Regeneration Characteristics of Mitomycin C-Dextran Conjugate in Relation to Its Activity
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概要
- 論文の詳細を見る
The regeneration characteristics and biological activities of mitomycin C-dextran conjugate (MMC-D) were investigated in comparison with those of free mitomycin C (MMC), and the following results were obtained. (1) MMC is coupled at the 1a-nitrogen position via an amide linkage to a carboxyl group of ε-aminocaproic acid (6-aminohexanoic acid) which was introduced onto dextran as a spacer. (2) MMC-D was stabler than MMC against acid-catalyzed and metabolic degradation. (3) MMC was liberated from MMC-D with a half-life of about 24 h under physiological conditions (pH 7.4,37℃) and more rapidly at higher pH. (4) Liver homogenate did not accelerate the liberation of MMC from MMC-D. (5) Antimicrobial activity of MMC-D against Escherichia coli B was less than one-eighteenth of that of MMC. (6) MMC-D showed about one-tenth of the antitumor activity of MMC in vitro in contact with L1210 leukemia cells, but showed almost equal efficiency in the i. p.-i. p. system in vivo, suggesting that MMC-D exhibited activity after being regenerated to the parent drug in the body.
- 公益社団法人日本薬学会の論文
- 1983-06-25
著者
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瀬崎 仁
Faculty Of Pharmaceutical Sciences Kyoto University
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瀬崎 仁
京都大学
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高倉 喜信
京都大学大学院薬学研究科病態情報薬学分野
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村西 昌三
Department of Biopharmaceutics, Kyoto Pharmaceutical University
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松本 聡
京都大学 薬
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佐々木 均
Faculty Of Pharmaceutical Sciences Nagasaki University
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橋田 充
Faculty Of Pharmaceutical Sciences Kyoto University
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松本 聡
Faculty of Pharmaceutical Sciences, Kyoto University
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高倉 喜信
Faculty of Pharmaceutical Sciences, Kyoto University
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加藤 晃良
Faculty of Pharmaceutical Sciences, Kyoto University
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小嶋 拓己
Faculty of Pharmaceutical Sciences, Kyoto University
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村西 昌三
Kyoto College of Pharmacy
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村西 昌三
Department Of Biopharmaceutics Kyoto Pharmaceutical University
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小嶋 拓巳
Faculty Of Pharmaceutical Sciences Kyoto University
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加藤 晃良
Faculty Of Pharmaceutical Sciences Kyoto University
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