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-,-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 (), -dehydrocholesterol () and cholecalciferol () were tested. The enzyme activities of MC3T3-1 cells were increased 3.0-fold by 10 μM 1 and 2.-fold by 10 μM . 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 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.

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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．

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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 M1-2 mixing ratio δ, and the 0-2 mixing ratio μ_k are obtained for 818. 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.

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A monoclonal antibody, 9 established from mice injected with dolphin peripheral blood lymphocytes (PBLs) was characterized. In addition to its reactivity against .% of dolphin PBLs, 9 reacted with 33.1% of bovine PBLs of which % were CD ⁺, 11.1% were -. 9 recognized a 34 kD protein on the surface of dolphin and bovine PBLs. Analysis of the protein's N-terminal amino acid sequence indicated that 9 recognizes bovine major histocompatibility complex (MHC) class II antigens. These results suggested that 9 recognized MHC class II antigens on bovine PBLs. As we have already produced an anti-dolphin MHC class I monoclonal antibody, analysis of immune system using these monoclonal antibodies will advance our understanding of the evolution of the mammalian immune system.

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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 % 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.

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N-n-ヘキシル-マレイミド (I), N-シクロヘキシル-マレイミド (II), N-ベンジル-マレイミド (III) の単独重合, 共重合をアゾビスイソブチロニトリル (IV) を開始剤としてテトラヒドロフラン中, 60℃で行った. 単独重合の初速度 (R_p) はR_p=k [I]

2.5

[IV]

0.80

, R_p=>k [II] ^2.8 [IV]

0.80

, R_p=>k [III]

2.7

[IV] ^0.54となった. kは速度定数である. 全重合の活性化エネルギー (

E

), 頻度係数 (A) は

E

=

22

.8kcal/mol (I),

22

.2kcal/mol (II), 24.1kcal/mol (III), A=9.

5

×10¹¹ (I),

6

.

4

×10¹¹ (II),

6

.

6

×10¹² (III) となった. またN-置換マレイミドとメタクリル酸メチル (V) との共重合におけるモノマー反応性比r₁, r₂およびQ,

e

値を次のように決定した. I (M₁) -V (M₂) 系でr₁=0.17, r₂=2.02, Q₁=0.56,

e₁

=1.43, II (M₁) -V (M₂) 系でr₁=0.13, r₂=2.29, Q₁=0.50,

e₁

=1.50, III (M₁) -V (M₂) 系でr₁=0.14, r₂=1.54, Q₁=0.79,

e₁

=1.63となった.

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Chemical properties of ergosta-, , 8(14), -tetraen-3-one (1) were investigated. Though 1 is rather stable to acids or bases, it reacts easily with two moleculres of oxygen on irradiation with UV light to give , 9α-epidioxy-14α-hydroperoxyergosta-, , -trien-3-one (2), which is transformed successively to , ;8α, 9α-diepoxy-14α-hydroperoxyergosta-, -dien-3-one (3) and 14α-hydroperoxy-9α-hydroxyergosta-, , -triene-3, -dione () under these reaction conditions.

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Eight new sterols, , 8α-epidioxy-(, 24R)-23-methylergosta-, -dien-3β-ol (1), 3β, , 9α-trihydroxy-(, 24R)-23-methylergosta-, -dien--one (2), 3β, , 9α-trihydroxy-(24S)-ergost--en--one (3), 3β, , 9α, 14α-tetrahydroxy-(, 24R)-ergosta-, -dien--one (), (, 24R)-ergosta-, -diene-3β, , , 9α-tetrol (), , 9α-epidioxy-3β-hydroxy-(, 24R)-ergosta-, -dien--one (), , 9α-epidioxy-3β-hydroxy-(24S)-ergost--en--one () and , -epoxy-(, 24R)-ergosta-8, -diene-3β, , 14α-triol (8), have been isolated from five edible mushrooms, Lentinus edodes, Flammulina velutipes, Hypsizigus marmoreus, Pleurotus ostreatus and Pholiota nameko together with fifteen known ones (9-23), of which two (16 and 17) are reported for the first time from a fungal source. The structures of these new compounds were elucidated on the basis of their spectral data.

