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-,-diene-,,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-,,6β-triol (), -dehydrocholesterol () and cholecalciferol (6) were tested. The enzyme activities of MCT-1 cells were increased .0-fold by 10 μM 1 and 2.-fold by 10 μM . However, 2, , and 6 did not induce MCT-1 cell ALP activity at 0.1—10 μM. These results suggested that the OH groups at C- and/or C-6 of 1 and 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 gamma-ray spectrum and the conversion-electron spectrum are measured in the decay of the ^116mIn activity. Directional correlations are also measured for 818–1293 and 1097–1293 keV cascades. The M1-2 mixing ratio δ, and the 0-2 mixing ratio μ_k are obtained for 818. keV +→2₁⁺ transition to be δ=1.52−

0.22

+0.26, and μ_k≤6.1×10−

4

respectively. The

E

2 branching ratio

B

(

E

2;

2₂

+→0_g⁺):

B

(

E

2;

2₂

+→2₁⁺):

B

(

E

2;

2₂

+→0₁⁺) is determined to be 0.0158:1.0:

5

.

86

.

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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, , 6-trien--one. The side chain on the steroid was then constructed by means of a Wittig reaction followed by introduction of the bond by standard methods and its protection with 1-phenyl-1, 2, -triazoline-, -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 , -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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This study aimed to determine the prevalence of fecal carriage of extended spectrum β-lactamase (ESBL) and/or plasmidic AmpC β-lactamase (pAmpC) producing Escherichia coli among dogs (n=428) in Turkey. Polymerase chain reaction (PCR) and sequencing were used to characterize genes encoding β-lactamase and plasmid mediated quinolone resistance (PMQR). Antimicrobial susceptibility testing and PCRs for virulence genes and phylogenetic groups were also performed. Cefotaxime resistant

. coli isolates were detected in 95 (.2%) of the swab samples. Sequencing analysis results showed occurrence of various β-lactamase genes: bla_CTX-M-15 (62), blaTEM-

1b

(42), bla_CMY-2 (

22

), blaCTX-M-

3

(16), bla_CTX-M-1 (15), bla_OXA-1 (

9

) and bla_SHV-12 (

3

) alone or in combination. The most frequently encountered phylogenetic group was group A₁ (35.8%), followed by group

D₂

(

22

.1%),

B

1 (15.8%),

D₁

(

9

.

5

%), A₀ (

7

.

4

%),

B2₂

(

5

.

3

%) and

B2₃

(

4

.2%), respectively. PMQR genes, aac(6’)-Ib-cr, qnrS1 and qnrB10 were detected in 25.

3

, 10.

5

and 1.1% of the isolates, respectively. While all isolates were susceptible to imipenem and amikacin, resistance rates to non-β-lactam antibiotics ranged from 20.0% for tobramycin to 56.8% for tetracycline. The virulence genes were only detected in 34 (36.2%) of the isolates and this isolates carried single or various combination of virulence genes of iucD, papC, papE, f17a-A and eaeA. Four isolates were identified as human virulent pandemic CTX-M-15 producing

E

. coli clone O25

b

:ST131/

B

2. To the best of our knowledge, this is the first study to show fecal carriage of ESBL/pAmpC type β-lactamase producing

E

. coli isolates among dogs in Turkey.

