11-Amino-, a, , 8, , 10, 10a, 11-octahydrodibebenzo[, ]thiepines (a-) and -oxepines (a-) were synthesized by the Leuckart reaction of , a, , 8, , 10, 10a, 11-octahydro-11-oxodibenzo[, ]thiepines (1a, )and -oxepines (2a, ) followed by hydrolysis of the reaction products 4a- and 5a-, respectively. The four diastereomers, cis(a-H, 10a-H)-cis(10a-H, 11-H) a and a, cis(a-H, 10a-H)-trans(10a-H, 11-H) and , trans(a-H, 10a-H)-trans(10a-H, 11a-H)c and c, and trans(a-H, 10a-H)-cis(10a-H, 11-H) and , were isolated and their configurations and conformations were elucidated by chemical methods together with ¹H-nuclear magnetic resonance spectroscopic and X-ray crystallographic analyses.

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Two new partially saturated tricyclic ring systems, , a, , 8, , 10, 10a, 11-octahydro-11-oxodibenz [, ] oxepins (3a and 3), and -thiepins (4a and 4) were synthesized. Compounds 4a and 4 were desulfurized to give a pair of isomeric 2-methylbenzoylcyclohexanes (10a and 10). Deuterated 4a and 4 (11a and 11) were prepared starting from butadiene- (12). The stereochemical features of 3a (trans), 3 (cis), 4a (trans) and 4 (cis) are compared with those of 10a, 10, 11a and 11 on the basis of proton nuclear magnetic resonance data.

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We screened the differentiation-inducing activities of 39 mushroom extracts from Akita prefecture, Japan, on the mouse osteoblastic cell line, MC3T3-1. Sixteen phosphate buffered saline (PBS), 8 boiled PBS, 14 ethanol and 12 methanol extracts induced alkaline phosphatase (ALP) activities, an indicator of MC3T3-1 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-3β,5α,-triol (1). 1 induced ALP activities of MC3T3-1 cells and promoted cell proliferation. To investigate the relationships between the chemical structure and differentiation-inducing activity of the compound, ALP-inducing activities of MC3T3-1 cells by 1, ergosterol (2), ergocalciferol (3), cholesta-3β,5α,-triol (4), -dehydrocholesterol (5) and cholecalciferol () were tested. The enzyme activities of MC3T3-1 cells were increased 3.0-fold by 10 μM 1 and 2.4-fold by 10 μM 4. However, 2, 3, 5 and did not induce MC3T3-1 cell ALP activity at 0.1—10 μM. These results suggested that the OH groups at C-5 and/or C- of 1 and 4 played an important role in their differentiation-inducing activities on MC3T3-1 cells. Furthermore, 1 suppressed induction of MC3T3-1 cell apoptosis by serum starvation.

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Chemical properties of ergosta-4, , 8(14), -tetraen-3-one (1) were investigated. Though 1 is rather stable to acids or bases, it reacts easily with two moleculres of oxygen on irradiation with UV light to give , -epidioxy-14α-hydroperoxyergosta-4, , -trien-3-one (2), which is transformed successively to , ;8α, -diepoxy-14α-hydroperoxyergosta-4, -dien-3-one (3) and 14α-hydroperoxy--hydroxyergosta-4, , -triene-3, -dione (4) under these reaction conditions.

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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 (3), (4), (5) X(), Y () and Z (8) were confirmed by extensive 1 and 2 NMR spectral data and X-ray analysis. Blazeispirols A (1), (2), C (3), (4) and (5) were des-A-ergostane type compounds having spiroacetal structure as a side chain. Blazeispirols X () and Y () were determined to be (20S, S, 23R, 24S)-1 (10→) abeo-14β, :, 25-diepoxyergosta-5,,,11-tetraene-3α,23-diol and (20S, S, 23R, 24S)-14β,:,25-diepoxy-,23-dihydroxyergosta-4,,11-triene-3,-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-4, C-5 and C-1, C-10 bonds on retro aldol condensation and Michael reaction via such as intermediate A as shown in Fig. 4. 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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Natural sedimentary clays exhibit ageing effects on their behaviour when subjected to both consolidation and shearing. Attempts to characterising the in-situ 'structure'of soft marine clays have been made in case studies performed in Ariake (Japan) and in Bangkok (Thailand), each showing a typical profile of aged clay-structure with depth reflecting its site-specific geological consolidation history. In each site, profiles of Atterberg limits, natural water content, overconsolidation ratio (OCR), quasi-elastic shear modulus G_max and the undrained shear strength c_u with depth were attained from various laboratory tests, together with the a comparable profile of quasi-elastic shear modulus from insitu seismic survey G_f. Quantitative assessment of the aged clay-structure was made by using two different measures, metastability index MI (G) and the soil constant reflecting structure S (Jamiolkowski et al., 1994). The profiles of MI (G) and the S-value with depth were both determined based on the corresponding G_max behaviour of the reconstituted sample. "Disturbance"of laboratory samples retrieved by using two different samplers (i.., Laval and Japanese thin-walled samplers) with two different sampling techniques (i.., pre-boring and displacement methods) was discussed. A new approach to estimate c_u"in the ground", termed by the authors the MILK (Metastability Index coupled with Laboratory K_o test) method, is proposed. A trial of the MILK-method is demonstrated in soft Bangkok clay, the texture of which is similar to "soft cheese".

