ; methods ; Prospective Studies

The present study aims to investigate the lignan constituents from Sambucus williamsii and their proliferation effects on osteoblast-like UMR106 cells. Seven compounds were isolated and purified by macroporous resin D101, silica gel, Sephadex LH-20, Toyopearl HW-40, ODS column chromatographies and Preparative HPLC(C-18). Their structures were elucidated by spectroscopic methods as threo-guaiacylglycerol-beta-0-4'-conifery ether (1), lirioresinol A (2), 1-hydroxypinoresinol (3), 5-methoxybalanophonin (4), balanophonin (5), 5-methoxy-trans-dihydrodehydrodiconiferyl alcohol (6), and p-hydroxybenzaldehyde (7). Compounds 3-7 were obtained from this genus for the first time. The proliferation effects of all isolated compounds on osteoblast-like UMR106 cells were determined. Compounds 1-7 (1 x 10(-12)-1 x 10(-7) mol x L(-1)) increased UMR106 cell proliferation to some extent.
Cell Line ; Cell Proliferation ; drug effects ; Lignans ; isolation & purification ; pharmacology ; Osteoblasts ; cytology ; drug effects ; Plant Stems ; chemistry ; Sambucus ; chemistry

OBJECTIVE: To investigate the relationship among perceived stress,sleep and fatigue status; and to analyze the effect of sleep status in mediating and regulating perceived stress and fatigue status in soldiers that were acutely exposed to high altitude for the first time. METHODS: A total of 700 soldiers that were acutely exposed to high altitude for the first time were investigated with convenient sampling. They were evaluated using Perceived Stress Scale,Sleep Status Self-evaluation Test,and Fatigue Scale-14. The mediating effect was analyzed by structural equation model,and the moderating effect was analyzed by hierarchical regression analysis. RESULTS: The total score of fatigue among soldiers that often took part in recreational activities was significant lower than that who did not( P < 0. 01). The total score of fatigue among soldiers that had training injury was significant higher than that who had not( P < 0. 01). The total score of fatigue among soldiers that had high training expectations was significant higher than that that didn't have high training expectations( P < 0. 01). Sleep status,sense of overload and training expectations had remarkable predicting effect on fatigue status among soldiers that were acutely exposed to high altitude for the first time( P < 0. 01). Sleeping status has a complete mediating effect on the sense of prediction,sense of overload and fatigue status( P < 0. 01),and has a moderating effect on the sense of control,sense of overload and fatigue status( P < 0. 01). CONCLUSION:s Perceived stress and sleeping status had close relationship with fatigue status among soldiers that were acute exposed to high altitude for the first time. Sleeping status has intermediary and regulating effect between senses of overload and fatigue state.

OBJECTIVETo study the plasma protein binding rate of methyl protodioscin.

METHODThe ultrafiltration was employed to determine the plasma protein binding rate of methyl protodioscin. The plasma concentrations of methyl protodioscin were measured by HPLC-MS-MS.

RESULTThe plasma protein binding rate of methyl protodioscin with rat plasma at the concentration of 20.0, 100 and 200 microg x mL(-1) were (94.6 +/- 0.16)%, (91.6 +/- 0.35)% and (86.10 +/- 0.60)%, respectively, while the plasma protein binding rate of methyl protodioscin with normal human plasma at the above concentrations were (82.11 +/- 5.12)%, (84.54 +/- 0.32)% and (88.52 +/- 1.02)%, respectively.

CONCLUSIONThe binding rate of methyl protodioscin with plasma protein is high.

Animals ; Antineoplastic Agents ; metabolism ; Blood Proteins ; metabolism ; Calibration ; Chromatography, High Pressure Liquid ; Diosgenin ; analogs & derivatives ; metabolism ; Female ; Humans ; Male ; Protein Binding ; Rats ; Saponins ; metabolism ; Sensitivity and Specificity ; Tandem Mass Spectrometry ; Ultrafiltration

OBJECTIVETo study effects of hypericin associated with light irradiation on human laryngeal squamous cell carcinoma strain Hep-2.

