(

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, '-N and -N positions were examined. The MICs of these derivatives against tobramycin sensitive strains indicated that '-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 '-N or '-N ethylation protects the drug against inactivation by AAC(') or AAC('), respectively, and '-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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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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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 -dB frequency bandwidth, group delay ripple, rd-order distortion, and rd-order input intercept point (IIP) were 200MHz, .%, ≤ -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.V supply. Wide spurious-free dynamic range (SFDR) characteristics were confirmed up to high frequencies.

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Two new polyacetylene compounds (4, , 12)-1-acetoxy--isovaleryloxytetradeca-4, , 12-trien-, 10-diyn-14-ol (B), and (4, , 12)-1-acetoxy--(-methylbutyryloxy)tetradeca-4, , 12-trien-, 10-diyn-14-ol () have been isolated along with (4, , 12)-1-acetoxy--senecioyloxytetradeca-4, , 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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A biosynthetic pathway for (

)-methyl cinnamate formation was evaluated in Tricholoma matsutake by tracer experiments using

13C

- and

2H

-labeled precursors. One hundred percent selective

13C

incorporation was observed when L-[1,

2

,

3

,4,5,

6

,7,

8

,

9

-

13C₉

, ^15/N]phenylalanine was converted to (

E

)-[1,

2

,

3

,4,5,

6

,7,

8

,

9

-

13C₉

]cinnamate and (

E

)-[1,

2

,

3

,4,5,

6

,7,

8

,

9

-

13C₉

]methyl cinnamate. Similarly, 100% selective

13C

incorporation was observed when (

E

)-[1,

2

,

3

,4,5,

6

,7,

8

,

9

-

13C₉

]cinnamate was converted to (

E

)-[1,

2

,

3

,4,5,

6

,7,

8

,

9

-

13C₉

]methyl cinnamate. In contrast, the

2H

incorporation selectivities were

82

.1% and 81.4% when L-[

2

,

3

,4,5,

6

,7,7,

8

-

2H₈

]phenylalanine was converted to (

E

)-[

2

,

3

,4,5,

6

,7,

8

-

2H₇

]cinnamate and (

E

)-[

2

,

3

,4,5,

6

,7,

8

-

2H₇

]methyl cinnamate, respectively. Thus, T. matsutake synthesizes (

E

)-methyl cinnamate from L-phenylalanine via (

E

)-cinnamate. (

E

)-cinnamate was likely formed through two pathways: one was major and the other was a minor.

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The correction factor (η_ie) for the ultimate bearing capacity of a footing placed adjacent to a slope, taking into account the combined effect of horizontal and vertical seismic loads, represented by horizontal and vertical seismic coefficients, k_h and k_v, respectively, was derived using a modified Janbu's slice method. The influence of slope angles ‘α’ on the values of ‘η_ie’ are studied here. It was found that the values of η_ie can be expressed as an exponential function of ‘k_h/(1-k_v)’ and ‘α’, with a measurable interdependency between ‘α’ and ‘η_ie’. The influence of ‘α’ on the value of ‘η_ie’ increases as the input value of ‘k_h/(1-k_v)’ increases. Equations derived based on the analytical results are proposed to account for this effect. Based on the analyses of 11 near-fault seismographers obtained in the 1999 Chi-Chi earthquake in Taiwan, a ratio between the vertical and the horizontal seismic coefficients, λ, of between ±0.25 is suggested for including the combined effect of vertical and horizontal seismic forces in evaluating the seismic bearing capacity of footings located in near-fault areas.

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At present, analytical or empirical formula for seismic bearing capacity of footings adjacent to slopes is not available. This study uses a pseudo-static-based approach in conjunction with rigorous Janbu's slice method to derive analytical values of seismic bearing capacity factors (N_γ) and correction factors for the effects of inertia of soil mass and load inclinations for a rigid footing adjacent to cohesionless slopes. It is shown that both the bearing capacity factors (N_γ) and the correction factors for the seismic bearing capacity of footings placed on level ground derived herein are comparable with those reported in the literature. Empirical equations regarding the effects of slope angles and load inclinations, expressed using generalized forms of those proposed in the literature, are also derived. It is also found that the empirical equations derived in the present study provide values of correction factors in good agreements with the analytical ones, indicating the validity of using these empirical equations for assessing the bearing capacity of rigid footings situated on the slope subjected to pseudo-static seismic loading.

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The Beckmann rearrangement of aliphatic ketone oximes, R(CHs)=NOH (R=Et (1); n-Pr (); iso-Pr (); iso-Bu (4)), with polyphosphoric acid (PPA), polyphosphate ester (PPE), and ester of phosphoric acid ( P-5 R) was carried out and migratory ratios ((a)/(b) in eq. (1)) were determined, The results are shown in Fig.1, , and , respectively.
In Fig.1 and , the migratory ratios decrease with reaction time and nearly approach to the ratios of anti-alkyl form/syn-alkylform in benzene(A1) or DMSO(A)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 A. 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 P-5 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 P-5 R.

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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 DESRA 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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This paper is concerned with dynamics of the standard penetration test (SPT). The usefulness of mounting strain gages at two different stations along a driven rod is described, together with a workable procedure of analysis. The analysis procedure makes use of the traveling time between the two gage points and enables one to identify the particle velocity, the displacement and the stress at any station of the rod, as well as the energy actually transmitted from a hammer to the rod. Particular attention is called for the consequence of inevitable, small errors in strain data upon such identifications. A pertinent procedure of error-correction is proposed and its validity is substantiated against the performance of well instrumented SPTs performed by the authors.

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We screened the differentiation-inducing activities of 39 mushroom extracts from Akita prefecture, Japan, on the mouse osteoblastic cell line, MCT-1. Sixteen phosphate buffered saline (PBS), boiled PBS, 14 ethanol and 12 methanol extracts induced alkaline phosphatase (ALP) activities, an indicator of MCT-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-7,-diene-,5α,-triol (1). 1 induced ALP activities of MCT-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 MCT-1 cells by 1, ergosterol (), ergocalciferol (), cholesta-,5α,-triol (4), 7-dehydrocholesterol (5) and cholecalciferol () were tested. The enzyme activities of MCT-1 cells were increased .0-fold by 10 μM 1 and .4-fold by 10 μM 4. However, , , 5 and did not induce MCT-1 cell ALP activity at 0.1—10 μM. These results suggested that the OH groups at -5 and/or - of 1 and 4 played an important role in their differentiation-inducing activities on MCT-1 cells. Furthermore, 1 suppressed induction of MCT-1 cell apoptosis by serum starvation.

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