著者

川島 純 赤木 小野 加藤 下田 本郷

雑誌

東京医科大学病院看護研究集録

巻号頁・発行日

vol.21, pp.140-144, 2001-02

著者

河野 彬 原 泰寛 菅田 節朗 松島 美一 上田 亨

出版者

The Pharmaceutical Society of Japan

雑誌

Chemical and Pharmaceutical Bulletin (ISSN:00092363)

巻号頁・発行日

vol.32, no.5, pp.1919-1921, 1984-05-25 (Released:2008-03-31)

参考文献数

15

被引用文献数

12 16

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A thymidine phosphorylase preparation was partially purified from human liver tumor tissues (poorly differentiated adenocarcinoma). The substrate specificity of the enzyme was investigated with eleven pyrimidine nucleosides. Thymidine and 2'-deoxyuridine were good substrates, while uridine, 3'-deoxyuridine, 5'-deoxyuridine, and 2', 3'-dideoxy-3'-hydroxy-methyluridine were not. Uridines substituted at the 5-position by a cyano, bromo, or chloro group were also phosphorolyzed by the enzyme, but the activity for 5-fluorouridine was much lower. 5'-Deoxy-5-fluorouridine was also cleaved. Either a 5-substituent or a 2'-deoxy structure seems to be essential for a good substrate.

著者

逆翁, 宗順

出版者

西村吉兵衛

巻号頁・発行日

vol.[1], 1655

著者

河野 彬 原 泰寛 菅田 節朗 加留部 善晴 松島 美一 石塚 秀夫

出版者

The Pharmaceutical Society of Japan

雑誌

Chemical and Pharmaceutical Bulletin (ISSN:00092363)

巻号頁・発行日

vol.31, no.1, pp.175-178, 1983-01-25 (Released:2008-03-31)

参考文献数

20

被引用文献数

77 93

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Activities of pyrimidine nucleoside phosphorylases were assayed in extracts of human tumors, normal tissues of the same organs and tumors of mice (Sarcoma-180) and guinea pigs (Line-10), with thymidine (dThd), uridine (Urd), and 5'-deoxy-5-fluorouridine (5'-DFUR) as substrates. The nucleoside cleaving activities were higher in extracts of human tumor tissues than in those of normal tissues of the same organs. In human tissues, phosphorolytic activitiy towards dThd was high, while that towards Urd was low. In animal tumors, Urd was the best substrate. 1-(2'-Deoxy-β-D-glucopyranosyl)-thymine (GPT), a specific inhibitor of uridine phosphorylase, inhibited the phosphorolysis of Urd and 5'-DFUR in extracts of animal tumors, but not that of dThd and 5'-DFUR in extracts of human tumors. A thymidine phosphorylase preparation was partialy purified from human lung cancer. Km values of the preparation were 2.43×10-4 M and 1.69×10-3 M for dThd and 5'-DFUR, respectively. We conclude that in human tumors a thymidine phosphorylase activity converts 5'-DFUR to 5-fluorouracil, an activated form.

著者

菅田 節郎 河野 彬 原 泰寛 加留部 善晴 松島 美一

出版者

The Pharmaceutical Society of Japan

雑誌

Chemical and Pharmaceutical Bulletin (ISSN:00092363)

巻号頁・発行日

vol.34, no.3, pp.1219-1222, 1986-03-25 (Released:2008-03-31)

参考文献数

16

被引用文献数

5 11

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A thymidine phosphorylase (TP) preparation was partially purified from human gastric cancer (poorly differentiated adenocarcinoma). The specific activity of the final preparation represented a 379-fold purification of the 7000g supernatant of tissue homogenate. The phosphorolytic activities toward thymidine (dThd), 5'-deoxy-5-fluorouridine (5'-DFUR), and 1-(tetrahydro-2-furanyl)-5-fluorouracil (Tegafur) remained closely in parallel during the whole purification procedure. The results provide evidence in support of the assumption that 5'-DFUR and Tegafur are converted into 5-fluorouracil, an activated form of the antitumor agents, in humn tumor tissues by a TP activity. The values of Km of the TP preparation were 1.68×10-4, 1.72×10-3, 1.33×10-2, and 4.76×10-2M for dThd, 5'-DFUR, Tegafur, and uridine, respectively.

