A biosynthetic pathway for (

)-methyl cinnamate formation was evaluated in Tricholoma matsutake by tracer experiments using ¹³C- and ²H-labeled precursors. One hundred percent selective ¹³C incorporation was observed when L-[1,2,,4,5,,,,-

13C₉

, ^15/N]phenylalanine was converted to (

E

)-[1,2,

3

,4,5,

6

,

7

,

8

,

9

-

13C₉

]cinnamate and (

E

)-[1,2,

3

,4,5,

6

,

7

,

8

,

9

-

13C₉

]methyl cinnamate. Similarly, 100% selective ¹³C incorporation was observed when (

E

)-[1,2,

3

,4,5,

6

,

7

,

8

,

9

-

13C₉

]cinnamate was converted to (

E

)-[1,2,

3

,4,5,

6

,

7

,

8

,

9

-

13C₉

]methyl cinnamate. In contrast, the ²H incorporation selectivities were

82

.1% and

81

.4% when L-[2,

3

,4,5,

6

,

7

,

7

,

8

-

2H₈

]phenylalanine was converted to (

E

)-[2,

3

,4,5,

6

,

7

,

8

-

2H₇

]cinnamate and (

E

)-[2,

3

,4,5,

6

,

7

,

8

-

2H₇

]methyl cinnamate, respectively. Thus, T. matsutake synthesizes (

E

)-methyl cinnamate from L-phenylalanine via (

E

)-cinnamate. (

E

)-cinnamate was likely formed through two pathways: one was major and the other was a minor.

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Background

The differences in conditions of enteric-coated acid-labile drug release and absorption between healthy subjects in bioequivalence studies and gastrointestinal patients in clinical practice can lead to significant differences in gastric stability of original PPIs and generics. Thus, pathologic duodenogastric reflux (PDGR) and the pH increasing within PPIs administration still remain unaccounted for.

Methods

Two-stage modified comparative dissolution testing of original omeprazole (OO) and four generics (G1;2;

;4) was performed. At first, we moved drugs from solution with pH 1.2 (1.2±.05) to pH . (.±.05) and measure concentration of omeprazole in solution by high-performance liquid chromatography. According to our self-developed formula, pH exposure time of resistance to PDGR for omeprazole is 4 minutes, i.. the active substance should not be released within 4 minutes at pH . The exposure at the second stage was conducted with pH 4 (4.±.05), that imitated gastric pH after PPI administration. And then we also moved drugs to pH with the subsequent measurement of omeprazole concentration.

Results

Omeprazole concentrations after 4, 10, 15, 20, 30, 45, 60 minutes in pH

solution at the first stage were different for OO and generics. For OO, these values were 4,±,%; 41,4±,%; 62,±4,%; 79,5±2,%; 83,5±2,%; ,±2,%; 80,±4,4%; for Generic1 - ; 49,±,%; 88, ±2,%; 90,4±,%; 88, 2±2,2%; 87,±2,%; 85,±1,1%; for Generic2 - ; 30,±,%; 66,±,2%; 76,4±,4%; ,±5,%; 86,±,%; 84,±,%: for Generic - 80,±,%; 83,5±1,%; 83, ±,2%; 83,±2,%; ,±2,1%; ,1±2,%; ,±2,4%; for Generic4 - ,5±1,%; 84,4±,%; 84,2±1,2%; , ±,%; ,±,%; ,±,%; ,±1,1%, respectively.

An analysis of the omeprazole concentration in pH

solution at the second stage revealed the following parameters after the same time: for OO - 4,4±,%; 40, 5±,%; 62,±2,%; 80,±,1%; 85,4±2,%; ,±,4%; 80,±,5%; for Generic1 - ; 67,±,%; 89,±2,%; 91, ±4,%; 89,1±1,%; 88,±1,4%; 87,±1,2%; for Generic2 - ; 42,2±5,%; 75,1±,%; ,±,%; 88,4±,2%; 88, ±1,%; 87,±1,%; for Generic4 - 85,5±,5%; 85,±,5%; 84,±,%; ,±,%; 84,4±,%; 84,4±,%; 84,±,4%, respectively. Generic release and degradation were completely realized at pH 4.

Conclusion

Decreased gastric stability of Generic

and Generic4 makes PDGR and inhibited gastric acid secretion due to PPIs administration the potential causes of decreased enteric-coated acid-labile drugs stability.

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The possibility of attenuation of microseismic waves due to the presence of an upward folding of the ocean bottom into the liquid is discussed in this paper. The upward folding of the ocean bottom has been idealized by means of an irregularity in the form of a rectangle intruding into the liquid and the evaluation of the displacement component at any point of the solid medium has been carried out in two stages. First, the change in the incident mode of the surface wave due to the presence of the rectangular irregularity has been determined, and second, the subsequent change of the resulting displacement components due to the termination of the liquid layer and the step change in elevation of the solid medium at the continental margin has been discovered. Finally, numerical calculation has been made to determine the attenuation of the microseismic waves of different periods due to the presence of the rectangular irregularity at the ocean bottom.

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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 (

E

), 頻度係数 (A) は

E

=26.4kcal/mol (I), 23.

3

kcal/mol (II),

22

.