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Agaricus blazei is an important fungus for producing bioactive compounds. There are some reports of polysaccharides and steroid derivatives from the fruiting bodies of A. blazei. However, the chemical examination of the secondary metabolites of the cultured mycelia of this species has not been reported. Eight compounds, an unprecedented skeleton have been isolated from the cultured mycelia of A. blazei. The structures of the novel compounds each named blazeispirols A (1), (2), C (), (), () X(6), Y () and Z (8) were confirmed by extensive 1 and 2 NMR spectral data and X-ray analysis. Blazeispirols A (1), (2), C (), () and () were des-A-ergostane type compounds having spiroacetal structure as a side chain. Blazeispirols X (6) and Y () were determined to be (20S, S, 23R, 24S)-1 (10→6) abeo-14β, :, 25-diepoxyergosta-,,,11-tetraene-α,23-diol and (20S, S, 23R, 24S)-14β,:,25-diepoxy-,23-dihydroxyergosta-,,11-triene-,6-dione by comparison of extensive 1 and 2 NMR spectral data with that of blazeispirol A. The biosynthesis of blazeispirol A was investigated by feeding ^<13>C-labeled acetates and methionine to the growing cultures of A. blazei. The labeling patterns of 1 derived from singly and doubly ^<13>C-labeled acetates were consistent with that of ergosterol reported previously except for the A-ring and then ^<14>C-labeled ergosterol was incorporated into blazeispirol A. Taking the structures of blazeispirols Z and into consideration, it can be assumed that blazeispirol A is biosynthesized from ergosterol by the cleavage of C-, C- and C-1, C-10 bonds on retro aldol condensation and Michael reaction via such as intermediate A as shown in Fig. . A large number of ergostane-type steroids have been isolated from many fungi. However, blazeispirol A is the first example of a naturally occurring des-A-ergostane-type steroid including a spiroacetal structure moiety as a side chain.

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The numerical values of the intervals betrween optieal levels are competed for the configurations *⁹4s, s, 6s and s 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 s, s, .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 ability of Climacodon septentrionalis to immobilize and kill a mycophagous nematode (Aphelenchoides sp.) in vitro is described for the first time. Two isolates produced droplets (20–45 μm in diameter) that formed at the apices of tall, stalked, and branching secretory cells (700–1,500 μm tall). On 2% modified malt extract agar, nematodes became enveloped in the droplets, which restricted their ability to move and resulted in complete immobilization and death within several hours of contact. The rate of decomposition of the nematodes varied considerably, with most individuals persisting for weeks whereas others were degraded within several days and appeared to be colonized by dense hyphal growth. This study provides the first documentation of a non-agaricoid fungus producing secretory cells that are able to immobilize nematodes.

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The performance of single pitch and multi pitch screw anchors during the application of installation torque is presented. An experimental testing program was conducted using five models of screw anchors with different geometry. The effect of the shape of the screw element, sand properties, and installation depth on the required installation torque value was examined. A theoretical model was developed from which the required installation torque value can be calculated in terms of the influencing factors. The required installation torque can be determined in terms of the ultimate uplift resistance calculated from any of the available theories. Based on the actual installation torque value measured in the field, the anticipated pullout capacity can be back calculated from the present theory. A comparison between theoretical and experimental results showed good agreement. Also, good agreement was observed when the present theoretical results were compared with the available field results reported in the literature.

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Two new vitamin analogues, 1α-hydroxy-24, 24-dimethyl--dehydrovitamin (13) and 1α, 25-dihydroxy-24, 24-dimethyl--dehydrovitamin (17), which are blocked for 24-hydroxylation by the methyl groups, were synthesized from 1α, -bismethoxymethoxypregn--ene-20Scarbaldehyde (6) by using the orthoester Claisen rearrangement for construction of the carbon skeleton of their side chains. These compounds (13 and 17) elicited a rise in serum calcium, but not in serum inorganic phosphorus in rats. In a bioassay for alkaline phosphatase, they were found to show much weaker activity than 1α-hydroxy vitamin ().

