著者

菅田 節朗 山之内 正子 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.25, no.5, pp.884-889, 1977-05-25 (Released:2008-03-31)

被引用文献数

20 30

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Three isomers of meso-tetrapyridylporphins, i. e. tetra (2-pyridyl)-(2), (3-pyridyl)-(3), and (4-pyridyl)-(4), porphin have been synthesized. They were soluble in acetic acid, chloroform and acidic aqueous solvents. Solubilities in chloroform, dimethylformamide and pyridine were in the order 3>2>4. Comparison of the visible spectra indicated that the intensities of the bands due to 0-0 transitions decreased (3>4>2) with an increase of the electron-withdrawing character of the pyridyl substituent. The copper (II) and zinc (II) complexes of 2 and 3 have been prepared. Infrared and nuclear magnetic resonance spectra and their assignments of the porphins and/or the metal complexes were described.

著者

河野 彬 菅田 節朗 原 泰寛 田中 睦子 加留部 喜晴 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.31, no.5, pp.1666-1669, 1983-05-25 (Released:2008-03-31)

参考文献数

19

被引用文献数

2

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A sensitive method for the assay of pyrimidine nucleoside phosphorylases in preparations of human and animal tissues by determination of pyrimidines is described. Pyrimidines formed enzymatically from thymidine, uridine, 5-fluorouridine, and 5'-deoxy-5-fluorouridine are determined by means of high-performance liquid chromatography with ultraviolet (UV) detection. The pyrimidines, after extraction with ethyl acetate, are separated by reversed-phase chromatography on μ-Bondapak C-18/Porasil. The limits of detection are 2.5, 1.0, and 2.0 pmol for thymine, uracil, and 5-fluorouracil, respectively.

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

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.