Two new partially saturated tricyclic ring systems, , a, , , , 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 -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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11-Amino-, a, , , , 10, 10a, 11-octahydrodibebenzo[, ]thiepines (a-d) and -oxepines (a-d) were synthesized by the Leuckart reaction of , a, , , , 10, 10a, 11-octahydro-11-oxodibenzo[, ]thiepines (1a, )and -oxepines (a, ) followed by hydrolysis of the reaction products a-d and a-d, respectively. The four diastereomers, cis(a-H, 10a-H)-cis(10a-H, 11-H) a and a, cis(a-H, 10a-H)-trans(10a-H, 11-H) and , trans(a-H, 10a-H)-trans(10a-H, 11a-H) and , and trans(a-H, 10a-H)-cis(10a-H, 11-H) d 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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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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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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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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New-type inducers of differentiation of human promyelocytic leukemia cells HL-60, i.

e

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

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Mycobacteriocin produced by human type tubercle bacilli could be demonstrated easily on eggmedium containing 0.05% tween by means of stab culture or streak plate methods, and elevenmycobacteriocin-types have been recognized on the basis of the inhibition pattern by using indicator strains of rapidly growing mycobacteria.
At present, types 1 (.%), (13%), (38.%), (%) and 11 (14.%) showed a stablemycobacteriocin pattern, but types (.%) and (.%) were apt to show type replacement totypes and , respectively, and strains belonging to types , and were few, less than 1.%to the total. In order to perform a reproducible mycobacteriocin typing, our previous typingscheme was revised to be consisted of five groups (A-). Among 438 strains, mycobacteriocingroup containing types and was 46.1% of strains tested, group containing types , and was .%, group containing type 11 was 15.1%, group A containing types 1 and was.%, group D containing types and 10 was .1%, and untypable strains were no more than .% among all tested strains.
Human type tubercle bacilli classified as type , which consisted of more than 45% of strainstested, could be divided into three sub-types from sensitivity to M. gordonae 1324 and M. terrae 1450.
Mycobacteriocin producing strains belonging to type D: showed an extremly wide antibacterialactivity to strains of more than % of rapidly growing mycobacteria (42 strains), to about 40% of slow growing mycobacteria (29 strains), and even to 10 strains of Staphylococcus aureus.

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From the fronds of Polystichum tripteron (KUNZE) P_R. a new norcarotenoid glycoside was isolated and shown to be (R, , R)--hydroxy-megastigma-, -dien--one--O-β-D-glucoside. The fronds of Dennstaedtia wilfordii (MOORE) CHRIST. contain the same glucoside.

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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

% 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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Six natural products, named -, -, -, -, -10, and -11, were isolated from ether and methylene chloride extracts of freeze-dried mycelium of Aspergillus amstelodami IFO-6667. - and -11 were found to be identical with neoechinulin () and echinulin (1), respectively, from spectroscopic and melting point data. Alkaline hydrolysis of -, -, and -10 gave indole--carbaldehydes (a, and ), respectively. Analysis of the spectroscopic data revealed the presence of a methylenediketopiperazine moiety in -, -, and -10. Based on these informations, the structures a, , and were assigned to -, -, and -10, respectively. These three alkaloids were synthesized by condensation of indole--carbaldehydes (a, , and ) with methylenediketopiperazine (). The stereochemistry of -, -, and -10 were determined as shown in the structures. A possible rationalization to explain the isopentenylation in the echinulin-neoechinulin alkaloid biosyntheses was presented.

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(,)-,-エポキシ-,,11,11-テトラメチルシクロウンデカ-,-ジエン()をフムレン1((,,)-,,11,11-テトラメチルシクロウンデカ-,,-トリエン)より合成する既知の合成法は実際に牧率が低く合成的に問題がある.さらに,の合成はその反応性や物性の研究のために簡単に高牧率で行われることが望まれる.今回,の新たな合成法と簡便な精製法を見いだし,を高牧率で1から合成することができたので報告する.1のジエポキシ化,続く再結晶により得られたジエポキシド()は二価のチタンにより還元されて,1(273%)と(25%)と少量のを含むを主生成物(42.%)として与えた.1とは原料として再利用できる.の精製は1と同様硝酸銀()錯体の結晶で行い,純粋なは1から通算牧率32.0%で得られた.の既知方法による合成は段階の反応と数回のカラム分離及び10%含浸シリカゲルカラム分離を必要とし牧率が極端に低い.今回,新しいの合成法は段階の反応で1回のカラム分離と再結晶により高い通算牧率を示す.