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[1] The purpose of this reserch is to make clear what type of design can give good effects to win the high readership score. At the begining I had to know what factors decide the readership score, and how to change the quality of the desing into numerical value. I have used the method of multi-dimentional analysis with the help of a computer, and got the estimation formula, with kinds of factors, as follows ; A^^〜=+C++K+aE+bF+cG. A^^〜=estimated values of the readership score. 1) , C, , K : these four factors are given as category values (so we call them); each factor is classified into several categories. =week day, classified into categories. C=pages of a newspaper, which are characterized by the kinds of articles, news, and the other reading matters, classified into categories. =kinds of goods and trades of the advertizement, classified into 14 catedories. K=constants, given to each 13 surveys. 2) , F, G : these factors are given as numerical values. G=area of advertizement, measured by the unit of column in the whole page length, being classified into 6 kinds of area (2., ., , , 10, 15) and 15 column means a whole page, about 2,000cm^2. , F are the marks obtained in the design of advertizements. =sum of the marks obtained in each design element on the advertizement. F=the marks obtained on the whole effect of the design. ) a, , c : coefficients Using the above formula with the category values and the coefficients, we can obtain the naked design effect from the actual value A of readership score: aE+bF=A-(+C++K+cG). In this research, I used 1,829 data of readership score from 1960 to 1968, being obtained by 13 survevs, spring and autumn twice a year. The sample of size each survey was ,541, 2,251, or 200 in the other 11 surveys. Multiple correlation coefficient between the estimated value A^^〜 and the actual value A is 0.951. The table 2^* shows the contribution indexes of each factor by kinds of expression-(1) Range : the absolute difference between the maximum and the minimum category values, (2) Standard deviations of the category values, () Partial correlation coefficient : the relationship between the actual values A and each factors. *see the table 2 in the thesis in Japanese. [2] The important point was in the determination of the values of , F. is the sum of the marks obtained in each design element, classified into four kinds : =_1+_2+_+_. design elements [table] _1, _2, _, _, these values have the grades, as 0, 1, 2, , and 0 is given to the design that has no attractive effect or no applicable element. And obtain the marks of 0 to grades as the sum of them. The values of F have also grades, 0 to . The principles to determine the values of , F are as follows : a) The marks obtained of , F must be the relative values among the each survey, and at the same time, they must have constancy within the same survey-the same elements of design must win the same marks obtained. ) They must be determined as to win the highest multiple correlation coefficient, when they are put into the estimation formula. c) They must be reasonable. In order to justify them, we must carry many researches on the actual condition. The frequency of accurence of each grade of , F values, as the table -, and - in the thesis in Japanese.

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The material consists of 120 sides of 60 Japanese fetus from to 10 months old. These 120 specimens were classified after the participating roots of the spinal nerves in 15 forms and types (I-V).
In the II and III types, which occur together in .% and may be called normal, the plexus consists of Rr. anteriores of Th₁₂, -, (II, 32.%) or L₁, - (X, 50.%). In the type IV (.0%) and V (8.%) are the roots of the plexus shifted caudal so that S, gives the share for the formation of the plexus, while in the type I (.8%) cranial so that the most caudal root of the plexus is S₂.
According to the forms of N. femoralis and ischiadicus which are the main parts of the plexus the type II is classified in (a, , c, , ), III in (a, , c, ), IV in 2 (a, ), and V in (a, , c).(Fig 1-13)
In animals the form of the plexus lumbosacralis is very simple, among them the mammals have the most complex forms which resemble to the man's plexus. In our 120 specimens there are 17 more simple and more complex forms.
Among our specimens there are 2 the most primitive forms of the brachial plexus, more primitive inclined. In the former 2 the lumbosacral plexus is a little simple and primitive in one specimen, while in the other not simple, but a little more complex, in the latter one is simple, 2 is complex while the other specimens normal.(Fig.14, 15) So there is no intimate correlation between Plexus brachialis and lumbosacralis in the phylogenetic primitiveness.
After the frequency of the furcal nerve (Jhering) which occurs in L (.%) or L (17.%) there is no difference between our Japanese and German (Eisler) or English (Paterson).(Table ) In our one example of type V form c there is no furcal, no lumbosacral trunk.(Fig. 10)
When our specimens are arranged after Bardeen and Elting the most frequent form . i. median origin occurs in 57.%, the proximal origin in 24.1%, distal origin in 18.%, while in case of the American white 36., 47. and 16.2 respectively.
There is no specimen of N. obturatorius accessorius, which occurs a little frequent in European.
The difference of form of the plexus between right and left is very slight so that the shifting of one complete segment in one side does not occur.

