Preparation of Dextran T70-Methotrexate Conjugate and Dextran T70-Mycophenolic Acid Conjugate, and in Vitro Effect of Dextran T70-Methotrexate on Dihydrofolate Reductase
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概要
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Alkylenediamine-dextran T70(T70-C_n) might be useful as a polymer support for anti-tumor polymeric drugs, and its preparation was investigated. Decylenediamine-dixtran T70(T70-C_<10>) was selected as the most suitable compound. Methotrexate (MTX) or mycophenolic acid was conjugated through an amide bond involving the carboxyl group of the drug and the amino group of T70-C_<10>. Stability tests under the conjugation reaction conditions confirmed that T70-C_<10> could be utilized as a polymer support. The conjugation reaction with 1-ethyl-3-(3-dimethylamino-prophyl)carbodiimide hydrochloride as the reagent was satisfactory. The inhibition of dihydrofolate reductase by the conjugate of T70-C_<10> and MTX (T70-C_<10>-MTX) was checked in vitro.
- 社団法人日本薬学会の論文
- 1986-06-25
著者
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永井 恒司
Department of Pharmaceutics, Hoshi University
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永井 恒司
Research Center Taisho Pharmaceutical Co. Ltd.
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大西 啓
Faculty of Pharmaceutical Sciences, Hoshi University
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永井 恒司
Faculty of Pharmaceutical Sciences, Hoshi University
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大西 啓
星薬科大学 医療薬剤学教室
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