During the course of preparing anticonvulsant paeonimetabolin-I adducts, new paeonilactone-A adducts: 9-phenylthiopaeonilactone-A, 9-(o-tolylthio)paeonilactone-A, 9-(m-tolylthio)paeonilactone-A. 9-(p-tolylthio)-paeonilactone-A and 9-(2-naphthylthio)paeonilactone-A, were obtained along with expected paeonimetabolin-I adducts by anaerobic incubation of paeoniflorin from peony roots with Lactobacillus brevis in the presence of the aromatic thiols, phenylthiol, o-tolylthiol, m-tolylthiol, p-tolylthiol and 2-naphthylthiol. The structures of these compounds were determined by spectroscopic methods including two dimensional (2D) NMR.

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We examined the genetic variation in the callus performance of the Al-tolerant and Al-susceptible genotypes of sorghum (Sorghum bicolor L.) on Al-containing medium. Addition of Al to the medium with a low pH, low Ca and low phosphate resulted in a severe decrease in the percentage of callus formation (CF) in both Al-tolerant and Al-susceptible genotypes. However, the percentage of callus formation in the explants from Al-tolerant genotypes was higher than that from susceptible genotypes on Al-containing medium. The genotypic difference in the relative growth of calli on Al-containing medium and in the suppression of callus formation by Al was in agreement with that in the hematoxylin staining score. Al might have been considered as a limiting factor that affected the callus growth. There was a significant correlation (r = -0.664*) between the percent relative suppression of callus formation by Al and the percentage of callus formation on Al-containing medium. The callus growth in fresh weight and size on Al -containing medium relative to that on Al-free medium (relative growth on Al-containing medium) was greater in Al-tolerant genotypes than in the other genotypes. The relative growth of callus in fresh weight and size on Al-containing medium significantly correlated (r = -0.820** and r = -0.956**, respectively) with the percent relative suppression of callus formation by Al. The tissue culture is considered to be a useful tool for selecting Al-tolerant haploids at the callus stage.

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The present study was conducted to evaluate the effects of Paeoniae Radix (PR), one of the most famous tonic traditional Chinese medicines, on the pharmacokinetics of carbamazepine (CBZ) in rats and to determine the possible interactions between PR and CBZ. The significant decrease in T_max indicated that simultaneous oral administration of PR contributed to more rapid absorption of CBZ. It is suggested that the faster absorption of CBZ might lead to the rapid onset of its clinical effect. There were no significant differences in maximum concentration (C_max), area under the plasma concentration–time curve (AUC), half-life (t_1/2), mean residence time (MRT), clearance/bioavailability (CL/F), and apparent volume of distribution/bioavailability (V_d/F) of CBZ between the two groups, showing that PR did not significantly affect the absorption extent, distribution, metabolism, and elimination of CBZ. A significant decrease in protein binding rate was found when CBZ was coadministered with PR. Further studies are in progress to clarify the clinical significance and the mechanism underlying the effects of PR on the protein binding of CBZ observed in the present study.

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Technical imidacloprid was evaluated for its effect on oxidative stress and Lipid peroxidation (LPO) in female rats for No Observed Effect Level (NOEL). Activities of Superoxide dismutase  (SOD), Catalase (CAT), Glutathione peroxidase (GPx), and level of Glutathione (GSH) and LPO were estimated in liver, kidney and brain of rats after oral administration of imidacloprid (5, 10, 20 mg/kg/day) for 90 days. Imidacloprid at 5 and 10 mg/kg/day has not produced changes in SOD, CAT, GPx and level of GSH and LPO in liver, brain and kidney. However 20 mg/kg/day has produced significant changes in SOD, CAT, GPx, GSH, LPO in liver; SOD, CAT and GPx in brain and LPO in kidney. Therefore, it is concluded that imidacloprid has not generated oxidative stress at 5 and 10mg/kg/day but induced changes at 20 mg/kg/day. Hence 10 mg/kg/day may be considered as NOEL through antioxidant enzymes and LPO in female rats.

