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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Two new polyacetylene compounds (, , 12)-1-acetoxy--isovaleryloxytetradeca-, , 12-trien-, 10-diyn-14-ol (), and (, , 12)-1-acetoxy--(2-methylbutyryloxy)tetradeca-, , 12-trien-, 10-diyn-14-ol () have been isolated along with (, , 12)-1-acetoxy--senecioyloxytetradeca-, , 12-trien-, 10-diyn-14-ol (A) from Atractylodes Rhizome (Karabyakujutu). The structures of these compounds were determined on the basis of their spectral data.

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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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The activities of tobramycin derivatives acetylated and ethylated on the '-N, 2'-N and -N positions were examined. The MICs of these derivatives against tobramycin sensitive strains indicated that 2'-N-ethylated and '-N-ethylated derivatives have a fairly good activity, and confirmed that the -N position is the most important one for antibiotic activity since -N derivatives were less active. The MICs of these derivatives against tobramycin resistant strains, and their inactivation by tobramycin modifying enzymes were examined. These results showed that 2'-N or '-N ethylation protects the drug against inactivation by AAC(2') or AAC('), respectively, and 2'-N-ethyltobramycin and '-N-ethyltobramycin were active against strains containing these modifying enzymes. On the other hand, -N ethylation protects the drug against inactivation by AAC() but -N-ethyl tobramycin does not inhibit strains containing this enzyme.

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The Beckmann rearrangement of aliphatic ketone oximes, R(CHs)=NOH (R=Et (1); n-Pr (2); iso-Pr (); iso-Bu ()), with polyphosphoric acid (PPA), polyphosphate ester (PPE), and ester of phosphoric acid (2 P- R) was carried out and migratory ratios ((a)/() in eq. (1)) were determined, The results are shown in Fig.1, 2, and , respectively.
In Fig.1 and 2, the migratory ratios decrease with reaction time and nearly approach to the ratios of anti-alkyl form/syn-alkylform in benzene(A1) or DMSO(A2)except for () (See Table 1). From this fact, it has been found that PPA and PPE are inactive for isomerization of the oximes andanti-alkyl oximes rearrange faster than syn-alkyl ones. ln the case of (), migratery ratios are smaller than Ai or A2. As acetonitrile is detected by GLC, it is presumed that fission has been occurred simultaneously with rearrangement in anti-alkyl oxime (eq. ()). In the case of 2 P- R, all modes of the reaction arethe same as in above, except that the rate of fission is tnuch faster than that in PPA and PPE.
The reaction of anti-alkyl ketone oximes having a bulky grouphas been greatly influenced by the use of sterically demanding catalysts such asPPA, PPE, and 2 P- R.

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New-type inducers of differentiation of human promyelocytic leukemia cells HL-60, i.

e

., - (, , , -tetrahydro-, , , -tetramethyl-2-naphthalenylcarbamoyl) benzoic acid (Am 80) and () -- [- (, -di-tert-butylphenyl) --oxo-l-propenyl] benzoic acid (Ch 55), suppress -myc expression as all-trans-retinoic acid (RA) does. The decreased level of -myc expression was detected within -14 h after the start of treatment, and preceded morphological differentiation and functional differentiation measured in terms of nitroblue tetrazolium (NBT) reduction. Treatment of HL-60 cells with 0.1 μm Am 80, Ch 55 or RA for h caused more than 90% suppression of -myc expression and around 10-fold increase in the percentage of NBT-positive cells.

