OBJECTIVE：To establish the method for content determination of 17 kinds of amino acids in Sargassum and its adulterants，and to carry out cluster analysis ，so as to provide reference for quality control of Sargassum. METHODS ：Totally of 18 batches of sample （S1-S6 as certified product ，S7-S18 as adulterants ）were collected. After acid hydrolysis ，amino acids contents were detected by using automatic amino acid analyzer. The separation was performed on LCAK 06/Na sulfonic acid cation exchange resin column with mobile phase consisted of buffer-regeneration system （gradient elution ）at the flow rate of 0.45 mL/min （elution pump ）and 0.25 mL/min（derivative pump ）. The detection wavelengths were set at 440 nm（proline）and 570 nm（other amino acids ），and the sample size volume was 50 μL. PASW Statistics 18.0 software was used ，and cluster analysis was conducted by using group connection method of cluster analysis with “square Euclidean distance ”as the measurement standard. RESULTS ：17 kinds of amino acids were well separated without interference from blank sample. The linear relationship between mass concentration and peak area was good （all r were over 0.998），and the upper and lower limits of the linear range were 48.06 μg/L （cystine）and 1.501 μg/L（glycine），respectively；RSDs of precision ，reproducibility and stability tests were lower than 2％. The average recoveries were between 90.60％-101.56％（RSDs were 0.88％-2.15％，n＝6）. 17 kinds of amino acids were detected in Sargassum and its adulterants ，among which the contents of glutamic acid ，aspartic acid ，leucine，alanine，glycine and valine were relatively high . Results of cluster analysis showed that 18 batches of sample were clustered into 4 categories，i.e. S 1-S6 into one category；S7-S9 into one category ；S10-S12，S16-S18 into one category ；S13-S15 into one category ；which was consistent with the identification result of Sargassum and its adulterants . CONCLUSIONS ：The method is simple ， rapid， accurate and reproducible，and can be used for the quantitative analysis and identification of amino acids in Sargassum and adulterants.

For drinking water security the German waterworks proceed on a comprehensive concept, i.e., the protection of all the regions from the recharge area to the client. It includes the protection of the recharge area by a precautionary management, a safe water treatment, a strict maintenance of the water distribution network, continuous control and an intensive training of staff. Groundwater protection zones together with effective regulations and control play a very important role. Three protection zones with different restrictions in land-use are distinguished. Water in reservoirs and lakes is also protected by Surface Water Protection Zones. Within the surrounding area the land-use is controlled, too. Special treatment is necessary if acidification happens caused by acid rain, or eutrophication caused by the inflow of sewage. Very important is the collaboration between waterworks and the farmers cultivating land in the recharge area in order to execute water-protecting ecological farming with the aim to reduce the application of fertilizers and plant protection agents. Probable financial losses have to be compensated by the waterworks.
Ecology ; Germany ; Water Pollutants ; isolation & purification ; Water Pollution ; prevention & control ; Water Purification ; methods ; Water Supply ; analysis

Worldwide, several regions suffer from water scarcity and contamination. The infiltration and subsurface storage of rain and river water can reduce water stress. Artificial groundwater recharge, possibly combined with bank filtration, plant purification and/or the use of subsurface dams and artificial aquifers, is especially advantageous in areas where layers of gravel and sand exist below the earth's surface. Artificial infiltration of surface water into the uppermost aquifer has qualitative and quantitative advantages. The contamination of infiltrated river water will be reduced by natural attenuation. Clay minerals, iron hydroxide and humic matter as well as microorganisms located in the subsurface have high decontamination capacities. By this, a final water treatment, if necessary, becomes much easier and cheaper. The quantitative effect concerns the seasonally changing river discharge that influences the possibility of water extraction for drinking water purposes. Such changes can be equalised by seasonally adapted infiltration/extraction of water in/out of the aquifer according to the river discharge and the water need. This method enables a continuous water supply over the whole year. Generally, artificially recharged groundwater is better protected against pollution than surface water, and the delimitation of water protection zones makes it even more save.
Filtration ; Fresh Water ; analysis ; Water Purification ; instrumentation ; methods ; Water Supply

This study was conducted to investigate the chemical constituents in the root of Dysosma versipellis (Hance) M. Cheng. The constituents were isolated by silica gel, lichroprep RP-C₁₈ and pharmadex LH-20 column chromatography and the IR, MS, NMR, 2D-NMR spectroscopic analysis were employed for the structural elucidation. Ten compounds were isolated from the 95% ethanol extract of Dysosma versipellis, their structures were elucidated as dysoverine D (1), dysoverine F (2), dysoverine A (3), podoverine A (4), α-peltatin (5), rutin (6), kaempferol-3-O-β-D-glucopyranoside (7), quercetin-3-O-β-D-glucopyranoside (8), kaempferol (9) and quercetin (10). Compound 2 is a new compound, and compounds 1 and 3-6 were isolated from this plant fo r the first time.

