Callipeltin A () is a cyclodepsipeptide from water sponge collected at New Caledonia. This compound shows anti-HIV and cytotoxic activities against KB and P388 cells and contains three new amino acid residues. β-methoxytyrosine (β-MeOTyr) (), (2R,3R,S)--amino--guanidino-2,-3-dihydroxyheptanoic acid (AGDHE) (5), (3S,R)-3,-dimethyl-L-glutamine (diMeGln) (). In addition, two new truncated open-chain derivatives of Callipeltin A (), named Callipeltin D (2) and (3) were isolated. The unique structure and intriguing biological activities of this compound led us to explore total synthesis of Callipeltin A () and to elucidate stereochemistry of β-MeOTyr (). We started to synthesize Callipeltin (3) which contains β-MeOTyr (). In order to synthesize four stereoisomer of β-MeOTyr (), we attempted Evans anti or syn-Aldol reaction as a key step. Evans direct anti-aldol reaction with chiral benzyloxazolidinones () and p-hydroxy benzaldehyde (9) promoted by catalytic amounts of MgCl_2 in the presence of triethylamine and chlorotrimethylsilane. This proceder provide 3: diastereoselelctivity and 70% yield of isolated anti-aldol product (10). And Enolizalion of isocyanate oxazolidinone (13) with di-n-butylboryl trifrate and diisopropylethylamine followed by treatment with aldehyde afford syn-aldol product 14 affording % yield and :5 anti: sin diastereomeric ratio. On the other hand, we tried Sharpless Asymmetric dihydroxylation () and Aminohydroxylation (AA) to give all four stereoisomers of β-MeOTyr. Treatment of olefin (18) with -mix α provided diol (19) and the α position alcohol of 19 was converted to sulfone regioselectively followed by azidation and treatment of 20 with PPh_3 to afford aziridine (21). Addition of aziridine (21) and _3・Et_2O in methanol produced α-amino β-methoxy adduct (). AA reaction protocol with t-butylcarbamate was successfully applied to afford desired in single step. Now we construct Callipeltin to determine absolute stereochemistry of β-MeOTyr (). In addition, we report the synthesis of diMeGln () and (2R,3R,S)-3-hydroxy-2---trimethyl hepanoic acid ().

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

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The gamma-ray spectrum and the conversion-electron spectrum are measured in the decay of the ^116mIn activity. Directional correlations are also measured for 818–1293 and 1097–1293 keV cascades. The M-2 mixing ratio δ, and the -2 mixing ratio μ_k are obtained for 818. keV +→2₁⁺ transition to be δ=−+, and μ_k≤.×10−

4

respectively. The

E

2 branching ratio

B

(

E

2;

2₂

+→+): (2; +→2₁⁺): (2; +→0₁⁺) is determined to be .0158:.:5.86.

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Based on the recommendations of Berezantzev et al., a new semi-empirical equation for settlement ratio of pile foundations in sand has been derived. The settlement ratios obtained using this equation have been compared with the actual measured values. The comparison indicates that the new equation predicts higher than actual settlement values and is therefore conservative. The new equation is therefore modified in the light of empirical evidence and presented in a generalised form which can be used for square, rectangular, and irregular pile groups. The procedures recommended for the use of the equation in preliminary designs are explained.

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The purpose of this cohort study was to identify the predictors of lifestyle-related disorders, such as dyslipidemia, hyperuricemia, and liver dysfunction in Japanese young male workers. As candidates for the predictors, we chose obesity at entry and weight gain. The study subjects were 166 Japanese male workers aged 28 to 35 years at two printing plants in Tokyo who showed no blood abnormalities on chemistry items, i.

