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  • Title: Inhibition of rat liver cytosolic glutathione S-transferase by silybin.
    Author: Bartholomaeus AR, Bolton R, Ahokas JT.
    Journal: Xenobiotica; 1994 Jan; 24(1):17-24. PubMed ID: 8165818.
    Abstract:
    1. The naturally occurring hepatoprotective compound silybin is a potent inhibitor of glutathione S-transferase isoenzymes 1-1, 2-2, 3-3, and 4-4, displaying a high degree of isoenzyme selectivity. 2. Using CDNB at a fixed concentration of 1 mM and varying the GSH concentration, silybin exhibited competitive inhibition of isoenzyme 2-2 with a Ki of 32 microM, non-competitive and predominantly non-competitive inhibition of isoenzymes 1-1 and 4-4 with Kis of 20 and 1.2 microM, respectively, and uncompetitive inhibition of isoenzyme 3-3 with a Ki of 0.2 microM. 3. With CDNB as the variable concentration substrate silybin exhibited competitive inhibition of isoenzyme 1-1 with a Ki of 8 microM, non-competitive inhibition of isoenzyme 2-2 with a Ki of 41 microM, and non-competitive inhibition of isoenzymes 3-3 and 4-4 with Kis of 0.8 and 0.5 microM, respectively.
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