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<p>Glycyrrhetinic acid (GA) and glycyrrhizin (GL), active ingredients derived from Glycyrrhiza, <i>Glycyrrhizae Radix</i> (The Japanese Pharmacopia), exhibit various pharmacological effects, such as anti-inflammatory and anti-allergic activities, and a side effect of licorice-induced pseudoaldosteronism. GA is also produced as a metabolite of GL in gastrointestinal bacterial flora when Glycyrrhiza-containing Kampo medicines are orally administered. The present study aimed to confirm that a galacturonic-glycyrrhizin (gala-GL), an analog of GL contained in Glycyrrhiza, contributes to gastrointestinal GA production as well as GL. Gala-GL was hydrolyzed to GA by the intestinal flora, although the hydrolysis rate was slower than that of GL. This is the first report to reveal hydrolyzation of gala-GL into GA in the intestinal flora. The gala-GL content in the 16 Kampo extracts containing 1.0–4.0 g/daily dose of Glycyrrhiza and 8 commercially available Shakuyakukanzoto (SKT) products containing 2.0–4.8 g/daily dose of Glycyrrhiza were 2.2–9.5 and 2.9–7.2 mg/daily dose, respectively. The gala-GL contents corresponded to 7.3–10.9% and 8.0–9.4% of the total GL contents (sum of GL and gala-GL) for the Kampo extracts and SKT products, respectively. These results suggest that gala-GL also can be as sources of gastrointestinal GA, although the contents in Glycyrrhiza-containing Kampo medicines and the hydrolytic rate of conversion to GA in intestinal bacterial flora were much smaller than those of GL.</p> Graphical abstract <p></p>

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Quantitative determination of galacturonic-glycyrrhizin in Kampo medicines containing Glycyrrhiza: a glucuronide involved in gastrointestinal production of glycyrrhetinic acid

  • 期刊论文

  • 发表日期：

    2026年1月20日

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  • Shinji Miyoshi,
  • Kosuke Doki,
  • Yuji Mukai,
  • Momoka Tada,
  • Hikari Ota,
  • Mitsuhiko Nose,
  • Masato Homma

摘要

Glycyrrhetinic acid (GA) and glycyrrhizin (GL), active ingredients derived from Glycyrrhiza, Glycyrrhizae Radix (The Japanese Pharmacopia), exhibit various pharmacological effects, such as anti-inflammatory and anti-allergic activities, and a side effect of licorice-induced pseudoaldosteronism. GA is also produced as a metabolite of GL in gastrointestinal bacterial flora when Glycyrrhiza-containing Kampo medicines are orally administered. The present study aimed to confirm that a galacturonic-glycyrrhizin (gala-GL), an analog of GL contained in Glycyrrhiza, contributes to gastrointestinal GA production as well as GL. Gala-GL was hydrolyzed to GA by the intestinal flora, although the hydrolysis rate was slower than that of GL. This is the first report to reveal hydrolyzation of gala-GL into GA in the intestinal flora. The gala-GL content in the 16 Kampo extracts containing 1.0–4.0 g/daily dose of Glycyrrhiza and 8 commercially available Shakuyakukanzoto (SKT) products containing 2.0–4.8 g/daily dose of Glycyrrhiza were 2.2–9.5 and 2.9–7.2 mg/daily dose, respectively. The gala-GL contents corresponded to 7.3–10.9% and 8.0–9.4% of the total GL contents (sum of GL and gala-GL) for the Kampo extracts and SKT products, respectively. These results suggest that gala-GL also can be as sources of gastrointestinal GA, although the contents in Glycyrrhiza-containing Kampo medicines and the hydrolytic rate of conversion to GA in intestinal bacterial flora were much smaller than those of GL.

Graphical abstract