e

., total cholesterol (TC), high-density lipoprotein cholesterol (HDL-C), uric acid (UA), aspartate aminotransferase (AST), alanine aminotransferase (ALT), and gamma glutamyl transferase (GGT); the subjects completed a self-administered questionnaire survey in 1993, and underwent blood examinations in 2000. Covariates we included in the models were age, drinking habit, smoking habit and regular exercise. Linear regression models revealed that weight gain was consistently associated with the above blood chemistry items at endpoint, whereas obesity was not a better predictive variable than weight gain except for UA. Logistic regression models showed that the odds ratios (ORs) of each 5% weight gain were .47 [95% confidence interval (CI): .-2.28] for high TC, .27 (.-.84) for high UA, 2.61 (.32-5.18) for high ALT, and . (.14-3.11) for high GGT. The ORs of obesity were 3.05 (.98-9.50) for high TC, 3. (.40-10.) for high UA, . (.05-23.) for high ALT, and .78 (.43-.31) for GGT. In conclusion, for a period during which workers do not undergo blood tests, weight gain, in combination with obesity, may be used as a predictor of the later occurrence of blood abnormalities.

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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 : () 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 JMA), () Elevation of Dam Site (higher than 100 m), (5) 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 (3 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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Using the so-called pseudo-static method, a stability analysis was made for the mountain slide that took place at Mitake-iriya village at the time of the Izu-Ohshima-Kinkai earthquake of January 14, 1978. Undisturbed samples of volcanic clay were obtained in blocks from the exposed surface of the deposit identified to have been the sliding surface. The partially saturated clay samples were tested under consolidated undrained conditions using the triaxial test equipment. Dynamic axial stresses with irregular time histories were applied to the specimens in combination with statically sustained axial stresses to determine the soil strength under the conditions simulating in-situ states of stress during the earthquake. The results of the tests were expressed in terms of the Mohr-Coulomb type failure criterion which showed that, while the angle of internal friction remained almost unchanged, the cohesion component in irregular loading increased above values obtained in the static loading. Using the strength parameters thus determined, a pseudo-static analysis was made to check the stability of the soil masses that had actually slid during the 1978 earthquake. The maximum horizontal acceleration required to cause the slide was computed. The computed accelerations were shown to cover a range between 400 and 500 gals which is consistent with the range estimated by other investigators on the basis of overturning of tombstones in the vicinity of the slide area.

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The semen quality of dogs ( to years old) with benign prostatic hyperplasia (BPH) was examined at the hospital of our university, and of the BPH dogs were diagnosed as azoospermic. The mean peripheral plasma estradiol-17β () level (17.3 pg/ml) of the 18 BPH dogs with spermatogenic function was higher than that of 5 normal male dogs and their mean T level (. ng/ml) was lower. The mean level (27.3 pg/ml) of the BPH dogs with azoospermia was significantly higher than the value in the BPH dogs with spermatogenic function (P<.01), and the mean T level (. ng/ml) was significantly lower (P<.05). Five normal male dogs were given 10 intramuscular injections of estradiol benzoate () 5 μg/kg, at 3-day intervals to investigate the relationship between high plasma levels and the cause of the BPH and azoospermia. Their testes and prostates were measured and biopsied both before and 30 days after the start of injections. At 30 days after the start of the injections, the mean peripheral plasma T levels had decreased by half, and the mean testicular volume had decreased to % of original volume. The numbers of spermatocytes, spermatids, and spermatozoa in the seminiferous tubules of all of the dogs were significantly lower (P<.05, .01). In addition, the mean prostatic volume increased to 130%, the mean height of the glandular epithelium decreased, and the glandular lumen became increased in diameter. These findings indicate that both BPH and serious spermatogenic dysfunction may be simultaneously induced by protracted high plasma levels in dogs.

