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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One method currently being considered for the disposal of high level radio-active waste is burial in the seabed. When a hot object is buried in soil, the temperature of the soil adjacent to the object is raised and there is transient heat flow away from the object. The rise in the temperature of the soil causes excess pore pressures to be generated and transient pore water diffusion also takes place. A finite element formulation of the coupled heat flow and consolidation problem is presented. The computer implementation of this formulation is found to compare favourably with analytical solutions based on the same physical principles.

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Repetitive liquefactions in angular and subangular gravels from an alluvial fan, in the case of two earthquakes with accelerations lower than that of a former which had caused liquefaction some months before, are described. The liquefaction took place from the surface, down to a depth of approximately 10 m. Water laden with sediments spouted out for some tens of minutes after the strong motion ceased. Knowledge of the grain size distribution of the sediments inside the body of the alluvial fan roughly defines the areas of the fan prone to future liquefaction. Non-repetitive liquefaction in overconsolidated fine fluvio-lacustrine sand of glacial origin at the unusual depth of 14 m to 16 m is also described. From the observation of sand lifted up for 10 m inside a large diameter well, and of that which spouted out from several microvents, it was estimated that extra-pore pressure was close to lithostatic conditions. Nevertheless, modeling of intrinsic pore pressure buildup on the DESRA2 programme gives lower values than the experimental one. Geotechnical characteristics of the 12 m-thick sandy stratum indicate that the upper part is unusually soft, either due to water circulation or past repetitive liquefactions which prevented reconsolidation. It is suggested that excess pore pressure generated by the earthquake was also due to redistribution of pressure from adjacent sediments.

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Two new partially saturated tricyclic ring systems, 6, 6a, , , , 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-d₆ (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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Nine isoquinoline alkaloids belonging to the protoberberine, proaporphine and bisbenzyl-isoquinoline series were isolated from Caryomene olivascens (Menispermaceae). Four compounds are new : (-)-2-norlimacine (4), (-)-caryolivine (6), (+)-1, 2-dehydro-2-norlimacusine () and N-formylstepharine (3). The last one is the first N-formyl derivative to be reported in the proaporphine group. Its biogenetic origin is discussed. Structures were established on the basis of 360 MHz (FT) nuclear magnetic resonance measurements and also by chemical correlation in the case of 3.

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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.mol%Mo-.mol%)=(Ni)++
:L (1355K, 62.mol%Ni-2.mol%Mo-30.mol%)=++
:L (1445K, 42.mol%Ni-30.6mol%Mo-10.3mol%)=(Ni)+NiMo+
P₁:L (1812K, 34.mol%Ni-42.3mol%Mo-.mol%)+MoB=+
P₂:L (1633K, 42.3mol%Ni-40.4mol%Mo-17.3mol%)+Mo=+
P₃:L (1812K, 53.mol%Ni-33.mol%Mo-12.mol%)+Mo=NiMo+
:L (1622K, 51.mol%Ni-31.6mol%W-17.4mol%)=(Ni)+W+
:L (1260K, 71.mol%Ni-.mol%W-.mol%)=(Ni)++
:L (1291K, 65.4mol%Ni-4.mol%W-29.mol%)=++
P₁:L (2115K, 23.mol%Ni-43.1mol%W-33.1mol%)+WB=+
P₂:L (1657K, 48.mol%Ni-33.1mol%W-18.mol%)+=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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The possibility of attenuation of microseismic waves due to the presence of an upward folding of the ocean bottom into the liquid is discussed in this paper. The upward folding of the ocean bottom has been idealized by means of an irregularity in the form of a rectangle intruding into the liquid and the evaluation of the displacement component at any point of the solid medium has been carried out in two stages. First, the change in the incident mode of the surface wave due to the presence of the rectangular irregularity has been determined, and second, the subsequent change of the resulting displacement components due to the termination of the liquid layer and the step change in elevation of the solid medium at the continental margin has been discovered. Finally, numerical calculation has been made to determine the attenuation of the microseismic waves of different periods due to the presence of the rectangular irregularity at the ocean bottom.

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A sample of [³H] tobrarnycin (, 000 Ci/Mole) has been synthetized and incubated with
the bacterial ribosome and its subunits. The results obtained show that this antibiotic has
two types of binding sites. The primary one is probably responsible for the inhibition of
protein synthesis whereas the secondary one is probably related to the misreading and reading
tiirough of the messenger RNA.

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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;3;4) was performed. At first, we moved drugs from solution with pH 1.2 (1.2±

.05) to pH . (.±.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 4 minutes, i.. the active substance should not be released within 4 minutes at pH . 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 with the subsequent measurement of omeprazole concentration.