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Paeoniflorin (PF) is an active glucoside in Shaoyao (peony root), and is transformed into an antispasmodic metabolite, paeonimetabolin-I (PM-I), by intestinal bacteria in the gut after oral administration of Shaoyao or Shaoyao-Gancao-tang (SGT, Shakuyaku-Kanzo-To in Japanese). SGT is a pain-relieving traditional Chinese formulation (Kampo-medicine in Japanese) and is often used together with antibacterial synthetic drugs, such as amoxicillin and metronidazole (AMPC-MET), in peptic ulcer therapy. Since the bioavailability of PF in SGT has been reported to be significantly reduced by co-administered antibacterial drugs, we investigated how to minimize this reducing effect of antibacterial treatment in the present study. We found that repetitive administration of SGT starting 24 h after AMPC-MET treatment rapidly restored the plasma PM-I concentration from SGT reduced by AMPC-MET, due to its restorative effect on the decreased PF-metabolizing activity of intestinal bacteria in rat feces. The present findings suggest that it may be clinically useful to administer SGT repetitively, starting 1 or 2 d after treatment with a mixture of AMPC-MET during their combination therapy, to accelerate the recovery of the reduced bioavailability of PF in SGT. Similar administration regimens may also be useful in other combination therapies involving traditional Chinese formulations and antibacterial synthetic drugs to ensure the efficacy of the bioactive glycosides in the formulations.

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The solid dispersion of naphthalene with heptakis-(2, 6-di-O-methyl)-β-cyclodextrin (DMCD) has been studied by using X-ray diffraction and thermal methods. The influence of the solid dispersion on the dissolution and sublimation of naphthalene were studied. X-Ray diffraction and thermal data indicated the amorphous state of naphthalene and DMCD. Enhanced dissolution and reduced sublimation characteristics were observed in the ground mixture and the coprecipitate. The sublimation rate of naphthalene from the ground mixture and the coprecipitate increased during storage at high relative humidity due to crystallization.

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A simple and reproducible HPLC method for the determination of paeoniflorin (PF)-metabolizing activity of intestinal bacteria in rat feces was developed and validated. Orally administered PF, a major active constituent of Paeoniae Radix, is metabolized into a bioactive compound, paeonimetabolin I (PM-I) by intestinal bacteria. Direct determination of the PF-metabolizing rate into PM-I is hard to achieve by HPLC due to the lack of intense chromophore in PM-I. However, when PF was incubated with Lactobacillus brevis, an intestinal bacterium, in the presence of phenylmercaptan, the metabolizing rate of PF into 8-phenylthio-paeonimetabolin I (PT-PM-I) was found to be equivalent to that of PF into PM-I. Thus, the PF-metabolizing activity of intestinal bacteria in rat feces was determined by measuring the rate of biotransformation of PF into PT-PM-I, which was detected by HPLC at 255 nm. This method can be utilized in the biopharmaceutical study of traditional Chinese formulations containing Paeoniae Radix.

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In the course of studies on the metabolism of active components of Huangqin-Tang (〓〓湯) by human intestinal flora (HIF), Huangqin-Tang and all individual herbs in the decoctions were incubated with a human fecal suspension separately. By using a high-performance liquid chromatographic (HPLC) method which was previously established in our laboratory, the metabolites in both the compound prescription and all the single herb decoctions were identified and determined both qualitatively and quantitatively. We found that the constituents of Huangqin-Tang, incluing baicalin (baicalein 7-glucuronide; BG), wogonoside (wogoninoglucuronide; WG), oroxylin-A-glucuronide (OG) from Scutellariae Radix, paeoniflorin (PF) from Paeoniae Radix, liquiritin (liquiritigenin 4′-O-glucoside; LG), isoliquirtin (isoliquiritigenin 4-glucoside; ILG) and glycyrrhizic acid (GL) from Glycyhhizea Radix, were converted to their metabolites baicalein (B), wogonin (W), oroxylin-A (O), paeonimetabolin-I (PM-I), liquiritigenin (L), isoliquiritigenin (IL) and glycyrrhetinic acid (GA) by HIF. The contents of the metabolites in Huangqin-Tang and in each single herb decoction increased significantly after incubation with intestinal flora. Comparing with single herb decoctions, the transformation of BG, WG, OG, LG and ILG in the compound prescription was promoted, however, that of PF and GL was inhibited. All the results suggested that the glycosides of many medicinal herbs could be converted to aglycones by HIF, and the metabolism of most glycosides was improved in the compound prescription.

