N-(2-フルオレニル) -マレイミド (I), N-1-(4-アセトキシナフチル) -マレイミド (II), N-2-(-アセトキシフルオレニル) -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] ^2.11 [IV] ^0.64, R_p=k [II] ^2.26 [IV] ^0.72, R_p=k [III] ^1.76 [IV] ^0.52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 (), 頻度係数 (A) は=26.4kcal/mol (I), 23.3kcal/mol (II), .kcal/mol (III), A=3.4×10¹⁵ (I), 2.7×10¹¹ (II), 1.×10¹¹ (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, Q, 値を次のように決定した.
I (M₁) -V (M₂) 系で, r₁=0.24, r₂=0.93, Q₁=0.43, =1., II (M₁) -V (M₂) 系で, r₁=0.17, , Q₁=0.51, =1.37, III (M₁) -V (M₂) 系で, r₁=0.068, r₂=1.34, Q₁=0., =1.90となった.

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This study aimed to determine the prevalence of fecal carriage of extended spectrum β-lactamase (ESBL) and/or plasmidic AmpC β-lactamase (pAmpC) producing Escherichia coli among dogs (n=428) in Turkey. Polymerase chain reaction (PCR) and sequencing were used to characterize genes encoding β-lactamase and plasmid mediated quinolone resistance (PMQR). Antimicrobial susceptibility testing and PCRs for virulence genes and phylogenetic groups were also performed. Cefotaxime resistant

. coli isolates were detected in 95 (.2%) of the swab samples. Sequencing analysis results showed occurrence of various β-lactamase genes: bla_CTX-M-15 (62), blaTEM-

1b

(42), bla_CMY-2 (

22

), bla_CTX-M-3 (16), bla_CTX-M-1 (15), bla_OXA-1 (

9

) and bla_SHV-12 (3) alone or in combination. The most frequently encountered phylogenetic group was group A₁ (35.

8

%), followed by group D₂ (

22

.1%),

B

1 (15.

8

%), D₁ (

9

.

5

%), A₀ (7.4%),

B2₂

(

5

.3%) and

B2₃

(4.2%), respectively. PMQR genes, aac(6’)-Ib-cr, qnrS1 and qnrB10 were detected in 25.3, 10.

5

and 1.1% of the isolates, respectively. While all isolates were susceptible to imipenem and amikacin, resistance rates to non-β-lactam antibiotics ranged from 20.0% for tobramycin to 56.

8

% for tetracycline. The virulence genes were only detected in 34 (36.2%) of the isolates and this isolates carried single or various combination of virulence genes of iucD, papC, papE, f17a-A and eaeA. Four isolates were identified as human virulent pandemic CTX-M-15 producing

E

. coli clone O25

b

:ST131/

B

2. To the best of our knowledge, this is the first study to show fecal carriage of ESBL/pAmpC type β-lactamase producing

E

. coli isolates among dogs in Turkey.

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The phase diagrams of the Ni-Mo- and Ni-W- ternary systems in the region of less than 50mol% were constructed by thermodynamic calculation, based on the data obtained by thermodynamic measurement of the related materials. We found three ternary eutectic points and three or two ternary peritecto-eutectic points as follows:
:L (1365K, 71.mol%Ni-6.0mol%Mo-.mol%)=(Ni)++
:L (1355K, 62.mol%Ni-2.mol%Mo-30.mol%)=++
:L (1445K, 42.0mol%Ni-30.6mol%Mo-10.3mol%)=(Ni)+NiMo+
P₁:L (1812K, 34.mol%Ni-42.3mol%Mo-.mol%)+MoB=+
P₂:L (1633K, 42.3mol%Ni-40.4mol%Mo-17.3mol%)+Mo=+
P₃:L (1812K, 53.mol%Ni-33.7mol%Mo-12.mol%)+Mo=NiMo+
:L (1622K, 51.0mol%Ni-31.6mol%W-17.4mol%)=(Ni)+W+
:L (1260K, 71.0mol%Ni-7.0mol%W-.0mol%)=(Ni)++
:L (1291K, 65.4mol%Ni-4.mol%W-29.mol%)=++
P₁:L (2115K, 23.mol%Ni-43.1mol%W-33.1mol%)+WB=+
P₂:L (1657K, 48.mol%Ni-33.1mol%W-18.0mol%)+=W+
The calculated phase diagrams are expected to be useful for the development of new Ni-based heat-, corrosion- or wear-resistance alloys.

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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 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.

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Brassinolide analogues, (R, 23R, 24R)-2α, 3α, , 23-tetrahydroxy--homo-7-oxa--ergostan-6-one (24-epibrassinolide) (10) and (S, 23S, 24R)-2α, 3α, , 23-tetrahydroxy--homo-7-oxa--ergostan-6-one (), 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-6-one (4) from brassicasterol mesylate (3), the acid-catalyzed rearrangement of 4 to (, 24R)--ergosta-2, -dien-6-one (6), and the Baeyer-Villiger oxidation of the tetrahydroxy -ergostan-6-ones 7 and .

