ラットに

3H

-CU-

83

(S)を25μg/kgで静脈内あるいは経口投与し，血液中濃度および尿糞中排泄を検討した．
静脈内投与後の血液中濃度推移は投与後5分より上昇し，投与後45分に25.74ng eq./mlのC_maxを示し，それ以後t_1/2

3

.05時間とt_1/2 33.09時間の二相で減少した．投与後72時間までのAUCは135.42ng eq.·hr/mlであった．
経口投与では，投与後

3

時間でC_max 4.10ng eq./mlに達し，以後t_1/2α 4.46時間とt_1/2β 26.

83

時間の二相で減少した．投与後72時間までのAUCは48.62ng eq.·hr/mlであった．
静脈内投与と経口投与のいずれの場合も，尿および糞中への放射能の排泄は，投与後48時間でほぼ終了した．静脈内投与では，投与後72時間までに投与量の30.52%が尿中に，60.42%が糞中に排泄された．経口投与では，同じく72時間までに40.34%が尿中に，69.24%が糞中に排泄された．

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The acetone extracts from three samples of the hepatopancreas of the poisonous scallops obtained on the Okhotsk Coast of Hokkaido Island were fractionated into two parts, hexane soluble fraction (fraction H) and 85% aqueous ethanol soluble fraction (fraction ) by partition to two layers. The majortoxic components in the mouse assay of “diarrheic shellfish toxin” by intra-peritoneal injection were found to be free unsaturated fatty acids showed the following toxicity in MU per g, 18:1 n-9 35, 18:2 n-6 , 18: n- 167, 18:4 n- , 20:5 n- 167, and :6 n- , respectively. Toxicity of the fraction Hin MUper g was much lower than that of the fraction . However, the toxicity of the fraction H per 1 g of the hepatopancreas was about twice that of the fraction , since the fraction Hwas much more abundant than the fraction in the hepatopancreas. The method for the assay of the diarrhetic shellfish toxin must be reexamined by considering the toxic effect of the free unsaturated fatty acids.

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A structure analysis of has been carried out to determine the deuterium trap sites by neutron powder diffraction with the Rietveld profile analysis. It is revealed that the deuterium atoms are located at octahedral () sites surrounded by six Ti atoms in the crystal structure of , space group P6₃/mcm. Local vibration spectra of hydrogen in measured by neutron inelastic scattering support this result; the energy eigenvalue of the primary vibration mode is found at 7.53 kJ/mol (78 meV). The hole radius and the spring constant of the Ti-H(D) bond are discussed.

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The EISCAT Svalbard Radar (ESR) has been used to obtain ion velocities in the lower thermosphere. By using beam swinging and assuming homogeneity and stationarity of the plasma, first approximations to the electric field have been deduced, and thus the thermospheric neutral wind has been estimated. From these derived parameters, we have estimated the gradient Richardson Number. Although many assumptions must be made, there is an indication that electrodynamics is able to contribute to enhancement or even production of neutral-air turbulence in the lower thermosphere. Finally, we outline a proposal for an analogy to the Reynolds Number, but reflecting the relative importance's of the contribution of ion-drag to the neutral dynamics and the kinematic viscosity.

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The numerical values of the intervals betrween optieal levels are competed for the configurations *⁹4s, 5s, 6s and 7s of Cu⁺, according to the general expression of energy-levels derived in the previous paper The self-consistent field radial functions computed by Hartree adn Hartree are used for1s, 2s, 2p, s, p and d. Those of 4s, 5s, .s and are ealenlated from Hartree Hartree's core-functions by the numerical integrations. The calculated results are shown in Table I.The agreement with experiment is satisfactory

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The nanocrystalline soft-magnetic ribbon alloy with a width of 10 mm prepared through annealing amorphous ribbon alloy at 698 K had a saturation magnetization flux density of 1. T and a coercivity of 11.8 A m⁻¹. The nanohetero-amorphous microstructure consisted of α-Fe nanocrystals with an average size of nm and amorphous neighbor phases. The results of polarization curves and electrochemical impedance spectra obtained in .5 M Na₂SO₄ and .5 M NaCl solutions demonstrated the positive shift of the corrosion potentials, the decrease in the passive current density, the increase in the breakdown potentials and the increase in the polarization resistance for the nanocrystalline ribbon alloy, compared with its amorphous counterpart alloy. The corrosion performance was improved via annealing, which is thought to result from the enrichment of constituent in the surface oxide layer.