著者

明愼懋官撰

巻号頁・発行日

vol.[7], 1000

著者

伏木 亨

出版者

フレグランスジャーナル社

雑誌

Aromatopia (ISSN:09184295)

巻号頁・発行日

vol.19, no.5, pp.33-36, 2010

著者

井本 稔

出版者

社団法人日本化学会

雑誌

化学教育 (ISSN:03862151)

巻号頁・発行日

vol.24, no.3, 1976-06-20

著者

西村, 直方

出版者

写

巻号頁・発行日

vol.巻1,

著者

曽根高 真弓 山本 光俊

出版者

The Institute of Electrical Engineers of Japan

雑誌

電気学会誌 = The journal of the Institute of Electrical Engineers of Japan (ISSN:13405551)

巻号頁・発行日

vol.130, no.8, pp.532-533, 2010-08-01

参考文献数

3

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本記事に「抄録」はありません。

著者

井口 利仁 岩垣 博巳 浜中 荘平 モレイラ ルイス・フエルナンド 難波 浩 岡林 孝弘 日伝 晶夫 折田 薫三

出版者

岡山医学会

雑誌

岡山医学会雑誌 (ISSN:00301558)

巻号頁・発行日

vol.103, no.11, pp.1171-1176, 1991

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A case of recurrence of colon cancer with marked tumor reduction after effective chemotherapy is reported. The patient was a 27-years-old female who was admitted to the 1st department of surgery because of a giant abdominal tumor. She had undergone surgery for cecal cancer 16 months before admission. Abdominal and pelvic CT-SCAN revealed a giant tumor (21×18cm) invading the rectum and uterus. Surgical cannulation was performed into bilateral internal iliac arteries, and anti-cancer drugs (5-FU : 5000mg, ADR : 40mg, CDDP : 200mg) were administered intraarterially. The occurrence of hyperkalemia and striking rises in LDH, CEA, CA19-9 after the chemotherapy strongly suggested the tumor lysis syndrome, which to our knowledge, has not been reported as a complication of the treatment of colon carcinoma.

著者

山下 正文 橋本 隆寿 平川 俊彦 福島 武雄 朝長 正道 原 泰寛 河野 彬 田中 睦子

出版者

The Japan Neurosurgical Society

雑誌

Neurologia medico-chirurgica (ISSN:04708105)

巻号頁・発行日

vol.25, no.8, pp.613-619, 1985-08-15 (Released:2006-09-21)

参考文献数

17

被引用文献数

1 2

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To evaluate the usefulness of 5'-deoxy-5-fluorouridine (5'-DFUR) therapy for brain tumor, the pharmacokinetics of 5'-DFUR and 5-fluorouracil (5-FU) in the tumor, in the white matter surrounding the tumor and in the serum were investigated, and the thymidine phosphorylase, the main activating enzyme of 5'-DFUR in human tissues, was also studied. Materials were obtained from 24 cases of primary brain tumors and from 4 cases of metastatic carcinoma. During the operation 500 or 1, 000 mg of 5'-DFUR was administrated intravenously, and blood, tumor tissue and white matter were taken mainly within 60 minutes and partly within 180 minutes after intravenous administration of 5'-DFUR. In some cases samplings were performed serially. Concentrations of 5'-DFUR and 5-FU were measured by high performance liquid chromatography, and thymidine phosphorylase activity in tissue extracts was obtained against d-thymidine and/or 5'-DFUR as substrates. The concentrations of 5'-DFUR and 5-FU in serum decreased immediately in an exponential mode after intravenous administration of 1, 000 or 500 mg of 5'-DFUR. High concentrations of 5'-DFUR and 5-FU in the tumor tissues were noticed in malignant tumors, such as glioblastoma, ependymoma and chondrosarcoma, and 5-FU concentrations in the tumor in two cases of glioblastoma and one of ependymoma were higher than that in their sera. An important characteristic of 5'-DFUR was that it was converted to 5-FU in various tissues predominantly in malignant neoplasms. Thymidine phosphorylase activity was more prominent in glioblastoma, metastatic carcinoma and chordoma. Although the 5'-DFUR concentration in white matter was considerable, the 5-FU concentration was negligible suggesting low enzyme activity. An effect of 5'-DFUR therapy on malignant brain tumor should be expected from the high concentration of 5' DFUR and 5-FU in the tumor tissue. However, these high concentrations rapidly decreased, therefore, the appropriate mode of prescription of 5'-DFUR should be considered in clinical practice.

