PHARMACOKINETIC STUDIES ON 1-(2-CHLOROETHYL)-3-ISOBUTYL-3-(β-MALTOSYL)-1-NITROSOUREA (TA-077). II. HYDROLYSIS BY TISSUE HOMOGENATES AND DRUG UPTAKE BY TUMOR CELLS IN VITRO
スポンサーリンク
概要
- 論文の詳細を見る
1-(2-Chloroethyl)-3-isobutyl-3-(β-maltosyl)-1-nitrosourea (TA-077) was hydrolyzed to its glucosyl metabolite TA-G by homogenates of guinea pig organs, rabbit VX-2 carcinoma and rat Yoshida sarcoma. The rate of TA-G formation by the kidney was the highest among the tissues examined and that by the diluted blood was undetectably low, reflecting their maltase activities. TA-077 was also hydrolyzed by suspensions of Yoshida sarcoma, AH130 hepatoma, L1210 leukemia, P388 leukemia and DBLA-10/C leukemia cells. The rate of TA-G formation was increased 10 fold by homogenizing the tumor cells. TA-G was taken up by the tumor cells much more efficiently than TA-077,explaining the higher sensitivities of the cultured tumor cells to TA-G than to TA-077. However, neither the maltase activity nor the membrane permeability to the drugs was a factor influential enough to explain the differences in drug sensitivity among the tumor cell lines.
- 公益社団法人日本薬学会の論文
著者
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TAKEYAMA Shigeyuki
Research Laboratories, Tanabe Seiyaku Co., Ltd.,
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HAYASHIDA KOHKICHI
Biological Research Laboratory, Tanabe Seiyaku Co., Ltd.
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ARAI YOSHIHISA
Biological Research Laboratory, Tanabe Seiyaku Co., Ltd.
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TAKEYAMA SHIGEYUKI
Biological Research Laboratory, Tanabe Seiyaku Co., Ltd.
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AKAIKE YUKIO
Biological Research Laboratory, Tanabe Seiyaku Co., Ltd.
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Akaike Y
Biological Research Laboratory Tanabe Seiyaku Co. Ltd.
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ODA KOHJI
Biological Research Laboratory, Tanabe Seiyaku Co., Ltd.
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Oda Kohji
Biological Research Laboratory Tanabe Seiyaku Co. Ltd.
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Hayashida Kohkichi
Biological Research Laboratory Tanabe Seiyaku Co. Ltd.
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TAKEYAMA Shigeyuki
Biological Research Laboratory and Organic Chemistry Research Laboratory, Tanabe Seiyaku Co., Ltd.
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