Effect of Glycyrrhetic Acid Derivatives on Regulation of Thymocyte Volume

We studied the effects of glycyrrhetinic acid (bioactive aglycone of glycyrrhizin) and its ester derivatives at positions C-3 and C-30 on the cell volume regulation in rat thymocytes under conditions of hypoosmotic stress. Native glycyrrhetinic acid completely suppressed this process with half-maximal concentration of 12.7±1.4 μM and Hill coefficient of 3.1±0.6. Formation of esters at C-3 (esters with the acetic, cinnamic and methoxi-cinnamic acid) and at C-30 (methyl ester) drastically decreased the inhibitory activity of the molecule, suggesting that intact hydroxyl group at C-3 and carboxyl group at C-30 are structurally important determinants of biological activity of glycyrrhetinic acid towards volume regulation of thymic lymphocytes.