We screened the differentiation-inducing activities of 39 mushroom extracts from Akita prefecture, Japan, on the mouse osteoblastic cell line, MC3T3-1. Sixteen phosphate buffered saline (PBS), 8 boiled PBS, 14 ethanol and 12 methanol extracts induced alkaline phosphatase (ALP) activities, an indicator of MC3T3-1 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-3β,,-triol (1). 1 induced ALP activities of MC3T3-1 cells and promoted cell proliferation. To investigate the relationships between the chemical structure and differentiation-inducing activity of the compound, ALP-inducing activities of MC3T3-1 cells by 1, ergosterol (2), ergocalciferol (3), cholesta-3β,,-triol (4), 7-dehydrocholesterol () and cholecalciferol () were tested. The enzyme activities of MC3T3-1 cells were increased 3.0-fold by 10 μM 1 and 2.4-fold by 10 μM 4. However, 2, 3, and did not induce MC3T3-1 cell ALP activity at 0.1—10 μM. These results suggested that the OH groups at C- and/or C- of 1 and 4 played an important role in their differentiation-inducing activities on MC3T3-1 cells. Furthermore, 1 suppressed induction of MC3T3-1 cell apoptosis by serum starvation.

抄録全体を表示

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 M1-2 mixing ratio δ, and the 0-2 mixing ratio μ_k are obtained for 818.7 keV +→2₁⁺ transition to be δ=1.52−

0.22

+0.26, and μ_k≤

6

.1×10⁻⁴ respectively. The

E

2 branching ratio B(

E

2;

2₂

+→0_g⁺): B(

E

2;

2₂

+→2₁⁺): B(

E

2;

2₂

+→0₁⁺) is determined to be 0.0158:1.0:

5

.

86

.

抄録全体を表示

The effects of the pressure of ambient gas and sample temperature on photo-acoustic displacement (PAD) were studied quantitatively using an extremely sensitive laser interferometric probe. For silicon, the PAD signal measured at atmospheric pressure increased by about 18% as compared to that obtained in a vacuum, and varied by less than 0.7% for a change in pressure of % around 1 atm. This effect was attributed to the decrease in refractive index of the gas adjacent to the sample. Temperature rise caused PAD to increase proportionally, and for GaAs, PAD varied 0.4% per degree. The variation of PAD with temperature was accurately explained by the temperature dependence of thermal expansion coefficient and thermal conductivity of the sample.

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

Callipeltin A (1) 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) (4), (2R,3R,4S)-4-amino-7-guanidino-2,-3-dihydroxyheptanoic acid (AGDHE) (), (3S,4R)-3,4-dimethyl-L-glutamine (diMeGln) (). In addition, two new truncated open-chain derivatives of Callipeltin A (1), 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 (1) and to elucidate stereochemistry of β-MeOTyr (4). We started to synthesize Callipeltin (3) which contains β-MeOTyr (4). In order to synthesize four stereoisomer of β-MeOTyr (4), we attempted Evans anti or syn-Aldol reaction as a key step. Evans direct anti-aldol reaction with chiral benzyloxazolidinones (8) and p-hydroxy benzaldehyde (9) promoted by catalytic amounts of MgCl_2 in the presence of triethylamine and chlorotrimethylsilane. This proceder provide 3:1 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 8 afford syn-aldol product 14 affording % yield and 1: 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 BF_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 (4). In addition, we report the synthesis of diMeGln () and (2R,3R,4S)-3-hydroxy-2-4--trimethyl hepanoic acid (7).

抄録全体を表示

The design implication of stress-confinement effect of nonwoven geotextile is addressed. The unconfined and confined strengths of a selected needle-punched nonwoven geotextile are used to conduct a comparative design of a granular soil retaining wall based on a limit equilibrium approach. A higher wall may be allowed when considering the confined strength as compared to the unconfined strength. For a selected wall height, confined strength allows for fewer geotextile layers when compared to that designed using unconfined strength. It is recommended that stress-confinement test procedure should be standardized so that confinement effect of some nonwoven geotextiles may be incorporated into an individual wall design procedure.

