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- 35, 18:2 n- , 18: n- 167, 18:4 n- , 20:5 n- 167, and : 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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The numerical values of the intervals betrween optieal levels are competed for the configurations *⁹4s, 5s, s 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 . 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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1. The chromosome numbers of 64 species have been studied on which 56 are investigated for the first time.
2. Morphological, anatomical and cytological findings on the Musaceae in the broad sense are considered from a phylogenetical standpoint and three distinct groups:
a) Musa-Ensete, b) Ravenala-Strelitzia-Phenakospermum and ) Holiconia are recognised as suggested by some authors. For these groups sub-familial status is proposed.
. Lowiaceae have been studied for the first time cytologically and their chromosome morphology, distinct from that of any other group of Zingiberales, confirms their claim to familial status.
4. Consideration of the conflicting theories proposed to account for the higher chromosome number in genera like Globba, Alpinia, and Phaemeria, etc. leads to rejection of Chakravorti's hypothesis of wholesale fragmentation of chromosomes and the acceptance of the opposed view of Raghavan and Venkatasubban and others.
5. Holttum's transference of the genus Zingiber to the tribe Hedychieae has been given cytological support on the following points:
a) the basic number in the genus Zingiber correlates with that of Kaempferia.
b) the new tribe Alpinieae (which is infact Zingibereae without Zingiber) have consistently 48 chromosomes in their somatic complements.
. It is suggested that the African representatives of Kaempferia should be given the status of genus; Cienkowskya on the following points:
a) the difference in floral morphology
b) geographical separateness and
) the difference in the number and morphology of the chromosomes. By comparing the present and past findings, various lines of evolution of the chromosome complements within each group are discussed.
7. The basic number 11 is considered to be probably the original one for the Zingiberales as a whole, being present in Ravenala which is the most primitive member in the order. From this secondary basic numbers have arisen through evolution.

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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 (2b) 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() bond are discussed.

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Clinical results of rotator cuff repairs using the same therapeutic exercises from an early stage after surgery were investigated and compared with the preoperative X-ray findings. 70 shoulders with rotator cuff tears treated operatively and followed by active-assistive exercises in a supine position from 1 week and active exercises standing from weeks after surgery were evaluated. The average age was 63 years old and follow-up periods were 11. months. The operative procedures were McLaughlin's method in 41 shoulders, side to side sutures in , acromioplasty in 17 and a tendon transfer in . The preoperative X-ray findings were classified into 5 groups: group A, superiorly migrated humeral head and narrowed joint space in 4 shoulders; group B, only superior migration in 7; group , only narrowed joint space in ; group , no changes in 36; group , subacromial spurs more than 5 mm without superior migration in 20. The postoperative results were assessed according to the JOA score and the failure rate of each group was investigated. No significant differences in the preoperative JOA score were found in the 5 groups. The postoperative JOA scores were 62.±. in group A, 75.1±12. in B, 78.0±12.2 in , .4±7.5 in , and .±11.1 in . Especially groups and treated by McLaughlin's methods showed a significant higher score at follow-up. Rotator cuff repairs with the same therapeutic exercises from an early stage after surgery for groups A, B and showed poor results. Groups A and B with a superior migration of the humeral head showed a high failure rate of 40 % compared with 4.7% in group , and with no superior migration. For these cases more careful postoperative exercises were recommended.

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Background: Exenatide (EXE), a prototypical GLP-1R agonist, has been reported as beneficial to the balance of bone turnover in hyperlipidic and hyperglucidic diet-induced obesity in rats (DIO). Objective: To identify the mediation by GLP-1R of insulin (INS), leptin (LEP), osteocalcin (OCN), calcitonin (CT), carboxy-terminal telopeptide of type 1 collagen (CTX-1), procollagen type 1 amino-terminal propeptide (P1NP) and bone mineral density of femur (BMDF) in DIO. Methods: 72-75-day-old male rats had access only to (i) hyperlipidic food (5.2 kcal/g) and 30% sucrose solution for drinking (1.2 kcal/mL), or (ii) received normocaloric diet (

