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

e

., - (, , 7, -tetrahydro-, , , -tetramethyl-2-naphthalenylcarbamoyl) benzoic acid (Am ) and () -- [3- (3, -di-tert-butylphenyl) -3-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 , Ch 55 or RA for 96 h caused more than 90% suppression of -myc expression and around 10-fold increase in the percentage of NBT-positive cells.

抄録全体を表示

The Beckmann rearrangement of aliphatic ketone oximes, R(CHs)=NOH (R=Et (1); n-Pr (2); iso-Pr (3); 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 3, 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 (3) (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 (3), 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. (3)). 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.

抄録全体を表示

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.

抄録全体を表示

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), (3) Distance to Epicenter (approximately to 14 km, which almost agrees with the location of seismic intensity 7 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), (7) Plan View of Dam Axis (3 or axes), () Surface Geology of Dam Site (non-cohesive soil type ground), () 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).

抄録全体を表示

(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.

抄録全体を表示

The activities of tobramycin derivatives acetylated and ethylated on the '-N, 2'-N and 3-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 3-N position is the most important one for antibiotic activity since 3-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, 3-N ethylation protects the drug against inactivation by AAC(3) but 3-N-ethyl tobramycin does not inhibit strains containing this enzyme.

抄録全体を表示

Two new polyacetylene compounds (, , 12)-1-acetoxy-3-isovaleryloxytetradeca-, , 12-trien-, 10-diyn-14-ol (), and (, , 12)-1-acetoxy-3-(2-methylbutyryloxy)tetradeca-, , 12-trien-, 10-diyn-14-ol () have been isolated along with (, , 12)-1-acetoxy-3-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.

抄録全体を表示

By employing an undrained cyclic loading ring-shear apparatus, a series of tests to reproduce the dynamic behavior of the Nikawa landslide induced by the January 17, 1995 Hyogoken-Nambu earthquake, is conducted. The test sample is Osaka-group coarse sandy soil taken from the landslide. The initial stress condition acting on a soil element in the sliding surface is applied to the sample. Based on the seismic records monitored at the JR Takarazuka Station, the input seismic wave is synthesized to reproduce the seismic stress acting on the sliding surface. The test results show that the soil failed due to the dynamic loading of the earthquake. The most important results are the excess pore water pressure generation and the acceleration of shear displacement continuing after the main shock. Combined with the grain crushing at the shear zone and the volume reduction in the drained constant-speed ring-shear test, the mechanism of this landslide is interpreted as, shear displacement causing grain crushing in the shear zone and volume reduction, and then resulting in a localized liquefaction phenomenon, "sliding-surface liquefaction". This geotechnical simulation test provides a reasonable interpretation of this highly mobile landslide.

抄録全体を表示

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.

抄録全体を表示

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.

抄録全体を表示

Two new partially saturated tricyclic ring systems, , a, 7, , , 10, 10a, 11-octahydro-11-oxodibenz [, ] oxepins (3a and 3), 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 3a (trans), 3 (cis), a (trans) and (cis) are compared with those of 10a, 10, 11a and 11 on the basis of proton nuclear magnetic resonance data.

抄録全体を表示

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 7th-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 7th-order LPF was newly developed by replacing OTAs with resistors. As a result, the -3dB frequency bandwidth, group delay ripple, 3rd-order distortion, and 3rd-order input intercept point (IIP3) were 200MHz, 2.2%, ≤ -55dB with a 100MHz input, and +10.3dBm, 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.

抄録全体を表示

Some existing analytical methods which have been used in geotechnical engineering are modified to handle the shear strength reduction with time due to softening in fissured, over-consolidated clays and mudstones. These are limit equilibrium analysis of slope stability, calculation of earth pressure and calculation of stress and displacement around a tunnel. The softening effect is incorporated in these analyses using the failure criterion and the time-dependent strength parameters proposed previously by the authors. Examples are presented which emphasize the importance of appreciating the softening effect in analyses and further illustrate that the effect of shear strength reduction with time due to softening could easily be captured with existing analytical methods.

抄録全体を表示

Leakage of water due to internal erosion through a dam body or foundation is a major problem with fill-type dams. Recent case histories and research suggest that most cases of internal erosion are possibly triggered by hydraulic fracturing. However, the quantitative mechanism of hydraulic fracturing still remains to be solved. Therefore in-situ hydraulic fracture tests were carried out with a cheap, concise apparatus using boreholes dug in the soft clayey volcanic soil foundation of a low earth dam (Oyachi Dam) in Niigata Prefecture. Water was injected into the foundation through a perforated pipe by two methods : one was under a controlled injection pressure and the other was a controlled injection flow rate. In the former method, the relationship between flow rate and injection pressure was observed and it was found that a yield pressure or fracture pressure existed in all the tests. By repeating the injection test it was confirmed that once a crack is developed, it is very easily reopened by a water pressure a little higher than the earth pressure exerted on the crack. In the latter method, the relationship between injection pressure and time was observed and it was found that fracture pressure varied with flow rate. The boreholes were excavated to observe the development of fracture cracks and it was also found that the cracks had developed perpendicular to the borehole periphery, which means that fracture cracks were induced by tensile stress and denies the explanation that fractures are caused by shear failure.

抄録全体を表示

A comparative study of the static and dynamic response of a slope is carried out, using the large deformation theory of the updated Lagrangian formulation and the conventional infinitesimal theory. In the static analysis, a strength reduction method proposed by one of the authors is used to evaluate the safety factor of the slope. It is found that by the large deformation theory, the safety factor is larger than that calculated by the infinitesimal theory, and this difference becomes large along with the reduction of elastic modulus. In the dynamic analysis, it is observed that the large deformation theory gives smaller sliding displacement and larger response acceleration than the infinitesimal approach. It is concluded that in many cases the large deformation approach gives more adequate solutions.

抄録全体を表示