シイタケ成分Eritadenine誘導体のコレステロール低下作用
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概要
- 論文の詳細を見る
Various kind of compounds related to the hypocholesteremic alkaloid, eritadenine, an active component of Japanese mushroom, Lentinus edodes SING, (Japanese name, Shiituke) were studied concerning structure-activity relationship. Compounds were administered orally to cholesterol-fed rats for 3 days. It may be concluded from the results as follows : 1) Eritadenine esters were found to be 10 times as active as the mother substance in serum cholesterol-lowering activity. 2) Among the 6-substituted analogs, hydroxyamino compound was found to possess a high biological activity, equivalent to that of eritadenine. Thus, basic substituents at the 6-position of the purine ring may be essential for the activity, as evidenced by the loss of activity of the 6-hydroxy, 6-mercapto, 6-chloro, and hydrogen compounds. 3) Dihydroxybutyric acid derivatives, having pyrimidine or other heterocyclic ring, were found to be inactive or less active than eritadenine. From these facts, it seems that presence of a purine ring in the structure is important for cholesterol-lowering activity. 4) Hypocholesteremic effect of eritadenine and its stereoisomers decreased in the following order : D-erythro (natural eritadenine), D-threo, L-erythro, L-threo (no effect). β-Deoxyeritadenine showed a moderate cholesterol-lowering activity, whereas α-deoxyeritadenine was ineffective. These results suggest that dihydroxybutyric acid is required for the potent hypocholesteremic activity, and especially, α-OH group is associated with the activity.
- 公益社団法人日本薬学会の論文
- 1974-06-25
著者
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竹縄 忠臣
藤沢薬品工業株式会社小金井分室
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清水 巌
Tokyo Research Laboratories Fujisawa Pharmaceutical Co. Ltd.
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菊地 博之
藤沢薬品工業株式会社小金井分室
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天正 明
藤沢薬品工業株式会社小金井分室
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清水 巖
藤沢薬品工業株式会社小金井分室
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六城 雅彙
藤沢薬品工業株式会社小金井分室
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紙谷 孝
藤沢薬品工業株式会社中央研究所
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紙谷 孝
藤沢薬品工業(株)生産技術研究所
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菊地 博之
藤沢薬品工業(株)中央研究所
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紙谷 孝
藤沢薬品工業 (株) 中央研究所
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