A sample of [³H] tobrarnycin (5, 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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 The stability of

‒tetrahydrocannabinol acetate (‒THC‒OAc) and ‒tetrahydrocannabinol acetate (‒THC‒OAc) in -liquid during storage was investigated. ‒THC‒OAc liquids in cartridges were stored at 80℃ or 30℃ for 28 days. The relative concentrations of cannabinoids in the liquids were measured by gas chromatography with flame ionization detection. ‒THC‒OAc decreased during storage at either temperature. ‒THC, a minor impurity, also decreased. ‒THC‒OAc liquid in a cartridge was stored at 80℃ for 57 days. The concentration of ‒THC‒OAc and ‒THC, a minor impurity, did not change during that time. Cannabinol acetate increased in all liquids, and unknown products were also detected by gas chromatography/mass spectrometry (GC/MS). The ‒THC‒OAc and ‒THC‒OAc liquids were subjected to GC/MS to detect representative diluents, glycerol, propylene glycol, and polyethylene glycol 400, but none of these were detected.

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This report describes a patient with extramedullary relapse of acute myeloid leukemia (AML) without involving bone marrow. A 57-year-old man was diagnosed as having acute monoblastic leukemia with t(;11)(p;q23) and trisomy . Ten months after achieving complete response (CR) with chemotherapy, masses developed in his left forearm and in the back of his thigh, preceded by enigmatic peripheral neurological symptoms. Aspiration from the forearm showed leukemic relapse, and fluorescence in situ hybridization (FISH) revealed that the majority of the cells had 11q23 anomaly and tetrasomy . Bone marrow or meningeal relapse was not observed. To our knowledge, this is the first case report of clonal evolution associated with the development of myeloid sarcoma as a relapse in AML.

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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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 We examined the stability of

-tetrahydrocannabinol acetate (-THC-OAc) and -tetrahydrocannabinol acetate (-THC-OAc) in -liquid products. Eight samples were heated at 30℃ for 28 days and one of them was heated at 70℃ for 2, 4, , 10, and 15 days. Residual ratios of -THC-OAc and -THC-OAc were evaluated by gas chromatography with flame ion detection and their degradation products were examined by gas chromatography/mass spectrometry (GC/MS). Some samples were tested for solubility in hexane and were submitted to GC/MS analysis to detect propylene glycol and glycerol. After a 28-day incubation at 30℃, -THC-OAc was slightly decomposed (residual ratio: 84.5–94.2%) but -THC-OAc was almost stable (residual ratio: 95.2–108.%). Heating at 70℃ decomposed not only -THC-OAc but also -THC-OAc. The decomposition proceeded rapidly in the initial 2 days then slowly until 15 days later. The degradation products, four putative one-oxygen-atom adducts and cannabinol, were detected but deacetylated products (-tetrahydrocannabinol and -tetrahydrocannabinol) were not detected. All the samples tested were completely dissolved in hexane differently from propylene glycol and glycerol. Propylene glycol and glycerol were not detected from the samples completely dissolved in hexane. This study indicated that deacetylation of -THC-OAc and -THC-OAc did not proceed when the sample did not contain propylene glycol and glycerol.

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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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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, 71.5mol%Ni-6.0mol%Mo-.5mol%)=(Ni)++
:L (1355K, 62.5mol%Ni-2.5mol%Mo-30.5mol%)=++
:L (1445K, 42.0mol%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, 53.5mol%Ni-33.7mol%Mo-12.mol%)+Mo=NiMo+
:L (1622K, 51.0mol%Ni-31.6mol%W-17.4mol%)=(Ni)+W+
:L (1260K, 71.0mol%Ni-7.0mol%W-.0mol%)=(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-18.0mol%)+=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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急性骨髄性白血病(AML)の寛解導入療法において，海外の基礎および臨床研究では，IDRの有用性が数多く報告され，IDRとシタラビン(Ara-C)の組み合わせが治療戦略の主体となっている。われわれは1995年5月から1998年10月までの当科におけるIDRを寛解導入療法に用いた初発AML41例について，その臨床経過，寛解率，再発率，予後について検討した。その成績は当科での92年から95年に行った，寛解導入にDNRを用いたJALSG-AML92登録26例の成績とほぼ同等であった。なお前者では，従来予後良好因子とされているt(;21)(q;q)を有する症例5例が全例再発し，IDRによる寛解導入療法ではこの染色体異常は予後を反映しないことが示唆されたが，CD56陽性など予後不良因子が加味していたことも疑われる。今後長期予後を期待するためには，寛解導入後の地固め療法をより強化することが必要と考えられた。

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Two new partially saturated tricyclic ring systems, 6, 6a, 7, , , 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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The Gujarat earthquake in India occurred in January, 2001, and caused significant damage in the province of Gujarat. The Japanese Geotechnical Society sent a small reconnaissance team to the damaged region after the quake. The present text presents the report from this activity. The major attention of the team was focused on geotechnical aspects of the damage which were related to earthfill dams and harbor land fills. It was found that a significant portion of damage was concentrated in fills resting on soft natural soils. Swedish weight soundings which were conducted at two places demonstrated the existence of such a soft subsoil. From this, it was concluded that amplification of earthquake shaking as well as the permanent deformation in the soft foundation soil induced such kinds of damage as subsidence, cracking, and lateral spreading in overlying artificial fills. For the better seismic resistance of those affected fills during future earthquakes, the improvement of soft subsoil seems essential.

