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Biotransformation of glycyrrhizin by human intestinal bacteria and its relation to biological activities

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  • Pharmacology, Toxicology & Pharmaceutics
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Abstract

The relationship between the metabolites of glycyrrhizin (18β-glycyrrhetinic acid-3-O-β-d-glucuronopyranosyl-(1→2)-β-d-glucuronide, GL) and their biological activities was investigated. By human intestinal microflora, GL was metabolized to 18β-glycyrrhetinic acid (GA) as a main product and to 18β-glycyrrhetinic acid-3-O-β-d-glucuronide (GAMG) as a minor product. The former reaction was catalyzed byEubacterium L-8 and the latter was byStreptococcus LJ-22. Among GL and its metabolites, GA and GAMG had more potentin vitro anti-platelet aggregation activity than GL. GA also showed the most potent cytotoxicity against tumor cell lines and the potent inhibitory activity on rotavirus infection as well as growth ofHelicobacter pylori. GAMG, the minor metabolite of GL, was the sweetest.

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Correspondence to Dong-Hyun Kim.

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Kim, DH., Hong, SW., Kim, BT. et al. Biotransformation of glycyrrhizin by human intestinal bacteria and its relation to biological activities. Arch Pharm Res 23, 172–177 (2000). https://doi.org/10.1007/BF02975509

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