抄録全体を表示

背景と目的：ステロイド性骨粗鬆症は，積極的な治療介入が必要とされる．その第一選択薬はビスホスホネート製剤（以下ビス）であるが，近年，デノスマブ（以下デノス）も注目を浴びている．ステロイド性骨粗鬆症の骨密度に対する両者の効果を比較検討した．

方法：ステロイド性骨粗鬆症の管理と治療ガイドライン：2014年改訂版の薬物療法開始の基準を満たした患者を対象とした．無治療群（N群）と，治療介入群として当初よりビスで治療したBB群，ビス後デノスに変更したBD群，デノスで治療したDD群，デノス後ビスに変更したDB群を抽出し，ステロイド投与を開始した時，ステロイド性骨粗鬆症に対する治療を開始した時または薬剤変更から

カ月後の腰椎，大腿骨頚部と大転子部の骨密度を測定し，それらの変化を統計学的に比較検討した．

結果：149例が抽出され，その内訳は，N群48例，BB群24例，BD群

例，DD群21例，DB群34例であった．治療開始時または薬剤変更からカ月後にBD群を除くすべての治療介入群で腰椎の骨密度が上昇した．大腿骨の骨密度は，BD群において薬剤変更後に上昇に転じた．

考察：デノスにはビスと同様の骨密度上昇効果があると考えられた．

結論：デノスは，ステロイド性骨粗鬆症治療の第一選択薬となり得る．

抄録全体を表示

In the first part of the present work the interaction of glycophorin with dimyristoylphosphatidylcholine (DMPC) is studied by freeze fracture electron microscopy, densitometry, calorimetry, and 90° static light scattering. An exothermic lipid/protein interaction energy of W_P=190 kJ•mol^-1 was found by application of the well known Van Laar relation for the displacement of the freezing point and the Gibbs-Duhem relationship. Secondly, the effects of Ca²⁺ on the lipid/protein interaction were studied. Following Ca²⁺ addition a remarkable decoupling of the interaction of the glycophorin head group with the bilayer surface was revealed by densitometry and gold-labeling electron microscopy. It is estimated that about 80% of lipid once disturbed by the adsorption of glycophorin head groups is decoupled after addition of Ca²⁺. Thirdly, the selective interaction of glycophorin with binary lipid mixtures was studied, including the mixtures of DMPC with dimyristoylphosphatidylserine (DMPS) and dilauroylphosphatidylcholine (DLPC), and the mixture of dipalmitoylphosphatidylcholine (DPPC) with DLPC.

抄録全体を表示

Amyloid β (Aβ) plays a key role in the pathology of Alzheimer’s disease (

) and is toxic owing to its ability to aggregate into oligomers and fibrils. Aβ has high aggregative ability and potent toxicity due to the “toxic turn” at positions and 23. Furthermore, APP knock-in mice producing P-Aβ with the toxic turn exhibited -related phenotypes such as cognitive impairment, Aβ plaque accumulation, and tau hyperphosphorylation. In these mice, it is suggested that the activation of neuroinflammation and dysregulation of hypoxia-inducible factor (HIF) expression in the hippocampus contribute to the pathogenesis of -related phenotype. However, it remains unclear which cells are responsible for the dysregulation of HIF expression and the neuroinflammation which was induced by P-Aβ with the toxic turn. Here, we investigated the effects of chronic treatment with P-Aβ42 and lipopolysaccharides (LPS) on the inflammatory response in BV-2 microglia. Chronic treatment with P-Aβ42 and LPS increased nitric oxide production and the expression of interleukin- (IL-), whereas it reduced the expression of HIF-1α and HIF-3α in BV-2 microglia. The reduction of HIF-1α caused by P-Aβ42 and LPS was milder than that caused by LPS. Furthermore, chronic treatment with P-Aβ42 and LPS increased the nuclear translocation of nuclear factor-kappaB (NF-κB). P-Aβ42 could enhance the inflammatory response of microglia with abnormal HIF signaling and contribute to the progression of pathology.

抄録全体を表示

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 (3) 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.

抄録全体を表示