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We previously reported that orthostatic dysregulation (OD) was relatively common in normal young females and that the Schellong test was a useful, practical procedure in the diagnosis of this condition.
We carried out a survey and analyzed date from both the Yatabe-Guiford Personality test (Y-G test) and the Cornell Medical Index-Health Questionnaire (CMI) in 167 females aged 18 to 24 years (mean age =19.7 years). OD was confirmed in 38 and suspected in 32; the remaining were considered to be normal from the results of the Questionnaire for OD.
Of the 167 young females, 33 (19.%) were type A in the Y-G test, 38 were type (.%), 27 type C (16.1%), 52 type D (31.1%) and 17 type (10.2%). Reports in the literature indicate that individuals with type and type Y-G results are apt to have mental and/or emotional “instability”. Of the normal subjects, 28 were type or type (28.%), of those with confirmed OD the number was 17 (44.7%) and of those with suspected OD it was 10 (31.2%). The difference between the normal subjects and those with confirmed OD was significant. Of 132 individuals with CMI types I and II 34 (25.%) were Y-G types and and of 35 individuals with CMI type III and IV 21 (60%) were Y-G types and .
These results suggest that there may be some correlation between OD and emotional and/or psychosomatic instability. Further studies on the practical implications of these testing procedures are necessary for the evaluation of individuals with OD.

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Condensation of anthranilamide and its derivatives with various 1, 3-cyclohexanediones a, or 2, 4-pentanediones under acidic conditions produced a variety of heterocycles, leading to the synthesis of tetrahydropyrido[2, 1-]-quinazolin-11-one derivatives. Condensation of anthranilamide with a or in the presence of p-toluenesulfonic acid at the reflux temperature of tetrahydrofuran (THF) afforded compound 6a (40%) and compound 7a (%) or compound 6 (47%) and compound 7 (39%), respectively. However, reflux of anthranilamide with a or in 6% ethanolic hydrogen chloride provided compounds 6a and 6 in 77% and 73% yields, respectively. Heating 7a with a in 6% ethanolic hydrogen chloride furnished 6a in .4% yield. Reaction of anthranilamide with c under the same conditions resulted in the formation of 11 (57%). Treatment of compounds 6a and 6 with NaBH₄ furnished a, (89, % yields), which were subsequently subjected to the Mitsunobu reaction to produce 6, 7, , -tetrahydro--methyl-11H-pyrido[2, 1-]quinazolin-11-one (a) and 6, 7, , -tetrahydro-7, 7, -trimethyl-11H-pyrido[2, 1-]quinazolin-11-one () in 56 and 72% yields, respectively. However, heating 14 with 15a in CH₃CN in the presence of p-toluenesulfonic acid furnished 19 in 31% yield. Under similar conditions, treatment of 21 with 15a provided 23a (42.4% yield), a key intermediate for the synthesis of rutaecarpine. Analogous reaction of 21 with 15, 15c and a provided -d in 63-99.3% yield, respectively.

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Six full-length cDNAs encoding pig cytochrome P450 (CYP) enzymes, CYP1A1, CYP2A19, CYP2, CYP2C33v4, CYP2C49, and CYP21, were isolated and sequenced. The cDNA sequences of pig CYP1A1, CYP2A19, CYP2, CYP2C49, and CYP21 showed high similarity to human CYP1A1 (85.4%), CYP2A13 (88.6%), (81.1%), CYP2C18 (85.3%), and (.%), respectively, and pig CYP2C33v4 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 CYP2C33v4 and > CYP2C49 > CYP1A1 and CYP2A19 > . In the kidney, the CYP2C33v4 gene was expressed at the same level as in the liver, but the CYP1A1, CYP2A19, and genes were expressed at lower levels than in the liver. Little renal gene expression of CYP2C49 and CYP21 was observed. We revealed for the first time the full-length cDNA sequences encoding pig CYP1A1 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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Melithasterols A-D (1-4), isolated from a gorgoinan coral Melithaea ocracea of Okinawa, were shown to be cholestane-, 24-methyl--dehydrocholestane-, -dehydrocholestane-, and 24-methylenecholestane-derivatives. respectively, having a common 3β, 7α -dihydroxy-α, 6α-epoxy-Δ^ steroid nucleus. This was confirmed by direct comparison with the authentic sample prepared by lead tetra-acetate oxydation of cholest-6-ene- 3β, α, α-triol 3-monoacetate. Twelve new polyhydroxysterols were isolated from an Alcyonium sp. (7,,), and Sclerophytum sp. (14,16,19,20,21,a,23,26,28) soft corals collected off the coasts of the Andaman and Nicobar Islands in the Indian Ocean. All the Sclerophytum sp. soft corals contained 17a or its 25-deacetyl derivative. Compounds 7 to were identified as 24-methylenecholest--ene- 3β, 16β-diol-3-0-α-L fucoside (7) and its 7β-() and 7α-hydroxy () derivatives. Compound 14 was shown to be 24S-24-methylcholest--ene-3β,25ξ,26-triol and was correlated to the known compound 15 by α, 6β-glycolation. Compound 16 was shown to be β, 6α-isomer of 17, correlating to 17 by PCC oxidation followed by dehydration. Compound 19 was identified with 25-deacetyl derivative of the known compound lobosterol (19a) by hydrolysis of authentic lobosterol. Compounds 20 and 21 were shown to be 7-dehydro-(20) and -dehydro-(21) derivative of 17a and 17, respectively, by comparisons of their spectral data with reference compounds. Compounds a and 23 were 24S-methylcholestane-3β, α 25-triol-6-one 25-monoacetate (a) and its 25-deacetoxyl derivative (23). Partial PCC oxidation of 17a afforded a. Compounds 26 (andamansterol) and 28 (nicobarsterol) were shown to be gorgost--ene-3β, α. 11α, 21-tetrol and novel secosteroid, 11,21-cyclo--homo-11-oxa-, 11-secoergostane-3β, 6α, 12ξ-triol--one, respectively, by spectral analyses (H-HCOSY, HMQC, HMBC).

