著者

Yifan Zhong Xiaoyan Han Shengbin Li Hui Qi Yali Song Xiaoqiang Qiao

出版者

The Pharmaceutical Society of Japan

雑誌

Chemical and Pharmaceutical Bulletin (ISSN:00092363)

巻号頁・発行日

vol.65, no.10, pp.904-910, 2017-10-01 (Released:2017-10-01)

参考文献数

30

被引用文献数

12

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N-Myristoyltransferase (NMT) has been validated pre-clinically as a target for treatment of fungal infections. Various substituted thiochroman-4-one derivatives have been synthesized by an efficient method. The synthesized compounds 7a–y and 8a–t were evaluated for their in vitro antifungal activity against the Canidia albicans, Cryptococcus neoformans, Epidermophyton floccosum, Mucor racemosus, Microsporum gypseum and Aspergillus nigerstrain. A series of compounds exhibited significant activity (minimal inhibitory concentrotion (MIC)=0.5–16 µg/mL) against Canidia albicans and Cryptococcus neoformans. The antifungal activity of compound 7b was reached to that of fluconazole, which can serve as a good starting point for further studies of structural diversity of the NMT inhibitors. The molecular docking studies revealed an interesting binding profile with very high receptor affinity for NMT of Canidia albicans.

著者

Tarek Fathy El-Moselhy Peter Ayoub Sidhom Eman Ahmed Esmat Nageh Ahmed El-Mahdy

出版者

The Pharmaceutical Society of Japan

雑誌

Chemical and Pharmaceutical Bulletin (ISSN:00092363)

巻号頁・発行日

vol.65, no.10, pp.893-903, 2017-10-01 (Released:2017-10-01)

参考文献数

47

被引用文献数

7

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Resurgence to target L-type voltage-dependent calcium channels has been applied by the synthesis of two series of nifedipine analogues where the ortho- or a meta-nitrophenyl ring is retained. A pre-synthetic molecular docking study with a receptor model followed by molecular alignment has been performed on 47 compounds to predict the most active member. The IC50 values revealed that some of the compounds are similar to or more active than nifedipine. Substitution of groups at the 3- and 5-positions of the dihydropyridine (DHP) ring gave 3k, which is more active than nifedipine. Our valid three-dimensional quantitative structure–activity relationship (3D-QSAR) model prefigures the influence of lipophilicity, bulkiness and chelating effects of the C3 and C5 substituents. Bulky groups interfere with ring-to-ring hydrophobic interaction with tyrosine (Tyr)4311 and limit the efficiency of increasing the length of the hydrocarbon chain of esters at the 3- and 5-positions of the DHP ring as an approach to increasing the activity. The presence of a chelating substituent on the phenyl ring at the 4-position of the DHP ring ensures strong binding to the receptor and hence stabilization of the closed-channel conformation. The validation of 3D-QSAR model indicated its proficiency in predicting activity of newly compounds belonging to the same chemical class.

著者

井上 貴嗣 稲田 智久 田川 善彦

出版者

バイオメディカル・ファジィ・システム学会

雑誌

バイオメディカル・ファジィ・システム学会誌 (ISSN:13451537)

巻号頁・発行日

vol.8, no.1, pp.1-10, 2006

参考文献数

6

被引用文献数

2

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車いすは元々下肢の障害や高齢による下肢の筋力低下によって歩行が困難な方の移動手段であり,下肢を駆動力とすることは考えられていなかった.一般的な上肢駆動の車いすでは,下肢は全く使用されず,肩の障害や下肢の筋力低下や関節の拘縮の原因となっている.一方,下肢駆動車いすは駆動時に下肢を動かすため,下肢の筋力低下や関節の拘縮などの予防や抑制を日常生活において行うことができる.しかしながら,下肢駆動車いすにも下肢に十分な筋力がなければ自力走行が困難であるという問題がある.そこで,我々は足漕ぎ車いす搭乗者の下肢に機能的電気刺激を印加すること,およびモータによるアシストをうことで問題の改善を試みる.本研究ではファジィ制御を用いた運動制御システムを構築し,健常人男性1名を被験者として屋外平坦路上で実験を行い,漕ぎ始めから滑らかなペダリング動作を実現した.