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　中国内蒙古草原地帯における伝統的発酵乳エードスンスー, アイラグおよびチェゲーのの3種類から計10試料を採取し, 理化学性状の分析と微生物の分離同定を行った。また, 製法が類似しているカルピス酸乳との関連性を検討した。内蒙古発酵乳10試料ならびにカルピス酸乳のすべてから乳酸菌と酵母が分離された。理化学性状の分析結果から, エードスンスーは発酵が緩慢であるため, 乳酸やアルコールの生成量が少なく, アイラグは製法や原料の違いで成分組成や微生物叢に差異が見られた。チェゲーは原料乳が馬乳であるため成分組成は他の発酵乳と異なったが, カルピス酸乳の主要菌種であるLactobacillus helveticusが優勢に分離された。アイラグの数試料からはL. helveticusのほかヘテロ発酵乳酸桿菌が分離され, カルピス酸乳との類似性が示唆された。また, アイラグ, チェゲーからケフィール粒の構成菌であるLactobacillus kefirgranumが多数検出された。

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The fewer the water resources, the greater the demand and the more important water becomes. This applies in Egypt, where rainfall is rare and most of the country is desert, except for a narrow strip of cultivated land and urban areas along the Nile river course. Like other large rivers, the Nile Delta region is characterized by large tracts of rich fertile agricultural land, overpopulation and unique and delicate environmental conditions caused by mixing drainage and freshwater. Managing these unique natural resource areas has become increasing critical, given the threat to the ecological balance in these areas due to an increase in water exploitation to boost population and the development of resources. Accordingly, the performance of water-delivery systems, particularly irrigation systems, must be clearly defined and assessed under these current or expected stressed conditions. This paper highlights irrigation, drainage and water-management projects in Egypt and presents the positive and negative effects as well as the role of government and users in operating and maintaining the system. The objective is to identify significant research programs and projects carried out over the last three decades that have impacted on irrigated agricultural practices in Egypt. The study documents both successful and failed cases of direct and indirect research uptake. Specific recommendations for increasing the research uptake, improving the penetration of research results and taking corrective measures to strengthen and encourage research uptake to irrigation and drainage practices are highlighted.

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いくつかの有機極性溶媒を用いてn-ヘキサンとジベンゾチオフェンからなるモデル軽油の抽出脱硫を行った。極性溶媒（5 g）を用いてモデル軽油（10 g）からジベンゾチオフェンの抽出を行ったところ，49〜86 %のジベンゾチオフェンが抽出された。検討した溶媒の中では，1-メチルピロリジン-2-オンが最も効果的であった。溶媒の抽出能力と性質の相関について検討を行い，溶媒の極性（双極子モーメント）と抽出率の間に一定の相関があることを見出した。次に，いくつかのベンゾチオフェン誘導体の抽出実験を行い，硫黄化合物の構造と抽出率の関係について検討したところ，芳香環の縮合度が高いほど抽出率は向上し，メチル基の導入は抽出率の大幅な低下をもたらすことが分かった。最後に分配平衡について検討したところ，抽出能力の低いアセトニトリルやγ-ブチロラクトンでは通常の分配平衡が観測され，実験結果と計算値がよく一致していたが，アミド系溶媒では，アミド使用量が少ない場合平衡からずれ，抽出量が計算値より小さくなる傾向があることが分かった。これはジベンゾチオフェンとアミド系溶媒の間に強い相互作用があるためと考えられる。