8

kcal/mol (III), A=

3

.4×10¹⁵ (I), 2.

7

×10¹¹ (II), 1.5×10¹¹ (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,

e

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,

e₁

=1.

82

, II (M₁) -V (M₂) 系で, r₁=

0

.17,

r₂2.29

, Q₁=

0

.51,

e₁

=1.37, III (M₁) -V (M₂) 系で, r₁=

0

.068, r₂=1.34, Q₁=

0

.87,

e₁

=1.90となった.

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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 () 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.

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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.%), (.1%), CYP2C18 (85.%), and (.5%), 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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We screened the differentiation-inducing activities of 39 mushroom extracts from Akita prefecture, Japan, on the mouse osteoblastic cell line, MCT-1. Sixteen phosphate buffered saline (PBS), boiled PBS, 14 ethanol and 12 methanol extracts induced alkaline phosphatase (ALP) activities, an indicator of MCT-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-,5α,-triol (1). 1 induced ALP activities of MCT-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 MCT-1 cells by 1, ergosterol (2), ergocalciferol (), cholesta-,5α,-triol (4), -dehydrocholesterol (5) and cholecalciferol () were tested. The enzyme activities of MCT-1 cells were increased .-fold by 10 μM 1 and 2.4-fold by 10 μM 4. However, 2, , 5 and did not induce MCT-1 cell ALP activity at .1—10 μM. These results suggested that the OH groups at C-5 and/or C- of 1 and 4 played an important role in their differentiation-inducing activities on MCT-1 cells. Furthermore, 1 suppressed induction of MCT-1 cell apoptosis by serum starvation.

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In Japan, aseptic meningitis cases due to enterovirus infections increase every summer in various degrees with an incidence peak usually in July. During the past 11 years from 1981 through 1991, a total of , 595 enterovirus isolations from aseptic meningitis cases were reported from 54 participating laboratories. Eight enterovirus types caused large epidemics; more than 100 isolations of each type from aseptic meningitis cases were reported for every epidemic year of the respective type. They were coxsackievirus (C) types and 5, echovirus () types 4, , , , 18 and 30. Among these, the highest meningitisassociating frequency was reported for 30, representing .% of the total isolations reported for the type during this period, followed by 4, 71.1%. The frequencies of , , and CB5 were in a range from 54.5% to 44.4%, while that of 18 was 37.% and that of CB 21.%. During the epidemics, enterovirusassociated meningitis was most frequently reported among children of 4- years of age. High frequencies were also shown in infants less than 1-year of age in some types. A total of 4, 240 enteroviruses were isolated from cerebrospinal fluid of aseptic meningitis cases, representing 49.% of the cases with enterovirus isolation.

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(,)-2,-エポキシ-,,11,11-テトラメチルシクロウンデカ-,-ジエン(2)をフムレン1((2,,)-,,11,11-テトラメチルシクロウンデカ-2,,-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,2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,2の新たな合成法と簡便な精製法を見いだし,2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2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.2の精製は1と同様硝酸銀()錯体の結晶で行い,純粋な2は1から通算牧率32.%で得られた.2の既知方法による合成は4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2の合成法は2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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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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Vibrio parahaemolyticus is a prevalent food-borne pathogen in Taiwan, Japan and other Asian countries. This work presents a novel ribotyping method for the molecular epidemiological examination of this pathogen. Genomic DNA was fragmented by HindIII digestion and hybridized with cDNA probe for Escherichia coli 16S and 23S RNA genes. A total of 121 isolates obtained from outbreaks during 1992 and 1994 in Taiwan were characterized by this ribotyping method. Four to seventeen restricted fragments were visualized in these isolates. After hierarchical cluster analysis, these isolates were grouped into thirty different ribotypes. In addition, A, A, and F1 were the major ribotypes, consisting of ., 13.2, .1, and .% of the isolates, respectively. A, , F, G and were the major groups, consisting of 46.2, 14., .1, ., and .% of the isolates, respectively. The discriminatory ability of this ribotyping method, as determined by Simpson's index of diversity, was ., which closely resembled that of a previously reported pulsed-field gel electrophoresis method.

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The correction factor (η_ie) for the ultimate bearing capacity of a footing placed adjacent to a slope, taking into account the combined effect of horizontal and vertical seismic loads, represented by horizontal and vertical seismic coefficients, k_h and k_v, respectively, was derived using a modified Janbu's slice method. The influence of slope angles ‘α’ on the values of ‘η_ie’ are studied here. It was found that the values of η_ie can be expressed as an exponential function of ‘k_h/(1-k_v)’ and ‘α’, with a measurable interdependency between ‘α’ and ‘η_ie’. The influence of ‘α’ on the value of ‘η_ie’ increases as the input value of ‘k_h/(1-k_v)’ increases. Equations derived based on the analytical results are proposed to account for this effect. Based on the analyses of 11 near-fault seismographers obtained in the 1999 Chi-Chi earthquake in Taiwan, a ratio between the vertical and the horizontal seismic coefficients, λ, of between ±.25 is suggested for including the combined effect of vertical and horizontal seismic forces in evaluating the seismic bearing capacity of footings located in near-fault areas.

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