著者
川口 健夫 鈴木 嘉樹 中原 葉子 南部 直樹 永井 恒司
出版者
The Pharmaceutical Society of Japan
雑誌
Chemical and Pharmaceutical Bulletin (ISSN:00092363)
巻号頁・発行日
vol.33, no.1, pp.301-307, 1985-01-25 (Released:2008-03-31)
参考文献数
17
被引用文献数
13 16

The activity of porcine liver esterase towards diesters of 5-fluoro-2'-deoxyuridine with saturated aliphatic acids including acetic, propionic, butyric, hexanoic, octanoic, decanoic and dodecanoic acids was investigated. The susceptibility of the 3', 5'-diesters increased as the acyl chain was lengthened up to octanoyl, but further increase in the acyl chain length resulted in a sharp decrease in the susceptibility. The susceptibility of 3'-and 5'-monoesters increased as the chain was lengthened to decanoyl and slightly decreased on going to dodecanoyl. These results suggest that the higher antitumor activity of longer alkyl chain diesters of 5-fluoro-2'-deoxyuridine is partly due to their slow rates of hydrolysis by non-specific esterase.

1 0 0 0 OA 諸家短冊帖

出版者
巻号頁・発行日
vol.波雄(至清堂)・義昌(阿久沢)・真文(棗栗園)・小松(千証庵)・玉世(桑樹園)・千守,
著者
川口 健夫 斉藤 政彦 鈴木 嘉樹 南部 直樹 永井 恒司
出版者
The Pharmaceutical Society of Japan
雑誌
Chemical and Pharmaceutical Bulletin (ISSN:00092363)
巻号頁・発行日
vol.33, no.4, pp.1652-1659, 1985-04-25 (Released:2008-03-31)
参考文献数
18
被引用文献数
21 24

The bioactivation characteristics of 3', 5'-diesters of 5-fluoro-2'-deoxyuridine (FUdR) esterified with saturated aliphatic acids, including acetic, propionic, butyric, hexanoic, octanoic, decanoic, dodecanoic and trimethylacetic acids, were studied by using rat tissue homogenates and plasma. The susceptibility of the esters to hydrolysis by the biological media increased as the acyl promoiety was lengthened up to octanoyl. Further elongation resulted in decreasing susceptibility. Antitumor activity against L1210 of the esters with a longer chain or branched acyl group administered intraperitoneally and orally to tumor-bearing mice was also examined. Both the antitumor activity and the therapeutic index (ILSmax/ILS30) of the esters improved as the acyl promoiety was lengthened from octanoyl to dodecanoyl. These results suggested that the higher antitumor activities of longer alkyl chain diesters of FUdR are due to their slow rates of FUdR regeneration with esterases.
著者
実吉 峯郎 両角 正海 小玉 健次郎 町田 治彦 国中 明 吉野 宏
出版者
The Pharmaceutical Society of Japan
雑誌
Chemical and Pharmaceutical Bulletin (ISSN:00092363)
巻号頁・発行日
vol.28, no.10, pp.2915-2923, 1980-10-25 (Released:2008-03-31)
参考文献数
24
被引用文献数
16 26

Enzymatic selective dephosphorylation of 1-β-D-arabinofuranosylcytosine 3', 5'-diphosphate (1) with nuclease-3'-nucleotidase P1 at 60° for 24 hr gave 1-β-D-arabinofuranosylcytosine 5'-phosphate (Ara CMP) (2) in good yield. The acylation of both N4- and the 2', 3'-hydroxyl groups of 2 followed by coupling with various alcohols and phenols in the presence of 2, 4, 6-triisopropylbenzenesulfonyl chloride and subsequent alkaline hydrolysis afforded the title compounds (4). The resulting 32 kinds of Ara CMP alkyl or aryl esters were examined to determine their biological activities, such as antiviral activity against herpes simplex type 1 in cultured human embryonic lung fibroblast cells, growth inhibitory activity against mouse leukemic L5178Y cells in culture and antileukemic activity against L-1210 in mice. Ara CMP esters were active in these assay systems.
著者
平賀 慎 杉田 洋 村川 三郎 近藤 貴道
出版者
日本建築学会
雑誌
日本建築学会計画系論文集 (ISSN:13404210)
巻号頁・発行日
vol.72, no.616, pp.153-158, 2007-06-30 (Released:2017-02-25)
参考文献数
12
被引用文献数
2 1

This paper proposes the cleanliness check system which is constructed by the evaluation of students for the purpose of efficient cleaning management. This system was applied to a certain university as a case study. First the viewpoints and judgment conditions on which the cleanliness of campus were evaluated were extracted by the hearing investigations to the students. Then, some items for the cleanliness check were decided based on these results. Furthermore, importance level to the check items and user satisfaction to the current conditions were investigated. As a result, the necessary knowledge to improve concretely the cleaning management was obtained.
著者
FUMIHIKO KANZAWA YUKA MATSUSHIMA JUNICHI ISHIHARA AKIO HOSHI TAKEO OHBA KENZO WATANABE
出版者
The Pharmaceutical Society of Japan
雑誌
Journal of Pharmacobio-Dynamics (ISSN:0386846X)
巻号頁・発行日
vol.9, no.8, pp.688-693, 1986 (Released:2008-02-19)
参考文献数
16
被引用文献数
5 5

