2 0 0 0 OA 泌乳の生化学
- 著者
- 榑谷 和男
- 出版者
- 公益社団法人 日本農芸化学会
- 雑誌
- 化学と生物 (ISSN:0453073X)
- 巻号頁・発行日
- vol.6, no.1, pp.2-9, 1968-01-25 (Released:2009-05-25)
- 参考文献数
- 43
- 著者
- 吉田 光二 星 昭夫 榑谷 和男 金井 貞 市野 元信
- 出版者
- The Japanese Cancer Association
- 雑誌
- GANN Japanese Journal of Cancer Research (ISSN:0016450X)
- 巻号頁・発行日
- vol.66, no.5, pp.561-564, 1975-10-31 (Released:2008-10-23)
- 参考文献数
- 12
Effect of substitution of 5-position of cyclocytidine with fluorine on its antitumor activity in cultured cells was examined. 5-Fluorocyclocytidine was active against cultured L-5178Y cells similar to cyclocytidine. IC50 of the compound was 0.054μg/ml. This compound inhibited thymidine incorporation into acid-insoluble fraction of the cells. Cell growth inhibition by 5-fluorocyclocytidine was reversed by deoxycytidine but not by thymidine and deoxyuridine. On the other hand, cell growth inhibition by 5-fluorouracil was reversed by thymidine and deoxyuridine. As a result, site of action of 5-fluorocyclocytidine was considered to be similar to that of cyclocytidine and not to 5-fluorouracil.
- 著者
- 星 昭夫 飯郷 正明 実吉 峯郎 榑谷 和男
- 出版者
- The Pharmaceutical Society of Japan
- 雑誌
- Chemical and Pharmaceutical Bulletin (ISSN:00092363)
- 巻号頁・発行日
- vol.21, no.7, pp.1535-1538, 1973-07-25 (Released:2008-03-31)
- 被引用文献数
- 4 4
Deamination of cytidine derivatives especially of cyclocytidine by mouse kidney cytidine deaminase was examined. Cyclocytidine was not deaminated at either pH6.5 or pH7.3 by the enzyme. Furthermore, cyclocytidine did not inhibit the deamination of aracytidine and ([I]/[S])0.5 value for cyclocytidine was over 100. As a result, cyclocytidine is found to be markedly active compound with resistance against cytidine deaminase.
- 著者
- 星 昭夫 官沢 文彦 飯郷 正明 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.66, no.5, pp.539-546, 1975-10-31 (Released:2008-10-23)
- 参考文献数
- 12
- 被引用文献数
- 2
Combination effect of antitumor agents, including cyclocytidine and cytosine arabinoside, was evaluated on the conception of pharmacological synergism and not of therapeutic synergism. Ascites sarcoma-180 and L-1210 leukemia were used as tumor systems. In sarcoma-180 system, combinations of cyclophosphamide plus cyclocytidine or cytosine arabinoside by simultaneous administration and cyclocytidine plus Daunorubicin or Vinblastine by alternate administration provided synergism. In L-1210 system, many compounds in combination with cyclocytidine or cytosine arabinoside in both simultaneous and alternate administrations provided synergism. Combination effect of agents was affected by the schedule of drug administration. It was found that the combination effect of drugs in one tumor system cannot be generalized to that in other tumor systems, even though equally effective doses of agents were administered in both tumor systems. Toxicity of cytosine arabinoside in combination with other drugs was affected by the schedule of administration. Compounds which provided synergism in simultaneous administration provided antagonism in alternate one. As a result, it was found that alternate administration of drugs is advantageous for the activity and diminution of toxicity to the host animal.
- 著者
- 星 昭夫 官沢 文彦 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.63, no.3, pp.353-360, 1972-06-30 (Released:2008-10-23)
- 参考文献数
- 12
- 被引用文献数
- 4
The antitumor activity of cyclocytidine was examined in a variety of tumors. Cyclocytidine was active against adenocarcinoma-755, Nakahara-Fukuoka sarcoma, ascites sarcoma-180, Ehrlich ascites carcinoma, L-1210 leukemia, and C-1498 leukemia. Cures (60-day survivors) were observed at 500mg/kg/day×5 or more of the compound in the L-1210 system and therapeutic ratio was as high as 50, though that of other known antitumor agents tested, including 1-β-D-arabinofuranosylcytosine (Ara-c), was less than 12. Therapeutic index of cyclocytidine in the solid and ascites tumors was always greater than that of Ara-c. Cumulative toxicity of cyclocytidine was surprisingly low and LD10 was 790mg/kg/day×5, whereas that of Ara-c was 82mg/kg/day×5. Cyclocytidine appears therefore to have advantages over Ara-c for clinical use.
- 著者
- 星 昭夫 官沢 文彦 榑谷 和男 実吉 峯郎 新井 祥子
- 出版者
- The Japanese Cancer Association
- 雑誌
- GANN Japanese Journal of Cancer Research (ISSN:0016450X)
- 巻号頁・発行日
- vol.62, no.2, pp.145-146, 1971-04-30 (Released:2008-10-23)
- 参考文献数
- 8
- 被引用文献数
- 4
2, 2'-O-Cyclocytidine was active against L-1210 leukemia. Cures were observed at the optimal dose of the compound, though no cures were obtained at any dose of any of the known antitumor agents. The compound was less toxic than 1-β-D-arabinofuranosyl-cytosine and resistant to cytidine deaminase.
- 著者
- 濱田 福三郎 杉原 太助 津山 伸吾 平山 八彦 金井 貞 西村 昌数 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.23, no.3, pp.586-591, 1975-03-25 (Released:2008-03-31)
- 被引用文献数
- 1 1
Newly synthesized 5-3H-cyclocytidine was injected intravenously in rhesus monkeys having a high level of cytidine deaminase which inactivates aracytidine, an antitumor substance analogous to cyclocytidine, in human plasma and tissues. After rapid distribution as intact molecule in the liver, kidney, spleen, and other organs, 46.5% of the administered radioactivity was excreted via the renal pathway within 160min. Metabolite analysis of 5-3H-cyclocytidine in plasma, tissues, and urine of the monkeys revealed that extensive or rapid degradation of cyclocytidine did not occur, and confirmed the resistance of cyclocytidine against the deaminase activity and its stability in biological condition in vivo. Phosphorylated derivatives of cyclocytidine were also detected in the monkey liver after injection.
- 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 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
- 星 昭夫 池川 哲郎 池田 善明 白川 貞雄 飯郷 正明 榑谷 和男 福岡 文子
- 出版者
- The Japanese Cancer Association
- 雑誌
- GANN Japanese Journal of Cancer Research (ISSN:0016450X)
- 巻号頁・発行日
- vol.67, no.2, pp.321-326, 1976-04-30 (Released:2008-10-23)
- 参考文献数
- 13
The antitumor activity of berberine, berberrubine, and their derivatives against sarcoma-180 ascites was determined by the total packed cell volume method. Berberine and tetrahydroberberine derivatives had no antitumor activity, but berberrubine (9-demethylberberine) and the ester derivatives of berberrubine had a strong antitumor activity. ED90 of berberrubine, its acetate and benzoate, were 15, 23, and 44mg/kg, respectively. The therapeutic indices (LD10/ED90 by the present method) of these compounds were as follows: Berberrubine hydrochloride, 6.7∼9.4; 9-acetyl-9-demethylberberine (9-acetylberberrubine) chloride, 7.6∼8.7; 9-benzoyl-9-demethylberberine (9-benzoylberberrubine) chloride, 3.4∼4.9.