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The phase diagrams of the Ni-Mo- and Ni-W- ternary systems in the region of less than 50mol% were constructed by thermodynamic calculation, based on the data obtained by thermodynamic measurement of the related materials. We found three ternary eutectic points and three or two ternary peritecto-eutectic points as follows:
:L (1365K, 71.mol%Ni-6.0mol%Mo-.mol%)=(Ni)++
:L (1355K, 62.mol%Ni-2.mol%Mo-30.mol%)=++
:L (1445K, 42.0mol%Ni-30.6mol%Mo-10.mol%)=(Ni)+NiMo+
P₁:L (1812K, 34.mol%Ni-42.mol%Mo-.8mol%)+MoB=+
P₂:L (1633K, 42.mol%Ni-40.mol%Mo-17.mol%)+Mo=+
:L (1812K, 53.mol%Ni-33.mol%Mo-12.8mol%)+Mo=NiMo+
:L (1622K, 51.0mol%Ni-31.6mol%W-17.mol%)=(Ni)+W+
:L (1260K, 71.0mol%Ni-.0mol%W-.0mol%)=(Ni)++
:L (1291K, 65.mol%Ni-.8mol%W-29.8mol%)=++
P₁:L (2115K, 23.8mol%Ni-43.1mol%W-33.1mol%)+WB=+
P₂:L (1657K, 48.mol%Ni-33.1mol%W-18.0mol%)+=W+
The calculated phase diagrams are expected to be useful for the development of new Ni-based heat-, corrosion- or wear-resistance alloys.

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Three new dibenzocyclooctadiene lignans, epigomisin O(1), gomisin () and angeloylgomisin Q(26), were isolated from the fruits of Schizandra chinensis BAILL.(Schizandraceae), which are used as an antitussive and a tonic under the names of "Hoku-gomisi" in Japan and "Wu-wei-zi" in China. 1) The structure of epigomisin O(1) was elucidated by correlation with known lignans, gomisins O(2) and N(). 2) Oxidation of with KMnO_ in a mixture of 2% NaOH and pyridine gave compounds and . Further oxidation of with KMnO_ gave . Reduction of with NaBH_ afforded deangeloylgomisin (6). The structure of gomisin () was elucidated by the same reaction to correlate with a known lignan, gomisin (8). ) The cleavage of the methylenedioxy group on the aromatic ring with Pb(OAc)_ in dry benzene into diphenol was studied(19-→19-). The structure of angeloylgomisin Q(26) was elucidated by the use of the above reaction to correlate with 6.

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From the fronds of Polystichum tripteron (KUNZE) P_R. a new norcarotenoid glycoside was isolated and shown to be (6R, , R)--hydroxy-megastigma-, -dien--one--O-β--glucoside. The fronds of Dennstaedtia wilfordii (MOORE) CHRIST. contain the same glucoside.

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Brassinolide analogues, (R, 23R, 24R)-2α, , , 23-tetrahydroxy--homo--oxa--ergostan-6-one (24-epibrassinolide) (10) and (S, 23S, 24R)-2α, , , 23-tetrahydroxy--homo--oxa--ergostan-6-one (), were synthesized from brassicasterol (a) in five steps and with ca. 20% overall yield. The key steps are the direct formation of (, 24R)-, -cyclo--ergost--en-6-one () from brassicasterol mesylate (), the acid-catalyzed rearrangement of to (, 24R)--ergosta-2, -dien-6-one (6), and the Baeyer-Villiger oxidation of the tetrahydroxy -ergostan-6-ones and 8.

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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;

;) was performed. At first, we moved drugs from solution with pH 1.2 (1.2±0.05) to pH .0 (.0±0.05) and measure concentration of omeprazole in solution by high-performance liquid chromatography. According to our self-developed formula, pH exposure time of resistance to PDGR for omeprazole is minutes, i.. the active substance should not be released within minutes at pH . The exposure at the second stage was conducted with pH (.0±0.05), that imitated gastric pH after PPI administration. And then we also moved drugs to pH with the subsequent measurement of omeprazole concentration.