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Six full-length cDNAs encoding pig cytochrome P450 (CYP) enzymes, CYPA, CYP2A19, CYP2, CYP2C33v, CYP2C49, and CYP2, were isolated and sequenced. The cDNA sequences of pig CYPA, CYP2A19, CYP2, CYP2C49, and CYP2 showed high similarity to human (85.%), CYP2A13 (.%), (81.%), CYP2C18 (85.3%), and (82.5%), respectively, and pig cDNA showed high similarity to rat CYP2C23 (79.2%). Reverse transcription-polymerase chain reaction (RT-PCR) assays revealed hepatic gene expression of all these pig CYP enzymes: the order of expression was and > CYP2C49 > and CYP2A19 > . In the kidney, the gene was expressed at the same level as in the liver, but the , CYP2A19, and genes were expressed at lower levels than in the liver. Little renal gene expression of CYP2C49 and CYP2 was observed. We revealed for the first time the full-length cDNA sequences encoding pig CYPA and five CYP enzymes belonging to the CYP2 gene family, thus making it possible to examine the gene expression levels of these CYP enzymes in pig tissues by RT-PCR.

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We screened the differentiation-inducing activities of 39 mushroom extracts from Akita prefecture, Japan, on the mouse osteoblastic cell line, MC3T3-. Sixteen phosphate buffered saline (PBS), boiled PBS, 14 ethanol and 12 methanol extracts induced alkaline phosphatase (ALP) activities, an indicator of MC3T3- 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-,-diene-3β,5α,-triol (). induced ALP activities of MC3T3- cells and promoted cell proliferation. To investigate the relationships between the chemical structure and differentiation-inducing activity of the compound, ALP-inducing activities of MC3T3- cells by , ergosterol (2), ergocalciferol (3), cholesta-3β,5α,-triol (), -dehydrocholesterol (5) and cholecalciferol () were tested. The enzyme activities of MC3T3- cells were increased 3.-fold by 10 μM and 2.-fold by 10 μM . However, 2, 3, 5 and did not induce MC3T3- cell ALP activity at .—10 μM. These results suggested that the OH groups at C-5 and/or C- of and played an important role in their differentiation-inducing activities on MC3T3- cells. Furthermore, suppressed induction of MC3T3- cell apoptosis by serum starvation.

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乳牛の分娩性起立不能症予防のための基礎的資料を得る目的で、分娩後2日以内に起立不能に陥ったホルスタイン種乳牛例の血漿25(OH)D₃濃度を調査した。初診日の血漿25(OH)D₃濃度は、15.～174.9(58.3±40.,M±SD)ng/mlと個体間の差が大きく、また、分娩前におけるV-剤の経口投与の有無により差異が認められた。すなわちV-剤投与牛(n=10)では.±40.ng/mlであり、非投与牛(n=12)の30.±.ng/mlに比べ、有意(P＜.01)な高値を示した。初診後の経過にともない25(OH)D₃濃度は、ほとんど変化がみられなかった。

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The characteristic mechanical activities of the smooth muscles found in all organs of the body are highly variable and depend mainly on the spatial arrangement of the muscle cells and the stroma: mass, orientation, relationships, links, constraints, which are deployed in various configurations. These structural features are examined here for their mechanical relevance, in light and electron microscopic views of several muscles of viscera and blood vessels, in a selection of mammalian species. Smooth muscles are incompressible and therefore maintain constant volume. They do not have available space and any movement of a part requires displacement of another part. Most of them have no terminations or points of attachment, and in hollow organs such as intestines, blood vessels and uro-genital tract they usually form structures closed onto themselves, such as rings or bag-like containers In these situations, changes in the size of the lumen is achieved very efficiently by a concentric inward enlargement that accompanies muscle contraction. The longitudinal arrangement of collagen blocks an elongation of small blood vessels upon contraction, further enhancing the efficiency of lumen reduction. In other muscles, links between layers and special arrangements of the stroma allow both shortening and elongation of a tubular organ to occur. The mechanics of smooth muscles has many characteristic features (some unique, some shared with those of hydrostats, some at variance with other muscles) and histological data are a contribution to our understanding of these properties.