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Background

The differences in conditions of enteric-coated acid-labile drug release and absorption between healthy subjects in bioequivalence studies and gastrointestinal patients in clinical practice can lead to significant differences in gastric stability of original PPIs and generics. Thus, pathologic duodenogastric reflux (PDGR) and the pH increasing within PPIs administration still remain unaccounted for.

Methods

Two-stage modified comparative dissolution testing of original omeprazole (OO) and four generics (G1;2;

;4) was performed. At first, we moved drugs from solution with pH 1.2 (1.2±.05) to pH 7. (7.±.05) and measure concentration of omeprazole in solution by high-performance liquid chromatography. According to our self-developed formula, pH 7 exposure time of resistance to PDGR for omeprazole is 4 minutes, i.. the active substance should not be released within 4 minutes at pH 7. The exposure at the second stage was conducted with pH 4 (4.±.05), that imitated gastric pH after PPI administration. And then we also moved drugs to pH 7 with the subsequent measurement of omeprazole concentration.

Results

Omeprazole concentrations after 4, 10, 15, 20, 30, 45, 60 minutes in pH 7 solution at the first stage were different for OO and generics. For OO, these values were 4,7±

,7%; 41,4±,%; 62,8±4,%; 79,5±2,9%; ,5±2,9%; ,6±2,9%; 80,6±4,4%; for Generic1 - ; 49,±9,9%; 88,8 ±2,8%; 90,4±,7%; 88, 2±2,2%; 87,±2,%; 85,9±1,1%; for Generic2 - ; 30,6±6,%; 66,7±8,2%; 76,4±7,4%; ,8±5,%; 86,±,7%; 84,6±,%: for Generic - 80,8±,6%; ,5±1,9%; , 8±,2%; ,±2,7%; ,9±2,1%; ,1±2,%; ,±2,4%; for Generic4 - ,5±1,7%; 84,4±,8%; 84,2±1,2%; , 9±,9%; ,9±,9%; ,9±,9%; ,8±1,1%, respectively.

An analysis of the omeprazole concentration in pH 7 solution at the second stage revealed the following parameters after the same time: for OO - 4,4±

,6%; 40, 5±,%; 62,8±2,%; 80,±,1%; 85,4±2,9%; ,8±,4%; 80,9±,5%; for Generic1 - ; 67,±7,8%; 89,7±2,%; 91, 9±4,%; 89,1±1,6%; 88,±1,4%; 87,8±1,2%; for Generic2 - ; 42,2±5,6%; 75,1±7,%; ,±6,%; 88,4±,2%; 88, 6±1,%; 87,9±1,%; for Generic4 - 85,5±,5%; 85,6±,5%; 84,7±,9%; ,7±,%; 84,4±,%; 84,4±,%; 84,±,4%, respectively. Generic release and degradation were completely realized at pH 4.

Conclusion

Decreased gastric stability of Generic

and Generic4 makes PDGR and inhibited gastric acid secretion due to PPIs administration the potential causes of decreased enteric-coated acid-labile drugs stability.