出版者

刊

巻号頁・発行日

vol.第9冊 (ものくさ太郎),

著者

神谷 大介 赤松 良久 渡邊 学歩 大槻 順朗 二瓶 泰雄 上鶴 翔悟

出版者

Japan Society of Civil Engineers

雑誌

土木学会論文集G(環境) (ISSN:21856648)

巻号頁・発行日

vol.70, no.5, pp.I_87-I_94, 2014

被引用文献数

1

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本論文では近年増加してきている局地的豪雨災害に対し,小規模集落での課題と適切な支援方策を検討するため,2013年に発生した山口・島根豪雨災害における萩市須佐川を対象として,調査・分析を行った.この結果,避難勧告の発令基準は雨量と水位によって規定されているが,実際には水位のみで判断されていた.雨量を基に判断すれば,1時間以上早く避難勧告が発令出来たことを示した.住民は周囲の状況を見て避難を判断しており,膝上以上の水位の中,危険な避難行動を行っていた.安全な避難を促すためには,事前のリスクコミュニケーションと雨量を基にした避難準備情報の発表が必要であることを示した.

著者

中野 晃一

出版者

上智大学

雑誌

若手研究(B)

巻号頁・発行日

2002

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1993年以降の政党政治の変動が地方分権改革の政治過程にどのような影響を与えたのかを探る観点から、以前の改革過程に比して、政策結果・政策過程・アクター・リソースに関して変化が見られたか否かに焦点を絞って研究を進めてきたが、平成14年度までに調査そのものは概ね完了し、平成15年度では、主として調査結果を英文論文の第としてまとめることに意を注いだ。研究計画の順調な進捗を受けて、平成16年度には、論文の最終的な国際学術誌・論集等への投稿(ないし寄稿)・出版を目的とした。そのため、補足的調査をし、論文の更なる推敲を行い最終稿をまとめることが本年度の研究活動の中心となった。従って、研究経費としては、研究補助・資料整理のための謝金、論文執筆のための図書・ソフトウェア・コンピュータ関連消耗品・文具等の物品費、地方分権改革関連資料についての補足調査を目的とした宮城県仙台市への国内旅費が主たるものとなった。本研究計画を締めくくる研究成果の発表としては、1990年代の日本における政党政治の変動(政権交代および連立政権)が、政策過程と政策そのものの変化に影響を与えた事例として、日本社会党と総評の役割に注目して、地方分権改革を(情報公開と立法府の行政府チェック機能強化とともに)考察した英文論文「‘Democratic Government' and the Left」をRikki Kersten・David Williams(編)、The Left in Japanese politics(Routledgecurzon/Leiden Series on Modern East Asian Politics & History)(Routledge,2005)に出版した。

著者

為永春水 作

出版者

大嶋屋伝右衛門

巻号頁・発行日

vol.二編中, 1841

著者

近藤 康久 熊澤 輝一 菊地 直樹 鎌谷 かおる 安富 奈津子 内山 愉太 林 憲吾 橋本 慧子 村松 伸

出版者

研究・イノベーション学会

雑誌

年次学術大会講演要旨集

巻号頁・発行日

vol.32, pp.656-659, 2017-10-28

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一般講演要旨

著者

杉山 昌広 朝山 慎一郎 小杉 隆信 石井 敦

出版者

研究・イノベーション学会

雑誌

年次学術大会講演要旨集

巻号頁・発行日

vol.32, pp.651-655, 2017-10-28

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一般講演要旨

著者

太田 和彦 立川 雅司

出版者

研究・イノベーション学会

雑誌

年次学術大会講演要旨集

巻号頁・発行日

vol.32, pp.645-650, 2017-10-28

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一般講演要旨

著者

小宮山 進

出版者

一般社団法人 日本物理学会

雑誌

大学の物理教育 (ISSN:1340993X)