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わが国における主要中晩生および香酸カンキツ染色体のクロモマイシン (CMA) 染色を行った. 染色体はCMA(+) バンドの有無および位置から種類に区分できた. すなわち, CMA(+) をA: 両端および動原体近傍に有する, : 一方の端部と動原体近傍に有する, : 両端に有する, D: 一方の端部に有する, : CMA(+) がない, である. 各種はこれらのうち, 種類の染色体を有し, 独自のCMAバンドパターンを示した. ハッサクでは1A+1+D+, ヒュウガナツではA++D+, ‘川野なつだいだい’では1A++D+, ‘宮内伊予柑’では1A+1+1+D+, タンカン‘垂水1号’では1A+1+1+D+, カボスでは++D+, スダチでは1++D+およびユズ‘山根’では+1+11D+であった. 以上の結果, 本研究においても近縁の種間では似通ったCMAバンドパターンが観察された.

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In order to elucidate the typhoid and paratyphoid phage type distributions in Japan, during the period of 1956-1965, a total of 1, 808 typhoid cases from 1, 002 foci and 114 paratyphoid cases from 87 foci were submitted for phage typing of their infected organisms, and the following results were obtained.
1. The typhoid strains tested fell into at least 30 Vi-phage types. The sequence of frequency as counted by foci was as follows : types D (20%), M1 (13%), 1 (12%), A (.%), N+D1 (.%), D1 (.%), D (.%), (.%), 39 (1.%), H (1.1%), J1 and 46 (0.%) ; , L1 and 41 (0.50%) ; 1, , , D, D10, , , , L, T, 28, 29, 36, 38 and 47 (less than 0.50%) . Distri-bution of typhoid Vi-phage types in Japan was characteristic of preponderance of types D and M1.
. Of the foci studied, .% could not be assigned that their causative organisms belonged to any hitherto recognized Vi-phage type.
. The prevalent typhoid Vi-phage types, D, M1, 1, A and N+D1 were evenly encountered throughout the last ten years and distributed among almost throughout the country.
. Some of the rearly recognized typhoid Vi-phage types were indigenous to the relatively limited areas.
. Three new Vi-phage types, 39, 41 and 47 were identified.
. Paratyphoid phage types encountered were as follows: Types a (49%), 1 (33%), (.%), Dundee (.%), aI (1.1%) and Beccles (1.1%) . The remainders could not he assigned to any known type.

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In this study, we attempted to isolate Escherichia coli from healthy adults in Ho Chi Minh City, Vietnam, and characterized its antimicrobial resistance profile, extended-spectrum β-lactamase (ESBL) genotype, phylogenetic grouping and virulence gene profile. A total of 103

. coli isolates were obtained, and most of them were antimicrobial resistant such to streptomycin (.%), tetracycline (67.0%), ampicillin (65.0%), sulfamethoxsazole/trimethoprim (48.%), nalidixic acid (43.%), chloramphenicol (34.0%), cefotaxime (15.%), ciprofloxacin (15.%), kanamycin (12.%), ceftazidime (10.%), fosfomycin (.%) and gentamicin (.%). However, all these

E

. coli strains were susceptible to imipenem. Surprisingly, of 103 strains, 74 (71.%) and 43 (41.%) strains showed resistance to more than and classes of antimicrobials, respectively. Furthermore, 10

E

. coli strains were ESBL-producers and positive for bla_CTX-M genes ( for blaCTX-M-

9

and

3

for bla_CTX-M-1), while five were additionally positive for bla_TEM genes. S1-nuclease pulsed-field gel electrophoresis analysis revealed that

7

and

3

strains of

E

. coli carry bla_CTX-M genes on their large plasmid and chromosome, respectively. Phylogenetic analysis exhibited that majority of the

E

. coli strains was grouped into A (44.

7

%), followed by

B

1 (23.

3

%),

B

2

(18.

4

%) and D (13.

6

%). Virulence genes associated with diarrheagenic

E

. coli, such as astA, EAF, eaeA, elt and eagg were also detected in ESBL-producing

E

. coli as well as antimicrobial resistant strains. These data suggest that commensal

E

. coli of healthy human could be a reservoir for antimicrobial resistance determinants and some of them might be harmful to human.

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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, '-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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