METHODSUsing techniques of tumor cells culture in vitro, Hep-2 cells were exposed to different concentration hypericin as 0.5, 1.0, 2.0, 3.0, 5.0 microg/ml, then 10 minutes 7.5 J/cm2 light irradiation was given after an hour. Other groups Hep-2 culture cells were also exposed to different concentration hypericin as 5.0, 10.0, 20.0, 25.0 microg/ml, without light irradiation. In all groups, contrast groups were set up. And 48 hours later, growth characteristics of Hep-2 cells were studied by morphological observation, fluorescence microscope, MTT assay and flow cytometry.

RESULTSIn normal contrast group, Hep-2 cells grew intensively and contacted with each other. However, cells which were treated with hypericin, combination with light irradiation were declined greatly. In higher dose hypericin group, necrosis could be found. MTT assay showed that hypericin associated with light irradiation inhibited growth of laryngeal cell with dose dependence manner. Flow cytometry showed that hypericin with light irradiation could block cell growth at G0/G1 phase, inducing apoptosis of laryngeal cell. Under fluorescence microscope, some sings of cell apoptosis including coagulation of chromatin, fragmentation of nuclei and apoptotic body could be found.

CONCLUSIONHuman laryngeal squamous cell carcinoma strain Hep-2 can be inhibited and induced into apoptosis by treated with hypericin combination with light irradiation.

Apoptosis ; drug effects ; radiation effects ; Carcinoma, Squamous Cell ; pathology ; Cell Proliferation ; drug effects ; radiation effects ; Hep G2 Cells ; Humans ; Laryngeal Neoplasms ; pathology ; Light ; Perylene ; analogs & derivatives ; pharmacology

Objective To explore the relationships between training burnout , body mass index (BMI), fasting plasma glucose ( FPG) and blood lipids of soldiers .Methods A total of 140 soldiers stationed in Xinjiang who had received intensive behavioral stress training before entering the plateau ( referred to as the "great intensity training") were studied by the integrated method of a questionnaire survey with test in situ .The questionnaire was a self-compiled soldiers′training burnout questionnaire ,in which BMI , FPG, and blood lipids were the observation indices .The relationships between the indices and training burnout were analyzed by linear regression analysis .Results The total score of training burnout and scores of training alienation among soldiers were significantly increased after high intensity training (P<0.01).While the values of FPG, TC, TG and BMI among soldiers were significantly decreased after high intensity training (P<0.05, P<0.01).After high intensity training, the total scores of training burnout and score of training alienation among overweight soldiers were significantly compared to higher than those who had normal BMI (P<0.05, P<0.01).After high intensity training, the total score of training burnout and scores of physical and mental exhaustion and training alienation among soldiers that had high levels of FPG were significantly increased those who had low levels of FPG (P<0.01).And the total score of training burnout and scores of physical and mental exhaustion and training alienation among soldiers that had high levels of cholesterol were significantly higher than those of soldiers who had low levels of cholesterol (P<0.01).Regres-sion analysis showed that there was a linear regression relationship between physical and mental exhaustion , training aliena-tion on one hand, and BMI, FPG, total cholesterol (TC),and triglycerides (TG) on the other hand among soldiers before and after intensive training (P<0.05, P<0.01).Conclusion Physical and mental exhaustion are important influencing factors of FPG and TC, while training alienation is an important influencing factor of TC and TG .

OBJECTIVETo observe the pathological and clinical characters of nonalcoholic steatohepatitis (NASH).

METHODSLiver biopsy tissues taken from 97 patients negative for common viral detection with serological test and immunohistochemistry as well as in situ hybridization, were observed by routine light microscopic examination. And the clinical data of patients with NASH was analyzed.

RESULTSAmong the chronic hepatitis patients with unknown etiology, the detection rate of NASH was 15.5% (15/97). The characteristic lesions in NASH patients included macrovesicular steatosis in zone 3 of lobules, hepatocytes ballooning degeneration, lobules diffused with acute and chronic inflammation, and perisinusoidal fibrosis. Grading and staging according to Brunt's method, histological lesions could be accounted for G1S1 in 7 patients, G2S2 in 3 patients, G3S1 in 4 patients and G3S2 in 1 patient. There were 14 patients with mild to moderate elevation of transaminase, 10 with hyperlipemia, 8 with diabetes and 9 with fatty liver by ultrasonography.

CONCLUSIONNonalcoholic steatohepatitis is a common form of unknown etiology chronic liver disease with certain clinic-pathological features.

Adult ; Biopsy ; Fatty Liver ; pathology ; Female ; Humans ; Liver ; pathology ; Male ; Middle Aged