OBJECTIVE：To i nvestigate the metabolism stabilities of novel hypoglycemic compound LSM- 13 in rat liver microsomes，and to analyze the possible metabolites. METHODS ：LSM-13 was dissolved in rat liver microsome incubation system initiated by reduced nicotinamide adenine dinucleotide phosphate ，and was incubated in water at 37 ℃. The reaction was terminated with acetonitrile at 0，5，10，15，30，45 and 60 min，respectively. Using indomethacin as internal standard ，the concentration of LSM-13 in incubation system was determined by HPLC. The residual percentage and enzyme kinetic parameters of LSM- 13 were calculated at different incubation time points with the concentration of LSM- 13 incubated for 0 min as reference. UPLC-Q-TOF/MS was used to analyze and speculate the metabolites of LSM- 13 in rat liver microsomes. RESULTS ：After 60 min incubation ，the remaining percentage of LSM- 13 was（56.07±0.95）％，the half-life was 42.78 min，and the intrinsic clearance was 0.032 4 mL/（min·mg）. Compared with total ion flow diagram of rat liver microsome blank samples ，three chromatographic peaks were added in the samples incubated for 60 min；the corresponding molecular ion peaks were m/z 505.133 8，417.102 4，293.111 7 [M+H]+；the possible metabolites may be dehydrogenation ，O-debentylation and hydrolysis products of LSM- 13. CONCLUSIONS ： The compound LSM- 13 has moderate stability in rat liver microsomes ，and may undergo dehydrogenation ，O-debentylation and hydrolysis.

OBJECTIVE：To establish the metho d for the concentration det ermination of foretinib derivative LWK- 126 in liver microsomes，and to study its metabolism stability in liver microsomes of rats ，Beagle dogs and human. METHODS ：In the in vitro incubation system of liver microsomes ，LWK-126 was dissolved in liver microsomal incubation systems of rats ，Beagle dog and human initiated by reduced nicotinamide adenine dinucleotide phosphate solution. After incubation in water at 37 ℃ for 0，5，10，20， 30 and 60 min，the reaction was terminated with acetonitrile containing internal standard （1 μg/mL tolbutamide）. UPLC-MS/MS method was applied to determine the concentration of LWK- 126 in the incubation systems. The determination was performed on Waters BEH C 18 column with mobile phase consisted of water （containing 0.1％ formic acid ）-acetonitrile（containing 0.1％ formic acid）by gradient elution at the flow rate of 0.4 mL/min. The column temperature was 30 ℃，and the sample size was 2 μL. The mass spectral analysis was performed in a positive electrospray ionization mode ，and the full MS experiment was run with the selective reaction monitoring mode with a scanning range of m/z 50→1 200. Taking the concentration of LWK- 126 at 0 min as reference，the remaining percentage and the enzyme kinetic parameters were calculated. RESULTS ：The linear range of LWK- 126 was 0.05-15 μg/mL（R 2＝0.999 2）；the lower limit of quantification was 0.05 μg/mL，and the lowest detection limit was 0.01 μg/mL. The precision，accuracy，extraction recovery and matrix effect all met the analysis requirements of biological samples. The remaining percentage of LWK- 126 in liver microsomes of human ，rats and Beagle dogs for 60 min were （33.17±4.52）％，（3.14± 6.73）％，（1.38±5.85）％；t1/2 of them were 33.15，11.76，5.62 min；the clearance rates were 38.45，118.81，245.76 μL（/ min·mg）， respectively. CONCLUSIONS ：The method for the content ； determination of LWK- 126 in liver microsomes is established successfully. The order of metabolic stability of LWK- 126 in 〔2016〕4015） liver microsomes of different species is human ＞rats＞Beagle dogs.

BACKGROUND/AIMS: The increase in the prevalence of obesity is attributed to increased food intake and decreased physical activity in addition to genetic factors. Altered gut functions have been reported in obese subjects, whereas, little is known on the possible alterations in brain-gut interactions in obesity. The aim of the study was to explore possible alterations in gastric myoelectrical activity, gastric emptying, autonomic functions and central neuronal responses to gastric stimulations in diet-induced obese rats. METHODS: Gastric myoelectrical activity, gastric emptying and heart rate variability were recorded in lean and obese rats; extracellular neuronal activity in the ventromedial hypothalamus and its responses to gastric stimulations were also assessed. RESULTS: (1) Gastric emptying was significantly accelerated but gastric myoelectrical activity was not altered in obese rats; (2) the normal autonomic responses to feeding were absent in obese rats, suggesting an impairment of postprandial modulation of autonomic functions; and (3) central neuronal responses to gastric stimulations (both balloon distention and electrical stimulation) were blunted in obese rats, suggesting impairment in the brain-gut interaction. CONCLUSIONS: In diet-induced obese rats, gastric emptying is accelerated, postprandial modulations of autonomic functions is altered and central neuronal responses to gastric stimulations are attenuated. These alterations in peripheral, autonomic and brain-gut interactions may help better understand pathogenesis of obesity and develop novel therapeutic approaches for obesity.
Animals ; Central Nervous System ; Eating ; Electric Stimulation* ; Gastric Emptying ; Gastrointestinal Motility ; Heart Rate ; Hypothalamus ; Motor Activity ; Obesity ; Prevalence ; Rats*

AIMTo find new peroxisome proliferator-activated y agonists with high activity and low toxicity.