A series of twenty six 5'-substituted FdUMP (5-fluoro-2'-deoxyuridine 5'-monophosphate) have been evaluated for their inhibitory effects on the proliferation of murine lymphoma L5178Y cells sensitive or resistant to FUdR (5-fluoro-2'-deoxyuridine). 5'-Octylphenylene-FdUMP was the most active among these active derivatives against the parent cell line (L5178Y/P). Several other FdUMP derivatives also proved as potent as FUdR in their antiproliferating activity on the L5178Y/P cell line. Activity of these derivatives was decresed considerably by a substituent with a long aliphatic chain and the introduction of acyl groups on the C-3' position. Eicosyl-FdUMP was found to show no or low cross-resistance on the L5178Y/FUdR subline which was about 19000-fold resistant to FUdR compared with the parent cell line. This derivative might penetrate cell membrane in an intact form and be converted into FdUMP by a phosphodiesterase inside the cell, because an anabolic enzyme, deoxyuridine kinase, was defective in cells of the L5178Y/FUdR subline. The derivatives were promising as antitumor agents for the treatment of relapsed patients following 5-fluorouracil therapy.
著者
官沢 文彦 星 昭夫 榑谷 和男
出版者
The Japanese Cancer Association
雑誌
GANN Japanese Journal of Cancer Research (ISSN:0016450X)
巻号頁・発行日
vol.65, no.1, pp.55-60, 1974-02-28 (Released:2008-10-23)
参考文献数
22
被引用文献数
3

Interaction of antitumor agents in activity and in toxicity was examined separately. Ascites sarcoma-180 and ddN mice were used as the tumor system.Interaction was evaluated on the concept of pharmacological synergism and not of therapeutic synergism. In activity, 18 out of 91 combinations provided synergism and most of them contained alkylating agents and antibiotics. Antitumor agents were therefore classified into two groups from the point of drug interaction. Synergism was observed in combinations of agents in Group I, alkylating agents, antibiotics, and alkaloids. In combination of agents in Group II (antimetabolites and others), additive action was observed. As a result, 18, 65, and 8 combinations provided synergism, additive action, and antagonism, respectively.On the other hand, in toxicity, 13, 27, and 38 out of 78 combinations provided synergism, additive action, and antagonism, respectively. The combination that provided synergism in activity and antagonism in toxicity were 8 out of 91 combinations tested. In general, fortunately, combinations of antitumor agents were more than additive in activity and less than additive in toxicity.
著者
吉田 光二 星 昭夫 / 実吉 峯郎 MINEO SANEYOSHI
出版者
The Pharmaceutical Society of Japan
雑誌
Chemical and Pharmaceutical Bulletin (ISSN:00092363)
巻号頁・発行日
vol.30, no.3, pp.1018-1023, 1982-03-25 (Released:2008-03-31)
参考文献数
23
被引用文献数
4 6

The mode of antiproliferative action of two 5-fluorocytosine nucleosides, 5-fluoro-cytidine (FCR) and 5-fluoro-2'-deoxycytidine (FCdR), was examined using mouse leukemia L5178Y cells in vitro. FCR and FCdR were markedly active against L5178Y cells, though the cells were deficient in cytidine deaminase activity. Both compounds increased the incorporation of 14C-labeled thymidine into the acid-insoluble fraction of L5178Y cells and decreased labeled deoxycytidine incorporation. In reversal studies, the antiproliferative effects of both compounds were almost abolished by simultaneous addition of thymidine or deoxyuridine. Deoxycytidine completely reversed the growth inhibition caused by FCdR, but not that caused by FCR. These results demonstrate that the cytotoxicity of both compounds is due to inhibition of thymidylate synthetase, presumably through formation of 5-fluoro-2'-deoxyuridine monophosphate (FdUMP) after deamination by deoxycytidylate deaminase in the pyrimidine de novo pathway.
著者
小松原 千里
出版者
神戸大学近代発行会
雑誌
近代 (ISSN:02872315)
巻号頁・発行日
no.70, pp.p119-136, 1991-06
著者
太田 達也
出版者
慶應義塾大学法学研究会
雑誌
法学研究 (ISSN:03890538)
巻号頁・発行日
vol.70, no.9, pp.85-122, 1997-09

資料はじめに受刑者の平均収容人員新受刑者女子受刑者死刑確定者社会化教育少年未決拘禁者再入者率仮出獄・釈放前帰休レミッション端正施設における事故保護観察対象者矯正施設の数矯正施設の収容定員と収容状況矯正施設における設備矯正施設の職員おわりに
著者
音藤 実雄
出版者
一般社団法人 資源・素材学会
雑誌
日本鉱業会誌 (ISSN:03694194)
巻号頁・発行日
vol.77, no.878, pp.546-560, 1961-08-25 (Released:2011-07-13)
参考文献数
17