巻号頁・発行日

vol.22, no.2, pp.79-82, 2016 (Released:2016-09-21)

参考文献数

7

被引用文献数

1

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1.はじめに大学初年級の電磁気学の講義は,クーロンの法則から始めて静磁気から電磁誘導に至り,最後の電磁波に入る前あたりでマクスウェル方程式がやっと顔を出す,という順番が定番だと思われま

著者

山本 祥一朗

出版者

公益財団法人 日本醸造協会

雑誌

日本醸造協会誌 (ISSN:09147314)

巻号頁・発行日

vol.99, no.2, pp.106-111, 2004-02-15 (Released:2011-09-20)

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酒精強化ワインであるボルトとマディラの伝統的な酒造場の訪問・体験記である。これらは輸出される比率が高く, 現地で一般的に飲まれる酒としての蔭はうすい。それでも今なお人々の誇りであり, 堂々とした存在感がある。その様な現地から眺めた日本の酒類消費に対する提言も汲み取っていただきたい。

巻号頁・発行日

vol.[45]貮拾貮下,

著者

鷲見 昭典 奥山 孝三 小林 薫 大谷 渡 大村 孝男

出版者

一般社団法人日本PDA製薬学会

雑誌

日本PDA学術誌 GMPとバリデーション (ISSN:13444891)

巻号頁・発行日

vol.2, no.1, pp.28-33, 2000 (Released:2006-08-01)

参考文献数

7

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Two major problems are expected to arise in the future in connection with plasma proteins. The first problem is the lack of source materials. The second problem is the risk of transmission of viral disease such as hepatitis, HIV or other yet-to-be identified viruses. Genetic engineering is the best approach to solve these problems. Plasma derived human serum albumin (pHSA) is one of the most useful plasma proteins. However, producing recombinant human serum albumin (rHSA) commercially via genetic engineering is not entirely straightforward. Two hurdles must be cleared in order to develop rHSA. One is cost and the other is quality. Albumin is typically administered in tens of gram quantities. At a purity level of 99.999% (a level considered sufficient for other recombinant protein preparations such as vaccine and cytokine), rHSA impurities on the order of one mg will still be injected into patients. So impurities from the host organism, in this case yeast, must be reduced to a minimum. Furthermore, purified rHSA must be identical to pHSA. Despite these stringent requirements, cost must be kept in check. One gram of pHSA costs a few dollars. Our goal is to produce rHSA at least as economically as pHSA. Thus to rein in rHSA costs, maximum quantities of albumin must be produced from minimum volumes of culture, and highly efficient, high-yield purification methods are required. Because of these special issues about rHSA development, purification methods were designed under conception described below. 1. Easy automatic control, 2. Easy scale up, 3. Use of no special materials, 4. Use of no complicated methods. The item No.1 is necessary for cost cutting and uniformity of quality. The item No. 2 is essential by the reason mentioned below. In the first stage of rHSA development, we examined purification methods based on 3 to 10 l fermentation scale. In the next stage of rHSA development, we confirmed and optimized purification methods established at the first stage using 1000 l fermentation scale. The final stage of rHSA development is commercial scale. We have the plan of fermentation scale being 50 m3. The purification methods of rHSA must be identical throughout these three stages. Easy scale up is a very important factor for process development. Column chromatography is the best approach to solve these problems. So we used a lot of column chromatography techniques in rHSA purification. The items No.3 and No.4 are necessary for the reason mentioned below. Affinity chromatography is usually a very efficient method. But in the case of rHSA, affinity chromatography is not efficient considering cost and capacity. Furthermore, gradient elution is a very efficient method for small size chromatography, but in rHSA purification, chromatography column is very large. Gel packing into large columns is much more difficult than in small ones, and also, chromatography patterns in large columns are often different from those of small ones. In other words, though impurities can be separated in small scale, separation efficiency becomes very low in large scale and thus the results of chromatography is different between large and small scales. Because of the reasons mentioned above, the media used in our process are very popular ones such as ion exchange, hydrophobic and gel filtration. The methods of chromatography we used are very simple, i.e., rHSA is adsorbed on the media, impurities are washed out, and then rHSA is eluted at a stretch. Or contrariwise, rHSA is flowed through the media while the impurities are adsorbed. In this way, scale up of chromatography is very simple. Same bed height and same linear flow give same results independent of gel volume.