METHODSBased on JTT-501 and JTT-20993, new isoxazolidine-3,5-dione and noncyclic 1,3-dicarbonyl compounds were designed and synthesized. Their insulin-sensitizing activities were evaluated.

RESULTSEight new compounds were obtained. The structures of synthesized compounds were characterized by NMR, MS and IR. Four compounds (1A-4A) showed insulin-sensitizing activities.

CONCLUSIONCompounds (1A and 3A) showed excellent insulin-sensitizing activities and should be worth further investigation.

3T3-L1 Cells ; Animals ; Glucose ; metabolism ; Hypoglycemic Agents ; agonists ; chemical synthesis ; pharmacology ; Insulin ; pharmacology ; Isoxazoles ; chemical synthesis ; pharmacology ; Mice ; PPAR gamma ; agonists ; chemical synthesis ; pharmacology

BACKGROUNDExposure of adult mice to more than 95% O(2) produces a lethal injury by 72 hours. Nitric oxide synthase (NOS) is thought to contribute to the pathophysiology of murine hyperoxia-induced acute lung injury (ALI). Osteopontin (OPN) is a phosphorylated glycoprotein produced principally by macrophages. OPN inhibits inducible nitric oxide synthase (iNOS), which generates large amounts of nitric oxide production. However, the relationship between nitric oxide and endogenous OPN in lung tissue during hyperoxia-induced ALI has not yet been elucidated, thus we examined the role that OPN plays in the hyperoxia-induced lung injury and its relationships with NOS.

METHODSOne hundred and forty-four osteopontin knock-out (KO) mice and their matched wild type background control (WT) were exposed in sealed cages > 95% oxygen or room air for 24- 72 hours, and the severity of lung injury was assessed; expression of OPN, endothelial nitric oxide synthase (eNOS) and iNOS mRNA in lung tissues at 24, 48 and 72 hours of hyperoxia were studied by reverse transcription-polymerase chain reaction (RT-PCR); immunohistochemistry (IHC) was performed for the detection of iNOS, eNOS, and OPN protein in lung tissues.

RESULTSOPN KO mice developed more severe acute lung injury at 72 hours of hyperoxia. The wet/dry weight ratio increased to 6.85 +/- 0.66 in the KO mice at 72 hours of hyperoxia as compared to 5.31 +/- 0.92 in the WT group (P < 0.05). iNOS mRNA (48 hours: 1.04 +/- 0.08 vs. 0.63 +/- 0.09, P < 0.01; 72 hours: 0.89 +/- 0.08 vs. 0.72 +/- 0.09, P < 0.05) and eNOS mRNA (48 hours: 0.62 +/- 0.08 vs. 0.43 +/- 0.09, P < 0.05; 72 hours: 0.67 +/- 0.08 vs. 0.45 +/- 0.09, P < 0.05) expression was more significantly increased in OPN KO mice than their matched WT mice when exposed to hyperoxia. IHC study showed higher expression of iNOS (20.54 +/- 3.18 vs. 12.52 +/- 2.46, P < 0.05) and eNOS (19.83 +/- 5.64 vs. 9.45 +/- 3.82, P < 0.05) in lung tissues of OPN KO mice at 72 hours of hyperoxia.

CONCLUSIONOPN can protect against hyperoxia-induced lung injury by inhibiting NOS.

Animals ; Hyperoxia ; genetics ; physiopathology ; Immunohistochemistry ; Lung ; metabolism ; Lung Injury ; etiology ; genetics ; metabolism ; Mice ; Mice, Knockout ; Nitric Oxide Synthase ; genetics ; metabolism ; Nitric Oxide Synthase Type II ; genetics ; Nitric Oxide Synthase Type III ; genetics ; Osteopontin ; genetics ; physiology ; Reverse Transcriptase Polymerase Chain Reaction

Adolescent ; Adult ; Aged ; Aged, 80 and over ; China ; epidemiology ; Female ; Genitalia, Female ; virology ; Humans ; Middle Aged ; Papillomaviridae ; classification ; isolation & purification ; Papillomavirus Infections ; epidemiology ; virology ; Young Adult