The ability of Climacodon septentrionalis to immobilize and kill a mycophagous nematode (Aphelenchoides sp.) in vitro is described for the first time. Two isolates produced droplets (20–45 μm in diameter) that formed at the apices of tall, stalked, and branching secretory cells (700–

,500 μm tall). On % modified malt extract agar, nematodes became enveloped in the droplets, which restricted their ability to move and resulted in complete immobilization and death within several hours of contact. The rate of decomposition of the nematodes varied considerably, with most individuals persisting for weeks whereas others were degraded within several days and appeared to be colonized by dense hyphal growth. This study provides the first documentation of a non-agaricoid fungus producing secretory cells that are able to immobilize nematodes.

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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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Failure problems of saturated soils are classified in the present study into the following four types : Type I : The failure of loose and/or normally consolidated soils under fully drained loading conditions. Type II : The same soils but under perfectly undrained conditions. Type III : The failure of dense and/or overconsolidated soils under fully drained conditions. Type IV : The same soils but under perfectly undrained conditions. The soil-water coupling limiting equilibrium analysis on the basis of the critical state concept is shown possible to draw a distinction between type I, II and IV problems, and the limitations of the analysis procedure happen in solving the type problem in the above. This is demonstrated experimentally, in which seepage failure experiments in laboratory with the use of a saturated silty sand are employed to make distinctions clearly between the four types of failure problems. The definite distinctions both in failure load and failure mode appeared in the four types of experiments are summarized as follows : () the smallest failure load in loose sand in the undrained condition, () the largest failure load with the largest failure region in dense sand under undrained loading, () the observation of no global deformation before failure within the soil under the fully drained condition that suggests the development of very localized shear deformation in the sand. Three out of four experiments are described well by the limit analysis computation mentioned above as far as the failure load and the shape and the size of the failure region after boiling failure are concerned, and thus the type III problem is identified to be the problem that should be solved by any other means in near future.

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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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The saponin fraction from the seeds of the tea plant [Camellia sinensis (L.) O. KUNTZE (Theaceae)] was found to exhibit potent protective effects on ethanol- and indomethacin-induced gastric mucosal lesions in rats. Five new triterpene saponins, theasaponins (), (), (), (), and (), were isolated together with 11 known saponins from the saponin fraction. The chemical structures of — were elucidated on the basis of chemical and physicochemical evidence. Among the isolated saponins, theasaponins (), (), and () and assamsaponin C (10) showed an inhibitory effect on ethanol-induced gastric mucosal lesions at a dose of .0 mg/kg, p.o. and their activities were stronger than that of omeplazole. With regard to the structure–activity relationships of theasaponins, the following structural requirements for a protective effect on ethanol-induced gastric lesions were suggested; ) the 21- and/or -acyl groups are essential for the activity, ) acetylation of the 16-hydroxyl group reduce the activity.

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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-. Sixteen phosphate buffered saline (PBS), boiled PBS, 14 ethanol and 12 methanol extracts induced alkaline phosphatase (ALP) activities, an indicator of MCT- 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-,,-triol (). induced ALP activities of MCT- 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- cells by , ergosterol (), ergocalciferol (), cholesta-,,-triol (), -dehydrocholesterol () and cholecalciferol () were tested. The enzyme activities of MCT- cells were increased .0-fold by 10 μM and .-fold by 10 μM . However, , , and did not induce MCT- cell ALP activity at 0.—10 μM. These results suggested that the OH groups at C- and/or C- of and played an important role in their differentiation-inducing activities on MCT- cells. Furthermore, suppressed induction of MCT- cell apoptosis by serum starvation.