著者

鈴木 治 井上 幹夫

出版者

一般社団法人日本PDA製薬学会

雑誌

日本PDA学術誌 GMPとバリデーション (ISSN:13444891)

巻号頁・発行日

vol.2, no.1, pp.34-39, 2000 (Released:2006-08-01)

参考文献数

9

被引用文献数

1

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The previous study has shown that stainless steel surfaces on piping could greatly be subject to rouging during the operation of high-purity water systems (Suzuki O et al.: Pharm Tech 22: 66-82, 1998). The follow-up study has hereupon been carried on to fed out what will potentially develop into such rouging on stainless steel, because the fouling-like rouging has always been an anxious matter to pharmaceutical engineers. The name of rouging is now given to a corrosive discoloration developed with various contaminants in the high-purity water treatment process, which will also occur in WFI (Water for Injection) systems or pure steam generators. Stainless steel elbow-piping sections, which surfaces were finished at such a high mill finish as mechanical polish and electropolish, were exposed to pure steam generated at 2 kg/cm2-g. The steam was also fed into the near-horizontal piping section not stagnant with distillate and the intentionally arranged section stagnant with distillate for 30 days. The inner surface after pure steam fed was visually inspected and analyzed by a physical technique of Auger electron spectroscopy so that rouging discoloration was detected to be mostly due to its surface oxidization of stainless steel. The oxidization is divided into two groups: namely, (1) reddish discoloration results from the vapor attack, and (2) blackish discoloration comes from long contact with condensate on stainless steel surfaces. The latter discoloration is further divided into two types in the chemical respect; namely, with carbon and without carbon. Although these kinds of discoloration may provide no deterioration for water quality because of very low solubility of metal oxides, a further study of this rouging mechanism should be made to acquire clear grounds for the final conclusion.

著者

井田 民男

出版者

一般社団法人 日本燃焼学会

雑誌

日本燃焼学会誌 (ISSN:13471864)

巻号頁・発行日

vol.57, no.181, pp.214-221, 2015 (Released:2018-01-26)

参考文献数

7

被引用文献数

1

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Currently, various energies such as fossil fuels and nuclear power are considerable expenditures. Resource depletion and environmental issues are taking place by activation of various problems and economic activity due to population growth in developing countries. However, in order for society to develop, energy, such as natural energy, is required have been studied for this purpose. We are grappling with new solid bioenergy development named Biocoke. This Biocoke has new solid fuel characteristics with high density and high compressive strength. Firstly, this article reported on new bio-solid fuel which has different density and observed its combustion phenomenon. Through the observation of combustion for bio-solid fuel with different density from 0.8∼1.4 g/cm3, we quantitatively derived ignition limit of biosolid fuel about the difference of density. Thus, we confirmed time continuing the flame and char combustion and observed the situation of spread of combustion into the inside of solid fuel. Finally, Kinki University launched the Great East Japan Earthquake Reconstruction Support Office in August 2012. Its two main themes are of the reconstruction assistance "From Zero to Plus" and rehabilitation support from the disaster of "To Zero from Minus". We suggested that Biocoke is stabilized for a long time from various data. Especially, we was carried to the dissolution test into water from Biocoke including of adhere radioactive Cs-147. Emission of radioactive material from Biocoke reduced until 25%.