Our Sorachi Mine situated in the northern part of the Ishikari Coal-Field in Hokkaido was opened for mining in 1890. Since then, we applied many systems of mine opening...such as drift from outcrop, the gallery entry, the shallow shaft, the steep shaft, and the incline method, Up to 1957, both three inclines let out only 800-900 tons per day, and then the coal reserves available, had only three years in a life of exploitation.The output production plan was decided in the maximan of 1600tons per day withoutincreasing the capacity of the washing plant and the National Railway. Due to the housing and water ways problems, it was impossible to increase the number of workers.In order to double the output total, it was either to increase the output per man shift at the face. cut (1), or decrease the number of indirect workers and transfer them to the face cut (2). In these two ways, the latter was decided by the reason that geological conditions were too complex and difficult to adapt the first way.Then a plan with a capital investment of 1600 millions yens was carried out. A speedy opening by a new field was struggled by means of:(1) Reconstruction of mine structure (Horizontal mining system)(2) Adoption of permanent spports(3) Synchronized rationalization of transportation (by automation and remote control)(4) As well as modernization and intensification of pitmouth equipment installations In three years time, from May 15, 1957 to. May 13, 1960 and with 390, 000 workers, the construction works were completed according to a plans.As a result, the output per day was increased from 839 tons average in 1959 to 1154 tons in January 1961, just 8 months after the completion. And the output per man-month was increased from 18.4 tons to 28.6 tons.And the man-powers per 100 tons of output in the face working was reduced to 38. 0 M. S, . in the indirect working 23.9 M.S.and in the under ground working 61.9 M. S. after all. While, the man-powers in the surface working was reduced to 17.4 M. S. These productivities of labour are already near the levels in the Wester Europe.
著者
池上 良正
出版者
日本宗教学会
雑誌
宗教研究 (ISSN:03873293)
巻号頁・発行日
vol.86, no.2, pp.193-217, 2012-09-30 (Released:2017-07-14)

日本語の「無縁供養」は、系譜上の祀り手を失った死者のほか、戦乱・事故・自然災害などの災禍によって非業の死をとげたと見なされた人々を追弔・慰撫する言葉として用いられている。広くは「苦しむ死者」を救済する代表的な言葉である。「死者供養」を東アジアで形成され民衆層に普及した、ユニークで動態的なひとつの「救済システム」として捉えるとき、そこには、(A)親孝行や先祖の孝養という側面と、(B)何らかの未練や怨念を残した死者(苦しむ死者)たちの救済という側面の二面性を指摘できるが、「無縁供養」に代表される(B)の「苦しむ死者の救済」は、このシステム全体を存続させる原動力を供給し続けてきたことが注目される。本稿ではこの「無縁供養」の構造と展開過程を考察する。そこに潜在していた「無遮」と「無主」との有機的な動態性は、救済システムとしての「死者供養」が広く民衆層に定着するさいの原動力になっていた、という見通しを示す。

1 0 0 0 OA 宮藁雑記

出版者
巻号頁・発行日
vol.[3],
著者
吉田 光二 榑谷 和男 星 昭夫
出版者
The Pharmaceutical Society of Japan
雑誌
Chemical and Pharmaceutical Bulletin (ISSN:00092363)
巻号頁・発行日
vol.26, no.2, pp.429-434, 1978-02-25 (Released:2008-03-31)
被引用文献数
2 3

5-Fluorouridine and 1-β-D-arabinofuranosylcytosine are active against various tumors as antimetabolites. Antitumor activity and mode of action of their nucleotides, 5-fluorouridine 5'-phosphate and 1-β-D-arabinofuranosylcytosine 5'-phosphate, were examined. 5-Fluorouridine 5'-phosphate was active similar to the nucleoside against L1210 leukemia, but the nucleotide showed higher therapeutic ratio than 5-fluorouracil and 5-fluorouridine. The mode of action of these nucleotides was examined by the incorporation of labeled precursors into acid-insoluble fraction of the cells for 30 min. Inhibition patterns of these nucleotides were the same as those of the nucleosides, but the potency of the nucleotides was very weak, and increased with time. Analysis showed that these nucleotides were dephosphorylated on the cell surface and the dephosphorylation was greater than that of phenolphthalein monophosphate. 5-Fluorouridine 5'-phosphate was considered to be a good candidate for an antitumor agent.
著者
佐藤 陽一
出版者
日本経営倫理学会
雑誌
日本経営倫理学会誌 (ISSN:13436627)
巻号頁・発行日
vol.8, pp.51-62, 2001-03-31 (Released:2017-07-28)

Since the Ikeda cabinet revived the current decoration system in 1963, many businessmen have been decorated. Nowadays, because of the increased tenacity of acquiring a decoration,senior executives pursue a higher position and stay there for a longer period.Aging and moral hazards have become conspicuous phenomena among them. If the current deplorable system is abolished,if aged leaders change their interest into a service to the public utilizing their insight and expertise, and if the younger generation demonstrate their ability as new leaders, then we can expect a vital ethical 21st century.