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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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This study was performed to clarify which factors affected damage to tame-ike (small embankment dams for irrigation) in Hokudan Town as a result of the January 17, 1995 Hyogoken-Nambu earthquake. Factors were assumed to be : Location (.g., Distance to Epicenter, etc.), Structure (.g., Angle to Nearest Fault, Embankment Volume, etc.), Soil Properties of Embankment, Geology of Dam Site and History (Era of Construction, Repaired, etc.). Multivariate statistical analyses were performed for documentary data (damaged : 181, undamaged : 328). Ordinary statistical analyses were conducted for the data investigated in situ for soil properties of the embankment. The results show that the factors causing damage to dam are : (1) Nearest Fault (Nojima, Mizukoshi and D2), (2) Distance to Nearest Fault (less than 500 m), () Distance to Epicenter (approximately to 14 km, which almost agrees with the location of seismic intensity JMA), () Elevation of Dam Site (higher than 100 m), () Embankment Volume (the greater the volume the more damage was caused), () Direction of Dam Axis (normal or diagonal to the epicenter or to nearest the fault), () Plan View of Dam Axis ( or axes), () Surface Geology of Dam Site (non-cohesive soil type ground), (9) Era of Construction (prior to 1891) and (10) Soil Properties of Embankment (sand, not silty sand or gravel, penetration resistance that is 10% smaller than the undamaged dams).

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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 th-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 th-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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Two new partially saturated tricyclic ring systems, , a, , , 9, 10, 10a, 11-octahydro-11-oxodibenz [, ] oxepins (a and ), and -thiepins (a and ) were synthesized. Compounds a and were desulfurized to give a pair of isomeric 2-methylbenzoylcyclohexanes (10a and 10). Deuterated a and (11a and 11) were prepared starting from butadiene- (12). The stereochemical features of a (trans), (cis), a (trans) and (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 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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The objective of this article is to propose and evaluate a sliding-block model to deal with very large displacements of slopes when a horizontal earthquake is applied. The slip surface consists of two inclinations on which full shear resistance is mobilized. Internal shearing exists along a sub-plane that intersects the angle between the two sub-planes that form the external slip surface. The ratio of the distance moved along the two external sub-planes depends on the inclination of the internal sub-plane. If there is a water table line, undrained conditions are assumed during motion and total stress analysis is performed. The governing equations of motion are formulated, analytical solutions are obtained for some cases, and back-analysis of four well-documented slides is performed.

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This paper is concerned with an extension of a rotational limit equilibrium method for determining the permanent displacements of slopes under seismic excitation. In the proposed procedure, the sliding mass is treated as a rigid rotating body defined by a log spiral trace. Permanent displacements are obtained by double-integration of the equation of motion in a manner similar to Newmark's translational sliding block method. The seismic slope stability analysis is based on the rotational (variational) limit equilibrium approach. This stability analysis was verified with dynamic experimental results obtained from centrifuge model testing. A series of parametric studies was conducted on"unstable"slopes, investigating the effects of soil properties and characteristics of excitation on the magnitude of permanent displacements. The higher the frictional angle, the smaller the permanent displacement of the slope is. Low excitation frequency yields larger slope displacement if the excitation is extended for the same time period of time. The effect of frequency becomes less distinct when a larger value of yield seismic coefficient is used. The proposed procedures produce a rational criterion to evaluate the seismic performance of simple slopes. This criterion is based on permanent displacement limit rather than factor of safety alone.

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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 (), (-)-caryolivine (), (+)-1, 2-dehydro-2-norlimacusine (9) and N-formylstepharine (). 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 .

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It has been shown after mathematical and mechanical investigation that Limit Equilibrium Method (LEM) can be considered as a method to obtain the necessary condition of Slip Line Method (SLM), and that the solution can be obtained under the condition that F_s=1 and ∂F_s/∂θ=O, where F_s is the safety factor and θ is the inclination of the plane on which the safety factor is defined. Next, the generalized LEM (GLEM) is proposed, dealing with the following points : (1) Triangular or quadrangular blocks can be treated; (2) Safety factors are defined also on interblock planes; and () All types of plastic problems, slope stability, bearing capacity, and earth pressure are identically formulated. Two situations regarding treatment of the moment equilibrium condition are discussed. GLEM is applied to well-known problems. The results agree well with those obtained by theoretical methods. GLEM can be used to obtain the distribution of earth pressure or bearing capacity. GLEM, Iike ordinary LEM, is very effective for the practical problems, but GLEM is more theoretical and it can result in more accurate solutions.

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