著者

横井 毅 山本 優衣 柴田 文佳 鈴木 美紀恵 島田 典招 若杉 隆伸 山木 光男 山守 育雄 中島 美紀 山崎 浩史

出版者

The Japanese Society for the Study of Xenobiotics

雑誌

薬物動態 (ISSN:09161139)

巻号頁・発行日

vol.15, no.supplement, pp.126-127, 2000 (Released:2007-03-29)

参考文献数

3

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Troglitazone, a new oral antidiabetic drug, has been reported to cause idiosyncratic hapatitis in certain individuals. The mechanism for hepatic failure was investigated with comparison between troglitazone and its metabolites and other thiazolidinedions. Oxidation pathway of troglitazone to a qunone-type metabolite was catalyzed mainly by CYP2C8 and CYP3A4 in human liver microsomes. Inhibitory effects of troglitazone and its metabolites on drug oxidation activities of human CYPs were not potent. Autoimmune antigen was identified in patients with idiosyncratic hepatitis. Hepatic toxicity did not appear in troglitazone treated rats after modifications of sulfotransferase, gluclonosyl-trasferase, or glutathione S-transferase activities. Treatment of HepG2 cell lines with troglitazone and a quinone type-metabolite showed time- and concentration-dependent cytotoxicity. Troglitazone induced apoptotic cell death in HepG2 cells. Taking these results into consideration, the causal factor(s) for idiosyncratic hepatitis in human remained unclear.

著者

横井 毅 山本 優衣 柴田 文佳 鈴木 美紀恵 島田 典招 山木 光男 若杉 隆伸 山守 育雄 中島 美紀 山崎 浩史

出版者

The Japanese Society for the Study of Xenobiotics

雑誌

薬物動態 (ISSN:09161139)

巻号頁・発行日

vol.16, no.2, pp.145-150, 2001 (Released:2007-03-29)

参考文献数

9

被引用文献数

1

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Troglitazone, a new oral antidiabetic drug, has been reported to cause idiosyncratic hepatitis in certain individuals. The mechanism for the hepatic failure was investigated with comparison between troglitazone and its metabolites and other thiazolidinediones, pioglitazone and rosiglitazone. Hepatic toxicity did not appear in rats in troglitazone-administered study after modifications of sulfotransferase and glucuronosyltrasferase activities and glutathione concentration. Oxidation pathway of troglitazone to a quinine-type metabolite was catalyzed mainly by CYP2C8 and CYP3A4 in human liver microsomes. Inhibitory effects of troglitazone and its metabolites on drug oxidation activities of human P450s would not be potent, based on its low blood concentrations and high protein binding ratio. An autoimmune antibody against aldolase B was identified in two patients with troglitazone-induced idiosyncratic hepatitis. However, this antibody was also detected in some other hepatic diseases, in spite of no cases in health control subjects. Treatment of HepG2 cell lines with troglitazone and a quinone type-metabolite showed time and concentration-dependent cytotoxicity. Troglitazone induced apoptotic cell death in HepG2 cells characterized by internucleosomal DNA fragmentation and nuclear condensation. Taking these results into consideration, the causal factor (s) for idiosyncratic hepatitis in human remained unclear.

巻号頁・発行日

vol.[89] 町人諸願之部, 1000

著者

谷野 忠嗣 青木 義広 吉田 達守 鷲見 裕 水田 泰一

出版者

一般社団法人日本PDA製薬学会

雑誌

日本PDA学術誌 GMPとバリデーション (ISSN:13444891)

巻号頁・発行日

vol.2, no.1, pp.19-27, 2000 (Released:2006-08-01)

参考文献数

8

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Fluidized-bed granulation has many operational parameters to be optimized in comparison with other simple wet granulation such as kneading or agitating. In addition, these parameters are not independent of each other: a change in one parameter often influences other parameters. Therefore, difficulties are sometime experienced with scale-up study of fluidized-bed granulation. It is a fact, however, that this granulation method has considerable merits to prepare highly compressible granules which can prevent capping incidents. It is experimentally known that tablets prepared by fluidized-bed granulation have usually higher hardness than those prepared by any other granulation methods. In this study, the authors discussed a scale-up and granule size control strategy on fluidized-bed granulation focusing on the moisture in granulation.