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（はじめに）血清クレアチニン（Ｃｒe）は性・年齢による影響をうけるため正確に 腎機能を反映しないとされる。このため日本腎臓病学会から腎機能の評価に―ＧＦＲを用いることが提唱されている。そこで、今回、本院のドック・健診受診者の腎機能を－ＧＦＲで評価し、その有用性について検討したので報告する。 （対象・方法）対象は平成２１年３月～７月までの受診者、男２１９名、女３５０名（計５６９名）である。改訂ＭＤＲＤ簡易式により血清Ｃｒｅから－ＧＦＲを算出し、性・年代別に集計し、有用性を評価した。 （結果）男性のＣｒｅ平均値は0.±0.11、女性は0.58±0.08（基準値：男0.～1.0・女0.2～0.）であった。男性の年代別の－ＧＦＲ平均値は、２０代.1±15.、３０代94.±10.0、４０代.±.1、５０代.1±12.、６０代76.±13.2、７０代↑75.±12.。女性の２０代104.±18.0、３０代96.3±15.6、４０代.1±13.、５０代83.0±11.、６０代80.±15.1、７０代↑74.±17.であった。日本腎臓病学会のＣＫＤステージ分類ではステージ_II_（－ＧＦＲ60～89）をＧＦＲ軽度低下としている。－ＧＦＲの結果からするとステージ_II_は、男性１３１名（59.％）、女性１６４名（46.％）。ステージ_III_は男性１６名（7.3％）、女性１４名（4.0％）であった。 （まとめ）腎機能の指標として－ＧＦＲは血清クレアチニンよりは鋭敏とみなされるが女性高齢者では体表面積で補正した－ＧＦＲで評価すべきと考えられた。　　

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We purified a sterol with antitumor activity from the edible mushroom Sarcodon aspratus (BERK.) S. ITO and identified it as ,-epidioxy--ergosta-6,(11),-trien-3β-ol (,11-dehydroergosterol peroxide ((11)-DHEP)). Purified (11)-DHEP was a more effective inhibitor of HL60 leukemia cell growth and stronger apoptosis-inducer than ,-epidioxy--ergosta-6,-dien-3β-ol (ergosterol peroxide (EP)) that we had previously identified as an apoptosis inducer. Moreover, (11)-DHEP selectively suppressed the growth of HT29 human colon adenocarcinoma cells but not WI38 normal human fibroblasts. After d incubation of HT29 with 7 μM (11)-DHEP, the number of S phase cells decreased from 23 to 15% of total diploid cells and 17% became hypodiploid. Expression of the cyclin-dependent kinase inhibitor 1A (p21, WAF1, Cip1) (CDKN1A), which has been shown to cause cell cycle arrest and apoptosis in HT29 cells, was induced by (11)-DHEP. These results suggest that (11)-DHEP inhibits HT29 cell growth by inducing CDKN1A expression, thus causing cell cycle arrest and apoptosis.

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Eight new sterols, , -epidioxy-(, 24R)-23-methylergosta-6, -dien-3β-ol (1), 3β, , -trihydroxy-(, 24R)-23-methylergosta-7, -dien-6-one (2), 3β, , -trihydroxy-(24S)-ergost-7-en-6-one (3), 3β, , , 14α-tetrahydroxy-(, 24R)-ergosta-7, -dien-6-one (4), (, 24R)-ergosta-7, -diene-3β, , 6α, -tetrol (), , -epidioxy-3β-hydroxy-(, 24R)-ergosta-7, -dien-6-one (6), , -epidioxy-3β-hydroxy-(24S)-ergost-7-en-6-one (7) and , 6α-epoxy-(, 24R)-ergosta-, -diene-3β, 7β, 14α-triol (), have been isolated from five edible mushrooms, Lentinus edodes, Flammulina velutipes, Hypsizigus marmoreus, Pleurotus ostreatus and Pholiota nameko together with fifteen known ones (-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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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), 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,,6β-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,,6β-triol (4), 7-dehydrocholesterol () and cholecalciferol (6) 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 6 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-6 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.

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