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All the cells of rat detrusor muscle fall into one of five ultrastructural types: muscle cells, fibroblasts, axons and glia, and vascular cells (endothelial cells and pericytes). The tissue is ~79% cellular and 21% non-cellular. Muscle cells occupy 72%, nerves ~

% (/3 axons, 2/3 glia), and fibroblast >3% of space. Muscle cells (up to µm across and ~600 µm long, packed to almost 100,000 per mm²) have surface-to-volume ratio of 2. µm²/µm³ ~93% of cell volume is contractile apparatus, 3.% mitochondria and 2.5% nucleus. Cell profiles are irregular but sectional area decreases regularly towards either end of the cell. Muscle cells are gathered into bundles (the mechanical units of detrusor), variable in length and size, but of constant width. The musculature is highly compact (without fascia or capsule) with smooth outer surfaces and extensive association and adhesion between its cells. Among many types of intercellular contact and junction, digitations are very common, each muscle cell issuing minute finger-like processes that abut on adjacent cells. Sealed apposition are wide areas of specialized contact, possibly forming a chamber between two muscle cells, distinct from the extracellular space at large (stromal space). The innervation is very dense, virtually all intramuscular axons being varicose (including afferent ones). There are identifiable neuro-muscular junctions on each muscle cell, often several junctions on a single cell. There are also unattached terminals. Fibroblasts (involved in the production of collagen), ~% of the total number of cells, do not make specialized contacts.

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This paper provides a comprehensive survey of the numerical methods related to geotechnical problems, most of which were reported in papers appearing in Soils and Foundations. The reason why most of the reviewed papers are concentrated in Soils and Foundations is that if we were to include papers appearing in other journals in the field of geotechnical engineering, closely related to numerical methods, .g., Computers and Geotechnics, Int. J. Numer. Anal. Meth. Geomech., etc., we would have to deal with almost all the papers in those journals. Firstly, we present a description of the current status of the numerical methods, and then give a brief review of the literature covering several topics in geotechnical applications. The scope of the review is limited, and thus, the authors do not profess to cover the entire range of literature.

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The gamma-ray spectrum and the conversion-electron spectrum are measured in the decay of the Tb¹⁵² activity. The L-subshell electron lines of the 586. keV +→2₁⁺ transition are separated by the ion-free beta-ray spectrometer. The M-2 mixing ratio, δ², and the dimensionless ratio X of -2 mixing of the 586. keV transition are obtained to be δ²≤.16 and .034≤X≤.038, respectively. The 2 branching ratio (2; +→+): (2; +→2₁⁺): (2; +→0₁⁺) is determined to be .023 : . : 5..

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Two new partially saturated tricyclic ring systems, , a, , , 9, 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.

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Natural sedimentary clays exhibit ageing effects on their behaviour when subjected to both consolidation and shearing. Attempts to characterising the in-situ 'structure'of soft marine clays have been made in case studies performed in Ariake (Japan) and in Bangkok (Thailand), each showing a typical profile of aged clay-structure with depth reflecting its site-specific geological consolidation history. In each site, profiles of Atterberg limits, natural water content, overconsolidation ratio (OCR), quasi-elastic shear modulus G_max and the undrained shear strength c_u with depth were attained from various laboratory tests, together with the a comparable profile of quasi-elastic shear modulus from insitu seismic survey G_f. Quantitative assessment of the aged clay-structure was made by using two different measures, metastability index MI (G) and the soil constant reflecting structure S (Jamiolkowski et al., 1994). The profiles of MI (G) and the S-value with depth were both determined based on the corresponding G_max behaviour of the reconstituted sample. "Disturbance"of laboratory samples retrieved by using two different samplers (i.., Laval and Japanese thin-walled samplers) with two different sampling techniques (i.., pre-boring and displacement methods) was discussed. A new approach to estimate c_u"in the ground", termed by the authors the MILK (Metastability Index coupled with Laboratory K_o test) method, is proposed. A trial of the MILK-method is demonstrated in soft Bangkok clay, the texture of which is similar to "soft cheese".

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