Corticosterone Secretion-Inducing Activity of Saikosaponin Metabolites Formed in the Alimentary Tract

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概要

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• The corticosterone secretion-inducing activities of saikosaponin a, saikosaponin c and saikosaponin d, isolated from the root of Bupleurum falcatum L., and 27 metabolites formed in the murine alimentary tract were studied in mice. Serum corticosterone was determined by high-performance liquid chromatography (HPLC). Intraperitoneal administration of saikosaponin a and its intestinal metabolite, prosaikogenin F, showed corticosterone secretion-inducing activity at a dose of 0.1 mmol/kg, and maximally increased it at a does of 0.4 mmol/kg. On the other hand, the genuine sapogenin, saikogenin F, was inactive. Saikosaponin b_1 and saikosaponin g, gastric metabolites of saikosaponin a, and their intestinal metabolites, prosaikogenin A, prosaikogenin H, saikogenin A and saikogenin H, were also inactive. Serum corticosterone was increased by the administration of saikosaponin d and its intestinal metabolite, prosaikogenin G, at a dose of 0.04 mmol/kg, and it reached the maximal level at the dose of 0.1 mmol/kg. Saikogenin G also showed a slight activity. A gastric metabolite of saikosaponin d, saikosaponin b_2,and its intestinal metabolites, prosaikogenin D and saikogenin D, were inactive. In the experiments on saikosaponin c and its metabolites, saikosaponin c was inactive but its intestinal metabolites, especially prosaikogenin E-2,showed activity almost equal to that of saikosaponin a. Saikosaponin h and saikosaponin i, gastric metabolites of saikosaponin c, were also inactive, but their prosaikogenins showed slight activities. When these compounds were orally administered, their corticosterone secretion-inducing activities were similar to those obtained in the intraperitoneal experiment.These results suggest that a proper polar balance between the sugar moiety and the aglycone is important for the corticosterone secretion-inducing activity of saikosaponins and their metabolites.

• 公益社団法人日本薬学会の論文
• 1989-10-25

著者

• 能勢 充彦

  名城大学薬学部生薬学

• 能勢 充彦

  Department of Pharmacognosy, Faculty of Pharmaceutical Sciences, Nagoya City University

• 雨谷 栄

  Department of Pharmacognosy, Faculty of Pharmaceutical Sciences, Nagoya City University

• 萩原 幸夫

  Department of Pharmacognosy, Faculty of Pharmaceutical Sciences, Nagoya City University

• 萩原 幸夫

  Department Of Pharmacognosy Faculty Of Pharmaceutical Sciences Nagoya City University

関連論文

• Studies on the Constituents of Xanthoceras sorbifolia BUNGE. IV. Structures of the Minor Prosapogenins
• New Derivatives of Saikosaponins
• 証を念頭に置いた基礎研究の可能性を探る
• Corticosterone Secretion-Inducing Activity of Saikosaponin Metabolites Formed in the Alimentary Tract
• New Derivatives of Saikosaponin c
• Studies on the Constituents of Xanthoceras sorbifolia BUNGE. III. Minor Prosapogenins from the Fruits of Xanthoceras sorbifolia BUNGE
• 3. 遺伝子発現から見る漢方方剤の作用(証を念頭に置いた基礎研究の可能性を探る, 第56回日本東洋医学会学術総会)
• 遺伝子発現から見る漢方方剤の作用(シンポジウム1「証を念頭に置いた基礎研究の可能性を探る」, 第56回日本東洋医学会学術総会)

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