著者

下田 義男

出版者

The Medical Association of Nippon Medical School

雑誌

日本医科大学雑誌 (ISSN:00480444)

巻号頁・発行日

vol.5, no.2, pp.173-183, 1934

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以上私ハ強迫性神經症者ノ一治驗例ヲ擧ゲ,其ノ本態竝ビニ治癒機制ニ就テ若干ノ分析考察ヲ加ヘテ見タ。今茲ニソノ要點ヲ再摘シテ見ルト,<BR>1. 本例患者ハ12歳癩病恐怖ヲ主徴候トシテ發病,爾來8年間症状ハ漸次増惡遂ニ現實的生活ノ積極的部分ヲモ犠牲トスルニ至ツタ強迫觀念症患者デアルガ,治療開始以來20日餘デ治癒ノ域ニ達シタモノデアル。<BR>1. 強迫神經症ノ本態ハ一定ノ基調的性格ニ何等カノ外部的原因ノ加ツタモノト認メラレル。<BR>1. 本症ノ基調的性格トシテハ,先ヅ性格ノ概念ヲ人ノ組織生物學的根據ノ上ニ立ツ氣質ニ後天的諸條件ノ影響シテ構成セラレルモノトスルト,本例患者ノ性格ヲ分析的ニ考察シタ結果ニ依レバ,クレツチユメルノ乖離性氣質ニ見ラレル「自己内生活」的傾向ト偏執病者ノ有スル偏執的傾向ニ精神幼稚性ノ加ツタモノトシテ説明スルコトガ可能デアル。カカル性格ハ理論的ニハ本症ノ基調的性格トシテ適切デハアルガ,他ニモ普遍的實在的デアル事ヲ證スルタメニハ更ニ多數例ノ觀察ニ俟ツノヲ妥當トスル。<BR>1. 本症ノ發生機制ニ就テハ,探索ヲ意識範圍ニ限局スル場合殆ンド説明不可能デアル。精神分析派ノ説明ニハ聽クベキ所多イト考ヘラレルガ未グ終極的結論ハ此方面カラモ得ラレナイ<BR>1. 本症ノ治癒機制ハ「矛盾」ノ體驗的認識ガ性格構成ノ後天的部分ニ或ル修正ヲ齎ラシ,之レガ強靱ナ意志ト俟ツテ症状ノ解消ヲ來スモノト考ヘラル。故ニ本症ニ在ツテハ治癒ハ基調性格ヲ遺シテノ症状ノ消失デアリ。此ノ意味ニ於テ比較治癒ナル語ガ適當デアルト考ヘラレル。擱筆ニ當リ御校閲下サツタ齋藤玉男先生,御鞭韃下サツタ長澤米藏先生及ビ種々御配慮下サツタ森崎院長,杉尾副院長ニ深甚ノ感謝ノ意ヲ表スルモノデアル。

著者

菅田 節朗

出版者

九州大学

巻号頁・発行日

1978

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博士論文

著者

IKUO ADACHI TERUO YAMAMORI YOSHIHARU HIRAMATSU KATSUNORI SAKAI SHIN-ICHI MIHARA MASARU KAWAKAMI MASAO MASUI OSAMU UNO MOTOHIKO UEDA

出版者

The Pharmaceutical Society of Japan

雑誌

Chemical and Pharmaceutical Bulletin (ISSN:00092363)

巻号頁・発行日

vol.36, no.11, pp.4389-4402, 1988-11-25 (Released:2011-02-08)

参考文献数

19

被引用文献数

31 49

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A series of 4-aryl-4, 7-dihydrothieno [2, 3-b] pyridine-5-carboxylate derivatives (I) was synthesized and tested for binding affinity to Ca2+ channels in rat cerebral cortex membranes, coronary vasodilator effect in isolated guinea pig hearts, and antihypertensive activity in spontaneously hypertensive rats.Several compounds had potent coronary vasodilator and antihypertensive activities.The structure-ctivity relationships of the series indicated that a lipophilic 3-alkyl substituent with moderate bulkiness was effective for enhancing the pharmacological potencies.Among them, methyl 4, 7-dihydro-3-isobuty1-6-methy1-4-(3-nitrophenyl) thieno [2, 3-b] pyridine-5-carboxylate (S-312) was selected as a promising cardiovascular agent.The relationship between the absolute configuration of S-312 and its biological activities is also presented.