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The boundary element method expanded in frequency domains is presented to analyze the dynamic interaction between an embedded flexible rectangular foundation and soil with consideration of the obliquely incident waves. Numerical results describing the influence of the flexibility of the foundation on the dynamic responses of the foundation due to obliquely incident waves indicate that the flexibility of actual foundations can diminish the reduction of translation responses and increase the rotational responses in the high frequency range. These phenomena are more conspicuous as the embedment ratio is larger and the value of the wave velocity ratio of the soil and the foundation approaches to unity. When the high frequency components of the input ground motion are important and the basement has higher flexibility (for example ₂v_s/₁v_s >0.4), the analysis method which considers the basement as a rigid foundation may lead to unsafety estimations and the estimation of the flexibility of the foundation is necessary as analysing the effective input motion with consideration of the incident waves.

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(³H) Tobramycin was used as a probe to determine the relationship between the structure of aminoglycoside antibiotics and their ability to remove this drug from its higher affinity binding site on the ribosome. The dissacharide moieties (neamine, tobramine, gentamine) appeared to have a common binding site, whereas the kanosamine, garosamine and ribose moieties determined the specificity of this binding. Amikacin and butikacin behaved in an anomalous manner in spite of their close structural relationship to tobramycin.

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In the first part of the present work the interaction of glycophorin with dimyristoylphosphatidylcholine (DMPC) is studied by freeze fracture electron microscopy, densitometry, calorimetry, and 90° static light scattering. An exothermic lipid/protein interaction energy of W_P=190 kJ•mol^-1 was found by application of the well known Van Laar relation for the displacement of the freezing point and the Gibbs-Duhem relationship. Secondly, the effects of Ca²⁺ on the lipid/protein interaction were studied. Following Ca²⁺ addition a remarkable decoupling of the interaction of the glycophorin head group with the bilayer surface was revealed by densitometry and gold-labeling electron microscopy. It is estimated that about 80% of lipid once disturbed by the adsorption of glycophorin head groups is decoupled after addition of Ca²⁺. Thirdly, the selective interaction of glycophorin with binary lipid mixtures was studied, including the mixtures of DMPC with dimyristoylphosphatidylserine (DMPS) and dilauroylphosphatidylcholine (DLPC), and the mixture of dipalmitoylphosphatidylcholine (DPPC) with DLPC.

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11-Amino-6, 6a, 7, , , 10, 10a, 11-octahydrodibebenzo[, ]thiepines (6a-d) and -oxepines (7a-d) were synthesized by the Leuckart reaction of 6, 6a, 7, , , 10, 10a, 11-octahydro-11-oxodibenzo[, ]thiepines (1a, )and -oxepines (2a, ) followed by hydrolysis of the reaction products 4a-d and 5a-d, respectively. The four diastereomers, cis(6a-H, 10a-H)-cis(10a-H, 11-H) 6a and 7a, cis(6a-H, 10a-H)-trans(10a-H, 11-H) 6 and 7, trans(6a-H, 10a-H)-trans(10a-H, 11a-H)6c and 7c, and trans(6a-H, 10a-H)-cis(10a-H, 11-H) 6d and 7d, 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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Brassinolide analogues, (R, 23R, 24R)-2α, 3α, , 23-tetrahydroxy--homo-7-oxa-5α-ergostan-6-one (24-epibrassinolide) (10) and (S, 23S, 24R)-2α, 3α, , 23-tetrahydroxy--homo-7-oxa-5α-ergostan-6-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-6-one (4) from brassicasterol mesylate (3), the acid-catalyzed rearrangement of 4 to (, 24R)-5α-ergosta-2, -dien-6-one (6), and the Baeyer-Villiger oxidation of the tetrahydroxy 5α-ergostan-6-ones 7 and .

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Melithasterols A-D (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, 7α -dihydroxy-5α, 6α-epoxy-Δ^ steroid nucleus. This was confirmed by direct comparison with the authentic sample prepared by lead tetra-acetate oxydation of cholest-6-ene- 3β, 5α, α-triol 3-monoacetate. Twelve new polyhydroxysterols were isolated from an Alcyonium sp. (7,,), 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 7 to were identified as 24-methylenecholest-5-ene- 3β, 16β-diol-3-0-α-L fucoside (7) and its 7β-() and 7α-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, 6β-glycolation. Compound 16 was shown to be 5β, 6α-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 7-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-6-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, 6α, 12ξ-triol--one, respectively, by spectral analyses (H-HCOSY, HMQC, HMBC).

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