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Using glyphosate agrochemical components, we investigated their acute toxicity to juvenile Japanese medaka (Oryzias latipes) as well as their toxic impact at gene expression level on the liver tissues of adult medaka using DNA microarray. In our acute toxicity test, juvenile medaka were exposed for 96 hr to each of the following glyphosate agrochemical components: 10~160 mg/l of glyphosate, 1.25~20 mg/l of fatty acid alkanolamide surfactant (DA), and 12~416 mg/l of a fully formulated glyphosate herbicide. As a result, LC₅₀ values of glyphosate, DA, and the glyphosate herbicide were > 160 mg/l, 8.5 mg/l, and 76.8 mg/l, respectively. On the other hand, adult male medaka fish were exposed to each of the glyphosate agrochemical components for 48 hr at the following concentrations: 16 mg/l of glyphosate, 0.5 mg/l of DA, and 16 mg/l-glyphosate/0.5 mg/l-DA mixture. Interestingly, DNA microarray analysis revealed that there were no significant gene expression changes in the medaka liver after exposure to glyphosate. Nevertheless, 78 and 138 genes were significantly induced by DA and the glyphosate/DA mixture, respectively. Furthermore, we identified five common genes that were affected by DA and glyphosate/DA mixture. These results suggested that glyphosate itself possessed very low toxicity as previously reported by some researchers at least to the small laboratory fish, and the major toxicity of the glyphosate agrochemical resided mainly in DA and perhaps in unintentionally generated byproduct(s) of glyphosate-DA mixture.

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3-[2-[p-(Un)substituted phenyl]imidazo[2, 1-b]benzothiazol-3-yl]propionic acid derivatives (2a-e) were prepared via the interaction of the corresponding 2-[p-(un)substituted phenyl]imidazo[2, 1-b]banzothiazoles (1a-e) with acrylic acid in the presence of acetic anhydride and acetic acid. Esterification of 2a-e produced methyl esters (3a-e). Upon the interaction of 3a with m-chloroperbenzoic acid, the S-dioxide (4a) was obtained. Compound 5a was prepared from 4a by alkaline hydrolysis. Vilsmeier formylation for 1a-e produced novel [2-[p-(un)substituted phenyl]imidazo[2, 1-b]benzothiazol-3-yl]formaldehyde derivatives (6a-e). Derivatives 6a-e reacted with ethyl bromoacetate to give ethyl 3-hydroxy-3-[2-[p-(un)substituted phenyl]imidazo[2, 1-b]benzothiazol-3-yl]propionate esters (7a-e). Compound dl-7a was resolved with l-(+)-tartaric acid.Compounds 2a-e showed weak or no activity in the carrageenin-induced paw edema assay. Compound 4a significantly inhibited the leakage of pontamine-sky blue dye into the peritoneal cavity of mice, in the capillary permeability inhibiton assay. Compound 5a inhibited the writhing by 62% in the acetic acid-induced writhing assay.

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  Direct carboxymethylations for aliphatic hydroxyl groups in weeds such as Tall fescue (Festuca arundinacea, TF), Sweeping lovegrass (Eragrostis curvula, SL) and Canada goldenrod (Solidago Canadensis, CG) were carried out in 2-propanol / 30 % NaOH at 55 °C for 3.5 hrs. Under the typical conditions, carboxyletylated TF (TF-CM), SL-CM and CG-CM were obtained at yields of 145%, 135% and 148% based on each dry weight of lignocellulosics, respectively. Although degrees of substitutions of these CM materials were only small values such as 0.08-0.11, almost all materials were easily dissolved into water. Structural features were investigated using FT-IR and UV-Vis. Visocosities of 1% (w/w) aqueous solutions or suspensions of CM derivatives were measured by vibrating viscometer under different temperatures and pH. Since there are differences on viscosities between TF and CG in spite of same degrees of substitution, properties were different due to different structures of plant tissues.

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Interrupt service routines are a key technology for embedded systems. In this paper, we introduce the standard approach for using Generalized Stochastic Petri Nets (GSPNs) as a high-level model for generating CTMC Continuous-Time Markov Chains (CTMCs) and then use Markov Reward Models (MRMs) to compute the performance for embedded systems. This framework is employed to analyze two embedded controllers with low cost and high performance, ARM7 and Cortex-M3. Cortex-M3 is designed with a tail-chaining mechanism to improve the performance of ARM7 when a nested interrupt occurs on an embedded controller. The Platform Independent Petri net Editor 2 (PIPE2) tool is used to model and evaluate the controllers in terms of power consumption and interrupt overhead performance. Using numerical results, in spite of the power consumption or interrupt overhead, Cortex-M3 performs better than ARM7.