著者

足達 郁夫

出版者

九州大学

巻号頁・発行日

1969

---

博士論文

著者

宋鄭樵撰

出版者

謝氏彷武英殿本刊

巻号頁・発行日

vol.[62], 1859

著者

加納 日出夫 足達 郁夫

出版者

The Pharmaceutical Society of Japan

雑誌

Chemical and Pharmaceutical Bulletin (ISSN:00092363)

巻号頁・発行日

vol.16, no.1, pp.117-125, 1968-01-25 (Released:2008-03-31)

被引用文献数

6 12

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Nine bicyclic isoxazolines (IVa-g and Va-b) were prepared by 1, 3-dipolar cycloaddition of nitrile oxides to the following heterocyclic olefins : 2, 3-and 2, 5-dihydrofurans, 5-methyl-2, 3-dihydrofuran, 2, 3-dihydropyran, and N-acetyl-2-piperidein. Acid-catalized cleavage of IVa-d gave the corresponding 4-substituted 3-phenylisoxazoles (VIa-c and IIIg). Nine 4-aminoalkyl-3-phenylisoxazoles (IIIa-i) were prepared for pharmacological testings in comparison with those of 3- and 5-aminoalkyl analogs (I and II). Base-catalized cleavage of the adducts (IVa-c and Va) was also investigated and in some cases the lactones (XIIa and XIIb) were obtained besides the isoxazoles (VIa and VIb). In this connection the Hofmann reactions of the bicyclic isoxazoline-3-carbon-amides (IVe'and IVf') were studied.

著者

足達 郁夫 加納 日出夫

出版者

The Pharmaceutical Society of Japan

雑誌

Chemical and Pharmaceutical Bulletin (ISSN:00092363)

巻号頁・発行日

vol.17, no.11, pp.2201-2208, 1969-11-25 (Released:2008-03-31)

被引用文献数

5 12

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Ring opening reactions with some bases were examined in the following quaternary salts : 2-ethyl-3, 4-diphenylisoxazolium chloroferrate (V), and 2, 4-dimethyl-3-phenyl-, 3, 4-diphenyl-2-methyl- and 2-methyl-3-phenylisoxazolium perchlorate (IXa, b and c). Treatments of V and IX with sodium alcoholate in alcohol gave the corresponding alkyl cinnamates (VIIa-e). By the use of aqueous sodium hydroxide, V and IXb gave the respective cinnamic anhydrides (Xa and b) contrary to the report of Kohler, et al., and IXa gave an unexpected product, 2, 5-diphenyl-1, 3, 4-trimethylpyrrole (XIa) along with usual ring cleaved products, XIIa and XIIIa. Reactions of IXa, b with several amines gave β-keto acid amides (XIIc-h), the ketones (XIIIa, b) and the pyrrole (XIa) (only from IXa), respectively. Reactions of IXa with Grignard reagents gave 5-substituted △3-isoxazolines (XIVa, b). Similar 5-amino-△3-isoxazolines (XVa-c) were obtained by cautious treatment of IXa, b with piperidine or morpholine. Solvolysis of X, XIV and XV were also investigated, and a tentative mechanism for the formation of the various products are presented.

著者

足達 郁夫 宮崎 理慧 加納 日出夫

出版者

The Pharmaceutical Society of Japan

雑誌

Chemical and Pharmaceutical Bulletin (ISSN:00092363)

巻号頁・発行日

vol.22, no.1, pp.70-77, 1974-01-25 (Released:2008-03-31)

被引用文献数

16 29

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Synthesis and thermal-reaction of 4-isoxazolines were investigated. Reaction of 3-unsubstituted isoxazolium salts with sodium borohydride yielded the corresponding 4-isoxazolines and their borane complexes together with β-hydroxyaminopropiophenone derivatives. Analogous reaction of 5-unsubstituted isoxazolium salt yielded two isomeric products, 4- and 3-isoxazoline derivatives. The 3-isoxazoline derivative underwent further reduction to give isoxazolidine derivatives. Thermal-conversion of some 4-isoxazolines and their borane complexes into 2-acylaziridine derivatives is also reported.