Results

Omeprazole concentrations after 4, 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 4,±,%; 41,4±3,%; 62,±4,%; 79,±2,%; 83,±2,%; 81,6±2,%; 80,6±4,4%; for Generic1 - ; 49,3±,%; 88, ±2,%; 90,4±3,%; 88, 2±2,2%; ,3±2,%; 85,±1,1%; for Generic2 - ; 30,6±6,3%; 66,±,2%; 76,4±,4%; ,±,3%; 86,±3,%; 84,6±3,3%: for Generic3 - 80,±3,6%; 83,±1,%; 83, ±3,2%; 83,3±2,%; 81,±2,1%; ,1±2,%; ,±2,4%; for Generic4 - ,±1,%; 84,4±,%; 84,2±1,2%; , ±,%; ,±,%; ,±,%; ,±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 - 4,4±,6%; 40, ±3,%; 62,±2,%; 80,±3,1%; 85,4±2,%; ,±3,4%; 80,±3,%; for Generic1 - ; 67,±,%; ,±2,3%; , ±4,3%; ,1±1,6%; 88,3±1,4%; ,±1,2%; for Generic2 - ; 42,2±,6%; 75,1±,3%; 81,±6,%; 88,4±3,2%; 88, 6±1,3%; ,±1,%; for Generic4 - 85,±,%; 85,6±,%; 84,±,%; ,±3,%; 84,4±,3%; 84,4±,3%; 84,3±,4%, respectively. Generic3 release and degradation were completely realized at pH 4.

Conclusion

Decreased gastric stability of Generic3 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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【目的】LASIK後眼に対しTotal Keratometry（TK）を用いたLASIK用IOL度数計算式と従来式による予測屈折誤差を比較し、TKの有用性を評価する。

【対象及び方法】近視LASIK術後で白内障手術を施行した18例27眼（平均年齢60.4±

.歳）を対象とした。眼軸長、角膜屈折力（K値）、TK値の平均±標準偏差（SD）は、26.±1.mm、39.±1.D、39.2±2.Dであった。比較式はBarrett TK True-K（-TK）式、EVO TK（-TK）式、Haigis TK（H-TK）式とBarrett True-K（）式、EVO（）式、Haigis-L（H）式、Shammas-PL（S）式、Camellin-Calossi（）式とした。予測屈折誤差の絶対値平均±SDと±.D以内の割合を比較した。

【結果】絶対値平均±SDと±

.D以内の割合は-TK式：.18±.16D（96％）、-TK式：.20±.16D（93％）、H-TK式：.46±.39D（52％）、式：.18±.35D（85％）、式（％）：.21±.32D、H式：.35±.25D（78％）、S式：.29±.27D（78％）、式：.37±.33D（56％）であった。

【結論】TK値を用いた

-TK式と-TK式はその他の式と比較して予測屈折誤差が同等又は小さく有用である。

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11-Amino-6, 6a, , , , 10, 10a, 11-octahydrodibebenzo[, ]thiepines (6a-d) and -oxepines (a-d) were synthesized by the Leuckart reaction of 6, 6a, , , , 10, 10a, 11-octahydro-11-oxodibenzo[, ]thiepines (1a, )and -oxepines (2a, ) followed by hydrolysis of the reaction products 4a-d and a-d, respectively. The four diastereomers, cis(6a-H, 10a-H)-cis(10a-H, 11-H) 6a and a, cis(6a-H, 10a-H)-trans(10a-H, 11-H) 6 and , trans(6a-H, 10a-H)-trans(10a-H, 11a-H)6 and , and trans(6a-H, 10a-H)-cis(10a-H, 11-H) 6d and d, 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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Pironetin 1 (PA-48153) is a novel unsaturated δ-lactone derivative isolated from the fermentation broths of Streptomyces species which shows immunosuppressive and plant growth regulating activities. Several total syntheses of 1 have been reported to date, but we show here a novel approach to 1 via a convergent route using our chiral building block, (1S,S,6R)--hydroxybicyclo[4.1.]heptan-2-one . We dissected pironetin at 6- and employed the coupling of the epoxide 16 with the dithiane 25, which would be derived from , as a key step. The THP ether of was methylated and the following reduction gave an inseparable mixture of four diastereomers . After etherification, removal of THP group afforded separable isomers a and in a ratio of 13 to 1. The desired major isomer a was oxidized to ketone 6. Oxidation of 6 via silyl enol ether with osmium tetroxide gave ketol 21 in quantitative yield. Reduction of cyclopropylketone moiety of 21 under Birch condition afforded a mixture of a and . The ketol moiety of a and was oxidatively cleaved with lead tetraacetate in benzene-methanol to give the single aldo-ester 23. Acetalization of 23 followed by reduction of ester group gave aldehyde 24. Introduction of 2-unit via Takai's protocol as -olefin formation followed by thioacetalization afforded the dithiane 25, as -14 unit of pironetin. Meanwhile, the epoxide 16 as 1-6 unit was prepared from known epoxy alcohol 3 in 6 steps. Coupling reaction of two units, the dithiane 25 and the the epoxide 16, successfully gave the product with the whole skeleton 26 in high yield. Mercuric ion assisted hydrolysis of the thioacetal 26 gave ketol 27. Selective reduction of β-hydroxyketone 27 by Mori's method afforded and-diol 28a predominantly (: ). Finally, desilylation and oxidation with manganese dioxide afforded pironetin 1.

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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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