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When a physical mixture of naphthalene and amorphized 2, 6-di-O-methyl-β-cyclodextrin was heated in a sealed container, a meta-stable complex was crystallized under a mild condition of heating, which showed excimer fluorescence emission of naphthalene. On the other hand, heating of the mixture at high temperature caused the crystallization of stable inclusion complex which showed monomer fluorescence emission.

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The liver X receptor is a nuclear hormone receptor that regulates lipid metabolism. Previously, we had demonstrated the antiviral properties of a liver X receptor antagonist associated with the hepatitis C virus and severe acute respiratory syndrome coronavirus 2. In this study, we screened a chemical library and identified two potential liver X receptor antagonists. Spectroscopic analysis revealed that the structures of both antagonists (compounds 1 and 2) were cyclic dimer and trimer of esters, respectively, that consisted of phthalate and 1,6-hexane diol. This study is the first to report the structure of the cyclic trimer of phthalate ester. Further experiments revealed that the compounds were impurities of solvents used for purification, although their source could not be traced. Both phthalate esters exhibited anti-hepatitis C virus activity, whereas the cyclic dimer showed anti-severe acute respiratory syndrome coronavirus 2 activity. Cyclic phthalate derivatives may constitute a novel class of liver X receptor antagonists and broad-spectrum antivirals.

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We investigated polyionic agents with regard to their effects as modulators of epidermal growth factor receptor (EGF-R) kinase activity. Many synthetic polypeptides containing glutamine as well as casein were phosphorylated, while polycationic compounds with tyrosine residues were not phosphorylatable and thus inhibited the EGF-R activity. Polyarginine, protamine sulfate, spermidine, heparin, and poly-L-lysine with a chain length of<20.5 kDa triggered the phosphorylation of poly(Tyr¹, Glu⁴). On the other hand, dextran sulfate and poly-L-lysine with chain lengths of<20.5 kDa inhibited the EGF-R kinase activity. Alteration of the state of autophosphorylation of EGF-R is not in agreement with the activity of EGF-R kinase towards poly(Tyr¹, Glu⁴). Casein and histone H1 both increased the autophosphorylation of EGF-R in a concentration-dependent manner, but only casein increased the activity of the enzyme towards an exogenous substrate. The compounds enhancing the EGF-R activity, such as poly-L-lysine, protamine, and poly-L-arginine, down-modulated the autophosphorylation reaction. We discuss the conse-quences of these effects as to in vivo conditions.

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Objectives of the research were to determine the best combination of mozzarella cheese whey and sugarcane molasses as agro-industrial wastes in producing bioethanol with the inoculation of indigenous yeasts. The research has been done experimentally by Completely Randomized Design (CRD) 3 × 3 factorial pattern, and the data was analyzed with ANOVA then continued with Tukey test. Treatments consisted of two factors, i.e. addition of sugarcane molasses (10%, 15%, 20%) and indigenous yeasts combination [C. tropicalis 1 + Blast. capitatus + C. tropicalis 2 (1:1:1), C. tropicalis 1 + Blast. capitatus (1:1), C. tropicalis 1 + C. tropicalis 2 (1:1)] that were replicated three times. Substrates fermented at ambient (25-27 °C) for 24 hours, then the bioethanol contents tested with chromium dichromate oxidation. Results show that the treatment combination of sugarcane molasses concentration and indigenous yeasts combination and single treatments of indigenous yeasts combination have shown significant effects towards the bioethanol contents, meanwhile the treatments of molasses concentration has shown nonsignificant effects. The best bioethanol contents (8.49%) was gained by the treatment combination of 15% sugar cane molasses concentration with the inoculation of C. tropicalis 1 + Blast. capitatus (1:1).

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To estimate specific power losses (SPL) of bulky magnetic hyperthermia heating mediators, a hysteresis loop measurement system in alternating magnetic field at a constant temperature was fabricated. Magnetic properties of a rectangular sample of La-Sr-Mn-Cu perovskite (LSMC) in a temperature range of 20～46°C were estimated from induced electromotive force which arose in a single turn pickup coil located at the center of exiting coil (1 MHz, 3 kA/m-rms). Complex permeability μ' and μ", coercive force H_c, and SPL of the LSMC decreased with increasing the temperature. Phase delay δ of magnetic flux density of the LSMC from the applied magnetic field were almost the same among measured temperature range.

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