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The advantages and disadvantages of using a back analysis of slope failures to evaluate soil shear strength are discussed. A methodology is presented herein that allows the implied level of reliability associated with soil shear strength parameters back calculated from slope failures to be estimated. A reliability approach is also used to estimate the probability of failure for a given limit equilibrium slope stability method, design factor of safety, and combination of back calculated Mohr-Coulomb shear strength parameters, c' and φ'. The methodology is illustrated using 39 landslides in the Orinda Formation in the San Francisco Bay area. The impact of additional case histories in the same geologic setting, i.., a larger data set, on the required design factor of safety for a given probability of failure is also investigated.

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A new analytical method is proposed for determining the inextensible grid reinforcement pullout resistance and pullout force/pullout displacement curve by using basic backfill soil and grid reinforcement properties. The pullout skin friction resistance/pullout displacement relationship is simulated by linear elastic-perfectly plastic model. A hyperbolic model has been proposed to represent the pullout bearing resistance/pullout displacement relationship in which the maximum bearing resistance of a single bearing member is determined using a new bearing capacity equation proposed in this paper. The influences of the grid bearing member spacing ratio, S/, the bearing member deflection rigidity, and the pullout softening behavior on the mobilization of pullout bearing resistance are explicitly included in the proposed model. Good agreement has been obtained between calculated values and laboratory test results.

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厚生省の高齢者の聴力に関する研究班は65歳以上の高齢者の聴力を調査した. 測定周波数の平均聴力レベルはA群 (65～69歳) で35.0dB, 群 (70～74歳) で42.1dB, C群 (75～79歳) で46. 1dB, 群 (～84歳) で52. 1dB, 群 (85歳以上) で55.dBであった. すべてのグループにおいて聴力の男女差はみられず, オージオグラムの型は大部分の例で高音漸傾型を示した. 平均語音弁別能はA群で75.4%, 群で70%, C群で63.8%, 群で59.%, 群で52.1%, また, SISI検査で70%以上を示した率はA群で45.2%, 群で49.3%, C群で47.%, 群で51.%, 群で59.%であった.

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Melithasterols A- (1-4), isolated from a gorgoinan coral Melithaea ocracea of Okinawa, were shown to be cholestane-, 24-methyl--dehydrocholestane-, -dehydrocholestane-, and 24-methylenecholestane-derivatives. respectively, having a common 3β, α -dihydroxy-5α, α-epoxy-Δ^8 steroid nucleus. This was confirmed by direct comparison with the authentic sample prepared by lead tetra-acetate oxydation of cholest--ene- 3β, 5α, 8α-triol 3-monoacetate. Twelve new polyhydroxysterols were isolated from an Alcyonium sp. (,8,), and Sclerophytum sp. (14,16,19,20,21,a,23,26,28) soft corals collected off the coasts of the Andaman and Nicobar Islands in the Indian Ocean. All the Sclerophytum sp. soft corals contained 17a or its 25-deacetyl derivative. Compounds to were identified as 24-methylenecholest-5-ene- 3β, 16β-diol-3-0-α-L fucoside () and its β-(8) and α-hydroxy () derivatives. Compound 14 was shown to be 24S-24-methylcholest-5-ene-3β,25ξ,26-triol and was correlated to the known compound 15 by 5α, β-glycolation. Compound 16 was shown to be 5β, α-isomer of 17, correlating to 17 by PCC oxidation followed by dehydration. Compound 19 was identified with 25-deacetyl derivative of the known compound lobosterol (19a) by hydrolysis of authentic lobosterol. Compounds 20 and 21 were shown to be -dehydro-(20) and -dehydro-(21) derivative of 17a and 17, respectively, by comparisons of their spectral data with reference compounds. Compounds a and 23 were 24S-methylcholestane-3β, 5α 25-triol--one 25-monoacetate (a) and its 25-deacetoxyl derivative (23). Partial PCC oxidation of 17a afforded a. Compounds 26 (andamansterol) and 28 (nicobarsterol) were shown to be gorgost-5-ene-3β, α. 11α, 21-tetrol and novel secosteroid, 11,21-cyclo--homo-11-oxa-, 11-secoergostane-3β, α, 12ξ-triol--one, respectively, by spectral analyses (H-HCOSY, HMQC, HMBC).