Results

Omeprazole concentrations after

, 10, 15, 20, 30, 45, 60 minutes in pH solution at the first stage were different for OO and generics. For OO, these values were ,±0,%; 41,±,0%; 62,8±,0%; 79,±2,%; ,±2,%; 81,6±2,%; 80,6±,%; for Generic1 - 0; 49,±,%; 88,8 ±2,8%; 90,±,%; 88, 2±2,2%; 87,±2,0%; 85,±1,1%; for Generic2 - 0; 30,6±6,%; 66,±8,2%; 76,±,%; ,8±,%; ,0±,%; 84,6±,%: for Generic - 80,8±,6%; ,±1,%; , 8±,2%; ,±2,%; 81,±2,1%; ,1±2,0%; ,0±2,%; for Generic - ,±1,%; 84,±0,8%; 84,2±1,2%; , ±0,%; ,±0,%; ,±0,%; ,8±1,1%, respectively.

An analysis of the omeprazole concentration in pH

solution at the second stage revealed the following parameters after the same time: for OO - ,±0,6%; 40, ±,0%; 62,8±2,0%; 80,0±,1%; 85,±2,%; ,8±,%; 80,±,%; for Generic1 - 0; 67,0±,8%; 89,±2,%; 91, ±,%; 89,1±1,6%; 88,±1,%; 87,8±1,2%; for Generic2 - 0; 42,2±,6%; 75,1±,%; 81,0±6,0%; 88,±,2%; 88, 6±1,%; 87,±1,0%; for Generic - 85,±0,%; 85,6±0,%; 84,±0,%; ,±,0%; 84,±0,%; 84,±0,%; 84,±0,%, respectively. Generic release and degradation were completely realized at pH .

Conclusion

Decreased gastric stability of Generic

and Generic 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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A boron treated copper bearing HSLA steel containing austenite formers like manganese and nickel, somewhat lower in amount than that in HSLA 100 variety of steel is chosen for the study. The role of thermomechanical processing on the microstructure and mechanical properties of the above steel has been investigated. Differential scanning calorimetric study is carried out for understanding the precipitation behaviour of copper in HSLA steel under the influence of boron. The microstructure of the experimental steel is found to consist of laths of martensites and bainite. MA constituents of ribbon like morphology are observed at the lath boundaries. Higher strength properties of the steel are attributed to the presence of finely distributed precipitates of copper and microalloy carbides.

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Activity-directed isolation of the ethyl acetate, methylene chloride and n-hexane fractions of Gloiopeltis furcata resulted in the isolation of 18 compounds. Their structures were elucidated as 2-(-hydroxy--oxotetrahydrofuran--yl)acetic acid (1), glutaric acid (2), succinic acid (), nicotinic acid (), ()--hydroxyhex-2-enoic acid (), cholesterol (6), -hydroxycholesterol (), uridine (8), glycerol (), -(hydroxymethyl)-2-methoxybenzene-1,-diol (10), (,)--oxodeca-,-dienoic acid (11), (Z)--ethylidene--methylpyrrolidine-2,-dione (12), dehydrovomifoliol (13), loliolide (14), cholesteryl stearate (15), palmitic acid (16), cis-,8,11,14,17-eicosapentaenoic acid (17) and α-linolenic acid (18) on the basis of spectroscopic and chemical evidences. Their anticholinesterase and antioxidant activities were evaluated via inhibitory activities on acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) as well as scavenging activities on 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical and peroxynitrite (ONOO⁻). All isolated compounds (1—18) exhibited moderate AChE inhibitory activities with IC₅₀ values ranging from 1.14—12.50 μg/ml, whereas 1, , , 17, and 18 showed mild BChE inhibitory activities with IC₅₀ values ranging from .57—15.89 μg/ml. Although most of the compounds isolated were lacking the scavenging activity on DPPH radical and ONOO⁻, and 10 showed good DPPH radical scavenging activity, and , 10, and 16 showed potent ONOO⁻ scavenging activity.

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