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Mace- extract obtained from seed covering of nutmeg is expected to show an antiarteriosclerotic effect due to its potentiation with unsaturated fatty acid, various vitamins, etc. In this study an effect of Mace- was examined from serum lipid and six constituents of thoracic aorta.
A total of 16 male rabbits of 38 months, including 8 with the Mcce- (M group), 4 with cholesterol (C group) and 4 with Mace- plus cholesterol (MC group) were used. to produce arterosclerosis cholesterol was orally given at 1g to the C and MC group. To the M and MC groups Mace- was given at 500mg/day. Sixteen weeks later referring to all the rabbits, total cholesterol (T. CHO), triglyceride (TRIG), β-lipoprotein (β-LIPO), HDL-cholesterol (HDL), 4 in total of serum lipids, were measured. Furthermore, all the rabbits were killed and constituents media of thoracic aorta were stained and observed histochemically, i. ., SMC with Azocarmine G stain, EL with Weigert's stain, CL with Van Gieson's stain, AMPS with Alcian blue stain and GP with PAS stain. T. CHO was 90.5mg/dl in M group, 369.8mg/dl in C group and .mg/dl in MC group respectively. The MC group showed no difference with M group but the significantly lower value than that of C group (p<.01). TRIG was 108.5mg/dl in M group, .mg/dl in C group and 94.4mg/dl in MC group respectively. No significant difference was observed among these groups. Beta-LIPO was 184.mg/dl in M group, 995.mg/dl in C group and 151.5mg/dl in MC group respectively. Compared with C group, M and MC groups showed significantly low value (p<.001-p<.01). HDL was 18.9mg/dl in M group, .mg/dl in C group and 26.5mg/dl in MC group respectively. There was no significant difference among those group, although it was highest in MC group. When histochemically observed, C group was strongly disturbed, while MC group showed slight swelling of SMC and cell nucleus that was not remarkable though, and damage of EL and CL was minimal. AMPS and GP remained unchanged. From changes of serum lipid and observation of arterial tissue, it was suggested that Mace- has an antisclerotic effect.

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We screened the differentiation-inducing activities of 39 mushroom extracts from Akita prefecture, Japan, on the mouse osteoblastic cell line, MCT-1. Sixteen phosphate buffered saline (PBS), 8 boiled PBS, 14 ethanol and 12 methanol extracts induced alkaline phosphatase (ALP) activities, an indicator of MCT-1 cell differentiation. The enzyme activities were markedly induced by extracts of Tricholoma auratum, and we isolated the active compound from methanol extracts of this mushroom. Physical data for the isolated active compound were identical to those for (,24R)-ergosta-7,-diene-,5α,6β-triol (1). 1 induced ALP activities of MCT-1 cells and promoted cell proliferation. To investigate the relationships between the chemical structure and differentiation-inducing activity of the compound, ALP-inducing activities of MCT-1 cells by 1, ergosterol (2), ergocalciferol (), cholesta-,5α,6β-triol (4), 7-dehydrocholesterol (5) and cholecalciferol (6) were tested. The enzyme activities of MCT-1 cells were increased .-fold by 10 μM 1 and 2.4-fold by 10 μM 4. However, 2, , 5 and 6 did not induce MCT-1 cell ALP activity at .1—10 μM. These results suggested that the OH groups at C-5 and/or C-6 of 1 and 4 played an important role in their differentiation-inducing activities on MCT-1 cells. Furthermore, 1 suppressed induction of MCT-1 cell apoptosis by serum starvation.

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The aim of the present study was to evaluate the predation efficacy of Bdellovibrio bacteriovorus on multidrug-resistant (MDR) or extensive drug resistant (XDR) gram-negative pathogens and their corresponding biofilms. In this study, we examined the ability of

. bacteriovorus to prey on MDR and XDR gram-negative clinical bacteria, including Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, and Acinetobacter baumannii. Results showed that

B

. bacteriovorus was able to prey on all planktonic cultures, among which the most efficient predation was observed for drug-resistant

E

. coli, with a .11 log10 reduction in viability. Furthermore,

B

. bacteriovorus demonstrated promising efficacy in preventing biofilm formation and dispersing the established biofilm. Reductions in biofilm formation of

E

. coli, K. pneumoniae, P. aeruginosa, and A. baumannii co-cultured with

B

. bacteriovorus were 65.2%, 37.1%, 44.7%, and 36.8%, respectively. Meanwhile, the established biofilms of

E

. coli, K. pneumoniae, P. aeruginosa, and A. baumannii were significantly reduced by .4%, .8%, .1%, and 79.9%, respectively. A visual analysis supported by scanning electron microscopy demonstrated the role of

B

. bacteriovorus in removing the established biofilms. This study highlights the potential use of

B

. bacteriovorus as a biological control agent with the capability to prey on MDR/XDR gram-negative pathogens and eradicate biofilms.