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Six new sterols, , ;8α, 9α-diepoxy-(, 24R)-ergost--ene-3β, -diol (1), , ;8α, 9α-diepoxy-(, 24R)-ergost--ene-3β, -diol (2), , -epoxy-(, 24R)-ergosta-8, -diene-3β, -diol (3), (, 24R)-23-methylergosta-, -diene-3β, , -triol (), (, 24R)-23-methulergosta-, -diene-3β, , , 9α-tetrol () and (24S)-ergost--ene-3β, , , 9α-tetrol (), have been isolated from seven mushrooms, Amanita pantherina, Amantia virgineoides, Lactarius piperatus, Lyophyllum shimeji, Tricholoma portentosum, Hypsizigus marmoreus and Lentinula edodes together with eighteen known ones (-24). The structures of these new compounds were elucidated on the basis of their spectral data.

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From the black coral Antipathies dichotoma, a sphingolipid (2S*,3S*,,)-2N-[tetradecanoyl]-(),8()-icosadiene-1,3-diol (1) and a steroid ()-methylcholesta-,-diene-1α,3β,-triol (2) were isolated. Other known compounds, 3β,-dihydroxy-cholest--ene (3), (,24S),,8α-epidioxy-24-methylcholesta-,-dien-3β-ol () and (,24S),,8α-epidioxy-24-methylcholesta-,9(11),-trien-3β-ol (). The structures were established on the basis of NMR spectroscopic analysis and comparison with literature. The antibacterial activity of five compounds was evaluated.

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Four new sterols, , -epoxy-(, 24R)-ergosta-8(14), -diene-3β, -diol (1), (, 24R)-ergosta-8, -diene-3β, , , -tetrol (2), (, 24R)-ergosta-, 9(11), -triene-3β, , -triol (3) and 3β, , -trihydroxy-(, 24R)-ergost--en--one (), have been isolated from the fruit bodies of Grifola frondosa (FR.) S. F. GRAY (Polyporaceae)together with fourteen known ones (-18), of which two ( and ) are reported for the first time from a natural source. The structures of these compounds were elucidated on the basis of spectral data.

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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 M1-2 mixing ratio, δ², and the dimensionless ratio X of 0-2 mixing of the 586. keV transition are obtained to be δ²≤0.16 and 0.034≤X≤0.038, respectively. The 2 branching ratio B(2; +→0_g⁺): B(2; +→2₁⁺): B(2; +→0₁⁺) is determined to be 0.023 : 1.0 : ..

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

e

., - (, , , 8-tetrahydro-, , 8, 8-tetramethyl-2-naphthalenylcarbamoyl) benzoic acid (Am ) and () -- [3- (3, -di-tert-butylphenyl) -3-oxo-l-propenyl] benzoic acid (Ch 55), suppress c-myc expression as all-trans-retinoic acid (RA) does. The decreased level of c-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 c-myc expression and around 10-fold increase in the percentage of NBT-positive cells.

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Brassinolide analogues, (R, 23R, 24R)-2α, 3α, , 23-tetrahydroxy-B-homo--oxa--ergostan--one (24-epibrassinolide) (10) and (S, 23S, 24R)-2α, 3α, , 23-tetrahydroxy-B-homo--oxa--ergostan--one (9), were synthesized from brassicasterol (3a) in five steps and with ca. 20% overall yield. The key steps are the direct formation of (, 24R)-3α, -cyclo--ergost--en--one () from brassicasterol mesylate (3b), the acid-catalyzed rearrangement of to (, 24R)--ergosta-2, -dien--one (), and the Baeyer-Villiger oxidation of the tetrahydroxy -ergostan--ones and 8.

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