A comparison of the antihepatotoxic activity between glycyrrhizin and glycyrrhetinic acid.
1994
Nose M. | Ito M. | Kamimura K. | Shimizu M. | Ogihara Y.
A comparison of antihepatotoxic activities between glycyrrhizin (18beta-GL) and its genuine aglycone, glycyrrhetinic acid (18beta-GA), was carried out using in vivo and in vitro assay methods. The oral administration of 18beta-GA at 1, 24, and 48 hours before D-galactosamine (GalN) treatment significantly reduced the increase of serum transaminase activities 24 hours after GalN treatment, whereas 18beta-GL did not inhibit the increase of serum transaminase activities. The intraperitoneal administration of 18beta-GA 1 hour before GalN treatment restored the increase of serum transaminase activities with lower doses than 18beta-GL. In CC14-induced cytotoxicity of primary cultured rat hepatocytes, 18beta-GA protected the CC14-induced leakage of transaminase at doses of 5 to 50 micro gramm/ml, whereas 18beta-GL inhibited slightly the leakage at a dose of 1000 micro gramm/ml. In the same way, 18alpha-GA, the aisomer of 18beta-GA, reduced the CCl4-induced cytotoxicity more strongly than 18alpha-GL. Furthermore, the adsorbability of 18alpha,beta-GA on primary cultured rat hepatocytes was higher than that of 18alpha,beta-GL. These results suggest that 18alpha,beta-GA is a more potent antihepatotoxic agent than 18alpha,beta-GL, and that the potency of the antihepatotoxic compounds parallels their adsorbability in hepatocytes.
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