kcal/g) and were allowed to feed and to drink water ad libitum. 122-125-day-old rats with 20% overweight were selected from i as obese and those with normal weight were selected from ii as control () animals. Thus, obese animals remained untreated (DIO) or were treated sc with 100μg of the competitive antagonist of GLP-1R, exendin (-39) () per kg (DIO-) daily, for 20 days. Plasma INS, LEP, OCN, CTX-1 (ng/mL), CT and P1NP (pg/mL) were measured by ELISA. BMDF (g/) was measured by X-rays. Results: DIO exhibited similar INS (12.±1., n=4) and CT (2.80±1.05, n=4), higher LEP (0.33±0.04, n=5) and lower CTX-1 (0.48±0., n=) than . The treatment of DIO with decreased CTX-1 (4.44±0.63, n=) and increased P1NP (163.40±39.80, n=). DIO- decreased INS (5.75±1.50, n=) in relation to DIO, at the same level than (10.58±1.49, n=4). LEP level in DIO- (0.23±0.02, n=) was intermediate in relation to DIO and (0.16±0.05, n=5). OCN, CT and BMDF were similar among , DIO and DIO-. Conclusions: Decreased CTX-1 and normal OCN, P1NP and BMDF reflect a relative normal balance in bone turnover in DIO. Since decreases CTX-1, a known effect of EXE in DIO, this alteration on CTX-1 extrapolates the GLP-1R binding and/or EXE and act as selective modulators with different actions in different targets. Furthermore, increases P1NP (not affected by EXE) and does not affect CT (increased by EXE). effects in DIO imply in increased osteoblastic and decreased osteoclastic activities, which promote an imbalance of bone turnover.

Supported by FAPESP, CNPq and CAPES

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Circuit techniques to enhance the linearity of input-voltage-to-current (V/I) conversion and to increase the output impedance of a current source by compensating for the low intrinsic gain of a transistor were introduced to realize a high-frequency operational transconductance amplifier (OTA) for a low supply voltage using sub-100-nm CMOS processes. Applying these techniques, a MOS 7th-order Gm- linear-phase low-pass filter (LPF) was realized using a 65nm CMOS process. A simplified biquad LPF that can serve as a component of a 7th-order LPF was newly developed by replacing OTAs with resistors. As a result, the -dB frequency bandwidth, group delay ripple, rd-order distortion, and rd-order input intercept point (IIP) were 200MHz, 2.2%, ≤ -55dB with a 100MHz input, and +10.dBm, respectively, all with a ±0.1Vp-p input signal at each input terminal in the pseudodifferential configuration. The LPF including an output buffer dissipated 60mW in the case of a 1.2V supply. Wide spurious-free dynamic range (SFDR) characteristics were confirmed up to high frequencies.

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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±0.05) to pH 7.0 (7.0±0.05) 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 (4.0±0.05), 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±0,7%; 41,4±

,0%; 62,8±4,0%; 79,5±2,%; ,5±2,%; 81,±2,%; 80,±4,4%; for Generic1 - 0; 49,±,%; 88,8 ±2,8%; ,4±,7%; 88, 2±2,2%; 87,±2,0%; 85,±1,1%; for Generic2 - 0; 30,±,%; 66,7±8,2%; 76,4±7,4%; ,8±5,%; 86,0±,7%; 84,±,%: for Generic - 80,8±,%; ,5±1,%; , 8±,2%; ,±2,7%; 81,±2,1%; ,1±2,0%; ,0±2,4%; for Generic4 - ,5±1,7%; 84,4±0,8%; 84,2±1,2%; , ±0,%; ,±0,%; ,±0,%; ,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±0,

%; 40, 5±,0%; 62,8±2,0%; 80,0±,1%; 85,4±2,%; ,8±,4%; 80,±,5%; for Generic1 - 0; 67,0±7,8%; 89,7±2,%; 91, ±4,%; 89,1±1,%; 88,±1,4%; 87,8±1,2%; for Generic2 - 0; 42,2±5,%; 75,1±7,%; 81,0±,0%; 88,4±,2%; 88, ±1,%; 87,±1,0%; for Generic4 - 85,5±0,5%; 85,±0,5%; 84,7±0,%; ,7±,0%; 84,4±0,%; 84,4±0,%; 84,±0,4%, 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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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

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

,179 deaths in men and 5,355 deaths in women during the median follow-up of 18. years for men and 19.4 years for women. Multivariate hazard ratios for the highest versus lowest quintile intakes in women were 0. (95% confidence interval [CI], 0.76–0.; P for trend < 0.0001) for vitamin , 0.85 (95% CI, 0.78–0.93; P for trend < 0.0001) for vitamin , 0.88 (95% CI, 0.81–0.96; P for trend = 0.0006) for β-carotene, and 0. (95% CI, 0.–0.98; P for trend = 0.0002) 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 , 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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A method for analyzing the uncertainties involving the use of empirical relationships in design is developed. It is applied to evaluate the reliability of the relationship s_u(mobilized)=(measured), whereby the pertinent uncertainties are analyzed using extensive laboratory and field observed data. On the average, the relationship s_u(mobilized)= (measured) is unbiased and the error implicit in the relationship is about 15%. When cone values are used to infer s'_p, additional uncertainties on the mobilized undrained strength will incur resulting mainly from the calibration uncertainty between σ'_p and the cone values. Alternatively, vane tests may be performed to infer the mobilized strength using Bjerrum correction factor. Results show that uncertainty level associated with using the vane tests is smaller than that using the cone values, provided that similar scatter is observed between measured vane and cone values at a given site. However, prediction of the mobilized strength is even more accurate if direct measurements can be made on the preconsolidation pressure. The proposed probabilistic method also assesses the benefit of additional tests besides comparing the accuracy of using various soil parameters for predicting mobilized undrained strength. Such information is essential for planning cost-effective site characterization program.