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Activity-directed isolation of the ethyl acetate, methylene chloride and n-hexane fractions of Gloiopeltis furcata resulted in the isolation of 18 compounds. Their structures were elucidated as -(-hydroxy--oxotetrahydrofuran--yl)acetic acid (), glutaric acid (), succinic acid (), nicotinic acid (), ()--hydroxyhex--enoic acid (), cholesterol (), -hydroxycholesterol (), uridine (), glycerol (), -(hydroxymethyl)--methoxybenzene-,-diol (10), (,)--oxodeca-,-dienoic acid (11), (Z)--ethylidene--methylpyrrolidine-,-dione (12), dehydrovomifoliol (13), loliolide (14), cholesteryl stearate (15), palmitic acid (16), cis-,,11,14,17-eicosapentaenoic acid (17) and α-linolenic acid (18) on the basis of spectroscopic and chemical evidences. Their anticholinesterase and antioxidant activities were evaluated via inhibitory activities on acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) as well as scavenging activities on ,-diphenyl--picrylhydrazyl (DPPH) radical and peroxynitrite (ONOO⁻). All isolated compounds (—18) exhibited moderate AChE inhibitory activities with IC₅₀ values ranging from .14—12.50 μg/ml, whereas , , , 17, and 18 showed mild BChE inhibitory activities with IC₅₀ values ranging from .57—15.89 μg/ml. Although most of the compounds isolated were lacking the scavenging activity on DPPH radical and ONOO⁻, and 10 showed good DPPH radical scavenging activity, and , 10, and 16 showed potent ONOO⁻ scavenging activity.

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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= 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 : () Triangular or quadrangular blocks can be treated; () 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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The effect of composition and controlled thermomechanical process parameters on the mechanical properties of HSLA steels is modelled using the Widrow-Hoff's concept of training a neural net with feed-forward topology by applying Rumelhart's back propagation type algorithm for supervised learning, using a Petri like net structure. The data used are from laboratory experiments as well as from the published literature. The results from the neural network are found to be consistent and in good agreement with the experimented results.

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Nアルキル,:,10-ペリレンテトラカルボン酸モノアンヒドリド=モノイミド[a～]と芳香族アミン(アニリン,p-トルイジン,p-アニシジン,,-キシリジン,-アミノナゾベンゼン,およびo-フェニレンジアミン)を縮合して非対称型,:,10-ペリレンビス(ジカルボキシミド)誘導体-N-アルキル-N'-アリール-,:,10-ペリレンビス(ジカルボキシミド)(〔a～〕,〔a～〕,〔a～〕,〔a～〕,〔a～〕,および〔10a～〕)を合成した. これらの各誘導体はすべて赤色系の色相を示し, 顔料試験の結果N-ブチル-N'-アリール-,:,10-ペリレンビス(ジカルボキシミド)(たとえば〔〕や〔〕)がとくにすぐれた耐光性を示した.

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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 (G

;;;) was performed. At first, we moved drugs from solution with pH . (.±0.05) to pH .0 (.0±0.05) 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 minutes, i.. the active substance should not be released within minutes at pH . The exposure at the second stage was conducted with pH (.0±0.05), 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

, 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 ,±0,%; 41,±,0%; 62,±,0%; 79,±,%; ,±,%; ,±,%; ,±,%; for Generic - 0; 49,±,%; 88, ±,%; 90,±,%; 88, ±,%; ,±,0%; 85,±,%; for Generic - 0; 30,±,%; 66,±,%; 76,±,%; ,±,%; 86,0±,%; 84,±,%: for Generic - ,±,%; ,±,%; , ±,%; ,±,%; ,±,%; ,±,0%; ,0±,%; for Generic - ,±,%; 84,±0,%; 84,±,%; , ±0,%; ,±0,%; ,±0,%; ,±,%, respectively.

An analysis of the omeprazole concentration in pH

solution at the second stage revealed the following parameters after the same time: for OO - ,±0,%; 40, ±,0%; 62,±,0%; ,0±,%; 85,±,%; ,±,%; ,±,%; for Generic - 0; 67,0±,%; 89,±,%; , ±,%; 89,±,%; 88,±,%; ,±,%; for Generic - 0; 42,±,%; 75,±,%; ,0±,0%; 88,±,%; 88, ±,%; ,±,0%; for Generic - 85,±0,%; 85,±0,%; 84,±0,%; ,±,0%; 84,±0,%; 84,±0,%; 84,±0,%, respectively. Generic release and degradation were completely realized at pH .

Conclusion

Decreased gastric stability of Generic

and Generic 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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Two new partially saturated tricyclic ring systems, , a, , , , 10, 10a, 11-octahydro-11-oxodibenz [, ] oxepins (a and ), and -thiepins (a and ) were synthesized. Compounds a and were desulfurized to give a pair of isomeric -methylbenzoylcyclohexanes (10a and 10). Deuterated a and (11a and 11) were prepared starting from butadiene- (12). The stereochemical features of a (trans), (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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