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Mycobacteriocin produced by human type tubercle bacilli could be demonstrated easily on eggmedium containing 0.05% tween by means of stab culture or streak plate methods, and elevenmycobacteriocin-types have been recognized on the basis of the inhibition pattern by using indicator strains of rapidly growing mycobacteria.
At present, types 1 (4.%), 2 (13%), 4 (38.5%), (2%) and 11 (14.8%) showed a stablemycobacteriocin pattern, but types 3 (.8%) and (.%) were apt to show type replacement totypes 2 and 4, respectively, and strains belonging to types 5, and 8 were few, less than 1.5%to the total. In order to perform a reproducible mycobacteriocin typing, our previous typingscheme was revised to be consisted of five groups (A-). Among 438 strains, mycobacteriocingroup C containing types 4 and was 46.1% of strains tested, group containing types 2, 3 and was .%, group containing type 11 was 15.1%, group A containing types 1 and 8 was5.5%, group containing types and 10 was 4.1%, and untypable strains were no more than .% among all tested strains.
Human type tubercle bacilli classified as type 4, which consisted of more than 45% of strainstested, could be divided into three sub-types from sensitivity to M. gordonae 1324 and M. terrae 1450.
Mycobacteriocin producing strains belonging to type : showed an extremly wide antibacterialactivity to strains of more than 90% of rapidly growing mycobacteria (42 strains), to about 40% of slow growing mycobacteria (29 strains), and even to 10 strains of Staphylococcus aureus.

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From the fronds of Polystichum tripteron (KUNZE) P_R. a new norcarotenoid glycoside was isolated and shown to be (R, , R)--hydroxy-megastigma-4, -dien-3-one--O-β--glucoside. The fronds of Dennstaedtia wilfordii (MOORE) CHRIST. contain the same glucoside.

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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

), bla_CTX-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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Using the so-called pseudo-static method, a stability analysis was made for the mountain slide that took place at Mitake-iriya village at the time of the Izu-Ohshima-Kinkai earthquake of January 14, 1978. Undisturbed samples of volcanic clay were obtained in blocks from the exposed surface of the deposit identified to have been the sliding surface. The partially saturated clay samples were tested under consolidated undrained conditions using the triaxial test equipment. Dynamic axial stresses with irregular time histories were applied to the specimens in combination with statically sustained axial stresses to determine the soil strength under the conditions simulating in-situ states of stress during the earthquake. The results of the tests were expressed in terms of the Mohr-Coulomb type failure criterion which showed that, while the angle of internal friction remained almost unchanged, the cohesion component in irregular loading increased above values obtained in the static loading. Using the strength parameters thus determined, a pseudo-static analysis was made to check the stability of the soil masses that had actually slid during the 1978 earthquake. The maximum horizontal acceleration required to cause the slide was computed. The computed accelerations were shown to cover a range between 400 and 500 gals which is consistent with the range estimated by other investigators on the basis of overturning of tombstones in the vicinity of the slide area.

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The gamma-ray spectrum and the conversion-electron spectrum are measured in the decay of the Tb¹⁵² activity. The L-subshell electron lines of the 586. keV +→2₁⁺ transition are separated by the ion-free beta-ray spectrometer. The M1-2 mixing ratio, δ², and the dimensionless ratio X of 0-2 mixing of the 586. keV transition are obtained to be δ²≤0.16 and 0.034≤X≤0.038, respectively. The 2 branching ratio (2; +→0_g⁺): (2; +→2₁⁺): (2; +→0₁⁺) is determined to be 0.023 : 1.0 : 5..

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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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Brassinolide analogues, (R, 23R, 24R)-2α, 3α, , 23-tetrahydroxy--homo--oxa-5α-ergostan--one (24-epibrassinolide) (10) and (S, 23S, 24R)-2α, 3α, , 23-tetrahydroxy--homo--oxa-5α-ergostan--one (), were synthesized from brassicasterol (3a) in five steps and with ca. 20% overall yield. The key steps are the direct formation of (, 24R)-3α, 5-cyclo-5α-ergost--en--one (4) from brassicasterol mesylate (3), the acid-catalyzed rearrangement of 4 to (, 24R)-5α-ergosta-2, -dien--one (), and the Baeyer-Villiger oxidation of the tetrahydroxy 5α-ergostan--ones and 8.

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Using two direct introduction methods, DNA synthesis or cell proliferation activities of three purified proteins from . coli, namely, human papillomavirus (HPV) proteins of type 16, a mutant type 16 (24 C-G) (transformation defective) and type , were measured in mouse fibroblast, C127 cells. By a microinjection method, the order of the cell mitotic indexes for the three proteins as determined by 5-bromo-2'-deoxy-uridine (BrdU) staining was type 16, and 16 (24 C-G). By the osmotic shock method, the ³H-TdR incorporation and coloration by (3-carboxymethoxy phenyl)-2-(4-sulfophenyl)-2H-tetolazorium (MTS) for the three proteins correlated with the pRb binding and focus forming activities previously reported (hunger et al. 1991). These results indicate that the simple osmotic shock method for direct protein introduction may be generally useful for transformation assays of oncoproteins.

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