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Chemical synthesis of (, 24R)- and (, 24S)-1, 24-dihydroxy--vitamin has been achieved starting with the commercially available dinorcholenic acid acetate. Synthesis involved introduction of the 1-hydroxy group by a reduction of the 1, 2-epoxide generated by epoxidation of the 1, 4, -trien--one. The side chain on the steroid was then constructed by means of a Wittig reaction followed by introduction of the Δ⁷ bond by standard methods and its protection with 1-phenyl-1, 2, 4-triazoline-, 5-dione. Subsequent reduction of the hydroxy groups in the steroid side chain followed by reduction of the Diels-Alder addition products yielded the both 24-isomers. The 5, 7-dienes were irradiated and the corresponding vitamin compounds isolated. Nuclear magnetic resonance was used to identify individual isomers. The (, 24S)-1, 24-hydroxyvitamin compound bound equally well to the chick intestinal cytosol receptor as 1, 25-dihydroxyvitamin , while the 24R-isomer was approximately ten times less active. In vivo, both isomers were less active than 1, 25-dihydroxyvitamin ; however, the 24S-isomer was considerably more active than the 24R-isomer approaching the activity of 1, 25-dihydroxyvitamin .

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(,)-2,-エポキシ-,7,11,11-テトラメチルシクロウンデカ-,-ジエン(2)をフムレン1((2,,)-,7,11,11-テトラメチルシクロウンデカ-2,,-トリエン)より合成する既知の合成法は実際に牧率が低く合成的に問題がある.さらに,2の合成はその反応性や物性の研究のために簡単に高牧率で行われることが望まれる.今回,2の新たな合成法と簡便な精製法を見いだし,2を高牧率で1から合成することができたので報告する.1のジエポキシ化,続く再結晶により得られたジエポキシド(8)は二価のチタンにより還元されて,1(273%)と8(25%)と少量のを含む2を主生成物(42.7%)として与えた.1とは原料として再利用できる.2の精製は1と同様硝酸銀()錯体の結晶で行い,純粋な2は1から通算牧率32.0%で得られた.2の既知方法による合成は4段階の反応と数回のカラム分離及び10%含浸シリカゲルカラム分離を必要とし牧率が極端に低い.今回,新しい2の合成法は2段階の反応で1回のカラム分離と再結晶により高い通算牧率を示す.

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This paper outlines a mathematical description of the stress dilatancy behaviour of granular materials which accounts for stress level and void ratio dependencies. The consideration of these aspects has important implications in the modelling of granular material behaviour. In fact, granular material mechanical response is largely dominated by the evolution of dilatancy, fabric and void ratio histories. The starting point in this study is the well established Rowe's theory which is revisited and ultimately modified by introducing a factor linked to governing state parameters in order to describe the complete behaviour of granular materials during deformation. Numerical simulations of triaxial tests on granular materials at different void ratios and stress levels are herein presented to illustrate the model.

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Virus-like particles (VLPs) were collected from geothermal vent water samples in the drift-way at Toyoha Mine, Hokkaido, Japan (−500 m level, 63.5°) whose VLP and bacterial abundance was (No/ml±SD, n: 500), VLP: .60±0.29×10⁸ and bacteria: .61±0.14×10⁶. VLPs ranged in diameter from 30 to 320 nm, and the major size distribution (ca 62%) was .33. nm (n: 843). Ultrafiltration followed by CsCl density equilibrium ultracentrifugation gave purified TY-VLPs: .64×10¹³. Regardless of UV treatment, TY-VLP reduced the efficiency of plating to 68.-.4% at a multiplicity of infection of ca 0. on Escherichia coli AB1157. Generalised transduction was observed on

E

. coli AB1157 with a frequency between 10^-4 and 10^-5 cells/particle using TY-VLPs without UV-treatment. The growth of generated

E

. coli transductants (TY--trans) was compared to that of an

E

. coli transductant (ST--trans) generated by Aquificales originating VLP (Chiura, 2002). The extent of the maximum growth of both transductants was ca 40% of the parental

E

. coli used as a recipient. TY--trans acquired "budding-like" particle productivity, which has been demonstrated for ST--trans. ST--trans produced five different size particles, whose DNA content ranged between 291. and 382.0 kb, and TY--trans produced ten different size particles between 68.5 and 190.2 kb, respectively.

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