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A structure analysis of has been carried out to determine the deuterium trap sites by neutron powder diffraction with the Rietveld profile analysis. It is revealed that the deuterium atoms are located at octahedral (2) sites surrounded by six Ti atoms in the crystal structure of , space group P6₃/mcm. Local vibration spectrum of hydrogen in measured by neutron inelastic scattering supports this result; the energy eigenvalue of the primary vibration mode is found at 7.53 kJ/mol (78 meV). The hole radius and the spring constant of the Ti–H(D) bond are discussed.

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Choke disease fungus Epichloe typhina is associated with resistance to leaf spot disease in timothy plants (Phleum pratense). We have proposed the hypothesis that this resistance is caused by antifungal compounds existing in infected plants. We investigated the fungitoxic constituents of the stromata of . typhina. Seventy-eight compounds were isolated, including twenty novel sesquiterpenoids chokols (1,2,7-17,19-21,23-26), five novel oxygenated fatty acids(27-31), gamahonolide A(34) and (37), gamahorin(38) and non-fungitoxic chokorin(71) and an anthrasteroid(80). Their structures were determined by spectroscopic methods. The absolute configuration of chokol (2) was elucidated by its CD spectrum with Eu(fod)_ and a chemical correlation with epicyclonerodiol oxide(5). Phytol(), phytyl acetate() and phytyl palmitate() were identified as an inducer of aerial hyphae formation of Cladosporium herbarum. Pinoresinol(60) and diosmetin(73) were metabolized in cultures of . typhina. Pinoresinol(60) was transformed into C6 norlignan(59) and α-ribofuranoside(87). Diosmetin(73) was transformed into 7-O-α-ribofuranoside(88). Antifungal activities of the isolated compounds were investigated.

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The applicability of a method for predicting 'bearing capacity increase'in reinforced sandy ground was examined using tests performed under various test conditions. It was found that the present method predicted, with reasonable accuracy, the bearing capacity increase in sandy ground, reinforced with stiff reinforcement. This method may not be applicable for sandy ground reinforced with extensible reinforcement due to the unsuccessful formation of a semirigid zone under the footing. An investigation into the settlement of a footing on reinforced sandy ground, at ultimate footing load condition, suggested that the settlement of footing for reaching peak footing load may be correlated to the 'deep-footing'and the 'wide-slab'mechanisms. That is, the ultimate settlement ratio between reinforced and unreinforced model sandy ground, SR_f, may be linearly correlated to 'BCR_D'and 'BCR_s', which represent 'deep-footing' and 'wide-slab'effects, respectively, on the ultimate bearing capacity increase in reinforced sandy ground.

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Background: Oxidative stress, the imbalance between pro- and antioxidants, has been implicated in the etiology and pathophysiology of the incidence and mortality of many diseases. We aim to investigate the relations of dietary intakes of vitamin C and

and main carotenoids with all-cause mortality in Japanese men and women.

Methods: The Japan Collaborative Cohort Study for Evaluation of Cancer Risk had

,795 men and 35,539 women, aged 40–79 years at baseline (1988–1990), who completed a valid food frequency questionnaire and were followed up to the end of 2009.

Results: There were 6,179 deaths in men and 5,355 deaths in women during the median follow-up of 18.9 years for men and 19.4 years for women. Multivariate hazard ratios for the highest versus lowest quintile intakes in women were

. (95% confidence interval [CI], .76–.90; P for trend < .0001) for vitamin C, .85 (95% CI, .78–.93; P for trend < .0001) for vitamin , .88 (95% CI, .–.96; P for trend = .0006) for β-carotene, and .90 (95% CI, .–.98; P for trend = .0002) for β-cryptoxanthin. The joint effect of any two of these highly correlated micronutrients showed significant 12–17% reductions in risk in the high-intake group compared with the low-intake group in women. These significant associations were also observed in the highest quintile intakes of vitamin C, vitamin , and β-carotene in female non-smokers but were not observed in female smokers, male smokers, and non-smokers.

Conclusions: Higher dietary intakes of antioxidant vitamins may reduce the risk of all-cause mortality in middle-aged Japanese women, especially female non-smokers.

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